I.Nutrition And Electrolytes
Use
A. Vitamins
CLASSIFICATION: FAT SOLUBLE
VITAMIN
GENERIC NAME: Vitamin E
BRAND NAME: Aquasol E
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Other dosing regimens may be used.
PO (Adults and Children): Determined by
nutritional intake or degree of deficiency.
Topical (Adults and Children): Apply to
affected areas as needed.
DRUG ACTION:
Prevents the oxidation (antioxidant) of other
substances. Protects RBC membranes
against hemolysis, especially in low-birth-
weight neonates
INDICATIONS:
PO: Used as a dietary supplement. Used in
low-birth-weight infants to prevent and treat
hemolysis due to vitamin E deficiency.
Topical: Treatment of irritated, chapped, or
dry skin.
CONTRAINDICATIONS:
Hypersensitivity to ingredients in
preparations (parabens, propylene, glycol).
SIDE EFFECTS:
CNS: fatigue, headache, weakness. EENT:
blurred vision, cramps, diarrhea, and
nausea. Derm: rash. Endo: gonadal
dysfunction.
ADVERSE REACTION:
GI: NECROTIZING ENTEROCOLITIS (oral
administration in low-birth-weight infants)
NURSING RESPONSIBILITIES:
Assessment
● Assess patient for signs of vitamin E
deficiency (neonates—irritability, edema,
hemolytic anemia, creatinuria;
adults/children [rare]—muscle weakness,
ceroid deposits, anemia, creatinuria) prior to
and periodically throughout therapy.
● Assess nutritional status through 24-hr
diet recall. Determine frequency of
consumption of vitamin E–rich foods.
Potential Nursing Diagnoses
Imbalanced nutrition: less than body
requirements
Implementation
● PO: Administer with or after meals.
● Chewable tablets should be chewed well
or crushed before swallowing. Solution may
be dropped directly into the mouth or mixed
with cereal, fruit juice, or other food.
calibrated dropper supplied by manufacturer
to measure solution accurately.
Evaluation/Desired Outcomes
● Prevention of or decrease in the
symptoms of vitamin E deficiency.
● Control of dry or chapped skin.
I.Nutrition And Electrolytes
B. MINERALS
Drug Classification: MINERALS
Generic Name: Iron (Ferrous Sulfate)
Brand Name: Feosal,Feratab,
Slow FE
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Iron Deficiency
Adult: PO Sulfate (30% elemental iron) 750–
1500 mg/day in 1–3 divided doses; Child:
PO Sulfate (30% elemental iron) Younger
than 6 y: 75–225 mg/day in divided doses;
6–12 y: 600 mg/day in divided doses;
Iron Supplement
Adult: PO Sulfate Pregnancy: 300–600
mg/day in divided doses.
DRUG ACTION
An essential mineral found in hemoglobin,
myoglobin, and many enzymes. Enters the
bloodstream and is transported to the
organs of the reticuloendothelial system
(liver, spleen, bone marrow), where it is
separated out and becomes part of iron
stores.
Therapeutic Effects:
Prevention/treatment of iron deficiency.
PHARMACOKINETICS
Absorption:5–10% of dietary iron is
absorbed (up to 30% in deficiency states).
Therapeutically administered PO iron may
be 60% absorbed via an active and passive
transport process. Well absorbed following
IM administration.
Distribution:Remains in the body for many
months. Crosses the placenta; enters breast
milk. Protein Binding: _90%.
Metabolism and Excretion:Mostly
recycled; small daily losses occurring via
desquamation, sweat, urine, and bile.
INTERACTIONS
Drug-drug: Antacids decrease iron
absorption; iron decreases absorption of
tetracyclines, ciprofloxacin, ofloxacin;
chloramphenicol may delay iron’s effects;
iron may decrease absorption of
penicillamine.
Drug-Food: Decreased absorption
withantacids, eggs or milk, coffee and tea;
avoidconcurrent administration of any of
these.
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INDICATION
Prevention and treatment of iron deficiency
anemias: Dietary supplement for iron:
Unlabeled use: Supplemental use during
epoetin therapy to ensure proper
hematologic response to epoetin
CONTRAINDICATION:
Contraindicated in: Hemochrs.omatosis,
hemosiderosis, or other evidence of iron
overload; Anemias
not due to iron deficiency; Some products
contain alcohol tartrazine, or sulfites and
should be avoided in patients with known
intolerance or hypersensitivity.
SIDE EFFECT:
Occasional: Mild, transient nausea.
Rare: Heartburn, anorexia, constipation,
diarrhea.
ADVERSE EFFECT:
CNS:IM, IV—seizures, dizziness, headache,
syncope.CV:IM, IV—hypotension,
hypertension, tachycardia. GI: nausea; PO,
constipation, dark stools, diarrhea,
Epigastric pain, GI bleeding; IM, IV, taste
disorder, vomiting. Derm:IM, IV—flushing,
urticaria. Resp: IV—cough, dyspnea. Local:
pain at IM Site (iron dextran), phlebitis at IV
site, skin staining at IM site (iron dextran).
MS:IM, IV—arthralgia, myalgia.
NURSING INTERVENTIONS
 Confirm that patient does have iron
deficiency anemia before treatment.
 Give drug with meals (avoiding milk,
eggs, coffee, and tea) if GI discomfort is
severe; slowly increase to build up
tolerance.
 Administer liquid preparations in water
or juiceto mask the taste and prevent
staining of teeth;have the patient drink
solution with a straw.
 Warn patient that stool may be dark or
green.
 Arrange for periodic monitoring of Hct
andHgb levels.
NURSING IMPLICATIONS
Assessment:
 Obtain a complete health history
including cardiovascular, GI, hepatic, or
renal disease.
 Obtain a drug history including allergies,
current prescription and OTC drugs, and
herbal preparations.
 Be alert to possible drug interactions.
Obtain a dietary history, including
alcohol use.
 Obtain baseline weight and vital signs.
Assess fatigue level.
 Evaluate appropriate laboratory findings
(e.g., CBC, electrolytes, transferring and
serum ferritin levels, renal and liver
function studies.)
Diagnoses:
 Activity Intolerance
 Imbalanced Nutrition, Less Than Body
Requirements
 Deficient Knowledge (drug therapy)
Risk for Injury, related to underlying
disorder or adverse drug effects
Planning:
The patient will:
 Experience therapeutic effects
dependent on the reason the drug is
being given (e.g., experience increase in
activity level, less fatigue and shortness
of breath on exertion).
 Be free from, or experience minimal,
adverse effects.
 Verbalize an understanding of the drug’s
use, adverse effects, and required
precautions.
 Demonstrate proper self-administration
of the medication (e.g., dose, timing,
when to notify provider).
Implementation:
 Instruct the patient on the need to return
for periodic laboratory work.
 Teach the patient to increase intake of
folic acid, vitamin B12, and iron-rich
 foods such as: folic acid: leafy green
vegetables, citrus fruits, and dried beans
and peas Vitamin B12: fish, meat,
poultry, eggs, milk and milk products,
and fortified breakfast cereals Iron:
meats, fish, poultry, lentils, and beans
 Teach the patient specific administration
guidelines, including: Folic acid: May be
taken on empty stomach or with food.
Instruct the patient to monitor for signs
and symptoms of hypokalemia (e.g.,
muscle weakness or cramping,
palpitations) and to report promptly.
 Teach the patient to increase fluid and
fiber intake as part of a healthy diet
while on iron preparations and to dilute
oral liquid formulations and sip thrs.ough
a straw placed in the back of the mouth.
 Encourage the patient to rest when
fatigued and to space activities
thrs.oughout the day to allow for
adequate rest periods.
 The patient, family, or caregiver should
be able to state the reason for the drug;
appropriate dose and scheduling; what
adverse effects to observe for and when
to report; and the anticipated length of
medication therapy.
 Teach the patient to keep iron
preparations and vitamins containing
Page | 2
 iron in a secure place if young children
are present in the home.
Evaluation:
 Evaluate the effectiveness of drug
therapy by confirming that patient goals
and expected outcomes have been met
(see “Planning”).
I.Nutrition And Electrolytes
C. FLUID AND ELECTROLYTES
Drug Classification: ELECTROLYTES
Generic Name: Potassium
(Potassium Chloride) Brand Name:
Kdur, Slow K, Klor Con, Ktab
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Hypokalemia
Adult: PO 10–100 Meq/Day In Divided
Doses IV 10–40 Meq/ Diluted To At Least
10–20 Meq/ 100 Ml Of Solution (Max: 200–
400 Meq/Day, Monitor Higher Doses
Carefully) Child: PO 1–2 Meq/Kg/Day In
Divided Doses; Sustained Release Tablets
Not Recommended IV 0.5–1 Meq/Kg/Dose
(Max: 40 Meq/Day).
DRUG ACTION:
Maintain acid-base balance, isotonicity, and
electrophysiologic balance of the cell.
Activator in many enzymatic reactions;
essential to transmission of nerve impulses;
contraction of cardiac, skeletal, and smooth
muscle; gastric secretion; renal function;
tissue synthesis; and carbohydrate
metabolism.
Therapeutic Effects:
Replacement.Prevention of deficiency.
Pharmacokinetics: Absorption: Well
absorbed following oral administration.
Distribution: Enters extracellular fluid; then
actively transported into cells. Metabolism
and Excretion: Excreted by the kidneys.
Half-life: Unknown.
DRUG-DRUG INTERACTIONS
Drug-drug: Potassium-sparing Diuretics,
Angiotensin converting Enzyme (Ace)
Inhibitors, Anticholinergic Agents May
Cause Hyperkalemia.
INDICATION:
PO, IV: Treatment/prevention of potassium
depletion.
IV: Arrhythmias due to digoxin toxicity.
CONTRAINDICATION
Contraindicated in: Hyperkalemia; Severe
renal impairment; Untreated Addison’s
disease; Some products may contain
tartrazine (FDC yellow dye #5) or alcohol;
avoid using in patients with known
hypersensitivity or intolerance; Hyperkalemic
familial periodic paralysis. Use Cautiously in:
Cardiac disease; Renal impairment;
Diabetes mellitus (liquids may contain
sugar); Hypomagnesemia (may make
correction of hypokalemia more difficult); GI
hypomotility including dysphagia or
esophageal compression from left atrial
enlargement (tablets, capsules); Patients
receiving potassium-sparing drugs.
ADVERSE REACTIONS/SIDE EFFECTS:
CNS:confusion, restlessness, weakness.
CV:arrhythmias,ECG changes.GI:abdominal
pain, diarrhea, flatulence,nausea, vomiting;
tablets, capsulesonly, GI ulceration, stenotic
lesions. Local:irritation at IV site. Neuro:
paralysis, paresthesia.
NURSING RESPONSIBILITIES:
Assessment
 Assess for signs and symptoms of
hypokalemia (weakness, fatigue, U
wave on ECG, arrhythmias, polyuria,
polydipsia) and hyperkalemia (see
Toxicity and Overdose).
 Monitor pulse, BP, and ECG periodically
during IV therapy.
 Lab Test Considerations: Monitor serum
potassium before and periodically during
therapy. Monitor renal function, serum
bicarbonate, and pH. Determine serum
magnesium level if patient has refractory
hypokalemia; hypomagnesemia should
be corrected to facilitate effectiveness of
potassium replacement. Monitor serum
chloride because hypochloremia may
occur if replacing potassium without
concurrent chloride.
 Toxicity and Overdose: Symptoms of
toxicity are those of hyperkalemia (slow,
irregular heartbeat; fatigue; muscle
weakness; paresthesia; confusion;
dyspnea; peaked T waves; depressed
ST segments; prolonged QT segments;
widened QRS complexes; loss of P
waves; and cardiac arrhythmias).
Diagnoses:
 Imbalanced nutrition: less than body
requirements (Indications)
Implementation:
 High Alert: Medication errors involving
too rapid infusion or bolus IV
administration of potassium chloride
have resulted in fatalities. See IV
administration guidelines below.
 For most purposes, potassium chloride
should be used, except for renal tubular
acidoses (hyperchloremic acidosis), in
which other salts are more appropriate
(potassium bicarbonate, potassium
citrate, or potassium gluconate).
Page | 3
 If hypokalemia is secondary to diuretic
therapy, consideration should be given
to decreasing the dose of diuretic,
unless there is a history of significant
arrhythmias or concurrent digitalis
glycoside therapy.
Evaluation:
 Prevention and correction of serum
potassium depletion.
 Cessation of arrhythmias caused by
digoxin toxicity.
II. AUTONONOMIC NERVOUS
SYSTEM AGENTS
A. ADRENERGIC AGONISTS/
SYMPATHOMIMETICS
Drug Classification: Alpha1
Adrenergic Agonists
Generic Name: Phenylephrine
Brand Name: Alnix, Dimetapp,
Congestap
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Adults
4 mg/day PO; may be increased to a
maximum of 8 mg/day if needed and
tolerated.
Pediatric patients
Safety and efficacy not established.
Patients with renal impairment
No dosage adjustment needed in mild to
moderate renal impairment. Limit dose to 4
mg/day PO in severe renal impairment.
Patients with hepatic impairment not
recommended for patients with severe
hepatic impairment.
DRUG ACTION
Constricts blood vessels by stimulating
alpha-adrenergic receptors.
Therapeutic Effects: Increased BP.
Pharmacokinetics: Absorption:Well
absorbed from IM sites.
Distribution:Unknown.
Metabolism and Excretion:Metabolized by
the liver and other tissues. Half-life:2.5 hrs..
INTERACTIONS
Drug-drug: Ergot alkaloids, guanethidine,
reserpine, tricyclic antidepressants increase
pressor effects of phenylephrs.ine;
halothane, digoxin increase risk of
arrhythmias; mao inhibitors cause
hypertensive crisis; oxytocin causes
persistent hypertension; alpha-blockers,
beta-blockers antagonize effects of
phenylephrs.ine.
INDICATION
Management of hypotension associated with
shock that may persist after adequate fluid
replacement. Management of hypotension
associated with anesthesia.
CONTRAINDICATION
Contraindicated in:Uncorrected fluid
volume deficits; Tachyarrhythmias;
Pheochrs.omocytoma; Angleclosure
Glaucoma; Acute pancreatitis; Hepatitis;
Hypersensitivity to bisulfites.
SIDE EFFECT
Frequent: Nasal: Rebound nasal
congestion due to overuse, esp. when used
longer than 3 days. Occasional: Mild CNS
stimulation (restlessness,nervousness,
tremors, headache, insomnia, particularly in
those hypersensitive to sympathomimetic,
such as elderly pts). Nasal: Stinging,
burning, and drying of nasal mucosa.
ADVERSE EFFECT
CNS: anxiety, dizziness, headache,
insomnia, nervousness, restlessness,
trembling, weakness.Resp:
dyspnea,respiratory distress.CV:
ARRHYTHMIAS, bradycardia, chest pain,
hypertension, tachycardia,
vasoconstriction.Derm: blanching, pallor,
piloerection, sweating.Local: phlebitis,
sloughing at IV sites.
Neuro: tremor.MS: IM, IV—arthrs.algia,
myalgia.
NURSING IMPLICATIONS
Assessment:
 Monitor BP every 2–3 min until
stabilized and every 5 min thereafter
during IV administration.
 Monitor ECG continuously for
arrhythmias during IV administration.
 Assess IV site frequently thrs.oughout
infusion. Antecubital or other large vein
should be used to minimize risk of
extravasation, which may cause tissue
necrosis. If extravasation occurs, the
site should be infiltrated promptly with
10–15 ml of 0.9% NaCl solution
containing 5–10 mg of phentolamine to
prevent necrosis and sloughing.
Diagnoses:
 Decreased cardiac output (Indications)
 Ineffective tissue perfusion (Indications)
Implementation:
 High Alert: Patient harm and fatalities
have occurred from medication errors
with phenylephrs.ine. Prior to
administration, have second practitioner
independently check original order, dose
calculations, concentration, and route of
Page | 4
 administration and infusion pump
settings. IV Administration
 IV: Blood volume depletion should be
corrected, if possible, before initiation of
IV phenylephrs.ine.
 Direct IV: Diluent: Dilute each 1 mg with
9 mL of sterile water for injection. Rate:
Administer each single dose over 1 min
 Continuous Infusion: Diluent: Dilute 10
mg in 250 or 500 mL of
dextrose/Ringer’s or lactated Ringer’s
combination, dextrose/saline
combinations, D5W, D10W, Ringer’s or
LR, 0.45% NaCl, or 0.9% NaCl.
Concentration: 125,000 or 150,000
solution, respectively. Rate: Titrate rate
according to patient's response. Infuse
via infusion pump to ensure accurate
dose rate.
Evaluation:
 Increase in BP to normal range.
 Prolonged duration of spinal anesthesia.
 Localization of regional anesthesia.
Drug Classification: ALPHA2
ADRENERGIC AGONISTS
Generic Name: Clonidine
Brand Name:Catapres
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Hypertension
Adult: PO 0.1 mg b.i.d., may increase by
0.1–0.2 mg/day until desired response is
achieved (max: 2.4 mg/day) Transdermal
0.1 mg patch once q7days, may increase by
0.1 mg q1–2wk Extended Release: 0.1 mg
daily
Geriatric: PO Start with 0.1 mg once daily
Severe Pain
Adult: Epidural Start infusion at 30 mcg/h
and titrate to response. Use rates greater
than 40 mcg/h with caution.
Child: Epidural Start infusion at 0.5 mcg/kg/h
and titrate to response.
ADHD (extended release tablets)
Adolescent/Child (over 6 y): PO 0.1 mg qhs.
DRUG ACTION
Stimulates alpha-adrenergic receptors in the
CNS, which results in decreased
sympathetic outflow inhibiting cardio
acceleration and vasoconstriction
centers.Prevents pain signal transmission to
the CNS by stimulating alpha-adrenergic
receptors in the spinal cord.
Therapeutic Effects: Decreased BP.
Decreased pain. Improvement in ADHD
symptoms.
Pharmacokinetics: Absorption: Well
absorbed from the GI tract and skin. Enters
systemic circulation following epidural use.
Some absorption follows sublingual
administration.
Distribution:Widely distributed; enters
CNS. Crosses the placenta readily; enters
breast milk in high concentrations.
Metabolism and Excretion:Mostly
metabolized by the liver; 40–60% eliminated
unchanged in urine.
INTERACTIONS
Drug-drug: Alcohol and other CNS
depressants add to CNS depression;
tricyclic antidepressants may reduce
antihypertensive effects. Opiate analgesics
increase hypotension with epidural
clonidine. Increased risk of bradycardia or
AV block when epidural clonidine is used
with digoxin, calcium channel blockers, or
beta blockers.
INDICATION
Hypertension, used alone or as part of
combination therapy; Treatment of severe
pain in cancer patients in combination with
opiates; epidural more effective with
neuropathic pain (Duration).
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Epidural— injection site infection,
anticoagulant therapy, orbleeding problems.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: drowsiness, depression, dizziness,
hallucinations,nervousness, nightmares.
EENT: dry eyes.CV:AV block, bradycardia,
hypotension (increase with epidural),
palpitations.
GI: dry mouth, constipation, nausea,
vomiting.GU: erectile dysfunction. Derm:
rash, sweating.Neuro: paresthesia.
NURSING IMPLICATIONS
Assessment:
 Hypertension: Monitor intake and
output ratios and daily weight, and
assess for edema daily, especially at
the beginning of therapy
 Monitor BP and pulse prior to starting,
frequently during initial dose
adjustment and dose increases and
periodically thrs.oughout therapy.
Titrate slowly in patients with cardiac
conditions or those taking other
sympatholytic drugs. Report significant
changes.
 Pain: Assess location, character, and
intensity of pain prior to, frequently
during the first few days, and routinely
thrs.oughout administration.
 Monitor for fever as potential sign of
catheter infection.
Page | 5
  Opioid Withdrawal: Monitor patient for
signs and symptoms of opioid
withdrawal (tachycardia, fever, runny
nose, diarrhea, sweating, nausea,
vomiting, irritability, stomach cramps,
shivering, unusually large pupils,
weakness, difficulty sleeping,
gooseflesh).
Diagnoses:
 Chrs.onic pain (Indications)
 Impaired social interaction (Indications)
 Risk for injury (Side Effects)
Patient/Family Teaching:
 Instruct patient to take clonidine at the
same time each day, even if feeling well.
Take missed dosed as soon as
remembered. If dose of extended-
release product is missed, omit dose
and take next dose as scheduled. Do
not take more than the prescribed daily
dose in any 24 hrs.. If more than 1 oral
dose in a row is missed or if transdermal
system is late in being changed by 3 or
more days, consult health care
professional. All routes of clonidine
should be gradually discontinued over
2–4 days to prevent rebound
hypertension.
 Advise patient to make sure enough
medication is available for weekends,
holidays, and vacations. A written
prescription may be kept in wallet in
case of emergency.
 May cause drowsiness, which usually
diminishes with continued use. Advise
patient to avoid driving or other activities
requiring alertness until response to
medication is known.
Implementation:
 Do not confuse Catapres (clonidine) with
Cataflam (diclofenac).
 Do not confuse clonidine with
clonazepam (Klonopin).
 Do not confuse clonidine with clozapine.
 Do not substitute between clonidine
products on a mg-per-mg basis,
because of differing pharmacokinetic
profiles.
Evaluation:
 Decrease in BP.
 Decrease in severity of pain.
 Decrease in the signs and symptoms of
opioid withdrawal.
 Improved attention span and social
interactions in ADHD.
Drug Classification: BETA1
ADRENERGIC AGONISTS
Generic Name: Dobutamine
Brand Name: Doparine, Dopnax
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IV (Adults and Children): 2.5–15
mcg/kg/min titrate to response (up to 40
mcg/kg/min).
IV (Neonates): 2–15 mcg/kg/min.
Availability Injection: 12.5 mg/mL in 20-,
40-, and 100-mL vials. Premixed infusion:
250 mg/250 mL, 500 mg/500 mL, 500
mg/250 mL, 1000 mg/250 mL.
DRUG ACTION
Stimulates beta1 (myocardial)-adrenergic
receptors with relatively minor effect on
heart rate or peripheral blood vessels.
Therapeutic Effects: Increased cardiac
output without significantly increased heart
rate.
Pharmacokinetics: Absorption:
Administered by IV infusion only, resulting in
complete bioavailability. Distribution:
Unknown. Metabolism and
Excretion:Metabolized by the liver and other
tissues. Half-life: 2 min.
INTERACTIONS
Drug-drug: General Anesthetics (especially
cyclopropanec and halothane) may
sensitizemyocardium to effects of
catecholaminessuch as dobutamine and
lead to serious arrhythmias—use with
extreme caution; betaadrenergicblocking
agents (e.g., metoprolol, propranolol)
maymake dobutamine ineffective
inincreasing cardiac output, but
totalperipheral resistance may increase—
Concomitant use generally avoided; MAO
inhibitors, tricyclic Antidepressants
potentiate pressor effects—use with extreme
caution.
INDICATION
For inotropic support in the short-term
treatment of adults with cardiac
decompensation due to depressed
contractility, resulting from either organic
heart disease or from cardiac surgical
procedures; Investigational use in children
with congenital heart disease undergoing
diagnostic cardiac catheterization, to
augment CV function.
CONTRAINDICATION
Contraindicated in:Hypersensitivity to
dobutamine or bisulfites; Idiopathic
hypertrophic subaortic stenosis.
SIDE EFFECT
Frequent (greater than 5%): Increased
heart rate, B/P.
Occasional (5%–3%): Pain at the injection
site.
Rare (3%–1%): Nausea, headache, anginal
pain, shortness of breath, fever.
Page | 6
ADVERSE EFFECT
CNS: Headache, tremors, paresthesias,
mild leg cramps, nervousness, fatigue (with
overdosage). CV: Increased heart rate and
BP, premature ventricular beats, palpitation,
anginal pain. GI: Nausea, vomiting.Other:
Nonspecific chest pain, shortness of breath.
NURSING IMPLICATIONS
Assessment:
 Monitor BP, heart rate, ECG, pulmonary
capillary wedge pressure (PCWP),
cardiac output, CVP, and urinary output
continuously during the administration.
Report significant changes in vital signs
or arrhythmias. Consult physician for
parameters for pulse, BP, or ECG
changes for adjusting dose or
discontinuing medication.
 Palpate peripheral pulses and assess
appearance of extremities routinely
thrs.oughout dobutamine administration.
Notify physician if quality of pulse
deteriorates or if extremities become
cold or mottled.
 Lab Test Considerations: Monitor
potassium concentrations during
therapy; may cause hypokalemia.
 Monitor electrolytes, BUN, creatinine,
and prothrs.ombin time weekly during
prolonged therapy.
 Toxicity and Overdose: If overdose
occurs, reduction or discontinuation of
therapy is the only treatment necessary
because of the short duration of
dobutamine
Diagnoses:
 Decreased cardiac output (Indications)
 Ineffective tissue perfusion (Indications)
Patient/Family Teaching
 Explain to patient the rationale for
instituting this medication and the need
for frequent monitoring.
 Advise patient to inform nurse
immediately if chest pain; dyspnea; or
numbness, tingling, or burning of
extremities occurs.
 Instruct patient to notify nurse
immediately of pain or discomfort at the
site of administration.
 Home Care Issues: Instruct caregiver on
proper care of IV equipment.
Implementation:
 High Alert: IV vasoactive medications
are potentially dangerous. Have second
practitioner independently check original
order, dosage calculations, and infusion
pump settings. Do not confuse
dobutamine with dopamine. If available
as floor stock, store in separate areas.
 Correct hypovolemia with volume
expanders before initiating dobutamine
therapy.
 Administer into a large vein and assess
administration site frequently.
Extravasation may cause pain and
inflammation.
Evaluation:
 Increase in cardiac output.
 Improved hemodynamic parameter.
 Increased urine output.
Drug Classification: BETA2
ADRENERGIC AGONISTS
Generic Name: Salmeterol
Brand Name:Adeflo
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Asthma
Inhaln (Adults and Children _4 yrs.s.): 50
mcg (1 inhalation) twice daily (approximately
12 hrs. apart).
Prevention of Exercise-Induced
Bronchospasm
Inhaln (Adults and Children _4 yrs.): 50 mcg
(1 inhalation) at least 30 minbefore exercise;
additional doses should not be used for at
least 12 hrs.
COPD
Inhaln (Adults): 50 mcg (1 inhalation) twice
daily (approximately 12 hrs. apart).
DRUG ACTION
Produces accumulation of cyclic adenosine
monophosphate (CAMP) at beta2-
adrenergic receptors. Relatively
specific for beta (pulmonary) receptors.
Therapeutic Effects: Bronchodilation.
Absorption: Minimal systemic absorption
follows inhalation.
Pharmacokinetics: Distribution: Action is
primarily local. Metabolism and Excretion:
Unknown. Half-life: 3–4 hrs.. Onset: 10–20
min. Peak: Effect 2 h. Duration: Up to 12 h.
Distribution: 94–95% protein bound.
Metabolism: Salmeterol is extensively
metabolizedby hydroxylation. Elimination:
Primarily in feces. Half-Life:3–4 h.
INTERACTIONS
Drug-drug: Effects antagonized by beta-
blockers, maois.
Drug-food: Food: High-fat meal: increased
drug bioavailability
INDICATION
Maintenance therapy for asthma and
prevention of bronchospasm in patients 4
yrs. and older with reversible obstructive
airway disease including nocturnal asthma:
Long-term maintenance treatment of
bronchospasm related to COPD: Prevention
Page | 7
of exercise-induced bronchospasm in
patients 4 yrs. and older
CONTRAINDICATION
Contraindicated in:Hypersensitivity;Acute
attack of asthma (onset of action is
delayed); Patients not receiving a long-term
asthma-control medication (e.g.,inhaled
corticosteroid);Patients whose asthma is
currently controlled on low- or medium-dose
inhaled corticosteroid therapy.
INTERACTIONS
Drug-drug: Effects antagonized by beta-
blockers, maois.
Drug-food: Food: High-fat meal: increased
drug bioavailability
ADVERSE REACTIONS/SIDE EFFECTS
CNS: headache, nervousness.CV:
palpitations, tachycardia.GI: abdominal pain,
diarrhea, nausea.MS: muscle
cramps/soreness.Neuro: trembling. Resp:
asthma-related death, paradoxical
bronchospasm, cough.cv: im,
IVhypotension, hypertension, tachycardia.
GI: nausea; PO, constipation, dark stools,
diarrhea, Epigastric pain, GI bleeding; IM,
IV, taste disorder, vomiting.Derm: IM, IV—
flushing, urticaria.Resp: IV—cough,
dyspnea.
NURSING IMPLICATIONS
Assessment:
 Assess lung sounds, pulse, and BP
before administration and periodically
during therapy
 Monitor pulmonary function tests before
initiating therapy and periodically during
therapy
 Observe for paradoxical bronchospasm
(wheezing, dyspnea, tightness in chest)
and hypersensitivity reaction (rash;
urticaria; swelling of the face, lips, or
eyelids). Frequently occurs with first use
of new canister or vial. If condition
occurs, withhold medication and notify
physician or other health care
professional immediately.
 Lab Test Considerations: May cause
increase in serum glucose
concentrations; occurs rarely with
recommended doses and is more
pronounced with frequent use of high
doses.
Diagnoses
 Ineffective airway clearance
(Indications)
Implementation
 Salmeterol should be used along with an
inhaled corticosteroid, not as
monotherapy. Patients taking salmeterol
twice daily should not use additional
doses for exercise-induced
bronchospasm.
 Inhaln: Once removed from foil
overwrap, discard diskus when every
blister has been used or 6 wk have
passed, whichever comes first.
 Do not use a spacer with powder for
inhalation.
Patient/Family Teaching
 Advice patient to take salmeterol as
directed. Do not use more than the
prescribed dose. If a regularly scheduled
dose is missed, use as soon as possible
and resume regular schedule. Do not
double doses. If symptoms occur before
next dose is due, use a rapid-acting
inhaled bronchodilator.
 Instruct patient using powder for
inhalation never to exhale into diskus
device and always to hold device in a
level horizontal position. Mouthpiece
should be kept dry; never wash.
 Caution patient not to use salmeterol to
treat acute symptoms. A rapid-acting
inhaled beta-adrenergic bronchodilator
should be used for relief of acute
asthma attacks.
Evaluation:
 Prevention of bronchospasm or
reduction of frequencyof acute asthma
attacks in patients withchronic asthma.
 Prevention of exercise-induced asthma.
B. ADRENERGIC BLOCKERS OR
SYMPATHOLYTICS
Drug Classification: SELECTIVE
ALPHA-ADRENERGIC BLOCKERS
Generic Name: Tamsulosin
Brand Name: Flomax
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Adults: 0.4 mg PO daily 30 min after the
same meal each day; if response is not
satisfactory in 2–4 wk, dosage may be
increased to 0.8 mg
PO daily 30 min after the same meal each
day. If therapy is interrupted for any reason
for several days, resume dosing at 0.4 mg
PO daily.
Pediatric patients: Safety and efficacy not
established
DRUG ACTION
Decreases contractions in smooth muscle of
the prostatic capsule by preferentially
binding to alpha1-adrenergic receptors.
Therapeutic Effects: Decreased
symptoms of prostatic hyperplasia (urinary
urgency, hesitancy, nocturia).
Pharmacokinetics: Absorption: Minimal
systemic absorption follows inhalation.
Distribution: Action is primarily local.
Page | 8
Metabolism and Excretion: Unknown.
Half-life: 3–4 hrs..
Pharmacokinetics: Absorption: Slowly
absorbed after oral administration.
Distribution: Widely distributed. Protein
Binding: 94–99%.
Metabolism and Excretion: Extensively
metabolized by the liver; _10% excreted
unchanged in urine. Half-life: 14 hrs..
INTERACTIONS
Drug-drug: Other alpha-adrenergic blocking
agents (e.g., doxazosin, prazosin, terazosin)
may increase alpha-blockade effects.
Sildenafil, tadalafil, vardenafil may cause
symptomatic hypotension. CYP3A4
inhibitors (e.g., clarithrs.omycin,
ketoconazole, ritonavir) may increase
concentration.
Drug-food: Grapefruit products may
increase risk for orthostatic hypotension.
INDICATION
Treatment of the signs and symptoms of
BPH.
Unlabeled use: Adjunct in managing
ureteral Stones
CONTRAINDICATION
Contraindicated in:Hypersensitivity to
tamsulosin; women; lactation, children.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: dizziness, headache.EENT: rhinitis.
CV: orthostatic hypotension.GU: priapism,
retrograde/diminished ejaculation.
NURSING IMPLICATIONS
Assessment:
 Assess patient for symptoms of prostatic
hyperplasia (urinary hesitancy, feeling of
incomplete bladder emptying,
interruption of urinary stream,
impairment of size and force of urinary
stream, terminal urinary dribbling,
straining to start flow, dysuria, urgency)
before and periodically during therapy.
 Assess patient for first-dose orthostatic
hypotension and syncope. Incidence
may be dose related. Observe patient
closely during this period and take
precautions to prevent injury.
 Monitor intake and output ratios and
daily weight, and assess for edema
daily, especially at beginning of therapy.
Report weight gain or edema.
 Rectal exams prior to and periodically
throughout therapy to assess prostate
size are recommended.
Diagnoses:
 Risk for injury (Side Effects)
 Impaired urinary elimination (Indications)
Patient/Family Teaching
 Emphasize the importance of continuing
to take thismedication, even if feeling
well. Instruct patient to take medication
at the same time each day. If a dose is
missed, take as soon as remembered
unless almost time for next dose. Do not
double doses.
 May cause dizziness. Advice patient to
avoid driving or other activities requiring
alertness until response to medication is
known.
Caution patient to change positions
slowly to minimize orthostatic
hypotension.
 Instruct patient to notify health care
professional of all Rx or OTC
medications, vitamins, or herbal
products being taken and consult health
care professional before taking any new
medications, especially cough, cold, or
allergy remedies. Emphasize the
importance of follow-up visits to
determine effectiveness of therapy.
Implementation:
 PO: Administer daily dose 30 min after
the same meal each day. Swallow
capsules whole; do not open, crush, or
chew.
 If dose is interrupted for several days at
either the 0.4-mg or 0.8-mg dose, restart
therapy with the 0.4-mg/day dose.
Evaluation:
 Decrease in urinary symptoms of benign
prostatic hyperplasia.
Drug Classification: NON-SELECTIVE
ALPHA- ADRENERGIC BLOCKERS
Generic Name: Trazodone
Brand Name: Desyrs.el
DOSAGE,ROUTE& FREQUENCY
Depression
PO (Adults): Immediate-release—150
mg/day in 3 divided doses; increase by 50
mg/day q 3–4 days until desiredresponse
(not to exceed 400 mg/day in outpatients or
600 mg/day in hospitalized patients).
PO (Geriatric Patients): 75 mg/day in
divided doses initially; may beqq 3–4 days.
Availability (generic available)
Page | 9
Tablets (immediate-release): 50 mg, 100
mg, 150 mg, 300 mg. Cost: Generic—All
strengths $10.83/ 100.
Tablets (extended-release) (Oleptro): 150
mg, 300 mg.
DRUG ACTION
Alters the effects of serotonin in the CNS.
Therapeutic Effects: Antidepressant action,
which may developonly over several weeks.
Pharmacokinetics: Absorption: Readily
from GI tract.Onset: 1–2 wk.Peak: 1–2
h.Distribution: Distributed into breast milk.
Metabolism: In liver (CYP2D6).
Elimination: 75% in urine, 25% in feces.
Half-Life: 5–9 h.
INTERACTIONS
Drug-drug: Antihypertensive agents may
potentiate hypotensive effects; alcohol and
other cns depressants add to depressant
effects; may increase digoxin or phenytoin
levels; mao inhibitors may precipitate
hypertensive crisis; ketoconazole, indinavir,
ritonavir, saquinavir may increase levels and
toxicity. Use of other serotonergic Agents
may increase risk of serotonin syndrome. Do
not use withconivaptan, ivabradine, linezolid,
mifepristone, saquinavir.
INDICATION
Treatment of pulmonary arterial
hypertension in patients with class II–class
IV symptoms, to improve exercise ability and
to decrease the rate of clinical worsening;
To diminish the rate of deterioration in
patients undergoing transition from
epoprostenol (Flolan).
CONTRAINDICATION
Hypersensitivity; Recovery period after MI;
Concurrent electroconvulsive therapy;
Concurrent use of MAO inhibitors or MAO-
like drugs (linezolid or methylene blue).
ADVERSE REACTIONS/SIDE EFFECTS
CNS: suicidal thoughts, drowsiness,
confusion, dizziness, fatigue, hallucinations,
headache, insomnia,nightmares, slurred
speech, syncope, weakness.EENT: blurred
vision, tinnitus. CV: hypotension,
arrhythmias, chest pain, hypertension,
palpitations, qt interval prolongation,
tachycardia.GI: dry mouth, altered taste,
constipation, diarrhea, excess salivation,
flatulence, nausea, vomiting.GU: hematuria,
erectile dysfunction, priapism, urinary
frequency. Derm: rash. HEMAT: anemia,
leukopenia. MS: myalgia.neuro: tremor.
NURSING IMPLICATIONS
Assessment:
 Monitor BP and pulse rate before and
during initial therapy. Monitor ECGs in
patients with pre-existing cardiac
disease before and periodically during
therapy to detect arrhythmias
 Assess for possible sexual dysfunction.
 Assess for serotonin syndrome (mental
changes [agitation, hallucinations,
coma], autonomic instability
[tachycardia, labile BP, hyperthermia],
neuromuscular aberrations [hyper-
reflexia, incoordination], and/or GI
symptoms [nausea, vomiting, diarrhea]),
especially in patients taking
otherserotonergic drugs (SSRIs, SNRIs,
triptans).
 Depression: Assess mental status
(orientation, mood, and behavior)
frequently.
 Assess for suicidal tendencies,
especially during early therapy. Restrict
amount of drug available to patient. Risk
may be increased in children,
adolescents, and adults _24 yrs.. After
starting therapy, children, adolescents,
and young adults should be seen by
health care professional at least weekly
for 4 wk, every 3 wk for next 4 wk, and
on advice of health care professional
thereafter.
 Lab Test Considerations: Assess CBC
and renal and hepatic function before
and periodically during therapy. Slight,
clinically insignificant decrease in
leukocyte and neutrophil counts may
occur.
Diagnoses:
 Ineffective coping (Indications)
 Sexual dysfunction (Side Effects)
Patient/family:
 Instruct patient to take medication as
directed. If a dose is missed, take as
soon as remembered. Do not take if
within 4 hrs.of next scheduled dose; do
not double doses. Oleptro should be
taken at bedtime. Consult health care
professional before discontinuing
medication; gradual dose reduction is
necessary to prevent aggravation of
condition. Advise patient to read
Medication Guide prior starting therapy.
 May cause drowsiness and blurred
vision. Caution patient to avoid driving
and other activities requiring alertness
until response to drug is known.
 Caution patient to change positions
slowly to minimize orthostatic
hypotension.
 Advise patient to avoid concurrent use
of alcohol or other CNS depressant
drugs.
Implementation:
Page | 10
 PO: Administer with or immediately after
meals to minimize side effects (nausea,
dizziness) and allow maximum
absorption of trazodone. A larger portion
of the total daily dose may begiven
atbedtime to decrease daytime
drowsiness and dizziness. Oleptro
should be administered on an empty
stomach at bedtime and swallowed
whole or broken along scored lines; do
not chew or crush
Evaluation:
 Resolution of depression.
 Increased sense of well-being.
 Renewed interest in surroundings.
 Increased appetite.
 Improved energy level.
 Improved sleep.
 Decrease in severity of pain in chronic
pain syndromes. Therapeutic effects are
usually seen within 1 wk, although 4 wk
may be required to obtain significant
therapeutic results.
Drug Classification: SELECTIVE BETA1-
ADRENERGIC BLOCKERS
Generic Name: Atenolol
Brand Name: Tenormin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Hypertension, Angina
Adult: PO 25–50 mg/day, mayincrease to
100 mg/day
Child: PO 0.8–1.5 mg/kg/day
(max: 2 mg/kg/day) MI
Adult: PO Start 50 mg/day
Renal Impairment Dosage
Adjustment
CrCl 15–35 mL/min: Max dose of
50 mg/day; less than 15 mL/min:
Max dose: 25 mg/day.
DRUG ACTION
Blocks stimulation of beta1(myocardial)-
adrenergic receptors. Does not usually
affect beta2(pulmonary, vascular, uterine)-
receptor sites.
Therapeutic Effects: Decreased BP and
heart rate. Decreased frequencyof attacks of
angina pectoris.Prevention of MI.
PHARMACOKINETICS: Absorption: 50–
60% absorbed after oral administration.
Distribution: Minimal penetration of CNS.
Crosses the placenta and enters breast milk.
Metabolism and Excretion: 40–50%
excreted unchanged by the kidneys;
remainder excreted in feces as unabsorbed
drug. Half-life: 6–9 hrs..
INTERACTIONS
Drug-drug: Atropine and other
anticholinergics may increase atenolol
absorption from GI tract; NSAIDS may
decrease hypotensive effects; may mask
symptoms of a hypoglycemic reaction
induced by insulin, sulfonylureas; may
increase Lidocaine levels and toxicity;
pharmacologic and toxic effects of both
atenolol and verapamil are increased.
Prazosin, terazosin may increase severe
hypotensive response to first dose of
atenolol.
INDICATION
Management of hypertension. Management
of angina pectoris. Prevention of MI.
CONTRAINDICATION
Contraindicated in:Sinus bradycardia,
greater than first-degree heart block,
uncompensated heart failure, cardiogenic
shock, abrupt discontinuation, untreated
phenochrormocytoma; pregnancy (category
D); lactation.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: fatigue, weakness, anxiety,
depression, dizziness, drowsiness,
insomnia, memory loss, mental status
changes, nervousness, nightmares.EENT:
blurred vision, stuffy nose. RESP:
bronchospasm,wheezing.CV: bradycardia,
hf, pulmonary edema,hypotension,
peripheral vasoconstriction.GI: constipation,
diarrhea, increase liver enzymes, nausea,
vomiting.
GU: erectile dysfunction, decrease libido,
urinary frequency. DERM:rashes. ENDO:
hyperglycemia, hypoglycemia.MS:
arthralgia, back pain, joint pain.MISC: drug-
induced lupus syndrome.
NURSING IMPLICATIONS
Assessment:
 Monitor BP, ECG, and pulse frequently
during dosage adjustment period and
periodically throughout therapy.
 Monitor intake and output ratios and
daily weights. Assess routinely for HF
(dyspnea, rales/crackles, weight gain,
peripheral edema, jugular venous
distention).
 Monitor frequency of prescription refills
to determine adherence.
 Angina: Assess frequency and
characteristics of angina periodically
throughout therapy.
Diagnoses:
 Decreased cardiac output (Side Effects)
 Noncompliance (Patient/Family
Teaching
Patient/Family:
 Instruct patient to take atenolol as
directed at the same time each day,
even if feeling well; do not skip or double
up on missed doses. Take missed
Page | 11
 doses as soon as possible up to 8
hrs.before next dose. Abrupt withdrawal
may cause life-threatening arrhythmias,
hypertension, or myocardial ischemia.
 Advise patient to make sure enough
medication is available for weekends,
holidays, and vacations. A written
prescription may be kept in wallet in
case of emergency
 Teach patient and family how to check
pulse and BP. Instruct them to check
pulse daily and BP biweekly and to
report significant changes
 May cause drowsiness or dizziness.
Caution patients to avoid driving or other
activities that require alertness until
response to the drug is known.
 Advise patients to change positions
slowly to minimize orthostatic
hypotension.
 Caution patient that atenolol may
increase sensitivity to cold.
 Instruct patient to notify health care
professional of all Rx or OTC
medications, vitamins, or herbal
products being taken, to avoid alcohol,
and to con
Implementation:
 PO: Take apical pulse before
administering drug. If 50 bpm or if
arrhythmia occurs, withhold medication
and notify physician or other health care
professional.
Evaluation:
 Decrease in BP.
 Reduction in frequency of angina.
 Increase in activity tolerance.
 Prevention of MI.
Drug Classification: Non-Selective Beta-
Adrenergic Blockers
Generic Name: Propranolol
Brand Name: Inderal
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Hypertension
Adult: PO Immediate release: 40mg b.i.d.,
usually need 160–48 mg/day in divided
doses; InnoPran XL dose 80 mg each night,
may increase to 120 mg at bedtime. Other
extended releaseforms: 80 mg daily
increase up to 120–160 mg
Angina
Adult: PO Immediate release: 10–20 mg/day
in divided doses(increase up to 160–320
mg/ day) extended release: 80 mg QD
(increase to 160–320 mg/ day)
Arrhythmias
Adult: PO 10–30 mg q6–8h IV 1–3 mg q4h
Post MI
Adult: PO 180–240 mg/day in divided doses
Migraine Prophylaxis
Adult: PO Immediate release: 80 mg/day in
divided doses, mayneed 160–240 mg/day
Extended release: 80 mg/day.
DRUG ACTION
Blocks stimulation of beta1(myocardial) and
beta2 (pulmonary, vascular, and uterine)-
adrenergic receptor sites.
Therapeutic Effects: Decreased heart rate
and BP. Suppression of arrhythmias.
Prevention of MI.
Pharmacokinetics: Absorption:Well
absorbed but undergoes extensive first-pass
hepatic metabolism. Distribution:Moderate
CNS penetration. Crosses the placenta;
enters breast milk.Protein Binding: 93%.
Metabolism and Excretion:Almost
completely metabolized by the liver
INTERACTIONS
Drug-drug: Phenothiazines have additive
hypotensive effects. Beta-adrenergic
agonists (e.g., albuterol) antagonize effects.
Atropine and tricyclic antidepressants block
bradycardia. Diuretics and other hypotensive
agents increase hypotension. High doses of
tubocurarine may potentiate neuromuscular
blockade. Cimetidine decreases clearance,
increases effects. Antacids, ascorbic acid
may decrease absorption. Herbal: black
pepper may increase plasma levels.
INDICATION
Hypertension alone or with other drugs,
especially diuretics; Angina pectoris caused
by coronary atherosclerosis; Idiopathic
hypertrophic subaortic stenosis to manage
associated stress-induced angina,
palpitations, and syncope; Atrial fibrillation;
to control rapid ventricular rate; To reduce
CV mortality in clinically stable patients 5–21
days after MI; Pheochromocytoma, an
adjunctive therapy after treatment with an
alpha-adrenergic blocker to manage
tachycardia before or during surgery or if the
pheochromocytoma is inoperable
CONTRAINDICATION
Contraindicated in:Hypersensitivity to
propranolol; greater than first-degree heart
block; right ventricular failure secondary to
pulmonary hypertension; ventricular
dysfunction; sinus bradycardia, cardiogenic
shock, significant aortic or mitral valvular
disease; bronchial asthma or
bronchospasm, severe COPD, pulmonary
edema; abrupt discontinuation; major
depression; PVD, Raynaud’s disease.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: fatigue, weakness, anxiety, dizziness,
drowsiness, insomnia, memory loss, mental
depression, mental status changes,
nervousness, nightmares. EENT: blurred
Page | 12
vision, dry eyes, and nasal stuffiness.RESP:
bronchospasm, wheezing. CV:
arrhythmias,bradycardia, hf, pulmonary
edema, orthostatic hypotension, peripheral
vasoconstriction.GI: constipation, diarrhea,
nausea.GU: erectile dysfunction, decrease
libido.DERM: erythema multiforme,
exfoliative dermatitis, stevens-johnson
syndrome, toxic epidermal necrolysis,
itching, rash.ENDO: hyperglycemia:
hypoglycemia (increase in children).MS:
arthralgia, back pain, muscle cramps,
myopathy.NEURO: paresthesia.
NURSING IMPLICATIONS
Assessment:
 Monitor BP and pulse frequently during
dose adjustment period and periodically
during therapy.
 Abrupt withdrawal of propranolol may
precipitate life-threatening arrhythmias,
hypertension, or myocardial ischemia.
 Pedi: Assess pediatric patients for signs
and symptoms of hypoglycemia,
particularly when oral foods and fluids
are restricted.
 Patients receiving propranolol IV must
have continuous ECG monitoring and
may have pulmonary capillary wedge
pressure (PCWP) or central venous
pressure (CVP) monitoring during and
for several hours after administration
 Assess for orthostatic hypotension when
assisting patient up from supine position
 Monitor intake and output ratios and
daily weight. Assess patient routinely for
evidence of fluid overload (peripheral
edema, dyspnea, rales/crackles, fatigue,
weight gain, jugular venous distention).
 Assess for rash periodically during
therapy. May cause Stevens-Johnson
syndrome. Discontinue therapy if severe
or if accompanied with fever, general
malaise, fatigue, muscle or joint aches,
blisters, oral lesions, conjunctivitis,
hepatitis and/or eosinophilia.
Diagnoses:
 Decreased cardiac output (Side Effects)
 Noncompliance (Patient/Family
Teaching)
Implementation:
 Administer with meals or directly after
eating to enhance absorption
 Swallow extended release tablets whole;
do not crush, break, or chew.
Propranolol tablets may be crushed and
mixed with food
 Mix propranolol oral solution with liquid
or semisolid food (water, juices,
applesauce, and puddings). To ensure
entire dose is taken, rinse glass with
more liquid or have patient consume all
of the applesauce or pudding. Do not
store after mixing.
Evaluation:
 Decrease in BP.
 Control of arrhythmias without
appearance of detrimental side effects.
 Reduction in frequency of anginal
attacks.
 Increase in activity tolerance.
 Prevention of MI.
 Prevention of vascular headaches.
 Management of thyrotoxicosis.
 Management of pheochromocytoma.
 Decrease in tremors.
 Management of
hypertrophiccardiomyopathy.
 Decrease in symptoms associated with
PTSD.
C. CHOLINERGIC AGONISTS
Drug Classification: DIRECT-ACTING
CHOLINERGIC AGONISTS/SELECTIVE
CHOLINERGIC AGONISTS
Generic Name: Pilocarpine
Brand Name: Salagen, Isopto Carpine
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Acute Glaucoma
Adult/Child: Ophthalmic 1 drop of 1–2%
solution in affected eye q5–10min for 3–6
doses, then 1 drop q1–3h until IOP is
reduced
Chronic Glaucoma
Adult/Child: Ophthalmic 1 drop of 0.5–4%
solution in affected eye q4–12h or 1 ocular
system (Ocusert) q7days
Miotic
Adult/Child: Ophthalmic 1 drop of 1%
solution in affected eye
Xerostomia
Adult: PO 5 mg t.i.d., may increase up to 10
mg t.i.d.
DRUG ACTION
Stimulates cholinergic receptors, resulting in
primarily muscarinic action, including
stimulation of exocrine glands. Other effects
include: Increased sweating, gastric
secretions, increased bronchial secretions,
increased tone and motility of the urinary
tract, gallbladder, and biliary duct smooth
muscle.
Therapeutic Effects: Increased salivary
gland secretion.
Pharmacokinetics: Absorption: Topical
penetrates cornea rapidly;readily
absorbedfrom GI tract. Onset: Miosis 10–30
min; IOP reduction60 min; salivary
stimulation 20 min. Peak: Miosis 30 min;
Page | 13
IOP reduction 75 min; salivary stimulation 60
min. Duration: Miosis 4–8 h; IOP reduction
4–14 h (7 days with Ocusert); salivary
stimulation 3–5 h.Metabolism: Inactivated
at neuronal synapsesand in
plasma.Elimination: Inurine.Half-Life:
0.76–1.35 h.
INTERACTIONS
Drug-drug: The actions of pilocarpine and
carbachol are additive when used
concomitantly. oral form may cause
conduction disturbances with beta-blockers
antagonizes the effects ofconcurrent
anticholinergic drugs (e.g., atropine,
ipratropium).
INDICATION\
Management of xerostomia, which may
occur as a consequence of radiation therapy
for cancer of the head and neck.Treatment
of dry mouth in patients with Sjögren’s
syndrome.
CONTRAINDICATION
Contraindicated in: Secondary glaucoma,
acute iritis, acute inflammatory disease of
anterior segment of eye; uncontrolled
asthma; lactation.Ocular therapeuticsystem:
Not used in acute infectious conjunctivitis,
keratitis, retinal detachment, or when
intense Miosis is required, or with contact
lens use.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: dizziness, headache,
weakness.EENT: amblyopia, epistaxis,
rhinitis.CV: edema, hypertension,
tachycardia. GI: nausea, vomiting,
dyspepsia, dysphagia.
GU: urinary frequency.Derm: flushing,
sweating.Neuro: tremors.Misc: chills, voice
change.
NURSING IMPLICATIONS
Assessment:
 Assess oral mucosa for dryness and
ulceration periodically during therapy.
Diagnoses:
 Impaired oral mucous membrane
(Indications) for maintenance.
Patient/family teaching:
 Instruct patient to take medication as
directed.
 Caution patient that pilocarpine may
cause visual changes, especially at
night; avoid driving or other activities
requiring alertness until effects of
medication are known.
 Advise patient to drink adequate daily
fluids (1500–2000 mL/day), especially if
sweating occurs. Less than adequate
fluid intake may lead to dehydration.
Implementation:
 Do not confuse Salagen (pilocarpine)
with selegiline.
 PO: Use lowest dose that is tolerated
and effective for maintenance.
Evaluation:
 Increased salivary gland secretion in
patients with xerostomia. Decrease in
dry mouth in patients with Sjögren’s
syndrome. Full effects in cancer patients
may not be seen for up to 12 week or 6
week in patients with Sjögren’s
syndrome.
Drug Classification: INDIRECT-
ACTING CHOLINERGIC AGONISTS
Generic Name: Echothiophate Iodide
Brand Name: Phospholine Iodide
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Adults: 1 drop of 0.125% solution 1–2 times
daily
Tinea Cruris, Tinea Corporis, Tinea
Pedis, Cutaneous Candidiasis
Adult/Child: Topical Apply sufficient amount
to affected areas twice daily, morning and
evening.
Tinea Versicolor
Adult: Topical Apply sufficient amount to
affected areas once daily.
DRUG ACTION& THERAPEUTIC EFFECT
Azole antifungal antibiotic with broad
spectrum of activity that disrupts normal
fungal cell membrane permeability.Active
against dermatophytes,yeasts, and many
otherfungi.
Absorption:Minimal percutaneous
absorptionthrs.ough intact skin; increased
absorption from denuded skin.
Peak:0.5–5 h.
Elimination: Less than 1% of applied dose
is eliminated in urine and feces.
INTERACTIONS
Drug-drug: The actions of pilocarpine and
carbachol are additive when used
concomitantly. oral form may cause
conduction disturbances with betablockers.
antagonizes the effects ofconcurrent
anticholinergic drugs (e.g., atropine,
ipratropium).
Drug-food: High-fat meal decreases
absorption of pilocarpine.
INDICATION
Management of xerostomia, which may
occur as a consequence of radiation therapy
for cancer of the head and neck.Treatment
of dry mouth in patients with Sjögren’s
syndrome.
CONTRAINDICATION
Page | 14
Contraindicated in:Infants younger than 3
months
ADVERSE REACTIONS/SIDE EFFECTS
Skin: Burning, stinging sensation, pruritus,
erythema.
NURSING IMPLICATIONS
Assessment:
 Assess oral mucosa for dryness and
ulceration periodicallyduring therapy.
Diagnoses:
 Impaired oral mucous membrane
(Indications) for maintenance.
Patient/family teaching:
 Instruct patient to take medication as
directed.
 Caution patient that pilocarpine may
cause visual changes, especially at
night; avoid driving or other activities
requiring alertness until effects of
medication are known.
 Advise patient to drink adequate daily
fluids (1500–2000 mL/day), especially if
sweating occurs. Less than adequate
fluid intake may lead to dehydration.
Implementation:
 Do not confuse Salagen (pilocarpine)
with selegiline.
 PO: Use lowest dose that is tolerated
and effective for maintenance.
Evaluation:
 Increased salivary gland secretion in
patients with xerostomia.
 Decrease in dry mouth in patients with
Sjögren’s syndrome. Full effects in
cancer patients may not be seen for up
to 12 week or 6 week in patients with
Sjögren’s syndrome.
D. ANTICHOLINERGICS /
CHOLINERGIC- BLOCKING
AGENTS/MUSCARINIC
ANTAGONISTS or
ANTIPARASYMPATHETIC
AGENTS
Drug Classification: ANTICHOLINERGIC
Generic Name: Glycopyrs.rolate
Brand Name: Robinul
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Peptic/Duodenal Ulcer
Adult: PO 1 mg t.i.d or 2 mg b.i.d. or t.i.d. in
equally divided intervals (max: 8 mg/day),
then decrease to 1 mg b.i.d. IM/IV 0.1–0.2
mg 3–4 × day
Reversal of Neuromuscular Blockade
Adult/Child: IV 0.2 mg administered with 1
mg of neostigmine or 5 mg pyridostigmine.
DRUG ACTION
Inhibits the action of acetylcholine at
postganglionic sites located in smooth
muscle, secretory glands, and the CNS
(antimuscarinic activity). Low doses
decrease sweating, salivation, and
respiratory secretions. Intermediate doses
result in increased heart rate. Larger doses
decrease GI and GU tract motility.
Therapeutic Effects: Decreased GI and
respiratory secretions.
Pharmacokinetics: Absorption:
Incompletely absorbed (_10%) after oral
administration. Well absorbed after IM
administration. Distribution: Distribution not
fully known. It does not significantly cross
the blood-brain barrier or eye. Crosses the
placenta. Metabolism and Excretion:
Eliminated primarily unchanged in the urine
and bile. Half-life: 1.7 hrs.(0.6–4.6 hrs.).
INTERACTIONS
Drug-drug: Amantadine, antihistamines,
tricyclic antidepressants, quinidine,
disopyramide, procainamide compound
anticholinergic effects; decreases levodopa
effects; methotrimeprazine may precipitate
extrapyramidal effects; decreases
antipsychotic effects (decreased absorption)
of phenothiazines.
INDICATION
Inhibits salivation and excessive respiratory
secretions when given preoperatively.
Reverses some of the secretory and vagal
actions of cholinesterase inhibitors used to
treat nondepolarizing neuromuscular
blockade (cholinergic adjunct). Adjunctive
management of peptic ulcer disease.Oral
solution: Reduce chronic severe drooling in
children with neurologic conditions
associated with drooling.
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Angle-closure glaucoma; Acute hemorrhage;
Tachycardia secondary to cardiac
insufficiency or thyrotoxicosis; Severe
ulcerative colitis; Toxic megacolon;
Myasthenia gravis; Obstructive uropathy;
Paralytic ileus; Concurrent use of oral
potassium chloride dosage forms (oral
solution only); Pedi: Injection contains
benzyl alcohol and should not be given to
neonates.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: headache, confusion,
drowsiness.EENT: nasal congestion, blurred
vision, cycloplegia, dry eyes, mydriasis.CV:
tachycardia, orthostatic hypotension,
palpitations. GI: dry mouth, vomiting,
Page | 15
constipation. GU:urinary hesitancy, urinary
retention.Derm: flushing.
NURSING IMPLICATIONS
Assessment:
 Assess heart rate, BP, and respiratory
rate before and periodically during
parenteral therapy.
 Monitor intake and output ratios in
geriatric or surgical patients;
glycopyrrolate may cause urinary
retention. Instruct patient to void before
parenteral administration.
 Assess patient routinely for abdominal
distention and auscultate for bowel
sounds. If constipation becomes a
problem, increasing fluids and adding
bulk to the diet may help alleviate the
constipating effects of the drug.
 Periodic intraocular pressure
determinations should be made for
patients receiving long-term therapy.
 Pedi: Monitor amount and frequency of
drooling periodically during therapy.
 Assess for hyperexcitability, a
paradoxical response that may occur in
children.
 Lab Test Considerations: Antagonizes
effects of pentagastrin and histamine
during the gastric acid secretion test.
Avoid administration for 24
hrs.preceding the test.
 May causedecrease in uric acid levels in
patients with gout or hyperuricemia.
 Toxicity and Overdose: If overdose
occurs, neoostigmine is the antidote.
Diagnoses:
 Impaired oral mucous membrane (Side
Effects)
 Constipation (Side Effects)
Implementation:
 Do not administer cloudy or discolored
solution.
 PO: Administer 30–60 min before meals
to maximize absorption.
 For drooling: Administer at least 1
hrs.before or 2 hrs.after meals.
 Do not administer within 1 hrs.of
antacids or antidiarrheal medications.
 Oral dose is 10 times the parenteral
dose.
 IM: May be administered undiluted (200
mcg/mL).
Evaluation:
 Mouth dryness preoperatively.
 Reversal of cholinergic medications.
 Decrease in GI motility and pain in
patients with peptic ulcer disease.
 Reduce chronic severe drooling in
children with
 Neurologic conditions associated with
drooling.
Drug Classification:
ANTIPARKINSON-
ANTICHOLINERGIC
Generic Name: Benztropine
Brand Name: Cogentin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Parkinsonism
Adult: PO/IM 0.5–1 mg/day, may gradually
increase if needed up to 6 mg/day
Extrapyramidal Reactions
Adult: PO/IM/IV 1–4 mg once or twice daily
Child (3 y and older): PO/IM/IV 0.02–0.05
mg/kg/dose once or twice daily
Acute Dystonia
Adult: IV 1–2 mg daily.
DRUG ACTION
Blocks cholinergic activity in the CNS, which
is partially responsible for the symptoms of
Parkinson’s disease. Restores the natural
balance of neurotransmitters in the CNS.
Therapeutic Effects: Reduction of rigidity
and tremors.
Pharmacokinetics: Absorption: Well
absorbed following PO and IM
administration. Distribution: Unknown.
Metabolism and Excretion: Unknown. Half-
life: Unknown.
INTERACTIONS
Drug-drug: Amantadine, tricyclic
antidepressants, MAO inhibitors,
phenothiazines, procainamide, quinidine
have additive anticholinergic effects and
cause confusion, hallucinations, paralytic
ileus.
INDICATION
 Adjunct in the therapy of parkinsonism
(postencephalitic, arteriosclerotic, and
idiopathic types)
 Control of extrapyramidal disorders
(except tardive dyskinesia) due to
neuroleptic drugs (phenothiazines)
CONTRAINDICATION
Contraindicated in:Narrowangle glaucoma;
myasthenia gravis; obstructive diseases of
GU and GI tracts; tendency to tachycardia;
tardive dyskinesia achalasia, myasthenia
gravis; megacolon; children younger than 3
y.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: confusion, depression, dizziness,
hallucinations, headache,
Page | 16
sedation,weakness.EENT:blurred vision, dry
eyes, mydriasis.CV: arrhythmias,
hypotension, palpitations, tachycardia.GI:
constipation, dry mouth, ileus, nausea. GU:
hesitancy, urinary retention. Misc:decreased
sweating.
NURSING IMPLICATIONS
Assessment:
● Assess for desired therapeutic
effects dependent on the reason for
the drug (e.g., decreased tremors,
bradykinesia, and rigidity).
● Continue periodic monitoring of vital
signs, mental status, and motor
function.
● Assess for and promptly report
adverse effects: hypotension,
increasing tremors, dizziness,
salivation, anorexia, dysphagia, or
changes in mental status, including
agitation or confusion.
Diagnoses:
● Impaired Physical Mobility Impaired
Swallowing
● Impaired Verbal Communication
● ConstipationSelf-Care Deficit
(feeding, bathing, hygiene, toileting)
● Deficient Knowledge (drug therapy)
● Risk for Injury; risk for Falls
Planning:
The patient will:
● Experience therapeutic effects
dependent on the reason the drug is
being given (e.g., improved physical
mobility and coordination,
decreased tremors, rigidity,
bradykinesia, and increased ability
in self-care activities).
● Be free from, or experience minimal,
adverse effects.
● Verbalize an understanding of the
drug’s use, adverse effects, and
required precautions.
● Demonstrate proper self-
administration of the
medication(e.g., dose, timing, when
to notify provider).
Implementation:
 Teach the patient, family, or
caregiver that improvement may be
gradual. The patient should report
increasing symptoms that are similar
to those before drug therapy was
initiated.
● Instruct the patient to call for
assistance prior to getting out of bed
or attempting to walk alone.
● Assess the ability of the patient,
family, or caregiver to carry out
ADLs at home and explore the need
for additional health care referrals.
● Evaluate home safety needs.
● Teach the patient to rise from lying
to sitting or standing slowly to avoid
dizziness or falls.
Evaluation:
● Evaluate effectiveness of drug
therapy by confirming that patient
goals and expected outcomes have
been met (see “Planning”).
Drug Classification:
ANTICHOLINERGIC-
ANTIMUSCARINIC
Generic Name: Tolterodine Tartrate
Brand Name: Detrol
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 2 mg twice daily as tablets;
may be lowered depending on response or
2–4 mg once daily as extended-release
capsules.
PO (Adults with impaired hepatic function or
concurrent enzyme inhibitors): 1 mg twice
daily.
DRUG ACTION
Acts as a competitive muscarinic receptor
antagonist resulting in inhibition of
cholinergically mediated bladder contraction.
Therapeutic Effects: Decreased urinary
frequency, urgency, and urge incontinence.
Pharmacokinetics: Absorption:77%
absorbed, decreased withfood.Peak: 1–2 h.
Distribution:96%protein
bound.Metabolism: In liver by CYP2D6
active metabolite. Elimination:77% in urine,
17% in feces.Half-Life: 1.9–3.7 h.
INTERACTIONS
Drug-drug: Additive anticholinergic effects
with amantadine, amoxapine, bupropion,
clozapine, cyclobenzaprine, disopyramide,
maprotiline, olanzapine, orphenadrine,
sedating h1-blockers, phenothiazines,
tricyclic antidepressants. Increased effects
with clarithromycin, cyclosporine,
erythromycin, itraconazole, or ketoconazole.
INDICATION
Treatment of overactive bladder function
that results in urinaryfrequency, urgency, or
urge incontinence.
CONTRAINDICATION
Contraindicated in:Hypersensitivity to
tolterodine or fesoterodine; uncontrolled
narrow-angle glaucoma; gastric retention;
urinary retention; lactation.Tolterodine ER:
Severe hepatic impairment (Child- Pugh
class C).
Page | 17
ADVERSE REACTIONS/SIDE EFFECTS
CNS: headache, dizziness, sedation.EENT:
blurred vision, dry eyes.GI: dry mouth,
constipation, dyspepsia.DERM: Stevens-
Johnson syndrome.MISC: anaphylaxis,
angioedema.
NURSING INTERVENTIONS
 Administer with milk if GI upset
occurs; do not give with food—
bioavailability is decreased by up to
16%.
 Use antacids other than sodium
bicarbonate if GI upset occurs.
 Arrange for periodic ophthalmologic
examination during long-term
therapy.
NURSING IMPLICATIONS
Assessment:
 Assess patient for urinary urgency,
frequency, and urge incontinence
periodically during therapy.
 Monitor for signs and symptoms of
anaphylaxis and
angioedema(difficultybreathing, upper
airway obstruction, fall in BP, rash,
swelling of face or neck). Have
emergency equipment readily available.
 Assess for rash periodically during
therapy. May cause Stevens-Johnson
syndrome or toxic epidermal necrolysis.
Discontinue therapy if severe or if
accompanied with fever, general
malaise, fatigue, muscle or joint aches,
blisters, oral lesions, conjunctivitis,
hepatitis and/oreosinophilia.
Diagnoses:
 Impaired urinary elimination (Indications)
 Urinary retention (Indications)
Planning:
 Instruct patient to take tolterodine as
directed.
 May cause dizziness and blurred vision.
Caution patient to avoid driving or other
activities requiring alertness until
response to medication is known.
 Instruct patient to notify health care
professional immediately if rash or signs
and symptoms of anaphylaxis or
angioedema occur.
Implementation:
 PO: Administer without regard to food.
 Extended-release capsules should be
swallowed whole; do not open, crush,
dissolve, or chew.
Evaluation:
 Decreased urinary frequency, urgency,
and urge incontinence.
Drug Classification: Anticholinergics
For Treating Motion Sickness
Generic Name: Dimenhydrinate
Brand Name: Dramamine
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults and Children _12 yrs.): Motion
sickness—25–50 mg 1 hrs.before exposure;
may repeat in24 hrs.; vertigo—25–100
mg/day in divided doses.
Availability (generic available)
Tablets: 12.5 mg, 25 mgRx, OTC, 50 mg.
DRUG ACTION
H1-receptor antagonist with antiemetic
action thought to involve ability to inhibit
cholinergic stimulation in vestibular and
associated neural pathways. It has been
reported to inhibit labyrinthine stimulation for
up to 3 h. has antiemeticand anti-vertigo
activity.
Therapeutic Effects: Decreased motion
sickness. Decreased vertigofrom vestibular
pathology.
Pharmacokinetics: Absorption: Readily
absorbed from GItract. Onset: 15–30 min
PO; immediateIV; 20–30 min
IM.Duration:3–6 h.Distribution: Distributed
intobreast milk.Elimination: In urine.
INTERACTIONS
Drug-drug: Alcohol and other CNS
depressants enhance CNS depression,
drowsiness; tricyclic Antidepressants
compound anticholinergic effects.
INDICATION
Prevention and treatment of nausea,
vomiting, or vertigo of motion sickness
CONTRAINDICATION
Contraindicated in:Narrow angle
glaucoma, BPH; GI obstruction; urinary tract
obstruction; CNS depression; lactation,
neonates.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: Drowsiness, headache,
incoordination,dizziness, blurred vision,
nervousness,restlessness, insomnia
(especially children). CV: Hypotension,
palpitation.GI: Dry mouth, nose, throat;
anorexia,constipation or
diarrhea.Urogenital: Urinary frequency,
dysuria.
NURSING IMPLICATIONS
Assessment:
 Assess patient for level of sedation after
administration.
 Motion Sickness: Assess patient for
nausea and vomiting before and 60 min
after administration.
Page | 18
 Vertigo: Assess degree of vertigo
periodically in patients receiving
meclizine for labyrinthitis.
 Lab Test Considerations: May cause
false-negative results in skin tests using
allergen extracts. Discontinue meclizine
72 hrs.before testing.
Diagnoses:
 Risk for injury (Side Effects)
Implementation:
 Do not confuse Antivert (meclizine) with
Axert (almotriptan).
 PO: Administer oral doses with food,
water, or milk to minimize GI irritation.
Evaluation:
 Prevention and relief of symptoms in
motion sickness.
 Prevention and treatment of vertigo due
to vestibular pathology.
III. NEUROLOGIC
&NEUROMUSCULAR AGENTS
A. CENTRAL NERVOUS SYSTEM
STIMULANTS
Drug Classification: AMPHETAMINE-
LIKE DRUGS FOR ADHD
Generic Name: Methylphenidate
Hydrochloride
Brand Name: Ritalin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): ADHD—5–20 mg 2–3 times
daily as prompt-release tablets. When
maintenance dose is determined, may
change to extended-release formulation.
Narcolepsy—10 mg 2–3 times/day;
maximum dose 60 mg/day.
PO (Children _6 yrs.): Prompt release
tablets—0.3 mg/kg/dose or 2.5–5 mg before
breakfast and lunch; increase by 0.1
mg/kg/dose or by 5–10 mg/day at weekly
intervals (not to exceed 60 mg/day or 2
mg/kg/day).
DRUG ACTION
Produces CNS and respiratory stimulation
with weak sympathomimetic activity.
Therapeutic Effects: Increased attention
span in ADHD. Increased motor activity,
mental alertness, and diminished fatigue in
narcoleptic patients.
Pharmacokinetics: Absorption: Slow and
incomplete after oral administration;
absorption of sustained or extended-release
tablet (SR) is delayed and provides
continuous release; well absorbed from skin.
Metadate CD, Concerta, Ritalin
LA—provides initial rapid release followed
by a second continuous release (biphasic
release).
Distribution: Unknown.
Metabolism and Excretion: Mostly
metabolized (80%) by the liver.
Half-life: 2–4 hrs..
INTERACTIONS
Drug-drug: Anticonvulsants,
phenylbutazone, selective serotonin
reuptake inhibitors, tricyclic antidepressants,
warfarin: inhibited metabolism and increased
effects of these drugs Guanethidine:
antagonism of hypotensive effect
Halogenated anesthetics: sudden blood
pressure increase MAO inhibitors,
vasopressors: hypertensive crisis
Drug-Food: Excessive use of caffeine-
containingfoods or beverages (coffee, cola,
tea) may cause increase in CNS stimulation.
INDICATION
Treatment of ADHD
(adjunct).Oral:Symptomatic treatment of
narcolepsy.
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Hyperexcitable states; Hyperthyroidism;
Patients with psychotic personalities or
suicidal or homicidal tendencies; Personal or
family history of Tourette’s syndrome;
Glaucoma; Motor tics; Concurrent use or
use within 14 days of MAO inhibitors;
Fructose intolerance, glucose-galactose
malabsorption, or sucrose-isomaltase
insufficiency; Surgery.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: hyperactivity, insomnia, restlessness,
tremor, behavioral disturbances, dizziness,
hallucinations, headache, irritability, mania,
thought disorder.EENT:blurred vision, teeth
grinding.CV: sudden death, hypertension,
palpitations, tachycardia, hypotension,
peripheral vasculopathy.GI: anorexia,
constipation, cramps, diarrhea,
drymouth,metallic taste, nausea,
vomiting.Derm: contact sensitization
(erythema, edema, papules, vesicles)
(transdermal), erythema, rashes.Metab:
growth suppression, weight loss (may occur
with prolonged use).Neuro: akathisia,
dyskinesiatics.Misc: anaphylaxis,
angioedema, fever, physical dependence,
psychological dependence, tolerance.
NURSING IMPLICATIONS
Assessment:
 Monitor BP, pulse, and respiration
before administering and periodically
during therapy. Obtain a history
(including assessment of family history
of sudden death or ventricular
arrhythmia), physical exam to assess for
Page | 19
 cardiac disease, and further evaluation
(ECG and echocardiogram), if indicated.
If exertional chest pain, unexplained
syncope, or other cardiac symptoms
occur, evaluate promptly.
 Monitor closely for behavior change.
 Monitor for signs and symptoms of
peripheral vasculopathy (numbness and
burning in fingers, digital changes). May
require reduction in dose or
discontinuation.
 Pedi: Monitor growth, both height and
weight, in children on long-term therapy.
 May produce a false sense of euphoria
and wellbeing. Provide frequent rest
periods and observe patient for rebound
depression after the effects of the
medication have worn off.
 Methylphenidate has a high abuse
potential; may lead to tolerance and
psychological dependence.
Diagnoses:
 Disturbed thought process (Side Effects)
Implementation:
 Do not confuse Metadate ER/CD
(methylphenidate), or methylphenidate
with methadone. Do not confuse
Metadate CD with Metadate ER. Do not
confuse Ritalin LA with Ritalin SR.
 PO: Administer immediate and
sustained-release tablets on an empty
stomach (30–45 min before a meal).
Sustained-release tablets should be
swallowed whole; do not break, crush,
or chew. Medate CD and Ritalin LA
capsules may be opened and sprinkled
on cool applesauce; entire mixture
should be ingested immediately and
followed by a drink of water. Do not
store for future use. Concerta may be
administered without regard to food, but
must be taken with water, milk, or juice.
Evaluation:
 Improved attention span and social
interactions in ADHD.
 Decreased frequency of narcoleptic
symptoms.
Drug Classification: AMPHETAMINES
FOR ADHD
Generic Name: Amphetamine
Sulfate
Brand Name:Adderall
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Narcolepsy
Adult: PO 5–60 mg/day divided q4–6h in 2–
3 doses
Child: PO Older than 12 y: 10 mg/day, may
increase by 10 mg at weeklyintervals; 6–12
y: 5 mg/day, may increase by 5 mg at
weekly intervals
Attention Deficit Disorder
Adult/Adolescent: PO 10 mg extended
release once daily in a.m.; may increase by
5–10 mg at weekly intervals if needed to
max of 30 mg/day.
Child: PO 6 y: 5 mg 1–2 × day, may
increase by 5 mg at weekly intervals (max:
40 mg/day); 3–5 y: 2.5 mg 1–2 × day, may
increase by 2.5 mg at weekly intervals; 10
mg extended release once daily in a.m.;
may increase by 5–10 mg at weekly
intervals if needed to max of 30 mg/day.
Obesity Dosage Adjustment
Adult: PO 5–10 mg 1 h before meals.
DRUG ACTION
Causes release of norepinephrine from
nerve endings. Pharmacologic effects are:
CNS and respiratory stimulation,
Vasoconstriction, Mydriasis (pupillary
dilation).
Therapeutic Effects: Increased motor
activity, mental alertness, and decreased
fatigue in narcoleptic patients. Increased
attention span in ADHD.
Pharmacokinetics: Absorption: Well
absorbed after oral administration.
Distribution: Widely distributed in body
tissues, with high concentrations in the brain
and CSF. Crosses placenta and enters
breast milk.
Metabolism and Excretion: Some
metabolism by the liver. Urinary excretion is
pH-dependent. Alkaline urine promotes
reabsorption and prolongs action.
Half-life: Children 6–12 yrs.s: 9–11 hrs.;
Adults: 10– 13 hrs. (depends on urine
pH).
INTERACTIONS
Drug-drug: Acetazolamide,sodium
bicarbonate decrease amphetamine
elimination; ammonium chloride, ascorbic
acid increase amphetamine elimination;
effects of both amphetamine and
barbiturates may be antagonized if given
together; furazolidone may increase BP
effects of amphetamines, and interaction
may persist for several weeks after
furazolidone is discontinued; guanethidine
antagonizes antihypertensive effects;
Drug-food: Caffeine: increased stimulant
effect
INDICATION
ADHD. Narcolepsy.
CONTRAINDICATION
Contraindicated in: Hyperexcitable states
including hyperthyroidism; Psychotic
personalities; Suicidal or homicidal
tendencies; Chemical dependence;
Page | 20
Glaucoma; Structural cardiac abnormalities
(may increase the risk of sudden death);
OB: Potentially embryotoxic.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: hyperactivity, insomnia, restlessness,
tremor, aggression, anger, behavioral
disturbances, dizziness, hallucinations,
headache, mania, irritability, skin picking,
talkativeness, thought disorder,
tics.EENT:blurred vision, mydriasis. CV:
sudden death, palpitations, tachycardia,
cardiomyopathy (increased with prolonged
use, high doses), hypertension,hypotension,
peripheral vasculopathy. GI: anorexia,
constipation, cramps, diarrhea, dry mouth,
metallic taste, nausea, vomiting.GU: erectile
dysfunction,increase libido.Derm: alopecia,
urticaria.Endo: growth inhibition (with long
term use in children).Neuro:
paresthesia.Misc: psychological
dependence.
NURSING INTERVENTIONS
Assessment:
 Monitor BP, pulse, and respiration
before and periodically during therapy.
Obtain a history (including assessment
of family history of sudden death or
ventricular arrhythmia), physical exam to
assess for cardiac disease, and further
evaluation (ECG and echocardiogram),
if indicated. If exertional chest pain,
unexplained syncope, or other cardiac
symptoms occur, evaluate promptly.
 May produce a false sense of euphoria
and well-being. Provide frequent rest
periods and observe patient for rebound
depression after the effects of the
medication have worn off.
 Monitor closely for behavior change.
 Has high dependence and abuse
potential.
 Tolerance to medication occurs rapidly;
do not increase dose.
Diagnoses:
 Disturbed thought process (Side Effects)
Implementation:
 Do not confuse Adderall with Inderal or
AdderallXR.
 PO: Use the lowest effective dose.
 May be taken without regard to food.
 Extended-release capsules may be
swallowed wholeor opened and
sprinkled on applesauce;
swallowcontents without chewing.
Applesauce should beswallowed
immediately; do not store. Do not
dividecontents of capsule; entire
contents of capsuleshould be taken.
 ADHD: Pedi: When symptoms are
controlled, dosereduction or interruption
of therapy may be possibleduring
summer months or may be given on
each of the 5 school days, with
medication-freeweekends and holidays.
Evaluation:
 Improved attention span.
 Decrease in narcoleptic symptoms.
Drug Classification: AMPHETAMINE-
LIKE DRUGS FOR NARCOLEPSY
Generic Name: Modafinil
Brand Name:Provigil
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 200 mg/day as a single dose.
Hepatic Impairment
PO (Adults): Severe hepatic impairment—
100 mg/ day as a single dose.
DRUG ACTION
Primary sites of CNS stimulant activity of
modafinil appear to be in the hippocampus,
the centrolateral nucleus of the thalamus,
and the central nucleus of the amygdala.
Modafinil may increase excitatory
transmission in the thalamus and
hippocampus. Modafinil causes
wakefulness,increased locomotor
activity,and psychoactive and euphoric
effects.
Therapeutic Effects: Decreased daytime
drowsiness in patients with narcolepsy and
obstructive sleep apnea. Decreased
drowsiness during work in patients with shift
work sleep disorder.
Pharmacokinetics: Absorption: Rapidly
absorbed; bioavailability unknown.
Distribution: Well distributed; moderately
(60%) bound to plasma proteins.
Metabolism and Excretion: Highly (90%)
metabolized by the liver; _10% eliminated
unchanged.Half-life: 15 hrs.
INTERACTIONS
Drug-drug: Increased plasma levels of
triazolam when used concurrently; triazolam
dosage may need reduction; Possible
decreased effectiveness of hormonal
contraceptives; suggest the use of barrier
contraceptives; Risk of increased levels and
effects of warfarin, phenytoin, and TCAs;
monitor patient and decrease dosage as
appropriate
INDICATION
To improve wakefulness in patients with
excessive daytime drowsiness due to
narcolepsy, obstructive sleep apnea, or shift
work sleep disorder.
CONTRAINDICATION
Hypersensitivity; History of left Ventricular
hypertrophy or ischemic ECG changes,
Chest pain, arrhythmia, or other significant
manifestations of mitral valve prolapse in
association with CNS Stimulant use.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: suicidal ideation, headache,
aggression, amnesia, anxiety, cataplexy,
confusion, delusions, depression, dizziness,
Page | 21
hallucinations, insomnia, mania,
nervousness, seizures. EENT: rhinitis,
abnormal vision, amblyopia, epistaxis,
pharyngitis. Resp: dyspnea, lung disorder.
CV: arrhythmias, chest pain, hypertension,
hypotension, syncope, vasodilation. GI:
increase liver enzymes, nausea, anorexia,
diarrhea, gingivitis, mouth ulcers, thirst,
vomiting. GU: abnormal ejaculation,
albuminuria, urinary retention. Derm:
Stevens-Johnson syndrome, dry skin,
herpes simplex, rash. Endo: hyperglycemia.
Hemat: eosinophilia. MS: joint disorder,
neck pain. Neuro: ataxia, dyskinesia,
hypertonia, paresthesia, tremor. Misc:
infection.
NURSING IMPLICATIONS
Assessment:
 Observe and document frequency of
narcoleptic episodes.
 Monitor closely for changes in behavior
that could indicate the emergence or
worsening of suicidal thoughts or
behavior or depression.
 Assess for rash periodically during
therapy. May cause Stevens-Johnson
syndrome. Discontinue therapy if severe
or if accompanied with fever, general
malaise, fatigue, muscle or joint aches,
blisters, oral lesions, conjunctivitis,
hepatitis and/or eosinophilia.
 Monitor for signs and symptoms of
angioedema or anaphylaxis (rash,
swelling of face, eyes, lips, tongue or
larynx; difficulty in swallowing or
breathing; hoarseness).
 Lab Test Considerations: May cause
elevated liver enzymes.
Diagnoses:
 Disturbed thought process (Side Effects)
 Deficient knowledge, related to
medication regimen (Patient/Family
Teaching)
Implementation:
 PO: Administer as a single dose in the
morning for patients with narcolepsy or
obstructive sleep apnea. Administer 1
hrs.before the start of work shift for
patients with shift work sleep disorder.
Evaluation:
 Decrease in narcoleptic symptoms and
an enhanced ability to stay awake.
Drug Classification: ANOREXIANTS
Generic Name: Phentermine
Hydrochloride
Brand Name: Suprenza
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Obesity
Adult/Adolescent: PO 15–37.5 mg each
morning
DRUG ACTION& THERAPEUTIC EFFECT
Sympathetic amine with actions that include
CNS stimulation and blood pressure
elevation.Appetite suppression or metabolic
effects along with diet adjustment result in
weight loss in obese individuals.
Pharmacokinetics: Absorption:
Phentermine—Unknown; Topiramate— 80%
absorbed following oral administration.
Distribution: Phentermine—Unknown;
Topiramate— Unknown.
Metabolism and Excretion: Phentermine—
metabolized by the liver; Topiramate—70%
excreted unchanged in urine.
Half-life: Phentermine—19–24
hrs.;Topiramate— 21 hrs..
INTERACTIONS
Drug-drug: MAO inhibitors, furazolidone
may increase pressor response resulting in
hypertensive crisis. Tricyclic antidepressants
may decrease anorectic response. May
decrease hypotensive effects of
guanethidine.
INDICATION
Weight management as part of a program
including caloric restriction and increased
exercise in patients with an initial body mass
index (BMI) of _30 kg/m2 or a BMI of _27
kg/m2 with at least one other risk factor
(hypertension, type 2 diabetes mellitus or
dyslipidemia).
CONTRAINDICATION
Contraindicated in:Hypersensitivity
/idiosyncracy to sympathomimetics; OB:
Pregnancy (may cause fetal harm);
Lactation: Breast feeding should be avoided;
Glaucoma; Hyperthyroidism; During/within
14 days of MAO inhibitors; Severe renal
impairment (CCr <30 mL/min); Severe
hepatic impairment; History of suicidal
thought/active suicidal ideation.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: seizures (following abrupt
discontinuation), headache, insomnia,
cognitive impairment, dizziness, mood
disorders, suicidal ideation. EENT: acute
myopia, blurred vision, eye pain, secondary
angle closure glaucoma. CV: tachycardia,
hypotension, palpitations. GI: hepatotoxicity,
altered taste, constipation, dry mouth.
GU:increase in creatinine, kidney stones.
Derm: serious skin reactions including
Erythema multiforme, Stevens-Johnson
syndrome and toxic epidermal necrolysis,
alopecia, oligohydrosis (psweating). Endo:
hypoglycemia. F and E: metabolic acidosis,
hypokalemia. Neuro: paraesthesia. Misc:
hyperthermia.
Page | 22
NURSING IMPLICATIONS
Assessment:
 Monitor patients for weight loss and
adjust concurrent medications
(antihypertensives, antidiabetics, lipid-
lowering agents) as needed. Evaluate
weight loss after each 12 weeks of
therapy.
 Monitor closely for notable changes in
behavior that could indicate the
emergence or worsening of suicidal
thoughts or behavior or depression.
Discontinue phentermine/topiramate if
these occur.
 Monitor BP and heart rate periodically
during therapy; may cause increase in
resting heart rate. May cause
hypotension in patients treated with
antihypertensives.
Diagnoses:
 Disturbed body image (Indications)
Imbalanced nutrition: more than body
requirements (Indications) Deficient
knowledge, related to medication
regimen (Patient/Family Teaching)
Implementation:
 Qsymia is only available through
certified pharmacies that are enrolled in
the Qsymia certified pharmacy network.
PO: Administer once daily in the
morning without regard to food. Avoid
dosing in the evening; may cause
insomnia.
Drug Classification: LIPASE
INHIBITORS
Generic Name: Orlistat
Brand Name: Xenical, Alli
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Adults
120 mg t.i.d PO with each main meal
containing fat. For OTC use, 60 mg PO with
each meal containing fat, not exceeding 3
capsules/day.
Pediatric patients 12 yrs. and older
120 mg PO tid with fat-containing meals;
OTC not for use in children.
Pediatric patients younger than 12 yrs.
Safety and efficacy not established.
DRUG ACTION
Decreases the absorption of dietary fat by
reversibly inhibiting enzymes (lipases),
which are necessary for the breakdown and
subsequent absorption of fat.
Therapeutic Effects: Weight loss and
maintenance inobese patients. Delayed
onset of type 2 diabetes.
Absorption: Minimal systemic absorption.
Distribution: Action is local, within the GI
tract. Protein Binding: Minimally absorbed
drug is _99% bound to plasma proteins.
Metabolism and Excretion: Major route is
fecal elimination of unabsorbed drug.
Half-life: 1–2 hrs.
INTERACTIONS
Drug-Drug: Decrease absorption of some
fat-soluble vitamins, beta-carotene,
levothyroxine (separate orlistat and
levothyroxine by _4 hrs.), and cyclosporine
(give cyclosporine 3 hrs. after orlistat). May
decrease effectiveness of anticonvulsants.
INDICATION
Obesity management (weight loss and
maintenance) when used in conjunction with
a reduced-calorie diet in patients with an
initial BMI _30 kg/m2 or _27 kg/m2 in the
presence of additional risk factors (diabetes,
hypertension, hyperlipidemia). Reduces the
risk of weight regain after prior loss.May
delay onset of type 2 diabetes in prediabetic
patients.
CONTRAINDICATION
Contraindicated in:Hypersensitivity;
Chronic malabsorption syndrome or
cholestasis; OB: Pregnancy (weight loss not
recommended during pregnancy).
ADVERSE REACTIONS/SIDE EFFECTS
Body as a Whole: Fatigue. CNS:
Headache, dizziness,anxiety. CV:
Hypertension, stroke. GI: Oily spotting,
flatus with discharge,fecal urgency, fatty/oily
stool,oily evacuation, increased defecation,
fecal incontinence, abdominal pain/
discomfort, nausea, infectious
diarrhea,rectal pain/discomfort, tooth
disorder,gingival disorder, vomiting. Skin:
Rash. Urogenital: Menstrual irregularity.
NURSING INTERVENTIONS
WARNING: Counsel patient about the use of
barrier contraceptives while using this drug;
pregnancy should be avoided because of
the possible risk to the fetus.
 Be aware that patient may be at
increased risk for severe liver injury;
monitor liver enzymes before and
periodically during therapy.
 Ensure that patient is participating in a
weight-loss diet and exercise program.
 Administer with meals.
 Arrange for administration of fat-soluble
vitamins.
 Do not administer with orlistat; separate
doses.
NURSING IMPLICATIONS
Assessment
 Monitor patients for weight loss and
adjust concurrent medications
(antihypertensives, antidiabetics, lipid-
lowering agents) as needed.
Diagnoses
 Disturbed body image (Indications)
Imbalanced nutrition: more than body
requirements (Indications)
Implementation:
Page | 23
 Do not confuse Xenical (orlistat) with
Xeloda (capecitabine).
 PO: Administer one capsule 3 times
daily with or up to 1 hrs. After a meal. If
a meal is missed or containsno fat, dose
of orlistat can be omitted.A
supplemental multivitamin containing
vitamins A,D, E, K, and beta-carotene
should be taken daily, atleast 2
hrs.before or after orlistat dose.
 Psyllium 6 g with each dose or 12 g at
bedtime may decrease GI side effects.
Evaluation:
 Slow, consistent weight loss when
combined with a reduced-calorie diet
 Delayed onset of type 2 diabetes
Drug Classification: Analeptics
Generic Name: Caffeine Citrate
Brand Name: Cafcit, NoDoz
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Mental Stimulant
Adult: PO 100–200 mg q3–4h prn
Circulatory Stimulant
Adult: IM 200–500 mg prn
Apnea of Prematurity (Caffeine
Citrate Only)
Neonate (28–33 week gestation): PO/IV 20
mg/kg (loading dose); then, after 24 h, 5
mg/kg/day.
DRUG ACTION& THERAPEUTC EFFECT
Stimulates medullary respiratory
center.Appears to increase sensitivity of
respiratory center to stimulatory effects of
CO2.
Absorption: Rapid. Peak: 15–45 min.
Distribution: Widely throughout body;
crosses blood–brain barrier and placenta.
Metabolism: In liver. Elimination: In urine
as metabolites; excreted in breast milk in
small amounts. Half-Life: 3–5 h in adults,
36–144 h in neonates.
INTERACTIONS
Drug-drug: Increased CNS effects of
caffeine with cimetidine, hormonal
contraceptives, disulfiram, ciprofloxacin,
mexiletine; Decreased effects of caffeine
while smoking; Increased serum levels of
theophylline, clozapine with caffeine.
Drug-food: Decreased absorption of iron if
taken with or 1 hrs. after coffee or tea
INDICATION
An aid in staying awake and restoring
mental awareness; Adjunct to analgesic
formulations; IM: Possibly an analeptic in
conjunction with supportive measures to
treat respiratory depression associated with
overdose with CNS depressants; Caffeine
citrate: Short-term treatment of apnea of
prematurity in infants between 28 and 33
week gestation.
Unlabeled uses: Headache, obesity,
alcohol intoxication, postprandial
hypotension
CONTRAINDICATION
Contraindicated in: Acute MI, symptomatic
cardiac arrhythmias, palpitations; peptic
ulcer; pulmonary disease; insomnia, panic
attacks.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: Insomnia, restlessness, excitement,
nervousness, tinnitus, muscular
tremor,headaches, light-headedness. CV:
Tachycardia, hypertension, extrasystoles,
palpitations. GI: Nausea, vomiting, diarrhea,
stomach pain. GU: Diuresis. Other:
Withdrawal syndrome: Headache, anxiety,
muscle tension
NURSING IMPLICATIONS
Assessment:
 Assess respiratory status frequently
throughout therapy.
 Monitor patient for signs of necrotizing
enterocolitis (abdominal distension,
vomiting, bloody stools, and lethargy).
May be fatal.
 Lab Test Considerations: Monitor serum
caffeine levels before and periodically
during therapy in infants previously
treated with theophylline or in infants
whose mothers consumed caffeine
before delivery.
 Monitor serum glucose levels. May
cause hypoglycemia or hyperglycemia.
 Lab Test Considerations: Therapeutic
range: 8– 20 mcg/mL.
 Toxicity and Overdose: Serum caffeine
levels of 50 mcg/mL have been
associated with serious toxicity. Monitor
serum levels and adjust dose in
neonates with impaired hepatic or renal
function to avoid toxicity.
Diagnoses:
 Ineffective breathing pattern
(Indications)
Implementation:
 PO:Maintenance doses may also be
administered orally
Evaluation:
 Decrease in apneic episodes in
premature infant
Drug Classification: RESPIRATORY
STIMULANTS
Generic Name: Doxapram
Hydrochloride
Brand Name: Dopram
Page | 24

DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Postanesthesia
Adult: IV 0.5–1 mg/kg single injection (not
more than 1.5 mg/ kg), may repeat q5min up
to 2 mg/kg total dose; infusion of 0.5–1
mg/kg (max total dose: 4 mg/kg)
Drug-Induced CNS Depression
Adult: IV 1–2 mg/kg repeat in 5 min, then
q1–2h until patient awakens [if relapse
occurs, resume q1–2h injections (max total
dose: 3 g), if no response after priming
dose, may give 1–3 mg/min for up to 2 h
until patient awakens]
Chronic Obstructive Pulmonary
Disease
Adult: IV 0.5–2 mg/kg OR 1–2 mg/min for a
max of 2 h (max rate: 3 mg/min).
DRUG ACTION& THERAPEUTIC EFFECT
Short-acting stimulant capable of stimulating
all levels of the cerebrospinal axis.
Respiratory stimulation by direct medullary
action increases tidal volume and slightly
increases respiratory rate. Decreases Pco2
and increases Po2 by increasing alveolar
ventilation. Effectively used to stimulate
respiration postanesthesia, for drug-induced
CNSdepression, and for chronic pulmonary
disease associated with acute hypercapnia.
Pharmacokinetics: Onset: 20–40 s. Peak:
1–2 min. Duration:
5–12 min. Metabolism: Rapidly
metabolized. Elimination: In urine as
metabolites.
INTERACTIONS
Drug-drug: General anesthetics: increased
risk of self-limiting arrhythmias MAO
inhibitors, sympathomimetics: potentiation of
adverse cardiovascular effects
INDICATION
To stimulate respiration in patients with
druginduced postanesthesia respiratory
depression or apnea; also used to “stir up”
patients in combination with oxygen
postoperatively; To stimulate respiration,
hasten arousal in patients experiencing
drug-induced CNS depression; As a
temporary measure in hospitalized patients
with acute respiratory insufficiency
superimposed on COPD
Unlabeled use: Treatment of apnea of
prematurity when methylxanthines have
failed, obstructive sleep apnea,
laryngospasm secondary to tracheal
extubation
CONTRAINDICATION
Contraindicated in:Epilepsy and other
convulsive disorders; head injury, cerebral
edema; ventilator disorders, pulmonary
fibrosis, flail chest, pneumothorax, airway
obstruction, extreme dyspnea, or acute
bronchial asthma; severe hypertension,
severe coronary artery disease,
uncompensated heart failure, CVA;
lactation.
ADVERSE REACTIONS
CNS: Headache, dizziness, apprehension,
disorientation, pupillary dilation,
increasedreflexes, hyperactivity, seizures,
muscle spasticity, clonus, pyrexia, flushing
sweating
CV: Arrhythmias, chest pain, tightness in the
chest, increased BP. GI: Nausea, vomiting,
diarrhea. GU: Urinary retention,
spontaneous voiding,proteinuria.
Hematologic: Decreased Hgb, Hct.
Respiratory: Cough, dyspnea,
tachypnea,laryngospasm, bronchospasm,
hiccups,rebound hypoventilation,
hyperventilation
NURSING IMPLICATIONS:
Assessment
 History: Epilepsy, incompetence of the
ventilator mechanism, flail chest,
hypersensitivity to doxapram, head
injury, pneumothorax, acute bronchial
asthma, pulmonary fibrosis, severe
hypertension, CVA, lactation, pregnancy
 Physical: T; skin color; weight; R,
adventitious sounds; P, BP, ECG;
reflexes; urinary output; arterial blood
gases, CBC
B. CENTRAL NERVOUS SYSTEM
DEPRESSANTS
1. SEDATIVE HYPNOTICS
Drug Classification: BARBITURATE;
LONG-ACTING BARBITURATES
Generic Name: Phenobarbital
Brand Name:
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Oral
● Sedation: 30–120 mg/day in two to thrs.ee
divided doses. No more than 400 mg per 24
hrs.
● Hypnotic: 100–200 mg at bedtime.
● Antiepileptic: 60–200 mg/day.
Pediatric patients
Oral
● Sedation: 2 mg/kg/dose PO t.i.d. 8–32 mg/
dose.
● Hypnotic: Determine dosage using age
and weight charts.
● Antiepileptic: 3–6 mg/kg/day.
DRUG ACTION
Produces all levels of CNS depression.
Depresses the sensory cortex, decreases
motor activity, and alters cerebellar function.
Page | 25
Inhibits transmission in the nervous system
and raises the seizure threshold. Capable
of inducing (speeding up) enzymes in the
liver that metabolize drugs, bilirubin, and
other compounds.
Therapeutic Effects: Anticonvulsant
activity. Sedation.
Absorption: Absorption is slow but
relatively complete (70–90%). Metabolism
and Excretion: 75% metabolized by the
liver, 25% excreted unchanged by the
kidneys. Half-life: Neonates: 1.8–8.3 days;
Infants: 0.8–5.5 days; Children: 1.5–3 days;
Adults: 2–6 days. Distribution: Crosses
placenta; enters breast milk
INTERACTIONS
Drug-drug: Alcohol, other CNS depressants
(e.g., Lorazepam, morphine) may increase
effects. May decrease effects of warfarin,
oral contraceptives. Valproic acid may
increase concentration, risk of toxicity.
Herbal: Evening primrose may decrease
seizure threshold. Gotu kola, kava kava, St.
John’s wort, valerian may increase CNS
depression.
INDICATION
Oral or parenteral: Sedative; Oral or
parenteral: Hypnotic, treatment of insomnia
for up to 2 weeks; Oral: Long-term treatment
of generalized tonic-clonic and cortical focal
seizures; Oral: Emergency control of certain
acute seizures (e.g., those associated with
status epilepticus, eclampsia, meningitis,
tetanus, and toxic reactions to strychnine or
local anesthetics).
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Comatose patients or those with pre-existing
CNS depression; severerespiratory disease
with dyspnea or obstruction; uncontrolled
severe pain; Known alcohol intolerance
(elixir only); Lactation: Discontinue drug or
bottle feed.
ADVERSE REACTIONS/SIDE EFFECTS
CNS: hangover, delirium, depression,
drowsiness, excitation, lethargy, vertigo.
Resp: respiratory depression; IV,
Laryngospasm, bronchospasm. CV: IV—
hypotension. GI: constipation, diarrhea,
nausea, vomiting. Derm: photosensitivity,
rashes, urticaria. Local: phlebitis at IV site.
MS: arthralgia, myalgia, neuralgia. Misc:
hypersensitivity reactions including
Angioedema and Serum Sickness, physical
dependence, psychological dependence.
NURSING IMPLICATIONS
Assessment:
 Monitor respiratory status, pulse, and
BP and signs and symptoms of
angioedema (swelling of lips, face,
throat, dyspnea) frequently in patients
receiving phenobarbital IV. Equipment
for resuscitation and artificial ventilation
should be readily available.
 Respiratory depression is dose-
dependent.Prolonged therapy may lead
to psychological or physical
dependence. Restrict amount of drug
available to patient, especially if
depressed, suicidal, or with a history of
addiction.
 Geri: Elderly patients may react to
phenobarbital with marked excitement,
depression, and confusion. Monitor for
these adverse reactions.
 Seizures: Assess location, duration, and
characteristics of seizure activity.
 Sedation: Assess level of consciousness
and anxiety when used as a
preoperative sedative.
 Assess postoperative patients for pain
with a pain scale. Phenobarbital may
increase sensitivity to painful stimuli.
Diagnoses:
 Risk for injury (Indications, Side Effects)
 Acute confusion (Side Effects)
Implementation:
 Do not confuse phenobarbital with
pentobarbital.
 Supervise ambulation and transfer of
patients following administration. Two
side rails should be raised and call bell
within reach at all times. Keep bed in
low position. Institute seizure and fall
precautions.
 When changing from phenobarbital to
another anticonvulsant, gradually
decrease phenobarbital dose while
concurrently increasing dose of
replacement medication to maintain
anticonvulsant effects.
 PO: Tablets may be crushed and mixed
with food or fluids (do not administer
dry) for patients with difficulty
swallowing. Oral solution may be taken
undiluted or mixed with water, milk, or
fruit juice. Use calibrated measuring
device for accurate measurement of
liquid doses.
 IM: Injections should be given deep into
the gluteal muscle to minimize tissue
irritation. Do not inject 5 mL into any one
site, because of tissue irritation.
Evaluation:
 Decrease or cessation of seizure activity
without excessive sedation. Several
weeks may be required to achieve
maximum anticonvulsant effects.
 Preoperative sedation.
 Improvement in sleep patterns.
Page | 26
 Decrease in serum bilirubin levels.
Drug Classification: INTERMEDIATE-
ACTING BARBITURATES
Generic Name:Mephobarbital
Brand Name:Butisol
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Daytime Sedation
Adult: PO 15–30 mg t.i.d. or q.i.d.
Preoperative Sedation
Adult: PO 50–100 mg 60–90 min
before surgery
Child: PO 2–6 mg/kg/dose (max:
100 mg)
Insomnia
Adult: PO 100 mg at bedtime
DRUG ACTION& THERAPEUTCI
EFFECT
Intermediate-acting barbiturate that
appears to act at thalamus level of the
brain, where it interferes with
transmission of impulses to the cerebral
cortex. Preoperative sedativeagent that
also is an effectiveantianxiety agent.
Pharmacokinetics: Absorption:
Readily from GI tract. Onset: 40–60min.
Peak: 3–4 h. Duration: 6–8 h.
Distribution: Crosses placenta;
distributed into breast milk. Metabolism:
In liver. Elimination: In urine primarily
as metabolites. Half-Life: Average 100
h.
INTERACTIONS
Drug-drug: Alcohol and other cns
depressants add to cns and respiratory
depression; butabarbital increases the
metabolism of oral anticoagulants,
betablockers, corticosteroids,
doxycycline, griseofulvin, quinidine,
theophyllines, oral
contraceptives,decreasing their
effectiveness.
Herbal: Kava, valerian may
potentiatesedation.
INDICATION
Short-term use as a sedative and
hypnotic
CONTRAINDICATION
Contraindicated in; Porphyria;
uncontrolled pain; severe respiratory
disease; history of addiction; lactation.
ADVERSE REACTIONS
CNS: Drowsiness, residual sedation
(“hangover”), headache. GI: Nausea,
vomiting, constipation, diarrhea.
Skin: Urticaria, skin rash.
Musculoskeletal:
Muscle or joint pain.
SIDE EFFECT
NURSING IMPLICATIONS
Assessment:
 Monitor respiratory status, pulse,
and BP and signs and symptoms of
angioedema (swelling of lips, face,
throat, dyspnea) frequently in
patients receiving phenobarbital IV.
Equipment for resuscitation and
artificial ventilation should be readily
available. Respiratory depression is
dosedependent.
 Prolonged therapy may lead to
psychological or physical
dependence. Restrict amount of
drug available to patient, especially if
depressed, suicidal, or with a history
of addiction.
Diagnoses:
 Risk for injury (Indications) (Side
Effects)
 Acute confusion (Side Effects)
Implementation:
 Do not confuse phenobarbital with
pentobarbital.
 Supervise ambulation and transfer of
patients following administration.
Two side rails should be raised and
call bell within reach at all times.
Keep bed in low position. Institute
seizure and fall precautions.
 When changing from phenobarbital
to another anticonvulsant, gradually
decrease phenobarbital dose while
concurrently increasing dose of
replacement medication to maintain
anticonvulsant effects.
 PO: Tablets may be crushed and
mixed with food or fluids (do not
administer dry) for patients with
difficulty swallowing. Oral solution
may be taken undiluted or mixed
with water, milk, or fruit juice. Use
calibrated measuring device for
accurate measurement of liquid
doses
Page | 27
 IM: Injections should be given deep
into the gluteal muscle to minimize
tissue irritation. Do not inject 5 mL
into any one site, because of tissue
irritation.
Evaluation:
 Decrease or cessation of seizure
activity without excessive sedation.
Several weeks may be required to
achieve maximum anticonvulsant
effects.
 Preoperative sedation.
 Improvement in sleep patterns.
 Decrease in serum bilirubin levels.
Drug Classification: SHORT-ACTING
BARBITURATES
Generic Name:Pentobarbital
Brand Name:Nembutal
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Preoperative Sedation
Adult: IM 150–200 mg in 2 divided
doses
Child: IV 1–3 mg/kg (max: 100 mg)
Hypnotic
Adult: IM 150–200 mg IV 100 mg q1–
3min up to 500 mg dose
Child: IM 2–6 mg/kg (max: 100 mg)
Status Epilepticus
Adult: IV 2–15 mg/kg loading, then 0.5–
3 mg/kg/h
Child: IM 5–15 mg/kg loading, then 0.5–
5 mg/kg/h
DRUG ACTION
Short-acting barbiturate with
anticonvulsant properties.Potent
respiratory depressant. Initially,
barbiturates suppress rem sleep, but
with chronic therapy rem sleep returns
to normal. Effective as a sedative and
hypnotic and anticonvulsant.
Therapeutic actions: General CNS
depressant; barbiturates inhibit impulse
conduction in the ascending RAS,
depress the cerebral cortex, alter
cerebellar function, depress motor
output, and can produce excitation,
sedation, hypnosis, anesthesia, and
deep coma; at anesthetic doses, has
antiseizure activity.
Pharmacokinetics: Onset:10– 15 min
IM; 1 min IV. Duration:15 min IV.
Distribution: Crosses placenta.
Metabolism: Primarily in liver.
Elimination: In urine. Half-Life: 4–50 h.
INTERACTIONS
Drug-drug: Phenmetrazine antagonizes
effects of pentobarbital; CNS
depressants, alcohol, sedatives add to
CNS depression; MAO inhibitors cause
excessive CNS depression;
methoxyflurane creates risk of
nephrotoxicity.
INDICATION
Sedative; Preanesthetic in pediatric
patients; Antiepileptic, in anesthetic
doses, for emergency control of certain
acute seizure episodes (e.g., status
epilepticus, eclampsia, meningitis,
tetanus, toxic reactions to strychnine or
local anesthetics).
CONTRAINDICATIONS
Contraindicated in:History of sensitivity
to barbiturates; parturition, fetal
immaturity, uncontrolled pain; ethanol
intoxication; hepatic encephalopathy;
porphyria; suicidal ideation; pregnancy
(category D), lactation.
ADVERSE REACTIONS
CNS: Somnolence, agitation, confusion,
hyperkinesia, ataxia, vertigo, CNS
depression, nightmares, lethargy,
residual sedation (hangover),
paradoxical excitement, nervousness,
psychiatric disturbance, hallucinations,
insomnia, anxiety, dizziness, thinking
abnormality
CV: Bradycardia, hypotension, syncope.
GI: Nausea, vomiting, constipation,
diarrhea,
epigastric pain. Respiratory:
Hypoventilation, apnea, respiratory
depression, laryngospasm, bronchospasm,
circulatory collapse. Other: Tolerance,
psychological andphysical dependence;
withdrawal syndrome.
NURSING IMPLICATIONS
Assessment:
 Monitor respiratory status, pulse, andBP
frequently in patients receiving
pentobarbital IV. Equipment for
resuscitation and artificial ventilation
should be readily available. Respiratory
depression is dose dependent.
 Prolonged therapy may lead to
psychological or physical dependence.
Page | 28
 Restrict amount of drug available to
patient, especially if depressed, suicidal,
or previously addicted.
 Assess postoperative patients for pain.
Pentobarbital may increase
responsiveness to painful stimuli.
 Therapeutic ranges: Sedation 1– 5
mcg/mL; Sleep: 5– 15 mcg/mL; Coma:
20– 40 mcg/mL.
 Sleep: Assess sleep patterns prior to
and periodically throughout course of
therapy. Hypnotic doses of pentobarbital
suppress REM sleep. Patient may
experience an increase in dreaming
upon discontinuation of medication.
 Cerebral Edema: Monitor intracranial
pressure and level of consciousness in
patients in barbiturate coma.
 Seizures: Assess location, duration, and
characteristics of seizure activity.
Implement seizure precautions.
Diagnoses:
 Insomnia (Indications) Risk for injury
(Side Effects) Deficient knowledge,
related to medication regimen
(Patient/Family Teaching)
Implementation:
 Do not confuse pentobarbital with
phenobarbital.
 Supervise ambulation and transfer of
patients following administration.
Remove cigarettes. Side rails should be
raised and call bell within reach at all
times. Keep bed in low position.
 PO: Elixir may be administered
undiluted or diluted in water, milk, or fruit
juice. Use calibrated measuring device
for accurate dosage. Do not use cloudy
solutions.
Evaluation:
 Improvement in sleep pattern without
excessive daytime sedation. Therapy is
usually limited to a 2-wk period.
Prevention of cerebral anoxia.
 Decrease or cessation of seizures
without excessive sedation.
Drug Classification:
BENZODIAZEPINES OR
MINORTRANQUILIZER OR
ANXIOLYTIC
Generic Name:Alprazolam
Brand Name:Xanax
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Anxiety Disorders
Adult: PO 0.25–0.5 mg t.i.d. (max: 4 mg/day)
Geriatric: PO 0.125–0.25 mg b.i.d.
Panic Attacks
Adult: PO 1–2 mg t.i.d. (max: 8 mg/day);
sustained release: Initiate with 0.5–1 mg
once/day. Depending on the response, the
dose may be increased at intervals of 3 to 4
days in increments of no more than 1
mg/day. Target range 3–6 mg/day (max: 10
mg/ day).
Hepatic Impairment
Dosage Adjustment
Reduce dose by 50% in hepatic impairment.
Do not discontinue abruptly.
DRUG ACTION
It acts at many levels in the CNS to produce
anxiolytic effect. It May produce CNS
depression. Effects may be mediated by
GABA, an inhibitory neurotransmitter.
Therapeutic Effects: Relief of anxiety.
Pharmacokinetics: Absorption: Well
absorbed (90%) from the GI tract;
absorption is slower with extended-release
tablets. Distribution: Widely distributed,
crosses bloodbrain barrier. Probably crosses
the placenta and enters breast milk.
Accumulation is minimal. Metabolism and
Excretion: Metabolized by the liver
(CYP3A4 enzyme system) to an active
compound that is subsequently rapidly
metabolized.
Half-life: 12–15 hrs.
INTERACTIONS
Drug-drug: Increased CNS depression with
alcohol, other CNS depressants,
propoxyphene; Increased effect with
cimetidine, disulfiram, omeprazole,
isoniazid, hormonal contraceptives, valproic
acid.
Drug-food: Decreased metabolism and risk
of toxic effects if combined with grapefruit
juice; avoid this combination
INDICATION
Management of anxiety disorders, short-
termrelief of symptoms of anxiety; anxiety
associatedwith depression; Treatment of
panic attacks with or withoutagoraphobia
(Niravam, Xanax, Xanax XR).
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Cross-sensitivity with other benzodiazepines
may exist; Pre-existing CNS depression;
Severe uncontrolled pain; Angleclosure
glaucoma; Obstructive sleep apnea or
pulmonary disease; Concurrent use with
itraconazole
or ketoconazole; OB, Lactation:
ADVERSE REACTIONS
CNS: dizziness, drowsiness, lethargy,
confusion, hangover, headache, mental
depression, paradoxic excitation. EENT:
blurred vision. GI: constipation, diarrhea,
nausea, vomiting, weight gain. Derm: rash.
Misc: physical dependence, psychological
dependence, tolerance.
Page | 29

NURSING IMPLICATION
Assessment:
 Assess degree and manifestations of
anxiety and mental status (orientation,
mood, behavior) prior to and periodically
during therapy
 Assess patient for drowsiness, light-
headedness, and dizziness. These
symptoms usually disappear as therapy
progresses. Dose should be reduced if
these symptoms persist
 Geri: Assess CNS effects and risk of
falls. Institute falls prevention strategies.
 Prolonged high-dose therapy may lead
to psychological or physical
dependence. Risk is greater in patients
taking <4 mg/day. Restrict the amount of
drug available to patient. Assess
regularly for continued need for
treatment.
Diagnoses:
 Anxiety (Indications)
 Risk for injury (Side Effects)
 Risk for falls (Side Effects)
Implementation:
 Do not confuse Xanax (alprazolam) with
Zantac (ranitidine) or Fanapt
(iloperidone).
 Do not confuse alprazolam with
lorazepam.
 If early morning anxiety or anxiety
between doses occurs, the same total
daily dose should be divided into more
frequent intervals
 PO: May be administered with food if GI
upset occurs. Administer greatest dose
at bedtime to avoid daytime sedation.
 Tablets may be crushed and taken with
food or fluids if patient has difficulty
swallowing. Do not crush, break, or
chew extended-release tablets.
 Taper by 0.5 mg q 3 days to prevent
withdrawal. Some patients may require
longer tapering period (months).
Evaluation:
 Decreased sense of anxiety without
CNS side effects.
 Decreased frequency and severity of
panic attacks.
 Decreased symptoms of premenstrual
syndrome.
Drug Classification:
NONBENZODIAZEPINES
Generic Name: Zaleplon
Brand Name: Sonata
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults <65 yrs.): 10 mg (range 5–20
mg) at bedtime.
PO (Geriatric Patients or Patients <50
kg): Initiate therapy at 5 mg at bedtime (not
to exceed 10 mg at bedtime).
Hepatic Impairment PO (Adults): Initiate
therapy at 5 mg at bedtime (not to exceed
10 mg at bedtime).
DRUG ACTION
Produces CNS depression by binding to
GABA receptors in the CNS and has no
analgesic properties.
Therapeutic Effects: Induction of sleep.
Pharmacokinetics: Absorption: Rapidly
absorbed following oral administration.
Distribution: Enters breast milk.
Metabolism and Excretion: Extensively
metabolized in the liver (mostly by aldehyde
oxidase and some by CYP 450 3A4
enzymes). Half-life: Unknown.
INTERACTIONS
Drug-drug: Cimetidine decrease in
metabolism and increase in effects (initiate
therapy at a lower dose). Additive CNS
depression with other CNS depressants
including alcohol, antihistamines, opioid
analgesics, other sedative/hypnotics,
phenothiazines, and tricyclic
antidepressants. Effects may be decrease
by drugs that induce the CYP 450 3A4
enzyme system including rifampin,
phenytoin, carbamazepine, and
phenobarbital.
Drug-Food: Concurrent ingestion of a high-
fat meal slows the rate of absorption.
INDICATION
Short-term management of insomnia in
patients unable to get at least 4 hrs.of sleep;
especially useful in sleep initiation disorders.
CONTRAINDICATION
Contraindicated in:Hypersensitivity;
Severe hepatic impairment; OB, Lactation:
Pregnancy or lactation.
ADVERSE REACTIONS
CNS: Headache, Amnesia, Anxiety,
Hallucinations, Light-Headedness,
Dizziness, Drowsiness, Depersonalization,
Transient Memory or Psychomotor
Impairment, Incoordination, Malaise,
Vertigo, Asthenia, Hyperesthesia,
Paresthesia, Tremor; CV: Peripheral
Edema; GI: Nausea, Abdominal Pain,
Colitis, Dyspepsia, Anorexia; GU:
Dysmenorrhea; Musculoskeletal: Myalgia;
Page | 30
Skin: Photosensitivity; Other: Altered Sense
of Smell, Fever
NURSING INTERVENTIONS
Assessment:
 Assess mental status, sleep patterns,
and potential for abuse prior to
administering this medication. Zaleplon
is used to treat short-term difficulty in
falling asleep; decreases time to sleep
onset. May not increase total sleep time
or decrease number of awakenings after
falling asleep. Prolonged use of 7–10
days may lead to physical and
psychological dependence. Limit
amount of drug available to the patient.
 Assess alertness at time of peak effect.
Notify health care professional if desired
sedation does not occur.
 Assess patient for pain. Medicate as
needed. Untreated pain decreases
sedative effects
Diagnoses:
 Insomnia (Indications)
 Risk for injury (Side Effects)
Implementation:
 Do not confuse Sonata with Soriatane.
Before administering, reduce external
stimuli and provide comfort measures to
increase effectiveness of medication.
 Protect patient from injury. Supervise
ambulation and transfer of patients after
administration. Remove cigarettes. Side
rails should be raised and call bell within
reach at all times.
 PO: Tablets should be swallowed whole
with full glass of water immediately
before bedtime or after going to bed and
experiencing difficulty falling asleep. Do
not administer with or immediately after
a high-fat or heavy meal.
Evaluation:
 Improved ability to fall asleep;
decreased time to sleep onset.
Drug Classification: MELATONIN
AGONISTS
Generic Name: Ramelteon
Brand Name: Rozerem
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Adults: 8 mg P.O. within 30 minutes of
going to bed
Insomnia
Adult:PO 10 mg at bedtime (max: 20 mg at
bedtime)
Geriatric:PO 5 mg at bedtime (max: 10 mg
at bedtime)
DRUG ACTION
Activates melatonin receptors, which
promotes maintenance of circadian rhythm,
a part of the sleep-wake cycle.
Therapeutic Effects: Easier onset of sleep.
Pharmacokinetics: Absorption: Well
absorbed (84%), but bioavailability is low
(1.8%) due to extensive first pass liver
metabolism. Absorption increased by a high
fat meal. Distribution: Widely distributed to
body tissues. Metabolism and Excretion:
Extensively metabolized by the liver; mainly
by CYP1A2 enzyme system. Metabolites are
excreted mostly in urine (88%); 4% excreted
in feces. Half-life: 1–2.6 hrs.
INTERACTIONS
Drug-drug: Concurrent use with ethanol
produces additive CNS depressant effects;
Ketoconazole,itraconazole, and fluvoxamine
increase ramelteon levels; Other cyp1a2
inhibitors (e.g., ciprofloxacin,enoxacin,
mexiletine,norfloxacin, tacrine) may also
increase ramelteon levels; Rifampin
decreases ramelteon levels.
Drug-Food: High-fat meal, grapefruit or
grapefruit juice increase Ramelteon levels.
INDICATION
Treatment of insomnia characterized by
difficult sleep onset.
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
History of angioedema with previous use;
Severe hepatic impairment; Concurrent use
of fluvoxamine; Lactation: Lactation; Pedi:
Safety not established.
ADVERSE REACTIONS
CNS: Dizziness, somnolence, depression,
insomnia, headache, complex sleep
disorders; GI: Nausea, diarrhea; GU:
Decreased testosterone levels (decreased
libido, fertility issues), increased prolactin
levels (galactorrhea, amenorrhea, problems
with fertility); Respiratory: URIs; Other:
Influenza, arthralgia, myalgia, decreased
cortisol levels, anaphylaxis, angioedema.
NURSING IMPLICATIONS
Assessment:
 Assess sleep patterns before and
periodically throughout therapy.
Diagnoses:
 Insomnia (Indications)
 Risk for injury (Side Effects)
Implementation:
 Do not confuse Rozerem (ramelteon)
with Razadyne (galantamine).
 Do not administer with or immediately
after a high fat meal.
 Before administering, reduce external
stimuli and provide comfort measures to
increase effectiveness of medication.
Page | 31
 PO: Administer 30 min prior to going to
bed.
Evaluation:
 Relief of insomnia.
Drug Classification:
BENZODIAZEPINE Antagonist
Generic Name: Flumazenil
Brand Name: Romazicon
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Adults:Initially, 0.2 mg I.V. injected over 30
seconds; follow with 0.3 mg if desired level
of consciousness isn’t reached. May give
further doses of 0.5 mg at 60-second
intervals until therapeutic response occurs
or cumulative dosage of 3 mg is given. If
partial response is achieved at 3 mg,
patients may rarely need additional doses
up to a total of 5 mg. If sedation recurs,
repeat dose at 20-minute intervals.
Maximum dosage is 3 mg/hour.
Children:Initially 0.01 mg/kg (maximum
dosage 0.2 mg) with repeat doses of 0.01
mg/kg (maximum dosage 0.2 mg) given q
minute to maximum cumulative dosage of 1
mg.
DRUG ACTION
Flumazenil is a benzodiazepine derivative
that antagonizesthe CNS depressant effects
of benzodiazepinecompounds. It has no
effect on CNS depression fromother causes,
including opioids, alcohol, barbiturates,or
general anesthetics.
Therapeutic Effects: Reversal of
benzodiazepine effects.
Pharmacokinetics: Absorption: IV
administration results in complete
bioavailability.
Distribution: Unknown.
Protein Binding: 50% primarily to albumin.
Metabolism and Excretion: Metabolism of
flumazenil occurs primarily in the liver.
Half-life: Children: 20–75 min; Adults: 41–
79 min.
INTERACTIONS
Drug-drug: May antagonize effects of
Zaleplon, Zolpidem; May cause convulsions
or arrhythmias with Tricyclic
Antidepressants.
Drug-food: Ingestion of food during IV
infusion decreases serum levels and
effectiveness.
INDICATION
Complete or partial reversal of the sedative
effects of benzodiazepines when general
anesthesia has been induced or maintained
with them, and when sedation has been
produced for diagnostic and therapeutic
procedures. Management of benzodiazepine
overdose.
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
flumazenil or to benzodiazepines; Patients
given a benzodiazepine for control of a life-
threatening condition; Patients showing
signs of cyclic antidepressant overdose;
Seizure-prone individuals; During labor and
delivery.
ADVERSE REACTIONS
CNS: Dizziness, vertigo, agitation,
nervousness, dry mouth, tremor,
palpitations, emotional lability, confusion,
crying, vision changes, seizures; CV:
Vasodilation, flushing, arrhythmias, chest
pain; GI: Nausea, vomiting, hiccups; Other:
Pain at injection site, increasedsweating
NURSING INTERVENTIONS
Assessment:
 Assess level of consciousness and
respiratory status before and during
therapy. Observe patient for at least 2
hrs. After administration for the
appearance of resedation.
Hypoventilation may occur.
 Overdose: Attempt to determine time of
ingestion and amount and type of
benzodiazepine taken. Knowledge of
agent ingested allows an estimate of
duration of CNS depression.
Diagnoses:
 Risk for injury (Indications)
 Risk for poisoning (Indications)
Implementation:
 Ensure that patient has a patent airway
before administration of flumazenil.
 Observe IV site frequently for redness or
irritation. Administer through a free-
flowing IV infusion into a large vein to
minimize pain at the injection site.
 Optimal emergence should be
undertaken slowly to decrease
undesirable effects including confusion,
agitation, emotional lability, and
perceptual distortion.
 Institute seizure precautions. Seizures
are more likely to occur in patients who
are experiencing sedative/hypnotic
withdrawal, patients who have recently
received repeated doses of
benzodiazepines, or those who have a
previous history of seizure activity.
Seizures may be treated with
benzodiazepines, barbiturates, or
phenytoin. Larger than normal doses of
benzodiazepines may be required.
 Suspected Benzodiazepine Overdose: If
no effects are seen after administration
Page | 32
 of flumazenil, consider other causes of
decreased level of consciousness
(alcohol, barbiturates, and opioid
analgesics).
Evaluation:
 Improved level of consciousness.
 Decrease in respiratory depression
caused by benzodiazepines.
2. ANESTHETICS
Drug Classification: LOCAL
ANESTHETICS SHORT-ACTING (0.5-1
HRS.)
Generic Name: Procaine
Hydrochloride
Brand Name: Novocaine
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Infiltration anesthesia
Adults: 350 to 600 mg of 0.25% to 0.5% of
diluted solution injected as a single dose into
area to be anesthetized
Peripheral nerve block
Adults: 100 ml of 1% diluted solution or 50
ml of 2% solution injected into area where
peripheral nerve block is needed, or up to
200 ml of 0.5% diluted solution
Spinal anesthesia
Adults: 0.5, 1, or 2 ml of 10% solution
injected into spinal area to be anesthetized,
diluted in 0.5, 1, or 2 ml (respectively) of
normal saline solution, sterile distilled water,
or spinal fluid. Administer at 1 ml/5 seconds.
DRUG ACTION
It decreases sodium flux into nerve cell, thus
depressing initial depolarization and
preventing propagation and conduction of
the nerve impulse. Local anesthetic action
produces lossof sensation and motor activity
incircumscribed areas that are treated.
Pharmacokinetics: Absorption: Rapidly
from injection site. Onset: 2–5 min.
Duration: 1 h. Metabolism: Hydrolyzed by
plasma
pseudocholinesterases. Elimination: 80%
of metabolites excreted inurine. Half-Life:
7.7 min.
INTERACTIONS
Drug-drug: May antagonize effects of
sulfonamides; increased risk of hypotension
with MAOIS, antihypertensive.
INDICATION
Infiltration anesthesia; Peripheral nerve
block; and Spinal anesthesia.
CONTRAINDICATION
Contraindicated in: Known hypersensitivity
to procaine or to other drugs of similar
chemical structure, to PABA, and to
parabens; generalized septicemia,
inflammation, or sepsis at proposed injection
site; cerebrospinal diseases (e.g.,
meningitis, syphilis); heart block,
hypotension, hypertension; bowel pathology,
GI hemorrhage; coagulopathy,
anticoagulants, thrombocytopenia.
ADVERSE REACTIONS
CNS: Anxiety, nervousness,
dizziness,circumoral paresthesia, tremors,
drowsiness, sedation,
convulsions,respiratory arrest. With spinal
anesthesia: postspinal
headache,arachnoiditis, palsies, spinal
nerve paralysis, meningism. Special
Senses: Tinnitus, blurred vision. CV:
Myocardial depression, arrhythmiasincluding
bradycardia (alsofetal bradycardia);
hypotension. GI: Nausea, vomiting. Skin:
Cutaneouslesions of delayed onset,
urticaria, pruritus, angioneurotic
edema,sweating, syncope, anaphylactoid
reaction.
NURSING INTERVENTIONS
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine,
and stool; WBC) at beginning of and
during therapy.
 Obtain a history to determine previous
use of and reactions to penicillins,
cephalosporins, or other beta-lactam
antibiotics.
 Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
 Observe patient for signs and symptoms
of anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug
and notify health care professional
immediately if these symptoms occur.
Keep epinephrine, an antihistamine, and
resuscitation equipment close by in case
of an anaphylactic reaction.
Diagnoses:
 Risk for infection (Indications, Side
Effects)
 Noncompliance (Patient/Family
Teaching)
Implementation:
 PO: Administer around the clock.
Penicillin V may be administered without
regard for meals.
 Use calibrated measuring device for
liquid preparations. Solution is stable for
14 days if refrigerated.
 IM: Reconstitute according to
manufacturer’s directions with sterile
water for injection,D5W,or 0.9%NaCl.
Evaluation:
 Resolution of signs and symptoms of
infection. Length of time for complete
Page | 33
 resolution depends on the organism and
site of infection.
Drug Classification: MODERATE-
ACTING (1-3 HRS.)
Generic Name: Lidocaine
Brand Name: Xylocaine
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Ventricular Arrhythmias
Adult: IV 50–100 mg bolus at a rate of 20–
50 mg/min, may repeat in 5 min, then start
infusion of 1–4 mg/min immediately after
first bolus, not more than 300 mg/h; IM 200–
300 mg, may repeat once after 60–90 min
Child: IV 1 mg/kg bolus dose, then 20–50
mcg/kg/min infusion
Anesthetic Uses
Adult: Infiltration 0.5–1% solution; Nerve
Block 1–2% solution; Epidural 1–2%
solution; Caudal 1–1.5% solution; Spinal
5% with glucose; Saddle Block 1.5% with
dextrose; Topical 2.5–5% jelly, ointment,
cream, or solution.
Post-Herpetic Neuralgia
Adult: Topical Apply up to 3 patches over
intact skin in most painful areas once for up
to 12 h per 24 h period.
DRUG ACTION
IV, IM: Suppresses automaticity and
spontaneous depolarizationof the ventricles
during diastole by alteringthe flux of sodium
ions across cell membraneswith little or no
effect on heart rate. Local: Produces local
anesthesia by inhibiting transport of ions
acrossneuronal membranes, thereby
preventing initiation and conduction of
normal nerve impulses.
Therapeutic Effects: Control of ventricular
arrhythmias.Local anesthesia.
Pharmacokinetics: Absorption: Topical
application is 3% absorbedthrough intact
skin.
Onset: 45–90 sec IV; 5–15 min IM; 2–5min
topical. Duration: 10–20 minIV; 60–90 min
IM; 30–60 min topical;greater than 100 min
injectedfor anesthesia. Distribution:
Crossesblood–brain barrier and
placenta;distributed into breast milk.
Metabolism: In liver via CYP3A4 and 2D6.
Elimination: In urine. Half-Life: 1.5–2 h.
INTERACTIONS
Drug-drug: Increased Lidocaine Levels
With Beta Blockers (Propranolol, Metoprolol,
Nadolol, Pindolol, Atenolol), Cimetidine
Prolonged Neuromuscular Blockade With
Succinylcholine.
INDICATION
IV: Ventricular arrhythmias. IM: Self-injected
or when IV unavailable (during transport to
hospital facilities).
Local: Infiltration/mucosal/topical
anesthetic. Patch: Pain due to post-herpetic
neuralgia.
CONTRAINDICATION
Contraindicated in:Hypersensitivity; cross-
sensitivity may occur; Third-degree heart
block.
Use Cautiously in:Liver disease, HF,
patients weighing _50 kg, and geriatric
patients (decrease bolus and/ or
maintenance dose); Respiratory depression;
Shock; Heart block; OB, Lactation: Safety
not established; Pedi: Safety not established
for transdermal patch.
ADVERSE REACTIONS
CNS:Seizures, Confusion, Drowsiness,
Blurred Vision, Dizziness, Nervousness,
Slurred Speech, and Tremor.EENT:
Mucosal use - decrease or absent Gag
Reflex. CV:Cardiac arrest, arrhythmias,
Bradycardia, HeartBlock, Hypotension.
GI:Nausea, Vomiting.
Resp:Bronchospasm. Hemat:
Methemoglobinemia. Local: Stinging,
Burning, Contact Dermatitis,
Erythema.MS:chondrolysis. MISC:Allergic
Reactions, including Anaphylaxis.
NURSING INTERVENTIONS
Assessment:
 Antiarrhythmic: Monitor ECG
continuously and BP and respiratory
status frequently during administration.
 Anesthetic: Assess degree of numbness
of affected part.
 Transdermal: Monitor for pain intensity
in affected area periodically during
therapy.
 Lab Test Considerations: Serum
electrolyte levels should be monitored
periodically during prolonged therapy.
 IM administration may cause increase in
CPK levels.
 Toxicity and Overdose: Serum lidocaine
levels should be monitored periodically
during prolonged or high-dose IV
therapy. Therapeutic serum lidocaine
levels range from 1.5 to 5 mcg/mL.
Signs and symptoms of toxicity include
confusion, excitation, blurred or double
vision, nausea, vomiting, ringing in ears,
tremors, twitching, seizures, difficulty
breathing, severe dizziness or fainting,
and unusually slow heart rate.
 If symptoms of overdose occur, stop
infusion and monitor patient closely.
Diagnoses:
 Decreased cardiac output (Indications)
Page | 34
 Acute pain (Indications)
Implementation:
 High Alert: Lidocaine is readily absorbed
through mucous membranes.
Inadvertent over-dosage of lidocaine
jelly and spray has resulted in patient
harm or death from neurologic and/or
cardiac toxicity. Do not exceed
recommended doses.
 Throat Spray: Ensure that gag reflex is
intact before allowing patient to drink or
eat.
 IM: IM injections are recommended only
when ECG monitoring is not available
and benefits outweigh risks. Administer
IM injections only into deltoid muscle
while frequently aspirating to prevent IV
injection.
Evaluation:
 Decrease in ventricular arrhythmias.
 Local anesthesia.
Drug Classification:
LONG-ACTING (3-10 HRS.S)
Generic Name: Tetracaine
Hydrochloride
Brand Name: Pontocaine
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Local Anesthesia
Adult: Topical Before procedure, 1–2 drops
of 0.5% solution or 1.25–2.5 cm of ointment
in lower conjunctival fornix or 0.5% solution
or ointment to nose or throat
Spinal 1% solution diluted with equal
volume of 10% dextrose injected in
subarachnoid space.
DRUG ACTION
A potent and toxic local anesthetic that
depresses initial depolarization phase of the
action potential, thus preventing propagation
and conduction of the nerve impulse.
Effectiveness indicated by loss ofsensation
and motor activity incircumscribed body
areas close toinjection or application site.
Pharmacokinetics: Onset: 1 min eye; 3
min mucosal surface;3 min spinal.
Duration: Up to 15 mineye; 30–60 min
mucosal surface; 1.5–3 h spinal.
Metabolism: In liverand plasma.
Elimination: In urine.
INTERACTIONS
Drug-Drug: May antagonize effects of
Sulfonamides.
INDICATION
indicated for topical anesthesia in
ophthalmic practice. Representative
ophthalmic procedures in which the
preparation provides good local anesthesia
include measurement of intraocular pressure
(tonometry), removal of foreign bodies and
sutures from
the cornea, conjunctival scraping
in diagnosis and gonioscopic examination; it
is also indicated for use as a
topical anesthetic prior to surgical operations
such as cataract extraction.
CONTRAINDICATION
This preparation is contraindicated in
patients with known hypersensitivity to any
component of the solution.
ADVERSE REACTIONS
Body as a Whole: Anaphylactic reactions,
convulsions,faintness, syncope.
CNS: Post spinal headache, headache,
spinalnerve paralysis, anxiety,
nervousness,and seizures.
CV: Bradycardia,arrhythmias, hypotension.
Special Senses: Stinging; corneal
erosion,retardation or prevention of
healingof corneal abrasion, transient
pittingand sloughing of corneal surface,dry
corneal epithelium; dry mucous membranes,
prolonged depressionof cough reflex.
NURSING IMPLICATIONS
Assessment:
 Assess the degree and duration of
visual disturbance.
 Orient the patient to the new
environment.
 Describe the perioperative routine.
 Suggest to run the day-to-day living
habits when able.
 Encourage participation of family or
people who mean to patient care.
Diagnosis:
 Fear or anxiety related to sensory
impairment and lack of
understanding of post-operative
care, drug delivery.
 Acute pain related to trauma,
increased IOP, surgical intervention
or administration inflammatory eye drops
Planning:
 Acknowledge feelings and identify
healthy ways to deal with them.
 Appear relaxed, able
to rest/sleep appropriately.
 Report decreased fear and anxiety
reduced to a manageable level.
Intervention:
 Give medication to control pain and
IOP as prescribed.
 Give cold compress on demand for
blunt trauma.
 Reduce lighting levels.
 Encourage the use of sunglasses in
strong light.
 Give instructions to the patient or
the person nearest the signs and
Page | 35
 symptoms, complications should be
immediately reported to the doctor.
 Give oral and written instructions for
the patient and the person who
means the right techniques in
delivering drugs.
 Evaluation of the need for
assistance after discharge.
 Teach the patient and family guide
vision techniques.
 Tell the patient about the disease.
 Teach self-care during illness.
 Teach hatching procedure eyedrops
and replacement bandage on the
patient and family.
 Discuss the symptoms of the rise in
IOP and visual impairment.
Evaluation:
 Decreased anxiety
 Patients understand medication
instructions.
 Patients using verbal
communication to express the
symptoms to be reported.
2. Drug Classification: GENERAL
ANESTHETICS
Generic Name: Profonol
Brand Name: Diprivan
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Induction of Anesthesia
Adult: IV 2–2.5 mg/kg q10sec until induction
onset
Adult (55 y or older): IV 1–1.5 mg/kg
q10sec until induction onset
Adolescent/Child (3 y or older): IV 2.5–3.5
mg/kg over 20–30 sec
Maintenance of Anesthesia
Adult: IV 100–200 mcg/kg/min
Adult (55 y or older): IV 50–100 mcg/kg/min
Child/Infant (2 mo. or older): IV 125–150
mcg/kg/min
Conscious Sedation
Adult: IV 5 mcg/kg/min for at least 5 min,
may increase by 5–10 mcg/kg/min q5–
10min until desired level of sedation is
achieved (may need maintenance rate of 5–
80 mcg/kg/min)
DRUG ACTION
Short-acting hypnotic. Mechanism of action
is unknown. Produces amnesia.Has no
analgesic properties.
Therapeutic Effects: Induction and
maintenance of anesthesia.
Pharmacokinetics: Absorption:
Administered IV only, resulting in complete
absorption. Distribution: Rapidly and widely
distributed.
Crosses the blood-brain barrier well; rapidly
redistributed to other tissues. Crosses the
placenta and enters breast milk. Protein
Binding: 95–99%. Metabolism and
Excretion: Rapidly metabolized by the liver.
Half-life: 3–12 hrs.(Blood-brain equilibration
half-life 2.9 min).
INTERACTIONS
Drug-Drug: Additive CNS and respiratory
depression with alcohol, antihistamines,
opioid analgesics, and sedative/hypnotics
(dose decrease may be required).
Theophylline may antagonize the CNS
effects of propofol. Propofol may increase
levels of alfentanil. Cardiorespiratory
instability can occur when used with
acetazolamide. Serious bradycardia can
occur with concurrent use of fentanyl in
children. Increase risk of
hypertriglyceridemia with intravenous
fatemulsion.
INDICATION
Induction of general anesthesia in children
>3 yrs. and adults. Maintenance of
balanced anesthesia when used with other
agents in children >2 mo. and adults.
Initiation and maintenance of monitored
anesthesia care (MAC). Sedation of
intubated, mechanically ventilated patients
in intensive care units (ICUs).
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
propofol or propofol emulsion, which contain
soybean oil and egg phosphatide; patients
with increased intracranial pressure or
impaired cerebral circulation; obstetrical
procedures; lactation.
ADVERSE REACTIONS
CNS: dizziness, headache. Resp: APNEA,
cough. CV: bradycardia, hypotension,
hypertension. GI: abdominalcramping,
hiccups, nausea, vomiting. Derm: flushing.
Local: burning, pain, stinging, coldness,
numbness,tingling at IV site. MS: involuntary
muscle movements, perioperative
myoclonia.
NURSING INTERVENTIONS
Assessment:
 Assess respiratory status, pulse, and BP
continuously throughout propofol
therapy. Frequently causes apnea
lasting >= 60 sec. Maintain patent
airway and adequate ventilation.
Propofol should be used only by
individuals experienced in endotracheal
intubation, and equipment for this
procedure should be readily available.
Page | 36
 Assess level of sedation and level of
consciousness throughout and following
administration.
 When using for ICU sedation, wake-up
and assessment of CNS function should
be done daily during maintenance to
determine minimum dose required for
sedation. Maintain a light level of
sedation during these assessments; do
not discontinue. Abrupt discontinuation
may cause rapid awakening with
anxiety, agitation, and resistance to
mechanical ventilation.
 Monitor for propofol infusion syndrome
(severe metabolic acidosis,
hyperkalemia, lipemia, rhabdomyolysis,
and hepatomegaly, cardiac and renal
failure). Most frequent with prolonged,
high-dose infusions (>5 mg/kg/hrs. for
>48 hrs.) but has also been reported
following large-dose, short-term
infusions during surgical anesthesia. If
prolonged sedation or increasing dose is
required, or metabolic acidosis occurs,
consider alternative means of sedation.
Diagnoses:
 Ineffective breathing pattern (Adverse
Reactions)
 Risk for injury (Side Effects)
Implementation:
 Do not confuse Diprivan (propofol) with
Diflucan (fluconazole) or Ditropan
(oxybutynin).
 Dose is titrated to patient response.
 Propofol has no effect on the pain
threshold. Adequate analgesia should
always be used when propofol is used
as an adjunct to surgical procedures.
Evaluation:
 Induction and maintenance of
anesthesia.
 Amnesia.
 Sedation in mechanically ventilated
patients in an intensive care setting.
C. ANTICONVULSANTS
Drug Classification: HYDANTOINS
GENERIC NAME: PHENYTOIN
Brand Name: Dilantin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Anticonvulsant
Adult: PO 15–20 mg/kg loading dose, then
300 mg/day in 1–3 divided doses, may be
gradually increased by 100 mg/week until
seizures are controlled IV 10–15 mg/kg then
300 mg/day in divided doses
Child: PO/IV 15–20 mg/kg loading dose,
then 5 mg/kg in 2 divided doses; titrate to
response (usually 4–8 mg/kg/day)
DRUG ACTION
Limits seizure propagation by altering ion
transport.May also decrease synaptic
transmission.Antiarrhythmic properties as a
result of shortening the action potential and
decreasing automaticity.
Therapeutic Effects: Diminished seizure
activity. Termination ofventricular
arrhythmias.
Pharmacokinetics: Absorption: Absorbed
slowly from the GI tract. Bioavailability
differs among products; the Dilantin and
Phenytek preparations are considered to be
“extended” products. Other products are
considered to be prompt release.
Distribution: Distributes into CSF and other
body tissues and fluids. Enters breast milk;
crosses the placenta, achieving similar
maternal/fetal levels. Preferentially
distributes into fatty tissue. Protein
Binding: Adults 90–95%; decrease in
protein binding in neonates (up to 20% free
fraction available), infants (up to 15% free),
and patients with hyperbilirubinemia,
hypoalbuminemia, severe renal dysfunction
or uremia. Metabolism and Excretion:
Mostly metabolized by the liver; minimal
amounts excreted in the urine.
Half-life: 22 hrs. (Range 7–42 hrs.s.).
INTERACTIONS
Drug-drug: Alcohol decreases phenytoin
effects; otheranticonvulsants may increase
or decrease phenytoin levels; phenytoin may
decrease absorption and increase
metabolism of oral anticoagulants; phenytoin
increases metabolism of corticosteroids,
oralcontraceptives, and nisoldipine,
decreasing their effectiveness; amiodarone,
chloramphenicol, omeprazole, and
ticlopidine increasephenytoin levels;
antituberculosisagents decrease phenytoin
levels. Closely.
INDICATION
Treatment/prevention of tonic-clonic (grand
mal) seizures and complex partial seizures.
Unlabeled Use: As an antiarrhythmic,
particularly for ventricular arrhythmias
associated with digoxin toxicity, prolonged
QT interval, and surgical repair of congenital
heart diseases in children. Management of
neuropathic pain, including trigeminal
neuralgia.
CONTRAINDICATION
Contraindicated in:
Hypersensitivity;Hypersensitivity to
Page | 37
propylene glycol (phenytoin injection only);
Alcohol intolerance (phenytoin injection and
liquid only); Sinus bradycardia, sinoatrial
block, 2nd- or 3rd-degree heart block, or
Stokes-Adams syndrome (phenytoin
injection only); Concurrent use of
delavirdine.
ADVERSE REACTIONS
CNS: Suicidal Thoughts, Ataxia, Agitation,
Confusion, Dizziness, Drowsiness,
Dysarthrs.ia, Dyskinesia, Extrapyrs.amidal
Syndrome, Headache, Insomnia, Weakness.
Eent: Diplopia, Nystagmus. CV:
Hypotension (Increase With IV Phenytoin),
Tachycardia. Gi: Gingival Hyperplasia,
Nausea, Constipation, Drug-Induced
Hepatitis, Vomiting.Derm: Stevens-Johnson
Syndrome, Toxic Epidermal Necrolysis,
Hypertrichosis, Rash, Exfoliative Dermatitis,
Pruritus, Purple Glove Syndrome.
Hemat: Agranulocytosis, Aplastic Anemia,
Leukopenia, Megaloblastic Anemia,
Thrs.ombocytopenia. MS: Osteomalacia,
Osteoporosis. Misc: Fever,
Lymphadenopathy.
SIDE EFFECTS:
Most listed are for chronic use of phenytoin
CNS: ataxia, agitation, confusion, dizziness,
drowsiness, dysarthria, dyskinesia,
extrapyramidal syndrome, headache,
insomnia, weakness. EENT: diplopia,
nystagmus. CV: hypotension (increased with
IV phenytoin), tachycardia. GI: gingival
hyperplasia, nausea, constipation, drug-
induced hepatitis, vomiting.Derm:
hypertrichosis, rash, exfoliative dermatitis,
pruritus, purple glove syndrome. Hemat:
leukopenia, megaloblastic anemia,
thrombocytopenia. MS: osteomalacia,
osteoporosis. Misc: fever, lymphadenopathy.
NURSING INTERVENTIONS
Assessment:
 Monitor closely for notable changes in
behavior that could indicate the
emergence or worsening of suicidal
thoughts or behavior or depression.
 Assess oral hygiene. Vigorous cleaning
beginning within 10 days of initiation of
phenytoin therapy may help control
gingival hyperplasia.
 Assess patient for phenytoin
hypersensitivity syndrome (fever, skin
rash, lymphadenopathy). Rash usually
occurs within the first 2 wk of therapy.
Hypersensitivity syndrome usually
occurs at 3– 8 wk but may occur up to
12 wk after initiation of therapy. May
lead to renal failure, rhabdomyolysis, or
hepatic necrosis; may be fatal.
Diagnoses:
 Risk for injury (Indications) Impaired
 oral mucous membrane (Side Effects)
Implementation:
 Implement seizure precautions.
 When transferring from phenytoin to
another anticonvulsant, dosage
adjustments are made gradually over
several weeks.
 When substituting fosphenytoin for oral
phenytoin therapy, the same total daily
dose may be given as a single dose.
Unlike parenteral phenytoin,
fosphenytoin may be given safely by the
IM route
Evaluation:
 Decrease or cessation of seizures
without excessive sedation
 Suppression of arrhythmias
 Relief of neuropathic pain
Drug Classification: BARBITURATES
GENERIC Name: Pentobarbital
Brand Name: Luminal
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Anticonvulsant
Adult: PO/IV 1–3 mg/kg/day in divided
doses Child: PO/IV 4–8 mg/kg/day in
divided doses
Status Epilepticus
Adult: IV 300–800 mg, then 120–240 mg
q20min (total max: 1–2 g). Child: IV 10–20
mg/kg in single or divided doses, then 5
mg/kg/ dose q15–30min (total max: 40
mg/kg)
Neonate: IV 15–20 mg/kg in single or
divided doses
Sedative/Hypnotic
Adult: PO 30–120 mg/day IV/IM 100–320
mg/day. Child: PO 2 mg/kg/day in 3 divided
doses IV/IM 3–5 mg/kg
Renal Impairment Dosage
Adjustment
CrCl less than 10 mL/min: Dose q12–16h
Hemodialysis Dosage Adjustment
20–50% dialyzed
DRUG ACTION
Produces all levels of CNS depression.
Depresses the sensory cortex, decreases
motor activity, and alters cerebellar function.
Inhibits transmission in the nervous system
and raises the seizure threshold. Capable of
inducing (speeding up) enzymes in the liver
that metabolize drugs, bilirubin, and other
compounds.
Therapeutic Effects: Anticonvulsant
activity. Sedation.
Pharmacokinetics: Absorption:
Absorption is slow but relatively complete
(70–90%).
Distribution: Unknown. Metabolism and
Excretion: 75% metabolized by the liver,
Page | 38
25% excreted unchanged by the kidneys.
Half-life: Neonates: 1.8–8.3 days; Infants:
0.8–5.5 days; Children: 1.5–3 days; Adults:
2–6 days.
INTERACTIONS
Drug-drug: Alcohol, CNS depressants
compound CNS depression; phenobarbital
may decrease absorption and increase
metabolism of oral anticoagulants; increases
metabolism of corticosteroids, oral
contraceptives, anticonvulsants, digitoxin,
possibly decreasing their effects;
antidepressants potentiate adverse effects
of phenobarbital; griseofulvin decreases
absorption of phenobarbital; quinine
increases plasma levels.
Herbal: Kava, valerian may potentiate
sedation.
INDICATION
 Sedative
 Preanesthetic in pediatric patients
 Antiepileptic, in anesthetic doses, for
emergency control of certain acute
seizure episodes (e.g., status
epilepticus, eclampsia, meningitis,
tetanus, toxic reactions to strychnine or
local anesthetics).
CONTRAINDICATION
Contraindicated in:Hypersensitivity;
Comatose patients or those with pre-existing
CNS depression; Severe respiratory disease
with dyspnea or obstruction; Uncontrolled
severe pain; Known alcohol intolerance
(elixir only); Lactation: Discontinue drug or
bottle Feed.
ADVERSE REACTIONS/ SIDE EFFECT:
CNS: hangover, delirium, depression,
drowsiness, excitation, lethargy, vertigo.
Resp: respiratory depression; IV,
laryngospasm, bronchospasm. CV: IV—
hypotension. GI: constipation, diarrhea,
nausea, vomiting. Derm: photosensitivity,
rashes, urticaria. Local: phlebitis at IV site.
MS: arthrs.algia, myalgia, neuralgia. Misc:
hypersensitivity reactions including
angioedema and serum sickness, physical
dependence, psychological dependence.
NURSING INTERVENTIONS
Assessment:
 Monitor respiratory status, pulse, and
BP and signs and symptoms of
angioedema (swelling of lips, face,
throat, dyspnea) frequently in patients
receiving phenobarbital IV. Equipment
for resuscitation and artificial ventilation
should be readily available. Respiratory
depression is dose-dependent.
 Prolonged therapy may lead to
psychological or physical dependence.
Restrict amount of drug available to
patient, especially if depressed, suicidal,
or with a history of addiction.
 Geri: Elderly patients may react to
phenobarbital with marked excitement,
depression, and confusion. Monitor for
these adverse reactions.
 Seizures: Assess location, duration, and
characteristics of seizure activity.
 Sedation: Assess level of consciousness
and anxiety when used as a
preoperative sedative.
 Assess postoperative patients for pain
with a pain scale. Phenobarbital may
increase sensitivity to painful stimuli.
 Monitor serum folate concentrations
periodically during therapy because of
increased folate requirements of
patients on long-term anticonvulsant
therapy with phenobarbital.
Diagnoses:
 Risk for injury (Indications, Side Effects)
 Acute confusion (Side Effects)
Implementation:
 Do not confuse phenobarbital with
pentobarbital.
 Supervise ambulation and transfer of
patients following administration. Two
side rails should be raised and call bell
within reach at all times. Keep bed in
low position. Institute seizure and fall
precautions.
 When changing from phenobarbital to
another anticonvulsant, gradually
decrease phenobarbital dose while
concurrently increasing dose of
replacement medication to maintain
anticonvulsant effects.
 PO: Tablets may be crushed and mixed
with food or fluids (do not administer
dry) for patients with difficulty
swallowing. Oral solution may be taken
undiluted or mixed with water, milk, or
fruit juice. Use calibrated measuring
device for accurate measurement of
liquid doses.
Evaluation:
 Decrease or cessation of seizure activity
without excessive sedation. Several
weeks may be required to achieve
maximum anticonvulsant effects.
 Preoperative sedation.
 Improvement in sleep patterns.
 Decrease in serum bilirubin levels.

Drug Classification: SUCCINIMIDES
Generic Name: ETHOSUXIMIDE
Brand Name: Zarontin
Page | 39
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults and Children 6 yrs.):
250 mg bid initially; may increase by 250
mg/day every 4– 7 days until control
achieved (usual maintenance dose 20– 40
mg/kg/day in 2 divided doses).
PO (Children 3– 6 yrs.):
250 mg once daily initially; may increase by
250 mg/day every 4– 7 days until control
achieved (optimal dose for most children is
20 mg/kg/day in 2 divided doses).
DRUG ACTION& THERAPEUTIC EFFECT
Succinimide anticonvulsant that reduces the
current in T-type calcium channel found on
primary afferent neurons. Activation of the T
channel causes low-threshold calcium
spikes in neurons, believed to play a role in
the spikeand- wave pattern observed during
absence (petit mal) seizures. Reduces
frequency of epileptiform attacks, apparently
by depressing motor cortex and elevating
CNS threshold to stimuli.
Pharmacokinetics: Absorption: Readily
from GI tract. Peak: 4h; steady state: 4–7
days. Metabolism: In liver. Elimination: In
urine; small amounts in bile and feces. Half-
Life: 30 h (child), 60 h (adult).
INTERACTIONS
Drug-drug: Carbamazepine decreases
ethosuximide levels; isoniazid significantly
increases ethosuximide levels; levels of both
phenobarbital and ethosuximide may be
altered with increased seizure frequency.
Herbal: Ginkgo may decrease
anticonvulsant effectiveness.
INDICATION
Control of absence (petit mal) seizures; may
be given in combination with other
antiepileptics especially when other forms of
epilepsy coexist with absence seizures
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
succinimides; severe liver or kidney disease;
bone marrow suppression; use alone in
mixed types of epilepsy (may increase
frequency of grand mal seizures).
ADVERSE REACTIONS/SIDE EFFECT
CNS: Drowsiness, hiccups, ataxia,
dizziness,headache, euphoria, restlessness,
irritability, anxiety, hyperactivity,
aggressiveness, inability to concentrate,
lethargy, confusion, sleep disturbances,
night terrors, hypochondriacal behavior,
muscle weakness, fatigue. Special
Senses: Myopia. GI: Nausea, vomiting,
anorexia, epigastric distress, abdominal
pain, weight loss, diarrhea, constipation,
gingival hyperplasia. Urogenital: Vaginal
bleeding. Hematologic: Eosinophilia,
leukopenia,thrombocytopenia,
agranulocytosis,pancytopenia,
aplasticanemia, positive direct Coombs’ test.
Skin: Hirsutism, pruritic erythematousskin
eruptions, urticaria,alopecia, erythema
multiforme, exfoliativedermatitis.
NURSING INTERVENTIONS
Assessment:
 Assess location, duration, frequency,
and characteristics of seizure activity.
 Assess patient’s mood, behavioral
patterns, and facial expressions.
Patients with a history of psychiatric
disorders have an increased risk of
developing behavioral changes. These
symptoms may necessitate withdrawal
of the medication.
 Monitor closely for changes in behavior
that could indicate the emergence or
worsening of suicidal thoughts or
behavior or depression.
 Assess for rash periodically during
therapy. May cause Stevens-Johnson
syndrome. Discontinue therapy if severe
or if accompanied with fever, general
malaise, fatigue, muscle or joint aches,
blisters, oral lesions, conjunctivitis,
hepatitis and/or eosinophilia
Diagnoses:
 Risk for injury (Indications) (Side
Effects)
 Deficient knowledge, related to
medication regimen (Patient/Family
Teaching)
Implementation:
 PO:Measure liquid preparations with
calibrated measuring device.
 Administer with food or milk to minimize
GI irritation.
Evaluation:
 Decrease or cessation of seizure activity
without excessive sedation.
Drug Classification:
BENZODIAZEPINES
Generic Name: Diazepam
Brand Name: Valium
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Muscle Spasm
Adult/Adolescent/Child (5 y or older): IV 5–
10 mg q3–4h prn(larger dose for tetanus)
PO 210mg 3–4 × dayChild/Infant (1 mo.–5
y): IV 1–2 mg q3–4h prn
Anxiety
Adult/Adolescent: IV 2–10 mg repeats if
needed in 3–4 h PO2–10 mg 2–4 × day
Child/Infant (6 mo. or older): IV 0.04–0.3 mg
q2–4h (max:0.6 mg/kg/8 h)
Alcohol Withdrawal
Page | 40
Adult: IV 10 mg then 5–10 mg in 3–4 h PO
10 mg 3 or 4 × on day 1 then 5 mg 3–4 ×
day PRN
Preoperative
Adult: IV 5–15 mg 5–10 min before
procedure.
DRUG ACTION
Depresses the CNS, probably by
potentiating GABA, an inhibitory
neurotransmitter.Produces skeletal muscle
relaxation by inhibiting spinal polysynaptic
afferent pathways.Has anticonvulsant
properties due to enhanced presynaptic
inhibition.
Therapeutic Effects: Relief of anxiety.
Sedation.Amnesia.Skeletalmuscle
relaxation.Decreased seizure activity.
Pharmacokinetics: Absorption: Readily
from GI tract; erratic IM absorption.Onset:
30–60 min PO; 15–30 min IM; 1–5 min IV.
Peak: 1–2 h PO. Duration: 15 min– 1 h IV;
up to 3 h PO. Distribution: Crosses blood–
brain barrier and placenta; distributed into
breast milk. Metabolism: In liver to active
metabolites. Elimination: Primarily in urine.
Half-Life: 20–50 h.
INTERACTIONS
Drug-drug: Alcohol, CNS depressants,
anticonvulsantspotentiate CNS depression;
cimetidine increases diazepam plasma
levels, increases toxicity; may decrease
antiparkinson effects of levodopa; may
increase phenytoin levels; smoking
decreases sedative andantianxiety effects.
Herbal: Kava, valerian may potentiate
sedation.
INDICATION
Adjunct in the management of: Anxiety
Disorder, Athetosis, Anxiety relief prior to
cardioversion (injection), Stiffman
Syndrome, Preoperative sedation,
Conscious sedation (provides light
anesthesia and anterograde amnesia).
Treatment of status epilepticus/uncontrolled
seizures (injection). Skeletal muscle
relaxant. Management of the symptoms of
alcohol withdrawal. Unlabeled Use: Anxiety
associated with acute myocardial infarction,
insomnia.
CONTRAINDICATION
Hypersensitivity to diazoxide or other
thiazides; cerebral bleeding, eclampsia;
aortic coarctation; AV shunt, significant
coronary artery disease;
pheochromocytoma; lactation. Use of oral
diazoxide for functional hypoglycemia or in
presence of increased bilirubin in newborns.
ADVERSE REACTIONS/SIDE EFFECT
CNS: dizziness, drowsiness, lethargy,
depression, hangover, ataxia, slurred
speech, headache, paradoxical excitation.
EENT: blurred vision. Resp: respiratory
depression. CV: hypotension (IV only). GI:
constipation, diarrhea (may be caused by
propylene glycol content in oral solution),
nausea, vomiting, weight gain. Derm:
rashes. Local: pain (IM), phlebitis (IV), and
venous thrombosis. Misc: physical
dependence, psychological dependence,
tolerance.
NURSING INTERVENTIONS
Assessment:
 Monitor BP, pulse, and respiratory rate
prior to and periodically throughout
therapy and frequently during IV
therapy.
 Assess IV site frequently during
administration; diazepam may cause
phlebitis and venous thrombosis.
 Prolonged high-dose therapy may lead
to psychological or physical
dependence. Restrict amount of drug
available to patient. Observe depressed
patients closely for suicidal tendencies.
 Conduct regular assessment of
continued need for treatment.
 Anxiety: Assess mental status
(orientation, mood, behavior) and
degree of anxiety.
 Assess level of sedation (ataxia,
dizziness, slurred speech) prior to and
periodically throughout therapy.
Diagnoses:
 Anxiety (Indications)
 Impaired physical mobility (Indications)
 Risk for injury (Side Effects)
Implementation:
 Patient should be kept on bedrest and
observed for at least 3 hrs.following
parenteral administration.
 If opioid analgesics are used
concurrently with parenteral diazepam,
decrease opioid dose by 1/3 and titrate
dose to effect.
 Use lowest effective dose. Taper by 2
mg every 3 days to decrease withdrawal
symptoms. Some patients may require
longer taper periods (mo).
 PO: Tablets may be crushed and taken
with food or water if patient has difficulty
swallowing.
 Mix Intensol preparation with liquid or
semisolid food such as water, juices,
soda, applesauce, or pudding.
Administer entire amount immediately.
Do not store.
Page | 41
 IM: IM injections are painful and
erratically absorbed. If IM route is used,
inject deeply into deltoid muscle for
maximum absorption.
Evaluation:
 Decrease in anxiety level. Full
therapeutic antianxiety effects occur
after 1–2 wk of therapy.
 Decreased recall of surgical or
diagnostic procedures.
 Control of seizures.
 Decrease in muscle spasms.
 Decreased tremulousness and more
rational ideation when used for alcohol
withdrawal.
Drug Classification:
IMINOSTILBENES
Generic Name: Carbamazepine
Brand Name: Tegretol
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Seizures
Adult: PO 200 mg b.i.d. gradually increased
to 800–1200 mg/day in 3–4 divided doses.
Tegretol XR dosed b.i.d.
Child: PO Younger than 6 y: 10–20
mg/kg/day, may gradually increase weekly
(recommended max: 35 mg/kg/day in 3–4
divided doses); 6–12 y: 100 mg b.i.d.,
graduallyincreased to 400–800 mg/day in3–
4 divided doses (max: 1 g/day); younger
than 6 y: 20–30mg/kg/day in 3–4 divided
doses
Trigeminal Neuralgia
Adult: PO 100 mg b.i.d., gradually increased
by 100 mg increments q12h until relief;
usual dose 200–800 mg/day in 3–4 divided
doses (max: 1.2 g/day).
Tegretol XR dosed b.i.d. Bipolar Disorder
(Equetro)
Adult: PO 200 mg b.i.d.
DRUG ACTION
Decreases synaptic transmission in the CNS
by affecting sodium channels in neurons.
Therapeutic Effects: Prevention of
seizures. Relief of pain in
trigeminalneuralgia.Decreased mania.
Absorption: Slowly from GI tract. Peak:
2–8 h. Distribution: Widely distributed;
high concentrations in CSF; crosses
placenta; distributed into breast milk.
Metabolism: In liver by CYP3A4; can
induce liver microsomal enzymes.
Elimination: In urineand feces. Half-Life:
Variable due to auto-induction: 25–65 h then
14–16 h (with repeated use).
INTERACTIONS
Drug-drug: May significantly levels of
nefazodone; concurrent use contraindicated.
May decrease levels/ effectiveness of
corticosteroids, doxycycline, felbamate,
quinidine, warfarin, estrogen-containing
contraceptives, barbiturates, cyclosporine,
benzodiazepines, theophylline, lamotrigine,
phenytoin, topiramate, valproic acid,
bupropion, and haloperidol.
Drug-Food: Grapefruit juice increase serum
levels and oral bioavailability by 40% and
therefore may increase effects.
INDICATION
Treatment of tonic-clonic, mixed, and
complex-partial seizures. Management of
pain in trigeminal neuralgia or diabetic
neuropathy. Equetro only: Acute mania and
mixed mania. Unlabeled Use: Other forms of
neurogenic pain.
CONTRAINDICATION
Contraindicated in: Hypersensitivity; Bone
marrow suppression; Concomitant use or
use within 14 days of MAO inhibitors;
Concurrent use of nefazodone; OB: Use
only if potential benefits outweigh risks to
the fetus; additional vitamin K during last
weeks of pregnancy has been
recommended; Lactation: Discontinue drug
or bottle feed.
ADVERSE REACTIONS/SIDE EFFECT:
CNS: suicidal thoughts,ataxia, drowsiness,
fatigue, psychosis, sedation, vertigo. EENT:
blurred vision, corneal opacities, nystagmus.
Resp: pneumonitis. CV: HF, edema,
hypertension, hypotension, syncope. GI:
hepatitis, increase liver enzymes,
pancreatitis, weight gain. GU: hesitancy,
urinary retention. Derm: Stevens- Johnson
syndrome, toxic epidermal necrolysis, nail
shedding, photosensitivity, rash, urticaria. F
andE: syndrome of inappropriate antidiuretic
hormone (SIADH), hyponatremia. Hemat:
agranulocytosis, aplastic anemia,
thrombocytopenia, eosinophilia, leukopenia,
lymphadenopathy. Misc: chills, fever, multi-
organ hypersensitivity reactions.
NURSING INTERVENTIONS
Assessment:
 Monitor closely for notable changes in
behavior that could indicate the
emergence or worsening of suicidal
thoughts or behavior or depression.
 Monitor for changes in skin condition in
early therapy. Stevens-Johnson
syndrome and toxic epidermal
necrolysis are significantly more
common in patients with a particular
human leukocyte antigen (HLA) allele,
HLA-B*1502 (occurs almost exclusively
in patients with Asian ancestry, including
South Asian Indians).
Diagnoses:
 Risk for injury (Indications, Side Effects)
 Chronic pain (Indications)
Page | 42
 Disturbed thought process (Indications)
Implementation:
 Do not confuse carbamazepine with
oxcarbazepine. Do not confuse Tegretol
with Trental or Tegretol XR.
 Implement seizure precautions as
indicated.
 PO: Administer medication with food to
minimize gastric irritation. May take at
bedtime to reduce daytime sedation.
Tablets may be crushed if patient has
difficulty swallowing. Do not crush or
chew ex
Evaluation:
 Absence or reduction of seizure activity.
 Decrease in trigeminal neuralgia pain.
Patients with trigeminal neuralgia who
are pain-free should be re-evaluated
every 3 mo to determine minimum
effective dose
 Decreased mania and depressive
symptoms in bipolar I disorder.
Drug Classification: VALPROATE
Generic Name: Valproic Acid
Brand Name: Depakote, Depakene,
Depacon
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Management of Seizures
Adult/Child (10 y or older): PO/IV
10–15 mg/kg/day in divided doses when
total daily dose greater than 250 mg,
increase at 1 wk intervals by 5–10 mg/kg/
day until seizures are controlled or adverse
effects develop (max: 60 mg/kg/day)
Conversion of PO to IV: Give normal dose in
divided doses q6h
Migraine Headache Prophylaxis
Adult: PO 250 mg b.i.d. (max: 1000 mg/day)
or Depakote ER500 mg daily × 1 wk, may
increase to 1000 mg daily
Mania
Adult: PO 750 mg/day administered in
divided doses OR
Extended release: 25 mg/kg/day
DRUG ACTION
Increase levels of GABA, an inhibitory
neurotransmitter in the CNS.
Therapeutic Effects: Suppression
of seizure activity. Decreased manic
episodes.Decreased frequency of migraine
headaches.
Absorption: Well absorbed following oral
administration; divalproex is enteric-coated,
and absorption is delayed. ER form
produces lower blood levels. IV
administration results in complete
bioavailability. Distribution: Rapidly
distributed into plasma and extracellular
water. Cross blood-brain barrier and
placenta; enters breast milk.
Protein Binding: 80–90% decreased in
neonates, elderly, renal impairment, or
chronic hepatic disease.
Metabolism and Excretion: Mostly
metabolized by the liver; minimal amounts
excreted unchanged in urine.
Half-life: Adults: 9–16 hrs.
INTERACTIONS
Drug-drug: Alcohol and other CNS
depressants potentiate depressant effects;
other anticonvulsants, barbiturates increase
or decrease anticonvulsant and barbiturate
levels; haloperidol, loxapine, maprotiline,
maois, phenothiazines, thioxanthenes,
tricyclic antidepressants can increase CNS
depression or lower seizure threshold;
aspirin, dipyridamole, warfarin increase risk
of spontaneous bleeding; clonazepam may
precipitate absence seizures; salicylates,
cimetidine, isoniazid may increase valproic
acid levels and toxicity. mefloquinecan
decrease valproic acid levels; meropenem
may decrease valproic acid levels;
cholestyramine may decrease absorption.
Herbal: Ginkgo may decrease
anticonvulsant effectiveness.
INDICATION
Monotherapy and adjunctive therapy for
simple and complex absence
seizures.Monotherapy and adjunctive
therapy for complex partial seizures.
Adjunctive
therapy for patients with multiple seizure
types, including absence seizures.
Divalproex sodium only.Manic episodes
associated with bipolar disorder. Prevention
of migraine headache.
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
valproate sodium; hepatic disease or
significant hepatic function impairment; urea
cycle disorders.Hyperammonemia,
encephalopathy; suicidal ideations;
thrombocytopenia, patient with bleeding
disorders or liver dysfunction or disease,
cirrhosis, hepatitis; drug induced
pancreatitis; congenital metabolic disorders,
those with severe seizures, or on multiple
anticonvulsant drugs; AIDS; mitochondrial
disorders caused by mutations in
mitochondrial DNA POLG and children
younger than 2 y who are suspected of
having a POLG-related disorder; fluid
restriction or decreased food intake;
pregnancy (category D); lactation.
ADVERSE REACTIONS/SIDE EFFECT:
CNS: suicidal thoughts,agitation, dizziness,
headache, insomnia, sedation, confusion,
depression. CV: peripheral edema. EENT:
Page | 43
visual disturbances. GI: Hepatotoxicity,
pancreatitis, abdominal pain, anorexia,
diarrhea, indigestion, nausea, vomiting,
constipation, increase appetite. Derm:
alopecia, rashes. Endo: weight gain.
Hemat: leukopenia, thrombocytopenia.
Metab: hyperammonemia. Neuro:
hypothermia, tremor, ataxia.
NURSING INTERVENTIONS
Assessment:
 Seizures: Assess location, duration, and
characteristics of seizure activity.
Institute seizure precautions.
 Bipolar Disorder: Assess mood,
ideation, and behavior frequently.
 Migraine Prophylaxis: Monitor frequency
and intensity of migraine headaches.
 Geri: Assess geriatric patients for
excessive somnolence.
 Assess for suicidal tendencies,
especially during early therapy. Restrict
amount of drug available to patient. Risk
may be increased in children,
adolescents, and adults <=24 yrs.
Diagnoses:
 Risk for injury (Indications)
Implementation:
 Do not confuse Depakote ER and
regular dose forms. Depakote ER
produces lower blood levels than
Depakote dosing forms. If switching
from Depakote to Depakote ER,
increase dose by 8-20%.
 Single daily doses are usually
administered at bedtime because of
sedation.
 PO: Administer with or immediately after
meals to minimize GI irritation.
Extended-release and delayed- release
tablets and capsules should be
swallowed whole, do not open, break, or
chew; will cause mouth or throat
irritation and destroy extended release
mechanism. Do not administer tablets
with milk or carbonated beverages (may
cause premature dissolution). Delayed-
release divalproex sodium may cause
less GI irritation than valproic acid
capsules.
 Shake liquid preparations well before
pouring. Use calibrated measuring
device to ensure accurate dose. Syrup
may be mixed with food or other liquids
to improve taste.
Evaluation:
 Decreased seizure activity.
 Decreased incidence of manic episodes
in patients with bipolar disorders.
 Decreased frequency of migraine
headaches.
Drug Classification: PYRSROLIDINE
Generic Name: Levetiracetam
Brand Name: Keppra
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Adults and children older than 16 yrs.
 Partial-onset seizures: 1,000 mg/day
given as 500 mg PO or IV bid; may be
increased in 1,000-mg/day increments
every 2 wk; maximum dose, 3,000
mg/day. ER tablets: 1,000 mg/day PO;
increase every 2 wk in 1,000 mg/day
intervals to maximum dosage 3,000
mg/day.
 Generalized tonic-clonic seizures:
Initially, 1,000 mg/day PO given as 500
mg bid; increase by 1,000 mg/day every
2 wk to recommended 3,000 mg/day.
Adults and children 12 yrs. and older
 Myoclonic seizures: 1,000 mg/day given
as 500 mg PO bid; slowly increase to
recommend maximum dose, 3,000
mg/day.
Pediatric patients 6–15 yrs.
 Generalized tonic-clonic seizures:
Initially, 20 mg/kg/day PO in two divided
doses of 10 mg/kg. Increase every 2 wk
by 20-mg/kg increments to
recommended dosage of 60 mg/kg/day
given as 30 mg/kg bid.
Pediatric patients 4–16 yrs.
 Partial-onset seizures: 10 mg/kg PO bid
 (500–1,000 mg/day) may be increased
every 2 wk in 20 mg/kg increments to 30
mg/kg bid (1,500–3,000 mg/day). To
determine daily dose of oral solution:
total dose (mL/day) _daily dose
(mg/kg/day)patient weight (kg) divided
by 100 mg/mL.
DRUG ACTION
Appears to inhibit burst firing without
affecting normal neuronal excitability and
may selectively prevent
hypersynchronization of epileptiform burst
firing and propagation of seizure activity.
Therapeutic Effects: Decreased incidence
and severity of seizures.
Pharmacokinetics: Absorption: Rapidly
and completely absorbed following oral
administration.
Distribution: Unknown.
Protein Binding: <10%.
Metabolism and Excretion: 66% excreted
unchanged by the kidneys; some
metabolism by the liver (metabolites
inactive).
Half-life: 7.1 hrs. (Increase in renal
impairment)
Page | 44
INTERACTIONS
Drug-drug: Levetiracetam does not affect
estrogen, warfarin, or digoxin levels or affect
levels of other antiepileptic drugs.
Sevelamer, colesevelam may decrease
effectiveness.
INDICATION
Partial onset seizures (adjunct). Primary
generalized tonic-clonic seizures (adjunct)
(immediate-release and injection only).
Myoclonic seizures in patients with juvenile
myoclonic epilepsy (adjunct) (immediate-
release and injection only).
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
levetiracetam; suicidal ideation; labor;
lactation; Extended release tablets:
children younger than 12.
ADVERSE REACTIONS /SIDE EFFECT
CNS: Suicidal Thoughts, Aggression,
Agitation, Anger, Anxiety, Apathy,
Depersonalization, Depression, Dizziness,
Hostility, Irritability, Personality Disorder,
Weakness, Drowsiness, Dyskinesia,
Fatigue.Neuro: Coordination Difficulties
(Adults Only). Derm:Stevens-Johnson
Syndrome, Toxic Epidermal Necrolysis.
NURSING IMPLICATIONS
Assessment:
 Assess location, duration, and
characteristics of seizure activity.
 Assess patient for CNS adverse effects
throughout therapy. These adverse
effects are categorized as somnolence
and fatigue (asthenia), coordination
difficulties (ataxia, abnormal gait, or
incoordination), and behavioral
abnormalities (agitation, hostility,
anxiety, apathy, emotional lability,
depersonalization, depression) and
usually occur during the first 4 wk of
therapy.
 Monitor mood changes. Assess for
suicidal tendencies, especially during
early therapy. Restrict amount of drug
available to patient.
 Assess for rash periodically during
therapy. May cause Stevens-Johnson
syndrome. Discontinue therapy if severe
or if accompanied with fever, general
malaise, fatigue, muscle or joint aches,
blisters, oral lesions, conjunctivitis,
hepatitis and/or eosinophilia.
Diagnoses:
 Risk for injury (Side Effects)
Implementation:
 Do not confuse Keppra (levetiracetam)
with Kaletra (lopinavir/ritonavir).
 IV doses should be used temporarily
when oral route is not feasible. To
convert IV to PO, equivalent dose and
frequency may be used.
 PO: May be administered without regard
to meals.
 Administer tablets whole; do not
administer partial tablets. Do not break,
crush, or chew XR tablets.
 Pedi: Patients _20 kg should receive
oral solution. Administer with calibrated
measuring device for accurate dose.
 Discontinue gradually minimizing the
risk of increase in seizure frequency.
Evaluation:
 Decrease in the frequency of or
cessation of seizures.
Drug Classification: AMPA
RECEPTOR ANTAGONISTS
Generic Name: Perampanel
Brand Name: Fycompa
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults and Children_12 yrs.): 2 mg
once daily at bedtime initially, may be
increased by 2 mg weekly up to 4–12 mg
daily; concurrent enzyme-inducers—4 mg
once daily at bedtime initially may be
increased by 2 mg weekly up to 12mg daily.
Daily dose should not exceed 12 mg.
PO (Geriatric Patients): 2 mg once daily at
bedtime initially, may be increased by 2 mg
every 2 wk up to 4–12 mg daily; concurrent
enzyme inducers— 4 mg once daily at
bedtime initially may be increased by 2 mg
every 2 wk up to 12 mg daily. Daily dose
should not exceed 12 mg.
DRUG ACTION
Acts as a non-competitive -amino-3 hydroxy-
5– methyl-4– isoxazolepropionic acid
(AMPA) antagonist on post-synaptic
neuronal glutamate (excitatory)
receptors.Therapeutic Effects: Decreased
incidence and severity of partial-onset
seizures.
Pharmacokinetics: Absorption: Rapidly
and completely absorbed following oral
administration. Distribution: Unknown.
Protein Binding: 95– 96%. Metabolism
andExcretion: Extensively metabolized by
CYP3A4/5 enzyme systems; excreted in
urine and feces primarily as metabolites.
Half-life: 105 hrs.
INTERACTIONS
Drug-drug: Doses >12 m g/day may
decrease effectiveness of levonorgestrel-
containing hormonal contraceptives.
Page | 45
CYPP450 inducers including
carbamazepine, oxcarbazepine,
phenobarbital, phenytoin, primidone, and
topiramate can decrease levels and
effectiveness; careful monitoring is required
especially during initiation and withdrawal.
Dosage adjustments may be required.
Increase risk of CNS depression with other
CNS depressants including alcohol,
sedating antihistamines, barbiturates,
benzodiazepines, opioids and
sedative/hypnotics
Drug-Natural Products: Levels and
effectiveness may bepby St. John’s wort;
concurrent use should be avoided.
INDICATION
Adjunctive treatment (with other antiepileptic
drugs [AEDs])of partial-onset seizures with
or without secondarily generalized seizures
in epileptic patients 12 yrs.
CONTRAINDICATION
Contraindicated in: Strong P450 inducers
(other than AEDs); severe hepatic
impairment.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: dizziness, drowsiness, headache,
aggression, anger, fatigue,
psychiatric/behavioral problems, hostility,
irritability, suicidal ideation, vertigo. Metab:
weight gain. Neuro: ataxia, balance
disorder, gait disturbance. Misc: falls.
NURSING INTERVENTIONS
Assessment:
 Assess location, duration, and
characteristics of seizure activity.
Institute seizure precautions. Assess
response to and continued need for
perampanel periodically during therapy.
 Monitor closely for notable changes in
behavior that could indicate the
emergence or worsening of suicidal
thoughts or behavior, new or worse
aggressive behavior, or depression.
Diagnoses:
 Risk for injury (Indications)
Implementation:
 PO: Administer once daily at bedtime.
Evaluation:
 Decreased seizure activity.
Drug Classification: CARBONIC
ANHYDRASE INHIBITOR
Generic Name: Acetazolamide
Brand Name: Diamox
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): Glaucoma (open angle)—250–
1000 mg/day in 1–4 divided doses (up to
250 mg q 4 hrs.) or 500-mg extended-
release capsules twice daily. Epilepsy— 4–
16 mg/kg/day in 1–4 divided doses
(maximum 30 mg/kg/day or 1 g/day).
Altitude sickness— 250 mg 2–4 times daily
started 24–48 hrs.before ascent, continued
for 48 hrs.or longer to control symptoms.
Antiurolithic—250 mg at bedtime.Edema—
250–375 mg/day.Urine alkalinization—5
mg/kg/ dose repeated 2–3 times over 24
hrs..
PO (Children): Glaucoma—8–30 mg/kg
(300– 900 mg/m2/day) in 3 divided doses
(usual range 10– 15 mg/kg/day). Edema—5
mg/kg/dose once daily.Epilepsy—4–16
mg/kg/day in 1–4 divided doses (maximum
30 mg/kg/day or 1 g/day).
PO (Neonates): Hydrocephalus—5
mg/kg/dose q 6 hrs.increase by 25
mg/kg/day up to a maximum of 100 mg/kg/
day.
DRUG ACTION
Inhibition of carbonic anhydrase in the eye
results in decreased secretion of aqueous
humor. Inhibition of renal carbonic
anhydrase, resulting in self-limiting urinary
excretion of sodium, potassium,
bicarbonate, and water. CNS inhibition of
carbonic anhydrase and resultant diuresis
may decrease abnormal neuronal firing.
Alkaline diuresis prevents precipitation of
uric acid or cystine in the urinary tract.
Therapeutic Effects: Lowering of
intraocular pressure. Control of some types
of seizures.Prevention and treatment of
acute altitude sickness.Diuresis and
subsequent mobilizationof excess
fluid.Prevention of uric acid or cystine renal
calculi.
Absorption: Dose dependent; erratic with
doses 10 m g/kg/day. Distribution: Crosses
the placenta and blood-brain barrier; enters
breast milk. Protein Binding: 95%.
Metabolism andExcretion: Excreted
mostly unchanged in urine. Half-life: 2.4–
5.8 hrs.
INTERACTIONS
Drug-drug: Excretion of barbiturates,
aspirin, and lithium is increase and may lead
to decrease effectiveness. Excretion of
amphetamine, quinidine, procainamide, and
possibly tricyclic antidepressants is increase
and may lead to toxicity. May increase
cyclosporine levels.
INDICATION
Lowering of intraocular pressure in the
treatment of glaucoma.Management of
acute altitude sickness. Edema due to HF.
Adjunct to the treatment of refractory
seizures
CONTRAINDICATION
Page | 46
Contraindicated in: Hypersensitivity or
cross-sensitivity with sulfonamides may
occur; Hepatic disease or insufficiency;
Concurrent use with ophthalmic carbonic
anhydrase inhibitors (brinzolamide,
dorzolamide) is not recommended; OB:
Avoid during first trimester of pregnancy.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: Depression, Fatigue, Weakness,
Drowsiness. EENT: Transient
Nearsightedness. GI: Anorexia, Metallic
Taste, Nausea, Vomiting, Melena. GU:
Crystalluria, Renal Calculi. DERM: Stevens-
Johnson Syndrome, Rashes. Endo:
Hyperglycemia. F and E: Hyperchloremic
Acidosis, Hypokalemia, Growth Retardation
(In Children Receiving Chronic Therapy).
Hemat: Aplastic Anemia, Hemolytic Anemia,
Leukopenia. Metab: Weight Loss,
Hyperuricemia. Neuro: Paresthesias. Misc:
Allergic Reactions Including Anaphylaxis.
NURSING IMPLICATIONS
Assessment:
 Observe for signs of hypokalemia
(muscle weakness, malaise, fatigue,
ECG changes, vomiting).
 Assess for allergy to sulfonamides.
 Intraocular Pressure: Assess for eye
discomfort or decrease in visual acuity.
 Seizures: Monitor neurologic status in
patients receiving acetazolamide for
seizures. Initiate seizure precautions.
 Altitude Sickness: Monitor for decrease
in severity of symptoms (headache,
nausea, vomiting, fatigue, dizziness,
drowsiness, shortness of breath). Notify
health care professional immediately if
neurologic symptoms worsen or if
patient becomes more dyspneic and
rales or crackles develop.
Diagnoses:
 Disturbed sensory perception (visual)
(Indications)
Implementation:
 Do not confuse acetazolamide with
acetohexamide. Do not confuse Diamox
with Diabinese.
 Encourage fluids to 2000–3000 mL/day,
unless contraindicated, to prevent
crystalluria and stone formation.
 A potassium supplement without
chloride should be administered
concurrently with acetazolamide.
Evaluation:
 Decrease in intraocular pressure when
used for glaucoma. If therapy is not
effective or patient is unable to tolerate
one carbonic anhydrase inhibitor, using
another may be effective and more
tolerable.
 Decrease in the frequency of seizures.
 Reduction of edema.
 Prevention of altitude sickness.
 Prevention of uric acid or cystine stones
in the urinary tract.
Drug Classification: CARBAMATE
Generic Name: Felbamate
Brand Name: Felbatol
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Partial Seizures
Adult: PO Initiate with 1200 mg/ day in 3–4
divided doses, may increase by 600 mg/day
q2wk (max: 3600 mg/day); when converting
to monotherapy, reduce dose of concomitant
anticonvulsants by 1/3 when initiating
felbamate, then continue to decrease other
anticonvulsants by 1/3 with each increase in
felbamate q2wk; when using as adjunctive
therapy, decrease other anticonvulsants by
20% when initiating felbamate and note that
further reductions in other anticonvulsants
may be required to minimize side effects
and drug interactions
Lennox–Gastaut Syndrome
Child: PO Start at 15 mg/kg/day in 3 or 4
divided doses, reduce concurrent
antiepileptic drugs by 20%, further
reductions may be required to minimize side
effects due to drug interactions, may
increase felbamate by 15 mg/kg/ day at
weekly intervals (max: 45 mg/kg/day)
DRUG ACTION
Anticonvulsant that blocks repetitive firing of
neurons and increases seizure threshold;
prevents seizure spread. Increases seizure
thresholdand prevents seizure spread.
Therapeutic Effects: Decreased incidence
of seizures.
Absorption: 90% from GI tract.
Absorptionof tablet not affected by
food.Onset:
Therapeutic effect approximately 14
days.Peak: Peak plasma levels at 1–6 h.
Distribution: 20–25% protein bound readily
crosses the blood–brain barrier.
Metabolism: In the liver via the cytochrome
P450 system. Elimination: 40–50%
excreted unchanged in urine, rest excreted
in urine as metabolites. Half-Life: 20–23 h.
INTERACTIONS
Drug-drug: Felbamatereduces serum
carbamazepinelevels by a mean of 25%,but
increases levels of its activemetabolite,
increases serum phenytoinlevels
approximately 20%,and increases valproic
acid levels.
Page | 47
Herbal: Gingko may decrease
anticonvulsanteffectiveness.
INDICATION
Used alone (monotherapy) or as adjunctive
therapy with other anticonvulsants in
treatment of partial seizures. Adjunctive
therapy with other anticonvulsants in
children (2– 14 yr) who have partial or
generalized seizures associated with
LennoxGastaut syndrome. Because of
deaths due to aplastic anemia and acute
liver failure, felbamate should never be used
as a first-line therapy, but should be
reserved for patients whose epilepsy is so
severe that these risks are considered
acceptable given the drug’s benefit.
CONTRAINDICATION
Containdicated in: Hypersensitivity to
felbamate, history of blood dyscrasia or
hepatic dysfunction; bone marrow
depression; active liver Disease; elevated
serum AST or ALT; Severe anemia.
NURSING INTERVENTIONS
Assessment
 Assess location, duration, and
characteristics of seizure activity.
 Monitor closely for notable changes in
behavior that could indicate the
emergence or worsening of suicidal
thoughts or behavior or depression.
 Lab Test Considerations: Monitor CBC
with differential to determine baseline
levels prior to and frequently during
therapy. Ifpin WBC, hemoglobin,
hematocrit, or platelet count occurs,
monitor closely and discontinue
felbamate.
 Monitor hepatic function prior to and
frequently during therapy. May
causeqserum bilirubin, AST, and ALT
levels. Discontinue felbamate
immediately if any indication of liver
injury develops.
 Toxicity and Overdose: When used as
adjunctive therapy with other
anticonvulsants, monitor serum blood
levels of other anticonvulsants
throughout therapy.
Diagnoses
 Risk for injury (Indications) (Side
Effects) Deficient knowledge, related to
medication regimen (Patient/Family
Teaching) Implementation
 Implement seizure precautions. Obtain
written, informed consent from patient
before initiating therapy.
 PO:May be administered with food or
antacids to minimize gastric irritation.
 Shake oral suspension well before
administering. Store at room
temperature.
Evaluation
 Absence or reduction of seizure activity
Drug Classification: GABA Analogs
Generic Name: Pregabalin
Brand Name: Lyrica
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Diabetic Neuropathic Pain
PO (Adults): 50 mg 3 times daily, increase
over 7 days up to100 mg 3 times daily.
Postherpetic Neuralgia
PO (Adults): 75 mg twice daily or 50 mg 3
times daily initially, may be increase over 7
days to 300 mg/day in 2–3 divided doses;
after 2–4 wk may be increased to 600
mg/day in 2–3 divided doses.
Fibromyalgia
PO (Adults): 75 mg twice daily initially, may
be increased to 150 mg twice daily within 1
wk based on efficacy and tolerability. Maybe
increased to 225 twice daily.
DRUG ACTION
Binds to calcium channels in CNS tissues
which regulate neurotransmitter
release.Does not bind to opioid receptors.
Therapeutic Effects: Decreased
neuropathic or post-herpetic pain.
Decreased partial-onset seizures.
Pharmacokinetics: Absorption: Well
absorbed (90%) following oral
administration. Distribution: Probably
crosses the blood-brain barrier. Metabolism
and Excretion: Minimally metabolized, 90%
excreted unchanged in urine.
Half-life: 6 hrs.
INTERACTIONS
Drug-drug: Concomitant use with
thiazolidinediones may exacerbate weight
gain and fluid retention.
INDICATION
Neuropathic pain associated with diabetic
peripheral neuropathy. Postherpetic
neuralgia.Fibromyalgia.Neuropathic pain
associated with spinal cord injury. Adjunctive
therapy of partial-onset seizures in adults.
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
pregabalin or gabapentin; suicidal ideation
or worsening of depression or unusual
changes in mood or behavior; lactation.
ADVERSE REACTIONS/ SIDE EFFECT
Page | 48
CNS: suicidal thoughts, dizziness,
drowsiness, impaired attention/
concentration/thinking. CV: edema. EENT:
blurred vision. GI: dry mouth, abdominal
pain, constipation, increase appetite,
vomiting. Hemat: thrombocytopenia. Metab:
weight gain. Misc: allergic reactions, fever.
NURSING IMPLICATIONS
Assessment:
 Monitor closely for notable changes in
behavior that could indicate the
emergence or worsening of suicidal
thoughts or behavior or depression.
 Diabetic Peripheral Neuropathy, Post
herpetic Neuralgia, Fibromyalgia, and
Spinal Cord Injury Pain: Assess location,
characteristics, and intensity of pain
periodically during therapy.
 Seizures: Assess location, duration, and
characteristics of seizure activity.
 Lab Test Considerations: May cause
increase creatine kinase levels.
Diagnoses:
 Risk for injury (Adverse Reactions)
Implementation:
 Do not confuse Lyrica (pregabalin) with
Lopressor (metoprolol).
 Pregabalin should be discontinued
gradually over at least 1 wk. Abrupt
discontinuation may cause insomnia,
nausea, headache, anxiety, sweating,
and diarrhea when used for pain and
may cause increase in seizure
frequency when treating seizures.
 PO: May be administered without regard
to meals. Oral solution may be stored at
room temperature.
Evaluation:
 Decrease in intensity of chronic pain.
 Decrease in the frequency or cessation
of seizures.
Drug Classification: GABA
REUPTAKE INHIBITORS
Generic Name: Tiagabine
Brand Name: Gabitril
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Adults
4 mg PO daily for 1 wk; may be increased
by 4–8 mg/wk until desired response is
seen; maximum dose, 56 mg/day in two to
four divided doses. Usual maintenance dose
is 32–56 mg daily.
Pediatric patients 12–18 yrs.
4 mg PO daily for 1 wk; may be increased to
8 mg/day in two divided doses for 1 wk; then
Increased by 4–8 mg/wk up to a maximum
of 32 mg/day in two to four divided doses.
DRUG ACTION
Enhances the activity of gamma
aminobutyric acid, an Inhibitory
neurotransmitter.
Therapeutic Effects: Decreased frequency
of seizures.
Pharmacokinetics: Absorption: 90%
absorbed following oral administration.
Distribution: Unknown. Protein Binding:
96%. Metabolism and Excretion: Mostly
metabolized by the liver; 2% excreted
unchanged in urine. Half-life: Without
enzyme-inducing antiepileptic drugs—7–9
hrs.;with enzyme-inducing antiepileptic
drugs—4–7 hrs..
INTERACTIONS
Drug-drug: Carbamazepine, phenytoin,
primidone, and phenobarbital induce
metabolism and decrease blood levels;
although concurrent therapy is usually
necessary, adjustments may be required
when altering regimens.
INDICATION
Adjunctive therapy in patients older than 12
yrs. with partial seizures
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
tiagabine; lactation.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: suicidal thoughts, dizziness,
drowsiness, nervousness, weakness,
cognitive impairment, confusion, difficulty
concentrating, hallucinations, headache,
mental depression, personality disorder.
Eent: abnormal vision, ear pain, tinnitus.
Resp:dyspnea, epistaxis. CV: chest pain,
edema, hypertension, palpitations,
syncope, tachycardia. GI:abdominal pain,
gingivitis, nausea, stomatitis.
GU:dysmenorrhea, dysuria, metrorrhagia,
urinary incontinence. Derm:alopecia,
dry skin, rash, sweating. Metab:weight gain,
weight loss. MS:arthrs.algia, neck pain.
NEURO: ataxia, tremors. Misc:allergic
reactions, chills, lymphadenopathy.
NURSING IMPLICATIONS
Assessment:
 Assess location, duration, and
characteristics of seizure activity.
 Assess mental status. May cause
impaired concentration, speech or
language problems, confusion, fatigue,
and drowsiness. Symptoms may
decrease with dose reduction or
discontinuation.
 Monitor closely for notable changes in
behavior that could indicate the
emergence or worsening of suicidal
thoughts or behavior or depression.
Page | 49
 Toxicity and Overdose: Therapeutic
serum levels have not been determined.
However, levels may be monitored prior
to and following changes in the
therapeutic regimen.
Diagnoses:
 Risk for injury (Side Effects)
Implementation:
 Do not confuse tiagabine with tizanidine.
 PO: Administer with food.
 Discontinue tiagabine gradually. Abrupt
discontinuation may cause increase in
seizure frequency.
Evaluation:
 Decrease in the frequency or cessation
of seizures.
Drug Classification: NEURONAL
POTASSIUM CHANNEL OPENERS
Generic Name: Ezogabine
Brand Name: Potiga
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 100 mg 3 times daily for 1 wk,
then increase by 150 mg/day at weekly
intervals to maintenance dose of 200– 400
mg 3 times daily (not to exceed 1200
mg/day).
PO (Geriatric Patients): 50 mg 3 times
daily initially, and then increase by 150
mg/day at weekly intervals to maintenance
dose not to exceed 750 mg/day.
Renal Impairment PO (Adults): CCr< 50
mL/min—50 mg 3 times daily initially, and
then increase by 150 mg/ day at weekly
intervals to maintenance dose not to exceed
600 mg/day.
DRUG ACTION
Enhances trans membrane potassium
currents (enhances KCNQ channels),
stabilizes resting membrane potential and
decreases excitability. May also increase
GABA-mediated currents.
Therapeutic Effects: Decreased
occurrence of partial-onset seizures
Absorption:Well absorbed (60%) following
oral administration. Distribution: Unknown.
Metabolism and Excretion: Extensively
metabolized, one metabolite (NAMR) has
anti-epileptic activity; 36% excreted
unchanged in urine. Half-life: 7– 11 hrs.
INTERACTIONS
Drug-drug: Blood levels and effectiveness
may be decrease by carbamazepine or
phenytoin; larger doses may be required.
One metabolite may decrease excretion of
digoxin; monitoring is recommended.
Concurrent use of alcohol increase blood
levels and risk of adverse reactions.
INDICATION
Adjunctive treatment of partial-onset
seizures.
CONTRAINDICATION
Contraindicated in: Lactation: Breast
feeding not recommended.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: dizziness, drowsiness, aphasia,
confusion, dysarthria, fatigue, hallucinations,
impaired attention, impaired memory,
psychoses, suicidal thoughts/ideation
.EENT: blurred vision, conjunctival
discoloration, diplopia, retinal pigment
changes, scleral discoloration. Neuro:
abnormal coordination, balance disorder,
gait disturbance, tremor. GU: urinary
retention. Derm: blue skin discoloration.
Misc: physical dependence.
NURSING INTERVENTIONS
Assessment
 Assess location, duration, and
characteristics of seizure activity.
Institute seizure precautions. Assess
response to and continued need for
Ezogabine periodically during therapy.
 Monitor patient for signs and symptoms
of urinary retention (inability to urinate,
pain with urination), especially patients
with increased risk (benign prostatic
hyperplasia, patients unable to
communicate symptoms, patients taking
concomitant mediations that may affect
voiding such as anticholinergics).
 Monitor closely for notable changes in
behavior that could indicate the
emergence or worsening of suicidal
thoughts or behavior or depression.
 Obtain systematic visual monitoring,
including visual acuity and dilated
fundus photography, by an
ophthalmologist at baseline and every 6
months during therapy. If abnormalities
in pigment of retina or vision changes
are detected, discontinue therapy unless
benefits outweigh risks of potential
vision loss.
Diagnoses:
 Risk for injury (Indications)
Implementation:
 PO: Administer 3 times daily without
regard to food. Swallow tablets whole;
do not crush, break or chew.
Evaluation:
 Decreased seizure activity.
Drug Classification: TRIAZINE
Page | 50
Generic Name: Lamotrigine
Brand Name: Lamictal
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): Following discontinuation of
valproate (if current dose 100 mg/day)—qto
150 mg/day for 1 wk, then 200 mg/day;
Following discontinuation of carbamazepine,
phenobarbital, phenytoin, primidone, or
rifampin (if current dose 400 mg/day)—400
mg/day for 1 wk, then 300 mg/day for1 wk,
then 200 mg/day; Following discontinuation
of other psychotropic—maintain previous
dose.
DRUG ACTION
Stabilizes neuronal membranes by inhibiting
sodium transport.
Therapeutic Effects: Decreased incidence
of seizures. Delayed time to recurrence of
mood episodes.
Pharmacokinetics: Absorption: 98%
absorbed following oral administration.
Distribution: Enters breast milk. Highly
bound to melanin-containing tissues (eyes,
pigmented skin). Metabolism and
Excretion: Mostly metabolized by the liver
to inactive metabolites; 10% excreted
unchanged by the kidneys. Half-life:
Children taking enzyme–inducing
antiepileptic drugs (AEDs): 7–10 hrs.;
Children taking enzyme inducers and
valproic acid : 15–27 hrs.; Children taking
valproic acid: 44–94 hrs.; Adults: 25.4 hrs.
(duringchronic therapy of lamotrigine alone).
INTERACTIONS
Drug-drug: Carbamazepine, phenobarbital,
primidone, phenytoin, fosphenytoin,
rifampin, oral contraceptives may decrease
lamotrigine levels. Valproicacid may
increase lamotrigine levels. Lamotrigine may
decrease serum levels of valproic acid. May
affect efficacy of ORAL contraceptives.
chronicacetaminophen use may affect
serum concentrations of lamotrigine.
Herbal: Ginkgo may decrease
anticonvulsant effectiveness. Evening
primrose oil may affect seizure threshold.
INDICATION
Adjunct treatment of partial seizures in
adults and children with epilepsy
(immediate-release, extended release,
chewable, and orally disintegrating tablets).
Lennox-Gastaut syndrome (immediate-
release, chewable, and orally disintegrating
tablets only). Adjunct treatment of primary
generalized tonic-clonic seizures
in adults and children (immediate-release,
extendedrelease, chewable, and orally
disintegrating tablets). Conversion to
monotherapy in adults with partial seizures
receiving carbamazepine, phenytoin,
phenobarbital, primidone, or valproate as
the single antiepileptic drug (immediate-
release, extended-release, chewable, and
orally disintegrating tablets only).
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
lamotrigine, development of any skin rash
unless it is clearly not related to the drug;
suicidal ideation especially if severe or
abrupt in onset; lactation. Lamotrigine ER is
not approved for children younger than 13 y.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: aseptic meningitis, suicidal thoughts,
ataxia, dizziness, headache, behavior
changes, depression, drowsiness, insomnia,
tremor. EENT: blurred vision, double vision,
rhinitis. GI: hepatic failure, nausea, vomiting.
GU: vaginitis. DERM: photosensitivity,
rash(higher incidence in children, patients
taking valproic acid, high initial doses, or
rapid dose increases). MS: arthralgia. MISC:
multi-organ hypersensitivity reactions,
stevens-johnson syndrome.
NURSING IMPLICATIONS
Assessment:
 Monitor closely for notable changes in
behavior that could indicate the
emergence or worsening of suicidal
thoughts or behavior or depression.
 Assess patient for skin rash frequently
during therapy. Discontinue lamotrigine
at first sign of rash; may be life-
threatening. Stevens-Johnson syndrome
or toxic epidermal necrolysis may
develop. Rash usually occurs during the
initial 2–8 wk of therapy and is more
frequent in patients taking multiple
antiepileptic agents, especially valproic
acid, and much more frequent in
patients _16 yrs..
 Monitor for signs and symptoms of
multiorgan hypersensitivity reactions
(rash, fever, lymphadenopathy) May be
associated with other organ involvement
(hepatitis, hepatic failure, blood
dyscrasias, acute multiorgan failure). If
cause cannot be determined,
discontinue lamotrigine immediately.
Diagnoses:
 Risk for impaired skin integrity (Adverse
Reactions)
 Risk for injury (Side Effects)
Implementation:
 Do not confuse lamotrigine (Lamictal)
with lamivudine (Epivir) or levothyroxine.
 When converting from immediate-
release to XR form, initial dose of XR
should match the total daily dose of
immediate-release lamotrigine; monitor
closely and adjust and needed.
Page | 51
 PO: May be administered without regard
to meals. Swallow XR tablets whole; do
not break, crush, or chew.
Evaluation:
 Decrease in the frequency of or
cessation of seizures.
 Decreased incidence of mood swings in
bipolar disorders.
Drug Classification:
MISCELLANEOUS
ANTICONVULSANTS
Generic Name: Magnesium sulfate
Brand Name: Epsom Salt
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Treatment of Deficiency (Expressed as
mg of Magnesium)
IM, IV (Adults): Severe deficiency—8 12
g/day in divided doses; mild deficiency—1 g
q 6 hr for 4 doses or 250 mg/kg over 4 hr.
IM, IV (Children >1 mo): 25–50 mg/kg/dose
q 4– 6 hr for 3–4 doses, maximum single
dose: 2 g. IV (Neonates): 25–50
mg/kg/dose q 8–12 hr for 2–3 doses.
DRUG ACTION
Essential for the activity of many
enzymes.Plays an important role in
neurotransmission and muscular excitability.
Therapeutic Effects: Replacement in
deficiency states. Resolution of eclampsia.
Pharmacokinetics: Absorption: IV
administration results in complete
bioavailability; well absorbed from IM sites.
Distribution: Widely distributed. Crosses
the placenta and is present in breast milk.
Metabolism and Excretion: Excreted
primarily by the kidneys. Half-life: Unknown.
INTERACTIONS
Drug-drug: May potentiate calcium channel
blockers and neuromuscular blocking
agents.
INDICATION
Treatment/prevention of
hypomagnesaemia.Treatment of
hypertension. Prevention of seizures
associated with severe eclampsia, pre-
eclampsia, or acute nephritis.
Unlabeled Use: Preterm labor. Treatment of
torsade de pointes.Adjunctive treatment for
bronchodilation in moderate to severe acute
asthma.
CONTRAINDICATION
 Hypermagnesemia
 Heart block
 Myocardial damage
 Active labor or within 2 hours of delivery
ADVERSE REACTIONS/ SIDE EFFECT
CNS: drowsiness. Resp: decrease
respiratory rate. CV: arrhythmias,
bradycardia, hypotension. GI: diarrhea. MS:
muscle weakness. Derm: flushing,
sweating. Metab: hypothermia.
NURSING IMPLICATIONS
Assessment
 Hypomagnesemia/Anticonvulsant:
Monitor pulse, BP, respirations, and
ECG frequently throughout
administration of parenteral magnesium
sulfate. Respirations should be at least
16/min before each dose.
 Monitor neurologic status before and
throughout therapy. Institute seizure
precautions. Patellar reflex (knee jerk)
should be tested before each parenteral
dose of magnesium sulfate. If response
is absent, no additional doses should be
administered until positive response is
obtained.
 Monitor newborn for hypotension,
hyporeflexia, and respiratory depression
if mother has received magnesium
sulfate.
 Monitor intake and output ratios. Urine
output should be maintained at a level of
at least 100 mL/4 hr.
Diagnoses
 Risk for injury (Indications, Side Effects)
Implementation:
 High Alert: Accidental overdosage of IV
magnesium has resulted in serious
patient harm and death. Have second
practitioner independently doublecheck
original order, dose calculations, and
infusion pump settings. Do not confuse
milligram (mg), gram (g), or
millequivalent (mEq) dosages.
 IM: Administer deep IM into gluteal sites.
Administer subsequent injections in
alternate sides. Dilute to a concentration
of 200 mg/mL prior to injection.
Evaluation:
 Normal serum magnesium
concentrations.
 Control of seizures associated with
toxemias of pregnancy.
D. DRUGS FOR PARKINSONISM
Page | 52

Drug Classification: ANTICHOLINERGICS
Generic Name: Benztropine
Brand Name: Cogentin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Parkinsonism
Adult: PO/IM 0.5–1 mg/day, may gradually
increase if needed up to 6 mg/day
Extrapyramidal Reactions
Adult: PO/IM/IV 1–4 mg once or twice daily
Child (3 y and older): PO/IM/IV 0.02–0.05
mg/kg/dose once or twice daily
Acute Dystonia
Adult: IV 1–2 mg daily
DRUG ACTION
Blocks cholinergic activity in the CNS, which
is partially responsible for the symptoms of
Parkinson’s disease. It restores the natural
balance of neurotransmitters in the CNS.
Therapeutic Effects: Reduction of rigidity
and tremors.
Pharmacokinetics: Absorption: Well
absorbed following PO and IM
administration. Onset: 15 min IM/IV; 1 h PO.
Duration: 6–10 h.
INTERACTIONS
Drug-drug: Additive anticholinergic effects
with drugs sharing anticholinergic properties,
such as antihistamines, phenothiazines,
quinidine, disopyramide, and tricyclic
antidepressants. It counteracts the
cholinergic effects of bethanechol, antacids
and antidiarrheals may decrease absorption.
Drug-natural products: Increase
anticholinergic effect with angel’s trumpet,
jimson weed, and scopolia.
INDICATION
Adjunctive treatment of all forms of
Parkinson’s disease, including drug-induced
extrapyramidal effects and acute dystonic
reactions.
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Children < 3 yrs.; Angle-closure glaucoma;
Tardive dyskinesia.
Use Cautiously in: Prostatic hyperplasia;
Seizure disorders; Cardiac arrhythmias; OB,
Lactation: Safety not established; Geri:
increase risk of adverse reactions.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: confusion, depression, dizziness,
hallucinations, headache, sedation,
weakness. EENT: blurred vision, dry eyes,
mydriasis. CV: arrhythmias, hypotension,
palpitations, tachycardia. GI: constipation,
dry mouth, ileus, nausea. GU: hesitancy,
urinary retention. Misc: decreased sweating.
NURSING IMPLICATIONS
Assessment
 Assess parkinsonian and
extrapyramidal symptoms (restlessness
or desire to keep moving, rigidity,
tremors, pill rolling, masklike face,
shuffling gait, muscle spasms, twisting
motions, difficulty speaking or
swallowing, loss of balance control)
before and throughout therapy.
 Assess bowel function daily. Monitor for
constipation, abdominal pain,
distention, or absence of bowel sounds.
Monitor intake and output ratios and
assess patient for urinary retention
(dysuria, distended abdomen,
infrequent voiding of small amounts,
overflow incontinence).
 Patients with mental illness are at risk
of developing exaggerated symptoms
of their disorder during early therapy
with benztropine. Withhold drug and
notify physician or other health care
professional if significant behavioral
changes occur.
 IM/IV: Monitor pulse and BP closely
and maintain bed rest for 1 hrs. after
administration. Advise patients to
change positions slowly to minimize
orthostatic hypotension.
Diagnoses
 Impaired physical mobility (Indications)
 Risk for injury (Indications)
Implementation:
 PO: Administer with food or
immediately after meals to minimize
gastric irritation. May be crushed and
administered with food if patient has
difficulty swallowing.
 IM: Parenteral route is used only for
dystonic reactions.
Evaluation:
 Decrease in tremors and rigidity and an
improvement in gait and balance.
Therapeutic effects are usually seen 2–
3 days after the initiation of therapy.
Drug Classification: Dopaminergics
Generic Name: Levodopa, Carbidopa-
Levodopa
Brand Name: L-dopa, Sinemet
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Parkinson’s disease in Patients
Not Currently Receiving Levodopa
Adult: PO 1 tablet containing 10 mg
carbidopa/100 mg levodopa or 25 mg
carbidopa/100 mg levodopa t.i.d., increased
by 1 tablet daily or every other day up to 6
tablets/day
Patients Receiving Levodopa
Adult: PO 1 tablet of the 25/250 mixture t.i.d.
or q.i.d., adjusted by ½–1 tablet as needed
Page | 53
up to 8 tablets/day (start at 20–25% of initial
dose of levodopa)
DRUG ACTION
Levodopa is converted to dopamine in the
CNS, where it serves as a neurotransmitter.
Carbidopa, a decarboxylase inhibitor,
prevents peripheral destruction of levodopa.
Therapeutic Effects: Relief of tremor and
rigidity in Parkinson’s syndrome.
Pharmacokinetics: Absorption: Well
absorbed following oral administration.
Distribution: Widely distributed.
Levodopa—enters the CNS in small
concentrations. Carbidopa— does not cross
the blood-brain barrier but does cross the
placenta. Both enter breast milk.
Metabolism and Excretion: Levodopa
mostly metabolized by the GI tract and liver.
Carbidopa— 30% excreted unchanged by
the kidneys. Half-life: Levodopa—1 hr;
Carbidopa—1–2 hr.
INTERACTIONS
Drug-drug: Use with MAO inhibitors may
result in hypertensive reactions. Increase
risk of arrhythmias with inhalation
hydrocarbon anesthetics (especially
halothane; if possible discontinue 6–8 hr
before anesthesia). Phenothiazines,
haloperidol, papaverine, phenytoin, and
reserpine may decrease effect of levodopa.
Large doses of pyridoxine may decrease
beneficial effects of levodopa. Concurrent
use with methyldopa may alter the
effectiveness of levodopa and increase risk
of CNS side effects. Increase hypotension
may result with concurrent
antihypertensives. Anticholinergics may
decrease absorption of levodopa. Increase
risk of adverse reactions with selegilene or
cocaine.
Drug-Food: Ingestion of foods containing
large amounts of pyridoxine may decrease
effect of levodopa.
INDICATION
Parkinson’s disease. Not useful for drug-
induced extrapyramidal reactions.
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Angle-closure glaucoma; MAO inhibitor
therapy; Malignant melanoma; Undiagnosed
skin lesions; some products contain
tartrazine, phenylalanine, or aspartame and
should be avoided in patients with known
hypersensitivity.
Use cautiously in: History of cardiac,
psychiatric, or ulcer disease; OB, Pedi:
Safety not established; Lactation: may
decrease serum prolactin.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: involuntary movements, anxiety,
dizziness, hallucinations, memory loss,
psychiatric problems, urges (gambling,
sexual). EENT: blurred vision, mydriasis.
GI: nausea, vomiting, anorexia, dry mouth,
hepatotoxicity. Derm: melanoma. Hemat:
hemolytic anemia, leukopenia. Misc:
darkening of urine or sweat.
NURSING INTERVENTIONS
Assessment
 Assess parkinsonian symptoms
(akinesia, rigidity, tremors, pill rolling,
shuffling gait, mask-like face, twisting
motions, and drooling) during therapy.
“On-off phenomenon” may cause
symptoms to appear or improve
suddenly.
 Assess BP and pulse frequently during
period of dose adjustment.
 May cause increase serum glucose.
Dipstick for urine ketones may reveal
false-positive results.
 Monitor hepatic and renal function and
CBC periodically in patients on long-
term therapy. May cause increase in
AST, ALT, bilirubin, alkaline
phosphatase, LDH, and serum protein-
bound iodine concentrations. May cause
decrease in BUN, creatinine, and uric
acid.
 May cause decrease in hemoglobin,
decrease in hematocrit, agranulocytosis,
hemolytic and nonhemolytic anemia,
thrombocytopenia, leukopenia, and
increase WBC.
 Toxicity and Overdose: Assess for signs
of toxicity (involuntary muscle twitching,
facial grimacing, spasmodic eye
winking, exaggerated protrusion of
tongue, behavioral changes). Consult
healthcare professional if symptoms
occur.
Diagnoses
 Impaired physical mobility (Indications)
 Risk for injury (Indications)
Implementation:
 In the carbidopa/levodopa combination,
the number following the drug name
represents the milligrams of each
respective drug.
 In preoperative patients or patients who
are NPO, confer with health care
professional about continuing
medication administration.
 PO:Administer on a regular schedule.
Hospitalized patients should be
continued on same schedule as at
home. Administer while awake, not
around the clock to improve sleep and
prevent side effects.
 Controlled-release tablets may be
administered as whole or half tablets,
but they should not be crushed or
chewed.
 For orally disintegrating tablets, just prior
to administration remove tablet from
bottle with dryhands. Immediately place
tablet on top of tongue.Tablet will
dissolve in seconds, then swallow
Page | 54
 withsaliva. Administration with liquid is
not necessary.
Evaluation:
 Resolution of parkinsonian signs and
symptoms. Therapeutic effects usually
become evident after 2–3 wk of therapy
but may require up to 6 mo. Patients
who take this medication for several yr
may experience a decrease in the
effectiveness of this drug.
Drug Classification: DOPAMINE
AGONISTS
Generic Name: Pramipexole
Dihydrochloride
Brand Name: Mirapex
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Parkinson’s disease
Adult: PO Immediate release:Start with
0.125 mg t.i.d. gradually increase every 5–7
days to a maximum dose of 1.5 mg t.i.d.
Extended release: 0.375 mg PO daily may
increase after 5 days up to a maximum of
4.5 mg/day.
Restless Legs Syndrome
Adult: PO 0.125 mg taken 2–3 h before bed;
dose can be increased every 4–7 days
Renal Impairment Dosage
Adjustment:CrCl35–60 mL/min: Same
titration schedule dosed b.i.d. (max: 1.5 mg
b.i.d.); 15–35 mL/ min: Same titration
schedule dosed daily (max: 1.5 mg daily)
DRUG ACTION
Stimulates dopamine receptors in the
striatum of the brain.
Therapeutic Effects:Decreased tremor and
rigidity in Parkinson’s disease. Decreased
leg restlessness.
Pharmacokinetics: Absorption: >90%
absorbed following oral administration.
Distribution: Widely distributed.
Metabolism and Excretion: 90% excreted
unchanged in urine. Half-life: 8 hr (increase
in geriatric patients and patients with renal
impairment).
INTERACTIONS
Drug-drug: Concurrent levodopa increase
risk of hallucinations and dyskinesia.
Effectiveness may be increase by
cimetidine. Effectiveness may be decrease
by dopamine antagonists, including
butyrophenones, metoclopramide,
phenothiazines, or thioxanthenes.
Drug-Food: All foods delay peak drug
plasma levels by 1 hr (extent of absorption
not affected).
INDICATION
Management of Parkinson’s
disease.Restless leg syndrome (immediate-
release only).
CONTRAINDICATION
Contraindicated in: Hypersensitivity
Use cautiously in: Renal impairment
(increase dosing interval recommended if
CCr <60 mL/min [immediate release] or CCr
<50 mL/min [extended-release]); OB,
Lactation, Pedi: Safety not established;
Geri: increase risk of hallucinations.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: Sleep attacks, amnesia, dizziness,
drowsiness, hallucinations, weakness,
abnormal dreams, confusion, dyskinesia,
extrapyramidal syndrome, headache,
insomnia, urges (gambling, sexual). CV:
orthostatic hypotension. Derm: melanoma,
pruritis. Endo: SIADH. GI: constipation, dry
mouth, dyspepsia, nausea, tooth disease.
GU: urinary frequency. MS: leg cramps.
Neuro: hypertonia, unsteadiness/falling.
NURSING INTERVENTIONS
Assessment
 Assess patient for confusion or
hallucinations. Notify health care
professional if these occur.
 Assess patient for drowsiness and sleep
attacks. Drowsiness is a common side
effect of pramipexole, but sleep attacks
or episodes of falling asleep during
activities that require active participation
may occur without warning. Assess
patient for concomitant medications that
have sedating effects or may increase
serum pramipexole levels
 Parkinson’s Disease:Assess patient for
signs and symptoms of Parkinson’s
disease (tremor, muscle weakness and
rigidity, ataxia) before and throughout
therapy.
 Restless Leg Syndrome:Assess sleep
patterns and frequency of restless leg
disturbances.
Diagnoses
 Impaired physical mobility (Indications)
 Risk for injury (Indications, Side Effects)
Implementation:
 Do not confuse Mirapex (pramipexole)
with Miralax (polyethylene glycol).
 An attempt to reduce the dose of
levodopa/carbidopa may be made
cautiously during pramipexole therapy.
 PO:Administer with meals to minimize
nausea; usually resolves with continued
therapy. Swallow extended-release
tablets whole; do not crush, break, or
chew.
Evaluation:
 Decreased tremor and rigidity in
Parkinson’s disease.
 Decrease in restless legs and improved
sleep.
Page | 55
Drug Classification: MAO-B
INHIBITORS
Generic Name: Seligiline
Hydrochloride
Brand Name: Eldepryl
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 5 mg twice daily, with
breakfast and lunch (some patients may
require further dividing of doses—2.5 mg 4
times daily).
PO (Adults): Orally disintegrating tablets—
1.25 mg once daily for at least 6 wk. After 6
wk, may increase to 2.5 mg if effect not
achieved and patient is tolerating
medication.
DRUG ACTION
Following conversion by MAO to its active
form, selegiline inactivates MAO by
irreversibly binding to it at type B (brain)
sites. Inactivation of MAO leads to increased
amounts of dopamine available in the CNS.
Pharmacokinetics: Absorption: Appears
to be well absorbed following oral
administration.
Distribution: Widely distributed.
Metabolism and Excretion: Metabolism
involves some conversion to amphetamine
and methamphetamine. 45% excreted in
urine as metabolites.
Half-life: Unknown; orally disintegrating
tablets 1.3 hr
INTERACTIONS
Drug-Drug: Severe adverse effects to
fatalities if combined with meperidine,
fluoxetine: Avoid these combinations; Use
extreme caution with opioid analgesics;
Concurrent use of carbamazepine,
oxcarbazepine is contraindicated
Drug-food: Avoid tyramine-rich foods and
beverages starting on first day of therapy
with 9- or 12-mg patch; continue to avoid for
2 wk after reduction to 6-mg patch or
discontinuation of 9- or 12-mg patch
INDICATION
Management of Parkinson’s disease (with
levodopa or levodopa/carbidopa) in patients
who fail to respond to levodopa/carbidopa
alone.
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Concurrent meperidine or opioid analgesic
therapy (possible fatal reactions);
Concurrent use of SSRIs or tricyclic
antidepressants.
Use Cautiously in: Doses >10 mg/day
(increased risk of hypertensive reactions
with tyramine-containing foods and some
medications); History of peptic ulcer
disease.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: confusion, dizziness, fainting,
hallucinations, insomnia, urges (gambling,
sexual), vivid dreams. Derm: melanoma. GI:
nausea, abdominal pain, dry mouth.
NURSING INTERVENTIONS
Assessment
 Assess patient for signs and symptoms
of Parkinson’s disease (tremor, muscle
weakness and rigidity, ataxic gait) prior
to and during therapy.
 Assess BP periodically during therapy.
Diagnoses
 Impaired physical mobility (Indications)
 Risk for injury (Indications, Side Effects)
Implementation:
 An attempt to reduce the dose of
levodopa/carbidopa by 10–30% may be
made after 2–3 days of selegiline
therapy.
 PO:Administer 5-mg tablet with
breakfast and lunch.
 Administer orally disintegrating tablets in
the morning, before breakfast and
without liquid. Remove tablet gently from
blister pack with clean, dry hands
immediately before administering. Do
not attempt to push tablet through
backing. Tablet will disintegrate within
seconds when placed on tongue. Avoid
food or liquid within 5 min of
administering orally disintegrating
tablets.
Evaluation:
 Improved response to
levodopa/carbidopa in patients with
Parkinson’s disease.
Drug Classification: COMT Inhibitors
Generic Name: Entacapone
Brand Name: Comtan
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 200 mg with each dose of
levodopa/carbidopa up to a maximum of 8
times daily.
DRUG ACTION
Acts as a selective and reversible inhibitor of
the enzyme catechol O-methyltransferase
(COMT). Inhibition of this enzyme prevents
the breakdown of levodopa, increasing
availability to the CNS.
Therapeutic Effects: Prolongs duration of
response to levodopawith end-of-dose motor
fluctuations. Decreased signsand symptoms
of Parkinson’s disease.
Pharmacokinetics: Absorption: 35%
absorbed following oral administration;
absorption is rapid.
Distribution: Unknown.
Protein Binding: 98%.
Page | 56
Metabolism and Excretion: Minimal
amounts excreted unchanged; highly
metabolized followed by biliary excretion.
Half-life: Initial phase—0.4–0.7 hr; second
phase—2.4 hr.
INTERACTIONS
Drug-drug: Extreme caution must be used if
administered with a nonselective MAOI;
bitolterol, dobutamine,
dopamine,epinephrine,
isoetharine,isoproterenol, methyldopa,
norepinephrine may increase heart rates;
possibly cause arrhythmias, excessive
changes in BP.
INDICATION
With levodopa/carbidopa to treat idiopathic
Parkinson’s disease when signs and
symptoms of end-of-dose “wearing-off” (so-
called fluctuating patients) occur.
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Concurrent nonselective MAO inhibitor
therapy.
Use Cautiously in: Hepatic impairment;
Concurrent use of drugs that are
metabolized by COMT; OB, Lactation:
Safety not established; Pedi: No identified
use in children.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: Neuroleptic Malignant Syndrome,
Dizziness, Hallucinations, Syncope, Urges
(Gambling, Sexual). RESP: Pulmonary
Infiltrates, Pleural Effusion, Pleural
Thickening. CV: Hypotension. DERM:
Melanoma. GI: Abdominal Pain, Colitis,
Diarrhea, Nausea (During Initiation),
Retroperitoneal Fibrosis. GU: Brownish-
Orange Discoloration Of Urine. MS:
Rhabdomyolysis. NEURO: Dyskinesia.
NURSING IMPLICATIONS
Assessment
 Assess parkinsonian and extrapyramidal
symptoms (restlessness or desire to
keep moving, rigidity, tremors, pill
rolling, mask-like face, shuffling gait,
muscle spasms, twisting motions,
difficulty speaking or swallowing, loss of
balance control) prior to and during
therapy. Dyskinesia may increase with
therapy.
 Monitor patient for development of
diarrhea. Usually occurs within 4 to 12
wk of start of therapy, but may occur as
early as the first week and as late as
months after initiation of therapy.
 Monitor patient for signs similar to
neuroleptic malignant syndrome
(elevated temperature, muscular rigidity,
altered consciousness, elevated CPK).
Diagnoses
 Impaired physical mobility (Indications)
 Risk for injury (Indications)
Implementation:
 PO:Always administer entacapone with
levodopa/carbidopa. Entacapone has no
antiparkinsonism effects of its own.
Evaluation:
 Decreased signs and symptoms of
Parkinson’s disease.
E. DRUGS FOR ALZHEIMER’S
DISEASE
Drug Classification:
ACETYCHOLINESTERASE
INHIBITORS
Generic Name: Donepezil
Brand Name: Aricept
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Mild to Moderate Alzheimer’s Disease
PO (Adults): 5 mg once daily; after 4–6 wk
may increase to 10 mg once daily (dose
should not exceed 5 mg/day in frail, elderly
females).
Severe Alzheimer’s Disease
PO (Adults): 5 mg once daily; may increase
to 10 mg once daily after 4–6 wk; after 3 mo,
may then increase to 23 mg once daily.
DRUG ACTION
Inhibits acetylcholinesterase thus improving
cholinergic function by making more
acetylcholine available.
Therapeutic Effects: May temporarily
lessen some of the dementia associated
with Alzheimer’s disease. Enhances
cognition.Does not cure the disease.
Pharmacokinetics: Absorption: Well
absorbed after oral administration.
Distribution: Unknown. Protein Binding:
96%. Metabolism and Excretion: Partially
metabolized by the liver (CYP2D6 and
CYP3A4 enyzmes) and partially excreted by
kidneys (17% unchanged). Two metabolites
are pharmacologically active.
Half-life: 70 hr.
INTERACTIONS
Drug-drug: Exaggerates muscle relaxation
from succinylcholine. Interferes with the
action of anticholinergics. Increase
cholinergic effects of bethanechol. May
increase risk of GI bleeding from NSAIDs.
Quinidine and ketoconazole decrease
metabolism of donepezil. Rifampin,
carbamazepine, dexamethasone,
phenobarbital, and phenytoin induce the
enzymes that metabolize donepezil and may
decrease its effects.
INDICATION
Mild, moderate, or severe dementia/
neurocognitive disorder associated with
Alzheimer’s disease.
Page | 57

CONTRAINDICATION
Contraindicated in: Hypersensitivity to
donepezil or piperidine derivatives.
Use Cautiously in: Underlying cardiac
disease, especially sick sinus syndrome or
supraventricular conduction defects; History
of ulcer disease or currently taking NSAIDs;
History of seizures; History of asthma or
obstructive pulmonary disease; OB,
Lactation, Pedi: Safety not established;
assumed to be secreted in breast milk.
Discontinue drug or bottle-feed.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: headache, abnormal dreams,
depression, dizziness, drowsiness, fatigue,
insomnia, syncope, sedation (unusual). CV:
atrial fibrillation, hypertension, hypotension,
vasodilation. GI: diarrhea, nausea, anorexia,
vomiting, weight gain (unusual). GU:
frequent urination. Derm: ecchymoses.
Metab: hot flashes, weight loss. MS:
arthritis, muscle cramps.
NURSING IMPLICATIONS
Assessment
 Assess cognitive function (memory,
attention, reasoning, language, ability to
perform simple tasks) periodically during
therapy.
 Monitor heart rate periodically during
therapy. May cause bradycardia.
Diagnoses
 Disturbed thought process (Indications)
 Impaired environmental interpretation
syndrome (Indications)
 Risk for injury (Indications)
Implementation:
 PO: Administer in the evening just
before going to bed. May be taken
without regard to food.
 Oral disintegrating tablets should be
allowed to dissolve on tongue; follow
with water.
 Swallow 23 mg tablet whole. Do not
split, crush, or chew; may increase rate
of absorption.
Evaluation:
 Improvement in cognitive function
(memory, attention, reasoning,
language, ability to perform simple
tasks) in patients with Alzheimer’s
disease.
F. DRUGS FOR MYASTHENIA GRAVIS
Drug Classification:
ACETYLCHOLINESTERASE INHIBITORS
Generic Name: Pyridostigmine
Brand Name: Mestinon
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Myasthenia Gravis
PO (Adults): Tablets/syrup—30–60mg q 3–
4 hr initially; then adjusted as required; usual
maintenance dose is 600 mg/day in divided
doses (range 60–1500 mg/day). Extended-
release tablets—180–540 mg 1–2 times
daily (dosing interval should be at least 6 hr;
may be associated with increased risk of
cholinergic crisis; concurrent immediate
release products may be required).
PO (Children): 7 mg/kg (200 mg/m2)/day in
5–6 divided doses.
IM, IV (Adults): 2 mg (1/30 of oral dose);
may be repeated q 2–3 hr. During
labor/delivery—1 mg before second stage of
labor is complete.
IM (Neonates Born to Myasthenic
Mothers): 50– 150 mcg/kg q 4–6 hr.
Antidote for Nondepolarizing
Neuromuscular Blocking Agents
IV (Adults): 10–20 mg; pretreat with 0.6–1.2
mg atropine IV.
Prevention of Soman Nerve Gas Effects
PO (Adults): 30 mg every 8 hr before
exposure, stopped on exposure to gas.
DRUG ACTION
Inhibits the breakdown of acetylcholine and
prolongs its effects (anticholinesterase).
Effects include: Miosis, Increased intestinal
and skeletal muscle tone, Bronchial and
ureteral constriction, Bradycardia, Increased
salivation, Lacrimation, Sweating.
Pharmacokinetics: Absorption: Poorly
absorbed after oral administration,
necessitating large oral doses compared
with parenteral doses. Distribution:
Appears to cross the placenta. Metabolism
and Excretion: Metabolized by plasma
cholinesterases and the liver. Half-life:
PO—3.7 hr; IV—1.9 hr.
Therapeutic Effects: Improved muscular
function inpatients with myasthenia gravis.
Reversal of paralysisfrom nondepolarizing
neuromuscular blocking agents.Prevention
of Soman nerve gas toxicity.
INTERACTIONS
Drug-Drug: Cholinergic effects may be
antagonized by other drugs possessing
anticholinergic properties, including
antihistamines, antidepressants, atropine,
haloperidol, phenothiazines, procainamide,
quinidine, or disopyramide. Prolongs the
action of depolarizing muscle-relaxing
agents and cholinesterase inhibitors
(succinylcholine, decamethonium). Increase
toxicity with other cholinesteraseinhibitors,
including echothiophate.
INDICATION
Used to increase muscle strength in the
symptomatic treatment of myasthenia
gravis. Reversal of nondepolarizing
neuromuscular blocking agents.Prophylaxis
of lethal effects of poisoning with the nerve
agent soman.
CONTRAINDICATION
Page | 58
Contraindicated in: Hypersensitivity to
pyridostigmine or bromides; Mechanical
obstruction of the GI or GU tract; Known
alcohol intolerance (syrup only).
Use Cautiously in: History of asthma; Ulcer
disease; Cardiovascular disease; Epilepsy;
Hyperthyroidism; OB: May cause uterine
irritability after IV administration near term;
20% of newborns display transient muscle
weakness; Lactation: Pedi: Safety not
established.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: Seizures, dizziness, weakness.
EENT: lacrimation, miosis. Resp:
bronchospasm, excessive secretions. CV:
bradycardia, hypotension. GI: abdominal
cramps, diarrhea, excessive salivation,
nausea, vomiting. Derm: sweating, rashes.
NURSING IMPLICATIONS
Assessment
 Assess pulse, respiratory rate, and BP
before administration. Report significant
changes in heart rate.
 Myasthenia Gravis:Assess
neuromuscular status, including vital
capacity, ptosis, diplopia, chewing,
swallowing, hand grasp, and gait before
administering and at peak effect.
Patients with myasthenia gravis may be
advised to keep a daily record of their
condition and the effects of this
medication.
 Assess patient for overdose, underdose,
or resistance. Both have similar
symptoms (muscle weakness, dyspnea,
dysphagia), but symptoms of
overdosage usually occur within 1 hr of
administration, whereas symptoms of
underdose occur >=3 hr after
administration. Overdose (cholinergic
crisis) symptoms may also include
increased respiratory secretions and
saliva, bradycardia, nausea, vomiting,
cramping, diarrhea, and diaphoresis. A
Tensilon test (edrophonium chloride)
may be used to differentiate between
overdosage and underdosage.
Diagnoses
 Impaired physical mobility (Indications)
 Ineffective breathing pattern
(Indications)
Implementation:
 For patients who have difficulty chewing,
pyridostigmine may be administered 30
min before meals.
 Oral dose is not interchangeable with IV
dose. Parenteral form is 30 times more
potent.
 When used as an antidote to
nondepolarizing neuromuscular blocking
agents, atropine may be ordered before
or currently with large doses of
pyridostigmine to prevent or to treat
bradycardia and other side effects.
 PO: Administer with food or milk to
minimize side effects. Extended-release
tablets should be swallowed whole; do
not crush, break, or chew. Regular
tablets or syrup may be administered
with extended- release tablets for
optimum control of symptoms. Mottled
appearance of sustained-release tablet
does not affect potency.
Evaluation:
 Relief of ptosis and diplopia; improved
chewing, swallowing, extremity strength,
and breathing without the appearance of
cholinergic symptoms.
 Reversal of nondepolarizing
neuromuscular blocking agents in
general anesthesia.
 Prevention of Soman nerve gas toxicity.
Drug Classification: Acute Attack Phase
Generic Name: Corticotropin
Brand Name: Acthar Gel
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Adults
 Therapy: 40–80 units IM or
subcutaneously every 24–72 hr; when
indicated, gradually reduce dosage by
increasing intervals between injections
or decreasing the dose injected, or both.
 Acute exacerbations of MS: 80–120
units/ day IM for 2–3 wk.
Pediatric patients
 Use only if necessary, and only
intermittently and with careful
observation. Prolonged use will inhibit
skeletal growth.
 Infantile spasms: 20–40 units/day or 80
units every other day IM for 3 mo or 1
mo after cessation of seizures.
DRUG ACTION
Normally produced by the pituitary,
stimulates the adrenal gland to produce both
corticosteroids (hydrocortisone) and
mineralocorticoids (aldosterone). Action
requires intact adrenal responsiveness.
Actions resemble those of corticosteroid
administration and include suppression of
the normal immune response and
inflammation. Additional numerous intense
metabolic effects.Potent mineralocorticoid
(sodium retention).Suppresses adrenal
function with chronic use. Mechanism of
anticonvulsant action is unknown.
Therapeutic Effects: Reduction in
frequency of multiple sclerosis
exacerbations. Suppression of spasm.
Pharmacokinetics: Metabolism: T1/2: 15
min Distribution: Does not cross placenta;
may enter breast milk
Page | 59
Duration: 2-4hr
INTERACTIONS
Drug-drug: Decreased effects with
barbiturates; Decreased effects of
anticholinesterases with corticotropin;
profound muscular depression is possible;
Decreased effectiveness of insulin,
antidiabetics; monitor patient closely and
increase dosage as needed
Drug-Natural Products: Additive
hypokalemia with licorice.
INDICATION
Allergic states unresponsive to conventional
treatments; Therapy of some glucocorticoid-
sensitive disorders; Nonsuppurative
thyroiditis; Hypercalcemia associated with
cancer; Acute exacerbations of MS;
Tuberculous meningitis with subarachnoid
block; Trichinosis with neurologic or
myocardial involvement; Rheumatic,
collagen, dermatologic, allergic,
ophthalmologic, respiratory, hematologic,
edematous, and GI diseases, Palliative
management of leukemias, lymphomas
Unlabeled use: Treatment of infantile
spasms.
CONTRAINDICATION
Contraindicated with adrenocortical
insufficiency or hyperfunction; infections,
especially systemic fungal infections, ocular
herpes simplex; scleroderma, osteoporosis;
recent surgery; heart failure, hypertension;
allergy to pork or pork products
(corticotropin is isolated from porcine
pituitaries); liver disease; ulcerative colitis
with impending perforation; recent GI
surgery; active or latent peptic ulcer;
inflammatory bowel disease;
hypothyroidism; pregnancy, lactation.
Use cautiously with mental disturbances,
diabetes, diverticulitis, renal impairment,
myasthenia gravis.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: Seizures, vertigo, headaches,
pseudotumor cerebri, euphoria, insomnia,
mood swings, depression, psychosis,
intracerebralhemorrhage, reversible cerebral
atrophy ininfants, cataracts, increased IOP,
glaucoma; CV: Hypertension, heart failure,
necrotizingangiitis; Endocrine: Growth
retardation, decreasedcarbohydrate
tolerance, diabetes mellitus,cushingoid
state, secondary adrenocortical and pituitary
unresponsiveness; GI: Peptic or esophageal
ulcer, pancreatitis,abdominal distention;GU:
Amenorrhea, irregular menses;
Hematologic: Fluid and electrolyte
disturbances,negative nitrogen balance;
Hypersensitivity:
Anaphylactoidorhypersensitivity reactions;
Musculoskeletal: Muscle weakness,steroid
myopathy, loss of muscle mass,
osteoporosis,spontaneous fractures.
NURSING IMPLICATIONS
Assessment
 Monitor BP and daily weight periodically
during therapy. If hypertension develops
during treatment, sodium restriction and
diuretic therapy are used instead of
discontinuation of corticotropin.
 Assess for signs and symptoms of
infection (fever, cough, vomiting,
diarrhea) of patient and family members
throughout therapy.
 Lab Test Considerations: Monitor CBC,
serum calcium, electrolytes,
phosphorus, serum fasting and
postprandial glucose, and renal function
tests with urinalysis before initiation of
therapy. Use caution if results are
abnormal.
 Monitor serum calcium, electrolytes, and
phosphorus, and urinalysis with urine
glucose periodically during therapy.
Diagnoses
 Deficient knowledge, related to
medication regimen (Patient/Family
Teaching)
Implementation
 IM: Shake suspension well before
drawing up dose. Refrigerate. Warm to
room temperature before administering.
Use 22-gauge needle. Administer deep
IM; massage well. Rotate sites. Inform
patient that injection is painful.
Evaluation
 Reduction in frequency of exacerbations
with multiple sclerosis
G. DRUGS FOR MULTIPLE SCLEROSIS
Drug Classification: STEROIDS
Generic Name: Methylprednisolone
Brand Name: Medrol
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Adult: PO 2–60 mg/day in 1 or more divided
doses IM (Acetate) 10–80 mg/wk;
(Succinate) 10–80 mg daily IV 10–40 mg prn
or 30 mg/kg q4–6h × 48 h
Child: PO/IM/IV 0.5–1.7 mg/ kg/day divided
q6–12h
Status Asthmaticus
Adult/Child: IV 2 mg/kg then 1–5 mg/kg qh
Acute Spinal Cord Injury
Adult/Child: IV 30 mg/kg over 15 min,
followed in 45 min by 5.4 mg/kg/h × 23 h
DRUG ACTION
Page | 60
Intermediate-acting synthetic adrenal
corticosteroid with glucocorticoid activity. It
inhibits phagocytosis, and release of allergic
substances. It also modifies the immune
response of the body to various stimuli.
Sodium succinate form is characterized by
rapid onset of action and is used for
emergency therapy of short duration and
has anti-inflammatory and
immunosuppressive properties.
Therapeutic Effects: Suppression of
inflammation and modification of the normal
immune response. Replacement therapy in
adrenal insufficiency.
Absorption: Readily absorbed from GItract.
Peak: 1–2 h PO; 4–8 days IM.
Duration: 1.25–1.5 days PO; 1–5 wk IM.
Metabolism: In liver.
Half-Life: Greater than 3.5 h; HPA
suppression:18–36 h.
INTERACTIONS
Drug-drug: Amphotericin B, Furosemide,
ThiazideDiuretics increase potassium
loss;with attenuated virus vaccines,may
enhance virus replication orincrease vaccine
adverse effects; Isoniazid, Phenytoin,
Phenobarbital, Rifampin decrease
effectivenessof Methylprednisolonebecause
they increase metabolismof steroids.
INDICATION
Short-term management of various
inflammatory and allergic disorders, such as
rheumatoid arthritis, collagen diseases (eg,
SLE), dermatologic diseases (eg,
pemphigus), status asthmaticus, and
autoimmune disorders (eg, MS).
Hematologic disorders: Thrombocytopenia
purpura, erythroblastopenia; Ulcerative
colitis, acute exacerbations of MS, and
palliation in some leukemias and
lymphomas; Trichinosis with neurologic or
myocardial involvement; Prevention of
nausea and vomiting associated with
chemotherapy.
CONTRAINDICATION
Contraindicated in: Active untreated
infections (may be used in patients being
treated for some forms of meningitis);
Lactation: Avoid chronic use; Known
alcohol, bisulfite, or tartrazine
hypersensitivity or intolerance (some
products contain these and should be
avoided in susceptible patients);
Administration of live virus vaccines.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: depression, euphoria, headache,
increase intracranial pressure (children
only), personality changes, psychoses,
restlessness. EENT: cataracts, increase
intraocular pressure. CV: hypertension. GI:
Peptic Ulceration, anorexia, nausea,
vomiting. Derm: acne, decrease wound
healing, ecchymoses, fragility, hirsutism,
petechiae. Endo: adrenal suppression,
hyperglycemia. F andE: fluid retention (long-
term high doses), hypokalemia, hypokalemic
alkalosis. Hemat: Thromboembolism,
thrombophlebitis .Metab: weight gain. MS:
muscle wasting, osteoporosis, avascular
necrosis of joints, muscle pain. Misc:
cushingoid appearance (moon face, buffalo
hump), increase susceptibility to infection.
NURSING IMPLICATIONS
Assessment
 This drug is indicated for many
conditions. Assess involved systems
before and periodically during therapy.
 Assess for signs of adrenal insufficiency
(hypotension, weight loss, weakness,
nausea, vomiting, anorexia, lethargy,
confusion, restlessness) before and
periodically during therapy.
 Monitor intake and output ratios and
daily weights.
 Observe patient for peripheral edema,
steady weight gain, rales/crackles, or
dyspnea. Notify health care professional
if these occur.
 Cerebral Edema: Assess for changes in
level of consciousness and headache
during therapy.
Diagnoses
 Risk for infection (Side Effects)
 Disturbed body image (Side Effects)
Implementation:
 Periods of stress, such as surgery, may
require supplemental systemic
corticosteroids.
 Patients with mild to moderate Crohn’s
disease may be switched from oral
prednisolone without adrenal
insufficiency by gradually decreasing
prednisolone doses and adding
budesonide.
 PO: Administer with meals to minimize
GI irritation.
 Tablets may be crushed and
administered with food or fluids for
patients with difficulty swallowing.
Capsules and extended-release tablets
should be swallowed whole; do not
open, crush, crush, break, or chew.
 Use calibrated measuring device to
ensure accurate dose of liquid forms.
 For orally disintegrating tablets (ODT),
remove tablet from blister just prior to
dosing. Peel blister pack open, and
place tablet on tongue; may be
swallowed whole or allowed to dissolve
in mouth, with or without water. Tablets
are friable; do not cut, split, or break.
 Avoid consumption of grapefruit juice
during therapy with budesonide or
methylprednisolone.
Evaluation:
 Decrease in presenting symptoms with
minimal systemic side effects.
 Suppression of the inflammatory and
immune responses in autoimmune
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 disorders, allergic reactions, and
neoplasms.
 Management of symptoms in adrenal
insufficiency.
 Improvement of symptoms/sequelae of
Crohn’s disease and ulcerative colitis
(decreased frequency of liquid stools,
decreased abdominal complaints,
improved sense of well-being).
 Improvement in symptoms of ulcerative
colitis. Clinical symptoms usually
improve in 3–5 days. Mucosal
appearance may require 2–3 mo.
improving.
Drug classification: REMISSION-
EXACERBATION PHASE: BIOLOGIC
RESPONSE MODIFIERS
Generic name: Mitoxantrone
Brand name: Novantrone
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Acute Nonlymphatic Leukemia
IV (Adults): Induction—12 mg/m2/day for 3
days (usually given with cytosine
arabinoside 100 mg/m2/ day for 7 days); if
incomplete remission occurs, a 2ndinduction
may be given. Consolidation—12 mg/m2/
day for 2 days (usually given with cytosine
arabinoside 100 mg/m2/day for 5 days),
given 6 wk after induction with another
course 4 wk later.
Advanced Prostate Cancer
IV (Adults): 12–14 mg/m2 single dose as a
short infusion (with corticosteroids).
Multiple Sclerosis
IV (Adults): 12 mg/m2 q 3 mo.
DRUG ACTION
Inhibits DNA synthesis (cell-cycle phase–
nonspecific).
Therapeutic Effects: Death of rapidly
replicating cells, particularly malignant ones.
Decreased pain in patients with advanced
prostate cancer. Decreased disability
and slowed progression of MS.
Pharmacokinetics: Absorption: IV
administration results in complete
bioavailability.
Distribution: Widely distributed; limited
penetration of CSF. Metabolism and
Excretion: Mostly eliminated by
hepatobiliary clearance; <10% excreted
unchanged by the kidneys. Half-life: 5.8
days.
INTERACTIONS
Drug-drug: Increase bone marrow
depression with other antineoplastics or
radiation therapy. Risk of cardiomyopathy
increase by previous anthracycline
antineoplastics (daunorubicin, doxorubicin,
idarubicin) or mediastinal radiation. May
decrease antibody response to live-virus
vaccines and increase risk of adverse
reactions.
INDICATION
Acute nonlymphocytic leukemia (ANLL) in
adults (with other antineoplastics). Initial
chemotherapy for patients with pain
associated with advanced hormone-
refractory prostate cancer. Secondary
(chronic) progressive, progressive relapsing,
or worsening relapsing-remitting multiple
sclerosis (MS).
CONTRAINDICATION
Contraindicated in: Hypersensitivity; OB,
Lactation: Pregnancy or lactation.
ADVERSE REACTIONS/SIDE EFFECT
CNS: Seizures, headache. EENT: blue-
green sclera, conjunctivitis. Resp: Cough
dyspnea. CV: Cardiotoxicity, arrhythmias,
ECG changes. GI: abdominal pain, diarrhea,
hepatic toxicity, nausea, stomatitis, vomiting.
GU: blue-green urine, gonadal suppression,
renal failure. Derm: alopecia, rashes.
Hemat: anemia, leukopenia, secondary
leukemia, thrombocytopenia. Metab:
hyperuricemia. Misc: fever, hypersensitivity
reactions.
NURSING INTERVENTIONS
Assessment
 Monitor for hypersensitivity reaction
(rash, urticaria, bronchospasm,
tachycardia, and hypotension). If these
occur, stop infusion and notify physician.
 Monitor for bone marrow depression.
Assess for bleeding (bleeding gums,
bruising, petechiae, guaiac stools, urine,
and emesis) and avoid IM injections and
taking rectal temperatures if platelet
count is low.
 Monitor intake and output, appetite, and
nutritional intake. Assess patient for
nausea and vomiting. Antiemetics may
be administered prophylactically. Adjust
diet as tolerated to help maintain fluid
and electrolyte balance and nutritional
status. Monitor for symptoms of gout
(increase in uric acid levels and joint
pain and swelling). Encourage patient to
drink at least 2 L of fluid per day.
Diagnoses
 Risk for injury (Side Effects)
 Risk for infection (Side Effects)
 Disturbed body image (Side Effects)
Implementation:
 Solution should be prepared in a
biologic cabinet. Wear gloves, gown,
and mask while handling medication.
Discard equipment in designated
containers.
 Avoid contact with skin. Use Luer-Lok
tubing to prevent accidental leakage. If
contact with skin occurs, immediately
wash skin with soap and water.
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 Clean all spills with an aqueous solution
of calcium hypochlorite. Mix solution by
adding 5.5 parts (per weight) of calcium
hypochlorite to 13 parts water.
Evaluation:
 Decrease in the production and spread
of leukemic cells.
 Decreased pain in patients with prostate
cancer.
 Decrease in the frequency of relapse
(neurologic dysfunction) in patients with
relapsing-remitting multiple sclerosis.
Drug Classification:
Immunosuppressant
Generic Name: Cyclophosphamide
Brand Name: Cytoxan
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 1–5 mg/kg/day.
PO (Children): Induction—2–8 mg/kg/day
(60– 250 mg/m2/day) in divided doses for 6
days or longer. Maintenance — 2–5 mg/kg
(50–150 mg/m2/day) twice weekly.
IV (Adults): 40–50 mg/kg in divided doses
over 2–5 days or 10–15 mg/kg q 7–10 days
or 3–5 mg/kg twice weekly or 1.5–3
mg/kg/day. Other regimens may use larger
doses.
IV (Children): Induction—2–8 mg/kg/day
(60– 250 mg/m2/day) in divided doses for 6
days or longer. Total dose for 7 days may be
given as a single weekly dose.
Maintenance—10–15 mg/kg every 7–10
days or 30 mg/kg q 3–4 wk.
ACTION
Interferes with DNA replication and RNA
transcription, ultimately disrupting protein
synthesis (cell-cycle phase–nonspecific).
Therapeutic Effects: Death of rapidly
replicating cells, particularly malignant ones.
Also has immunosuppressant action in
smaller doses.
Pharmacokinetics: Absorption: Inactive
parent drug is well absorbed from the GI
tract. It is converted to active drug by the
liver.
Distribution: Widely distributed. Limited
penetration of the blood-brain barrier.
Crosses the placenta; enters breast milk.
Metabolism and Excretion: Converted to
active drug by the liver; 30% eliminated
unchanged by the kidneys.
Half-life: 4–6.5 hr.
INTERACTIONS
Drug-drug: Phenobarbital or rifampin may
increase toxicity of cyclophosphamide.
Concurrent allopurinol or thiazide diuretics
may exaggerate bone marrow depression.
May prolong neuromuscular blockade from
succinylcholine. Cardiotoxicity may be
additive with other cardiotoxic agents (e.g.,
cytarabine, daunorubicin, doxorubicin). May
decrease serum digoxin levels. Additive
bone marrow depression with other
antineoplastics or radiation therapy. May
potentiate the effects of warfarin. May
decrease antibody response to live-virus
vaccines and increase risk of adverse
reactions. Prolongs the effects of cocaine.
INDICATION
Alone or with other modalities in the
management of: Hodgkin’s disease,
Malignant lymphomas, Multiple myeloma,
Leukemias, Mycosis fungoides,
Neuroblastoma, Ovarian carcinoma, Breast
carcinoma, and a variety of other tumors.
Minimal change nephrotic syndrome in
children.
CONTRAINDICATION
Contraindicated in: Hypersensitivity; OB,
Lactation: Pregnancy or lactation.
Use cautiously in: Active infections; Bone
marrow depression; other chronic
debilitating illnesses; OB: Patients with
childbearing potential.
ADVERSE REACTIONS/ SIDE EFFECT
Resp: Pulmonary Fibrosis. Cv: Myocardial
Fibrosis, Hypotension. Gi: Anorexia,
Nausea, Vomiting. Gu: Hemorrhagic
Cystitis, Hematuria. Derm: Alopecia. Endo:
Gonadal Suppression, Syndrome of
Inappropriate Antidiuretic Hormone (Siadh).
Hemat: Leukopenia, Thrombocytopenia,
Anemia. Metab: Hyperuricemia. Misc:
Secondary Neoplasms.
NURSING INTERVENTIONS
Assessment
 Monitor BP, pulse, respiratory rate, and
temperaturefrequently during
administration. Report significant
changes.
 Monitor urinary output frequently during
therapy. To reduce the risk of
hemorrhagic cystitis, fluid intake should
be at least 3000 mL/day for adults and
1000–2000 mL/day for children. May be
administered with mesna.
 Monitor for bone marrow depression.
Assess for bleeding (bleeding gums,
bruising, petechiae, guaiac stools, urine,
and emesis) and avoid IM injections and
taking rectal temperatures if platelet
count is low. Apply pressure to
venipuncture sites for 10 min. Assess for
signs of infection during neutropenia.
Anemia may occur. Monitor for
increased fatigue, dyspnea, and
orthostatic hypotension.
 Assess nausea, vomiting, and appetite.
Weigh weekly. Antiemetics may be
given 30 min before administration of
medication to minimize GI effects.
 Anorexia and weight loss can be
minimized by feeding frequent light
meals. Assess cardiac and respiratory
status for dyspnea,rales/crackles,
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 cough, weight gain, edema. Pulmonary
toxicity may occur after prolonged
therapy. Cardiotoxicity may occur early
in therapy and is characterized by
symptoms of HF.
 Urinalysis should be evaluated before
initiating therapy and frequently during
therapy to detect hematuria or change in
specific gravity indicative ofSIADH.
Diagnoses
 Risk for infection (Side Effects)
 Disturbed body image (Side Effects)
Implementation:
 PO: Administer in the morning. Swallow
tablets whole; do not crush, break, or
chew.
 IV: Prepare solution for IV administration
in a biologic cabinet. Wear gloves,
gown, and mask while handling IV
medication. Discard IV equipment in
specially designated containers.
Evaluation:
 Decrease in size or spread of malignant
tumors.
 Improvement of hematologic status in
patients with leukemia. Maintenance
therapy is instituted if leukocyte count
remains between 2500 and 4000/mm3
and if patient does not demonstrate
serious side effects.
 Management of minimal change
nephrotic syndrome in children.
H. CNETRALLY-ACTING MUSCLE
RELAXANTS
Drug Classification: ANXIOLYTICS
Generic Name: Diazepam
Brand Name: Valium
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Status Epilepticus
Adult:IV/IM 5–10 mg, repeat if needed at
10–15 min intervals up to 30 mg, then
repeat if needed q2–4h
Child (5 y or older): IV 1 mg/kg q2–5min
(max: 10 mg), may repeat in 2–4 h
Child/Infant (1 mo–5 y): IV 0.2–0.5 mg
slowly q2–5min up to5 mg
Neonate: IV 0.1–0.3 mg/kg q15–30min (max
total dose: 2 mg)
Muscle Spasm
Adult/Adolescent/Child (5 y or older):IV
5–10 mg q3–4h prn(larger dose for tetanus)
PO 2–10mg 3–4 × day
Child/Infant (1 mo–5 y): IV 1–2 mg q3–4h
prn
Anxiety
Adult/Adolescent: IV 2–10 mg, repeats if
needed in 3–4 h PO 2–10 mg 2–4 × day
Child/Infant (6 mo or older): IV 0.04–0.3
mg q2–4h (max:0.6 mg/kg/8 h)
Alcohol Withdrawal
Adult:IV 10 mg then 5–10 mg in3–4 h PO
10 mg 3 or 4 × on day1 then 5 mg 3–4 × day
PRN
Preoperative
Adult:IV 5–15 mg 5–10 min before
procedure
DRUG ACTION
Depresses the CNS, probably by
potentiating GABA, an inhibitory
neurotransmitter.Produces skeletal muscle
relaxation by inhibiting spinal polysynaptic
afferent pathways.Has anticonvulsant
properties due to enhanced presynaptic
inhibition.
Therapeutic Effects:
Relief of anxiety.Sedation.Amnesia.Skeletal
muscle relaxation.Decreased seizure
activity.
Pharmacokinetics: Absorption: Readily
from GI tract; erratic IM absorption. Onset:
30–60 min PO; 15–30 min IM; 1–5 min IV.
Peak: 1–2 h PO. Duration: 15 min– 1 h IV;
up to 3 h PO. Distribution: Crosses blood–
brain barrier and placenta; distributed into
breast milk. Metabolism: In liver to active
metabolites. Elimination: Primarily in urine.
Half-Life: 20–50 h.
INTERACTIONS
Drug-drug: Alcohol,antidepressants,
antihistamines, and opioid analgesics—
concurrent use results in additive CNS
depression. Cimetidine,
hormonalcontraceptives, disulfiram,
fluoxetine, isoniazid, ketoconazole,
metoprolol, propranolol, or valproic acid may
decrease the metabolism of diazepam,
enhancing its actions. May decrease the
efficacy of levodopa. Rifampin or
barbiturates may increase the metabolism
an decrease effectiveness of diazepam.
Sedative effects may be decrease by
theophylline. Concurrent use of ritonavir is
not recommended.
Drug-Natural Products: Concomitant use
of kava-kava, valerian, or chamomile
canqCNS depression.
INDICATION
Adjunct in the management of: Anxiety
Disorder, Athetosis, Anxiety relief prior to
cardioversion (injection), Stiffman
Syndrome, Preoperative sedation,
Conscious sedation (provides light
anesthesia and anterograde amnesia).
Treatment of status
epilepticus/uncontrolledseizures
(injection).Skeletal muscle
relaxant.Management of the symptoms of
alcohol withdrawal.
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Cross-sensitivity with other benzodiazepines
may occur; Comatose patients; Myasthenia
gravis; Severe pulmonary impairment;
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Sleep apnea; severe hepatic dysfunction;
Pre-existing CNS depression; Uncontrolled
severe pain; Angle- closure glaucoma;
Some products contain alcohol, propylene
glycol, or tartrazine and should be avoided
in patients with known hypersensitivity or
intolerance; OB: increase risk of congenital
malformations; Pedi: Children <6 mo. (for
oral; safety not established); Lactation:
Recommend to discontinue drug or bottle-
feed.
Use Cautiously in: Severe renal
impairment;
ADVERSE REACTIONS/ SIDE EFFECT
CNS: dizziness, drowsiness, lethargy,
depression, hangover, ataxia, slurred
speech, headache, paradoxical excitation.
EENT: blurred vision. Resp: Respiratory
Depression. CV: hypotension (IV only). GI:
constipation, diarrhea (may be caused by
propylene glycol content in oral solution),
nausea, vomiting, weight gain. Derm:
rashes. Local: pain (IM), phlebitis (IV), and
venous thrombosis. Misc: physical
dependence, psychological dependence,
tolerance.
NURSING INTERVENTIONS
Assessment
 Monitor BP, pulse, and respiratory rate
prior to and periodically throughout
therapy and frequently during IV
therapy.
 Assess IV site frequently during
administration; diazepam may cause
phlebitis and venous thrombosis.
 Conduct regular assessment of
continued need for treatment.
 Anxiety:Assess mental status
(orientation, mood, behavior) and
degree of anxiety.
 Assess level of sedation (ataxia,
dizziness, slurred speech) prior to and
periodically throughout therapy.
 Seizures: Observe and record intensity,
duration, and location of seizure activity.
The initial dose of diazepam offers
seizure control for 15–20 min after
administration. Institute seizure
precautions.
 Muscle Spasms:Assess muscle spasm,
associated pain, and limitation of
movement prior to and during therapy.
 Toxicity and Overdose:Flumazenil is
an adjunct in the management of toxicity
or overdose. (Flumazenil may induce
seizures in patients with a history of
seizures disorder or who are on tricyclic
antidepressants.).
Diagnoses
 Anxiety (Indications)
 Impaired physical mobility (Indications)
 Risk for injury (Side Effects)
Implementation:
 Patient should be kept on bedrest and
observed for at least 3 hr following
parenteral administration.
 PO: Tablets may be crushed and taken
with food or water if patient has difficulty
swallowing.
 Mix Intensol preparation with liquid or
semisolid food such as water, juices,
soda, applesauce, or pudding.
Administer entire amount immediately.
Do not store.
 IM: IM injections are painful and
erratically absorbed. If IM route is used,
inject deeply into deltoid muscle for
maximum absorption.
Evaluation:
 Decrease in anxiety level. Full
therapeutic antianxiety effects occur
after 1–2 week of therapy.
 Decreased recall of surgical or
diagnostic procedures.
 Control of seizures.
 Decrease in muscle spasms.
 Decreased tremulousness and more
rational ideation when used for alcohol
withdrawal.
Drug Classification: MUSCLE
RELAXANTS FOR SPASTICITY:
CENTRALLY-ACTING
Generic Name: Baclofen
Brand Name: Lioresal
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 5 mg 3 times daily. May
increase q 3days by 5 mg/dose up to 80
mg/day (some patients may have a better
response to 4 divided doses).
PO (Children >=8 yr): 30–40 mg daily
divided q 8 hr; titrate to a maximum of 120
mg/day.
PO (Children 2–7 yr): 20–30 mg daily
divided q 8 hr; titrate to a maximum of 60
mg/day.
PO (Children <2 yr): 10–20 mg daily
divided q 8 hr; titrate to a maximum of 40
mg/day.
IT (Adults): 100–800 mcg/day infusion;
dose is determined by response during
screening phase.
IT (Children >=4 yr): 25–1200 mcg/day
infusion (average 275 mcg/day); dose is
determined by response during screening
phase.
DRUG ACTION
Inhibits reflexes at the spinal level.
Therapeutic Effects:
Decreased muscle spasticity; bowel and
bladder function may also be improved.
Pharmacokinetics: Absorption: Well
absorbed after oral administration.
Distribution: Widely distributed; crosses the
placenta. Protein Binding: 30%.
Page | 65
Metabolism and Excretion: 70–80%
eliminated unchanged by the kidneys.
Half-life: 2.5–4 hr.
INTERACTIONS
Drug-Drug: Increase CNS depression with
other CNS depressants including alcohol,
antihistamines, opioid analgesics, and
sedative/hypnotics. Usewith MAO inhibitors
may lead to increase in CNS depression or
hypotension.
INDICATION
PO: Treatment of reversible spasticity due to
multiple sclerosis or spinal cord lesions. IT:
Treatment of severe spasticity of cerebral or
spinal origin (should be reserved for patients
who do not respond or are intolerant to oral
baclofen) (should wait at least one year in
patients with traumatic brain injury before
considering therapy).
CONTRAINDICATION
Contraindicated in: Coagulopathy,
bacteremia, intramuscular or intrathecal
administration; lactation.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: Seizures (IT), dizziness, drowsiness,
fatigue, weakness, confusion, depression,
headache, insomnia. EENT: nasal
congestion, tinnitus. CV: edema,
hypotension. GI: nausea, constipation. GU:
frequency. Derm: pruritus, rash. Metab:
hyperglycemia, weight gain. Neuro: ataxia.
Misc: hypersensitivity reactions, sweating.
NURSING INTERVENTIONS
Assessment
 Assess muscle spasticity before and
periodically during therapy.
 Observe patient for drowsiness,
dizziness, or ataxia. May be alleviated
by a change in dose.
 IT: Monitor patient closely during test
dose and titration. Resuscitative
equipment should be immediately
available for life-threatening or
intolerable side effects.
Diagnoses
 Impaired wheelchair mobility
(Indications)
 Risk for injury (Adverse Reactions)
Implementation:
 PO: Administer with milk or food to
minimize gastric irritation.
 IT: For screening phase, dilute for a
concentration of 50 mcg/mL with sterile
preservative-free NaCl for injection. Test
dose should be administered over at
least 1 min. Observe patient for a
significant decrease in muscle tone or
frequency or severity of spasm. If
response is inadequate, 2 additional test
doses, each 24 hr apart, 75 mcg/1.5 mL
and 100 mcg/2 mL respectively, may be
administered. Patients with an
inadequate response should not receive
chronic IT therapy.
 Dose titration for implantable IT pumps
is based on patient response. If no
substantive response after dose
increase, checks pump function and
catheter patency.
Evaluation:
 Decrease in muscle spasticity and
associated musculoskeletal pain with an
increased ability to perform activities of
daily living.
 Decreased pain in patients with
trigeminal neuralgia. May take weeks to
obtain optimal effect.
Drug Classification: DIRECT ACTING
Generic Name: Dantrolene Sodium
Brand Name: Dantrium
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Relief of Spasticity
Adult: PO 25 mg once/day, increase to 25
mg b.i.d. to q.i.d., may increase q7days up
to 100 mg b.i.d. to q.i.d.
Child (over 5 y): PO 0.5 mg/kg b.i.d.,
increase to 0.5 mg/kg t.i.d. or q.i.d., may
increase by 0.5 mg/kg up to 3 mg/kg b.i.d. to
q.i.d. (max: 100 mg q.i.d.)
Malignant Hyperthermia Treatment
Adult/Child: IV 1 mg/kg rapid direct IV push
repeated prn up to a total of 10 mg/kg PO
May be necessary to continue orally with 1–
2 mg/kg q.i.d. for 1–3 days to prevent
recurrence
Malignant Hyperthermia Preoperatively
Adult: IV 2.5 mg/kg infusion over 1 h may be
repeated
Adult/Child (over 5 y): PO 4–8 mg/kg/day in
divided doses for 1–2 days prior to surgery
Hepatic Impairment Dosage Adjustment
Do not use in active liver disease
DRUG ACTION
Acts directly on skeletal muscle, causing
relaxation by decreasing calcium release
from sarcoplasmic reticulum in muscle cells.
Prevents intense catabolic process
associated with malignant hyperthermia.
Therapeutic Effects: Reduction of muscle
spasticity. Prevention of malignant
hyperthermia.
Pharmacokinetics: Absorption: 35%
absorbed after oral administration.
Distribution: Unknown. Metabolism and
Excretion: Almost entirely metabolized by
the liver. Half-life: 8.7 hr.
INTERACTIONS
Drug-drug: Additive CNS depression with
CNS depressants, including alcohol,
antihistamines, opioid analgesics,
sedative/hypnotics, and parenteral
magnesium sulfate. Increase risk of
hepatotoxicity with other hepatotoxic agents
or estrogens. Increase risk of arrhythmias
Page | 66
with verapamil. Increase neuromuscular
blocking effects of vecuronium.
Drug-Natural Products: Concomitant use
of kava-kava, valerian, chamomile, or hops
can increase CNS depression.
INDICATION
PO: Treatment of spasticity associated with:
Spinal cord injury, stroke, cerebral palsy,
multiple sclerosis. Prophylaxis of malignant
hyperthermia.IV: Emergency treatment of
malignant hyperthermia.
CONTRAINDICATION
Contraindicated in: No contraindications to
IV form in treatment of hyperthermia;
Lactation: Lactation; Situations in which
spasticity is used to maintain posture or
balance.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: drowsiness, muscle weakness,
confusion, dizziness, headache, insomnia,
malaise, nervousness. EENT: excessive
lacrimation, visual disturbances. Resp:
pleural effusions, respiratory depression.
CV: changes in BP, heart failure,
tachycardia. GI: HEPATOTOXICITY,
diarrhea, anorexia, cramps, dysphagia, GI
bleeding, nausea, vomiting. GU: crystalluria,
dysuria, frequency, erectile dysfunction,
incontinence, nocturia. Derm: pruritus,
sweating, urticaria. Hemat: anemia, aplastic
anemia, eosinophilia, leukopenia,
thrombocytopenia. Local: irritation at IV site,
phlebitis. MS: myalgia. Misc:
ANAPHYLAXIS, chills, drooling, fever.
NURSING INTERVENTIONS
Assessment
 Assess bowel function periodically.
Persistent diarrhea may warrant
discontinuation of therapy.
 Muscle Spasticity: Assess
neuromuscular status and muscle
spasticity before initiating and
periodically during therapy to determine
response.
 Malignant Hyperthermia: Assess
previous anesthesia history of all
surgical patients.
 Monitor ECG, vital signs, electrolytes,
and urine output continuously when
administering IV for malignant
hyperthermia.
 Evaluate renal function and CBC before
and periodically during therapy in
patients receiving prolonged therapy.
Diagnoses
 Impaired physical mobility (Indications)
 Acute pain (Indications)
 Risk for injury (Side Effects)
Implementation:
 PO: If gastric irritation becomes a
problem, may be administered with food.
Oral suspensions may be made by
opening capsules and adding them to
fruit juices or other liquids. Drink
immediately after mixing.
 Oral dose for spasticity should be
divided into 4 doses/day.
 Oral dose is not indicated for neuroleptic
malignant syndrome.
Evaluation:
 Relief of muscle spasm in
musculoskeletal conditions. One wk or
more may be required
Drug Classification: Centrally-Acting
Muscle Relaxant
Generic Name: Methocarbamol
Brand Name: Robaxin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 1.5 g 4 times daily initially (up
to 8 g/ day) for 2–3 days, then 4–4.5 g/day
in 3–6 divided doses; may be followed by
maintenance dosing of 75 mg q 4 hr or 1 g 4
times daily or 1.5 g 3 times daily.
IM, IV (Adults): 1–3 g/day for not more than
3 days; course may be repeated after a 48-
hr rest.
DRUG ACTION
Skeletal muscle relaxation, probably as a
result of CNS depression.
Therapeutic Effects: Skeletal muscle
relaxation.
Pharmacokinetics: Absorption: Rapidly
absorbed from the GI tract.
Distribution: Widely distributed. Crosses
the placenta; enters breast milk in small
amounts.
Metabolism and Excretion: Metabolized by
the liver. Half-life: 1–2 hr.
INTERACTIONS
Drug-drug: Additive CNS depression with
other CNS depressants, including alcohol,
antihistamines, opioid analgesics, and
sedative/hypnotics.
INDICATION
Adjunctive treatment of muscle spasm
associated with acute painful
musculoskeletal conditions (with rest and
physical therapy).
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Hypersensitivity to polyethylene glycol
(parenteral form); renal impairment
(parenteral form).
ADVERSE REACTIONS/ SIDE EFFECT
CNS: Seizures (IV, IM only), dizziness,
drowsiness, light-headedness. EENT:
blurred vision, nasal congestion. CV: IV—
bradycardia, hypotension. GI: anorexia, GI
upset, nausea. GU: brown, black, or green
urine. Derm: flushing (IV only), pruritus,
Page | 67
rashes, urticaria. Local: pain at IM site,
phlebitis at IV site. Misc: allergic reactions
including Anaphylaxis (IM, IV use only),
fever.
NURSING IMPLICATIONS
Assessment
 Assess patient for pain, muscle
stiffness, and range of motion before
and periodically throughout therapy.
 Monitor pulse and BP every 15 min
during parenteral administration.
 Geri: Assess geriatric patients for
anticholinergic effects (sedation and
weakness).
 Assess patient for allergic reactions
(skin rash, asthma, hives, wheezing,
and hypotension) after parenteral
administration. Keep epinephrine and
oxygen on hand in the event of a
reaction.
 Monitor IV site. Injection is hypertonic
and may cause thrombophlebitis. Avoid
extravasation.
 May cause falsely increased urinary 5-
hydroxyindoleacetic acid (5-HIAA) and
vanillylmandelic acid (VMA)
determinations.
Diagnoses
 Acute pain (Indications)
 Impaired physical mobility (Indications)
 Risk for injury (Side Effects)
Implementation:
 Provide safety measures as indicated.
Supervise ambulation and transfer of
patients.
 PO:May be administered with food to
minimize GI irritation. Tablets may be
crushed and mixed with food or liquids
to facilitate swallowing. For
administration via NG tube, crush tablet
and suspend in water or saline.
 IM:Do not administer sub-cut. IM
injections should contain no more than 5
mL (500 mg) at a time in the gluteal
region.
Evaluation:
 Decreased musculoskeletal pain and
muscle spasticity.
 Increased range of motion.
Drug Classification: DEPOLARIZING
MUSCLE RELAXANT (ADJUNCT TO
ANESTHESIA)
Generic Name: Succinylcholine
Brand Name: Anectine
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Surgical and Anesthetic Procedures
Adult: IV 0.3–1.1 mg/kg administered over
10–30 sec, may give additional doses prn IM
2.5–4 mg/kg up to 150 mg
Child: IV 1–2 mg/kg administered over 10–
30 sec, may give additional doses prn IM
2.5–4 mg/ kg up to 150 mg
Prolonged Muscle Relaxation
Adult: IV 0.5–10 mg/min by continuous
infusion
Obesity Dosage Adjustment
Dose based on IBW
DRUG ACTION
Synthetic, ultra short-acting depolarizing
neuromuscular blocking agent with high
affinity for acetylcholine (ACh) receptor
sites.Initial transientcontractions and
fasciculations arefollowed by sustained
flaccid skeletalmuscle paralysis produced by
state ofaccommodation that develops in
adjacentexcitable muscle membranes.
Therapeutic Effects: Skeletal muscle
paralysis.
Pharmacokinetics: Onset: 0.5– 1 min IV;
2–3 min IM. Duration: 2–3 min IV; 10–30
min IM.
Distribution: Crosses placenta in small
amounts. Metabolism: In plasma by
pseudocholinesterases. Elimination: In
urine.
INTERACTIONS
Drug-Drug: Aminoglycosides, Colistin,
Cyclophosphamide, Cyclopropane,
Echothiophate Iodide, Halothane, Lidocaine,
Magnesium Salts, Methotrimeprazine,
Narcotic Analgesics,
OrganophosphamideInsecticides, MAO
Inhibitors, Phenothiazines, Procaine,
Procainamide, Quinidine, Quinine,
Propranolol May Prolong Neuromuscular
Blockade;Digitalis Glycosides may
Increaserisk of Cardiac Arrhythmias.
INDICATION
Used during surgical procedures to
produce skeletal muscle paralysis after
induction of anesthesia and provision of
opioid analgesics.
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
succinylcholine; family history of malignant
hyperthermia; burns; trauma.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: Muscle fasciculations, profound
andprolonged muscle relaxation,
musclepain. CV: Bradycardia,
tachycardia,hypotension,
hypertension,arrhythmias, sinus arrest.
Respiratory: Respiratory depression,
bronchospasm,hypoxia, apnea. Body as a
Whole: Malignant hyperthermiaincreased
IOP, excessive salivation,enlarged salivary
glands. Metabolic: Myoglobinemia,
hyperkalemia. GI: Decreased tone and
motility of GItract (large doses).
NURSING INTERVENTIONS
Page | 68
Assessment
 Assess respiratory status continuously
throughout use of succinylcholine.
Succinylcholine should be used only by
individuals experienced in endotracheal
intubation, and equipment for this
procedure should be immediately
available.
 Monitor neuromuscular response to
succinylcholine with a peripheral nerve
stimulator intraoperatively. Paralysis is
initially selective and usually occurs
consecutively in the following muscles:
levator muscles of eyelids, muscles of
mastication, limb muscles, abdominal
muscles, muscles of the glottis,
intercostal muscles, and the diaphragm.
 Monitor ECG, heart rate, and BP
throughout use of succinylcholine.
 Assess patient for history of malignant
hyperthermia before administration.
Monitor for signs of malignant
hyperthermia (tachycardia, tachypnea,
hypercarbia, jaw muscle spasm, lack of
laryngeal relaxation, hyperthermia)
throughout administration.
 Observe patient for residual muscle
weakness and respiratory distress
during the recovery period.
 Lab Test Considerations: May cause
hyperkalemia, especially in patients with
severe trauma, burns, or neurologic
disorders.
 Toxicity and Overdose: If overdose
occurs, use peripheral nerve stimulator
to determine degree of neuromuscular
blockade. Maintain airway patency and
ventilation until recovery of normal
respirations occurs.
Diagnoses
 Ineffective breathing pattern
(Indications) Impaired verbal
communication (Side Effects)
Implementation
 High Alert: Unplanned administration of
a neuromuscular blocking agent instead
of administration of the intended
medication, or administration of a
neuromuscular blocking agent in the
absence of ventilatory support has
resulted in serious harm and death.
Watch for packaging similarities and
double check for correct medication and
dose.
 Succinylcholine has no effect on
consciousness or the pain threshold.
Adequate anesthesia should always be
used when succinylcholine is used as an
adjunct to surgical procedures or when
painful procedures are performed. To
avoid patient distress, administer after
unconsciousness has been achieved.
Benzodiazepines and/or analgesics
should be administered concurrently
when prolonged succinylcholine therapy
is used for ventilator patients because
patient is awake and able to feel all
sensations.
Patient/Family Teaching
 Explain all procedures to patient
receiving succinylcholine therapy
without anesthesia, because
consciousness is not affected by
succinylcholine alone. Provide emotional
support.
 Reassure patient that communication
abilities will return as the medication
wears off.
Evaluation
 Adequate suppression of the twitch
response when tested with peripheral
nerve stimulation, with subsequent
muscle paralysis.
Drug Classification: Non-Depolarizing
Muscle Relaxant (Adjunct to
Anesthesia)
Generic Name: Pancuronium
Bromide
Brand Name: Pavulon
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IV (Adults and Children >1 mo): Initial
intubating dose—0.06–0.1 mg/kg initially;
additional dosesof 0.01 mg/kg may be given
q 25–60 min to maintainparalysis.
Continuous infusion—1–2 mcg/kg/min.
DRUG ACTION
Prevents neuromuscular transmission by
blocking the effect of acetylcholine at the
myoneural junction.Has no analgesic or
anxiolytic properties.
PHARMACOKINETICS
Pharmacokinetics: Absorption: Following
IV administration, absorption is essentially
complete. Distribution: Rapidly distributes
into extracellular fluid; small amounts cross
the placenta. Metabolism and Excretion:
Excreted mostly unchanged by the kidneys;
small amounts are eliminated in bile. Half-
life:2 hr.
INTERACTIONS
Drug-drug: Intensity and duration of
paralysis may be prolonged by pretreatment
with succinylcholine, general anesthesia
(inhalation), aminoglycosides, vancomycin,
tetracyclines, polymyxin B, colistin,
cyclosporine, calcium channel blockers,
clindamycin, lidocaine, and other local
Page | 69
anesthetics, lithium, quinidine,
procainamide, betablockers, potassium-
losing diuretics, or magnesium. Inhalation
anesthetics including enflurane, isoflurane,
halothane, desflurane, sevoflurane may
enhance effects. Higher infusion rates may
be requiredand duration of action may be
shortened in patientsreceiving long-term
carbamazepine, steroids (chronic),
azathioprine or phenytoin.
INDICATION
Induction of skeletal muscle paralysis and
facilitation of intubation after induction of
anesthesia in surgical
procedures.Facilitation of compliance during
mechanical ventilation.
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Hypersensitivity to bromides; Pedi: Products
containing benzyl alcohol should be avoided
in neonates.
ADVERSE REACTIONS/ SIDE EFFECT
Resp: bronchospasm. CV: hypertension,
tachycardia. GI: excessive salivation. Derm:
rash. Misc: allergic reactions including
Anaphylaxis.
NURSING INTERVENTIONS
Assessment
 Assess respiratory status continuously
throughout therapy with neuromuscular
blocking agents. These medications
should be used only to facilitate
intubation or in patients already
intubated. Monitor ECG, heart rate, and
BP throughout administration.
 Observe the patient for residual muscle
weakness and respiratory distress
during the recovery period.
 Monitor infusion site frequently. If signs
of tissue irritation or extravasation occur,
discontinue and restart in another vein.
 Toxicity and Overdose:If overdose
occurs, use peripheral nerve stimulator
to determine the degree of
neuromuscular blockade. Maintain
airway patency and ventilation until
recovery of normal respirations occurs.
Diagnoses
 Ineffective breathing pattern
(Indications)
 Impaired verbal communication (Side
Effects)
 Fear (Side Effects)
Implementation:
 High Alert:Unintended administration of
a neuromuscular blocking agent instead
of administration of the intended
medication or administration of a
neuromuscular blocking agent in the
absence of ventilatory support has
resulted in serious harm or death.
Confusing similarities in packaging and
insufficiently controlled access to these
medications are often implicated in
these medication errors. Store these
products in a separate, locked container.
Evaluation:
 Adequate suppression of the twitch
response when tested with peripheral
nerve stimulation and subsequent
muscle paralysis.
 Improved compliance during mechanical
ventilation.

IV. PAIN AND INFLAMMATION
MANAGEMENT AGENTS
A. FIRST-GENERATION
NSAIDS
Drug Classification: SALICYLATES
Generic Name:
Brand Name: ASA, Ecotrin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Mild to Moderate Pain, Fever
Adult: PO/PR 350–650 mg q4h (max: 4
g/day)
Child: PO/PR 10–15 mg/kg in 4–6 h (max:
3.6 g/day)/
Arthritic Conditions
Adult: PO 3.6–5.4 g/day in 4–6 divided
doses
Child: PO 80–100 mg/kg/day in 4–6 divided
doses (max: 130 mg/ kg/day)
Thromboembolic Disorders
Adult: PO 81–325 mg daily
TIA Prophylaxis
Adult: PO 650 mg b.i.d.
MI Prophylaxis
Adult: PO 80–325 mg/day
DRUG ACTION
Produce analgesia and reduce inflammation
and fever by inhibiting the production of
prostaglandins. AspirinOnly: Decreases
platelet aggregation.
Pharmacokinetics: Absorption: Aspirin—
Well absorbed from the upper small
intestine; absorption from enteric-coated
preparations may be unreliable; rectal
absorption is slow and variable. Choline and
magnesium salicylates—well absorbed after
oral administration. Salsalate— Splits into 2
molecules of salicylic acid after oral
administration; absorbed in the small
intestine. Distribution: All salicylates are
rapidly and widely distributed; cross the
placenta and enter breast milk. Metabolism
and Excretion: Extensively metabolized by
the liver; inactive metabolites excreted by
the kidneys. Amount excreted unchanged by
the kidneys depends on urine pH; as pH
increases, amount excreted unchanged
increases from 2–3% up to 80%. Half-life:
2–3 hr for low doses; up to 15–30 hr with
Page | 70
larger doses because of saturation of liver
metabolism.
INTERACTIONS
Drug-drug: Aspirin may increase the risk of
bleeding with warfarin, heparin, heparin-like
agents, thrombolyticagents, ticlopidine,
clopidogrel, abcixi mab, tirofiban, or
eptifibatide, although these agents are
frequently used safely in combination and in
sequence. Ibuprofen may negate the cardio-
protective antiplatelet effects of low-dose
aspirin. Aspirin may increase risk of bleeding
with cefoperazone, cefotetan, and valproic
acid. May increase activity of penicillins,
phenytoin, methotrexate, valproic acid, oral
hypoglycemicagents, and sulfonamides.
May decrease beneficial effects of
probenecid. Corticosteroids may decrease
serum salicylate levels. Urinary acidification
increase reabsorption and may decrease
serum salicylate levels. Alkalinization of the
urine or the ingestion of large amounts of
antacids decrease excretionand decrease
serum salicylate level. May bluntthe
therapeutic response to diuretics, and
antihypertensives.Increase risk of GI
irritation with NSAIDs.
Drug-Food: Foods capable of acidifying the
urine may increase serum salicylate levels.
INDICATION
Inflammatory disorders including:
Rheumatoid arthritis, Osteoarthritis. Mild to
moderate pain.Fever.Aspirin: Prophylaxis
of transient ischemic attacks and MI.
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
aspirin, tartrazine (FDC yellow dye #5), or
other salicylates; Cross sensitivity with other
NSAIDs may exist (less with nonaspirin
salicylates); Bleeding disorders or
thrombocytopenia (more important with
aspirin); Children or adolescents with viral
infections (may increase the risk of Reye’s
syndrome); peri-operative pain from
coronary artery bypass graft (CABG)
surgery.
ADVERSE REACTIONS/ SIDE EFFECT
EENT: Tinnitus. GI: Gi Bleeding, dyspepsia,
epigastric distress, nausea, abdominal pain,
anorexia, hepatotoxicity, vomiting. Derm:
salsalate—Exfoliative Dermatitis, Stevens-
Johnson Syndrome, Toxic Epidermal
Necrolysis. Hemat: aspirin—anemia,
hemolysis, increased bleeding time. Misc:
allergic reactions including Anaphylaxis and
Laryngeal Edema.
NURSING INTERVENTIONS
Assessment
 Patients who have asthma, allergies,
and nasal polyps or who are allergic to
tartrazine are at an increased risk for
developing hypersensitivity reactions.
 Assess for rash periodically during
therapy. May cause Stevens-Johnson
syndrome or toxic epidermal necrolysis.
Discontinue therapy if severe or if
accompanied with fever, general
malaise, fatigue, muscle or joint aches,
blisters, oral lesions, conjunctivitis,
hepatitis, and/or eosinophilia.
 Pain:Assess pain and limitation of
movement; note type, location, and
intensity before and at the peak after
administration.
 Fever:Assess fever and note associated
signs (diaphoresis, tachycardia, malaise,
chills). Monitor serum salicylate levels
periodically with prolonged high-dose
therapy to determine dose, safety, and
efficacy, especially in children with
Kawasaki disease.
 Aspirin:Prolongs bleeding time for 4–7
days and, in large doses, may cause
prolonged prothrombin time. Monitor
hematocrit periodically in prolonged
high-dose therapy to assess for GI blood
loss.
 Toxicity and Overdose: Monitor patient
for the onset of tinnitus, headache,
hyperventilation, agitation, mental
confusion, lethargy, diarrhea, and
sweating. If these symptoms appear,
withhold medication and notify health
care professional immediately.
Diagnoses
 Acute pain (Indications)
 Impaired physical mobility (Indications)
Implementation:
 Use lowest effective dose for shortest
period of time.
 PO: Administer after meals or with food
or an antacid to minimize gastric
irritation. Food slows but does not alter
the total amount absorbed.
 Do not crush or chew enteric-coated
tablets. Do not take antacids within 1–2
hr of enteric-coated tablets.
 Chewable tablets may be chewed,
dissolved in liquid, or swallowed whole.
Some extended-release tablets may be
broken or crumbled but must not be
ground up before swallowing. See
manufacturer’s prescribing information
for individual products.
Evaluation:
 Relief of mild to moderate discomfort.
 Increased ease of joint movement. May
take 2–3 wk for maximum effectiveness.
 Reduction of fever.
 Prevention of transient ischemic attacks.
 Prevention of MI.
Drug Classification: SALICYLATE
DERIVATIVES
Generic Name: Olsalazine Sodium
Brand Name: Dipentum
Page | 71
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 500 mg twice daily.
DRUG ACTION
Locally acting anti-inflammatory action in the
colon, where activity is probably due to
inhibition of prostaglandin synthesis.
Pharmacokinetics: Absorption: Acts
locally in colon, where 98–99% is converted
to mesalamine (5-aminosalicylic acid).
Distribution: Action is primarily local and
remains in the colon. Metabolism and
Excretion: 2% absorbed into systemic
circulation is rapidly metabolized; mostly
eliminated as mesalamine in the feces.
Half-life: 0.9 hr.
INTERACTIONS
Drug-drug: Increase risk of bleeding after
neuraxial anesthesia with low molecular
weight heparins and heparinoids;
discontinue olsalazine before initiation of
therapy or monitor closely if discontinuation
not possible. May decrease metabolism, and
increase effects/toxicity of mercaptopurine
or thioguanine with and increase risk of
myelosuppression (use lowest possible dose
and monitor closely).Increase risk of
developing Reye’s syndrome; avoid
olsalazine during 6 wk after varicella
vaccine.
INDICATION
Ulcerative colitis (when patients cannot
tolerate sulfasalazine).
CONTRAINDICATION
Contraindicated in: Hypersensitivity
reactions to salicylates; Cross-sensitivity
with furosemide, sulfonylurea hypoglycemic
agents, or carbonic anhydrase inhibitors
may exist; Glucose-6–phosphate
dehydrogenase (G6PD) deficiency; Urinary
tract or intestinal obstruction; Porphyria;
Lactation: Lactation; Pedi: Children <2 yr
(safety not established).
ADVERSE REACTIONS/ SIDE EFFECT
CNS: ataxia, confusion, dizziness,
drowsiness, headache, mental depression,
psychosis, restlessness. GI: diarrhea,
abdominal pain, anorexia, exacerbation of
colitis, drug-induced hepatitis, nausea,
vomiting. Derm: itching, rash. Hemat: blood
dyscrasias.
NURSING INTERVENTIONS
Assessment
 Assess patient for allergy to
sulfonamides and salicylates.
 Patients allergic to sulfasalazine may
take mesalamine or olsalazine without
difficulty, but therapy should be
discontinued if rash or fever occurs.
 Monitor intake and output ratios. Fluid
intake should be sufficient to maintain a
urine output of at least 1200–1500 mL
daily to prevent crystalluria and stone
formation.
 Inflammatory Bowel Disease:Assess
abdominal pain and frequency, quantity,
and consistency of stools at the
beginning of and throughout therapy.
 Olsalazine may cause increase AST and
ALT levels.
Diagnoses
 Acute pain (Indications)
 Diarrhea (Indications)
Implementation:
 PO:Administer with food in evenly
divided doses every 12 hr.
Evaluation:
 Decrease in diarrhea and abdominal
pain.
 Return to normal bowel pattern in
patients with inflammatory bowel
disease. Effects may be seen within 3–
21 days. The usual course of therapy is
3–6 wk.
 Maintenance of remission in patients
with inflammatory bowel disease.
 Decrease in pain and inflammation, and
increase in mobility in patients with
rheumatoid arthritis.
Drug Classification: PARA-
CHLOROBENZOIC ACID ACID
DERIVATIVES OR INDOLES
Generic Name: Indomethacin
Brand Name: Indocin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IV (Neonates): Treatment—0.2 mg/kg
initially, then 2 subsequent doses at 12–24
hr intervals of 0.1 mg/kg if age <48 hr at time
of initial dose; 0.2 mg/kg if 2–7 days at initial
dose; 0.25 mg/kg if age >7 days at initial
dose Prophylaxis—0.1–0.2 mg/kg initially,
then 0.1 mg/kg q 12–24 hr for 2 doses.
DRUG ACTION
Inhibits prostaglandin synthesis. In the
treatment of PDA, decreased prostaglandin
production allows the ductus to close.
PHARMACOKINETICS
Absorption: Well absorbed after oral
administration in adults, incomplete oral
absorption in neonates. Distribution:
Crosses the blood-brain barrier and the
placenta. It enters breast milk. Protein
Binding: 99%.
Metabolism and Excretion: Mostly
metabolized by the liver. Half-life: Neonates
<2 weeks: 20 hr; >2 weeks: 11 hr; Adults:
2.6–11 hr.
INTERACTIONS
Drug-drug: Concurrent use with aspirin may
decrease effectiveness. Additive adverse GI
effects with aspirin, other NSAIDs,
corticosteroids, or alcohol. Chronic use of
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acetaminophen increase risk of adverse
renal reactions. May decrease effectiveness
of diuretics or antihypertensives. May
increase hypoglycemia from insulins or oral
hypoglycemic agents. May increase risk of
toxicity from lithium or zidovudine (avoid
concurrent use with zidovudine). Increase
risk of toxicity from methotrexate.
Probenecid increase risk of toxicity from
indomethacin. Increase risk of bleeding with
cefotetan, cefoperazone, valproicacid,
thrombolytics, warfarin, and drugs
affectingplatelet function including
clopidogrel, ticlopidine, abciximab,
eptifibatide, or tirofiban. Increase risk of
adverse hematologic reactions with
antineoplastics or radiation therapy.
Increase risk of nephrotoxicity with
cyclosporine. Concurrent use with
potassium-sparing diuretics may result in
hyperkalemia. May increase levels of
digitalisglycosides, methotrexate, lithium,
and aminoglycosides when used IV in
neonates.
INDICATION
PO: Inflammatory disorders including:
Rheumatoid arthritis, Gouty arthritis,
Osteoarthritis, Ankylosing spondylitis.
Generally reserved for patients who do not
respond to less toxic agents.IV: Alternative
to surgery in the management of patent
ductus arteriosus (PDA) in premature
neonates.
CONTRAINDICATION
Contraindicated in: Hypersensitivity;
Known alcohol intolerance (suspension);
Cross-sensitivity may exist with other
NSAIDs, including aspirin; Active GI
bleeding; Ulcer disease; Proctitis or recent
history of rectal bleeding; Intraventricular
hemorrhage; Thrombocytopenia; Pedi:
Increase risk of necrotizing enterocolitis and
bowel perforation in premature infants with
PDA.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: dizziness, drowsiness, headache,
psychic disturbances. EENT: blurred vision,
tinnitus. CV: hypertension, edema. GI: PO—
Drug-Induced Hepatitis, GI Bleeding,
constipation, dyspepsia, nausea, vomiting,
discomfort, necrotizing enterocolitis. GU:
cystitis, hematuria, renal failure. Derm:
rashes. F and E: hyperkalemia; IV, dilutional
hyponatremia; IV, hypoglycemia. Hemat:
thrombocytopenia, blood dyscrasias,
prolonged bleeding time. Local: phlebitis at
IV site. Misc: allergic reactions including
Anaphylaxis.
NURSING IMPLICATIONS
Assessment
 Patients who have asthma, aspirin-
induced allergy, and nasal polyps are at
increased risk for developing
hypersensitivity reactions. Monitor for
rhinitis, asthma, and urticaria.
 Arthritis: Assess limitation of movement
and pain—note type, location, and
intensity before and 1–2 hr after
administration.
 PDA:Monitor respiratory status, heart
rate, and BP, echocardiogram, and
heart sounds routinely throughout
therapy.
 Monitor intake and output. Fluid
restriction is usually instituted
throughout therapy. Serum potassium,
BUN, serum creatinine, AST, and ALT
tests may show increase levels. Blood
glucose concentrations may be altered.
Hemoglobin and hematocrit
concentrations, leukocyte and platelet
counts, and CCr may be decrease.
 Urine glucose and urine protein
concentrations may be increase.
 Leukocyte and platelet count may be
decrease. Bleeding time may be
prolonged for several days after
discontinuation.
Diagnoses
 Acute pain (Indications)
 Impaired physical mobility (Indications)
Implementation:
 If prolonged therapy is used, dose
should be reduced to the lowest level
that controls symptoms.
 PO: Administer after meals, with food, or
with antacids to decrease GI irritation.
Do not break, crush, or chew sustained-
release capsules.
 Shake suspension before
administration. Do not mix with antacid
or any other liquid.
Evaluation:
 Decrease in severity of moderate pain.
 Improved joint mobility. Partial arthritic
relief is usually seen within 2 wk, but
maximum effectiveness may require up
to 1 mo of continuous therapy. Patients
who do not respond to one NSAID may
respond to another.
 Successful PDA closure.
Drug Classification: PHENYLACETIC
ACIDS
Generic Name: Dicoflenac Sodium
Brand Name: Voltaren XR
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Delayed release daily or 100 mg
Sustained release daily
Child: po 25 mg b.i.d. Or t.i.d.
Osteoarthritis
Adult: po 100–150 mg/day in
3–4 divided doses; 75 mg
Delayed release daily; 100 mg
Sustained release daily topical
Page | 73
(gel) 4 g for each knee, ankle or
Foot q.i.d. (solution) 40 drops to
Each affected knee q.i.d.
Ankylosing spondylitis
Adult: po 25 mg q.i.d. And 25 mg
At bedtime
Cataract surgery
Adult: ophthalmic 1 drop of 0.1%
Solution in affected eye q.i.d.
Beginning 24 h after surgery and
Continuing for 2 wk
Actinic keratosis
Adult: topical apply to affected
Area b.i.d. For 60–90 days
Acute pain (flector)
Adult: transdermal apply one patch
To most painful area b.i.d.
DRUG ACTION
Inhibits prostaglandin synthesis.
Therapeutic Effects: Suppression of pain
and inflammation. Relief of acute migraine
attacks. Topical (Solaraze): Clearance of
actinic keratosis lesions
Pharmacokinetics: Absorption:
Undergoes first-pass metabolism by liver
which results in 50% bioavailability. Oral
diclofenac sodium is a delayed-release dose
form. Diclofenac potassium is an immediate-
release dose form. 6– 10% of topical gel is
systemically absorbed. Distribution:
Crosses the placenta. Protein Binding:
99%. Metabolism and Excretion:
Metabolized by the liver (primarily by
CYP2C9) to several metabolites; 65%
excreted in urine, 35% in bile. Half-life: 2 hr.
INTERACTIONS
Primarily noted for oral administration
Drug-drug: Increase adverse GI effects with
aspirin, other NSAIDs, or corticosteroids.
May decrease effectiveness of diuretics or
antihypertensives.May increase levels/risk of
toxicity from cyclosporine, lithium, or
methotrexate. Increase risk of bleeding with
somecephalosporins, thrombolytic agents,
antiplatelet agents, or warfarin. CYP2C9
inhibitors including voriconazole may
increase levels/risk of toxicity. CYP2C9
inducers, including rifampin may decrease
levels/effectivness. Concurrent use of oral
NSAIDs during topical diclofenac therapy
should be minimized.
Drug-Natural Products: increase bleeding
risk with arnica, chamomile, clove, dong
quai, feverfew, garlic, ginger, ginkgo, Panax
ginseng, and others.
INDICATION
PO: Management of inflammatory disorders
including: Rheumatoid arthritis,
Osteoarthritis, Ankylosing spondylitis.
Primary dysmenorrhea.Relief of mild to
moderate pain.Acute treatment of migraines
(powder for oral solution).
TopicalManagement of: Actinic keratoses
(Solaraze), Osteoarthritis (Voltaren Gel,
Pennsaid [for knees]). Transdermal Acute
pain due to minor strains, sprains, and
contusions
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
diclofenac or other components of
formulation; Cross-sensitivity may occur with
other NSAIDs including aspirin; Active GI
bleeding/ulcer disease; Patients undergoing
coronary artery bypass graft surgery;
Exudative dermatitis, eczema, infectious
lesions, burns, or wounds. Use Cautiously
in: Severe renal/hepatic disease;
Cardiovascular disease or risk factors for
cardiovascular disease (may increase risk of
serious cardiovascular thrombotic events,
myocardial infarction, and stroke, especially
with prolonged use); Heart failure or edema;
History of porphyria; History of peptic ulcer
disease and/or GI bleeding; Geri: Dose
decrease recommended; more susceptible
to adverse reactions, including GI bleeding;
Bleeding tendency or concurrent
anticoagulant therapy; OB, Lactation: Not
recommended for use during second half of
pregnancy; Pedi: Safety not established.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: dizziness, headache. CV:
hypertension. EENT: tinnitus. Gi: gi
bleeding, hepatotoxicity, abdominal pain,
constipation, diarrhea, dyspepsia, flatulence,
heartburn, increase liver enzymes, nausea,
vomiting. GU: acute renal failure, hematuria.
Derm: exfoliative dermatitis, Stevens-
Johnson syndrome, toxic epidermal
necrolysis,pruritis, rashes, eczema,
photosensitivity. F and e: edema. Hemat:
anemia, prolonged bleeding time. Local:
topical only— contact dermatitis, dry skin,
exfoliation.misc:allergic reactions including
anaphylaxis
NURSING INTERVENTIONS
Assessment
 Monitor BP closely during initiation of
treatment and periodically during
therapy in patients with hypertension.
 Assess patient for skin rash frequently
during therapy. Discontinue at first sign
of rash; may be lifethreatening. Stevens-
Johnson syndrome may develop. Treat
symptomatically; may recur once
treatment is stopped.
 Pain: Assess pain and limitation of
movement
 Arthritis: Assess arthritic pain (note type,
location, intensity) and limitation of
movement
 Actinic Keratosis: Assess lesions prior to
and periodically during therapy.
Page | 74
 Lab Test Considerations: Diclofenac has
minimal effect on bleeding time and
platelet aggregation.
 Monitor CBC and liver function tests
within 4–8 wk of initiating diclofenac and
periodically during therapy. May
causeqserum alkaline phosphatase,
LDH, AST, and ALT concentrations.
Diagnoses
 Acute pain (Indications)
 Impaired physical mobility (Indications)
Implementation
 PO: Take with food or milk to minimize
gastric irritation. May take first 1–2
doses on an empty stomach for more
rapid onset. Do not crush or chew
enteric- coated or extended-release
tablets.
 Topical: Dispense solution 10 drops at a
time either directly onto knee or first into
the hand and then onto knee.
 Transdermal: Apply patch to the most
painful area twice a day.
Patient/Family Teaching
 Caution patient to avoid concurrent use
of alcohol, aspirin, acetaminophen, other
NSAIDs, or other OTC medications
without consulting health care
professional.
 Instruct patient to notify health care
professional of
medication regimen before treatment or
surgery.
Evaluation
 Decrease in severity of mild-to-moderate
pain.
 Increased ease of joint movement.
Patients who do not respond to one
NSAID may respond to another. May
require 2 wk or more for maximum
effects.
Drug Classification: Propionic Acid
Derivatives
Generic Name: Ibuprofen
Brand Name: Motrin, Advil
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Inflammatory Disease
Adult: PO 400–800 mg t.i.d. or q.i.d. (max:
3200 mg/day)
Child: PO Weight less than 20 kg: Up to 400
mg/day in divideddoses; weight 20–30 kg:
Up to600 mg/day in divided doses; weight
30–40 kg: Up to 800 mg/day in divided
doses
Dysmenorrhea
Adult: PO 400 mg q4–6h up to 1200 mg/day
Mild to Moderate Pain
Adult: PO 400 mg q4–6h up to 1200 mg/day
IV 400 mg q4–6h prn or 100–200 mg q4h
prn
Fever
Adult: PO 200–400 mg t.i.d. or q.i.d. (max:
1200 mg/day)
Child (6 mo–12 y): PO 5–10 mg/ kg q4–6h
up to 40 mg/kg/day
DRUG ACTION
Inhibits prostaglandin synthesis.
Pharmacokinetics: Absorption: Oral
formulation is well absorbed (80%) from the
GI tract; IV administration results in
complete bioavailability. Distribution: Does
not enter breast milk in significant amounts.
Protein Binding: 99%. Metabolism and
Excretion: Mostly metabolized by the liver;
small amounts (1%) excreted unchanged by
the kidneys.
Half-life: Neonates: 26–43 hr; Children: 1–2
hr; Adults: 2–4 hr.
INTERACTIONS
Drug-drug: May limit the cardioprotective
effects of low-dose aspirin. Concurrent use
with aspirin may decrease effectiveness of
ibuprofen. Additive adverse GI side effects
with aspirin, oral potassium, other
NSAIDs,corticosteroids, or alcohol. Chronic
use with acetaminophen may increase risk
of adverse renal reactions. May decrease
effectiveness of diuretics, ACE inhibitors, or
other antihypertensives. May increase
hypoglycemic effects of insulin or oral
hypoglycemic agents. May increase serum
lithium levels and risk of toxicity. Increase
risk of toxicity from methotrexate.
Probenecid increase risk of toxicity from
ibuprofen. Increase risk of bleeding with
cefotetan, cefoperazone, corticosteroids,
valproic acid, thrombolytics, warfarin, and
drugs affectingplatelet function including
clopidogrel, ticlopidine, abciximab,
eptifibatide, or tirofiban. Increase risk of
adverse hematologic reactions with
antineoplasticsor radiation therapy. Increase
risk of nephrotoxicity with cyclosporine.
INDICATION
PO, IV: Treatment of: Mild to moderate pain,
Fever.
PO: Treatment of: Inflammatory disorders
including rheumatoid arthritis (including
juvenile) and osteoarthritis, Dysmenorrhea.
IV: Moderate to severe pain with opioid
analgesics. Closure of a clinically significant
PDA in neonates weighing 500–1500 g and
≤32 weeks gestational age (ibuprofen lysine
only)
CONTRAINDICATION
Contraindicated in: Hypersensitivity (cross-
sensitivity may exist with other NSAIDs,
including aspirin); Active GI bleeding or ulcer
disease; Chewable tablets contain
aspartame and should not be used in
patients with phenylketonuria; Peri-operative
pain from coronary artery bypass graft
(CABG) surgery; OB: Avoid after 30 wk
gestation (may cause premature closure of
fetal ductus arteriosus); Pedi: Ibuprofen
lysine: Preterm neonates with untreated
infection, congenital heart disease where
Page | 75
patency of PDA is necessary for pulmonary
or systemic blood flow, bleeding,
thrombocytopenia, coagulation defects,
necrotizing enterocolitis, significant renal
dysfunction.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: headache, dizziness, drowsiness,
intraventricular hemorrhage (ibuprofen
lysine), psychic disturbances. EENT:
amblyopia, blurred vision, tinnitus. CV:
arrhythmias, edema, hypertension. GI: GI
Bleeding, Hepatitis, constipation, dyspepsia,
nausea, necrotizing enterocolitis (ibuprofen
lysine), vomiting, abdominal discomfort. GU:
cystitis, hematuria, renal failure. Derm:
Exfoliative Dermatitis, Stevens - Johnson
syndrome, Toxic Epidermal Necrolysis,
rashes, injection site reaction. Hemat:
anemia, blood dyscrasias, prolonged
bleeding time. Misc: allergic reactions
including Anaphylaxis.
NURSING INTERVENTIONS
Assessment
 Patients who have asthma, aspirin-
induced allergy, and nasal polyps are at
increased risk for developing
hypersensitivity reactions. Assess for
rhinitis, asthma, and urticaria.
 Assess for signs and symptoms of GI
bleeding (tarry stools, lightheadedness,
hypotension), renal dysfunction
(elevated BUN and creatinine levels,
decreased urine output), and hepatic
impairment (elevated liver enzymes,
jaundice). Geri: Higher risk for poor
outcomes or death from GI bleeding.
Agerelated renal impairment increases
risk of hepatic and renal toxicity.
 Assess patient for skin rash frequently
during therapy. Discontinue ibuprofen at
first sign of rash; may be life-
threatening. Stevens-Johnson syndrome
or toxic epidermal necrolysis may
develop. Treat symptomatically; may
recur once treatment is stopped.
 Pain:Assess pain (note type, location,
and intensity) prior to and 1–2 hr
following administration.
 Arthritis:Assess pain and range of
motion prior to and 1–2 hr following
administration.
 Fever:Monitor temperature; note signs
associated with fever (diaphoresis,
tachycardia, malaise).
 PDA Closure:Monitor preterm neonates
for signs of bleeding, infection and
decreased urine output.Monitor IV site
for signs of extravasation.
 May cause prolonged bleeding time;
may persist for <1 day following
discontinuation.
Diagnoses
 Acute pain (Indications)
 Impaired physical mobility (Indications)
 Ineffective thermoregulation
(Indications)
Implementation:
 Administration of higher than
recommended doses does not provide
increased pain relief but may increase
incidence of side effects.
 Patient should be well hydrated before
administration to prevent renal adverse
reactions. Do not give to neonates with
urine output <0.6 mL/kg/hour.
 Use lowest effective dose for shortest
period of time, especially in the elderly.
 Coadministration with opioid analgesics
may have additive analgesic effects and
may permit lower opioid doses.
 PO: For rapid initial effect, administer 30
min before or 2 hr after meals. May be
administered with food, milk, or antacids
to decrease GI irritation. Tablets may be
crushed and mixed with fluids or food;
800-mg tablet can be dissolved in water.
 Dysmenorrhea: Administer as soon as
possible after the onset of menses.
Prophylactic treatment has not been
shown to be effective.
Evaluation:
 Decrease in severity of pain.
 Improved joint mobility. Partial arthritic
relief is usually seen within 7 days, but
maximum effectiveness may require 1–2
wk of continuous therapy.
 Patients who do not respond to one
NSAID may respond to another.
 Reduction in fever.
Drug Classification: FENAMATES OR
ANTHRANILIC ACIDS
Generic Name: Mefenamic Acid
Brand Name:
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Mild to Moderate Pain
Adult: PO Loading Dose 500 mg; PO
Maintenance Dose 250 mg q6h prn
DRUG ACTION
NSAID that inhibits COX-1 and COX-2
enzymes necessary for prostaglandin
synthesis. It affects platelet function.
Analgesic andanti-inflammatory actions.
Pharmacokinetics: Absorption: Rapidly
and completely fromGI tract. Peak: 2–4 h.
Duration: 6 h. Distribution: Distributed in
breast milk.
Metabolism: Partially in liver. Elimination:
50% in urine, 50% in feces. Half-Life: 2 h.
INTERACTIONS
Drug-drug: Mefenamic acid may prolong
bleeding time with Oral Anticoagulants,
heparin;May increase lithium toxicity;
increases pharmacologic and toxic activity of
Page | 76
phenytoin, Sulfonylureas, Sulfonamides,
warfarin because of protein binding
displacement.
Drug-Herbal: Feverfew, garlic, ginger
ginkgo increase bleeding potential.
INDICATION
Relief of moderate pain when therapy will
not exceed 1 wk
 Treatment of primary dysmenorrhea
CONTRAINDICATION
Contraindicated with hypersensitivity to
mefenamic acid, aspirin or NSAID allergy,
and as treatment of perioperative pain with
coronary artery bypass grafting.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: Drowsiness, insomnia,
dizziness,nervousness, confusion,
headache. GI: Severe diarrhea, ulceration,
andbleeding; nausea, vomiting,
abdominalcramps, flatus,
constipation,hepatic toxicity. Hematologic:
Prolongedprothrombin time, severe
autoimmunehemolytic anemia
(longtermuse), leukopenia,
eosinophilia,agranulocytosis,
thrombocytopenicpurpura, megaloblastic
anemia,pancytopenia, bone marrow
hypoplasia. Urogenital:
Nephrotoxicity,dysuria, albuminuria,
hematuria, elevationof BUN. Skin: Urticaria,
rash,facial edema. Special Senses: Eye
irritation,loss of color vision
(reversible),blurred vision, ear pain. Body
as a Whole: Perspiration. CV: Palpitation.
Respiratory: Dyspnea; acute
exacerbationof asthma;
bronchoconstriction(in patients sensitive to
aspirin).
NURSING RESPONSIBILITIES
Assessment
 Patients who have asthma, aspirin-
induced allergy, and nasal polyps are at
increased risk for developing
hypersensitivity reactions. Monitor for
rhinitis, asthma, and urticaria.
 Assess patient for skin rash frequently
during therapy. Discontinue
meclofenamate at first sign of rash; may
be life-threatening. Stevens-Johnson
syndrome or toxic epidermal necrolysis
may develop. Treat symptomatically;
may recur once treatment is stopped.
 Arthritis: Assess pain and range of
movement before and periodically
during therapy.
Diagnosis
 Acute pain (Indications)
 Impaired physical mobility (Indications)
Implementation
 Administration in higher than
recommended doses does not provide
increased effectiveness but may cause
increased side effects.
 Coadministration with opioid analgesics
may have additive analgesic effects and
may permit lower opioid doses.
 PO: For rapid initial effect, administer 30
min before or 2 hr after meals. May be
administered with food, milk, or antacids
to decrease GI irritation.
 Dysmenorrhea: Administer as soon as
possible after the onset of menses.
Prophylactic treatment has not been
shown to be effective.
Evaluation/Desired Outcome
 Decreased severity of pain.
 Improved joint mobility. Partial arthritic
relief is usually seen within a few days,
but maximum effectiveness may require
2–3 wk of continuous therapy. Patients
who do not respond to one NSAID may
respond to another.
 Decreased menstrual flow.
Drug Classification: OXICAMS
Generic Name: Meloxicam
Brand Name: Mobic
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 7.5 mg once daily; some
patients may require 15 mg/day.
PO (Children 2–17 yr and _ 12 kg): 0.125
mg/kg once daily up to 7.5 mg/day.
Availability (generic available)
Tablets: 7.5 mg, 15 mg. Cost: Generic—7.5
mg $9.02/100, 15 mg $7.41/100. Oral
suspension
(contains sorbitol) (raspberry flavor): 7.5
mg/5 mL. Cost: Generic—$105.16/100 mL.
DRUG ACTION
Inhibits prostaglandin synthesis, probably by
inhibiting the enzyme cyclooxygenase.
Therapeutic Effects: Decreased pain and
inflammation associated with osteoarthritis.
Also decreases fever.
Pharmacokinetics: Absorption: Well
absorbed following oral administration.
Distribution: Unknown. Protein Binding:
99.4%. Metabolism and Excretion: Mostly
metabolized to inactive metabolites by the
liver via the P450 enzyme system;
metabolites are excreted in urine and feces.
Half-life: 20.1 hr
INTERACTIONS
Drug-drug: May decrease antihypertensive
effects of ACE inhibitors. May decrease
diuretic effects of furosemide or thiazide
diuretics. Concurrent use with aspirinq
meloxicam blood levels and may increase
risk of adverse reactions. Concurrent use
with cholestyramine decrease blood levels.
Increase plasma lithium levels (close
monitoring recommended when meloxicam
is introduced or withdrawn). May increase
Page | 77
risk of bleeding with anticoagulants,
including warfarin. Concurrent use with
sodiumpolystyrene sulfonate may increase
risk of colonic necrosis; concurrent use
should be avoided.
INDICATION
Relief of signs and symptoms of
osteoarthritis and rheumatoid arthritis
(including juvenile rheumatoid arthritis).
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
meloxicam, aspirin, salicylates, or NSAIDs;
GI bleeding; severe hepatic disease;
perioperative pain with CABG surgery;
lactation.
ADVERSE REACTIONS/ SIDE EFFECT
CV: edema. GI: gi bleeding, increase liver
enzymes, diarrhea, dyspepsia, nausea.
DERM: exfoliative dermatitis, stevens-
johnson syndrome, toxic epidermal
necrolysis,
pruritus. GU: delayed ovulation. Hemat:
anemia, leukopenia, thrombocytopenia.
NURSING INTERVENTIONS
Assessment
 Patients who have asthma, aspirin-
induced allergy, and nasal polyps are at
increased risk for developing
hypersensitivity reactions. Assess for
rhinitis, asthma, and urticaria.
 Assess pain and range of motion prior to
and 1–2 hr following administration.
 Assess for rash periodically during
therapy. May cause Stevens-Johnson
syndrome or toxic epidermal necrolysis.
Discontinue therapy if severe or if
accompanied with fever, general
malaise, fatigue, muscle or joint aches,
blisters, oral lesions, conjunctivitis,
hepatitis and/or eosinophilia.
Diagnoses
 Acute pain (Indications)
 Impaired physical mobility (Indications)
Implementation
 Administration in higher than
recommended doses does not provide
increased effectiveness but may cause
increased side effects. Use lowest
effective dose for shortest period of
time.
 PO: May be administered without regard
to food.
 Pedi: Use oral suspension to ensure
accuracy of dosing in children.
Patient/Family Teaching
 Advise patient to take this medication
with a full glass of water and to remain
in an upright position for 15–30 min after
administration.
 Instruct patient to take medication as
directed. Take missed doses as soon as
remembered but not if almost time for
the next dose. Do not double doses.
Instruct parent/caregiver to read the
Medication Guide prior to use and with
each Rx refill; new information may be
available.
 Advise female patient to notify health
care professional if pregnancy is
planned or suspected or if breast
feeding. Avoid if attempting to get
pregnant.
Evaluation
 Relief of pain.
 Improved joint mobility. Patients who do
not respond to one NSAID may respond
to another.
Drug Classification:
NAPHTHYLALKANONES
Generic Name: Nabumetone
Brand Name: Relafen
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 1000 mg/day as a single dose
or divided dose twice daily; may bequp to
2000 mg/day; use lowest effective dose
during chronic therapy.
Availability (generic available)
Tablets: 500 mg, 750 mg.
DRUG ACTION
Inhibits prostaglandin synthesis.
Therapeutic Effects: Suppression of pain
and inflammation.
Pharmacokinetics: Absorption:
Nabumetone (a prodrug) is 80% absorbed
after oral administration; 35% is rapidly
converted to 6-methoxy-2-naphthylacetic
acid (6-MNA), which is the active drug.
Distribution: Unknown.
Protein Binding: _99%. Metabolism and
Excretion: 6-MNA is metabolized by the
liver to inactive compounds. Half-life: 24 hr
(increased in severe renal impairment).
INTERACTIONS
Drug-Drug: Increase adverse GI effects
with aspirin, other NSAIDs, potassium
supplements, corticosteroids, or alcohol.
Chronic use with acetaminophen may
increase risk of adverse renal reactions.
Maydecrease effectiveness of diuretics or
antihypertensives. May increase
hypoglycemic effects of insulins or oral
hypoglycemicagents. Increase risk of toxicity
from methotrexate. Increase risk of bleeding
with cefotetan, cefoperazone, valproicacid,
anticoagulants, ticlopidine, clopidogrel,
eptifibatide, tirofiban, or thrombolytic agents.
Increase risk of adverse hematologic
reactions with antineoplastics or radiation
therapy. Concurrent use with cyclosporine
mayqrisk of renal toxicity.
INDICATION
Page | 78
Symptomatic management of rheumatoid
arthritis and osteoarthritis.
CONTRAINDICATION
Contraindicated in: Hypersensitivity; Use
with other NSAIDs, including aspirin; cross-
sensitivity may occur; Active GI bleeding or
ulcer disease; Peri-operative pain from
coronary artery bypass graft (CABG)
surgery; Lactation: Lactation.
Use Cautiously in: Severe renal, or hepatic
disease; History of ulcer disease; OB: Avoid
using during 2nd half of pregnancy due to
potential of NSAIDs to cause premature
closure of ductus arteriosus; Pedi:
Safety not established.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: agitation, anxiety, confusion,
depression, dizziness, drowsiness, fatigue,
headache, insomnia, malaise, weakness.
EENT: abnormal vision, tinnitus.
Resp: dyspnea, hypersensitivity
pneumonitis. CV: edema, fluid retention,
vasculitis. GI: GI bleeding, abdominal
pain, diarrhea,qliver function tests, anorexia,
constipation, dry mouth, dyspepsia,
flatulence, gastritis, gastroenteritis,qappetite,
nausea, stomatitis, vomiting. GU:
albuminuria, azotemia, interstitial nephritis.
Derm: exfoliative dermatitis, stevensjohnson
syndrome, toxic epidermal necrolysis,
increased sweating, photosensitivity,
pruritus, rash. Hemat: prolonged bleeding
time.Metab: weight gain. Neuro:
paresthesia, tremor. Misc: allergic reactions
including anaphylaxis, angioneurotic edema.
NURSING INTERVENTIONS
Assessment
 Assess pain and range of motion before
and periodically throughout therapy.
 Lab Test Considerations: Evaluate BUN,
serum reatinine, CBC, and liver function
periodically in patients receiving
prolonged therapy.
 Serum potassium, BUN, serum
creatinine, alkaline phosphatase, LDH,
AST, and ALT tests may showq levels.
Blood glucose, hemoglobin, and
hematocrit concentrations, leukocyte
and platelet counts, and CCr may bep.
 May cause prolonged bleeding time.
Diagnoses
 pain (Indications)
 Impaired physical mobility (Indications)
Implementation
 Administration in higher than
recommended doses does not provide
increased effectiveness but may cause
increased side effects. Use lowest
effectivedose for the shortest duration
possible to minimize cardiac risks.
 PO: Administer with meals or antacids to
decreaseGI irritation and increase
absorption.
Patient/Family Teaching
 Advise patient to take this medication
with a fullglass of water and to remain in
an upright positionfor 15–30 min after
administration.
Evaluation
 Decreased pain and improved joint
mobility. Partialarthritic relief is usually
seen within 1 wk, but maximum
effectiveness may require 2 wk.
B. SECOND-GENERATION NSAIDS
Drug Classification: SELECTIVE COX-2
INHIBITORS ORSELECTIVE
CYCLOOXYGENASE-2 INHIBITORS
Generic Name: Celecoxib
Brand Name: Celix
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Initially, 100 mg PO bid; may increase to
200 mg/day PO bid as needed.
 Acute pain, dysmenorrhea: 400 mg,
then 200 mg PO bid.
 FAP: 400 mg PO bid.
 Ankylosing spondylitis: 200 mg/day PO;
after 6 wk, a trial of 400 mg/day may be
tried for 6 wk; if no effect is seen,
suggest another therapy.
Pediatric patients 2 yr and older
10 kg or 25 kg or less: 50 mg capsule PO
bid. More than 25 kg: 100 mg capsule PO
bid.
Patients with hepatic impairment
Reduce dosage by 50%.
DRUG ACTION:
Inhibits the enzyme COX-2. This enzyme is
required for the synthesis of prostaglandins.
Has analgesic, anti-inflammatory, and
antipyretic properties.
TherapeuticEffects: Decreased pain and
inflammation caused by arthritis or
spondylitis. Decreased pain.
Pharmacokinetics: Absorption:
Bioavailability unknown. Distribution: 97%
bound to plasma proteins; extensive tissue
distribution.
Metabolism and Excretion: Mostly
metabolized by the hepatic CYP2C9
isoenzyme; the CYP2C9 enzyme system
exhibits genetic polymorphism; poor
metabolizers may have significantly increase
celecoxib concentrations and an increased
risk of adverse effects; _3% excreted
unchanged in urine and feces. Half-life: 11
hr.
INTERACTIONS
Drug-drug: CYP2C9 inhibitors may
increase levels. May decrease
effectiveness of ACE inhibitors, thiazide
diuretics, and furosemide. Fluconazole
increase levels (use lowest recommended
dosage). May increase risk of bleeding with
warfarin and aspirin. May increase serum
Page | 79
lithium levels. Does not inhibit the cardio
protective effect of low-dose aspirin.
INDICATION:
Relief of signs and symptoms of
osteoarthritis, rheumatoid arthritis,
ankylosing spondylitis, and juvenile
rheumatoid arthritis. Management of acute
pain including primary dysmenorrhea.
CONTRAINDICATION
Contraindicated in: Hypersensitivity to
celecoxib, salicylate, or sulfonamide;
asthmatic patients with aspirin triad; GI
bleeding; advanced Renal disease;
development of S&S of renal impairment
due to Drug; severe hepatic impairment;
Development of S&S of hepatic Impairment
due to drug; anemia; Pain from CABG
surgery; pregnancy (category d third
trimester); Lactation.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: dizziness, headache, insomnia. CV:
Myocardial infarction, stroke, thrombosis,
edema. GI: GI bleeding, abdominal pain,
diarrhea, dyspepsia, flatulence, nausea.
Derm: exfoliative dermatitis, stevens-
Johnson syndrome, toxic epidermal
necrolysis, Rash.
NURSING INTERVENTIONS
Assessment
 Assess range of motion, degree of
swelling, and pain in affected joints
before and periodically throughout
therapy.
 Assess patient for allergy to
sulfonamides, aspirin, or NSAIDs.
Patients with these allergies should not
receive celecoxib.
 Assess patient for skin rash frequently
during therapy. Discontinue at first sign
of rash; may be lifethreatening. Stevens-
Johnson syndrome may develop. Treat
symptomatically; may recur once
treatment is stopped.
 Lab Test Considerations: May cause
increase AST and ALT levels.
Diagnoses
 Impaired physical mobility (Indications)
 Acute pain (Indications)
Implementation
 Do not confuse with Celexa (citalopram)
or Cerebyx (fosphenytoin).
 PO: May be administered without regard
to meals. Capsules may be opened and
sprinkled on applesauce and ingested
immediately with water. Mixture may be
stored in the refrigerator for up to 6 hr.
Patient/Family Teaching
 Instruct patient to take celecoxib exactly
as directed. Do not take more than
prescribed dose.
 Advise patient to notify health care
professional promptly if signs or
symptoms of GI toxicity (abdominal pain,
black stools), skin rash, unexplained
weight gain, edema, or chest pain
occurs.
Evaluation/Desired Outcomes
 Reduction in joint pain in patients with
osteoarthritis.
 Reduction in joint tenderness, pain, and
joint swelling in patients with
rheumatoid.
C. CORTICOSTEROIDS
Drug Classification:
CORTICOSTEROIDS
Generic Name: Dexamethasone
Brand Name: Dexasone
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Allergies, Inflammation, Neoplasias
Adult: PO 0.25–4 mg b.i.d. to q.i.d.
IM 8–16 mg q1–3wk or 0.8–1.6 mg
intralesional q1–3wk IV 0.75–0.9
mg/kg/day divided q6–12h
Child: PO/IV/IM 0.08–0.3 mg/
kg/day divided q6–12h
Adrenocorticol Function
Abnormalities
Adult: PO/IV 0.75–9 mg/day in
divided doses, adjust to patient response
Child: PO/IV 0.03–0.3 mg/kg/ day in divided
doses, adjust to patient response
Cerebral Edema
Adult: IV 10 mg followed by 4 mg q6h,
reduce dose after 2–4 days then taper over
5–7 days
Child: PO/IV/IM 1–2 mg/kg loading dose,
then 1–1.5 mg/kg/ day divided q4–6h × 5
days (max: 16 mg/day)
Shock
Adult: IV 1–6 mg/kg as a single dose or 40
mg repeated q2–6h if needed or 20 mg
bolus then 3 mg/kg/day
Dexamethasone Suppression Test
Adult: PO 0.5 mg q6h for 48 h
Cushing’s Syndrome Diagnosis
Adult: PO 2 mg q6h × 48h
Inflammation
Adult/Child: Ophthalmic/
Topical/Inhalation/Intranasal
See Appendix A.
DRUG ACTION & THERAPEUTIC EFFECT
Long-acting synthetic adrenocorticoid with
intense anti-inflammatory (glucocorticoid)
activity and minimal mineralocorticoid
activity.Antiinflammatoryaction: Prevents
Accumulation of inflammatory cells at sites
of infection; inhibits phagocytosis, lysosomal
enzyme release, and synthesis of potent
mediators of inflammation, prostaglandins,
and leukotrienes; reduces capillary dilation
and permeability. Immunosuppression:
Probably due to preventionor suppression of
delayedhypersensitivity immune reaction.
Has anti-inflammatory and
immunosuppression properties.
Page | 80
Pharmacokinetics: Absorption: Readily
from GI tract. Onset: Rapid. Peak: 1–2 h
PO; 8 h IM.
Duration: 2.75 days PO; 6 days IM; 1–3 wk
intra lesional, intraarticular. Distribution:
Crosses placenta; distributed into breast
milk.
Elimination: Hypothalamus-pituitary axis
suppression: 36–54 h. Half-Life: 3–4.5 h.
INTERACTIONS
Drug-drug: Barbiturates, phenytoin,
rifampin increase steroid metabolism—
dosage Of dexamethasone may need to be
increased; amphotericin B, diuretics
compound potassium loss; ambenonium,
neostigmine,pyridostigmine may cause
severe muscle weakness in patients with
myasthenia gravis; may inhibit antibody
response to vaccines, toxoids.
Drug-Food: Grapefruit juice increase serum
levels and effects of budesonide (avoid
concurrent use).
INDICATION
Hypercalcemia associated with cancer;
Cancer chemotherapy–induced nausea and
vomiting; Short-term management of various
inflammatory and allergic disorders, such as
rheumatoid arthritis, collagen diseases
(SLE), dermatologic diseases (pemphigus),
status asthmaticus, and autoimmune
disorders; Hematologic disorders:
Thrombocytopenic purpura,
erythroblastopenia; Trichinosis with
neurologic or myocardial involvement;
Ulcerative colitis, acute exacerbations of
MS, and palliation in some leukemias and
lymphomas; Cerebral edema associated
with brain tumor, craniotomy, or head injury;
Testing adrenocortical hyperfunction
Unlabeled uses: Antiemetic for
cisplatininduced vomiting, diagnosis of
depression
CONTRAINDICATION
Systemic fungal infection, acute infections,
active or resting tuberculosis, vaccinia,
varicella, administration of live virus
vaccines (to patient, family members), latent
or active amebiasis; Cushing’s syndrome;
neonates or infants weighing less than 1300
g; lactation. Topical use: Rosacea, perioral
dermatitis; venous stasis ulcers.
Ophthalmic use: Primary open-angle
ADVERSE REACTIONS/ SIDE EFFECT
CNS: depression, euphoria, headache,
increase intracranial Pressure (children
only), personality changes, psychoses,
Restlessness.Eent: cataracts, increase
intraocular pressure. CV: hypertension. GI:
peptic ulceration, Anorexia, nausea,
vomiting. Derm: acne, decrease wound
Healing, ecchymoses, fragility, hirsutism,
petechiae.Endo: adrenal suppression,
hyperglycemia. F andE: fluid retention (long-
term high doses), hypokalemia,
Hypokalemic alkalosis.Hemat:
thromboembolism, Thrombophlebitis.metab:
weight gain. Ms: Muscle wasting,
osteoporosis, avascular necrosis of Joints,
muscle pain. Misc: cushing oid appearance
(moon face, buffalo hump), increase
susceptibility to infection.
NURSING IMPLICATIONS
Assessment
 These drugs are indicated for many
conditions. Assessinvolved systems
before and periodically duringtherapy.
 Assess for signs of adrenal insufficiency
(hypotension,weight loss, weakness,
nausea, vomiting, anorexia,lethargy,
confusion, restlessness) before
andperiodically during therapy.
 Monitor intake and output ratios and
daily weights.Observe patient for
peripheral edema, steady weightgain,
rales/crackles, or dyspnea. Notify health
careprofessional if these occur.
 Children should have periodic
evaluations of growth.
 Cerebral Edema: Assess for changes in
level ofconsciousness and headache
during therapy.
Diagnoses
 Risk for infection (Side Effects)
 Disturbed body image (Side Effects)
Implementation
 Do not confuse prednisone with
prednisolone. Do not confuse Solu-
Cortef with Solu-Medrol.
 If dose is ordered daily or every other
day, administer in the morning to
coincide with the body’s normal
secretion of cortisol.
 Periods of stress, such as surgery, may
require supplemental systemic
corticosteroids.
 Patients with mild to moderate Crohn’s
disease may be switched from oral
prednisolone without adrenal
insufficiency by gradually decreasing
prednisolone doses and adding
budesonide.
 PO: Administer with meals to minimize
GI irritation.
Patient/Family Teaching
 Instruct patient on correct technique of
medication administration. Advise
patient to take medication as directed.
Take missed doses as soon as
remembered
 unless almost time for next dose. Do not
double doses. Stopping the medication
suddenly may result in adrenal
insufficiency (anorexia, nausea,
weakness, fatigue, dyspnea,
hypotension, hypoglycemia). If these
signs appear, notify health care
professional immediately. This can be
life threatening.
Page | 81
 Advise patient to avoid consumption of
grapefruit juice during therapy with
budesonide or methylprednisolone.
 Corticosteroids cause
immunosuppression and may mask
symptoms of infection. Instruct patient to
avoid people with known contagious
illnesses and to report possible
infections immediately.
Evaluation
 Decrease in presenting symptoms with
minimal systemic side effects.
 Suppression of the inflammatory and
immune responses in autoimmune
disorders, allergic reactions, and
neoplasms.
 Management of symptoms in adrenal
insufficiency.
 Improvement of symptoms/sequelae of
Crohn’s disease and ulcerative colitis
(decreased frequency of liquid stools,
decreased abdominal complaints,
improved sense of well being).
 Improvement in symptoms of ulcerative
colitis. Clinical symptoms usually
improve in 3–5 days. Mucosal
appearance may require 2–3 mo to
improve.
D. DISEASE-MODIFYING
ANTIRHEUMATIC DRUGS (DMARDs)
Drug Classification: DMARDs;
Immunosuppressive Agents
Generic Name: Azathioprine
Brand Name: Imuran
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Renal Allograft Rejection Prevention
PO, IV (Adults and Children): 3–5
mg/kg/day initially; maintenance dose 1–3
mg/kg/day.
Rheumatoid Arthritis
PO (Adults and Children): 1 mg/kg/day for
6–8 wk, increase by 0.5 mg/kg/day q 4 wk
until response or up to 2.5 mg/kg/day, then
decrease by 0.5 mg/kg/day q 4–8 wk to
minimal effective dose.
Inflammatory Bowel Disease (Crohn’s
Disease or Ulcerative Colitis) (unlabeled
use)
PO (Adults and Children): 50 mg once
daily; may increase by 25 mg/day every 1–2
wk as tolerated to target dose of 2–3
mg/kg/day.
Availability (generic available)
Tablets: 50 mg, 75 mg, 100 mg. Injection:
100 mg/vial.
DRUG ACTION
Antagonizes purine metabolism with
subsequent inhibition of DNA and RNA
synthesis.
Therapeutic Effects: Suppression of cell-
mediated immunity and altered antibody
formation.
Pharmacokinetics: Absorption: Readily
absorbed after oral administration.
Distribution: Crosses the placenta. Enters
breast milk in low concentrations.
Metabolism and Excretion: Metabolized to
mercaptopurine, which is further
metabolized (one route is by thiopurine
methyltransferase [TPMT] to form an
inactive metabolite). Minimal renal excretion
of unchanged drug. Half-life: 3 hr.
INTERACTIONS
Drug-drug: Additive myelosuppression with
antineoplastics, cyclosporine, and
myelosuppressive agents. Allopurinol
inhibits the metabolism of azathioprine,
increasing toxicity. Dose of azathioprine
should bepto 25–33% of the usual dose
when used with allopurinol. Maypantibody
response to livevirus vaccines andqthe risk
of adverse reactions.
Drug-Natural Products: Concommitant
use with echinacea and melatonin may
interfere with immunosuppression.
INDICATIONS
Prevention of renal transplant rejection (with
corticosteroids, local radiation, or other
cytotoxic agents). Treatment of severe,
active, erosive rheumatoid arthritis
unresponsive to more conventional therapy.
Unlabeled Use: Management of Crohn’s
disease or ulcerativecolitis.
CONTRAINDICATIONS
Contraindicated in: Hypersensitivity;
Concurrent use of mycophenolate; OB: Has
been shown to cause fetal harm; Lactation:
Appears in breast milk .
Use Cautiously in: Infection;
Malignancies;pbone marrow reserve;
Previous or concurrent radiation therapy;
Other chronic debilitating illnesses; Severe
renal impairment/oliguria (qsensitivity);
Patients with TPMT enzyme deficiency
(substantial dosepare required to avoid
hematologic adverse events); OB: Patients
with childbearing potential; Pedi:qrisk of
hepatosplenic T-cell lymphoma [HSTCL] in
patients with inflammatory bowel disease.
ADVERSE REACTIONS/ SIDE EFFECT
EENT: retinopathy. Resp: pulmonary
edema. GI: anorexia, hepatotoxicity,
nausea, vomiting, diarrhea,mucositis,
pancreatitis. Derm: alopecia, rash. Hemat:
anemia, leukopenia, pancytopenia,
thrombocytopenia. MS: arthralgia. MISC:
malignancy (includingpost-transplant
lymphoma, hstcl, and skincancer), serum
sickness, chills, fever, raynaud’s
phenomenon,retinopathy.
NURSING IMPLICATIONS
Assessment
 Assess for infection (vital signs, sputum,
urine, stool, WBC) during therapy.
Page | 82
 Monitor intake and output and daily
weight. Decreased urine output may
lead to toxicity with this medication.
 Rheumatoid Arthritis: Assess range of
motion; degree of swelling, pain, and
strength in affected joints; and ability to
perform activities of daily living before
and periodically during therapy.
 Lab Test Considerations: Monitor renal,
hepatic, and hematologic functions
before beginning therapy, weekly during
the 1st mo, bimonthly for the next 2–3
mo, and monthly thereafter.
 Leukocyte count of _3000 or platelet
count of _100,000/mm3 may necessitate
a reduction in dose or temporary
discontinuation.
 pin hemoglobin may indicate bone
marrow suppression.
 Hepatotoxicity may be manifested
byqalkaline phosphatase, bilirubin, AST,
ALT, and amylase concentrations.
Usually occurs within 6 mo of transplant,
rarely with rheumatoid arthritis, and is
reversible on discontinuation of
azathioprine.
 May decrease serum and urine uric acid
and plasma albumin.
Diagnoses
 Risk for infection (Indications)
Implementation
 Do Not Confuse Azathioprine With
Azacitidine.
 Protect transplant patients from staff
members and visitors who may carry
infection. Maintain protective isolation as
indicated.
 PO: May be administered with or after
meals or in divided doses to minimize
nausea.
Patient/Family Teaching
 Instruct patient to take azathioprine as
directed. If a dose is missed on a once-
daily regimen, omit dose; if on several-
times-a-day dosing, take as soon as
possible or double next dose. Consult
health care
professional if more than 1 dose is
missed or if vomiting occurs shortly after
dose is taken. Do not discontinue
without consulting health care
professional.
 Advise patient to report unusual
tiredness or weakness; cough or
hoarseness; fever or chills; lower back
or side pain; painful or difficult urination;
severe diarrhea; black, tarry stools;
blood in urine; or transplant rejection to
health care professional immediately.
Evaluation
 Prevention of transplant rejection.
 Decreased stiffness, pain, and swelling
in affected joints in 6–8 wk in
rheumatoid arthritis. Therapy is
discontinued if no improvement in 12
wk.
Drug Classification:
Immunomodulators; Interleukin
Receptor Antagonist
Generic Name: Anakinra
Brand Name: Kineret
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Rheumatoid Arthritis Subcut (Adults 18
yr): 100 mg/day. Neonatal-Onset
Multisystem Inflammatory Disease
Subcut (Adults and Children): 1– 2
mg/kg/day given in 1– 2 divided doses; may
be increased by 0.5– 1 mg/kg/day as
needed (maximum 8 mg/kg/day).
DRUG ACTION
Blocks the destructive effects of interleukin-1
on cartilage and bone resorption by
inhibiting its binding at specific tissue
receptor sites.
Therapeutic Effects: Slowed progression of
rheumatoid arthritis. Reduction in NOMID
symptoms.
Phamacokinetics: Absorption: Well
absorbed (95%) following subcut
administration.
Distribution: Unknown.
Metabolism and Excretion: Unknown.
Half-life: 4– 6 hr.
INTERACTIONS
Drug-drug: Increase risk of serious infection
with TNF blocking agents, such as
etanercept. May decrease antibody
response to and increase the risk of adverse
reactions from vaccines; avoid concurrent
administration of live vaccines.
INDICATIONS
Reduction of the signs and symptoms of
moderately to severely active rheumatoid
arthritis in patients who have failed other
DMARDs (may be used in combination with
other DMARDs other than tumor necrosis
factor [TNF] blocking agents).
Neonatalonset multisystem inflammatory
disease (NOMID).
CONTRAINDICATIONS
Contraindicated in: Active infections;
Hypersensitivity; Hypersensitivity to other
Escherichia coli– derived products.
Use Cautiously in: Other chronic
debilitating illness; Underlying
immunosuppression; Renal impairment; OB,
Lactation, Pedi: Safety not established; Geri:
May be more sensitive to toxicity due to age-
related decline in renal function; increased
incidence of infection in geriatric population.
Exercise Extreme Caution in: Concurrent
use of TNF blocking agents such as
etanercept (higher risk of serious infections).
Page | 83
ADVERSE REACTIONS/ SIDE EFFECT
CNS: headache. GI: diarrhea, nausea.
Hemat: neutropenia. Local: injection site
reactions.Misc: infections, hypersensitivity
reactions (rare).
NURSING INTERVENTIONS
Assessment
 Assess for signs and symptoms of
infection (fever, elevated WBC) prior to
and periodically during therapy. Screen
for latent TB prior to beginning therapy;
treat if screen is positive. Anakinra
should not be instituted in patients with
active infections and should be
discontinued if patient develops a
serious infection.
 Observe patient for hypersensitivity
reactions (urticaria, dyspnea,
hypotension). Discontinue anakinra if
severe reaction occurs. Medications
(antihistamines, acetaminophen,
corticosteroids, epinephrine) and
equipment should be readily available in
the event of a severe reaction.
 Rheumatoid Arthritis: Assess patient’s
range of motion and degree of swelling
and pain in affected joints before and
periodically during therapy.
 Neonatal-Onset Multisystem
Inflammatory Disease: Assess
symptoms of NOMID (fever, rash, joint
pain, vomiting, headache) prior to and
periodically during therapy.
 Lab Test Considerations: Monitor
neutrophil count prior to and during
therapy, then monthly for 3 mo and
quarterly thereafter for up to 1 yr.
Diagnoses
 Impaired physical mobility (Indications)
Acute pain (Indications)
Implementation.
 Administration of higher than
recommended doses did not result in
higher responses.
 Subcut: Administer 1 dose/day. Do not
administer solutions that are discolored
or contain particulate matter or are
beyond expiration date. Provided in
single-use prefilled syringes. Store in
refrigerator; do not freeze. Remove from
refrigerator and allow to reach room
temperature for 30 min prior to injection.
Avoid injecting into areas that are red or
swollen.
Patient/Family Teaching
 Instruct patient in correct technique for
injection and care and disposal of
equipment. Advise patient/parent to read
Patient Information and Instructions for
Use prior to starting therapy and with
each Rx refill, in case of changes.
 Inform patient of the signs and
symptoms of hypersensitivity reactions
and injection site reactions (pain,
erythema, swelling, purities, brusing,
mass, inflammation, dermatitis, edema,
urticaria, vesicles, warmth, and
hemorrhage). Advise patient of
appropriate actions if reactions occur.
 Advise patient to notify health care
professional of all Rx or OTC
medications, vitamins, or herbal
products being taken and to consult with
health care professional before taking
other medications.
 Advise patients not to receive live
vaccines during therapy with anakinra
without consulting health care
professional.
 Advise female patients to notify health
care professional if pregnancy is
planned or suspected, or if breast
feeding.
 Home Care Issues: Instruct patient and
family on preparation and correct
technique for administration of injection
and care and disposal of equipment.
Caution patients and caregivers not to
reuse needles, syringes, or drug
product.
Evaluation
 Reduction of signs and symptoms and
slowed progression of moderate to
severe active rheumatoid arthritis.
 Decrease in signs and symptoms of
NOMID.
Drug Classification:
IMMUNOMODULATORS; TUMOR
NECROSIS FACTOR BLOCKERS
Generic Name: Nabumetone
Brand Name: Relafen
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Crohn’s Disease
Adult: IV 5 mg/kg infused over at least 2 h,
repeat at 2 and 6 wk for fistulizing disease,
then q8wk Child: IV 5 mg/kg at weeks 0, 2,
and 6, then 5 mg/kg q8wk
Rheumatoid Arthritis
Adult: IV 3 mg/kg at weeks 0, 2, and 6, then
q8wk
Ulcerative Colitis
Adult: IV 5 mg/kg at weeks 0, 2, and 6, then
5 mg/kg q8wk
Ankylosing Spondylitis
Adult: IV 5 mg/kg at weeks 0, 2, and 6, then
5 mg/kg q6wk
Page | 84
DRUG ACTION
Neutralizes and prevents the activity of
tumor necrosis factor-alpha (TNF-alpha),
resulting in anti-inflammatory and
antiproliferative activity.
Therapeutic Effects: Decreased pain and
swelling, decreased rate of joint destruction
and improved physical function in
ankylosing spondylitis, rheumatoid or
psoriatic arthritis. Reduction and
maintenance of closure of fistulae in
Crohn’s disease.Decreased symptoms,
maintaining remission and mucosal healing
with decreased corticosteroid use in
ulcerative colitis. Decrease in induration,
scaling and erythema of psoriatic lesions.
Pharmacokinetics: Absorption: IV
administration results in complete
bioavailability.
Distribution: Predominantly distributed
within the vascular compartment.
Metabolism and Excretion: Unknown.
Half-life: 9.5 days.
INTERACTIONS
Drug-drug: Increased hypoglycemic
effectsof insulin with MAOIs, beta blockers,
salicylates, or alcohol; Delayed recovery
fromhypoglycemic episodes and masked
signs andsymptoms of hypoglycemia if
taken with beta adrenergic blocking drugs.
Decreased effectivenessof insulin with
corticosteroids, diuretics,atypical
antipsychotics
Drug-alternative therapy: Increasedrisk of
hypoglycemia if taken with juniperberries,
ginseng, garlic, fenugreek,
coriander,dandelion root, celery
INDICATIONS
Active rheumatoid arthritis (moderate to
severe, with methotrexate).Active Crohn’s
disease (moderate to severe).Active
psoriatic arthritis.Active ankylosing
spondylitis.Active ulcerative colitis
(moderate to severe) with inadequate
response to conventional therapy: reducing
signs and symptoms, and inducing and
maintaining clinical remission and mucosal
healing, and eliminating corticosteroid use.
Plaque psoriasis (chronic severe).
CONTRAINDICATIONS
Contraindicated in: Severe hypersensitivity
to infliximab; serious infection, sepsis;
murine protein hypersensitivity; lactation.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: fatigue, headache, anxiety,
depression, dizziness, insomnia. EENT:
conjunctivitis. Resp: upper respiratory tract
infection, bronchitis, cough, dyspnea,
laryngitis, pharyngitis, respiratory tract
allergic reaction, rhinitis, sinusitis. CV: chest
pain, hypertension, hypotension, pericardial
effusion, tachycardia, HF. GI:abdominal
pain, nausea, vomiting, constipation,
diarrhea, dyspepsia, flatulence,
hepatotoxicity, intestinal obstruction, oral
pain, tooth pain, ulcerative stomatitis.
GU: dysuria, urinary frequency, urinary tract
infection. Derm: acne, alopecia, dry skin,
ecchymosis, eczema, erythema, flushing,
hematoma, hot flashes, pruritus, psoriasis,
rash, sweating, urticaria.
Hemat:neutropenia. MS: arthralgia, arthritis,
back pain, involuntary muscle contractions,
myalgia. Neuro: paresthesia. Misc:
infections (including reactivation tuberculosis
and other opportunistic infections due to
bacterial, invasive fungal, viral,
mycobacterial, and parasitic pathogens),
malignancy (including lymphoma,
hstcl, leukemia, and skin cancer), fever,
Sarcoidosis, infusion reactions, chills, flu-like
syndrome, herpes simplex, herpes zoster,
hypersensitivity reactions, lupus-like
syndrome, moniliasis, pain, peripheral
edema, vasculitis.
NURSING INTERVENTIONS
Assessment
 Assess for infusion-related reactions
(fever, chills, urticaria, pruritus) during
and for 2 hr after infusion. Symptoms
usually resolve when infusion is
discontinued. Reactions are more
common after 1st or 2nd infusion.
Frequency of reactions may be reduced
with immunosuppressant agents.
 Monitor patients who develop a new
infection while taking infliximab closely.
Discontinue therapy in patients who
develop a serious infection or sepsis. Do
not initiate therapy in patients with active
infections.
 Assess for signs and symptoms of
systemic infections (fever, malaise,
weight loss, sweats, cough, dyspnea,
pulmonary infiltrates, serious systemic
illness with or without concomitant
shock). Ascertain if patient lives in or
has traveled to areas of endemic
mycoses. Consider empiric antifungal
treatment for patients at risk of
histoplasmosis and other invasive fungal
infections until the pathogens are
identified. Consult with an infectious
diseases specialist. Consider stopping
infliximab until the infection has been
diagnosed and adequately treated.
Diagnoses
 Chronic pain (Indications)
 Diarrhea (Indications)
Implementation
 Do not confuse infliximab with rituximab.
Patient/Family Teaching
 Advise patient that adverse reactions
(myalgia, rash, fever, polyarthralgia,
pruritus) may occur 3–12 days after
delayed (_2 yr) retreatment with
infliximab. Symptoms usually decrease
or resolve within 1–3 days. Instruct
patient to notify health care professional
if symptoms occur.
Page | 85
 May cause dizziness. Caution patient to
avoid driving or other activities requiring
alertness until response to medication is
known.
 Advise patient to notify health care
professional promptly if symptoms of
fungal infection occur.
 Advise patient of risk of malignancies
such as hepatosplenic T-cell lymphoma.
Instruct patient to report signs and
symptoms (splenomegaly,
hepatomegaly, abdominal pain,
persistent fever, night sweats, weight
loss) to health care professional
 promptly.
 Advise patient to examine skin
periodically during therapy and notify
health care professional of any changes
in appearance of skin or growths on
skin.
Evaluation
 Decreased pain and swelling with
decreased rate ofjoint destruction and
improved physical function inpatients
with ankylosing spondylitis, psoriatic, or
rheumatoid arthritis.
 Decrease in the signs and symptoms of
Crohn’s disease and a decrease in the
number of draining enterocutaneous
fistulas. Decreased symptoms,
maintaining remission and mucosal
healing with decreased corticosteroid
use in ulcerative colitis.
 Decrease in induration, scaling and
erythema of psoriatic lesions.
Drug Classification:
Immunomodulators; Monoclonal
Antibodies
Generic Name: Rituximab
Brand Name: Rituxan
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Non-Hodgkin’s Lymphoma
Adult: IV Varies based on disease
specific parameters, consult package insert
Rheumatoid Arthritis
Adult: IV 1000 mg on days 1 and 15 (with
methotrexate) CLL
Adult: IV 375 mg/m2 on day 1 then 500
mg/m2 (in combination with fludarabine
/cyclophosphamide) on day 1 of cycles 2–6.
Wegener’s Granulomatosis/
Microscopic Polyangiitis
Adult: IV 375 mg/m2 weekly × 4 wk
DRUG ACTION
Binds to the CD20 antigen on the surface of
lymphoma cells, preventing the activation
process for cell cycle initiation and
differentiation.
Therapeutic Effects: Death of lymphoma
cells. Prolonged progression-free survival in
CLL.Reduced signs and symptoms of
rheumatoid arthritis.Achievement of
complete remission in GPA and MPA.
Pharmacokinetics: Absorption: IV
administration results in complete
bioavailability.
Distribution: Binds specifically to CD20
binding sites on lymphoma cells.
Metabolism and Excretion: Unknown.
Half-life: 59.8–174 hr (depending on tumor
burden).
INTERACTIONS
Drug-drug: Antihypertensive agents should
be stopped 12 h prior to avoid excessive
hypotension; cisplatin may cause additive
nephrotoxicity.
INDICATIONS
Treatment of mild to moderate dementia of
the Alzheimer’s type; Treatment of mild to
moderate dementia associated with
Parkinson’s disease
Unlabeled use: Treatment of behavioral
effects of Lewy-body dementia
CONTRAINDICATIONS
Contraindicated in: Hypersensitivity to
murine (mouse) proteins; OB: Can pass
placental barrier potentially causing fetal B-
cell depletion. Give only if clearly needed;
Lactation: Potential for immunosuppression
in infant. Discontinue nursing.
Use Cautiously in: Pre-existing bone
marrow depression; Hepatitis B infection
(may reactivate infection during and for
several months after treatment); Systemic
lupus erythematosus (may cause fatal
progressive multifocal
leukoencephalopathy); HIV infection
(may increase risk of HIV-associated
lymphoma); Pedi: Safety not established.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: progressive multifocal
leukoencephalopathy, Headache. Resp:
bronchospasm, cough, dyspnea.
CV: Arrhythmias, hypotension, peripheral
edema. GI: abdominal pain, altered taste,
dyspepsia. GU: renal
failure. Derm:Mucocutaneous Skin
Reactions, flushing, urticaria. Endo:
hyperglycemia. F and E:hypocalcemia.
Hemat: anemia, Neutropenia,
Thrombocytopenia. MS: arthralgia, back
pain. Misc: allergic reactions including
Anaphylaxis And Angioedema,
Hepatitis B Reactivation, Infusion Reactions,
Tumor Lysis Syndrome, fever/chills/rigors
(infusion related), infections.
NURSING INTERVENTIONS
Assessment
 Monitor patient for fever, chills/rigors,
nausea, urticaria, fatigue, headache,
pruritus, bronchospasm, dyspnea,
sensation of tongue or throat swelling,
Page | 86
 rhinitis, vomiting, hypotension, flushing,
and pain at disease sites. Infusion-
related events occur frequently within 30
min–2 hr of beginning first infusion and
may resolve with slowing or
discontinuing infusion and treatment
with IV saline, diphenhydramine, and
acetaminophen.
 Monitor ECG during and immediately
after infusion in patients with pre-
existing cardiac conditions (arrhythmias,
angina) or patients who have developed
arrhythmias during previous infusions of
rituximab. Life-threatening arrhythmias
may occur.
 Assess for signs of progressive
multifocal leukoencephalopathy
(hemiparesis, apathy, confusion,
cognitive deficiencies, and ataxia)
periodically during therapy.
 Assess for infection during and for 1 yr
after therapy. Bacterial, fungal, and new
or reactivated viral infections may occur.
Screen patient for hepatitis B infection
prior to therapy. Discontinue rituximab
and any concomitant chemotherapy in
patients who develop viral hepatitis or
other serious infections, and institute
appropriate treatment.
Diagnoses
 Risk for infection (Side Effects)
Implementation
 Do not confuse rituximab with infliximab.
 Transient hypotension may occur during
infusion; antihypertensive medications
may be held for 12 hr before infusion.
 Rheumatoid Arthritis: Administer 100 mg
methylprednisolone IV or equivalent 30
min prior to each infusion to minimize
infusion reactions.
 GPA and MPA: Administer
methylprednisolone 1000 mg IV per day
for 1 to 3 days followed by oral
prednisone 1 mg/kg/day (not to exceed
80 mg/day and tapered per clinical
need) to treat severe vasculitis
symptoms. Begin regimen within 14
days prior to or with the initiation of
rituximab and may continue during and
after the 4 wk course of rituximab
treatment.
 Prophylaxis against Pneumocystis
jiroveci pneumonia and herpes virus
recommended during treatment and for
up to 12 mo following treatment as
appropriate for patients with CLL, and
during and for at least 6 mo following
last rituximab infusion for patients with
WG and MPA.
Patient/Family Teaching
 Inform patient of the purpose of the
medication. Advise patient to read the
Medication Guide prior to starting
therapy and before each infusion in case
of changes.
 Advise patient to report infusion-related
events or symptoms of hypersensitivity
reactions immediately.
 Advise patient to consult health care
professional prior to receiving any
vaccinations.
 Instruct patient to use effective
contraception during therapy and for 12
mo following therapy, and to avoid
breast feeding.
Evaluation
 Decrease in spread of malignancy.
 Reduced signs and symptoms of
rheumatoid arthritis.
 Achievement of complete remission in
GPA and MPA.
Drug Classification :
IMMUNOMODULATORS;SELECTIVE
T CELL COSTIMULATION
MODULATOR
Generic Name: Abatacept
Brand Name: Orencia
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Rheumatoid Arthritis
Adult: IV Initial dose: Weight less
than 60 kg: 500 mg; 60–100 kg: 750 mg;
weight greater than 100 kg: 1000 mg. Give
dose atwk 2 and 4, then monthly.
Juvenile Idiopathic Arthritis
Child (at least 6 y): IVWeight less than 75
kg: 10 mg/kg, repeat atwk 2 and 4, then
monthly (max:1000 mg); weight 75–100 kg:
750 mg at wk 2 and 4, then monthly; weight
at least 100 kg: 1000 mg at wk 2 and 4, then
monthly.
DRUG ACTION
Therapeutic actions: Interferes with
platelet membrane function by inhibiting
fibrinogen binding and platelet–
platelet interactions; inhibits platelet
aggregation and prolongs bleeding time;
effect is irreversible for life of the platelet.
Pharmacokinetics: Metabolism: Cellular;
T 1/2: less than 10 min, then 30 min
Distribution: Crosses placenta; may enter
breast milk Excretion: Unknown
INTERACTIONS
Drug-drug: Risk of increased bleeding
ifcombined with anticoagulants, antiplatelets,
orthrombolytics; monitor patient accordingly.
INDICATIONS
 Adjunct to percutaneous coronary
intervention (PCI) for the prevention of
cardiac ischemic complications in
patients undergoing PCI and with
unstable angina not responding to
conventional therapy when PCI is
planned within 24 hr; intended to be
used with heparin and aspirin therapy
Page | 87
 Unlabeled uses: Early treatment of
acute MI or acute ischemic stroke
CONTRAINDICATIONS
Contraindicated in: Known hypersensitivity
to abatacept, live vaccines; active infections;
coadministration with anakinra, TNF
antagonists, other biologic RA therapy;
lactation.
ADVERSE REACTION/SIDE EFFECT
Side effects/adverse reaction: cns:
headache, dizziness. Misc: hypersensitivity
reactions including anaphylaxis, infections,
infusion-related events.
NURSING IMPLICATIONS
Assessment
 Assess range of motion, degree of
swelling, and pain in affected joints
before and periodically during therapy.
 Assess for infusion-related reaction
(dizziness, headache, hypertension) and
signs of allergic reaction (hypotension,
urticaria, dyspnea). Infusion-related
reactions usually occur within 1 hr of
start of infusion. Keep epinephrine, an
antihistamine, and resuscitation
equipment close by in case of an
anaphylactic reaction.
Diagnosis
 Impaired physical mobility (Indications)
 Acute pain (Indications)
Implementation
 Subcut: Remove prefilled syringe from
refrigerator and allow to reach room
temperature for 30–60 min; do not use
other methods to warm solution. Leave
needle cover on during warming.
Inspect solution; do not administer
solutions that are discolored, contain
particulate matter; are expired, or do not
have the correct amount of fluid in
syringe. Front of thigh is the preferred
site; abdomen except for 2 inches from
navel or upper arm if administered by
caregiver, may also be used.
 Pinch skin and inject at a 45_ angle. Do
not rub injection site. Rotate each
injection at least 1 inch from last
injection, avoid areas where skin is
tender, bruised, red, or hard, or contains
scars or stretchmarks.
Evaluation
 Reduction in symptoms of rheumatoid
arthritis.
Drug Classification:
IMMUNOMODULATORS;JANUS
KINASE INHIBITORS (JAK)
Generic Name: Tofacitinib
Brand Name: Xeljanz
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 5 mg twice daily; Concurrent
use of strong CYP3A4 inhibitors or
moderate CYP3A4 inhibitors/ strong
CYP2C19 inhibitors—5 mg oncedaily;
dosage adjustments recommended for
neutropenia,anemia or infection.
Renal Impairment
PO (Adults): Moderate to severe renal
impairment— 5 mg once daily.
Hepatic Impairment
PO (Adults): Moderate hepatic
impairment—5 mg once daily.
Availability
Tablets: 5 mg.
DRUG ACTION
Acts as a Janus kinase (JAK) inhibitor.
Some results of inhibition include decreased
hematopoiesis and immune cell function.
Decreases circulating killer cells, increases
in B cell count and decreases serum C
reactive protein (CRP).
Therapeutic Effects: Improvement
in clinical and symptomatic parameters of
rheumatoid arthritis.
Pharmacokinetics: Absorption: well
absorbed following oral administration
(74%).
Distribution: Distributes equally between
red blood cells and plasma.
Metabolism and Excretion: 70%
metabolized by the liver (primarily CYP3A4
with some contribution from CYP2C19).
30% renal excretion of the parent drug.
Half-life: 3 hr.
INTERACTIONS
Drug-drug: May increase risk of adverse
reactions and decrease antibody response
to live vaccines (avoid concurrent use).
Blood levels and effects may be increase by
strong CYP3A4 inhibitors including
ketoconazole or moderate CYP3A4
inhibitors/strong CYP2C19 inhibitors
including fluconazole; dose decrease
recommended. Blood levels and
effectiveness may be decreasedstrong
CYP3A4 inducers including rifampin.
Increase risk of immunosuppression when
used concurrently with other potent
immunosuppressants including azathioprine,
cyclosporine, tacrolimus, antineoplastics or
radiation therapy.
Herbal: St. John’s wort may decrease the
levels of tofacitinib.
INDICATIONS
Treatment of adults with moderately to
severely active rheumatoid arthritis who
have had an inadequate response/
intolerance to methotrexate. Can be used as
monotherapy or with methotrexate or other
nonbiologic disease-modifying antirheumatic
drugs (DMARDs). Not be used with biologic
DMARDs or potent immunosuppressants
including azathioprine and cyclosporine.
Page | 88
CONTRAINDICATIONS
Contraindicated in: Active infection;
Administration of live vaccines; Severe
hepatic impairment; Lymphocyte count _500
cells/mm3, absolute neutrophil count (ANC)
1000 cells/mm3, or hemoglobin levels
9g/dL; Lactation: Should not be used in
nursing mothers.
Use Cautiously in: Patients with risk of
gastric perforation; Geri: Infection risk may
be increase; OB: Use during pregnancy only
if potential benefit justifies potential fetal risk;
Pedi: Safety and effectiveness not
established.
ADVERSE REACTIONS/ SIDE EFFECT
Cns: Fatigue, Headache, Insomnia. Cv:
Peripheral Edema. Gi: Gastric Perforation,
Abdominal Pain, Diarrhea, Dyspepsia,
Gastritis, increase liver Enzymes, Vomiting.
Gu: increase serum Creatinine. Derm:
Erythema, Pruritus, Rash. F And E:
Dehydration.Metab: increase lipids. Ms:
Arthralgia, Joint Swelling, Musculoskeletal
Pain, Tendonitis.Neuro: Paresthesia. Misc:
Serious Infections Including Tuberculosis,
Invasive Fungal Infections, Bacterial,
Viral, And Other Infections Due To
Opportunistic Pathogens,Qrisk Of
Malignancy, Fever.
NURSING IMPLICATIONS
Assessment
 Assess pain and range of motion before
and periodically during therapy.
 Assess for signs of infection (fever,
dyspnea, flu-like symptoms, frequent or
painful urination, redness or swelling at
the site of a wound), including
tuberculosis, prior to and periodically
during therapy. Tofacitinib is
contraindicated in patients with active
infection. New infections should be
monitored closely; most common are
upper respiratory tract infections,
bronchitis, and urinary tract infections.
Infections may be fatal, especially in
patients taking immunosuppressive
therapy.
 Assess for signs and symptoms of
systemic fungal infections (fever,
malaise, weight loss, sweats, cough,
dypsnea, pulmonary infiltrates, serious
systemic illness with or without
concomitant shock). Ascertain if patient
lives in or has traveled to areas of
endemic mycoses. Consider empiric
antifungal treatment for patients at risk
of histoplasmosis and other invasive
fungal infections until the pathogens are
identified. Consult with an infectious
diseases specialist. Consider stopping
tofacitinib until the infection has been
diagnosed and adequately treated.
 Lab Test Considerations: Monitor CBC
prior to and periodically during therapy.
Do not initiate tofacitinib in patients with
lymphocyte count _500 cells/mm3, an
absolute neutrophil count (ANC) _1000
cells/mm3, or who have hemoglobin
level _9 g/dL..
Diagnoses
 Impaired physical mobility (Indications)
 Risk for infection (Adverse Reactions)
Implementation
 Administer a tuberculin skin test prior to
administrationof tofacitinib. Patients with
active latent TBshould be treated for TB
prior to therapy.
 Immunizations should be current prior to
initiating. Patients on tofacitinib should
not receivelive vaccines.
 PO: Administer twice daily without
regard to food.
Patient/Family Teaching
 Instruct patient to take tofacitinib as
directed. Advisepatient to read
Medication Guide before startingand
with each Rx refill in case of changes.
 Caution patient to notify health care
professionalimmediately if signs of
infection (fever, sweating,chills, muscle
aches, cough, shortness of breath,blood
in phlegm, weight loss, warm, red, or
painfulskin or sores, diarrhea or
stomach pain, burningon urination or
urinating more often than normal,feeling
very tired) or stomach or intestinal
perforation(fever, stomach-area pain
that does not goaway, change in bowel
habits) occur.
 Advise patient to notify health care
professional ofall Rx or OTC
medications, vitamins, or herbalproducts
being taken and to consult with
healthcare professional before taking
other medications.
 Instruct patient to notify health care
professional ofmedication regimen prior
to treatment or surgery.
 Inform patient of increased risk of
lymphoma andother cancers.
Evaluation
 Decreased pain and swelling with
improved physicalfunctioning and
decreased rate of joint destructionin
patients with rheumatoid arthritis.
E. ANTIMALARIALS
Drug Classification: ANTIMALARIALS
Generic Name: Hydroxychloroquine
Brand Name: Plaquenil
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): Suppression or
chemoprophylaxis—310 mg once weekly;
start 1–2
wk prior to entering malarious area; continue
for 4 wk after leaving area. Treatment—620
Page | 89
mg, then 310 mg at 6 hr, 24 hr, and 48 hr
after initial dose.
PO (Children): Suppression or
chemoprophylaxis—5 mg/kg once weekly;
start
1–2 wk prior to entering malarious area;
continue for 4 wk after leaving area.
Treatment—10 mg/kg initially, then 5 mg/kg
at 6–8 hr, 24 hr, and 48 hr after initial dose.
DRUG ACTION
Inhibits protein synthesis in susceptible
organisms by inhibiting DNA and RNA
polymerase.
TherapeuticEffects: Death of plasmodia
responsible for causing malaria. Also has
anti-inflammatory properties.
Pharmacokinetics: Absorption: highly
variable (31–100%) following oral
administation.
Distribution: widely distributed; high
concentrations in RBCs; crosses the
placenta; excreted into breast milk.
Metabolism and Excretion: Partially
metabolized by the liver to active
metabolites; partially excreted unchanged by
the kidneys. Half-life: 72–120 hr.
INTERACTIONS
Drug-drug: May increase the risk of
hepatotoxicity when administered with
hepatotoxic drugs. May increase the risk of
hematologic toxicity when administered with
penicillamine. May increase risk of
dermatitis when administered with other
agents having dermatologic toxicity. May
decrease serum titers of rabies antibody
when given concurrently with human diploid
cell rabies vaccine. Urinary acidifiers may
increase renal excretion. May increase
levels of digoxin.
INDICATIONS
Suppression / chemoprophylaxis of
malaria.Treatment of severe rheumatoid
arthritis/systemic lupus erythematosus.
CONTRAINDICATIONS
Contraindicated in: Hypersensitivity to
hydroxychloroquine or chloroquine; Previous
visual damage from hydroxychloroquine or
chloroquine.
Use Cautiously in: Concurrent use of
hepatotoxic drugs; History of liver disease,
alcoholism or renal impairment; Severe
neurological disorders; Severe blood
disorders; Retinal or visual field changes;
G6PD deficiency; Psoriasis; Bone marrow
depression; Obesity (determine dose by
ideal body weight); OB, Lactation: Avoid use
unless treating/preventing malaria or treating
amebic abscess; Pedi: Long-term use may
increase sensitivity to effects.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: Seizures, aggressiveness, anxiety,
apathy, confusion, fatigue, headache,
irritability, personality changes, psychoses.
EENT: keratopathy, ototoxicity, retinopathy,
tinnitus, visual disturbances. CV: ECG
changes, hypotension. GI: abdominal
cramps, anorexia, diarrhea, epigastric
discomfort, nausea, vomiting,
hepatic failure. Derm: bleaching of hair,
alopecia, hyperpigmentation,
photosensitivity, Stevens-Johnson
syndrome. Hemat: agranulocytosis,
aplastic anemia, leukopenia,
thrombocytopenia. Neuro: neuromyopathy,
peripheral neuritis.
NURSING IMPLICATIONS
Assessment
 Assess deep tendon reflexes
periodically to determinemuscle
weakness. Therapy may be
discontinuedshould this occur.
 Patients on prolonged high-dose therapy
shouldhave eye exams prior to and
every 3–6 mo duringtherapy to detect
retinal damage.
 Malaria or Lupus Erythematosus:
Assess patientfor improvement in signs
and symptoms of conditiondaily
throughout course of therapy.
 Rheumatoid Arthritis: Assess patient
monthly forpain, swelling, and range of
motion.
 Lab Test Considerations: Monitor CBC
andplatelet count periodically throughout
therapy. Maycause decreased RBC,
WBC, and platelet counts. Ifsevere
decreases occur that are not related to
thedisease process, hydroxychloroquine
should be discontinued.
Diagnoses
 Risk for infection (Indications)
 Chronic pain (Indications)
Implementation
 PO: Administer with milk or meals to
minimize GI distress.
 Tablets may be crushed and placed
inside empty capsules for patients with
difficulty swallowing. Contents of
capsules may also be mixed with a
teaspoonful of jam, jelly, or Jell-O prior
to administration.
 Malaria Prophylaxis:
Hydroxychloroquine therapy should be
started 2 wk prior to potential exposure
and continued for 4–6 wk after leaving
the malarious area.
Patient/Family Teaching
 Instruct patient to take medication
exactly as directed and continue full
course of therapy even if feeling better.
Missed doses should be taken as soon
as remembered unless it is almost time
for next dose. Do not double doses.
 Advise patients to avoid use of alcohol
while taking hydroxychloroquine.
 Caution patient to keep
hydroxychloroquine out of reach of
Page | 90
 children; fatalities have occurred with
ingestion of 3 or 4 tablets.
Evaluation
 Prevention or resolution of malaria.
 Improvement in signs and symptoms of
rheumatoid arthritis.
 Improvement in symptoms of lupus
erythematosus.
F. ANTIGOUT DRUGS
Drug Classification:
ANTIINFLAMMATORY GOUT DRUGS
Generic Name: Colchicine
Brand Name: Colcrys
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Acute Gouty Flare
Adult: PO 1.2 mg followed by 0.6 mg one
hour later (max: 1.8 mg in one hour).
Prophylaxis
Adult: PO 0.6 mg once or twice daily. Adult
with concurrent CYP3A4 inhibitor use PO
0.3 mg every day or every other day
Familial Mediterranean Fever
Adult: PO 1.2–2.4 mg in 1 or 2 doses.
Renal Impairment Dosage
Adjustment
CrCl 30 mL/min: Use 50% of normal dose
DRUG ACTION
Interferes with the functions of WBCs in
initiating and perpetuating the inflammatory
response to monosodium urate crystals.
Therapeutic Effects: Decreased pain and
inflammation in acute attacks of gout.
Reduced number of attacks of gout and
familial Mediterranean fever.
Pharmacokinetics: Absorption: absorbed
from the GI tract, then re-enters GI tract
from biliary secretions, when more
absorption may occur; bioavailability_45%.
Distribution: Concentrates in WBCs.
Metabolism and Excretion: Partially
metabolized by the liver by CYP3A4; also a
substrate for P-glycoprotein. Secreted in bile
back into GI tract; eliminated in the feces.
40–65% excreted in the urine as unchanged
drug. Half-life: 27–31 hr.
INTERACTIONS
Drug-drug: May decrease intestinal
absorption of vitamin B12. Do not use with
protease inhibitors. avoid CYP3A4 inhibitors.
Drug-Food : Grapefruit juice mayqlevels
and risk of toxicity;pcolchicine dose.
INDICATIONS
Prophylaxis and treatment of acute attacks
of gouty arthritis.Familial Mediterranean
fever.UnlabeledUse: Treatment of hepatic
cirrhosis.
CONTRAINDICATIONS
Contraindicated in: Hypersensitivity; Use
of P-glycoprotein inhibitors or strong
CYP3A4 inhibitors in patients with renal or
hepatic impairment.
Use Cautiously in: Geri: Elderly or
debilitated patients (toxicity may be
cumulative); Renal impairment (dose
decrease suggested if CCr _80 mL/min);
OB, Lactation, Pedi: Safety not established
for gout.
ADVERSE REACTIONS/ SIDE EFFECT
Gi: Diarrhea, Nausea, Vomiting, Abdominal
Pain. Derm: Alopecia. Hemat:
Agranulocytosis, Aplastic Anemia,
Leukopenia, Thrombocytopenia. Neuro:
Peripheral Neuritis.
NURSING IMPLICATIONS
Assessment
 Monitor intake and output ratios. Fluids
should beencouraged to promote a
urinary output of at least2000 mL/day.
 Gout: Assess involved joints for pain,
mobility, andedema throughout therapy.
During initiation oftherapy, monitor for
drug response every 1–2 hr.
 Familial Mediterranean fever: Assess for
signsand symptoms of familial
Mediterranean fever (abdominalpain,
chest pain, fever, chills, recurrentjoint
pain, red and swollen skin lesions)
periodicallyduring therapy.
 Lab Test Considerations: In patients
receivingprolonged therapy, monitor
baseline and periodicCBC; report
significantpin values. May
causepplatelet count, leukopenia,
aplastic anemia, andagranulocytosis.
 May causeqin AST and alkaline
phosphatase.
 May cause false-positive results for
urine hemoglobin.
 May interfere with results of urinary 17-
hydroxycorticosteroidconcentrations.
Diagnoses
 Acute pain (Indications)
 Impaired walking (Indications)
Implementation
 Do not confuse colchicine with
Cortrosyn.
 Intermittent therapy with 3 days between
courses may be used to decrease risk of
toxicity.
 PO: Administer without regard to meals.
Patient/Family Teaching
 Review medication administration
schedule. Take missed doses as soon
as remembered unless almost time for
next dose. Do not double doses.
 Instruct patients taking prophylactic
doses not to increase to therapeutic
doses during an acute attack to prevent
toxicity. An NSAID or corticosteroid,
preferably via intrasynovial injection,
should be used to treat acute attacks.
Page | 91
 Advise patient to avoid grapefruit and
grapefruit juice during therapy; may
increase risk of toxicity.
 Advise patient to follow
recommendations of health care
professional regarding weight loss, diet,
and alcohol consumption.
 Instruct patient to report muscle pain or
weakness, tingling or numbness in
fingers or toes; pale or gray color to lips,
tongue, or palms of hands; severe
diarrhea or vomiting; unusual bleeding,
bruising, sore throat, fatigue, malaise, or
weakness or tiredness promptly.
Medication should be withheld if
symptoms of toxicity occur.
 Instruct patient to notify health care
professional of all Rx or OTC
medications, vitamins, or herbal
products being taken and to notify health
care professional before taking any
other Rx, OTC, or herbal products.
Evaluation
 Decrease in pain and swelling in
affected joints within 12 hr.
 Relief of symptoms within 24–48 hr.
 Prevention of acute gout attacks.
 Reduced number of attacks of familial
Mediterranean fever.
Drug Classification: URIC ACID
INHIBITORS
Generic Name: Allopurinol
Brand Name: Zyloprim, Aloprim
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Treatment of Hyperuricemia
Adult /Adolescent/Child (over 10):
PO 600–800 mg/day (in divided
doses) IV 200–400 mg/m2/day
(max: 600 mg/day) in 1–4 divided
doses
Child: PO 6–10 years: 300 mg/
day(less than 6 years): PO 150
mg/dayIV 200 mg/m2/day in
1–4 divided doses
Treatment of Recurrent Renal
Calculi
Adult: PO 200–300 daily (may
divide dose)
Renal Impairment Dosage
Adjustment
CrCl 10–20 ml/min: PO 200 mg/
dayIV 100 mg; 3–9 mL/min:
100 mg daily; less than 3 ml/min:
100 mg with extended interval
between doses (24 h or more)
Hemodialysis Dosage Adjustment
Administer dose after dialysis or use
50% supplemental dose.
DRUG ACTION
Inhibits the production of uric acid by
inhibiting the action of xanthine oxidase.
Therapeutic Effects: Lowering of serum
uric acid levels.
INTERACTIONS
Drug-drug: Use with mercaptopurine and
azathioprineqbone marrow depressant
properties— doses of these drugs should be
decrease. Use with ampicillin or amoxicillin
increase risk of rash. Use with oral
hypoglycemic agents and warfarin increase
effects of these drugs. Use with thiazide
diuretics or ACE inhibitors increase risk of
hypersensitivity reactions. Large doses of
allopurinol may increase risk of theophylline
toxicity. May increase cyclosporine levels.
Pharmacokinetics: Absorption: well
absorbed (80%) following oral
administration.
Distribution: Widely distributed in tissue
and breast milk. Protein Binding: _1%. A
Metabolism and Excretion: Metabolized to
oxypurinol, an active compound with a long
half-life. 12% excreted unchanged, 76%
excreted as oxypurinol. Half-life: 1–3 hr
(oxypurinol 18–30 hr). INDICATIONS PO:
Prevention of attack of gouty arthritis and
nephropathy. PO, IV: Treatment of
secondary hyperuricemia, which may occur
during treatment of tumors or leukemias.
CONTRAINDICATIONS
Contraindicated in: Hypersensitivity.
Use Cautiously in: Acute attacks of gout;
Renal insufficiency (doseprequired if CCr
_20 mL/min); Dehydration (adequate
hydration necessary); OB, Lactation: Rarely
used; Geri: Begin at lower end of dosage
range.
ADVERSE REACTIONS/ SIDE EFFECT
CV: hypotension, flushing, hypertension,
bradycardia, and heart failure (reported with
IV administration). CNS: drowsiness. GI:
diarrhea, hepatitis, nausea, vomiting. GU:
renal failure, hematuria. Derm: rash
(discontinue drug at first sign of rash),
urticaria. Hemat: bone marrow depression.
Misc: hypersensitivityreactions.
NURSING IMPLICATIONS
Assessment
 Monitor intake and output ratios.
Decreased kidney function can cause
drug accumulation and toxic effects.
Ensure that patient maintains adequate
fluid intake (minimum 2500–3000
mL/day) to minimize risk of kidney stone
formation.
 Assess patient for rash or more severe
hypersensitivity reactions. Discontinue
allopurinol immediately if rash occurs.
Therapy should be discontinued
permanently if reaction is severe.
Therapy may be reinstated after a mild
reaction has subsided, at a lower dose
(50 mg/day with very gradual titration). If
skin rash recurs, discontinue
permanently.
Page | 92
 Gout: Monitor for joint pain and swelling.
Addition of colchicine or NSAIDs may be
necessary for acute attacks.
Prophylactic doses of colchicine or an
NSAID should be administered
concurrently during the first 3–6 mo of
therapy because of an increased
frequency of acute attacks of gouty
arthritis during early therapy.
 Lab Test Considerations: Serum and
urine uric acid levels usually begin top2–
3 days after initiation of oral therapy.
 Monitor blood glucose in patients
receiving oral hypoglycemic agents. May
cause hypoglycemia.
Diagnoses
 Acute pain (Indications)
Implementation
 PO: May be administered after milk or
meals to minimize gastric irritation; give
with plenty of fluid. May be crushed and
given with fluid or mixed with food for
patients who have difficulty swallowing.
Patient/Family Teaching
 Instruct patient to take allopurinol as
directed. Take missed doses as soon as
remembered. If dosing schedule is once
daily, do not take if remembered the
next day. If dosing schedule is more
than once a day, take up to 300 mg for
the next dose.
 Instruct patient to continue taking
allopurinol along with an NSAID or
colchicine during an acute attack of
gout. Allopurinol helps prevent, but does
not relieve, acute gout attacks.
 Alkaline diet may be ordered. Urinary
acidification with large doses of vitamin
C or other acids may increase kidney
stone formation (see Appendix M).
Advise patient of need for increased
fluid intake.
 May occasionally cause drowsiness.
Caution patient to avoid driving or other
activities requiring alertness until
response to drug is known.
 Instruct patient to report skin rash, blood
in urine, or influenza symptoms (chills,
fever, muscle aches and pains, nausea,
or vomiting) to health care professional
immediately; skin rash may indicate
hypersensitivity.
 Advise patient that large amounts of
alcohol increase uric acid concentrations
and may decrease the effectiveness of
allopurinol.
 Emphasize the importance of follow-up
exams to monitor effectiveness and side
effects.
Evaluation
 Decreased serum and urinary uric acid
levels. May take 2–6 wk to observe
clinical improvement in patients treated
for gout.
Drug Classification: Uricosurics
Generic Name: Probenecid
Brand Name: Benemid
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Gout
Adult: PO 250 mg b.i.d. for 1 wk,
then 500 mg b.i.d. (max: 3 g/day)
Adjunct for Penicillin or
Cephalosporin Therapy
Adult: PO 500 mg q.i.d. or 1 g
with single dose therapy (e.g., gonorrhea)
Child (2–14 y or weight less than 50 kg):
PO 25–40 mg/kg/day in 4 divided doses
DRUG ACTION & THERAPEUTIC EFFECT
Competitively inhibits renal tubular
reabsorption of uric acid, thereby promoting
its excretion and reducing serum urate
levels. Prevents formation of new
tophaceousdeposits and uric acid buildup
in the serum and tissues. As an additive to
penicillin, it increases serum concentration
of penicillins and prolongs their serum
concentration.
Pharmacokinetics: Absorption: readily
from gi tract. Onset: 30 min. Peak: 2–4 h.
Duration: 8 h. Distribution: crosses
placenta. Metabolism: in liver. Elimination:
in Urine. Half-life: 4–17 h.
INTERACTIONS
Drug-drug: Salicylates may decrease
uricosuric activity; may decrease
methotrexate elimination, causing increased
toxicity; decreases nitrofurantoin efficacy
and increases its toxicity. Decreases
clearance of Penicillins, Cephalosporins,
and Nsaids.
INDICATIONS
 Treatment of hyperuricemia associated
with gout and gouty arthritis (adults)
 Adjuvant to therapy with penicillins or
cephalosporins, for elevation and
prolongation of plasma levels of the
antibiotic
CONTRAINDICATIONS
Contraindicated in: Blood dyscrasias; uric
acid kidney stones; during or within 2–3 wk
of acute gouty attack; overexcretion of uric
acid (greater than 1000 mg/day); patients
with creatinine clearance less than 50
mg/min; use with penicillin in presence of
known renal impairment; use for
hyperuricemia secondary to cancer
chemotherapy.
ADVERSE REACTIONS/ SIDE EFFECT
Body as a Whole: Flushing, dizziness,
fever, anaphylaxis. CNS: Headache.
GI: Nausea, vomiting, anorexia, sore gums,
hepatic necrosis (rare). Urogenital: Urinary
frequency. Hematologic: Anemia, hemolytic
Page | 93
anemia (possibly related to G6PD
deficiency), aplastic anemia (rare).
Musculoskeletal: Exacerbations of gout,
uric acid kidney stones. Skin: Dermatitis,
pruritus. Respiratory: Respiratory
depression.
NURSING IMPLICATIONS
Assessment
 Gout: Assess involved joints for pain,
mobility, and edema throughout course
of therapy.
 Monitor intake and output ratios. Fluids
should be encouraged to prevent urate
stone formation (2000– 3000 mL/day).
Alkalinization of the urine with sodium
bicarbonate, potassium citrate, or
acetazolamide may also be used for this
purpose.
 Lab Test Considerations: CBC, serum
uric acid levels, and renal function
should be monitored routinely during
long-term therapy.
 Serum and urine uric acid
determinations may be measured
periodically when probenecid is used to
treat hyperuricemia.
Diagnoses
 Acute pain (Indications)
 Impaired physical mobility (Indications)
 Deficient knowledge, related to
medication regimen (Patient/Family
Teaching)
Implementation
 Probenecid therapy is not used to treat
gouty arthritis but, rather, to prevent it. If
acute attacks occur during therapy,
probenecid is usually continued at full
dose along with colchicine or NSAIDs.
 PO: Administer with food or antacid to
minimize gastric irritation.
 Gradual dosage reduction should be
attempted if uric acid levels remain
stable following 6 mo of therapy.
Patient/Family Teaching
 Instruct patient to take medication
exactly as directed, not to discontinue
without consulting health care
professional. Irregular dosage schedules
may cause elevation of uric acid levels
and precipitate an acute gout attack.
 Explain purpose of the medication to
patients taking probenecid with
penicillin.
 Advise patient to follow
recommendations of health care
professional regarding weight loss, diet,
and alcohol consumption.
 Caution patient not to take aspirin or
other salicylates, because they
decrease the effects of probenecid.
 Instruct patient to report nausea,
vomiting, loss of appetite, abdominal
pain, unusual bleeding or bruising, sore
throat, fatigue, malaise, or yellowing of
the skin or eyes promptly.
Evaluation
 Decrease in pain and swelling in
affected joints and subsequent decrease
in frequency of gout attacks. May
require several months of continuous
therapy for maximum effects.
 Decrease in serum uric acid levels.
 Prolonged serum levels of penicillins
and other related antibiotics.
G. NONOPIOID ANALGESICS
1. NSAIDs (First and Second
Generation)
Drug Classification: FIRST AND SECOND
GENERATION NSAIDS
Generic Name: Aspirin
Brand Name: ASA
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO, Rect (Adults): 325–1000 mg q 4–6 hr
(not to exceed 4 g/day). Extended release
tablets—650 mg q 8 hr or 800 mg q 12 hr.
PO, Rect (Children 2–11 yr): 10–15
mg/kg/dose q 4–6 hr; maximum dose: 4 g/
day.
Inflammation
PO (Adults): 2.4 g/day initially; increased to
maintenance dose of 3.6–5.4 g/day in
divided doses (up to 7.8 g/day for acute
rheumatic fever).
PO (Children): 60–100 mg/kg/day in divided
doses (up to 130 mg/kg/day for acute
rheumatic fever).
Prevention of Transient Ischemic Attacks
PO (Adults): 50–325 mg once daily.
Prevention of Myocardial
Infarction/Antiplatelet effects
PO (Adults): 80–325 mg once daily
Suspected acute MI-160 mg as soon as MI
is suspected.
PO (Children): 3–10 mg/kg/day given once
daily (round dose to a convenient amount).
Kawasaki Disease
PO (Children): 80–100 mg/kg/day in 4
divided doses until fever resolves; may be
followed by maintenance dose of 3–
5mg/kg/day as a single dose for up to 8 wk.
DRUG ACTION
Drug-drug: Produce analgesia and reduce
inflammation and fever by inhibiting the
Page | 94
production of prostaglandins. Decreases
platelet aggregation.
Therapeutic Effects: Analgesia. Reduction
of inflammation. Reduction of fever.
Decreased incidence of transient ischemic
attacks and MI. Pharmacokinetics:
Absorption: Well absorbed from the upper
small intestine; absorption from enteric-
coated preparations may be unreliable;
rectal absorption is slow and variable.
Distribution: Rapidly and widely distributed;
crosses the placenta and enters breast milk.
Metabolism and Excretion: Extensively
metabolized by the liver; inactive
metabolites excreted by the kidneys.
Amount excreted unchanged by the kidneys
depends on urine pH; as pH increases,
amount excreted unchanged increases from
2– 3% up to 80%.
INTERACTIONS
*see aspirin
INDICATIONS
Inflammatory disorders including:
Rheumatoid arthritis, Osteoarthritis. Mild to
moderate pain. Fever. Prophylaxis of
transient ischemic attacks and MI.
Unlabeled Use: Adjunctive treatment of
Kawasaki disease.
CONTRAINDICATIONS
Hypersensitivity to aspirin or other
salicylates; Cross-sensitivity
with other NSAIDs may exist (less with
nonaspirin salicylates); Bleeding disorders
or thrombocytopenia; Pedi: May increase
risk of Reye’s syndrome in children
or adolescents with viral infections.
ADVERSE REACTIONS/ SIDE EFFECT
EENT: tinnitus. GI: GI BLEEDING,
dyspepsia, epigastric distress, nausea,
abdominal pain, anorexia, hepatotoxicity,
vomiting. Hemat: anemia, hemolysis. Derm:
rash, urticaria. Misc: allergic reactions
including anaphylaxis and laryngeal edema.
NURSING IMPLICATIONS
Assessment
 Patients who have asthma, allergies,
and nasal polyps or who are allergic to
tartrazine are at an increased risk for
developing hypersensitivity reactions.
 Pain: Assess pain and limitation of
movement; note type, location, and
intensity before and at the peak (see
Time/Action Profile) after administration.
 Fever: Assess fever and note
associated signs (diaphoresis,
tachycardia, malaise, chills).
Diagnosis
 Acute pain (Indications)
 Impaired physical mobility (Indications)
Implementation
 Use lowest effective dose for shortest
period of time.
 PO: Administer after meals or with food
or an antacid to minimize gastric
irritation.
 Food slows but does not alter the total
amount absorbed.
 Do not crush or chew enteric-coated
tablets. Do not take antacids within 1–2
hr of enteric-coated tablets. Chewable
tablets may be chewed, dissolved in
liquid, or swallowed whole. Some
extended-release tablets may be broken
or crumbled but must not be ground up
before swallowing. See manufacturer’s
prescribing information for individual
products.
Evaluation
 Relief of mild to moderate discomfort.
 Increased ease of joint movement. May
take 2–3 wk for maximum effectiveness.
 Reduction of fever. Prevention of
transient ischemic attacks.
 Prevention of MI.
G. NONOPIOID ANALGESICS
2. ANALGESIC
Drug Classification: ANALGESIC
Generic Name: Paracetamol
Brand Name: Biogesic, Calpol
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults and Children 12 yr): 325– 650
mg q 6 hr or 1 g 3– 4 times daily or 1300 mg
q 8 hr (not to exceed 3 g or 2 g/24 hr in
patients with hepatic/renal impairment).
PO (Children 1– 12 yr): 10– 15 mg/kg/dose
q 6 hr as needed (not to exceed 5 doses/24
hr).
PO (Infants): 10– 15 mg/kg/dose q 6 hr as
needed (not to exceed 5 doses/24 hr).
PO (Neonates): 10– 15 mg/kg/dose q 6– 8
hr as needed. IV (Adults and Children 13 yr
and 50 kg): 1000 mg q 6 hr or 650 mg q 4 hr
(not to exceed 1000 mg/dose, 4 g/day, and
less than 4 hr dosing interval).
IV (Adults and Children 13 yr and 50 kg):
15 mg/kg q 6 hr or 12.5 mg/kg q 4 hr (not to
exceed 15 mg/kg/dose, 75 mg/kg/day, and
less than 4 hr dosing interval).
IV (Children 2– 12 yr): 15 mg/kg q 6 hr or
12.5 mg/kg q 4 hr (not to exceed 15
mg/kg/dose, 75 mg/kg/day, and less than 4
hr dosing interval).
IV (Infants and Children 2yr): 7.5– 15
mg/kg/dose q 6 hr (not to exceed 60
mg/kg/day).
Rect (Adults and Children 12 yr): 325–
650 mg q 4– 6 hr as needed or1g3–4
times/day (not to exceed 4 g/24 hr).
Rect (Children 1– 12 yr): 10– 20
mg/kg/dose q 4– 6 hr as needed.
Page | 95
Rect (Infants): 10– 20 mg/kg/dose q 4– 6 hr
as needed.
Rect (Neonates): 10– 15 mg/kg/dose q 6– 8
hr as needed.
DRUG ACTION
Inhibits the synthesis of prostaglandins that
may serve as mediators of pain and fever,
primarily in the CNS.Has no significant anti-
inflammatory properties or GI toxicity.
TherapeuticEffects: Analgesia. Antipyresis.
Pharmacokinetics: Absorption: well
absorbed following oral administration.
Rectal absorption is variable. Intravenous
administration results in complete
bioavailability. Distribution: widely
distributed. Crosses the placenta; enters
breast milk in low concentrations.
Metabolism and excretion: 85– 95%
metabolized by the liver (cyp2e1 enzyme
system). Metabolites may be toxic in
overdose situation. Metabolites excreted by
the kidneys. Half-life: neonates: 7 hr; infants
and children: 3– 4 hr; adults: 1– 3 hr
INTERACTIONS
Drug-drug: Chronic high-dose
acetaminophen (2 g/day) may increase risk
of bleeding with warfarin (INR should not
exceed 4). Hepatotoxicity is additive with
other hepatotoxic substances, including
alcohol. Concurrent use of
isoniazid,rifampin, rifabutin, phenytoin,
barbiturates, and carbamazepine may
increase the risk of acetaminophen-induced
liver damage (limit self-medication); these
agents will also decrease therapeutic effects
of acetaminophen. Concurrent use of
NSAIDs may increase the risk of adverse
renal effects (avoid chronic concurrent use).
Propranolol decrease metabolism and may
increase effects. May decrease effects of
lamotrigine and zidovudine.
INDICATIONS
PO, Rect: Treatment of: Mild pain, Fever. IV
Treatment of: Mild to moderate pain,
Moderate to severe pain with opioid
analgesics, Fever.
CONTRAINDICATIONS
Contraindicated in: Previous
hypersensitivity; Products containing
alcohol, aspartame, saccharin, sugar, or
tartrazine (FDC yellow dye #5) should be
avoided in patients who have
hypersensitivity or intolerance to these
compounds; Severe hepatic
impairment/active liver disease.
ADVERSE REACTIONS/SIDE EFFECT
CNS: agitation (qin children) (IV), anxiety
(IV), headache (IV), fatigue (IV), insomnia
(IV). Resp: atelectasis (increase in children)
(IV), dyspnea (IV). CV: hypertension (IV),
hypotension (IV). GI: HEPATOTOXICITY (
increase DOSES), constipation ( increase in
children) (IV), increase liver enzymes,
nausea (IV), vomiting (IV). F and E:
hypokalemia (IV). GU: renal failure (high
doses/chronic use). Hemat: neutropenia,
pancytopenia. MS: muscle spasms (IV),
trismus (IV). Derm: acute generalized
exanthematous pustulosis,stevens-johnson
syndrome, toxic epidermal necrolysis, rash,
urticaria
NURSING IMPLICATIONS
Assessment
 Assess overall health status and alcohol
usage before administering
acetaminophen. Patients who are
malnourished or chronically abuse
alcohol are at higher risk of developing
hepatotoxicity with chronic use of usual
doses of this drug.
 Assess amount, frequency, and type of
drugs taken in patients self-medicating,
especially with OTC drugs. Prolonged
use of acetaminophen increases the risk
of adverse renal effects. For short-term
use, combined doses of acetaminophen
and salicylates should not exceed the
recom mended dose of either drug given
alone. Do not exceed maximum daily
dose of acetaminophen when
considering all routes of administration
and all combination products containing
acetaminophen.
 Pain: Assess type, location, and
intensity prior to and 30– 60 min
following administration.
 Fever: Assess fever; note presence of
associated signs (diaphoresis,
tachycardia, and malaise).
 Lab Test Considerations: Evaluate
hepatic, hematologic, and renal function
periodically during prolonged, high-dose
therapy.
 May alter results of blood glucose
monitoring. May cause falselypvalues
when measured with glucose
oxidase/peroxidase method, but
probably not with hexokinase/G6PD
method. May also cause falselyqvalues
with certain instruments; see
manufacturer’s instruction manual.
 Increased serum bilirubin, LDH, AST,
ALT, and prothrombin time may indicate
hepatotoxicity.
 Toxicity and Overdose: If overdose
occurs, acetylcysteine (Acetadote) is the
antidote. Potential
Diagnoses
Page | 96
  Acute pain (Indications)
 Risk for imbalanced body
temperature (Indications)
Implementation
 Do not confuse Tylenol with Tylenol PM.
 To prevent fatal medication errors
ensure dose in milligrams (mg) and
milliliters (mL) is not confused; dosing is
based on weight for patients under 50
kg; programming of infusion pump
accurate; and total daily dose of
acetaminophen from all sources does
not exceed maximum daily limits.
 When combined with opioids do not
exceed the maximum recommended
daily dose of acetaminophen.
 PO: Administer with a full glass of water.
 May be taken with food or on an empty
stomach.
Patient/Family Teaching
 Advise patient to take medication
exactly as directed and not to take more
than the recommended amount. Chronic
excessive use of 4 g/day (2 g in chronic
alcoholics) may lead to hepatotoxicity,
renal or cardiac damage. Adults should
not take acetaminophen longer than 10
days and children not longer than 5 days
unless directed by health care
professional. Short-term doses of
acetaminophen with salicylates or
NSAIDs should not exceed the
recommended daily dose of either drug
alone.
 Advise patient to avoid alcohol (3 or
more glasses per day increase the risk
of liver damage) if taking more than an
occasional 1– 2 dosesand to avoid
taking concurrently with salicylates or
NSAIDs for more than a few days,
unless directed by health care
professional.
 Advise patient to discontinue
acetaminophen and notify health care
professional if rash occurs.
 Inform patients with diabetes that
acetaminophen may alter results of
blood glucose monitoring. Advise patient
to notify health care professional if
changes are noted.
 Caution patient to check labels on all
OTC products. Advise patients to avoid
taking more than one product containing
acetaminophen at a time to prevent
toxicity.
Evaluation
 Relief of mild to moderate pain.
 Reduction of fever.
G. NONOPIOID ANALGESICS
3. MISCELLANEOUS ANALGESIC
Drug Classification:
MISCELLANEOUS ANALGESIC
Generic Name: Tramadol
Brand Name: Ultram
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Immediate-release PO (Adults 18 yr):
Rapid titration—50– 100 mg q 4– 6 hr (not to
exceed 400 mg/day [300 mg in patients 75
yr]). Gradual titration—25 mg/day initially,
increase by 25 mg/day q 3 days to reach
dose of 25 mg 4 times daily, then increase
by 50 mg/day q 3 days to reach dose of 50
mg 4 times daily; may then use 50– 100 mg
q 4– 6 hr (maximum dose 400 mg/day).
Renal Impairment PO (Adults): CCr 30
mL/min— increase dosing interval to q 12 hr
(not to exceed 200 mg/day).
Hepatic Impairment PO (Adults): 50 mg q
12 hr.
Extended-release PO (Adults): Ultram ER
and Conzip (not currently receiving
immediate-release)—100 mg once daily
initially, may then titrate q 5 days up to 300
mg/day; Ultram ER and Conzip (currently
receiving immediate-release)—calculate 24-
hr total dose of immediate-release product
and give same dose (rounded down to next
lowest 100-mg increment) of ER once daily
(maximum dose 300 mg/day).
DRUG ACTION
Binds to mu-opioid receptors.Inhibits
reuptake of serotonin and norepinephrine in
the CNS. Therapeutic Effects: Decreased
pain.
INTERACTIONS
Drug-drug: Increase risk of CNS
depression when used concurrently with
other CNS depressants, including alcohol,
antihistamines, sedative/hypnotics, opioid
analgesics, anesthetics, or psychotropic
agents. Increase risk of seizures with high
doses of penicillins, cephalosporins,
phenothiazines, opioid analgesics, or
antidepressants. Carbamazepine increase
metabolism and decrease effectiveness of
tramadol (increased doses may be
required). Use cautiously in patients who are
receiving MAO inhibitors ( increased risk of
adverse reactions). Quinidine, fluoxetine,
paroxetine, amitriptyline, ketoconazole, and
erythromycinmayqlevels.qrisk of serotonin
syndrome when used with SSRI and SNRI
antidepressants, TCAs, MAO inhibitors,
5HT1 agonists, CYP2D6 inhibitors, and
CYP3A4 inhibitors. Drug-Natural Products:
Concomitant use of kava-kava,valerian,
Page | 97
orchamomile canqCNS depression.qrisk of
serotonin syndrome when used with St.
Johns’ wort.
INDICATIONS
Moderate to moderately severe pain
(extended-release formulations indicated for
patients who require around-the-clock pain
management).
CONTRAINDICATIONS
Contraindicated in: Hypersensitivity;
Cross-sensitivity with opioids may occur;
Patients who are acutely intoxicated with
alcohol, sedatives/hypnotics, centrally acting
analgesics, opioid analgesics, or
psychotropic agents; Patients who are
physically dependent on opioid analgesics
(may precipitate withdrawal); OB, Lactation:
Pregnancy or lactation; ER only—CCr 30
mL/min or hepatic impairment.
Pharmacokinetics: Absorption:
immediate-release—75% absorbed after
oral administration; Extended-release
(Ultram)—85– 90% (compared with
immediate-release). Distribution: Crosses
the placenta; enters breast milk.
Metabolism and Excretion: Mostly
metabolized by the liver; one metabolite has
analgesic activity; 30% is excreted
unchanged in urine. Half-life: Tramadol—6–
8 hr, ER—7.9 hr; active metabolite—7– 9 hr;
both areqin renal or hepatic impairment.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: seizures, dizziness, headache,
somnolence, anxiety, CNS stimulation,
confusion, coordination disturbance,
euphoria, malaise, nervousness, sleep
disorder, weakness. EENT: visual
disturbances. CV: vasodilation. GI:
constipation, nausea, abdominal pain,
anorexia, diarrhea, dry mouth, dyspepsia,
flatulence, vomiting. GU: menopausal
symptoms, urinary retention/frequency.
Derm: pruritus, sweating. Neuro:hypertonia.
Misc: Serotonin Syndrome, physical
dependence, psychological dependence,
tolerance.
NURSING IMPLICATIONS
Assessment
 Assess type, location, and intensity of
pain before and 2– 3 hr (peak) after
administration.
 Assess BP and respiratory rate before
and periodically during administration.
Respiratory depression has not occurred
with recommended doses.
 Assess bowel function routinely.
Prevention of constipation should be
instituted with increased intake of fluids
and bulk and with laxatives to minimize
constipating effects.
 Assess previous analgesic history.
Tramadol is not recommended for
patients dependent on opioids or who
have previously received opioids for
more than 1 wk; may cause opioid
withdrawal symptoms.
 Prolonged use may lead to physical and
psychological dependence and
tolerance, although these may be milder
than with opioids. This should not
prevent patient from receiving adequate
analgesia. Most patients who receive
tramadol for pain do not develop
psychological dependence. If tolerance
develops, changing to an opioid agonist
may be required to relieve pain.
 Monitor patient for seizures. May occur
within recommended dose range. Risk is
increased with higher doses and in
patients taking antidepressants (SSRIs,
SNRIs, tricyclics, or MAO inhibitors),
opioid analgesics, or other drugs that
decrease the seizure threshold. Also
monitor for serotonin syndrome (mental-
status changes (e.g., agitation,
hallucinations, coma), autonomic
instability (e.g., tachycardia, labile BP,
hyperthermia), neuromuscular
aberrations (e.g., hyperreflexia,
incoordination) and/or gastrointestinal
symptoms (e.g., nausea, vomiting,
diarrhea) in patients taking these drugs
concurrently.
 Lab Test Considerations: May
causeqserum creatinine,qliver
enzymes,p hemoglobin, and proteinuria.
 Toxicity and Overdose: Overdose may
cause respiratory depression and
seizures. Naloxone may reverse some,
but not all, of the symptoms of overdose.
Treatment should be symptomatic and
supportive. Maintain adequate
respiratory exchange. Hemodialysis is
not helpful because it removes only a
small portion of administered dose.
Seizures may be managed with
barbiturates or benzodiazepines;
naloxone increases risk of seizures.
Potential Nursing
Diagnoses
 Acute pain (Indications)
 Risk for injury (Side Effects)
Implementation
 Do not confuse tramadol with trazodone.
 Tramadol is considered to provide more
analgesia than codeine 60 mg but less
Page | 98
 than combined aspirin 650 mg/codeine
60 mg for acute postoperative pain.
 For chronic pain, daily doses of 250 mg
of tramadol provide pain relief similar to
that of 5 doses/day of acetaminophen
300 mg/codeine 30 mg, 5 doses/day of
aspirin 325 mg/codeine 30 mg, or 2– 3
doses/day of acetaminophen 500
mg/oxycodone 5 mg.
 Explain therapeutic value of medication
before administration to enhance the
analgesic effect.
 Regularly administered doses may be
more effective than prn administration.
Analgesic is more effective if given
before pain becomes severe.
 Tramadol should be discontinued
gradually after long-term use to prevent
withdrawal symptoms.
 PO: Tramadol may be administered
without regard to meals. Swallow
extendedrelease tablets and capsules
whole; do not crush, break, dissolve, or
chew.
Patient/Family Teaching
 Instruct patient on how and when to ask
for pain medication.
 May cause dizziness and drowsiness.
Caution patient to avoid driving or other
activities requiring alertness until
response to medication is known.
 Advise patient to change positions
slowly to minimize orthostatic
hypotension.
 Caution patient to avoid concurrent use
of alcohol or other CNS depressants
with this medication. Advise patient to
notify health care professional before
taking other RX, OTC, or herbal
products concurrently.
 Advise patient to notify health care
professional if seizures or if symptoms
of serotonin syndrome occur.
 Encourage patient to turn, cough, and
breathe deeply every 2 hr to prevent
atelectasis.
 Advise female patients to notify health
care professional if pregnancy is
planned or suspected, or if breast
feeding.
Evaluation
 Decrease in severity of pain without a
significant alteration in level of
consciousness or respiratory status.H.
OPIOID ANALGESICS
Drug Classification: Opioids
Generic Name: Meperidine
Brand Name: Demerol
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO, IM, Subcut (Adults): Analgesia—50
mg q 3-4 hr; may be increase as needed
(not to exceed 600 mg/24 hr). Analgesia
during labor—50–100 mg IM or subcut when
contractions become regular; may repeat q
1–3 hr. Preoperative sedation—50–100 mg
IM or subcut 30–90 min before anesthesia.
PO, IM, Subcut (Children): Analgesia—1–
1.5 mg/kg q 3–4 hr (should not exceed 100
mg/dose). Preoperative sedation—1–2
mg/kg 30–90 min before anesthesia (not to
exceed adult dose).
IV (Adults): 15–35 mg/hr as a continuous
infusion; PCA—10 mg initially; with a range
of 1–5 mg/incremental dose, recommended
lockout interval is 6–10 min (minimum 5
min).
IV (Children): Continuous infusion—0.5–1
mg/kg loading dose followed by 0.3
mg/kg/hr, titrate to effect up to 0.5–0.7
mg/kg/hr.
Availability (generic available)
Tablets: 50 mg, 100 mg.
Syrup (banana flavor): 50 mg/5 mL.
Injection: 10 mg/mL, 25 mg/0.5 mL, 25
mg/mL, 50 mg/mL, 75 mg/mL, 100 mg/mL.
DRUG ACTION
Binds to opiate receptors in the CNS. Alters
the perception of and response to painful
stimuli, while producing generalized CNS
depression.
Therapeutic Effects:
Decrease in severity of pain.
Pharmacokinetics: Absorption: 50% from
the gi tract; well absorbed from im sites. Oral
doses are about half as effective as
parenteral doses.
Distribution: Widely distributed. Crosses
the placenta; enters breast milk. Protein
Binding: Neonates: 52%; Infants 3–18
mo:85%; Adults: 60–80%. Metabolism and
Excretion: Mostly metabolized by the liver;
some converted to normeperidine, which
may accumulate and cause seizures. 5%
excreted unchanged
by the kidneys. Half-life: Neonates: 12–39
hr; Infants 3–18 mo: 2.3 hr; Children 5–8 yr:
3 hr; Adults: 2.5–4 hr ( increase in impaired
renal or hepatic function [7–11 hr]).
INTERACTIONS
Drug-dug: Do not use in patients receiving
MAO inhibitors or procarbazine (may cause
fatal reaction—contraindicated within 14
days of MAO inhibitortherapy). Increase
CNS depression with alcohol,
antihistamines,and sedative/hypnotics.
Administration of agonist/antagonist opioid
analgesics may precipitate opioid withdrawal
in physically dependent patients. Nalbuphine
or pentazocine may decrease analgesia.
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Protease inhibitors may increase effects and
adverse reactions (concurrent use should be
avoided). Phenytoin increase metabolism
and may decrease effects. Chlorpromazine
and thioridazine may increase the risk of
adverse reactions (concurrent use should be
avoided). May aggravate side effects of
isoniazid. Acyclovir may increase plasma
concentrations of meperidine and
normeperidine.
Drug-Natural Product: Concomitant use of
kava-kava, valerian, or chamomile can
decrease CNS depression. St. John’s wort
may increase serious side effects,
concurrent use is not recommended.
INDICATIONS
Moderate or severe pain (alone or with
nonopioid agents). Anesthesia
adjunct.Analgesic during labor.Preoperative
sedation.Unlabeled Use: Rigors.
CONTRAINDICATIONS
Contraindicated in: Hypersensitivity;
Hypersensitivity to bisulfites (some
injectable products); Recent (within 14 days)
MAO inhibitor therapy; Severe respiratory
insufficiency; OB: Chronic use may pose risk
to the fetus including possible addiction;
Lactation: Excreted in breast milk and can
cause respiratory depression in the infant.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: SEIZURES, confusion, sedation,
dysphoria, euphoria, floating feeling,
hallucinations, headache, unusual
dreams. EENT: blurred vision, diplopia,
miosis. Resp: respiratory depression. CV:
hypotension, bradycardia. GI: constipation,
nausea, vomiting. GU: urinary retention.
Derm: flushing, sweating. Misc: allergic
reactions including anaphylaxis, physical
dependence, psychological dependence,
tolerance.
NURSING IMPLICATIONS
Assessment
 Assess type, location, and intensity of
pain prior toand 1 hr following PO,
subcut, and IM doses and 5min (peak)
following IV administration. When
titratingopioid doses, increases of 25–
50% should beadministered until there is
either a 50% reduction inthe patient’s
pain rating on a numerical or visual
analogue scale or the patient reports
satisfactory painrelief. A repeat dose
can be safely administered atthe time of
the peak if previous dose is
ineffectiveand side effects are minimal.
 An equianalgesic chart (see Appendix
K) should beused when changing routes
or when changing fromone opioid to
another.
 Assess BP, pulse, and respirations
before and periodicallyduring
administration. If respiratory rate
is10/min, assess level of sedation. Dose
may need tobe decreased by 25–50%.
Initial drowsiness will diminishwith
continued use.
 Assess bowel function routinely.
Prevention of constipationshould be
instituted with increased intakeof fluids
and bulk and with laxatives to
minimizeconstipating effects. Stimulant
laxatives should beadministered
routinely if opioid use exceeds 2–3days,
unless contraindicated.
Diagnoses
 Acute pain (Indications)
 Disturbed sensory perception (visual,
auditory) (SideEffects)
 Risk for injury (Side Effects)
Implementation
 High Alert: Accidental overdose of opioid
analgesicshas resulted in fatalities.
Before administering,clarify all
ambiguous orders; have second
practitionerindependently check original
order, dose calculations,and infusion
pump settings. Pedi: Medicationerrors
with opioid analgesics are common inthe
pediatric population and include
misinterpretationor miscalculation of
doses and use of
inappropriatemeasuring devices.
 Explain therapeutic value of medication
prior to administrationto enhance the
analgesic effect.
 Regularly administered doses may be
more effectivethan prn administration.
Analgesic is more effectiveif given
before pain becomes severe.
 Coadministration with nonopioid
analgesics may have
 Additive analgesic effects and permit
lower doses.
 Oral dose is _50% as effective as
parenteral. Whenchanging to oral
administration, dose may need tobe
increased (see Appendix K).
 Medication should be discontinued
gradually afterlong-term use to prevent
withdrawal symptoms.
 May be administered via PCA pump.
Diagnoses
 Acute pain (Indications)
 Disturbed sensory perception (visual,
auditory) (Side Effects)
 Risk for injury (Side Effects)
Implementation
 High Alert: Accidental overdose of opioid
analgesicshas resulted in fatalities.
Before administering,clarify all
ambiguous orders; have second
practitionerindependently check original
order, dose calculations,and infusion
pump settings. Pedi: Medicationerrors
with opioid analgesics are common inthe
pediatric population and include
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 misinterpretationor miscalculation of
doses and use of
inappropriatemeasuring devices.
 Explain therapeutic value of medication
prior to administrationto enhance the
analgesic effect.
 Regularly administered doses may be
more effectivethan prn administration.
Analgesic is more effectiveif given
before pain becomes severe.
 Coadministration with nonopioid
analgesics may haveadditive analgesic
effects and permit lower doses.
 Oral dose is _50% as effective as
parenteral. Whenchanging to oral
administration, dose may need tobe
increased (see Appendix K).
 Medication should be discontinued
gradually afterlong-term use to prevent
withdrawal symptoms.
 May be administered via PCA pump.
I. OPIOID AGONISTS-ANTAGONIST
Drug Classification: Opioid Agonist
Antagonist
Generic Name: Nalbuphine
Brand Name: Nubain
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Analgesia
IM, Subcut, IV (Adults): Usual dose is 10
mg q 3–6 hr (maximum: 20 mg/dose or 160
mg/day).
IM, Subcut, IV (Children): 0.1–0.15 mg/kg
q 3–6 hr (maximum: 20 mg/dose or 160
mg/day).
Supplement to Balanced Anesthesia
IV (Adults): Initial—0.3–3 mg/kg over 10–15
min. Maintenance—0.25–0.5 mg/kg as
needed.
Opioid-induced pruritus
IV (Adults): 2.5–5 mg; may repeat dose.
Availability (generic available)
Injection: 10 mg/mL, 20 mg/mL.
DRUG ACTION
Binds to opiate receptors in the CNS. Alters
the perception of and response to painful
stimuli while producing generalized CNS
depression. In addition, has partial
antagonist properties, which may result in
opioid withdrawal in physically dependent
patients.
TherapeuticEffects: Decreased pain.
INTERACTIONS
Drug-drug: Use with extreme caution in
patients receivingMAO inhibitors (may result
in unpredictable, severe reactions—
decrease initial dose of nalbuphine to 25%
of usual dose). Additive CNS depression
with alcohol, antihistamines, and
sedative/hypnotics. May precipitate
withdrawal in patients who are physically
dependent on opioid agonists. Avoid
concurrent use with other opioid analgesic
agonists (may diminish analgesic effect).
Drug-Natural Products: Concomitant use
of kava-kava, valerian, skullcap, chamomile,
or hops can increase CNS depression.
INDICATIONS
Moderate to severe pain.Also provides:
Analgesia during labor, Sedation before
surgery, Supplement to balanced
anesthesia. Prevention or treatment of
opioidinduced pruritus.
CONTRAINDICATIONS
Contraindicated in: Hypersensitivity to
nalbuphine or bisulfites; Patients physically
dependent on opioids and who have not
been detoxified (may precipitate withdrawal).
Use Cautiously in: Head trauma; increase
intracranial pressure; Severe renal, hepatic,
or pulmonary disease; Hypothyroidism;
Adrenal insufficiency; Alcoholism;
Undiagnosed abdominal pain; Prostatic
hyperplasia; Patients who have recently
received opioid agonists; OB: Has been
used during labor but may cause respiratory
depression in the newborn; Geri:
Dosepsuggested.
Pharmacokinetics: Absorption: well
absorbed after im and subcut administration.
Distribution: probably crosses the placenta
and enters breast milk. Protein Binding:
50%.
Metabolism and Excretion: Mostly
metabolized by the liver and eliminated in
the feces via biliary excretion. Minimal
amounts excreted unchanged by the
kidneys. Half-life: Children 1–8 yrs: 0.9 hr;
Adults: 3.5–5 hr.
ADVERSE REACTIONS/ SIDE EFFECT
CNS: dizziness, headache, sedation,
confusion, dysphoria, euphoria, floating
feeling, hallucinations, unusual
dreams. EENT: blurred vision, diplopia,
miosis (high doses). Resp: respiratory
depression. CV: hypertension, orthostatic
hypotension, palpitations. GI:dry mouth,
nausea, vomiting, constipation, ileus. GU:
urinary urgency. Derm: clammy feeling,
sweating. Misc: physical dependence,
psychological dependence, tolerance.
NURSING IMPLICATIONS
Assessment
 Assess type, location, and intensity of
pain before and 1 hr after IM or 30 min
(peak) after IV administration. When
titrating opioid doses, increases of 25–
50% should be administered until there
is either a 50% reduction in the patient’s
pain rating ona numeric or visual
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 analogue scale or the patient reports
satisfactory pain relief. A repeat dose
can be safely administered at the time of
the peak if previous dose is ineffective
and side effects are minimal.Patients
requiring doses higher than 20 mg
should be converted to an opioid
agonist. Nalbuphine is not
recommended for prolonged use or as
first-line therapy for acute or cancer
pain.
 An equianalgesic chart (see Appendix
K) should beused when changing routes
or when changing fromone opioid to
another.
 Assess BP, pulse, and respirations
before and periodicallyduring
administration. If respiratory rate
is_10/min, assess level of sedation.
Physical stimulationmay be sufficient to
prevent significant hypoventilation.Dose
may need to be decreased by 25–50%.
Nalbuphine produces respiratory
depression,but this does not markedly
increase with increaseddoses.
 Assess previous analgesic history.
Antagonisticproperties may induce
withdrawal symptoms
(vomiting,restlessness, abdominal
cramps, and increasedBP and
temperature) in patients
physicallydependent on opioids.
Potential Nursing Diagnoses
 Acute pain (Indications)
 Risk for injury (Side Effects)
 Disturbed sensory perception (visual,
auditory) (SideEffects)
Implementation
 High Alert: Accidental overdose of opioid
analgesicshas resulted in fatalities.
Before administering,clarify all
ambiguous orders; have second
practitionerindependently check original
order, dosecalculations, and infusion
pump settings.
 Explain therapeutic value of medication
before administrationto enhance the
analgesic effect.
 Regularly administered doses may be
more effectivethan prn administration.
Analgesic is more effectiveif
administered before pain becomes
severe.
 Coadministration with nonopioid
analgesics mayhave additive effects and
permit lower opioid doses.
 IM: Administer deep into well-developed
muscle.
 Rotate sites of injections.
Patient/Family Teaching
 Instruct patient on how and when to ask
for painmedication.
 May cause drowsiness or dizziness.
Advise patientto call for assistance when
ambulating and to avoiddriving or other
activities requiring alertness
untilresponse to the medication is
known.
 Caution patient to change positions
slowly to minimizeorthostatic
hypotension.
 Advise patient that frequent mouth
rinses, good oralhygiene, and sugarless
gum or candy may decreasedry mouth.
 Encourage patient to turn, cough, and
breathedeeply every 2 hr to prevent
atelectasis.
 Advise patient to avoid concurrent use
of alcohol orother CNS depressants with
this medication.
Evaluation/Desired Outcomes
 Decrease in severity of pain without
significant alteration in level of
consciousness or respiratory status.
J. OPIOID ANTAGONIST
Drug Classification: Opioid
Antagonist
Generic Name: Naloxone
Hydrochloride
Brand Name: Narcan
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Postoperative Opioid-Induced
Respiratory Depression IV (Adults): 0.02–
0.2 mg q 2– 3 min until response obtained;
repeat q 1– 2 hr if needed. IV (Children):
0.01 mg/kg; may repeat q 2– 3 min until
response obtained. Additional doses may be
given q 1– 2 hr if needed. IM, IV, Subcut
(Neonates): 0.01 mg/kg; may repeat q 2– 3
min until response obtained. Additional
doses may be given q 1– 2 hr if needed.
Opioid-Induced Respiratory Depression
During Chronic (1 wk) Opioid Use IV, IM,
Subcut (Adults 40 kg): 20– 40 mcg (0.02–
0.04 mg) given as small, frequent (q min)
boluses or as an infusion titrated to improve
respiratory function without reversing
analgesia. IV, IM, Subcut (Adults and
Children 40 kg): 0.005– 0.02 mg/dose given
as small, frequent (q min) boluses or as an
infusion titrated to improve respiratory
function without reversing analgesia.
Overdose of Opioids IV, IM, Subcut
(Adults): Patients not suspected of being
opioid dependent— 0.4 mg (10 mcg/kg);
may repeat q 2– 3 min (IV route is
preferred). Some patients may require up to
2 mg. Patients suspected to be opioid
dependent—Initial dose should be decrease
to 0.1– 0.2 mg q 2– 3 min. May also be
given by IV infusion at rate adjusted to
patient’s response. IV, IM, Subcut
(Children 5 yr or 20 kg): 2 mg/dose, may
repeat q 2– 3 min. IV, IM, Subcut (Infants up
to 5 yr or 20 kg): 0.1 mg/kg, may repeat q 2–
3 min.
Opioid-Induced Pruritus IV (Children): 2
mcg/kg/hr continuous infusion, may increase
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by 0.5 mcg/kg/hr every few hours if pruritus
continues.
DRUG ACTION
Competitively blocks the effects of opioids,
including CNS and respiratory depression,
without producing any agonist (opioid-like)
effects.
Therapeutic Effects: Reversal of signs of
opioid excess.
INTERACTIONS
Drug-drug: Can precipitate withdrawal in
patients physically dependent on opioid
analgesics. Larger doses may be required to
reverse the effects of buprenorphine,
butorphanol, nalbuphine, or pentazocine.
Antagonizes postoperative opioid
analgesics.
INDICATIONS
Reversal of CNS depression and respiratory
depression because of suspected opioid
overdose. Unlabeled Use: Opioid-induced
pruritus (low dose IV infusion). Management
of refractory circulatory shock.
CONTRAINDICATIONS
Contraindicated in: Hypersensitivity
Use Cautiously in: Cardiovascular disease;
Patients physically dependent on opioids
(may precipitate severe withdrawal); OB:
May cause acute withdrawal syndrome in
mother and fetus if mother is opioid
dependent; Lactation:Safety not established;
Pedi:May cause acute withdrawal syndrome
in neonates of opioid-dependent mothers.
Pharmacokinetics: Absorption:well
absorbed after im or subcut administration.
Distribution: rapidly distributed to tissues.
Crosses the placenta. Metabolism and
Excretion:Metabolized by the liver. Half-
life: 60– 90 min (up to 3 hr in neonates).
ADVERSE REACTIONS/ SIDE EFFECT
CV: Ventricular arrhythmias, hypertension,
hypotension.GI: nausea, vomiting
NURSING IMPLICATIONS
Assessment
 Monitor respiratory rate, rhythm, and
depth; pulse, ECG, BP; and level of
consciousness frequently for 3– 4 hr
after the expected peak of blood
concentrations. After a moderate
overdose of a short half-life opioid,
physical stimulation may be enough to
prevent significant hypoventilation. The
effects of some opioids may last longer
than the effects of naloxone, and repeat
doses may be necessary.
 Patients who have been receiving
opioids for 1 wk are extremely sensitive
to the effects of naloxone. Dilute and
administer carefully.
 Assess patient for level of pain after
administration when used to treat
postoperative respiratory depression.
Naloxone decreases respiratory
depression but also reverses analgesia.
 Assess patient for signs and symptoms
of opioid withdrawal (vomiting,
restlessness, abdominal cramps,
increased BP, and temperature).
Symptoms may occur within a few
minutes to 2 hr. Severity depends on
dose of naloxone, the opioid involved,
and degree of physical dependence.
 Lack of significant improvement
indicates that symptoms are caused by
a disease process or other non-opioid
CNS depressants not affected by
naloxone.
 Toxicity and Overdose: Naloxone is a
pure antagonist with no agonist
properties and minimal toxicity.
Diagnoses
 Ineffective breathing pattern(Indications)
 Ineffective coping (Indications) Acute
pain
Implementation
 Do not confuse naloxone with Lanoxin
(digoxin). Do not confuse Narcan
(naloxone) with Norcuron (vecuronium).
 Larger doses of naloxone may be
necessary when used to antagonize the
effects of buprenorphine, butorphanol,
nalbuphine, and pentazocine.
 Resuscitation equipment, oxygen,
vasopressors, and mechanical
ventilation should be available to
supplement naloxone therapy as
needed.
 Doses should be titrated carefully in
postoperative patients to avoid
interference with control of postoperative
pain.
Patient/Family Teaching
 As medication becomes effective,
explain purpose and effects of naloxone
to patient.
Evaluation
 Adequate ventilation.
 Alertness without significant pain or
withdrawal symptoms
K. DRUGS USED TO TREAT SEVERE
MIGRAINE HEADACHES
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Drug Classification: ERGOT
ALKALOIDS
Generic Name: Dihydroergotamine
mesylate
Brand Name: Migranal
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IM, Subcut (Adults): 1 mg; may repeat in 1
hr to a total of 3 mg (not to exceed 3 mg/
day or 6 mg/wk).
IM, Subcut (Children 6 yr): 0.5 mg; may be
repeated in 1 hr. IV (Adults): 0.5 mg; may
repeat in 1 hr (not to exceed 2 mg/day or 6
mg/wk). For chronic intractable headache,
0.5– 1 mg q 8 hr may be given until relief
(not to exceed 6 mg/wk).
IV (Children 6 yr): 0.25 mg; may be
repeated in 1 hr. IV (Children and
Adolescents 12– 16 yr ):Severe, acute
migraine—0.25– 0.5 mg; 1– 2 more doses
may be given q 20 min. IV (Children 9– 12
yr): Severe, acute migraine—0.2 mg; 1– 2
more doses may be given q 20 min. IV
(Children 6– 9 yr):Severe, acute migraine—
0.1– 0.15 mg; 1– 2 more doses may be
given q 20 min.
Intranasal (Adults): 1 spray (0.5 mg) in
each nostril, repeat after 15 min (2 mg total
dose); not to exceed 3 mg/24 hr or 4 mg/wk.
DRUG ACTION
Vasoconstriction of dilated blood vessels by
stimulating alpha-adrenergic and
serotonergic (5-HT) receptors. Larger doses
may produce alpha-adrenergic blockade and
vasodilation. Therapeutic Effects:
Constriction of dilated carotid artery bed with
resolution of vascular headache.
Pharmacokinetics: Absorption: rapidly
absorbed following im and subcut
administration and 32% absorbed from
nasal mucosa. Distribution: Unknown.
Protein Binding: 90%. Metabolism and
Excretion: Highly metabolized (90%) by
the liver. Some metabolites are active. Half-
life: 10 hours.
INTERACTIONS
Drug-Drug: Concurrent use of CYP 3A4
enzyme inhibitors (macrolide anti-infectives
and protease inhibitors) may produce
serious, life-threatening peripheral ischemia
and is contraindicated. Concurrent use with
beta blockers, oral contraceptives, or
nicotine (heavy smoking) may q risk of
peripheral vasoconstriction.
Dihydroergotamine antagonizes the
antianginal effects of nitrates. Concurrent
use with vasoconstrictors may have
increase effects (avoid concurrent use).
Concurrent use with sumatriptan may result
in prolonged vasoconstriction (allow 24 hr
between use).
INDICATIONS
Vascular headaches including: Migraine,
Cluster headaches.
CONTRAINDICATIONS
Contraindicated in: Peripheral vascular
disease; Ischemic heart disease;
Uncontrolled hypertension; Severe renal or
liver disease ; Malnutrition; Known alcohol
intolerance (injection only); OB: Pregnancy;
Lactation:Lactation; Concurrent use of CYP
3A4 enzyme inhibitors (macrolide anti-
infectives and protease inhibitors).
Use Cautiously in: Illnesses associated with
peripheral vascular pathology such as
diabetes mellitus; Concurrent administration
of other vasoconstricting agents; Pedi:
Children 6 yr (safety not established).
ADVERSE REACTIONS/ SIDE EFFECT
CNS: dizziness. EENT: rhinitis.
CV:Myocardial Infarction, hypertension,
angina pectoris, arterial spasm, intermittent
claudication. GI: abdominal pain, nausea,
vomiting, altered taste, diarrhea, polydipsia.
MS: extremity stiffness, muscle pain, stiff
neck, stiff shoulders. Neuro: leg weakness,
numbness or tingling in fingers or toes.Misc:
fatigue.
NURSING IMPLICATIONS
Assessment
 Assess frequency, location, duration,
and characteristics (pain, nausea,
vomiting, visual disturbances) of chronic
headaches. During acute attack, assess
type, location, and intensity of pain
before and 60 min after administration.
 Monitor BP and peripheral pulses
periodically during therapy. Report any
increases in BP.
 Assess for signs of ergotism (cold, numb
fingers and toes; nausea; vomiting;
headache; muscle pain; weakness).
 Assess for nausea and vomiting.
Ergotamine stimulates the
chemoreceptor trigger zone. For adults,
metoclopramide 10 mg IV may be
administered 3– 5 min before
administration of dihydroergotamine IV.
In children, metoclopramide or a
phenothiazine antiemetic may be given
orally as prophylaxis 1 hr before
administration of dihydroergotamine IV.
Oral administration may decrease risk of
extrapyramidal and other side effects
encountered with IV administration.
 Toxicity and Overdose: Toxicity is
manifested by severe ergotism (chest
pain, abdominal pain, persistent
paresthesia in the extremities) and
Page | 104
 gangrene. Vasodilators, dextran, or
heparin may be ordered to improve
circulation. Potential Nursing
Diagnoses
 Acute pain (Indications)
 Risk for injury (Side Effects)
Implementation
 Administer as soon as patient reports
prodromal symptoms or headache. IV
Administration
 pH: 3.4– 4.9.
 Direct IV: Dihydroergotamine may be
administered undiluted. Rate: Administer
each dose over 1 min.
 Syringe Compatibility: promethazine.
Patient/Family Teaching
 Instruct patient to use
dihydroergotamine at the first sign of an
impending headache and not to exceed
the maximum dose prescribed.
 Encourage patient to rest in a quiet, dark
room after taking ergotamine.
 Review symptoms of toxicity. Instruct
patient to report these promptly.
 Caution patient not to smoke and to
avoid exposure to cold; these
vasoconstrictors may further impair
peripheral circulation.
Evaluation
 Relief of pain from vascular headaches
K. DRUGS USED TO TREAT SEVERE
MIGRAINE HEADACHES
Drug Classification: SELECTIVE
SEROTONIN1 RECEPTOR
AGONISTS (TRIPTANS)
Generic Name: Sumatriptan
Brand Name: Imitrex
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Route/Dosage PO (Adults): 25 mg initially;
if response is inadequate at 2 hr, up to 100
mg may be given (initial doses of 25– 50 mg
may be more effective than 25 mg). If
headache recurs, doses may be repeated q
2 hr (not to exceed 300 mg/day). If PO
therapy is to follow subcut injection,
additional PO sumatriptan may be taken q 2
hr(not to exceed 200 mg/day).
Subcut (Adults): 6 mg; may repeat after 1
hr (not to exceed 12 mg in 24 hr).
Intranasal (Adults):Single dose of 5, 10, or
20 mg in one nostril; may be repeated in 2
hr, not to exceed 40 mg/24 hr or treatment
of 5 episodes/mo.
Transdermal (Adults): Apply one patch;
may be repeated in 2 hr, not to exceed 2
patches/24 hr.
Hepatic Impairment PO (Adults): 25 mg
initially; if response is inadequate at 2 hr, up
to 50 mg may be given (initial doses of 25–
50 mg may be more effective than 25 mg). If
headache recurs, doses may be repeated q
2 hr (not to exceed 300 mg/day). If PO
therapy is to follow subcut injection,
additional PO sumatriptan may be taken q 2
hr(not to exceed 200 mg/day); no single oral
dose should exceed 50 mg.
DRUG ACTION
Acts as a selective agonist of 5-HT1 at
specific vascular serotonin receptor sites,
causing vasoconstriction in large intracranial
arteries.Therapeutic Effects: Relief of
acute attacks of migraine.
INTERACTIONS
Drug-drug: The risk of vasospastic
reactions may be increase by concurrent
use of ergotamine or dihydroergotamine
(avoid within 24 hr of each other). Avoid
concurrent use with other 5HT1 agonists.
MAO inhibitors may increase levels (do not
use within 2 wk of discontinuing MAO
inhibitor). Increase risk of serotonin
syndrome when used with SSRI or SNRI
antidepressants.
Drug-Natural Products: increaserisk of
serotonergic side effects including serotonin
syndrome with St. John’s wortand SAMe.
INDICATIONS
Subcut, PO, Intranasal, Transdermal: Acute
treatment of migraine attacks. Subcut: Acute
treatment of cluster headache episodes.
CONTRAINDICATIONS
Contraindicated in: Hypersensitivity;
Ischemic heart disease or signs and
symptoms of ischemic heart disease,
Prinzmetal’s angina, or uncontrolled
hypertension; Stroke or transient ischemic
attack; Peripheral vascular disease
(including, but not limited to, ischemic bowel
disease); Concurrent MAO inhibitor therapy;
Hemiplegic or basilar migraine; Concurrent
use of (within 24 hr) ergotamine-containing
or ergot-type drugs or other 5HT1 agonists;
Severe hepatic impairment; Geri: Excessive
risk of cardiovascular complications
Pharmacokinetics: Absorption: well
absorbed (97%) after subcut administration.
Absorption after oral administration is
incomplete and significant amounts undergo
substantial hepatic metabolism, resulting in
poor bioavailability (14%). Well absorbed
after intranasal and transdermal
administration. Distribution: Does not cross
the blood-brain barrier. Remainder of
distribution not known.Metabolism and
Page | 105
Excretion:Mostly metabolized (80%) by the
liver. Half-life: 2 hr
ADVERSE REACTIONS/ SIDE EFFECT
All adverse reactions are less common after
oral administration CNS: dizziness, vertigo,
anxiety, drowsiness, fatigue, feeling of
heaviness, feeling of tightness, headache,
malaise, strange feeling, tight feeling in
head, weakness. EENT:alterations in vision,
nasal sinus discomfort, throat discomfort.
CV: MI, angina, chest pressure, chest
tightness, coronary vasospasm, ECG
changes, transient hypertension.
GI:abdominal discomfort, dysphagia. Derm:
tingling, warm sensation, burning sensation,
contact dermatitis (patch only), cool
sensation, flushing. Local: injection site
reaction.MS: jaw discomfort, muscle
cramps, myalgia, neck pain, neck stiffness.
Neuro: numbness
NURSING IMPLICATIONS
Assessment
 Assess pain location, intensity, duration,
and associated symptoms (photophobia,
phonophobia, nausea, vomiting) during
migraine attack.
 Give initial subcut dose under
observation to patients with potential for
coronary artery disease including
postmenopausal women, men 40 yr,
patients with risk factors for coronary
artery disease such as hypertension,
hypercholesterolemia, obesity, diabetes,
smoking, or family history. Monitor BP
before and for 1 hr after initial injection.
If angina occurs, monitor ECG for
ischemic changes.
 Monitor for serotonin syndrome in
patients taking SSRIs or SNRIs
concurrently with sumatriptan.
Diagnoses
 Acute pain (Indications)
Implementation
 Do not confuse sumatriptan with
sitagliptin or zolmitriptan.
 PO: Tablets should be swallowed whole;
do not crush, break, or chew. Tablets
are film-coated to prevent contact with
tablet contents, which have an
unpleasant taste and may cause nausea
and vomiting.
 Subcut: Administer as a single injection
just below the skin. Solution is clear and
colorless or pale yellow; do not use
dark-colored or cloudy or if beyond
expiration date..
Patient/Family Teaching
 Inform patient that sumatriptan should
be used only duringa migraine attack. It
is meant to be used for relief of migraine
attacks but not to prevent or reduce the
number of attacks.
 Instruct patient to administer
sumatriptan as soon as symptoms of a
migraine attack appear, but it may be
administered at any time during an
attack. If migraine symptoms return, a
second injection may be used. Allow at
least 1 hr between doses, and do not
use more than two injections in any 24-
hr period. Additional sumatriptan doses
are not likely to be effective, and
alternative medications may be used. If
no relief from 1st dose, unlikely 2nd
dose will provide relief. Advise patient to
read Patient Information prior to using
and with each Rx refill; new information
may be available.
 Advise patient that lying down in a
darkened room after sumatriptan
administration may further help relieve
headache.
 Advise patient that overuse (use more
than 10 days/month) may lead to
exacerbation of headache (migraine-like
daily headaches, or as a marked
increase in frequency of migraine
attacks). May require gradual withdrawal
of sumatriptan and treatment of
symptoms (transient worsening of
headache).
Evaluation
 Relief of migraine attack.
Drug Classification:
PHENOTHIAZINES - ALIPHATIC
Generic Name: Chlorpromazine
Brand Name: Thorazine
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): Psychoses: 10–25mg (2–
4times daily)
PO (Children): Psychoses/nausea and
vomiting: 0.55mg/kg (15mg/m2) q4–6hr as
needed
IM (Adults): Severe psychoses: 25–50mg
initially, may be repeated in 1hr; to
maximum of 400 mg q3–12hr if needed
(upto1g/day)
IM (Children 6mo): Psychoses/nausea and
vomiting: 0.55mg/kg (15mg/m2) q6–8hr
IV (Adults): Nausea/vomiting during
surgery: up to 25mg
IV (Children): Nausea/vomiting during
surgery: 0.275mg/kg
DRUG ACTION
Alters the effects of dopamine in the CNS.
Has significant anticholinergic/ alpha-
adrenergic blocking activity. Therapeutic
Effects: Diminished signs/symptoms of
psychosis. Relief of nausea/vomiting/
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intractable hiccups. Decreased symptoms of
porphyria.
Pharmacokinetics: Absorption:
TABLETS: Variable absorption; IM: Well
absorbed Distribution: Widely distributed;
high CNS concentrations. Crosses the
placenta; enters breastmilk Protein
Binding: 90%. Metabolism & Excretion:
Highly metabolized by the liver and GI
mucosa. Some metabolites are active.
Half-life: 30hrs
INTERACTION
Drug-Drug: Pimozide increase the risk of
potentially serious cardiovascular. May alter
serum phenytoin levels. Decrease pressor
effect of norepinephrine and eliminates
bradycardia. Antagonizes peripheral
vasoconstriction from epinephrine and may
reverse some of its actions. May decrease
elimination and increase effects of valproic
acid. May decrease the pharmacologic
effects of amphetamine. May decrease the
effectiveness of bromocriptine. May increase
effects of tricyclic antidepressants. Antacids
or absorbent antidiarrheals may decrease
absorption. Increase risk of anticholinergic
effects with antihistamines, tricyclic
antidepressants, quinidine, or disopyramide.
INDICATIONS:
Second-line treatment for schizophrenia and
psychoses after failure with atypical
antipsychotics. Hyperexcitable, combative
behavior in children. Nausea and vomiting.
Intractable hiccups. Preoperative sedation.
Acute intermittent porphyria. Unlabeled
Use: Vascular headache. Bipolar disorder
CONTRAINDICATIONS:
Hypersensitivity; Hypersensitivity to sulfites
(injectable); Cross-sensitivity with other
phenothiazines may occur; Angle-closure
glaucoma; Bone marrow depression; Severe
liver/cardiovascular disease; Concurrent
pimozideuse
Adverse Reactions/Side Effects
CNS: NEUROLEPTIC MALIGNANT
SYNDROME, sedation, extrapyramidal
reactions, tardive dyskinesia. EENT: blurred
vision, dry eyes, lensopacities.CV:
hypotension (increase with IM, IV),
tachycardia. GI: constipation, dry mouth,
anorexia, hepatitis, ileus, priapism. GU:
urinary retention. Derm: photosensitivity,
pigment changes, rash. Endo: galactorrhea,
amenorrhea. Hemat:
AGRANULOCYTOSIS, leukopenia. Metab:
hyperthermia. Misc: allergic reactions
NURSING INTERVENTIONS
ASSESSMENT:
 Assess mental status (orientation, mood,
behavior) prior to and periodically during
therapy.
 Assess weight and BMI initially and
throughout therapy.
DIAGNOSIS:
 Disturbed thought process
 Imbalanced nutrition: risk for more than
body requirements
PLANNING:
 Pt. will have relief of nausea and vomiting
or hiccups.
 Pt. will have a decrease in positive
(hallucinations, delusions, agitation)
symptoms of schizophrenia.
IMPLEMENTATION:
 Keep patient recumbent for at least 30min
following parenteral administration to
minimize hypotensive effects.
 PO: Administer oral doses with food, milk,
or a full glass of water to minimize gastric
irritation. Tablets may be crushed.
EVALUATION:
 Evaluate for development of neuroleptic
malignant syndrome (fever, respiratory
distress, tachycardia, convulsions,
diaphoresis, hypertension, pallor,
tiredness, severe muscle stiffness, loss of
bladder control). Report these symptoms
immediately.
 Evaluate level of anxiety following
administration.
Drug Classification:
PHENOTHIAZINES - PIPERIDINE
Generic Name: Thioridazine
Brand Name: Mellaril
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults and Children 12 yr): 50– 100
mg 3 times daily initially; may be gradually
increase to a maintenance dose of up to 800
mg/day PO (Children): 0.5 mg/kg/day in
divided doses initially; may be gradually
increase to a maintenance dose of up to 3
mg/kg/day.
DRUG ACTION
Alters the effects of dopamine in the CNS.
Possesses significant anticholinergic and
alpha-adrenergic blocking
activity. Therapeutic Effects: Diminished
signs and symptoms of psychoses.
Pharmacokinetics: Absorption:
Absorption from tablets is variable
Distribution: Widely distributed, high
concentrations in the CNS. Crosses the
placenta and enters breast milk.
Protein Binding: 90%.
Metabolism and Excretion: Highly
metabolized by the liver (primarily by
CYP2D6 isoenzyme) and GI mucosa;
Page | 107
(7% of population may be poor metabolizers
and may have significantly increase
thioridazine concentrations and a risk of
adverse effects). Half-life: 21– 24 hr.
INTERACTION
Concurrent fluvoxamine, propranolol,
pindolol, fluoxetine, other agents known to
inhibit the CYP450 2D6 enzyme, or agents
known to prolong the QT interval increase
risk of life-threatening arrhythmias. Additive
CNS depression with other CNS
depressants, including alcohol,
antihistamines. Additive anticholinergic
effects with other drugs possessing
anticholinergic properties, including
antihistamines, antidepressants, other
phenothiazines, and disopyramide.
Thioridazine may mask early signs of lithium
toxicity and increase the risk of
extrapyramidal reactions. increase risk of
agranulocytosis with antithyroid agents.
Concurrent use with epinephrine may result
in severe hypotension and tachycardia.
INDICATIONS
Treatment of refractory schizophrenia.
Considered 2nd-line treatment after failure
with atypical antipsychotics.
CONTRAINDICATIONS:
Hypersensitivity; Cross-sensitivity with other
phenothiazines may exist; Angle-closure
glaucoma; Bone marrow depression; Severe
liver or cardio vascular disease; Known
alcohol intolerance; Concurrent use of
fluvoxamine, propranolol, pindolol,
fluoxetine, other agents known to inhibit the
CYP2D6 enzyme, or agents known to
prolong the QT interval (risk of life-
threatening arrrhythmias); Hypokalemia; QT
interval 450 msec
Adverse Reactions/Side Effects
CNS: NEUROLEPTIC MALIGNANT
SYNDROME, sedation, extrapyramidal
reactions, tardive dyskinesia. EENT: blurred
vision, dry eyes, lens opacities, pigmentary
retinopathy (high
doses). CV: ARRHYTHMIAS, QTC
PROLONGATION, hypotension,
tachycardia. GI: constipation, dry mouth,
anorexia, drug-induced hepatitis, ileus,
weight gain. GU: urinary retention,
priapism. Derm: photosensitivity, pigment
changes, rashes. Endo: galactorrhea,
amenorrhea. Hemat:
AGRANULOCYTOSIS,leukopenia. Metab:
hyperthermia. Misc: allergic reactions.
NURSING INTERVENTIONS
ASSESSMENT:
 Watch for signs of neuroleptic malignant
syndrome, including hyperthermia,
diaphoresis, generalized muscle rigidity,
altered mental status, tachycardia,
changes in blood pressure (BP), and
incontinence.
 Assess heart rate, ECG, and heart sounds,
especially during exercise, a rapid heart
rate (tachycardia) or signs of other
arrhythmias, including palpitations, chest
discomfort, and shortness of breath,
fainting, and fatigue/weakness.
DIAGNOSIS:
 Disturbed thought process (Indications)
 Sexual dysfunction (Side Effects)
PLANNING:
 Pt. will have decrease in positive
symptoms (hallucinations ,delusions,
agitation) of schizophrenia
IMPLEMENTATION:
 PO: Administer with food, milk, or full glass
of water to minimize gastric irritation.
 Implement fall-prevention strategies
EVALUATION:
 Evaluate signs of agranulocytosis and
leukopenia, and signs of infection
 Evaluate motor function, and be alert for
extrapyramidal symptoms.
Drug Classification:
PHENOTHIAZINES - PIPERAZINE
Generic Name: Fluphenazine
Brand Name:Prolixin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Fluphenazine Decanoate
IM (Adults): 12.5– 25 mg initially; may be
repeated q 3 wk. Dose may be slowly
increase as needed (not to exceed 100
mg/dose)
Fluphenazine Hydrochloride
PO (Adults): 0.5– 10 mg/day in divided
doses q 6– 8 hr (maximum dose 40 mg/
day).
PO (Geriatric Patients or Debilitated
Patients): 1– 2.5 mg/day initially; increase
dose every 4– 7 days by 1– 2.5 mg/day as
needed (max dose 20 mg/day).
IM (Adults): 1.25– 2.5 mg q 6– 8 hr.
DRUG ACTION
Alters the effects of dopamine in the CNS.
Has anticholinergic and alpha-adrenergic
blocking activity. Therapeutic Effects:
Diminished signs and symptoms of
psychoses
Pharmacokinetics: Absorption: Well
absorbed after PO/IM administration.
Decanoate salt in sesame oil has delayed
onset and prolonged action because of
Page | 108
delayed release from oil vehicle and
subsequent delayed release from fatty
tissues. Distribution: Widely distributed.
Crosses the blood-brain barrier. Crosses the
placenta; enters breast milk. Protein
Binding: 90%. Metabolism and Excretion:
Highly metabolized by the liver; undergo
enterohepatic recirculation. Half-life:
Fluphenazine hydrochloride—33 hr;
fluphenazine decanoate— 6.8– 9.6 days.
INTERACTION
Drug-Drug: Concurrent use with drugs that
prolong the QT interval, including
antiarrhythmics, pimozide, erythromycin,
clarithromycin, fluoroquinolones,
methadone, and tricyclic antidepressants
may increase the risk for arrhythmias;
concurrent use should be avoided. Additive
hypotension with antihypertensives. Additive
CNS depression with other CNS
depressants, including alcohol,
antidepressants, antihistamines, opioids,
sedative/hypnotics, or general anesthetics.
Effects may be decrease by phenobarbital.
May increase the risk of lithium toxicity. Oral
absorption may be decrease by aluminum-
containing antacids. May decrease anti-
Parkinson activity of levodopa and
bromocriptine. May decrease the
vasopressor response to epinephrine and
norepinephrine. Effects may be increase by
beta blockers, chlorpromazine,
chloroquine, delavirdine, fluoxetine,
paroxetine, quinidine, quinine, ritonavir, and
ropinirole. Increased risk of anticholinergic
effects with other agents having
anticholinergic properties, including
antihistamines, tricyclic antidepressants,
disopyramide, or quinidine. Metoclopramide
may increase the risk of extrapyramidal
reactions
INDICATIONS
Acute and chronic psychoses.
CONTRAINDICATIONS:
Hypersensitivity; Cross-sensitivity with other
phenothiazines may exist; Subcortical brain
damage; Severe CNS depression; Coma;
Bone marrow depression; Liver disease;
Hypersensitivity to sesame oil (decanoate
salt); Some products contain alcohol or
tartrazine and should be avoided in patients
with known intolerance; Concurrent use of
drugs that prolong the QT interval; Pedi:
Children 6
mo (safety not established)
Adverse Reactions/Side Effects CNS:
NEUROLEPTIC MALIGNANT SYNDROME,
extrapyramidal reactions, sedation, tardive
dyskinesia. EENT: blurred vision, dry eyes.
CV: hypertension, hypotension, tachycardia.
GI: anorexia, constipation, drug-induced
hepatitis, dry mouth, ileus, nausea, weight
gain. GU: urinary retention. Derm:
photosensitivity, pigment changes, rashes.
Endo: galactorrhea. Hemat:
AGRANULOCYTOSIS, leukopenia,
thrombocytopenia. Misc: allergic reactions.
NURSING INTERVENTIONS
Assessment:
 Assess mental status (orientation, mood,
behavior) before and periodically during
therapy
 Monitor BP (sitting, standing, lying), ECG,
pulse, and respiratory rate before and
frequently during the period of dose
adjustment. May cause Q-wave and T-
wave changes in ECG.
DIAGNOSIS:
 Disturbed thought process (Indications)
 Noncompliance (Patient/Family Teaching)
PLANNING:
 Pt. will have a decrease in excitable,
paranoiac, or withdrawn behavior.
IMPLEMENTATION:
 PO: Dilute concentrate just before
administration in 120– 240 mL of water,
milk, carbonated beverage, soup, or
tomato or fruit juice. Do not mix with
beverages containing caffeine (cola,
coffee), tannics (tea), or pectinates (apple
juice).
 IM: IM dose of fluphenazine hydrochloride
is usually 30– 50% of oral dose. Because
fluphenazine hydrochloride has a shorter
duration of action, it is used initially to
determine the patient’s response to the
drug and to treat the acutely agitated
patient
EVALUATION:
 Evaluate for tardive dyskinesia
(uncontrolled rhythmic movement of
mouth, face, and extremities; lip smacking
or puckering; puffing of cheeks;
uncontrolled chewing; rapid or worm-like
movements of tongue). Report
immediately; may be irreversible.
 Evaluate CBC, liver function tests, and
ocular examinations periodically during
therapy. May cause decrease hematocrit,
hemoglobin, leukocytes, granulocytes, and
platelets. May cause increase bilirubin,
AST, ALT, and alkaline phosphatase.
Agranulocytosis may occur after 4– 10 wk
of therapy with recovery 1– 2 wk after
discontinuation.
Drug Classification:
BUTYROPHENONES
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Generic Name: Haloperidol
Brand Name: Haldol
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IM (Lactate): ADULTS, ELDERLY: 2–5
mg q1–8 as needed. CHILDREN 6–
12 YRS: 1–3 mg/dose q4–8h as
needed. Maximum: 0.15 mg/kg/day. Change
to PO as soon as possible.
PO: ADULTS: 0.5–5 mg 2–3 times/day.
Usual dose: 5–20 mg/day. Maximum:
100 mg/day. ELDERLY: 0.2–2 mg/day.
Usual dose: 5–20 mg/day. Maximum:
100 mg/day. CHILDREN WEIGHING MORE
THAN 40 KG, ADOLESCENTS: 0.5–
15 mg/day in 2–3 divided doses. May
increase at no less than 5–7 days.
Maximum: 15mg/day. CHILDREN 3–12YRS
(15–40 KG): 0.5 mg/day. May increase by
0.5 mg q5–7days. Range: 0.05–
0.15mg/kg/day in 2–3 divided doses.
Maximum: 15 mg/day.
DRUG ACTION
Competitively blocks postsynaptic
DOPamine receptors in brain. Therapeutic
Effect: Produces tranquilizing effect. Strong
extrapyramidal, antiemetic effects; weak
anticholinergic, sedative effects.
Pharmacokinetics: Absorption: Readily
absorbed from GI tract Distribution:
Concentrates in liver. Crosses placenta;
enters breastmilk Protein Binding: 92%
Metabolism: Metabolized in liver
Excretion: Excreted in urine. Not removed
by hemodialysis Half-life: 20 hrs.
DRUG INTERACTION
Drug-drug: Alcohol, other CNS
depressants (e.g., diphenhydrAMINE,
gabapentin, LORazepam, morphine)
may increase CNS depression. CYP3A4
inducers (e.g., carBAMazepine) ma
decrease concentration. Medications
prolonging QT interval (e.g., amiodarone,
ciprofloxacin, ondansetron) may increase
risk of QT prolongation. Medications
producing extrapyramidal symptoms (EPS)
(e.g., diphenhydrAMINE, benztropine) may
increase EPS. HERBAL: Gotu kola, kava
kava, St. John’s wort, valerian may increase
CNS depression.
INDICATIONS
Acute and chronic psychotic disorders
including: schizophrenia, manic states, drug-
induced psychoses. Patients with
schizophrenia who require long-term
parenteral (IM) antipsychotic therapy. Also
useful in managing aggressive or agitated
patients. Tourette’s syndrome. Severe
behavioral problems in children which may
be accompanied by: unprovoked,
combative, explosive hyperexcitability,
hyperactivity accompanied by conduct
disorders (short-term use when other
modalities have failed). Considered second-
line treatment after failure with a typical
antipsychotic
CONTRAINDICATIONS:
Hypersensitivity to haloperidol, CNS
depression, coma, Parkinson’s disease,
severe cardiac/hepatic disease. Cautions:
Renal/hepatic impairment, cardiovascular
disease, history of seizures, prolonged QT
syndrome, medications that prolong QT
interval, hypothyroidism, thyrotoxicosis,
electrolyte imbalance (e.g., hypokalemia,
hypomagnesemia), EEG abnormalities,
narrow–angle glaucoma, elderly, pts at
risk for pneumonia, decreased GI motility,
urinary retention, BPH, visual disturbances,
myelosuppression.
SIDE EFFECTS
CNS: SEIZURES, extrapyramidal reactions,
confusion, drowsiness, restlessness, tardive
dyskinesia. EENT: blurred vision, dry eyes.
Resp: respiratory depression. CV:
hypotension, tachycardia, ECG changes
(QT prolongation, torsade de
pointes),ventricular arrhythmias.GI:
constipation, dry mouth, anorexia, drug-
induced hepatitis, ileus, weight gain.GU:
impotence, urinary retention. Derm:
diaphoresis, photosensitivity, rashes. Endo:
amenorrhea, galactorrhea, gynecomastia.
Hemat: AGRANULOCYTOSIS, anemia,
leukopenia, neutropenia. Metab:
hyperpyrexia. Misc: NEUROLEPTIC
MALIGNANT SYNDROME, hypersensitivity
reactions.
ADVERSE EFFECTS:
Extrapyramidal symptoms (EPS)
appear to be dose related and typically
occur in first few days of therapy. Marked
drowsiness/lethargy, excessive
salivation, fixed stare may be mild to
severe in intensity. Less frequently noted
are severe akathisia (motor restlessness),
acute dystonias: torticollis (neck muscle
spasm), opisthotonos (rigidity of back
muscles), oculogyric crisis (rolling back of
eyes). Tardive dyskinesia (tongue
protrusion, puffing of cheeks, chewing/
puckering of the mouth) may occur
during long-term therapy or after drug
discontinuance and may be irreversible.
Elderly female pts have greater risk
of developing this reaction. May increase
risk of QT interval prolongation, cardiac
arrhythmias.
Page | 110
NURSING INTERVENTIONS
Assessment:
 Assess mental status (orientation, mood,
behavior) prior to and periodically during
therapy.
 Assess positive (hallucination, delusions)
and negative (social isolation) symptoms
of schizophrenia
DIAGNOSIS:
 Disturbed thought process (Indications)
 Disturbed sensory perception (specify:
visual, auditory, kinesthetic, gustatory,
tactile, olfactory) (Indications)
PLANNING:
 Pt. will be able to decrease hallucinations,
insomnia, agitation, hostility, and
delusions.
 Pt. will be able to decreased tics and
vocalization in Tourette’s syndrome.
IMPLEMENTATION:
 Direct IV: Diluent: May be administered
undiluted for rapid control of acute
psychosis or delirium. Concentration:
5mg/mL. Rate: Administer at a rate of
5mg/min
 Intermittent Infusion: Diluent: May be
diluted in 30–50mL of D5W. Rate: Infuse
over 30min
EVALUATION:
 Monitor serum prolactin prior to and
periodically during therapy. May cause
increased serum prolactin levels.
 Lab Test Considerations: Monitor CBC
with differential and liver function tests
periodically during therapy.
Drug Classification:
DIBENZOXAPINES
Generic Name: Loxapine
Brand Name: Loxitane
DOSAGE
PO (Adults): 10 mg twice daily, may be
increase gradually over the first 7– 10 days
as needed and tolerated. Usual
maintenance dose is 60– 100 mg/day
ACTION
Appears to block dopamine and serotonin at
postsynaptic receptor sites in the CNS.
Therapeutic Effects: Diminution of
psychotic behavior.
Pharmacokinetics:
Absorption: Bioavailability is approximately
30%. Distribution: Unknown.
Metabolism and Excretion: Extensively
metabolized by the liver; some conversion to
active antipsychotic compounds. Half-life:
3– 4 hr.
DRUG INTERACTION
Drug-Drug: Blocks the alpha-adrenergic
effects of epinephrine (may result in
hypotension and tachycardia). Additive CNS
depression with other CNS depressants,
including alcohol, antihistamines, opioid
analgesics, and sedative/ hypnotics.
Antacids or adsorbent antidiarrheals may
decrease absorption. Use with
antidepressants or MAO inhibitors may
result in prolonged CNS depression and
increase anticholinergic effects.
Drug-Natural Products: Concomitant use
of kava, valerian, skullcap, chamomile, or
hops can increase CNS depression.
INDICATIONS
Schizophrenia. Considered second-line
treatment after failure of atypical
antipsychotic. Unlabeled Use: Other
psychotic disorders. Bipolar disorder.
CONTRAINDICATIONS:
Hypersensitivity or intolerance to loxapine or
amoxapine;
Coma; CNS depression; OB: Safety not
established; weigh potential benefit against
possible risks to fetus; Lactation:
Discontinue drug or bottle-feed.
SIDE EFFECTS
CNS: NEUROLEPTIC MALIGNANT
SYNDROME, confusion, dizziness,
drowsiness, extrapyramidal reactions,
headache, insomnia, syncope, tardive
dyskinesia, weakness.
EENT: blurred vision, lens opacities, nasal
congestion. CV: orthostatic hypotension,
tachycardia. GI: constipation, drug-induced
hepatitis, dry mouth, ileus, nausea,
vomiting. GU: urinary retention. Derm:
dermatitis, edema, facial photosensitivity,
pigment changes, rashes, seborrhea. Endo:
galactorrhea. Hemat:
AGRANULOCYTOSIS.Neuro:ataxia.Misc:all
ergic reactions.
ADVERSE EFFECTS:
Allergic reaction, fast heart rate; a light-
headed feeling, like you might pass out;
confusion, slurred speech; seizure
(convulsions); sudden weakness or ill
feeling, fever, chills, sore throat, cough, cold
or flu symptoms; little or no urinating; severe
constipation; or severe nervous system
reaction--very stiff (rigid) muscles, high
fever, sweating, confusion, fast or uneven
heartbeats, tremors, feeling like you might
pass out.
NURSING INTERVENTIONS
Assessment:
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 Monitor patient’s mental status
(orientation, mood, behavior) before and
periodically during therapy.
 Assess positive (delusions, hallucinations,
agitation) and negative (social withdrawal)
symptoms of schizophrenia.
Diagnosis:
 Disturbed thought process (Indications)
 Disturbed sensory perception (specify:
visual, auditory, kinesthetic, gustatory,
tactile,or olfactory) (Indications)
Planning:
 Pt. Will have a decrease in positive
symptoms of schizophrenia (hallucinations,
delusions, agitation).
 Pt. Will have a decrease in excitable,
manic behavior
Implementation:
 Po: administer tablets and capsules with
food or milk to decrease gastric irritation.
 Do not administer antacids or
antidiarrheals within 2 hr of loxapine.
Evaluation:
 Evaluate lab test considerations: monitor
cbc and differential periodically throughout
therapy.
 Evaluate for development of neuroleptic
malignant syndrome (fever, respiratory
distress, tachycardia, convulsions,
diaphoresis, hypertension or hypotension,
pallor, tiredness, severe muscle stiffness,
loss of bladder control).
Drug Classification:
DIHYDROINDOLONES
Generic Name: Molindone
Brand Name: Moban
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Adult
-Recommended dose: 50 to 75 mg orally per
day, increasing the dose to 100 mg/day in 3
to 4 days
-Maximum dose: 225 mg/day
Mild symptomology: 5 to 15 mg orally 3 to
4 times a day
Moderate symptomology: 10 to 25 mg
orally 3 to 4 times a day
Severe symptomology: Up to 225 mg/day
12 to 18 years:
Initial Dosage Schedule:
-Recommended dose: 50 to 75 mg orally per
day, increasing the dose to 100 mg/day in 3
to 4 days
-Maximum dose: 225 mg/day
Maintenance Dosing Schedule:
-Mild symptomology: 5 to 15 mg orally 3 to 4
times a day
-Moderate symptomology: 10 to 25 mg orally
3 to 4 times a day
-Severe symptomology: Up to 225 mg/day
DRUG ACTION
Blocks the effects of dopamine in the
reticular-activating and limbic systems in the
brain. Therapeutic Effects: Diminished
psychoses associated with schizophrenic
behavior.
Pharmacokinetics:
Absorption: Rapidly absorbed from the
gastrointestinal tract.
Distribution: Not Available
Metabolism: Most likely hepatic. 36
metabolites have been recognized, some of
which may be active.
Excretion: Human metabolic studies show
molindone to be rapidly absorbed and
metabolized when given orally. There are 36
recognized metabolites with less than 2-3%
unmetabolized molindone being excreted in
urine and feces.
DRUG INTERACTION
The risk or severity of adverse effects can
be increased when Acepromazine and
Aceprometazine is combined with
Molindone. Molindone may increase the
antipsychotic activities of Amisulpride.
Molindone may decrease the stimulatory
activities of Amphetamine. Molindone may
increase the central nervous system
depressant (CNS depressant) activities of
Anisotropine methylbromide.
INDICATIONS
Schizophrenia. Second-line treatment after
failure with atypical
antipsychotics. Unlabeled Use: Other
psychotic disorders. Bipolar Disorder.
CONTRAINDICATIONS:
Hypersensitivity to molindone and sulfite
hypersensitivity. Caution: Agranulocytosis,
hematological disease, leukopenia,
neutropenia
Adverse Reactions/Side Effects
CNS: NEUROLEPTIC MALIGNANT
SYNDROME, extrapyramidal
reactions, sedation, depression, dizziness,
euphoria, headache, insomnia, tardive
dyskinesia. EENT: blurred vision, dry eyes,
nasal congestion. CV: hypotension,
tachycardia. GI: constipation, dry mouth,
anorexia, drug-induced hepatitis,
nausea. Derm: photosensitivity,
rashes. Endo: galactorrhea, increased
libido, irregular menses. Misc: allergic
reactions.
NURSING INTERVENTIONS
Assessment:
 Assess motor function, and be alert for
extrapyramidal symptoms.
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 Assess heart rate, ecg, and heart sounds,
especially during exercise
Diagnosis:
 Disturbed thought process (indications)
 Disturbed sensory perception (specify:
visual, auditory, kinesthetic, gustatory,
tactile,or olfactory) (indications)
Planning:
 Pt. Will be able to decrease hallucinations,
insomnia, agitation, hostility, and
delusions.
 Pt. Will be able to decreased tics and
vocalization in tourette’s syndrome.
Implementation:
 Guard against falls and trauma (hip
fractures, head injury, and so forth) caused
by drowsiness, blurred vision, or
extrapyramidal symptoms; implement fall
prevention strategies
 Because of the risk of tachycardia and
abnormal bp responses, use caution
during aerobic exercise and other forms of
therapeutic exercise.
Evaluation:
 Be alert for depression, euphoria, or other
changes in mood and behavior. Notify
physician if these changes become
problematic.
 Monitor signs of allergic reactions,
including pulmonary symptoms (laryngeal
edema, wheezing, dyspnea) or skin
reactions (rash, pruritus, urticaria).
Drug Classification:
THIOXANTHENES
Generic Name: Thiothixene
Brand Name: Navane
DOSAGE
PO (Adults): Mild conditions—2 mg 3
times daily (up to 15 mg/day if necessary;
Severe conditions—5 mg twice daily (up to
20– 30 mg/day; not to exceed 60 mg/
day).
ACTION
Alters the effect of dopamine in the CNS.
Therapeutic Effects: Diminished signs
And symptoms of psychoses.
Pharmacokinetics:
Absorption: Well absorbed following oral
administration.
Distribution: Widely distributed; crosses the
placenta.
Metabolism and Excretion: Mainly
metabolized by the liver.
Half-life: 30 hr.
DRUG INTERACTION
Drug-Drug: Additive hypotension with
antihypertensives, acute ingestion of
alcohol, and nitrates. Additive hypotension
may occur if epinephrine is given to
treat hypotension. Additive CNS depression
with other CNS depressants, including
alcohol, antihistamines, antidepressants,
opioid analgesics, and sedative/
hypnotics. Additive anticholinergic effects
with other drugs having anticholinergic
properties, including antihistamines,
antidepressants, quinidine, or disopyramide.
May dercease the effectiveness of levodopa.
increase risk of cardiac effects with
quinidine
INDICATIONS
Schizophrenia. Considered second-line
treatment after failure with atypical
antipsychotics.Unlabeled Use: Other
psychotic disorders, Bipolar disorder.
CONTRAINDICATIONS:
Hypersensitivity to thiothixene or other
phenothiazines
(cross-sensitivity may occur); Circulatory
collapse; Blood dyscrasias; Central nervous
system depression.
SIDE EFFECTS:
CNS: NEUROLEPTIC MALIGNANT
SYNDROME, extrapyramidal reactions,
sedation, tardive
dyskinesia, seizures. EENT: blurred vision,
dry eyes, lens opacities. CV: hypotension,
tachycardia, non-specific ECG changes. GI:
constipation, dry mouth, anorexia,
ileus, nausea. GU: urinary retention. Derm:
photosensitivity, pigment changes,
rashes. Endo: amenorrhea, breast
enlargement, galactorrhea. Hemat:
AGRANULOCYTOSIS, leukocytosis,
leukopenia, neutropenia. Metab:
hyperpyrexia. Misc: allergic reactions.
ADVERSE EFFECTS:
Twitching or uncontrollable movements of
your eyes, lips, tongue, face, arms, or legs;
stiffness in your neck, tightness in your
throat, trouble breathing or swallowing;
seizure (convulsions)
NURSING INTERVENTIONS
ASSESSMENT:
 Monitor patient’s mental status
(orientation, mood, behavior) prior to and
periodically during therapy.
 Assess weight and BMI initially and
throughout therapy
DIAGNOSIS:
 Disturbed thought process (Indications)
 Sexual dysfunction (Side Effects)
Page | 113
PLANNING:
 Decrease in positive symptoms
(hallucinations, delusions, agitation) of
schizophrenia.
 Decrease in excited, manic behavior
IMPLEMENTATION:
 Decrease in positive symptoms
(hallucinations, delusions, agitation) of
schizophrenia.
 Decrease in excited, manic behavior
EVALUATION:
 Evaluate development of neuroleptic
malignant syndrome (fever, respiratory
distress, tachycardia, convulsions,
diaphoresis, hypertension or hypotension,
pallor, tiredness, severe muscle stiffness,
loss of bladder control).
 Monitor for symptoms related to
hyperprolactinemia (menstrual
abnormalities, galactorrhea, sexual
dysfunction).
Drug Classification: ATYPICAL
ANTIPSYCHOTICS
Generic Name: Clozapine
Brand Name: Clozaril
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO: ADULTS: Initially, 12.5 mg
once or twice daily. May increase by
25–50 mg/day over 2 wks until target
dose of 300–450 mg/day is achieved.
May further increase by 50–100 mg/day
no more than once or twice wkly.
Range: 200–600 mg/day. Maximum: 900
mg/day. ELDERLY: Initially, 12.5 mg/day for
3 days, then 25 mg/day for 3 days. May
further increase in increments of 12.5–25
mg daily q3days. Mean dose: 300
mg/day. Maximum: 700 mg/day
DRUG ACTION
Interferes with binding of DOPamine and
serotonin receptor sites. Therapeutic
Effect: Diminishes schizophrenic behavior.
Pharmacokinetics: Absorption: Readily
absorbed from GI tract Distribution: Rapid
and extensive distribution; crosses blood-
brain barrier and placenta.
Protein Binding: 97% Metabolism:
Metabolized in liver Excretion: Excreted in
urine. Half-life: 12 hrs
DRUG INTERACTION
DRUG-DRUG: Antihypertensive
medications may increase risk of
hypotension. Alcohol, other CNS
depressants (e.g., lorazepam, morphine,
zolpidem) may increase CNS depressant
effects. Bone marrow depressants may
increase myelosuppression. Cimetidine,
citalopram, ciprofloxacin, erythromycin may
increase concentration. SSRIs (e.g.,
PARoxetine) may increase concentration.
Lithium may increase risk of confusion,
dyskinesia, and seizures. CYP3A4 inducers
(e.g., phenytoin, carbamazepine, rifAMPin)
may decrease concentration/effects.
HERBAL: St. John’s wort may
decrease concentration/ therapeutic effects.
Kava kava, gotu kola, valerian, St. John’s
wort may increase risk of CNS depression.
INDICATIONS
Schizophrenia unresponsive to or intolerant
of standard therapy with other antipsychotics
(treatment refractory).To reduce recurrent
suicidal behavior in schizophrenic patients.
CONTRAINDICATIONS:
Hypersensitivity; Bone marrow depression;
Severe CNS depression/coma; Uncontrolled
epilepsy; Clozapine-induced agranulocytosis
or severe granulocytopenia Lactation:
Discontinue drug or bottle-feed.
Adverse Reactions/Side Effects
CNS: NEUROLEPTIC MALIGNANT
SYNDROME, SEIZURES, dizziness,
sedation. EENT: visual disturbances. CV:
CARDIAC ARREST, DEEP VEIN
THROMBOSIS, MYOCARDITIS,
TORSADE DE POINTES, VENTRICULAR
ARRHYTHMIAS, hypotension, tachycardia,
bradycardia, ECG changes, hypertension,
syncope, QT interval prolongation. GI:
constipation, abdominal discomfort, dry
mouth, increased salivation, nausea,
vomiting, weight gain.GU: nocturnal
enuresis. Derm: rash, sweating. Endo:
hyperglycemia, hyperlipidemia, weight gain.
Hemat: AGRANULOCYTOSIS,
LEUKOPENIA. Neuro: extrapyramidal
reactions. Resp: PULMONARY
EMBOLISM. Misc: fever.
NURSING INTERVENTIONS
Assessment:
 Obtain baseline weight, glucose,
hgb a1c, wbc, absolute neutrophil
count (anc) before initiating treatment.
 Assess behavior, appearance,
emotional status, response to
environment, speech pattern, thought
content
Diagnosis:
 Disturbed thought process (indications)
 Risk for injury (sideeffects)
Planning:
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 Pt. Will be able to decrease positive
symptoms (delusions, hallucinations) of
schizophrenia.
 Pt. Will be able to decrease negative
symptoms (social withdrawal, flat, blunt
affect) of schizophrenia
Implementation:
 Po:administer capsules with food or milk to
decrease gastric irritation.
 Leave oral disintegrating tablet in blister
until time of use. Do not push tablet
through foil. Just before use,peel foil and
gently remove disintegrating tablet.
Immediately place tablet in mouth and
allow to disintegrate and swallow with
saliva
Evaluation:
 Monitor patient for onset of akathisia
(restlessness or desire to keep moving)
and extrapyramidal side effects
 Monitor frequency and consistency of
bowel movements. Increasing bulk and
fluids in the diet may help to minimize
constipation.
Drug Classification:
BENZODIAZEPINES
Generic Name: Diazepam
Brand Name: Valium
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO: ADULTS: Initially, 12.5 mg
once or twice daily. May increase by
25–50 mg/day over 2 wks until target
dose of 300–450 mg/day is achieved.
May further increase by 50–100 mg/day
no more than once or twice wkly. Range:
200–600 mg/day. Maximum: 900 mg/day.
ELDERLY: Initially, 12.5 mg/day for 3 days,
then 25 mg/day for 3 days. May further
increase in increments of 12.5–25 mg daily
q3days. Mean dose: 300 mg/day.
Maximum: 700 mg/day
DRUG ACTION
Depresses the CNS, probably by
potentiating GABA, an inhibitory
neurotransmitter. Produces skeletal muscle
relaxation by inhibiting spinal polysynaptic
afferent pathways. Has anticonvulsant
properties due to enhanced presynaptic
inhibition. Therapeutic Effects: Relief of
anxiety. Sedation. Amnesia. Skeletal muscle
relaxation. Decreased seizure activity
Pharmacokinetics:
Absorption: Rapidly absorbed from the GI
tract. Absorption from IM sites may be slow
and unpredictable. Well absorbed (90%)
from rectal mucosa. Distribution: Widely
distributed. Crosses the blood-brain barrier.
Crosses the placenta; enters breast milk
Protein Binding: 98% Metabolism:
Metabolized in liver Excretion: Excreted in
urine. Half-life: 20–70 hrs (increased
in hepatic dysfunction, elderly).
DRUG INTERACTION
Drug-Drug: Alcohol, antidepressants,
antihistamines, and opioid analgesics—
concurrent use results in additive CNS
depression. Cimetidine, hormonal
contraceptives, disulfiram, fluoxetine,
isoniazid, ketoconazole, metoprolol,
propranolol, or valproic acid may decrease
the metabolism of diazepam, enhancing its
actions. May decrease the efficacy of
levodopa. Rifampin or barbiturates may
increase the metabolism and decrease
effectiveness of diazepam. Sedative effects
may be decrease by theophylline.
Concurrent use of ritonavir is not
recommended.
INDICATIONS
Adjunct in the management of: Anxiety
Disorder, Athetosis, Anxiety relief prior to
cardioversion (injection), Stiffman
Syndrome, Preoperative sedation,
Conscious sedation (provides light
anesthesia and anterograde amnesia).
Treatment of status epilepticus/uncontrolled
seizures (injection). Skeletal muscle
relaxant. Management of the
symptoms of alcohol withdrawal
CONTRAINDICATIONS:
Hypersensitivity; Cross-sensitivity with other
benzodiazepines may occur; Comatose
patients; Myasthenia gravis; Severe
pulmonary impairment; Sleep apnea; Severe
hepatic dysfunction; Pre-existing CNS
depression; Uncontrolled severe pain;
Angle-closure glaucoma
Adverse Reactions/Side Effects
CNS: dizziness, drowsiness, lethargy,
depression, hangover, ataxia, slurred
speech,
headache, paradoxical excitation. EENT:
blurred vision. Resp: RESPIRATORY
DEPRESSION. CV: hypotension (IV only).
GI: constipation, diarrhea (may be caused
by propylene glycol content in oral solution),
nausea, vomiting, weight gain. Derm:
rashes. Local: pain (IM), phlebitis (IV),
venous thrombosis. Misc: physical
dependence, psychological dependence,
tolerance
NURSING INTERVENTIONS
Assessment:
 Assess b/p, pulse, respirations.
Page | 115
 Assess autonomic response (cold,
clammy hands; diaphoresis), motor
response (agitation, trembling, tension).
Diagnosis:
 Ineffective airway clearance (indications)
Planning:
 Pt. Will be able to decrease anxiety level.
Full therapeutic antianxiety effects occur
after 1–2wk of therapy..
 Pt. Will be able to decrease recall of
surgical or diagnostic procedures.
Implementation:
 Po:do not give fluids immediately after
administering to prevent dilution of vehicle.
Shake oral suspension well before
administration
Evaluation:
 Evaluate for therapeutic response
(decrease in intensity/frequency of
seizures; calm facial expression,
decreased restlessness; decreased
intensity of skeletal muscle pain).
Drug Classification: AZAPIRONES
Generic Name: Buspirone HCl
Brand Name: Buspar
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 7.5 mg twice daily;qby 5
mg/day q 2– 4 days as needed (not to
exceed
60 mg/day). Usual dose is 20– 30 mg/day
(in 2 divided doses)
DRUG ACTION
Binds to serotonin and dopamine receptors
in the brain. Increases norepinephrine
metabolism in the brain. Therapeutic Effects:
Relief of anxiety
Pharmacokinetics: Absorption: Rapidly
absorbed. Distribution: Unknown. Protein
Binding: 95% bound to plasma proteins.
Metabolism and Excretion: Extensively
metabolized by the liver (CYP3A4 enzyme
system); 20– 40% excreted in feces. Half-
life: 2– 3 hr
DRUG INTERACTION
Drug-Drug: Use with MAO inhibitors may
result in hypertension and is not
recommended. Erythromycin, nefazodone,
ketoconazole, itraconazole, ritonavir, and
other inhibitors of CYP3A4 increased blood
levels and effects of buspirone; dose
reduction is recommended (decrease to 2.5
mg twice daily with erythromycin; decrease
to 2.5 mg once daily with nefazodone).
Rifampin, dexamethasone, phenytoin,
phenobarbital, carbamazepine, and other
inducers of CYP3A4pblood levels and
effects of buspirone; dose adjustment may
be necessary. Avoid concurrent use with
alcohol.
Drug-Food: Grapefruit juice q serum levels
and effect; ingestion of large amounts of
grapefruit juice is not recommended.
INDICATIONS
Management of anxiety.
CONTRAINDICATIONS:
Hypersensitivity; Severe hepatic or renal
impairment; Concurrent use of MAO
inhibitors; Ingestion of large amounts of
grapefruit juice
SIDE EFFECTS
CNS: dizziness, drowsiness, excitement,
fatigue, headache, insomnia, nervousness,
weakness, personality changes. EENT:
blurred vision, nasal congestion, sore throat,
tinnitus, altered taste or smell, conjunctivitis.
Resp: chest congestion, hyperventilation,
shortness of breath. CV:chest pain,
palpitations, tachycardia, hypertension,
hypotension, syncope. GI: nausea,
abdominal pain, constipation, diarrhea, dry
mouth,
vomiting. GU: changes in libido, dysuria,
urinary frequency, urinary hesitancy.
Derm: rashes, alopecia, blisters, dry skin,
easy bruising, edema, flushing, pruritus.
Endo: irregular menses. MS: myalgia.
Neuro: incoordination, numbness,
paresthesia, tremor.Misc:clamminess,
sweating, fever.
ADVERSE EFFECTS:
IV route may produce pain, swelling,
thrombophlebitis, carpal tunnel syndrome.
Abrupt or too-rapid withdrawal may result in
pronounced restlessness, irritability,
insomnia, hand tremor, abdominal/muscle
cramps, diaphoresis, vomiting, seizures.
Overdose results in drowsiness, confusion,
diminished reflexes, CNS depression, coma.
NURSING INTERVENTIONS
Assessment:
● assess degree and manifestations of
anxiety before and periodically during
therapy.
● patients with a history of substance use
disorder should be assessed for tolerance
or impaired control. Restrict amount of
drug available to these patients.
Diagnosis:
 Anxiety (indications)
 Risk for injury (side effects)
Planning:
Page | 116
 Pt. Will be able to decrease anxiety level.
Full therapeutic antianxiety effects occur
after 1–2wk of therapy..
 Pt. Will be able to decrease recall of
surgical or diagnostic procedures.
Implementation:
● patients changing from other antianxiety
agents should receive gradually
decreasing doses. Buspirone will not
prevent withdrawal symptoms.
● po: may be administered with food to
minimize gastric irritation. Food slows but
does not alter extent of absorption
Evaluation:
 Evaluate for therapeutic response: calm
facial expression, decreased restlessness,
lessened insomnia, mental status.
Drug Classification:
BENZODIAZEPINE ANTAGONIST
Generic Name: Flumazenil
Brand Name: Romazicon
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
injectable solution
0.1mg/mL
ADULT
0.2 mg IV over 15 sec
IF after 45 sec no response, administer 0.2
mg again over 1 min; may repeat at 1 min
intervals; not to exceed 4 doses (1 mg)
IF resedation occurs, may repeat doses at
20-min intervals; not to exceed 1 mg/dose or
3 mg/hr
DRUG ACTION
Flumazenil is a benzodiazepine derivative
that antagonizes the CNS depressant
effects
of benzodiazepine compounds. It has no
effect on CNS depression from other
causes,
including opioids, alcohol, barbiturates, or
general anesthetics. Therapeutic Effects:
Reversal of benzodiazepine effects.
Pharmacokinetics:
Absorption: IV administration results in
complete bioavailability.
Distribution: Unknown.
Protein Binding: 50% primarily to albumin.
Metabolism and Excretion: Metabolism of
flumazenil occurs primarily in the
liver.
Half-life: Children: 20– 75 min; Adults:
41– 79 min
DRUG INTERACTION
Drug-Drug: None significant.
INDICATIONS
Complete/partial reversal of effects of
benzodiazepines used as general
anesthetics, or during diagnostic or
therapeutic procedures. Management of
intentional or accidental overdose of
benzodiazepines
CONTRAINDICATIONS:
Hypersensitivity to flumazenil or
benzodiazepines; Patients
receiving benzodiazepines for life-
threatening medical problems, including
status epilepticus or increase intracranial
pressure; Serious cyclic antidepressant over
dosage
Adverse Reactions/Side Effects CNS:
SEIZURES, dizziness, agitation, confusion,
drowsiness, emotional lability, fatigue,
headache, sleep disorders. EENT: abnormal
hearing, abnormal vision,
blurred vision. CV:arrhythmias, chest pain,
hypertension.GI: nausea, vomiting, hiccups.
Derm: flushing, sweating. Local:
pain/injection-site reactions, phlebitis.
Neuro: paresthesia.Misc:rigors, shivering
NURSING INTERVENTIONS
ASSESSMENT:
 Assess level of consciousness and
respiratory status before and during
therapy. Observe patient for at least 2 hr
after administration for the appearance of
resedation. Hypoventilation may occur.
 Overdose: Attempt to determine time of
ingestion and amount and type of
benzodiazepine taken. Knowledge of
agent ingested allows an estimate of
duration of CNS depression.
DIAGNOSIS:
 Risk for injury (Indications)
 Risk for poisoning (Indications)
PLANNING:
 Pt. will be able to respiratory depression
caused by benzodiazepines.
 Pt. will be able to Improved level of
consciousness
IMPLEMENTATION:
 Institute seizure precautions. Seizures are
more likely to occur in patients who are
experiencing sedative/hypnotic withdrawal,
patients who have recently received
repeated doses of benzodiazepines, or
those who have a previous history of
seizure activity. Seizures may be treated
with benzodiazepines, barbiturates, or
phenytoin. Larger than normal doses of
benzodiazepines may be required.
 Suspected Benzodiazepine Overdose: If
no effects are seen after administration of
Page | 117
 flumazenil, consider other causes of
decreased level of consciousness (alcohol,
barbiturates, opioid analgesics).
EVALUATION:
 Evaluate for therapeutic response: calm
facial expression, decreased restlessness,
lessened insomnia, mental status.
Drug Classification: TRICYCLIC
ANTIDEPRESSANTS (TCAs)
Generic Name: Clomipramine HCl
Brand Name: Anafranil
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Obsessive-Compulsive Disorder (OCD)
PO: ADULTS, ELDERLY: Initially,
25mg/day. May gradually increase to 100
mg/day in divided doses in the first 2 wks.
Maximum: 250 mg/day.
CHILDREN 10 YRS AND OLDER: Initially,
25 mg/day. May gradually increase up to
maximum of 3 mg/kg/day or 100 mg in
divided doses (whichever is lowest).
Maintenance: May further increase to 3
mg/kg or 200 mg/day (whichever is less).
DRUG ACTION
Blocks reuptake of neurotransmitters
(norepinephrine, serotonin) at CNS
presynaptic membranes, increasing
availability at postsynaptic receptor sites.
Therapeutic Effect: Reduces obsessive-
compulsive behavior.
Pharmacokinetics:
Absorption: Rapidly absorbed
Distribution: Widely distributed.
Metabolism: Metabolized in liver
Excretion: Eliminated in urine (51%–60%),
feces (24%–32%).
Half-life: 20–30 hrs
DRUG INTERACTION
DRUG: Alcohol, other CNS depressants
(e.g., lorazepam, morphine, zolpidem) may
increase CNS, respiratory depression,
hypotensive effect. Cimetidine,
haloperidol may increase
concentration, risk of toxicity.
May decrease effects of cloNIDine.
Phenobarbital may decrease
concentration, antidepressant effect.
MAOIs (e.g., phenelzine, selegiline) may
increase risk of neuroleptic malignant
syndrome, seizures, hyperpyresis,
hypertensive crisis. Phenothiazines (e.g.,
chlorpromazine, thioridazine) may
increase anticholinergic, sedative effects.
Sympathomimetics (e.g., dopamine,
norepinephrine) may increase the risk of
cardiac effects. FOOD: Grapefruit products
may increase concentration, toxicity
INDICATIONS
Treatment of obsessive-compulsive
disorder. OFF-LABEL: Depression, panic
attacks.
CONTRAINDICATIONS:
Hypersensitivity to clomiPRAMINE, other
tricyclic agents. Acute recovery period
after MI, use of MAOIs intended for
psychiatric disorders (concurrently or within
14 days of discontinuing either clomipramine
or MAOI). Initiation in pts receiving linezolid
or methylene blue.
SIDE EFFECTS
Frequent (30%–15%): Ejaculatory failure,
dry mouth, somnolence, tremors, dizziness,
headache, constipation, fatigue, nausea.
Occasional (14%–5%): Impotence,
diaphoresis, dyspepsia, sexual dysfunction,
dysmenorrhea, nervousness, weight gain,
pharyngitis. Rare (less than 5%):
Diarrhea, myalgia, rhinitis, increased
appetite, paresthesia, memory
impairment, anxiety, rash, pruritus,
anorexia, abdominal pain, vomiting,
flatulence, flushing, UTI, back pain.
ADVERSE EFFECTS:
Overdose may produce seizures,
cardiovascular effects (severe orthostatic
hypotension, dizziness, tachycardia,
palpitations, arrhythmias), altered
temperature regulation (hyperpyrexia,
hypothermia). Abrupt discontinuation after
prolonged therapy may produce headache,
malaise, nausea, vomiting, vivid dreams.
Anemia, agranulocytosis have been noted.
NURSING INTERVENTIONS
Assessment:
 Assess psychological status,
thought content, level of interest,
mood, behavior, suicidal ideation.
Diagnosis:
 Disturbed thought process (indications)
 Risk for injury (sideeffects)
Planning:
 Pt. Will be able to control obsessive-
compulsive disorder.
Implementation:
 Supervise suicidal-risk pt. Closely during
early therapy (as depression lessens,
energy level improves, increasing suicide
potential).
 Daily dose may be given at bedtime to
minimize daytime sedation.
Evaluation:
 Monitor patient for onset of akathisia
(restlessness or desire to keep moving)
and extrapyramidal side effects
Page | 118
 Monitor frequency and consistency of
bowel movements. Increasing bulk and
fluids in the diet may help to minimize
constipation
Drug Classification: SELECTIVE
SEROTONIN REUPTAKE
INHIBITORS (SSRIs)
Generic Name: Citalopram
Brand Name: Celexa
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO(Adults): 20mg once daily initially, may
be increase in 1 wk to 40mg/day (maximum
dose); Poor metabolizer of CYP2C19 or
concurrent use of CYP2C19 inhibitor—Do
not exceed dose of 20mg/day. PO
(Geriatric Patients): 20mg once daily
initially (do not exceed dose of 20mg/day in
patients 60yr).
DRUG ACTION
Selectively inhibits there uptake of serotonin
in the CNS. Therapeutic Effects:
Antidepressant action
Pharmacokinetics:
Absorption: 80% absorbed after oral
administration.
Distribution: Enters breastmilk.
Metabolism: Mostly metabolized by the liver
(10% by CYP3A4 and 2C19 enzymes)
Excretion: Excreted in urine
Half-life: 35 hrs
DRUG INTERACTION
DRUG: CYP2C19 inhibitors (e.g.,
fluconazole), other medications prolonging
QT interval (e.g., amiodarone, azithromycin,
ciprofloxacin, haloperidol) may increase
risk of QT prolongation. Linezolid, MAOIs
(e.g., phenelzine, selegiline), triptans may
cause serotonin syndrome (excitement,
diaphoresis, rigidity, hyperthermia,
autonomic hyperactivity, coma).
INDICATIONS
Treatment of depression. OFF-LABEL:
Treatment of alcohol abuse, diabetic
neuropathy, obsessive-compulsive disorder,
smoking cessation, GAD, panic disorder.
CONTRAINDICATIONS:
Hypersensitivity to citalopram, use of MAOIs
intended to treat psychiatric disorders
(concurrently or within 14 days of
discontinuing either citalopram or MAOI),
initiation in pts receiving linezolid or
methylene blue. Concurrent use with
pimozide.
Adverse Reactions/Side Effects
CNS: NEUROLEPTIC MALIGNANT
SYNDROME, SUICIDAL THOUGHTS,
apathy, confusion, drowsiness, insomnia,
weakness,agitation,amnesia,anxiety,plibido,
dizziness,fatigue,impairedconcentration,qde
pression, migraine headache. EENT:
abnormal accommodation. Resp: cough.CV:
TORSADE DE POINTES, postural
hypotension, QT interval prolongation,
tachycardia. GI: abdominal pain, anorexia,
diarrhea, dry mouth, dyspepsia, flatulence,
increase saliva, nausea, altered taste,
increase appetite, vomiting. GU:
amenorrhea, dysmenorrhea, ejaculatory
delay, erectile dysfunction, polyuria. Derm:
sweating, photosensitivity, pruritus, rash.
Metab: weightloss, weight gain. F and E:
hyponatremia. MS: arthralgia, myalgia.
Neuro: tremor, paresthesia. Misc:
SEROTONIN SYNDROME, fever, yawning.
NURSING INTERVENTIONS
ASSESSMENT:
 Monitor mood changes during therapy.
 Assess for sexual dysfunction (erectile
dysfunction; decreased libido).
DIAGNOSIS:
 Ineffective coping (Indications)
 Risk for injury (Side Effects)
 Sexual dysfunction (Side Effects)
PLANNING:
 Pt. will be able to Increase sense of well-
being.
 Pt. will be able to renew interest in
surroundings.
IMPLEMENTATION:
 PO: Administer as a single dose in the
morning or evening without regard to food.
 Supervise suicidal-risk pt closely
during early therapy (as depression
lessens, energy level improves,
increasing suicide potential).
EVALUATION:
 Report worsening depression,
suicidal ideation, and unusual
changes in behavior.
 Lab Test Considerations: Monitor
electrolytes (potassium and magnesium) in
patients at risk for electrolyte imbalances
prior to and periodically during therapy.
Drug Classification: SEROTONIN
NOREPINEPHRINE REUPTAKE
INHIBITORS (SNRIs)
Generic Name: Duloxetine
Brand Name: Cymbalta
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO(Adults): Major depressive disorder: 40–
60 mg/day (as 20mg or 30mg twice daily or
as 60mg once daily) as initial therapy, then
Page | 119
60mg once daily as maintenance therapy;
Generalized anxiety disorder—30–60mg
once daily as initial therapy (if initiated on
30mg once daily, should titrate to 60mg
once daily after 1wk), then 60–120mg once
daily as maintenance therapy; Neuropathic
pain—60mgonce daily; Fibromyalgia—
30mg once daily for 1wk, then increase to
60mg once daily.
DRUG ACTION
Appears to inhibit serotonin and
norepinephrine reuptake at CNS neuronal
presynaptic membranes; is a less
potent inhibitor of DOPamine reuptake.
Therapeutic Effect: Produces
antidepressant effect.
Pharmacokinetics:
Absorption: Well absorbed following oral
administration.
Distribution: Protein binding: greater than
90%.
Metabolism: Mostly metabolized, primarily
by the CYP2D6 and CYP1A2 enzyme
pathways.
Excretion: Excreted in urine (70%), feces
(20%).
Half-life: 12hr.
DRUG INTERACTION
DRUG: Alcohol increases risk of hepatic
injury. CYP1A2 and CYP2D6 inhibitors
may increase plasma concentration. Aspirin,
NSAIDs (e.g., ibuprofen, ketorolac,
naproxen) may increase risk of bleeding.
May increase concentration, potential
toxicity of tricyclic antidepressants.
Serotonergic drugs (e.g., triptans, lithium,
traMADol) may increase risk of serotonin
syndrome.
INDICATIONS
Major depressive disorder. Diabetic
peripheral neuropathic pain. Generalized
anxiety disorder. Fibromyalgia. Chronic
musculoskeletal pain (including chronic
lower back pain and chronic pain from
osteoarthritis).Unlabeled Use: Stress
urinary incontinence
CONTRAINDICATIONS:
Hypersensitivity; Concurrent use of MAO
inhibitors or MAO-like drugs (linezolid or
methylene blue);Uncontrolled angle-closure
glaucoma; End-stage renal disease; Chronic
hepatic impairment or substantial alcohol
use (increased risk of hepatitis); Lactation:
May enter breastmilk; discontinue or bottle-
feed.
Adverse Reactions/Side Effects
CNS: NEUROLEPTIC MALIGNANT
SYNDROME,SEIZURES, SUICIDAL
THOUGHTS, fatigue, drowsiness ,insomnia,
activation of mania, dizziness, nightmares.
EENT: blurred vision, increase intraocular
pressure. CV: increase BP. GI:
HEPATOTOXICITY, decrease appetite,
constipation, dry mouth, nausea diarrhea,
increase liver enzymes, gastritis, vomiting.
FandE: hyponatremia.GU: dysuria,
abnormal orgasm, erectile dysfunction,
decrease libido, urinary retention. Derm:
ERYTHEMA MULTIFORME, STEVENS-
JOHNSON SYNDROME, increase sweating,
pruritus, rash. Neuro: tremor. Misc:
SEROTONIN SYNDROME.
NURSING INTERVENTIONS
Assessment:
 Assess for sexual dysfunction (erectile
dysfunction; decreased libido).
 Monitor bp before and periodically during
therapy. Sustained hypertension may be
dose related; decreased dose or
discontinue therapy if this occurs.
Diagnosis:
 Ineffective coping (indications)
 risk for suicide(adverse reactions)
 Chronic pain (indications)
Planning:
 Pt. Will be able to decrease in neuropathic
pain associated with diabetic peripheral
neuropathy.
 pt. Will be able to decrease in anxiety.
Implementation:
 Po: may be administered without regard to
meals.
 Capsules should be swallowed whole. Do
not crush, chew, or open and sprinkle
contents on food or liquids; may affect
enteric coatin
Evaluation:
 Depression: assess mental status
(orientation, mood, and behavior). Inform
healthcare professional if patient
demonstrates significant increase in
anxiety, nervousness, or insomnia.
 Monitor blood sugar and hemoglobin A1C.
May cause slight increase in blood
glucose.
Drug Classification: MONOAMINE
OXIDASE INHIBITORS (MAOIs)
Generic Name: Phenelzine Sulfate
Brand Name: Nardil
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 15mg 3times daily; increase to
60–90mg/day in divided doses; after
maximal benefit achieved, gradually reduce
to smallest effective dose (15mg/day or
every other day).
Page | 120

DRUG ACTION
Inhibit the enzyme monoamine oxidase,
resulting in an accumulation of various
neurotransmitters (dopamine, epinephrine,
norepinephrine, and serotonin) in the body.
Therapeutic Effects: Improved mood in
depressed patients.
Pharmacokinetics:
Absorption: Well absorbed from the GI
tract;
Distribution: Cross the placenta and enter
breastmilk
Metabolism: Metabolized by the liver
Excretion: Excreted in urine as metabolites
and unchanged drug
Half-life: 12hr.
DRUG INTERACTION
Drug:Serious, potentially fatal adverse
reactions may occur with concurrent use of
other antidepressants (SSRIs, SSNRIs,
buproprion, tricyclics, tetracyclics,
nefazodone, trazodone), carbamazepine,
cyclobenzaprine, linezolid, procarbazine, or
selegiline. Hypertensive crisis may occur
with amphetamines, methyldopa, levodopa,
dopamine, epinephrine, norepinephrine,
methylphenidate, reserpine, or
vasoconstrictors. Hypertension or
hypotension, coma, seizures, respiratory
depression, and death may occur with
meperidine. Concurrent use with
dextromethorphan may produce psychosis
or bizarre behavior. Hypertension may occur
with concurrent use of buspirone. Additive
hypotension may occur with
antihypertensives, spinal anesthesia,
opioids, or barbiturates. Risk of seizures
may be increase with tramadol.
Drug-Food: Hypertensive crisis may occur
with ingestion of foods containing high
concentrations of tyramine. Consumption of
foods or beverages with high caffeine
content increase the risk of hypertension
and arrhythmias
INDICATIONS
Depression in patients who have failed other
modes of therapy (tricyclic antidepressants,
SSRIs, SSNRIs or electroconvulsive
therapy).
CONTRAINDICATIONS:
Hypersensitivity; Liver disease; Severe renal
disease; Cardiovascular disease;
Uncontrolled hypertension; Cerebrovascular
disease; Pheochromocytoma; Patients
undergoing elective surgery requiring
anesthesia. Concurrent nefazodone,
trazodone, procarbazine, selegilene,
linezolid, carbamazepine, cyclobenzaprine,
buspirone, dextromethorphan, narcotics,
alcohol, anesthetics, diuretics, tryptophan,
orantihistamines; Excessive consumption of
caffeine; tyramine, Lactation.
Adverse Reactions/Side Effects
CNS: SEIZURES, dizziness, headache,
anxiety, ataxia, confusion, drowsiness,
euphoria, insomnia, restlessness, tremor,
weakness. EENT: blurred vision, glaucoma,
nystagmus. CV: HYPERTENSIVE CRISIS,
arrhythmias, edema, orthostatic
hypotension. GI: diarrhea, weight gain,
abdominal pain, anorexia, constipation, dry
mouth, increase liver function tests, nausea,
vomiting. GU: dysuria, sexual dysfunction,
urinary incontinence, urinary retention.
Derm: pruritis, rashes. Endo: hypoglycemia.
MS: arthralgia. Neuro: paresthesia.
NURSING INTERVENTIONS
Assessment:
 Assess mental status (orientation, mood,
behavior) and anxiety level frequently.
 Assess for suicidal tendencies, especially
during early therapy. Restrict amount of
drug available to patient.
Diagnosis:
 Risk for falls (sideeffects)
 Imbalanced nutrition: more than body
requirements (sideeffects)
Planning:
 Pt. Will be able to improve mood
 Pt. Will be able to decrease anxiety.
Implementation:
 Po: tablets may be crushed and mixed with
food or fluids for patients with difficulty
swallowing.
 Do not administer these medications in the
evening because the psychomotor
stimulating effects may cause insomnia or
other sleep disturbances.
Evaluation:
 Monitor weight and BM Iinitially and
throughout treatment.
 Lab Test Considerations: Assess
hepatic function periodically during
prolonged or high-dose therapy.
Drug Classification: ATYPICAL
ANTIDEPRESSANTS
Generic Name: Trazodone
Brand Name: Desyrel
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO(Adults): Immediate-release—150
mg/day in 3 divided doses; increase by
50mg/day q3–4 days until desired response
(not to exceed 400mg/day in outpatients or
600mg/day in hospitalized patients). PO
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(GeriatricPatients): 75mg/day in divided
doses initially; may be increase q3–4 days.
DRUG ACTION
Alters the effects of serotonin in the CNS.
Therapeutic Effects: Antidepressant action,
which may develop only over several weeks.
Pharmacokinetics:
Absorption: Well absorbed after oral
administration.
Distribution: Widely distributed.
Protein Binding: 89–95%.
Metabolism: Extensively metabolized by
the liver (CYP3A4 enzyme system)
Excretion: Minimal excretion of unchanged
drug by the kidneys.
Half-life: 12hr.
DRUG INTERACTION
DRUG: CYP3A4 inhibitors (e.g., ritonavir,
ketoconazole) increase concentration/
effects. May increase concentration of
digoxin, phenytoin.
INDICATIONS
Major depression. Unlabeled Use:
Insomnia, chronic pain syndromes, including
diabetic neuropathy, and anxiety.
CONTRAINDICATIONS:
Hypersensitivity; Recovery period after MI;
Concurrent electroconvulsive therapy;
Concurrent use of MAO inhibitors or MAO-
like drugs (linezolid or methylene blue).
Adverse Reactions/Side Effects
CNS: SUICIDAL THOUGHTS, drowsiness,
confusion, dizziness, fatigue, hallucinations,
headache, insomnia, nightmares, slurred
speech, syncope, weakness. EENT:
blurredvision, tinnitus. CV: hypotension,
arrhythmias, chest pain, hypertension,
palpitations, QT interval prolongation,
tachycardia. GI: dry mouth, altered taste,
constipation, diarrhea, excess salivation,
flatulence, nausea, vomiting. GU: hematuria,
erectile dysfunction, priapism, urinary
frequency. Derm: rash. Hemat: anemia,
leukopenia. MS: myalgia. Neuro: tremor.
NURSING INTERVENTIONS
Assessment:
 Assess for possible sexual dysfunction
 Assess mental status (orientation, mood,
and behavior) frequently.
Diagnosis:
 Ineffective coping (indications)
 Sexual dysfunction (sideeffects)
Planning:
 Pt. Will be able to have a resolution of
depression.
 Pt. Will be able to increased sense of well-
being.
Implementation:
 Po: administer with or immediately after
meals to minimize side effects (nausea,
dizziness) and allow maximum absorption
of trazodone. A larger portion of the total
daily dose may be given at bedtime to
decrease daytime drowsiness and
dizziness.
Evaluation:
 Lab Test Considerations: Assess CBC and
renal and hepatic function before and
periodically during therapy. Slight, clinically
insignificant decrease in leukocyte and
neutrophil counts may occur.
 Pain: Assess location, duration, intensity,
and characteristics of pain before and
periodically during therapy. Use pain scale
to assess effectiveness of medicine.
Drug Classification:
NOREPINEPHRINE & DOPAMINE
REUPTAKE INHIBITOR (NDRI)
Generic Name: Bupropion
Brand Name: Wellbutrin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO(Adults): Immediate-release—100mg
twice daily initially; after 3days may increase
to100mg 3times daily; after atleast 4wk of
therapy, may increase up to 450 mg/day in
divided doses (not to exceed 150mg/dose;
wait atleast 6hr between doses at the
300mg/day dose or atleast 4hr between
doses at the 450-mg/day dose). Sustained-
release—150mg once daily in the morning;
after 3days, may increase to 150mg twice
daily with atleast 8hr between doses; after at
least 4wk of therapy, may increase to a
maximum daily dose of 400mg given as
200mg twice daily. Extended-release
(Wellbutrin XL)—150mg once daily in the
morning, may be increase after 4days to
300mg once daily; some patients may
require up to 450mg/day as a single daily
dose.
DRUG ACTION
Decreases neuronal reuptake of dopamine
in the CNS. Diminished neuronal uptake of
serotonin and norepinephrine (less than
tricyclic antidepressants). Therapeutic
Effects: Diminished depression. Decreased
craving for cigarettes.
Pharmacokinetics:
Absorption: Although well absorbed,
rapidly and extensively metabolized by the
liver Distribution: Unknown.
Metabolism and Excretion: Extensively
metabolized by the liver into 3 active
Page | 122
metabolites (CYP2B6 involved information
of one of the active metabolites).
Half-life: 14hr (active metabolites may have
longer half-lives).
DRUG INTERACTION
Concurrent use with MAO-inhibitor like
drugs, such as linezolid or methylene blue
may increase risk of hypertensive reactions;
concurrent use contraindicated; do not start
therapy in patients receiving linezolid or
methylene blue; if linezolid or methylene
blue need to be started in a patient receiving
bupropion, immediately discontinue
bupropion and monitor for 2wk or until 24hr
after last dose of linezolid or methylene blue,
whichever comes first (may resume
bupropion therapy 24hr after last dose of
linezolid or methylene blue). Increase risk of
adverse reactions when used with
amantadine, or levodopa. Increase risk of
seizures with phenothiazines,
antidepressants, theophylline,
corticosteroids, OTC stimulants/anorectics,
or cessation of alcohol or benzodiazepines.
Ritonavir, lopinavir/ritonavir, and efavirenz
may decrease levels; may need to increase
bupropiondose. May increase italopram
levels. Carbamazepine may decrease blood
levels and effectiveness. Concurrent use
with nicotine replacement may cause
hypertension. Increase risk of bleeding with
warfarin. Bupropion and one of its
metabolites inhibit the CYP2D6 enzyme
system and may increase levels and risk of
toxicity from antidepressants (SSRIs and
tricyclic), haloperidol, risperidone,
thioridazine, haloperidol, betablockers,
flecainide, and propafenone. May decrease
levels and efficacy of tamoxifen. May
decrease the efficacy of tamoxifen.
INDICATIONS
Treatment of depression (with
psychotherapy). Depression with seasonal
affective disorder (Aplenzin and Wellbutrin
XL only). Unlabeled Use: Treatment of
ADHD in adults (SRonly). To increase
sexual desire in women.
CONTRAINDICATIONS:
Hypersensitivity; Concurrent use of MAO
inhibitors or MAO-like drugs (linezolid or
methylene blue); Concurrent use of ritonavir;
Seizure disorders; Arteriovenous
malformation, severe head injury, CNS
tumor, CNS infection, severe stroke,
anorexia nervosa, bulimia, or abrupt
discontinuation of alcohol, benzodiazepines,
barbiturates, or antiepileptic drugs
(increased risk of seizures); Lactation:
Potential for serious adverse reactions in
nursing infants.
Adverse Reactions/Side Effects
CNS: SEIZURES,SUICIDAL
THOUGHTS/BEHAVIOR, agitation,
headache, aggression, anxiety, delusions,
depression, hallucinations, hostility,
insomnia, mania, panic, paranoia,
psychoses. GI: dry mouth, nausea, vomiting,
change in appetite, weight gain, weight loss.
Derm: photosensitivity. Endo:
hyperglycemia, hypoglycemia, syndrome of
inappropriate ADH secretion. Neuro: tremor.
NURSING INTERVENTIONS
ASSESSMENT:
 Assess mental status and mood changes,
especially during initial few months of
therapy and during dose changes.
 Monitor mood changes. Inform healthcare
professional if patient demonstrates
significant increase in anxiety,
nervousness, or insomnia.
DIAGNOSIS:
 Ineffective coping (Indications)
PLANNING:
 Pt. will be able to have an increase in
sense of well-being.
 Pt. will be able to have renewed interest in
surroundings. Acute episodes of
depression may require several months of
treatment.
IMPLEMENTATION:
 Administer doses in equally spaced time
increments during the day to minimize the
risk of seizures. Risk of seizures increases
four fold in doses greater than 450mg per
day.
 PO: Swallow sustained-release or
extended-release tablets whole; do not
break, crush, or chew.
EVALUATION:
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Drug Classification: MOOD
STABILIZERS
Generic Name: Carbamazepine
Brand Name: Tegretol
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO(Adults):Anticonvulsant—200mg twice
daily (tablets) or 100mg 4times daily
(suspension); increase by 200mg/day q7
days until therapeutic levels are achieved
(range is 600–1200mg/day in divided doses
q6–8hr; not to exceed 1g/day in 12–15-yr-
olds. Extended-release products are given
twice daily (XR,CR). Antineuralgic—
100mg twice daily or 50mg 4times daily
(suspension); increase by up to 200mg/day
Page | 123
until pain is relieved, then maintenance
dose of 200–1200mg/day in divided
doses(usual range,400–800mg/day). PO
(Children 6–12 yr): 100mg twice daily
(tablets) or 50mg 4times daily
(suspension).increase by 100 mg weekly
until therapeutic levels are obtained (usual
range 400–800mg/day; not to exceed
1g/day). Extended-release products
(XR,CR) are given twice daily. PO (Children
6 yr): 10–20mg/kg/day in 2–3 divided doses;
may be increase at weekly intervals until
optimal response and therapeutic levels are
acheived. Usual maintenance dose is 250–
350mg/day (not to exceed 35mg/kg/day).
DRUG ACTION
Decreases sodium ion influx into neuronal
membranes, reducing post-tetanic
potentiation at synapses. Therapeutic
Effect: Produces anticonvulsant effect.
Pharmacokinetics:
Absorption: Slowly, completely absorbed
from GI tract.
Distribution: Widely distributed. Crosses
the blood brain barrier. Crosses the placenta
rapidly and enters breastmilk in high
concentrations. Protein binding: 75%–
90%.
Metabolism: Metabolized by the liver
Excretion: Primarily excreted in urine.
Half-life: 25–65hrs (decreased with chronic
use).
DRUG INTERACTION
DRUG: CYP3A4 inhibitors (e.g., cimetidine,
clarithromycin, azole antifungals, protease
inhibitors) may increase concentration.
CYP3A4 inducers (e.g., rifAMPin, phenytoin)
may decrease concentration/ effects.
May decrease concentration/effects
of hormonal contraceptives, warfarin,
traZODone. FOOD: Grapefruit products may
increase absorption, concentration.
INDICATIONS
Treatment of tonic-clonic, mixed, and
complex-partial seizures. Management of
pain in trigeminal neuralgia or diabetic
neuropathy. Equetro only: Acutemania and
mixed mania.
CONTRAINDICATIONS:
Contraindications: Concomitant use or
within 14 days of use of MAOIs,
myelosuppression. Concomitant use of
delavirdine or other NNRT inhibitors,
hypersensitivity to carBAMazepine, tricyclic
antidepressants.
Adverse Reactions/Side Effects
CNS: SUICIDALTHOUGHTS, ataxia,
drowsiness, fatigue, psychosis, sedation,
vertigo. EENT: blurred vision,
cornealopacities, nystagmus. Resp:
pneumonitis. CV: HF, edema, hypertension,
hypotension, syncope. GI: hepatitis,
increase liver enzymes, pancreatitis, weight
gain.GU: hesitancy, urinary retention. Derm:
STEVENS-JOHNSON SYNDROME, TOXIC
EPIDERMAL NECROLYSIS, nail shedding,
photosensitivity, rash, urticaria. F and E:
syndrome of inappropriate antidiuretic
hormone (SIADH),hyponatremia. Hemat:
AGRANULOCYTOSIS, APLASTICANEMIA,
THROMBOCYTOPENIA, eosinophilia,
leukopenia, lymph adenopathy. Misc: chills,
fever, multi-organ hypersensitivity reactions.
NURSING INTERVENTIONS
ASSESSMENT:
 Monitor closely for notable changes in
behavior that could indicate the
emergence or worsening of suicidal
thoughts or behavior or depression
 Bipolar Disorder: Assess mental status and
cognitive abilities before therapy.
DIAGNOSIS:
 Risk for injury
 Chronic pain (Indications)
 Disturbed thought process(Indications)
PLANNING:
 Pt. will be able to have absence or
reduction of seizure activity.
 Pt. will be able to decrease mania and
depressive symptoms in bipolar I disorder.
IMPLEMENTATION:
 Implement seizure precautions as
indicated.
 PO: Administer medication with food to
minimize gastric irritation.
EVALUATION:
 Monitor serum ionized calcium levels every
6mo or if seizure frequency increases
 Monitor ECG and serum electrolytes
before and periodically during therapy.
May cause hyponatremia.
Drug Classification: NARROW-
SPECTRUM PENICILLINS OR
PENICILLINASE-SENSITIVE
(PENICILLINS)
Generic Name: Penicillin G
Brand Name: Pfizerpen
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IM, IV (Adults): Most infections—1–5million
units q4–6hr. IM, IV (Children): 8333–
16,667units/kg q4hr; 12,550–
25,000units/kgq6hr; up to 250,000units/
kg/day in divided doses, some infections
may require up to 300,000 units/kg/day. IV
(Infants 7days): 25,000 units/kg q8hr;
meningitis—50,000–75,000units/kg q6hr.
Page | 124
IV(Infants 7days): 25,000units/kg q12hr;
Streptococcus B meningitis—100,000–
150,000 units/kg/day in divided doses.
DRUG ACTION
Action Bind to bacterial cell wall, resulting in
cell death. Therapeutic Effects:
Bactericidal action against susceptible
bacteria.
Pharmacokinetics: Absorption: Variably
absorbed from the GI tract. Penicillin V—
resists acid degradation in the GI tract.
Procaine and benzathine penicillin—IM
absorption is delayed and prolonged and
results in sustained therapeutic blood
levels.Distribution: Widely distributed,
although CNS penetration is poor in the
presence of uninflamed meninges. Cross
the placenta and enter breastmilk.
Proteinbinding: 60% Metabolism:
Metabolized by the liver Excretion:
Primarily excreted in urine.
Half-life: 0.5–1 hr (increased in renal
impairment).
DRUG INTERACTION
DRUG: Probenecid increases concentration.
May decrease effectiveness of oral
contraceptive agents.
INDICATIONS
Treatment of a wide variety of infections
including: Pneumococcal pneumonia,
Streptococcal pharyngitis, Syphilis,
Gonorrhea strains. Treatment of
enterococcal infections (requires the
addition of an aminoglycoside).Prevention of
rheumatic fever. Should not be used as a
single agent to treat anthrax
CONTRAINDICATIONS:
Hypersensitivity to any penicillin. Cautions:
Renal/hepatic impairment, seizure disorder,
hypersensitivity to cephalosporins, pts with
asthma.
Adverse Reactions/Side Effects
CNS: SEIZURES. GI:
PSEUDOMEMBRANOUS COLITIS,
diarrhea, epigastric distress, nausea,
vomiting. GU: interstitial nephritis. Derm:
rash, urticaria. Hemat: eosinophilia,
hemolytic anemia, leukopenia. Local: pain
at IM site, phlebitis at IV site. Misc: allergic
reactions including ANAPHYLAXIS and
SERUM SICKNESS, superinfection.
NURSING INTERVENTIONS
ASSESSMENT:
 Assess for history of allergies,
particularly penicillins, cephalosporins.
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; WBC) at beginning of and during
therapy.
DIAGNOSIS:
 Risk for infection (Indications, Side Effects)
 Noncompliance (Patient/ Family Teaching)
PLANNING:
 Pt. will be able to have resolution of signs
and symptoms of infection. Length of time
for complete resolution depends on the
organism and site of infection.
IMPLEMENTATION:
 PO: Administer around the clock. Penicillin
V may be administered without regard for
meals.
 IM: Shake medication well before injection.
Inject penicillin deep into a well- developed
muscle mass at a slow, consistent rate to
prevent blockage of the needle. Massage
well. Accidental injury near or into a nerve
can result in severe pain and dysfunction
EVALUATION:
 Observe patient for signs and symptoms of
anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug and
notify healthcare professional immediately
if these symptoms occur. Keep
epinephrine, an antihistamine, and
resuscitation equipment close by incase of
an anaphylactic reaction.
Drug Classification: NARROW-
SPECTRUM PENICILLINS OR
PENICILLINASE-RESISTANT OR
ANTISTAPHYLOCOCCAL
PENICILLINS (PENICILLINS)
Generic Name: Oxacillin
Brand Name: Bactocil
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IM, IV (Adults and Children 40 kg): 250–
2000 mg q4–6hr (up to 12g/day). IM, IV
(Children 40 kg): 100–200mg/kg/day divided
q4–6hr, maximum: 12g/day. IM, IV
(Neonates 1200 g): — 25mg/kg q12hr. IM,
IV (Neonates 2 kg): — 25mg/kg q8hr for the
first 7days of life, then 25mg/kg q6hr. IM, IV
(Neonates1.2–2kg): — 25mg/kg q12hr for
the first 7 days of life, then 25mg/kg q8hr.
DRUG ACTION
Bind to bacterial cell wall, leading to cell
death. Not inactivated by penicillinase
enzymes. Therapeutic Effects: Bactericidal
action
Pharmacokinetics:
Absorption: Completely absorbed following
IV administration; well absorbed from IM
sites Distribution: Widely distributed;
penetration into CSF is minimal, but
sufficient in the presence of inflamed
Page | 125
meninges; cross the placenta and enter
breastmilk..
Metabolism: Partially metabolized by the
liver (49%)
Excretion: Partially excreted unchanged by
the kidneys.
Half-life: Neonates: 1.6hr; Children up to
2yr: 0.9–1.8hr; Adults: 0.3–0.8hr (increase
in severe hepatic impairment).
DRUG INTERACTION
Drug-Drug: Probenecid increase renal
excretion and increase blood levels
(treatment may be combined for this
purpose). May decrease effectiveness of
oral contraceptive agents. May decrease
elimination of methotrexate and increase
risk of serious toxicity..
INDICATIONS
Treatment of the following infections due to
penicillinase - producing staphylococci:
Respiratory tract infections, Sinusitis, Skin
and skins tructure infections. Dicloxacillin:
Osteomyelitis. Nafcillin, oxacillin: Are also
used to treat: Bone and joint infections,
Urinary tract infections, Endocarditis,
Septicemia, Meningitis.
CONTRAINDICATIONS:
Hypersensitivity to penicillins (cross-
sensitivity with cephalosporins may exist).
Use Cautiously in: Severe renal or hepatic
impairment; OB, Lactation: Safety not
established.
Adverse Reactions/Side Effects
CNS: SEIZURES (high doses). GI:
PSEUDOMEMBRANOUS COLITIS,
diarrhea, nausea, vomiting, drug-induced
hepatitis. GU: interstitial nephritis. Derm:
rashes, urticaria. Hemat: eosinophilia,
leukopenia. Local: pain at IM sites, phlebitis
at IV sites. Misc: allergic reactions including
ANAPHYLAXIS and SERUM SICKNESS,
superinfection.
NURSING INTERVENTIONS
ASSESSMENT:
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; WBC) at beginning of and during
therapy.
 Obtain specimens for culture and
sensitivity prior to initiating therapy. First
dose may be given before receiving
results.
DIAGNOSIS:
 Risk for infection (Indications, Side Effects)
 Noncompliance (Patient/ Family Teaching)
PLANNING:
 Pt. will be able to have resolution of signs
and symptoms of infection. Length of time
for complete resolution depends on the
organism and site of infection.
IMPLEMENTATION:
 PO: Administer around the clock on an
empty stomach at least 1hr before or 2hr
after meals. Take with a full glass of water;
acidic juices may decrease absorption of
penicillins.
 Use calibrated measuring device for liquid
preparations. Shake well. Solution is stable
for 14days if refrigerated.
EVALUATION:
 Assess vein for signs of irritation and
phlebitis. Change IV site every 48hr to
prevent phlebitis.
 Lab Test Considerations: May cause
leukopenia and neutropenia, especially
with prolonged therapy or hepatic
impairment.
 Observe patient for signs and symptoms of
anaphylaxis (rash, pruritus, laryngeal
edema, wheezing, abdominal pain).
Discontinue the drug and notify healthcare
professional immediately if these occur.
Drug Classification: BROAD-
SPECTRUM PENICILLINS OR
AMINOPENICILLINS (PENICILLINS)
Generic Name: Amoxicillin
Brand Name: Moxatag
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 250–500mg q8hr or 500–
875mg q12hr (not to exceed 2–3g/day). PO
(AdultsandChildren 12 yr): Extended-
release tablets (for Strep throat)—775mg
once daily for 10days. PO (Children 3mo):
25–50mg/kg/day in divided doses q8hr or
25–50mg/kg/day individual doses q12hr;
Acute otitis media due to highly resistant
strains of S. pneumoniae— 80–90mg/kg/day
divided q12hr; Post exposure inhalational
anthrax prophylaxis—40kg:45mg/kg/day in
divided doses q8hr; 40kg:500mg q8hr. PO
(Infants 3mo and neonates): 20–30mg/kg/
day in divided doses q12hr.
DRUG ACTION
Binds to bacterial cell wall, causing cell
death. Therapeutic Effects: Bactericidal
action; spectrum is broader than penicillins
Pharmacokinetics:
Absorption: Well absorbed from duodenum
(75– 90%). More resistant to acid
inactivation than other penicillins..
Distribution: Diffuses readily into most
body tissues and fluids. CSF penetration
increased when meninges are inflamed.
Crosses placenta; enters breast milk in
small amounts. Protein binding: 20%
Page | 126
Metabolism: 30% metabolized by the liver
Excretion: 70% excreted unchanged in
urine Half-life: Neonates: 3.7hr; Infants and
Children: 1– 2hr; Adults: 0.7– 1.4hr.
DRUG INTERACTION
Drug-Drug: Probenecid decrease renal
excretion and increase blood levels of
amoxicillin—therapy may be combined for
this purpose. May increase effect of
warfarin. May decrease effectiveness of oral
contraceptives. Allopurinol may increase
frequency of rash.
INDICATIONS
Treatment of: Skin and skin structure
infections, Otitis media, Sinusitis,
Respiratory infections, genitourinary
infections. Endocarditis prophylaxis. Post
exposure inhalational anthrax prophylaxis.
Management of ulcer disease due to
Helicobacter pylori
CONTRAINDICATIONS:
Hypersensitivity to penicillins (cross-
sensitivity exists to cephalosporins and other
beta-lactams).
Adverse Reactions/Side Effects
CNS: SEIZURES (high doses).GI:
PSEUDOMEMBRANOUS COLITIS,
diarrhea, nausea, vomiting, increase liver
enzymes. Derm: rash, urticaria. Hemat:
blood dyscrasias. Misc: allergic reactions
including ANAPHYLAXIS, SERUM
SICKNESS, superinfection.
NURSING INTERVENTIONS
ASSESSMENT:
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; WBC) at beginning of and
throughout the therapy.
DIAGNOSIS:
 Risk for infection (Indications, Side Effects)
 Noncompliance (Patient/ Family Teaching)
PLANNING:
 Pt. will be able to have resolution of signs
and symptoms of infection. Length of time
for complete resolution depends on the
organism and site of infection and prevents
inhalational anthrax (post exposure).
IMPLEMENTATION:
 PO: Administer around the clock. May be
given without regard to meals or with
meals to decrease GI side effects. Capsule
contents may be emptied and swallowed
with liquids. Extended-release tablets
should be swallowed whole; do not crush,
break, or chew. Chewable tablets should
be crushed or chewed before swallowing
with liquids.
 Shake oral suspension before
administering. Suspension may be given
straight or mixed in formula, milk, fruit
juice, water, or ginger ale. Administer
immediately after mixing. Discard
refrigerated reconstituted suspension after
10 days
EVALUATION:
 Observe patient for signs and symptoms of
anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug and
notify healthcare professional immediately
if these symptoms occur. Keep
epinephrine, an antihistamine, and
resuscitation equipment close by incase of
an anaphylactic reaction.
 Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to healthcare
professional promptly as a sign of
pseudomembranous colitis.
Drug Classification: EXTENDED-
SPECTRUM PENICILLIN OR
ANTIPSEUDOMONAL PENICILLIN
Generic Name: Tazobactam
Brand Name: Tazocin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IV (Adults): Most infections—3.375 g q 6 hr.
Nosocomial pneumonia—4.5 g q
6 hr.
IV (Adults): Nosocomial pneumonia—4.5 g
q 6 hr.
IV (Adults and Children 40 kg):
Appendicitis and/or peritonitis—3.375 g q
6 hr.
IV (Children 9 mo and 40 kg): Appendicitis
and/or peritonitis—300 mg piperacillin
component/kg/day divided q 8 hr.
IV (Infants 2–9 mo): Appendicitis and/or
peritonitis—240 mg piperacillin
component/kg/day divided q 8 hr.
IV (Infants and Children 6 mo): 240– 400
mg/piperacillin component/kg/day
divided q 6– 8 hr (higher end of dosing
range for serious pseudomonal infections);
Max dose: 16 g piperacillin/day.
IV (Infants 6 mo): 150– 300 mg/piperacillin
component/kg/day divided q 6– 8 hr.
Renal Impairment
IV (Adults): CCr 20– 40 mL/min—2.25 g q 6
hr (3.375 g q 6 hr for nosocomial
pneumonia); CCr 20 mL/min—2.25 g q 8 hr
(2.25 g q 6 hr for nosocomial pneumonia);
Hemodialysis—2.25 g q 12 h (2.25 g q 8 hr
for nosocomial pneumonia).
DRUG ACTION
Inhibits beta-lactamase, an enzyme that can
destroy penicillins. Therapeutic Effects:
Death of susceptible bacteria. Spectrum:
Active against piperacillin-resistant, beta-
lactamase– producing: Bacteroides fragilis,
Page | 127
E. coli, Acinetobacter baumanii, Klebsiella
pneumoniae, Pseudomonas aeruginosa,
Staphylococcus aureus, Haemophilus
influenzae.
Pharmacokinetics: Absorption:
Piperacillin is well absorbed (80%) from IM
sites. Distribution: Widely distributed. Enter
CSF well only when meninges are inflamed.
Crosses the placenta and enters breast milk
in low concentrations. Metabolism and
Excretion: Piperacillin (68%) and
tazobactam (80%) are mostly excreted
unchanged by the kidneys. Half-life:
Adults: 0.7– 1.2 hr; Children 6 mo– 12 yr:
0.7– 0.9 hr; Infants 2– 5 mo:
1.4 hr
DRUG INTERACTION
Drug-Drug: Probenecid decrease renal
excretion and increase blood levels. May
alter excretion of lithium. Potassium-losing
diuretics, corticosteroids, or amphotericin B
may increase risk of hypokalemia. Increase
risk of hepatotoxicity with other hepatotoxic
agents. May decrease levels/effects of
aminoglycosides in patients with renal
impairment. May increase levels and risk of
toxicity from methotrexate.
INDICATIONS
Appendicitis and peritonitis. Skin and skin
structure infections. Gynecologic infections.
Community-acquired and nosocomial
pneumonia caused by piperacillin-resistant,
beta-lactamase– producing bacteria.
CONTRAINDICATIONS:
Hypersensitivity to penicillins, beta-lactams,
cephalosporins, or tazobactam (cross-
sensitivity may occur).
Adverse Reactions/Side Effects
CNS: SEIZURES (higher doses), confusion,
dizziness, headache, insomnia, lethargy.
GI: PSEUDOMEMBRANOUS COLITIS,
diarrhea, constipation, drug-induced
hepatitis, nausea, vomiting. GU: interstitial
nephritis. Derm: STEVENS-JOHNSON
SYNDROME, TOXIC EPIDERMAL
NECROLYSIS, rashes (qin cystic fibrosis
patients), urticaria. Hemat: bleeding,
leukopenia, neutropenia, thrombocytopenia.
Local: pain, phlebitis at IV site. Misc:
hypersensitivity reactions, including
ANAPHYLAXIS and SERUM SICKNESS,
fever (qin cystic fibrosis patients),
superinfection.
NURSING INTERVENTIONS
ASSESSMENT:
 Assess patient for infection (vital signs;
appearance of wound, sputum, urine, and
stool; WBC) at beginning of and during
therapy.
 Obtain specimens for culture and
sensitivity prior to initiating therapy. First
dose may be given before receiving
results.
DIAGNOSIS:
 Risk for infection (Indications) (Side
Effects)
 Deficient knowledge, related to medication
regimen (Patient/Family Teaching)
PLANNING:
 Pt. will be able to have resolution of signs
and symptoms of infection. Length of time
for complete resolution depends on the
organism and site of infection.
IMPLEMENTATION:
 Intermittent Infusion: Reconstitute each 1 g
of piperacillin with at least 5 mL of 0.9%
NaCl, sterile water for injection, or D5W.
Diluent: Dilute further in 50–100 mL of
0.9% NaCl, D5W, D5/0.9% NaCl, or LR.
Reconstituted vials stable for 24 hr at room
temperature or 48 hr if refrigerated.
Infusion stable for 24 hr at room
temperature or 7 days if refrigerated. Rate:
Infuse over 30 min
EVALUATION:
 Observe patient for signs and symptoms of
anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug and
notify healthcare professional immediately
if these symptoms occur. Keep
epinephrine, an antihistamine, and
resuscitation equipment close by incase of
an anaphylactic reaction.
 Lab Test Considerations: Evaluate renal
and hepatic function, CBC, serum
potassium, and bleeding times prior to and
routinely during therapy.
Drug Classification: First Generation
Cephalosporin Generic Name:
Cephalexin
Brand Name: Keflex
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): Most infections—250–500mg
q6 hr. Uncomplicated cystitis, skin and soft-
tissue infections, streptococcal pharyngitis—
500mg q12 hr. PO (Children): Most
infections—25–50mg/kg/ day divided q6–8hr
(can be administered q12hr in skin/skin
structure infections or streptococcal
pharyngitis). Otitis media—18.75–25mg/kg
q6hr (maximum 4g/day).
DRUG ACTION
Bind to bacterial cell wall membrane,
causing cell death. Therapeutic Effects:
Page | 128
Bactericidal action against susceptible
bacteria
Pharmacokinetics: Absorption: Well
absorbed following oral administration.
Distribution: Widely distributed. Cross the
placenta and enter breastmilk in low
concentrations. Minimal CSF penetration
Protein binding: 10%–15%
Metabolism and Excretion: Primarily
excreted unchanged in urine. Moderately
removed by hemodialysis. Half-life: 0.9–1.2
hrs (increased in renal impairment).
DRUG INTERACTION
Drug-Drug: Probenecid decrease excretion
and increase blood levels of renally excreted
cephalosporins. Concurrent use of loop
diuretics or aminoglycosides may increase
risk of renal toxicity.
INDICATIONS
Treatment of the following infections caused
by susceptible organisms: Skin and skin
structure infections (including burn wounds),
Pneumonia, Urinary tract infections, Bone
and joint infections, Septicemia. Not suitable
for the treatment of meningitis. Cephalexin:
For Otitis media
CONTRAINDICATIONS:
Hypersensitivity to cephalosporins; Serious
hypersensitivity to penicillins.
Adverse Reactions/Side Effects
CNS: SEIZURES (high doses). GI:
PSEUDOMEMBRANOUS COLITIS,
diarrhea, nausea, vomiting, cramps. Derm:
STEVENS-JOHNSON SYNDROME, rashes,
pruritis, urticaria. Hemat: agranulocytosis,
eosinophilia, hemolytic anemia, neutropenia,
thrombocytopenia. Local: pain at IM site,
phlebitis at IV site. Misc: allergic reactions
including ANAPHYLAXIS and SERUM
SICKNESS, superinfection.
NURSING INTERVENTIONS
ASSESSMENT:
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; WBC) at beginning of and
throughout the therapy.
 Obtain a history to determine previous use
of and reactions to penicillins or
cephalosporins. Persons with a negative
history of penicillin sensitivity may still have
an allergic response.
DIAGNOSIS:
 Risk for infection (Indications, Side Effects)
 Diarrhea (Adverse Reactions)
PLANNING:
 Pt. will be able to have resolution of signs
and symptoms of infection. Length of time
for complete resolution depends on the
organism and site of infection and prevents
inhalational anthrax (post exposure).
 Pt. will be able to have a decreased
incidence of infection when used for
prophylaxis.
IMPLEMENTATION:
 PO: Administer around the clock. May be
administered on full or empty stomach.
Administration with food may minimize GI
irritation. Shake oral suspension well
before administering. Use calibrated
measuring device with liquid preparations.
Refrigerate oral suspensions.
EVALUATION:
 Observe patient for signs and symptoms of
anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug and
notify healthcare professional immediately
if these symptoms occur. Keep
epinephrine, an antihistamine, and
resuscitation equipment close by incase of
an anaphylactic reaction.
 Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to healthcare
professional promptly as a sign of
pseudomembranous colitis.
Drug Classification: SECOND
GENERATION CEPHALOSPORIN
Generic Name: Cefuroxime
Brand Name: Zinacef
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IV ,IM: ADULTS, ELDERLY, CHILDREN
12YRS AND OLDER: 750mg– 1.5g q8h up
to 1.5g q6h for severe infections.
CHILDREN:3 MOS TO YOUNGER THAN
12YRS: 75–150 mg/kg/day divided q8h up to
100–200 mg/kg/day divided in 3–4 doses.
Maximum: 6 g/day. NEONATES:
50mg/kg/dose q8–12h. PO: ADULTS,
ELDERLY, CHILDREN 12 YRS AND
OLDER: 250–500mg twice a day.
CHILDREN 3 MOS TO YOUNGER THAN
12YRS: 20–30 mg/kg/day in 2 divided
doses. Maximum: 1g/day.
DRUG ACTION
Binds to bacterial cell wall membrane,
causing cell death. Therapeutic Effects:
Bactericidal action against susceptible
bacteria.
Pharmacokinetics:
Absorption: Well absorbed after oral and
IM administration; IV administration results
in complete bioavailability.
Page | 129
Distribution: Widely distributed. Penetrates
into CSF with IV administration. Crosses the
placenta and enters breast milk in low
concentrations.
Protein Binding: 50%
Metabolism and Excretion: Primarily
excreted unchanged in urine. Moderately
removed by hemodialysis. Half-life: 1.3hrs
(increased in renal impairment).
DRUG INTERACTION
Drug-Drug: Probenecid may increase
concentration. Antacids, H2-receptor
antagonists (e.g, cimetidine, thankp) may
decrease absorption.
INDICATIONS
Treatment of Respiratory tract infections,
Skin and skin structure infections, Bone and
joint infections (IV), Urinary tract infections,
Gynecologic infections, Septicemia (IV),
Otitis media (PO), Meningitis (IV), Lyme
disease (PO). Perioperative prophylaxis (IV).
CONTRAINDICATIONS:
Hypersensitivity to cephalosporins; Serious
hypersensitivity to penicillins.
Adverse Reactions/Side Effects
CNS: SEIZURES (high doses). GI:
PSEUDOMEMBRANOUS COLITIS,
diarrhea, nausea, vomiting, cramps. Derm:
rashes, urticaria, diaper dermatitis. Hemat:
bleeding, eosinophilia, hemolytic anemia,
leukopenia. Local: pain at IM site, phlebitis
at IV site. Misc: allergic reactions including
ANAPHYLAXIS, superinfection.
NURSING INTERVENTIONS
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; wbc) at beginning of and throughout
the therapy.
 Before initiating therapy, obtain a history to
determine previous use of and reactions to
penicillins or cephalosporins. Persons with
a negative history of penicillin sensitivity
may still have an allergic response
Diagnosis:
 Risk for infection (indications, side effects)
 Deficient knowledge, related to medication
regimen (patient/family teaching)
Planning:
 Pt. Will be able to have resolution of signs
and symptoms of infection. Length of time
for complete resolution depends on the
organism and site of infection and prevents
inhalational anthrax (post exposure).
 Pt. Will be able to have a decreased
incidence of infection when used for
prophylaxis.
Implementation:
 Po: administer around the clock. Tablets
can be administered on full or empty
stomach. Administration with food may
minimize gi irritation. Suspension must be
administered with food.
 Im: reconstitute im doses with sterile water
for injection. Inject deep into a well-
developed muscle mass; massage well.
Evaluation:
 Observe patient for signs and symptoms of
anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug and
notify healthcare professional immediately
if these symptoms occur. Keep
epinephrine, an antihistamine, and
resuscitation equipment close by incase of
an anaphylactic reaction.
 Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to healthcare
professional promptly.
.
Drug Classification: THIRD
GENERATION CEPHALOSPORIN
Generic Name: Ceftriaxone
Brand Name: Rocephin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IM, IV (Adults): Most infections—1– 2 g
every 12– 24 hr Gonorrhea—250 mg IM
(single dose). Meningitis—2 g every 12 hr.
Perioperative prophylaxis—1 g 0.5– 2 hr
before surgery (single dose).
IM, IV (Children): Most infections—50– 75
mg/kg/day (not to exceed 2 g/day) divided
every 12– 24 hr. Meningitis—100 mg/kg/day
(not to exceed 4 g/day) divided every 12– 24
hr or Uncomplicated gonorrhoea—125 mg
IM (single dose). Acute otitis media—50
mg/kg (not to exceed 1 g) IM single dose.
DRUG ACTION
Binds to the bacterial cell wall membrane,
causing cell death. Therapeutic Effects:
Bactericidal action against susceptible
bacteria
Pharmacokinetics:
Absorption: Well absorbed following IM
administration; IV administration results in
complete bioavailability.
Distribution: Widely distributed. CSF
penetration better than with first- and
second-generation agents. Crosses the
placenta; enters breast milk in low
concentrations. Protein Binding: 90%.
Metabolism and Excretion: 33– 67%
excreted in urine as unchanged drug;
remainder excreted in feces Half-life: : 6– 9
hr.
DRUG INTERACTION
Page | 130
Drug-Drug: Should not be administered
concomitantly with any calcium-containing
solutions.
INDICATIONS
Treatment of: Skin and skin structure
infections, Bone and joint infections,
Complicated and uncomplicated urinary tract
infections, Uncomplicated gynecological
infections including gonorrhea, Lower
respiratory tract infections, Intra-abdominal
infections, Septicemia, Meningitis, Otitis
media. Perioperative prophylaxis.
CONTRAINDICATIONS:
Hypersensitivity to cephalosporins; Serious
hypersensitivity to penicillins; Pedi:
Neonates 28 days (use in hyperbilirubinemic
neonates may lead to kernicterus); Pedi:
Neonates 28 days requiring calcium-
containingIV solutions (increased risk of
precipitation formation).
Adverse Reactions/Side Effects
CNS: SEIZURES (high doses). GI:
PSEUDOMEMBRANOUS COLITIS,
diarrhea, cholelithiasis, gallbladder sludging.
Derm: rashes, urticaria. Hemat: bleeding,
eosinophilia, hemolytic anemia, leukopenia,
thrombocytosis. Local: pain at IM site,
phlebitis at IV site. Misc: allergic reactions
including ANAPHYLAXIS, superinfection.
NURSING INTERVENTIONS
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; wbc) at beginning of and throughout
the therapy.
 Before initiating therapy, obtain a history to
determine previous use of and reactions to
penicillins or cephalosporins. Persons with
a negative history of penicillin sensitivity
may still have an allergic response
Diagnosis:
 Risk for infection (indications, side effects)
 Diarrhea (adverse reactions)
Planning:
 Pt. Will be able to have resolution of signs
and symptoms of infection. Length of time
for complete resolution depends on the
organism and site of infection and prevents
inhalational anthrax (post exposure).
 Pt. Will be able to have a decreased
incidence of infection when used for
prophylaxis.
Implementation:
 Im: reconstitute im doses with sterile water
for injection, or 0.9% nacl for injection. May
be diluted with lidocaine to minimize
injection discomfort.
 Inject deep into a well-developed muscle
mass; massage well.
Evaluation:
 Observe patient for signs and symptoms of
anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug and
notify healthcare professional immediately
if these symptoms occur. Keep
epinephrine, an antihistamine, and
resuscitation equipment close by incase of
an anaphylactic reaction.
 Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to healthcare
professional promptly as a sign of
pseudomembranous colitis.
Drug Classification: FOURTH
GENERATION
Generic Name: Cefepime
Brand Name: Maxipime
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IM (Adults): Mild-to-moderate
uncomplicated or complicated urinary tract
infections due to Escherichia coli—0.5– 1 g
every 12 hr. IV (Adults): Moderate-to-
severe pneumonia—1– 2 g every 12 hr.
Mild-to-moderate uncomplicated or
complicated urinary tract infections 0.5– 1 g
every 12hr. Severe uncomplicated or
complicated urinary tract infections,
moderate-tosevere uncomplicated skin and
skin structure infections, complicated intra-
abdominal infections—2 g every 12 hr.
Empiric treatment of febrile neutropenia—2
g every 8 hr. IV (Children 1 mo– 16 yr):
Uncomplicated and complicated urinary tract
infections, uncomplicated skin and skin
structure infections, pneumonia—50 mg/kg
every 12 hr (not to exceed 2 g/dose).Febrile
neutropenia—50 mg/kg every 8 hr (not to
exceed 2 g/dose).
IV (Neonates postnatal age 14 days): 50
mg/kg every 12 hr.
IV (Neonates postnatal age 14 days): 30
mg/kg every 12 hr; consider 50 mg/kg every
12 hr for Pseudomonas infections.
Renal Impairment
IM, IV (Adults) CCr 30– 60 mL/ min—0.5– 1
g every 24 hr or 2 g every 12– 24 hr; CCr
11– 29 mL/min—0.5– 2 g every 24 hr; CCr
11 mL/min—250 mg– 1 g every 24 hr.
DRUG ACTION
Binds to the bacterial cell wall membrane,
causing cell death. Therapeutic Effects:
Bactericidal action against susceptible
bacteria
Pharmacokinetics:
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Absorption: Well absorbed after IM
administration; IV administration results in
complete bioavailability.
Distribution: Widely distributed. Crosses
the placenta; enters breast milk in low
concentrations. Some CSF penetration.
Protein Binding: 20%.
Metabolism and Excretion: 85% excreted
unchanged in urine.
Half-life: Adults– 2 hr (qin renal
impairment); Children 2 mo– 6 yr— 1.7–
1.9hr.
DRUG INTERACTION
Drug-Drug: Probenecid decrease excretion
and increase blood levels. Concurrent use of
loop diuretics or aminoglycosides may
increase risk of nephrotoxicity.
INDICATIONS
Treatment of the following infections caused
by susceptible organisms: Uncomplicated
skin and skin structure infections, Bone and
joint infections, Uncomplicated and
complicated urinary tract infections,
Respiratory tract infections, Complicated
intra-abdominal infections (with
metronidazole), Septicemia. Empiric
treatment of febrile neutropenic patients.
CONTRAINDICATIONS:
Hypersensitivity to cephalosporins; Serious
hypersensitivity to penicillins
Adverse Reactions/Side Effects
CNS: SEIZURES (increase risk in renal
impairment), encephalopathy, headache. GI:
PSEUDOMEMBRANOUS COLITIS,
diarrhea, nausea, vomiting. Derm: rashes,
pruritis, urticaria. Hemat: bleeding,
eosinophilia, hemolytic anemia, neutropenia,
thrombocytopenia. Local: pain at IM site,
phlebitisat IV site. Misc:allergic reactions
including ANAPHYLAXIS, superinfection,
fever.
NURSING INTERVENTIONS
ASSESSMENT:
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; WBC) at beginning of and
throughout the therapy.
 Before initiating therapy, obtain a history to
determine previous use of and reactions to
penicillins or cephalosporins. Persons with
a negative history of penicillin sensitivity
may still have an allergic response
DIAGNOSIS:
 Risk for infection (Indications, Side Effects)
 Deficient knowledge, related to medication
regimen (Patient/Family Teaching)
PLANNING:
 Pt. will be able to have resolution of signs
and symptoms of infection. Length of time
for complete resolution depends on the
organism and site of infection and prevents
inhalational anthrax (post exposure).
IMPLEMENTATION:
 IM: Reconstitute IM doses with sterile or
bacteriostatic water for injection, 0.9%
NaCl, or D5W. May be diluted with
lidocaine to minimize injection
discomfort.
 Inject deep into a well-developed
muscle mass; massage well.
 IM route should only be used for treatment
of mild-to-moderate uncomplicated or
complicated urinary tract infections due to
Escherichia coli.
EVALUATION:
 Observe patient for signs and symptoms of
anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug and
notify healthcare professional immediately
if these symptoms occur. Keep
epinephrine, an antihistamine, and
resuscitation equipment close by incase of
an anaphylactic reaction.
 Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to healthcare
professional promptly as a sign of
pseudomembranous colitis.
 Lab Test Considerations: May cause
positive results for Coombs’ test in patients
receiving high doses or in neonates whose
mothers were given cephalosporins before
delivery.
Drug Classification: Fifth Generation
Generic Name: Ceftaroline
Brand Name: Teflaro
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IV (Adults 18 yr):Skin/skin structure
infections—600 mg every 12 hr for 5– 14
days; Community-acquired pneumonia—600
mg every 12 hr for 5– 7 days.
Renal Impairment
IV (Adults 18 yr): CCr 30 to 50 mL/min—
400 mg every 12 hr; CCr 15 to 30 mL/min—
300 mg every 12 hr; CCr 15 mL/min—200
mg every 12 hr.
DRUG ACTION
Binds to bacterial cell wall membrane,
causing cell death. Therapeutic Effects:
Bactericidal action against susceptible
bacteria.
Pharmacokinetics: Absorption: IV
administration results in complete
bioavailability of parent drug. Distribution:
Unknown. Metabolism and Excretion:
Page | 132
Ceftaroline fosamil is rapidly converted by
plasma phosphatases to ceftaroline, the
active metabolite; 88% excreted in urine, 6%
in feces. Half-life: 2.6 hr (after multiple
doses).
DRUG INTERACTION
Drug-Drug: None noted.
INDICATIONS
Treatment of acute bacterial skin/skin
structure infections and community-acquired
pneumonia.
CONTRAINDICATIONS:
Known serious hypersensitivity to
cephalosporins.
Adverse Reactions/Side Effects
GI: PSEUDOMEMBRANOUS COLITIS,
diarrhea, nausea.Derm:rash.Hemat:
hemolytic
anemia. Local: phlebitis at injection site.
Misc: hypersensitivity reactions including
ANAPHYLAXIS.
NURSING INTERVENTIONS
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; wbc) at beginning of and throughout
the therapy.
 Before initiating therapy, obtain a history to
determine previous use of and reactions to
penicillins or cephalosporins. Persons with
a negative history of penicillin sensitivity
may still have an allergic response
 Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
Diagnosis:
 Risk for infection (indications, side effects)
 Diarrhea (adverse reactions)
Planning:
 Pt. Will be able to have resolution of signs
and symptoms of infection. Length of time
for complete resolution depends on the
organism and site of infection and prevents
inhalational anthrax (post exposure).
Implementation:
 Intermittent infusion: reconstitute with 20
ml of sterile water for injection, 0.9% nacl,
d5w, or lr.diluent: dilute further with 50–
250 ml of same diluent unless
reconstituted with sterile water for injection,
then use 0.9% nacl, d5w, d2.5w, 0.45%
nacl, or lr. Mix gently to dissolve. Solution
is clear to light or dark yellow; do not
administer solutions that are discolored or
contain particulate matter. Solution is
stable for 6 hr at room temperature or 24
hr if refrigerated. Rate: infuse over 1 hr
Evaluation:
 Observe patient for signs and symptoms of
anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug and
notify healthcare professional immediately
if these symptoms occur. Keep
epinephrine, an antihistamine, and
resuscitation equipment close by in case of
an anaphylactic reaction.
 Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to healthcare
professional promptly as a sign of
pseudomembranous colitis.
 Lab Test Considerations: May cause
seroconversion from a negative to a
positive direct Coombs’ test. If anemia
develops during or after therapy, perform a
direct Coombs’ test. If drug-induced
hemolytic anemia is suspected,
discontinue ceftaroline and provide
supportive care.
Drug Classification: CARBAPENEMS
or BETA LACTAM ANTIBIOTICS
Generic Name: Aztreonam
Brand Name: Azactam
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IM, IV (Adults): Moderately severe
infections—1– 2 g q 8– 12 hr; severe or life
threatening infections (including those due
to Pseudomonas aeruginosa)—2 g q 6– 8
hr; urinary tract infections—0.5– 1 g q 8– 12
hr.
IV (Children 1 mo– 16 yr): Mild to moderate
infections infections—30 mg/kg q 8 hr;
moderate to severe infections infections—30
mg/kg q 6– 8 hr; cystic fibrosis—50 mg/kg q
6– 8 hr.
IV (Neonates 2 kg): 30 mg/kg q 6– 8 hr.
IV (Neonates 2 kg): 30 mg/kg q 8– 12 hr.
Inhaln (Adults and Children 7 yr): 75 mg
three times daily for 28 days.
DRUG ACTION
Binds to the bacterial cell wall membrane,
causing cell death. Therapeutic Effects:
Bactericidal action against susceptible
bacteria
Pharmacokinetics:
Absorption: Well absorbed following IM
administration. Low absorption follows
administration by inhalation.
Distribution: Widely distributed. Crosses
the placenta and enters breast milk in low
concentrations. High concentrations
achieved in sputum with inhalation.
Protein Binding: 56%.
Metabolism and Excretion: 60– 70%
excreted unchanged by the kidneys. 10% of
Page | 133
inhaled dose excreted unchanged in urine.
Small amounts metabolized by the liver.
Half-life: Adults: 1.5– 2 hr; Children: 1.7
hr; Neonates: 2.4– 9hr (increase in renal
impairment).
DRUG INTERACTION
Drug-Drug: Serum levels may be increase
by furosemide or probenecid.
INDICATIONS
Treatment of serious gram-negative
infections including: Septicemia, Skin and
skin structure infections, Intra-abdominal
infections, Gynecologic infections,
Respiratory tract infections, Urinary tract
infections. Useful for treatment of multi-
resistant strains of some bacteria including
aerobic gram-negative pathogens. Inhaln:
To improve respiratory symptoms in cystic
fibrosis (CF) patients with Pseudomonas
aeruginosa.
CONTRAINDICATIONS: Hypersensitivity
Adverse Reactions/Side Effects
CNS: SEIZURES. EENT: nasal congestion
(inhalation), nasopharyngeal pain
(inhalation). CV: chest discomfort
(inhalation). GI: PSEUDOMEMBRANOUS
COLITIS, abdominal pain (inhalation),
altered taste, diarrhea, nausea, vomiting.
Resp:cough (inhalation), wheezing
(inhalation), bronchospasm (inhalation).
Derm: rash. Local: pain at IM site, phlebitis
at IV site.Misc:allergic reactions including
ANAPHYLAXIS, fever (inhalation),
superinfection.
NURSING INTERVENTIONS
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; wbc) at beginning of and throughout
the therapy.
 Before initiating therapy, obtain a history to
determine previous use of and reactions to
penicillins or cephalosporins. Persons with
a negative history of penicillin sensitivity
may still have an allergic response
Diagnosis:
 Risk for infection (indications, side effects)
 Ineffective airway clearance (indications)
Planning:
 Pt. Will be able to have resolution of signs
and symptoms of infection. Length of time
for complete resolution depends on the
organism and site of infection and prevents
inhalational anthrax (post exposure).
 Pt. Will be able to have an improvement in
respiratory symptoms in patients with
cystic fibrosis
implementation:
 After adding diluent to vial, shake
immediately and vigorously.
 Im: use 15-ml vial and dilute each gram of
aztreonam with at least 3 ml of 0.9% nacl,
or sterile or bacteriostatic water for
injection. Stable at room temperature for
48 hr or 7 days if refrigerated.
Evaluation:
 Observe patient for signs and symptoms of
anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug and
notify healthcare professional immediately
if these symptoms occur.
Drug Classification:
GLYCOPEPTIDES
Generic Name: Vancomycin
Brand Name: Vancocin HCl
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Serious Systemic Infections
IV (Adults): 500 mg q 6 hr or 1 g q 12 hr (up
to 4 g/day).IV (Children 1 mo): 40
mg/kg/day divided q 6– 8 hr Staphylococcal
CNS infection—60 mg/kg/day divided q 6 hr,
maximum dose: 1 g/dose.IV (Neonates 1
wk– 1 mo): 1200 g: 15 mg/kg/day q 24 hr.
1200– 2000 g: 10–15 mg/kg/dose q 8– 12
hr. 2000 g: 15– 20 mg/kg/dose q 8 hr.
IV (Neonates 1 wk): 1200 g: 15 mg/kg/day
q 24 hr. 1200– 2000 g: 10– 15 mg/kg/dose q
12– 18 hr. 2000 g: 10– 15 mg/kg/dose q 8–
12 hr. IT (Adults): 20 mg/day. IT
(Children): 5– 20 mg/day.
IT (Neonates): 5– 10 mg/day.
DRUG ACTION
Binds to bacterial cell wall, resulting in cell
death. Therapeutic Effects: Bactericidal
action against susceptible organisms.
Pharmacokinetics: Absorption: Well
absorbed following IM administration; IV
administration results in complete
bioavailability. Distribution: Widely
distributed. CSF penetration better than with
first- and second-generation agents.
Crosses the placenta; enters breast milk in
low concentrations. Protein Binding: 90%.
Metabolism and Excretion: 33– 67%
excreted in urine as unchanged drug;
remainder excreted in feces Half-life: 6– 9
hr.
DRUG INTERACTION
Drug-Drug: Should not be administered
concomitantly with any calcium-containing
solutions.
INDICATIONS
Treatment of: Skin and skin structure
infections, Bone and joint infections,
Complicated and uncomplicated urinary tract
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infections, Uncomplicated gynecological
infections including gonorrhea, Lower
respiratory tract infections, Intra-abdominal
infections, Septicemia, Meningitis, Otitis
media. Perioperative prophylaxis.
CONTRAINDICATIONS:
Hypersensitivity to cephalosporins; Serious
hypersensitivity to penicillins; Pedi:
Neonates 28 days (use in hyperbilirubinemic
neonates may lead to kernicterus); Pedi:
Neonates 28 days requiring calcium-
containing IV solutions (increased risk of
precipitation formation).
Adverse Reactions/Side Effects
CNS: SEIZURES (high doses). GI:
PSEUDOMEMBRANOUS COLITIS,
diarrhea, cholelithiasis, gallbladder sludging.
Derm: rashes, urticaria. Hemat: bleeding,
eosinophilia, hemolytic anemia, leukopenia,
thrombocytosis. Local: pain at IM site,
phlebitis at IV site. Misc: allergic reactions
including ANAPHYLAXIS, superinfection.
NURSING INTERVENTIONS
ASSESSMENT:
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; WBC) at beginning of and
throughout the therapy.
 Before initiating therapy, obtain a history to
determine previous use of and reactions to
penicillins or cephalosporins. Persons with
a negative history of penicillin sensitivity
may still have an allergic response
DIAGNOSIS:
 Risk for infection (Indications, Side Effects)
 Diarrhea (Adverse Reactions)
PLANNING:
 Pt. will be able to have resolution of signs
and symptoms of infection. Length of time
for complete resolution depends on the
organism and site of infection and prevents
inhalational anthrax (post exposure).
 Pt. will be able to have a decreased
incidence of infection when used for
prophylaxis.
IMPLEMENTATION:
 IM: Reconstitute IM doses with sterile
water for injection, or 0.9% NaCl for
injection. May be diluted with lidocaine to
minimize injection discomfort.
 Inject deep into a well-developed muscle
mass; massage well.
EVALUATION:
 Observe patient for signs and symptoms of
anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug and
notify healthcare professional immediately
if these symptoms occur. Keep
epinephrine, an antihistamine, and
resuscitation equipment close by incase of
an anaphylactic reaction.
 Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to healthcare
professional promptly as a sign of
pseudomembranous colitis.
Drug Classification: MACROLIDES
Generic Name: Azithromycin
Brand Name: Zithromax
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Adult: PO Respiratory tract infections; Skin
and soft tissue infections As
tab/cap/immediate release suspension: 500
mg/day for 3 days, or 500 mg as single dose
on day 1 then 250 mg/day on days 2-5.
Uncomplicated genital infections due to
Chlamydia trachomatis; Chancroid 1 g as
a single dose. Uncomplicated gonorrhoea 1
g or 2 g as a single dose, combined with
ceftriaxone. Community-acquired
pneumonia as tab/cap/immediate release
suspension: 500 mg on day 1, then 250 mg
once daily on days 2-5.
As extended release suspension: 2 g as a
single dose. Acute bacterial sinusitis As
tab/cap/ immediate release suspension:
500 mg once daily
DRUG ACTION
Inhibits protein synthesis at the level of the
50 S bacterial ribosome. Therapeutic
Effects: Bacteriostatic action against
susceptible bacteria
Pharmacokinetics:
Absorption: Rapidly absorbed from the
gastrointestinal tract. Bioavailability: Approx
37%. Time to peak plasma concentration:
Approx 2-3 hours (oral, immediate release).
Distribution: Extensively distributed in the
tissues (skin, lungs, tonsils, cervix) and
sputum. Present in breastmilk. Volume of
distribution: 31-33 L/kg.
Protein Binding: 7-51%.
Metabolism: Metabolised in the liver to
inactive metabolites.
Excretion: Via bile (50%, as unchanged
drug); urine (6-14%, as unchanged drug).
Terminal elimination half-life: 68-72 hours
(conventional preparations); 59 hours
(extended release). Half-life: 68-72 hours
(conventional preparations); 59 hours
(extended release).
DRUG INTERACTION
Drug-Drug: Increased risk of prolonged QT
interval with class IA (e.g. quinidine,
procainamide) and class III (e.g. dofetilide,
amiodarone, sotalol) Increased serum
Page | 135
concentrations of digoxin, colchicine, and
ciclosporin. May potentiate the effects of oral
anticoagulants (e.g. warfarin).
INDICATIONS
Azithromycin is a macrolide antibiotic under
the azalide group. It inhibits RNA-dependent
protein synthesis by binding to the 50s
ribosomal subunit, preventing the
translocation of peptide chains.
CONTRAINDICATIONS:
Hypersensitivity to macrolide antibiotics.
History of hepatic
dysfunction/cholestatic jaundice
following previous antibiotic use
Adverse Reactions/Side Effects
CNS: dizziness, seizures, drowsiness,
fatigue, headache. CV:
TORSADESDEPOINTES, chestpain,
hypotension, palpitations, QT interval
prolongation. GI: HEPATOTOXICITY,
PSEUDOMEMBRANOUS COLITIS,
abdominal pain, diarrhea, nausea,
cholestatic jaundice, increase liver enzymes,
dyspepsia, flatulence, melena,
oralcandidiasis, pyloricstenosis. GU:
nephritis, vaginitis. Hemat: anemia,
leukopenia, thrombocytopenia. Derm:
STEVENS-JOHNSON SYNDROME, TOXIC
EPIDERMAL NECROLYSIS,
photosensitivity, rash. EENT: ototoxicity. F
and E: hyperkalemia. Misc: ANGIOEDEMA.
NURSING INTERVENTIONS
ASSESSMENT:
 Assess patient for skin rash frequently
during therapy. Discontinue azithromycin
at first sign of rash; may be life-
threatening. Stevens-Johnson syndrome
or toxic epidermal necrolysis may develop.
Treat symptomatically; may recur on
cetreatmentis stopped.
DIAGNOSIS:
 Risk for infection (Indications, Side Effects)
 Noncompliance (Patient/Family Teaching)
PLANNING:
 Pt. will be able to have resolution of signs
and symptoms of infection. Length of time
for complete resolution depends on the
organism and site of infection.
IMPLEMENTATION:
 PO: Administer 1hr before or 2hr after
meals
 For administration of single1-g packet,
thoroughly mix entire contents of packet
with 2oz (60mL) of water. Drink entire
contents immediately; add an additional
2oz of water, mix and drink to assure
complete consumption of dose. Do not use
the single packet to administer doses other
than 1000mg of azithromycin. Pedi:1-g
packet is not for pediatric use.
EVALUATION:
 Observe for signs and symptoms of
anaphylaxis (rash, pruritus, laryngeal
edema, wheezing).
Drug Classification: KETOLIDES
Generic Name: Telithromycin
Brand Name: Ketek
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): community-acquired
pneumonia—800 mg once daily for 7– 10
days.
DRUG ACTION
Blocks bacterial protein synthesis at the
level of the 50S ribosomal subunit.
Therapeutic Effects:Resolution of infection.
Pharmacokinetics: Absorption: 57%
absorbed following oral administration;
unaffected by food Distribution:
Concentrates in bronchial mucosa, epithelial
lining fluid and alveolar macrophages.
Metabolism and Excretion: 70%
metabolized by the liver (50% by CYP3A4),
13% excreted unchanged in urine, 7%
excreted unchanged via biliary/intestinal
elimination Half-life: 10 hr.
DRUG INTERACTION
Drug-Drug: Blood levels are increase by
ketoconazole and itraconazole. Increase
levels and risk of myopathy from
simvastatin, lovastatin, and racecadotril;
avoid concurrent use. Increase levels and
risk of toxicity with colchicine; avoid
concurrent use in patients with renal or
hepatic impairment; decrease dose of
colchicine if patients have normal renal and
hepatic function. Increase levels and risk of
excessive sedation with midazolam; careful
titration is required. Similar effects may
occur with triazolam. Increase levels of
metoprolol; use caution in patients with HF.
May also increase levels, effects and risk of
toxicity from ergot derivatives (ergotamine,
dihydroergotamine); concurrent use not
recommended; similar effects may occur
with carbamazepine,cyclosporine,
tacrolimus,sirolimus, hexobarbital, or
phenytoin. Rifampin decrease levels and
effectiveness; avoid concurrent use. Similar
effects may occur with phenytoin,
carbamazepine, or Phenobarbital
INDICATIONS
Community-acquired pneumonia
CONTRAINDICATIONS:
Page | 136
Hypersensitivity; History of hepatitis or
jaundice associated with use of
telithromycin; Hypersensitivity to macrolides
(erythromycin, azithromy cin,
clarithromycin); Concurrent use of pimozide,
ergot alkaloids, simvastatin, lovastatin,
atorvastatin, or rifampin; Congenital QTc
prolongation, uncorrected hypokalemia or
hypomagnesemia, bradycardia, concurrent
use of Class IA (quinidine, procainamide) or
Class III antiarrhythmics (dofetilide);
Concurrent use of colchicine in patients with
renal or hepatic impairment; Myasthenia
gravis; Lactation: Excreted in breast milk;
consider alternative to breast feeding
Adverse Reactions/Side Effects
CNS: confusion, hallucinations, loss of
consciousness. EENT: visual disturbances.
CV: arrhythmias, QTc interval prolongation.
GI: PSEUDOMEMBRANOUS COLITIS,
diarrhea, hepatitis, HEPATOTOXICITY,
nausea. Neuro: exacerbation of myasthenia
gravis..
NURSING INTERVENTIONS
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; wbc) at beginning of and throughout
the therapy.
 Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
Diagnosis:
 Riskforinfection(indications,sideeffects)
 Noncompliance (patient/family teaching)
Planning:
 Pt. Will be able to have resolution of signs
and symptoms of infection.
Implementation:
 Po: administer with or without food.
Swallow tablets whole; do not crush,
break, or chew
Evaluation:
 Monitor for signs or symptoms of hepatitis
(fatigue, malaise, anorexia, nausea,
jaundice, bilirubinuria, acholic stools, liver
tenderness or hepatomegaly). If these
occur, discontinue telithromycin
immediately and monitor liver function; do
not re-administer telithromycin.
 Lab Test Considerations:May
causeqplatelet count.
 Monitor liver function periodically during
therapy and if signs of hepatitis occur.
Drug Classification: LINCOSAMIDES
Generic Name: Clindamycin
Hydrochloride
Brand Name: Cleocin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Severe anaerobic infections
Adult: 150-300 mg 6 hrly, up to 450 mg in
severe infections. Max: 1.8 g/day.
Child: 3-6 mg/kg 6hrly. <10 kg: ≥37.5 mg 8
hrly. Severe anaerobic infections
Adult: 0.6-2.7 g daily in 2-4 divided doses,
increased to 4.8 g daily in life-threatening
infections. Infuse IV admin over 10-60 min
and at a rate of ≤30 mg/min. Single dose of
IM inj should not exceed 600 mg nor is
admin of above 1.2 g in a single 1 hr
infusion. Child:>1 mth 15-25 mg/kg daily in
3 or 4 divided doses; in severe infections,
increase to 40 mg/kg daily and a min dose
of 300 mg daily should be given regardless
of body wt. Acne Adult: As 1% preparation:
Apply a thin layer onto affected area bid.
Bacterial vaginosis Adult: As pessary or
2% cream: 100 mg at bedtime for 3-7 days.
DRUG ACTION
Inhibits protein synthesis of bacterial cell
wall by binding to bacterial ribosomal
receptor sites. Topically, decreases fatty
acid concentration on skin. Therapeutic
Effect: Bacteriostatic or bacteriocidal.
Pharmacokinetics:
Absorption: Well absorbed following PO/IM
administration. Minimal absorption following
topical/vaginal use.
Distribution: Widely distributed. Does not
significantly cross blood-brain barrier.
Crosses the placenta; enters breast milk.
Protein Binding: 94%
Metabolism: Mostly metabolized by the
liver.
Excretion: Via bile (50%, as unchanged
drug); urine (6-14%, as unchanged drug).
Terminal elimination half-life: 68-72 hours
(conventional preparations); 59 hours
(extended release).Half-life:: Neonates:
3.6– 8.7 hr; Infants up to 1 yr: 3 hr; Children
and adults: 2– 3 hr
DRUG INTERACTION
Drug-Drug: Kaolin/pectin may decrease GI
absorption. May enhance the neuromuscular
blocking action of other neuromuscular
blocking agents. Topical: Concurrent use
with irritants, abrasives, or desquamating
agents may result in additive irritation.
INDICATIONS
PO, IM, IV: Treatment of: Skin and skin
structure infections, Respiratory tract
infections, Septicemia, Intra-abdominal
infections, Gynecologic infections,
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Osteomyelitis, Endocarditis prophylaxis.
Topical Severe acne. Vag: Bacterial
vaginosis. Unlabeled Use: PO, IM, IV:
Treatment of Pneumocystis carinii
pneumonia, CNS toxoplasmosis, and
babesiosis.
CONTRAINDICATIONS:
Hypersensitivity; Regional enteritis or
ulcerative colitis (topical foam); Previous
pseudomembranous colitis; Severe liver
impairment; Diarrhea; Known alcohol
intolerance (topical solution, suspension).
Adverse Reactions/Side Effects
CNS: dizziness, headache, vertigo. CV:
arrhythmias, hypotension. GI:
PSEUDOMEMBRANOUS COLITIS,
diarrhea, bitter taste (IV only), nausea,
vomiting. Derm: rash. Local: local irritation
(topical products), phlebitis at IV site
NURSING INTERVENTIONS
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine,
and stool; wbc) at beginning of and
throughout the therapy.
 Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
Diagnosis:
 Risk for infection (indications) (side
effects)
 diarrhea (side effects)
Planning:
 Pt. Will be able to have resolution of
signs and symptoms of infection.
 Improvement in acne vulgaris lesions.
Improvement should be seen in 6 wk but
may take 8– 12 wk for maximum benefit.
Implementation:
 Po: administer with a full glass of water.
May be given with or without meals.
Shake liquid preparations well. Do not
refrigerate. Stable for 14 days at room
temperature.
 Im: do not administer 600 mg in a single
im injection.
Evaluation:
 Monitor bowel elimination. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to health care
professional promptly as a sign of
pseudomembranous colitis. This may
begin up to several weeks following the
cessation of therapy.
Drug Classification: LIPOPEPTIDES
Generic Name: Daptomycin
Brand Name: Cubicin
DOSAGE
IV (Adults): 4 mg/kg every 24 hr. Renal
Impairment IV (Adults): CCr 30 mL/min—4
mg/kg every 48 hr
ACTION
Causes rapid depolarization of membrane
potential following binding to bacterial
membrane; these results in inhibition of
protein, DNA, and RNA synthesis.
Therapeutic Effects: Death of bacteria with
resolution of infection
Pharmacokinetics:
Absorption: IV administration results in
complete bioavailability.
Distribution: Unknown
Protein Binding: 92%
Metabolism and Excretion: Metabolism not
known; mostly excreted by kidneys. Half-
life: 8.1 hr
DRUG INTERACTION
Drug-Drug: Tobramycin increase blood
levels. Concurrent HMG-CoA reductase
inhibitors may increase the risk of myopathy.
INDICATIONS
Complicated skin and skin structure
infections caused by aerobic Gram-positive
bacteria.
CONTRAINDICATIONS:
Hypersensitivity
Adverse Reactions/Side Effects
CNS: dizziness. Resp: EOSINOPHILIC
PNEUMONIA, dyspnea. CV: hypertension,
hypotension. GI: PSEUDOMEMBRANOUS
COLITIS, constipation, diarrhea, nausea,
vomiting, qliver enzymes. GU: renal
failure.Derm: pruritus, rash.Hemat:anemia.
Local: injection site reactions. MS: increase
CPK.Misc: fever.
NURSING INTERVENTIONS
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine,
and stool; wbc) at beginning of and
throughout the therapy.
 Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
Diagnosis:
 Risk for infection (indications) (side
effects)
Planning:
 Pt. Will be able to have resolution of
signs and symptoms of infection.
Implementation:
Page | 138
 Direct iv: reconstitute 500-mg vial with 10
ml of 0.9% nacl inserted toward wall of
vial. Rotate vial gently to wet powder.
Allow to stand for 10 min undisturbed.
Swirl vial gently to completely
reconstitute solution. Reconstituted vials
are stable for 12 hr at room temperature
or 48 hr if refrigerated. Concentration: 50
mg/ ml. Rate: administer over 2 min.
Evaluation:
 Monitor bowel elimination. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to health care
professional promptly as a sign of
pseudomembranous colitis. This may
begin up to several weeks following the
cessation of therapy.
 Monitor for signs and symptoms of
eosinophilic pneumonia (new onset or
worsening fever, dyspnea, difficulty
breathing, new infiltrates on chest
imaging studies). Discontinue
daptomycin if symptoms occur
 Monitor for development of muscle pain
or weakness, particularly of distal
extremities. Discontinue daptomycin in
patients with unexplained signs and
symptoms of myopathy in conjunction
with CPK elevation 1000 U/L, or in
patients without reported symptoms who
have marked elevations in CPK 2000
U/L. Consider temporarily suspending
agents associated with rhabdomyolysis,
(HMG-CoA reductase inhibitors) in
patients receiving daptomycin.
Drug Classification: SHORT-ACTING
TETRACYCLINE
Generic Name: Tetracycline
Brand Name: Sumycin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 250– 500 mg q 6 hr or 500
mg– 1 g q 12 hr. Chronic treatment of
acne—500 mg– 2 g/day for 3 wk, thenpto
125 mg– 1 g/day. PO (Children 8 yr): 6.25–
12.5 mg/kg q 6 hr or 12.5– 25 mg/kg q 12 hr
DRUG ACTION
Inhibits bacterial protein synthesis at the
level of the 30S bacterial ribosome.
Therapeutic Effects: Bacteriostatic action
against susceptible bacteria.
Pharmacokinetics:
Absorption: 60– 80% absorbed after oral
administration.
Distribution: Widely distributed some CSF
and good bone penetration; crosses the
placenta and enters breast milk.
Metabolism and Excretion: Excreted
mostly unchanged by the kidneys. Half-life:
6– 12 hr.
DRUG INTERACTION
Drug-Drug: May increase the effect of
warfarin. May decrease effectiveness of
estrogen-containing oral contraceptives.
Antacids, calcium, iron, and magnesium
form insoluble compounds (chelates) and
decrease absorption of tetracycline.
Sucralfate may bind to tetracycline and
prevent its absorption from the GI tract.
Cholestyramine orcolestipol decrease
absorption. Adsorbent antidiarrheal agents
may decrease absorption. Barbiturates,
phenytoin, or carbamazepine may decrease
activity of doxycycline. Drug-Food: Calcium
in foods or dairy products decrease
absorption by forming insoluble compounds
(chelates).
INDICATIONS
Complicated skin and skin structure
infections caused by aerobic Gram-positive
bacteria.
CONTRAINDICATIONS:
Hypersensitivity
Adverse Reactions/Side Effects
CNS: dizziness. Resp: EOSINOPHILIC
PNEUMONIA, dyspnea. CV: hypertension,
hypotension. GI: PSEUDOMEMBRANOUS
COLITIS, constipation, diarrhea, nausea,
vomiting, increase liver enzymes. GU: renal
failure. Derm: pruritus, rash. Hemat:
anemia. Local: injection site reactions. MS:
increase CPK. Misc: fever.
NURSING INTERVENTIONS
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine,
and stool; wbc) at beginning of and
throughout the therapy.
 Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
Diagnosis:
 Risk for infection (indications) (side
effects)
Planning:
 Pt. Will be able to have resolution of
signs and symptoms of infection.
Implementation:
Page | 139
 Direct iv: reconstitute 500-mg vial with 10
ml of 0.9% nacl inserted toward wall of
vial. Rotate vial gently to wet powder.
Allow to stand for 10 min undisturbed.
Swirl vial gently to completely
reconstitute solution. Reconstituted vials
are stable for 12 hr at room temperature
or 48 hr if refrigerated. Concentration: 50
mg/ ml. Rate: administer over 2 min.
Evaluation:
 Monitor bowel elimination. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to health care
professional promptly as a sign of
pseudomembranous colitis. This may
begin up to several weeks following the
cessation of therapy.
 Monitor for signs and symptoms of
eosinophilic pneumonia (new onset or
worsening fever, dyspnea, difficulty
breathing, new infiltrates on chest
imaging studies). Discontinue
daptomycin if symptoms occur
 Monitor for development of muscle pain
or weakness, particularly of distal
extremities. Discontinue daptomycin in
patients with unexplained signs and
symptoms of myopathy in conjunction
with CPK elevation 1000 U/L, or in
patients without reported symptoms who
have marked elevations in CPK 2000
U/L. Consider temporarily suspending
agents associated with rhabdomyolysis,
(HMG-CoA reductase inhibitors) in
patients receiving daptomycin.
Drug Classification: INTERMEDIATE
TETRACYCLINE Generic Name:
Demeclocycline HCl
Brand Name: Declomycin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults): 250– 500 mg q 6 hr or 500 mg–
1 g q 12 hr. Chronic treatment of acne—500
mg– 2 g/day for 3 wk, thenpto 125 mg–1
g/day.
PO (Children8 yr):6.25– 12.5 mg/kg q 6 hr or
12.5– 25 mg/kg q 12 hr
DRUG ACTION
Broad-spectrum, tetracycline antibiotic
isolated from mutant strain of Streptomyces
aureofaciens. Similar to tetracycline but is
absorbed more readily, excreted much more
slowly.
Pharmacokinetics:
Absorption: 60– 80% absorbed after oral
administration.
Distribution: Widely distributed, some CSF
and good bone penetration; crosses the
placenta and enters breast milk.
Metabolism and Excretion: Excreted
mostly unchanged by the kidneys.
Half-life: 6– 12 hr
DRUG INTERACTION
Drug-Drug: ANTACIDS, IRON
PREPARATION, calcium, magnesium, zinc,
kaolin-pectin, sodium bicarbonate can
significantly decrease demeclocycline
absorption; effects of desmopressin and
demeclocycline antagonized; increases
digoxin absorption, increasing risk of digoxin
toxicity; methoxyflurane increases risk of
renal failure.
Food: Dairy products significantly decrease
demeclocycline absorption; food may
decrease drug absorption also.
INDICATIONS
Treatment of various infections due to
unusual organisms, including: Mycoplasma,
Chlamydia, Rickettsia, Borrelia burgorferi.
Treatment of gonorrhea and syphilis in
penicillin-allergic patients. Prevention of
exacerbations of chronic bronchitis.
Treatment of acne.
CONTRAINDICATIONS:
Hypersensitivity; Some products contain
alcohol or bisulfites and should be avoided
in patients with known hypersensitivity or
intolerance; Pedi: Children 8 yr (permanent
staining of teeth); OB: Risk of permanent
staining of teeth in infant if used during last
half of pregnancy; Lactation:Lactation.
Adverse Reactions/Side Effects
Gastrointestinal: Anorexia, nausea,
vomiting, diarrhea, glossitis, dysphagia,
enterocolitis, pancreatitis and inflammatory
lesions (with monilial overgrowth) in the
anogenital region, increases in liver
enzymes, and hepatic toxicity has been
reported rarely. Skin: Maculopapular and
erythematous rashes, erythema multiforme.
Exfoliative dermatitis Renal toxicity: Acute
renal failure. Rise in BUN has been reported
and is apparently dose related.
Hypersensitivity reactions: Urticaria,
angioneurotic edema, polyarthralgia,
anaphylaxis, anaphylactoid purpura,
pericarditis exacerbation of systemic lupus
erythematosus, lupus like syndrome,
pulmonary infiltrates with eosinophilia. CNS:
Pseudotumor cerebri (benign intracranial
hypertension) in adults and bulging
fontanels in infants. Dizziness, headache,
tinnitus, and visual disturbances. Tooth
Page | 140
discoloration has occurred in pediatric
patients less than 8 years of age
NURSING INTERVENTIONS
ASSESSMENT:
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; WBC) at beginning of and
throughout the therapy.
 Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
DIAGNOSIS:
 Risk for infection (Indications) (Side
Effects)
PLANNING:
 Pt. will be able to have resolution of signs
and symptoms of infection.
IMPLEMENTATION:
 Direct IV: Reconstitute 500-mg vial with 10
mL of 0.9% NaCl inserted toward wall of
vial. Rotate vial gently to wet powder.
Allow to stand for 10 min undisturbed.
Swirl vial gently to completely reconstitute
solution. Reconstituted vials are stable for
12 hr at room temperature or 48 hr if
refrigerated. Concentration: 50 mg/ mL.
Rate: Administer over 2 min.
EVALUATION:
 Monitor bowel elimination. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to health care
professional promptly as a sign of
pseudomembranous colitis. This may
begin up to several weeks following the
cessation of therapy.
 Monitor for signs and symptoms of
eosinophilic pneumonia (new onset or
worsening fever, dyspnea, difficulty
breathing, new infiltrates on chest imaging
studies). Discontinue daptomycin if
symptoms occur
 Monitor for development of muscle pain or
weakness, particularly of distal extremities.
Discontinue daptomycin in patients with
unexplained signs and symptoms of
myopathy in conjunction with CPK
elevation 1000 U/L, or in patients without
reported symptoms who have marked
elevations in CPK 2000 U/L. Consider
temporarily suspending agents associated
with rhabdomyolysis, (HMG-CoA
reductase inhibitors) in patients receiving
daptomycin.
Drug Classification: LONG-ACTING
TETRACYCLINE
Generic Name: Doxycycline Hyclate
Brand Name: Vibramycin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
PO (Adults and Children 45 kg): Most
infections—100 mg q 12 hr on the 1st
day, then 100– 200 mg once daily or 50–
100 mg q 12 hr; Gonorrhea—100 mg q
12 hr for 7 days or 200 mg once daily for 7
days (delayed-release tablets) or 300 mg
followed 1 hr later by another 300-mg dose;
Malaria prophylaxis—100 mg once daily;
Lyme disease—100 mg twice daily;
Periodontitis– 20 mg twice daily; Rosacea—
40 mg once daily in morning.
DRUG ACTION
Inhibits bacterial protein synthesis at the
level of the 30S bacterial ribosome. Low-
dose products used in the management of
periodontitis inhibit collagenase.
Therapeutic Effects: Bacteriostatic action
against susceptible bacteria
Pharmacokinetics: Absorption: Well
absorbed from the GI tract. Distribution:
Widely distributed, some CSF and good
bone penetration; crosses placenta and
enters breast milk. Metabolism and
Excretion: 20– 40% excreted unchanged in
urine; some inactivation in intestine and
some enterohepatic circulation with
excretion in bile and feces. Half-life: 14– 17
hr (increase in severe renal impairment).
DRUG INTERACTION
Drug-Drug: May increase effect of warfarin.
May decrease effectiveness of estrogen-
containing oral contraceptives.
Antacids,calcium, iron, and magnesium form
insoluble compounds (chelates) and
decrease absorption of tetracyclines; this
effect is least with doxycycline.
Cholestyramine or colestipol decrease
absorption of tetracyclines. Adsorbent
antidiarrheals may decrease absorption.
Barbiturates, carbamazepine, or phenytoin
may decrease effectiveness.
Drug-Food: Calcium in foods or dairy
products decrease absorption by forming
insoluble compounds (chelates); this effect
is minimal with doxycycline
INDICATIONS
Treatment of various infections caused by
unusual organisms, including: Mycoplasma,
Chlamydia, Rickettsia, Borellia burgdorferi.
Treatment of inhalational anthrax
(postexposure) and cutaneous anthrax.
Treatment of gonorrhea and syphilis in
penicillin-allergic patients. Prevention of
exacerbations of chronic bronchitis.
Treatment of acne. Treatment of
inflammatory lesions associated with
rosacea (Oracea only). Malaria prophylaxis
Page | 141
CONTRAINDICATIONS:
Hypersensitivity; some products contain
alcohol or bisulfites and should be avoided
in patients with known hypersensitivity or
intolerance.
Adverse Reactions/Side Effects
CNS: benign intracranial hypertension
(higher in children), headache. GI:
Pseudomembranous
Colitis, diarrhea, nausea, vomiting,
esophagitis, hepatotoxicity, pancreatitis.
Derm: Drug rash with eosinophilia and
systemic symptoms, erythema
Multiforme, Stevens-Johnson Syndrome,
toxic epidermal necrolysis, photosensitivity,
rash. Hemat: blood dyscrasias. Local:
phlebitis at IV site. Misc: hypersensitivity
reactions, super infection.
NURSING INTERVENTIONS
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine,
and stool; wbc) at beginning of and
throughout the therapy.
 Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
Diagnosis:
 Risk for infection (indications) (side
effects)
 Noncompliance (patient/family teaching)
Planning:
 Pt. Will be able to have resolution of
signs and symptoms of infection.
 Pt. Will have decrease in acne lesions.
Implementation:
 Po: administer around the clock, at least
1 hr before or 2 hr after meals. May be
taken with food or milk if gi irritation
occurs. Administer with a full glass of
liquid and at least 1 hr before going to
bed to avoid esophageal ulceration. Use
calibrated measuring device for liquid
preparations. Shake liquid preparations
well. Do not administer within 1– 3 hr of
other medications
Evaluation:
 Assess for rash periodically during
therapy. May cause Stevens-Johnson
syndrome or toxic epidermal necrolysis.
Discontinue therapy if severe or if
accompanied with fever, general malaise,
fatigue, muscle or joint aches, blisters,
oral lesions, conjunctivitis, hepatitis
and/or eosinophilia
Drug Classification: GLYCYLCYCLINES
Generic Name: Tigecycline
Brand Name: Tygacil
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IV (Adults 18 yr): 100 mg initially, then 50
mg every 12 hr for 5– 14 days (skin/ skin
structure infections and intra-abdominal
infections) or 7– 14 days (pneumonia).
Hepatic Impairment IV (Adults 18 yr): Child-
Pugh C—100 mg initially, then 25 mg every
12 hr.
DRUG ACTION
Inhibits bacterial protein synthesis by
binding to the 30S ribosomal subunit.
Therapeutic Effects: Resolution of
infection.
Pharmacokinetics: Absorption: IV
administration results in complete
bioavailability. Distribution: Widely
distributed with good penetration into gall
bladder, lung, and colon; crosses the
placenta. Metabolism and Excretion:
Minimal metabolism; primary route of
elimination is biliary/fecal excretion of
unchanged drug and metabolites (59%),
33% renal (22% unchanged). Half-life: 27.1
hr (after 1 dose); 42.4 hr after multiple
doses.
DRUG INTERACTION
Drug-Drug: May decrease the effectiveness
of hormonal contraceptives. Effects on
warfarin are unknown (monitoring
recommended).
INDICATIONS
Complicated skin/skin structure infections,
complicated intra-abdominal infections,
or community-acquired bacterial pneumonia
caused by susceptible bacteria (Should
only be used when alternative treatments
are not suitable; should NOT be used for
diabetic foot infections).
CONTRAINDICATIONS:
Hypersensitivity; Diabetic foot infections;
Hospital-acquired or ventilator-associated
pneumonia; Pedi: Children
Adverse Reactions/Side Effects
CNS: Somnolence. Derm: Stevens-Johnson
Syndrome. GI: Pancreatitis,
Pseudomembranous Colitis, Nausea,
Vomiting, Altered Taste, anorexia, dry
mouth, hepatotoxicity, jaundice. GU:
increase serum creatinine. Endo:
hyperglycemia, hypoglycemia. F and E:
hypocalcemia, hyponatremia. Resp:
pneumonia. Local: injection site reactions.
Misc: Death, allergic reactions.
NURSING INTERVENTIONS
Page | 142
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine,
and stool; wbc) at beginning of and
throughout the therapy.
 Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
Diagnosis:
 Risk for infection (indications) (side
effects)
Planning:
 Pt. Will be able to have resolution of
signs and symptoms of infection.
Implementation:
 Po: administer around the clock, at least
1 hr before or 2 hr after meals. May be
taken with food or milk if gi irritation
occurs. Administer with a full glass of
liquid and at least 1 hr before going to
bed to avoid esophageal ulceration. Use
calibrated measuring device for liquid
preparations. Shake liquid preparations
well. Do not administer within 1– 3 hr of
other medications
Evaluation:
 Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to health care
professional promptly as a sign of
pseudomembranous colitis. May begin
up to several weeks following cessation
of therapy
 Assess patient for signs of pancreatitis
(nausea, vomiting, abdominal pain,
increased serum lipase or amylase)
periodically during therapy. May require
discontinuation of therapy.
Drug Classification:
AMINOGLYCOSIDES
Generic Name: Amikacin Sulfate
Brand Name: Amikin
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IM, IV (Adults and Children): 15 mg/kg/day
divided q 8– 12 hr (not to exceed 1.5 g/day).
Mycobacterium avium complex infection:
7.5– 15 mg/kg/day divided q 12– 24 hr.
IM, IV (Neonates): Loading dose—10
mg/kg. Maintenance dose—7.5 mg/kg q
12 hr.
Renal Impairment
IM, IV (Adults): Loading dose—7.5 mg/kg;
further dosing based on serum levels.
DRUG ACTION
Inhibits protein synthesis in bacteria at the
level of the 30S ribosome. Resists the action
of enzymes known to inactivate other
aminoglycosides. Therapeutic Effects:
Bactericidal action against susceptible
bacteria.
Pharmacokinetics: Absorption: Poorly
absorbed from the GI tract. Well absorbed
after IM administration; IV administration
results in complete bioavailability.
Distribution: Widely distributed throughout
extracellular fluid. Crosses the placenta;
small amounts enter breast milk. Poor
penetration into CSF (increase when
meninges inflamed). Metabolism and
Excretion: Excretion is mainly (90%) renal;
minimal amounts are metabolized by the
liver. Half-life: Infants 7 days: 4– 5 hr;
Children: 1.6– 2.5 hr; Adolescents: 0.5–
2.5 hr; Adults: 2– 3 hr (increase in renal
impairment, decrease in patients with
burns).
DRUG INTERACTION
Drug-Drug: Inactivated by extended-
spectrum penicillins when coadministered
to patients with renal insufficiency. May
potentiate effects of inhalation anesthetics
or neuromuscular blockers.increase
incidence of ototoxicity with loop diuretics.
increase incidence of nephrotoxicity with
other nephrotoxic drugs, such as
Amphotericin, vancomycin, acyclovir,
cisplatin, or cephalosporins.
INDICATIONS
Complicated skin/skin structure infections,
complicated intra-abdominal infections, or
community-acquired bacterial pneumonia
caused by susceptible bacteria (Should only
be used when alternative treatments are not
suitable; should NOT be used for diabetic
foot infections).
CONTRAINDICATIONS:
Hypersensitivity to amikacin, other
aminoglycosides, or bisulfites
Adverse Reactions/Side Effects
CNS: vertigo. EENT: ototoxicity (vestibular
and cochlear). GU: nephrotoxicity. Neuro:
enhanced neuromuscular blockade. Resp:
apnea. Misc: hypersensitivity reactions.
NURSING INTERVENTIONS
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; wbc) at beginning of and throughout
the therapy.
 Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
Diagnosis:
Page | 143
 Risk for infection (indications) (side effects)
Planning:
 Pt. Will be able to have resolution of signs
and symptoms of infection.
Implementation:
 Po: administer around the clock, at least 1
hr before or 2 hr after meals. May be taken
with food or milk if gi irritation occurs.
Administer with a full glass of liquid and at
least 1 hr before going to bed to avoid
esophageal ulceration. Use calibrated
measuring device for liquid preparations.
Shake liquid preparations well. Do not
administer within 1– 3 hr of other
medications
Evaluation:
 Lab test considerations: Monitor renal
function by urinalysis, specific gravity,
BUN, creatinine, and CCr before and
during therapy
 Monitor therapeutic blood levels
periodically during therapy. Timing of blood
levels is important in interpreting results.
Draw blood for peak levels 1 hr after IM
injection and 30 min after a 30-min IV
infusion is completed. Trough levels
should be drawn just before next dose.
Peak level range 20–30 mcg/mL; trough
level 10 mcg/mL.
Drug Classification:
FLUOROQUINOLONES or
QUINOLONES
Generic Name: Levofloxacin
Brand Name: Levaquin
DOSAGE
PO, IV (Adults): Most infections—250– 750
mg q 24 hr; Inhalational anthrax (post-
exposure)—500 mg daily for 60 days.
PO, IV (Children 50 kg): Inhalational
anthrax (post-exposure)—500 mg daily for
60 days; Plague—500 mg daily for 10– 14
days.
PO, IV (Children 50 kg and 6 mo):
Inhalational anthrax (post-exposure)–
8 mg/kg (max: 250 mg/dose) every 12 hr for
60 days. Plague—8 mg/kg (max: 250
mg/dose) every 12 hr for 10– 14 days; Other
infections—10 mg/kg/dose every 24 hr
(max: 500 mg/dose).
ACTION
Inhibits bacterial DNA synthesis by inhibiting
DNA gyrase enzyme. Therapeutic Effects:
Death of susceptible bacteria.
Pharmacokinetics:
Absorption: Well absorbed (99%) after oral
administration; IV administration results in
complete bioavailability.
Distribution: Widely distributed. High tissue
and urinary levels are achieved. Appears to
cross the placenta.
Protein Binding: 24– 38%.
Metabolism and Excretion: 87% excreted
unchanged in urine, small amounts
metabolized.
Half-life: 8 hr
DRUG INTERACTION
Drug-Drug: Concurrent use of amiodarone,
disopyramide, procainamide, quinidine,
dofetilide, or sotalol increase risk of torsade
de pointes in susceptible individuals (avoid
concurrent use).increase serum theophylline
levels and may lead to toxicity.
Administration with antacids, iron salts,
bismuth subsalicylate, sucralfate, and zinc
salts decrease absorption. May increase the
effects of warfarin. Serum levels may be
decrease by antineoplastic agents.
Cimetidine may interfere with elimination.
Probenecid prenal elimination. May increase
the risk of nephrotoxicity from cyclosporine.
Concurrent therapy with corticosteroids may
increase the risk of tendon rupture.
Drug-Food: Absorption is impaired by
concurrent enteral feeding (because of
metal cations).
INDICATIONS
PO, IV: Treatment of the following bacterial
infections: Urinary tract infections, including
cystitis, pyelonephritis, and prostatitis,
Respiratory tract infections, including acute
sinusitis, acute exacerbations of chronic
bronchitis, community-acquired pneumonia,
and nosocomial pneumonia, Uncomplicated
and complicated skin and skin structure
infections. Post-exposure treatment of
inhalational anthrax. Treatment and
prophylaxis of plague.
CONTRAINDICATIONS:
Hypersensitivity (cross-sensitivity within
class may exist); QTc interval prolongation;
Uncorrected hypokalemia or
hypomagnesemia; Concurrent use of Class
IA antiarrhythmics (disopyramide, quinidine,
procainamide) or Class III antiarrhythmics
(amiodarone, sotalol) (increased risk of QTc
interval prolongation and torsade de
pointes); History of myasthenia gravis (may
worsen symptoms including muscle
weakness and breathing problems); OB:
Pregnancy; Lactation: Not recommended.
Adverse Reactions/Side Effects
CNS: elevated intracranial pressure
(including pseudotumor cerebri), seizures,
agitation, anxiety, confusion, depression,
Page | 144
dizziness, drowsiness, hallucinations,
headache, insomnia, nightmares, paranoia,
tremor. CV: torsade de pointes, QT interval
prolongation. GI: HEPATOTOXICITY,
PSEUDOMEMBRANOUS COLITIS, nausea,
abdominal pain, diarrhea, vomiting. GU:
vaginitis. Derm: STEVENS-JOHNSON
SYNDROME, photosensitivity, rash. Endo:
hyperglycemia, hypoglycemia. Local:
phlebitis at IV site. Neuro: peripheral
neuropathy. MS: arthralgia, tendinitis,
tendon rupture. Misc: hypersensitivity
reactions including ANAPHYLAXIS.
NURSING INTERVENTIONS
ASSESSMENT:
● Assess for infection (vital signs;
appearance of wound, sputum, urine,
and stool; WBC; urinalysis; frequency
and urgency of urination; cloudy or foul-
smelling urine) at beginning of and during
therapy.
● Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
● Observe patient for signs and symptoms
of anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug and
notify physician or other health care
professional immediately if these
problems occur. Keep epinephrine, an
antihistamine, and resuscitation
equipment close by in case of an
anaphylactic reaction.
● Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to health care
professional promptly as a sign of
pseudomembranous colitis. May begin
up to several weeks following cessation
of therapy.
● Assess for rash periodically during
therapy. May cause Stevens-Johnson
syndrome. Discontinue therapy if severe
or if accompanied with fever, general
malaise, fatigue, muscle or joint aches,
blisters, oral lesions, conjunctivitis,
hepatitis and/or eosinophilia.
● Assess for signs and symptoms of
peripheral neuropathy (pain, burning,
tingling, numbness, and/or weakness or
other alterations of sensation including
light touch, pain, temperature, position
sense, and vibratory sensation)
periodically during therapy. Symptoms
may be irreversible; discontinue
levofloxacin if symptoms occur.
● Lab Test Considerations: May cause
increase serum AST, ALT, LDH, bilirubin,
and alkaline phosphatase.
● May also cause increase or decrease
serum glucose.
Diagnosis:
● Risk for infection (Patient/Family
Teaching)
Planning/Implementation:
● Do not confuse levofloxacin with
levetiracetam.
● PO: May be administered without regard
to meals. Products or foods containing
calcium, magnesium, aluminum, iron,
zinc should not be ingested for 4 hr
before and 2 hr after administration.
IV Administration
● pH: 3.8– 5.8.
● Intermittent Infusion: Diluent: Dilute to a
with 0.9% NaCl, D5W, D5/0.9% NaCl,
D5/0.45% NaCl, or D5/LR.
Concentration: 5 mg/mL. Also available
in premixed bottles and flexible
containers with D5W, which need no
further dilution. Discard unused solution.
Diluted solution is stable for 72 hr at
room temperature and 14 days if
refrigerated. Rate: Administer by infusion
over at least 60 min for 250–mg or 500–
mg doses and over 90 min for 750–mg
dose. Avoid rapid bolus injection to
prevent hypotension.
Evaluation:
● Resolution of the signs and symptoms of
bacterial infection. Time for complete
resolution depends on organism and site
of infection.
● Avoidance of signs and symptoms of
inhalational anthrax (postexposure
treatment).
● Prevention and treatment of plague.
Drug Classification:
CHLORAMPHENICOL
Generic Name: Chloramphenicol
Brand Name: Chloromycetin
DOSAGE
IV (Adults): 12.5 mg/kg q 6 hr (up to 100
mg/kg/day).
IV (Children): Most infections—12.5mg/kg q
6 hr (maximum daily dose 4 g).
Bacteremia/meningitis—up to 50– 100
mg/kg/day.
IV (Infants 2 wk): 12.5 mg/kg q 6 hr
(maximum daily dose 4 g). Bacteremia/
meningitis—up to 50– 100 mg/kg/day.
IV (Neonates 7 days and 2 kg): 25 mg/kg q
12 hr.
IV (Neonates birth– 7 days or 2 kg): 25
mg/kg once daily.
ACTION
Inhibits protein synthesis in susceptible
bacteria at the level of the 50S ribosome.
Therapeutic Effects: Bacteriostatic action.
Spectrum: Wide variety of grampositive
aerobic organisms including:Streptococcus
Page | 145
pneumoniae and other streptococci, Some
enterococci (especially vancomycin-
resistant). Gram-negative pathogens:
Haemophilus influenzae, Neisseria
meningitidis, Salmonella, Shigella.
Anaerobes: Bacteroides fragilis, Prevotella
melaninogenica. Other organisms inhibited:
Rickettsia, Chlamydia,Mycoplasma.
Pharmacokinetics:
Absorption: Some systemic and intraocular
absorption follows ophthalmic
administration.
Distribution: Widely distributed. Crosses
the blood-brain barrier with CSF levels 60%
of serum values. Crosses the placenta;
enters breast milk.
Metabolism and Excretion: Mostly
metabolized by the liver; 10% excreted
unchanged by the kidneys.
Half-life:1.5– 3.5 hr. Onset: rapid Peak:
end of infusion Duration: 6–12 hr
DRUG INTERACTION
Drug-Drug: May increase effects of the
following drugs: oral hypoglycemic agents,
warfarin, and phenytoin. Phenobarbital or
rifampin may decrease chloramphenicol
blood levels. May delay response to vitamin
B or folic acid therapy. Bone marrow
depression may be additive with bone
marrow-depressing agents (antineoplastic).
INDICATIONS
IV: Management of the following serious
infections when less toxic agents cannot be
used: Skin and soft-tissue infections, Intra-
abdominal infections, CNS infections
(including meningitis), Bacteremia. Ophth
Management of local infections.
CONTRAINDICATIONS:
Hypersensitivity; Previous toxic reaction to
chloramphenicol.
Adverse Reactions/Side Effects
CNS: confusion, delirium, depression,
headache. EENT: blurred vision, optic
neuritis. GI: bitter taste (IV only), diarrhea,
enterocolitis, glossitis, nausea, stomatitis,
vomiting. Derm: rashes, urticaria. Hemat:
aplastic anemia, bone marrow depression,
neutropenia, thrombocytopenia. Neuro:
peripheral neuritis. Misc: angioedema, gray
syndrome in newborns, fever.
NURSING INTERVENTIONS
Assessment:
 Assess for infection (vital signs;
appearance of wound, sputum, urine,
and stool; wbc) at beginning of and
throughout the therapy.
 Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
Diagnosis:
 Risk for infection (indications) (side
effects)
Planning:
 Pt. Will be able to have resolution of
signs and symptoms of infection.
Implementation:
 Medication should be administered
around the clock.
 Direct iv: reconstitute to a 10% solution
by adding 10 ml of sterile water for
injection or d5w to each 1 g. Do not use
preparations containing benzyl alcohol in
neonates. Concentration: final
concentration should not exceed 100
mg/ml. Rate: inject slowly over at least 1
min
Evaluation:
 Assess daily for signs of bone marrow
depression (petechiae, sore throat,
fatigue, unusual bleeding, bruising).
Patients who have impaired liver or renal
function, infants, children, and the elderly
are at the greatest risk of developing
adverse effects.
 Monitor therapeutic blood levels
periodically during therapy. Timing of
blood levels is important in interpreting
results. Draw blood for peak levels 1 hr
after IM injection and 30 min after a 30-
min IV infusion is completed. Trough
levels should be drawn just before next
dose. Peak level range 20–30 mcg/mL;
trough level 10 mcg/mL.
Drug Classification:
STREPTOGRAMINS
Generic Name:
Quinupristin/Dalfopristin
Brand Name: Synercid
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
IV (Adults and Children 12– 17 yr): 7.5
mg/kg q 12 hr for at least 7 days
DRUG ACTION
Quinupristin inhibits the late phase of protein
synthesis at the level of the bacterial
ribosome; dalfopristin inhibits the early
phase. Therapeutic Effects: Bacteriostatic
effect against susceptible organisms
Pharmacokinetics:
Absorption: IV administration results in
complete bioavailability.
Distribution: Unknown.
Protein Binding: Moderate.
Metabolism and Excretion: Both are
converted to compounds with additional
Page | 146
anti-infective activity; parent drugs and
metabolites are mostly excreted in feces
(75–77%); 15% of quinupristin and 17% of
dalfopristin excreted in urine.
Half-life: Quinupristin—0.85 hr;
dalfopristin—0.7 hr.
DRUG INTERACTION
Drug-Drug: Inhibits the cytochrome P450
3A4 drug metabolizing enzyme system;
inhibits metabolism of cyclosporine,
midazolam, and nifedipine and increase risk
of toxicity (careful monitoring required).
Similar effects may be expected with
concurrent use of delavirdine, nevirapine,
indinavir, ritonavir, vinca alkaloids,
docetaxel, paclitaxel, diazepam, verapamil,
diltiazem, HMG CoA reductase inhibitors,
tacrolimus, methylprednisolone,
carbamazepine, quinidine, lidocaine, and
disopyramide.
INDICATIONS
Complicated skin/skin structure infections
caused by Staphylococcus aureus
(methicillin, susceptible) or Streptococcus
pyogenes.
CONTRAINDICATIONS:
Hypersensitivity;
Adverse Reactions/Side Effects
CNS: headache. CV: thrombophlebitis. GI:
diarrhea, nausea, vomiting. Derm: pruritus,
rash. Local: edema/inflammation/pain at
infusion site, infusion site reactions. Misc:
allergic reactions, pain. GI:
Pseudomembranous Colitis Misc:
anaphylaxis
NURSING INTERVENTIONS
Assessment:
● Assess patient for infection (vital signs;
appearance of wound, sputum, urine,
and stool; wbc) at beginning of and
throughout therapy.
● Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
● Monitor patient for pain or inflammation
at the infusion site frequently throughout
infusion. Increasing the volume of diluent
from 250 ml to 500 ml or 750 ml or
infusing via a peripherally inserted central
catheter or central venous catheter may
be required.
● Observe patient for signs and symptoms
of anaphylaxis (rash, pruritus, laryngeal
edema, wheezing). Discontinue drug and
notify physician or other health care
professional immediately if these
problems occur. Keep epinephrine, an
antihistamine, and resuscitation
equipment close by in case of an
anaphylactic reaction.
● Assess patient for myalgia and arthralgia
after infusion. May be severe. Reducing
dose frequency to every 12 hr may
decrease pain. Symptoms usually
resolve upon discontinuation of
medication.
● Lab test considerations: may cause
increase serum total bilirubin
concentrations.
Diagnosis:
● Risk for infection (indications) (side
effects)
● Diarrhea (adverse reactions)
Planning/implementation:
Iv administration
● Ph: 5.0.
● Intermittent infusion: reconstitute the 500-
mg vial with 5 ml and the 600-mg vial
with 6 ml of d5w or sterile water for
injection, respectively, for a concentration
of 100 mg/ml. Avoid shaking to prevent
foam formation. Allow solution to sit until
all foam has disappeared. Diluent: dilute
further with 250 ml of d5w (100 ml can be
used for central line administration). May
dilute in 500 ml or 750 ml of d5w if
severe venous irritation occurs after
peripheral administration. Reconstituted
vials should be used within 30 min.
Infusion is stable for 5 hr at room
temperature or 54 hr if refrigerated. Rate:
infuse over 60 min. Flush line before and
after infusion with d5w.
Evaluation:
● Resolution of signs and symptoms of
infection. Length of time for complete
resolution depends on the organism and
site of infection.
Drug Classification:
OXAZOLIDINONES
Generic Name: Linezolid
Brand Name: Zyvox
DOSAGE,ROUTE& FREQUENCY
( RECOMMENDED)
Vancomycin-Resistant Enterococcus
faecium
Adult/Adolescent: PO/IV >12 y, 600 mg
q12h x 14–28 d
Child: PO/IV 2–11 y, 10 mg/kg q8 h x 14–
28d
Nosocomial or Community-Acquired
Pneumonia, Complicated Skin Infections
Adult/Adolescent: PO/IV >12 y, 600 mg
q12h x 10–14 d
Child: PO/IV 5–11 y, 10 mg/kg q8h x 10–14d
Uncomplicated Skin Infections
Page | 147
Adult/Adolescent: PO >12 y, 600 mg q12h x
10–14 d
Child: PO <5 y, 10 mg/kg q8h x 10–14 d 5–
11 y, 10 mg/kg q12h x 10–14 d
DRUG ACTION
Synthetic antibiotic of a new class, the
oxazolidinone group that is bacteriocidal
against gram-positive, gram-negative, and
anaerobic bacteria. It binds to a site on the
bacterial 23S ribosomal RNA of the bacteria
which prevents the bacterial RNA translation
process.
Pharmacokinetics:
Absorption: Rapidly or extensively
absorbed, 100% bioavailable.
Distribution: The plasma protein binding of
linezolid is approximately 31% and is
concentration-independent.
Metabolism and Excretion: Linezolid is
primarily metabolized by oxidation of the
morpholine ring, which results in two inactive
ring-opened carboxylic acid metabolites: the
aminoethoxyacetic acid metabolite (A), and
the hydroxyethyl glycine metabolite (B).
Nonrenal clearance accounts for
approximately 65% of the total clearance of
linezolid.
Half-life: 6–7 h. Onset: Peak: 1–2 h PO.
DRUG INTERACTION
Drug-Drug: Linezolid is a reversible,
nonselective inhibitor of monoamine
oxidase. Linezolid has the potential for
interaction with adrenergic and serotonergic
agents.
INDICATIONS
Treatment of Infections caused by
vancomycin-resistant Enterococcus faecium,
Nosocomial pneumonia caused by
Staphylococcus aureus (methicillin-
susceptible and methicillin-resistant strains),
Complicated skin/skin structure infections
caused by S. aureus (methicillin-susceptible
and methicillin-resistant strains),
Streptococcus pyogenes or S. agalactiae
(including diabetic foot infections),
Uncomplicated skin/skin structure infections
caused by S. aureus (methicillin-susceptible
and methicillin-resistant strains), S.
pyogenes, Community-acquired pneumonia
caused by Streptococcus pneumoniae
(including multidrug-resistant strains) or S.
aureus (methicillin-susceptible strains only).
CONTRAINDICATIONS:
Hypersensitivity
Adverse Reactions/Side Effects
CV: headache, insomnia. GI:
PSEUDOMEMBRANOUS COLITIS,
diarrhea, increased liver function tests,
nausea, taste alteration, vomiting. F and E:
lactic acidosis. Hemat: thrombocytopenia.
Neuro: optic neuropathy, peripheral
neuropathy.
NURSING INTERVENTIONS
Assessment:
 Assess heart rate, ECG, and heart
sounds, especially during exercise (See
Appendices G, H). Report any rhythm
disturbances or symptoms of increased
arrhythmias, including palpitations, chest
discomfort, shortness of breath, fainting,
and fatigue/weakness.
 Assess blood pressure periodically and
compare to normal. Report low blood
pressure (hypotension), especially if
patient experiences dizziness, fatigue, or
other symptoms.
Diagnosis:
 Risk for infection (indications) (side
effects)
Planning:
 Pt. Will be able to have resolution of
signs and symptoms of infection.
Implementation:
 Always wash hands thoroughly and
disinfect equipment (whirlpools,
electrotherapeutic devices, treatment
tables, and so forth) to help prevent the
spread of infection. Use universal
precautions or isolation procedures as
indicated for specific patients.
 Assess exercise tolerance frequently
(blood pressure, heart rate, fatigue
levels), and terminate exercise
immediately if any untoward responses
occur
Evaluation:
 Monitor signs of pseudomembranous
colitis, including diarrhea, abdominal
pain, fever, pus or mucus in stools, and
other severe or prolonged GI problems
(nausea, vomiting, and heartburn). Notify
physician or nursing staff immediately of
these signs.
 Monitor signs of lactic acidosis, including
confusion, lethargy, stupor, shallow rapid
breathing, tachycardia, hypotension,
nausea, and vomiting. Notify physician or
nursing staff immediately if these signs
occur.
Classification: AMINOCYCLITOL
Brand Name: Trobicin
Generic Name: Spectinomycin
Recommended Dosage, Route, and
Frequency:
Uncomplicated Gonorrhea
Page | 148
Adult: IM 2 g as single dose
Child: IM <45 kg, 40 mg/kg (max: 2 g); >45
kg, use adult dosing
Disseminated Gonorrhea
Adult: IM 2 g q12h for 7 d or until switched to
oral medication
Child: IM 8 y and 45 kg, 2 g q12h for 7 d
Drug Action: Antibiotic produced by
Streptomyces spectabilis. Action is usually
bacteriostatic. Variable activity against a
wide variety of gram-negative and gram-
positive organisms.
Absorption: Readily absorbed from IM site.
Metabolism and Excretion: Metabolized in
liver. Excreted in urine.
Half-life: 1.2–2.8 h. Onset: Peak: 1 hr
Drug-Drug and Drug-Food Interactions:
No clinically significant interactions
established.
Indications: Only for treatment of
uncomplicated gonorrhea in patients
sensitized or resistant to penicillin or other
effective drugs approved by US Centers for
Disease Control and Prevention.
Contraindications: Safety during
pregnancy (category B), lactation, and in
infants and children 8 y is not established.
Side Effects:
Skin: Pain and soreness at injection site,
urticaria, pruritus, transient rash. Body as a
Whole: Headache, dizziness, chills, fever,
insomnia, nervousness. GI: Nausea,
vomiting.
Adverse Reaction:
Metabolic: Decrease in Hgb, Hct, Clcr,
elevated serum alkaline phosphatase, ALT,
BUN.
Nursing Responsibilities:
Assessment:
● Observe patient for 45–60 min after
injection. Systemic anaphylaxis has been
reported (apprehension, pruritus,
hypertension, abdominal pain, collapse).
● Obtain serologic tests for syphilis at time of
diagnosis in patients with gonorrhea and
again after 3 mo.
● Monitor clinical effectiveness of drug to
detect antibiotic resistance.
● Culture all gonococcal infection sites 3–7 d
after spectinomycin therapy is completed
to verify eradication of infection.
● Lab tests: Monitor Hgb and Hct when
multiple doses are required.
DIAGNOSIS:
 Risk for infection (Indications) (Side
Effects)
PLANNING:
 Pt. Will be able to have resolution of signs
and symptoms of infection.
Implementation:
● Give IM injection deep into upper outer
quadrant of gluteus. No more than 5 ml
should be injected into single site (using
20-gauge needle). Injection may be
painful.
● Reconstitute with supplied diluent
(bacteriostatic water for injection with 0.9%
benzyl alcohol). Shake vial vigorously
immediately after adding diluent and
before withdrawing drug.
● Use solution within 24 h of reconstitution.
Evaluation:
 Monitor signs of pseudomembranous
colitis, including diarrhea, abdominal pain,
fever, pus or mucus in stools, and other
severe or prolonged GI problems (nausea,
vomiting, heartburn). Notify physician or
nursing staff immediately of these signs.
 Monitor signs of lactic acidosis, including
confusion, lethargy, stupor, shallow rapid
breathing, tachycardia, hypotension,
nausea, and vomiting. Notify physician or
nursing staff immediately if these signs
occur.
Classification: SULFONAMIDES &
TRIMETHOPRIM
Brand Name: Bactrim, Bactrim DS,
Septra
Generic Name: Sulfamethoxazole
Recommended Dosage, Route, and
Frequency:
Bacterial Infections
PO, IV (Adults and Children 2 mo): Mild-
moderate infections—6– 12 mg TMP/kg/day
divided q 12 hr; Serious
infection/Pneumocystis—15– 20 mg TMP/
kg /day/divided q 6– 8 hr.
PO (Adults): Urinary tract infection/chronic
bronchitis—1 double strength tablet (160 mg
TMP/800 mg SMX) q 12 hr for 10– 14 days.
Urinary Tract Infection Prophylaxis
PO, IV (Adults and Children 2 mo): 2 mg
TMP/kg/dose daily or 5 mg TMP/kg/ dose
twice weekly.
P. jirovecii Pneumonia (Prevention)
PO (Adults): 1 double strength tablet (160
mg TMP/800 mg SMX) daily (may also be
given 3 times weekly).
PO (Children 1 mo): 150 mg TMP/m2 /day
divided q 12 hr or given as a single dose on
3 consecutive days/wk (not to exceed 320
mg TMP/1600 mg SMX per day).
Page | 149

Drug Action: Combination inhibits the
metabolism of folic acid in bacteria at two
different points. Therapeutic Effects:
Bactericidal action against susceptible
bacteria. Spectrum: Active against many
strains of gram-positive aerobic pathogens
including: Streptococcus pneumoniae,
Staphylococcus aureus, Group A beta-
hemolytic streptococci, Nocardia,
Enterococcus. Has activity against many
aerobic gram-negative pathogens, such as:
Acinetobacter, Enterobacter, Klebsiella
pneumoniae, Escherichia coli, Proteus
mirabilis,Shigella, Xanthomonas maltophilia,
Haemophilus influenzae, including
ampicillin-resistant strains. P. jirovecii. Not
active against Pseudomonas aeruginosa.
Pharmacokinetics:
Absorption: Well absorbed from the GI
tract.
Distribution: Widely distributed. Crosses
the blood-brain barrier and placenta and
enters breast milk.
Metabolism and Excretion: Some
metabolism by the liver (20%); remainder
excreted unchanged by the kidneys.
Half-life: Trimethoprim—6– 11 hr;
sulfamethoxazole—9– 12 hr, both prolonged
in renal failure. Onset: PO rapid IV rapid
Peak: PO 2–4 hr IV end of infusion
Duration: PO 6–12 hr IV 6–12 hr
Drug-Drug and Drug-Food Interactions:
Drug-Drug: May increase half-life, decrease
clearance, and exaggerate folic acid
deficiency caused by phenytoin. May
increases effects of sulfonylureas,
pioglitazone, rosiglitazone, repaglinide,
phenytoin, digoxin, and warfarin
Indications: Treatment of: Bronchitis,
Shigella enteritis, Otitis media,
Pneumocystis jirovecii pneumonia (PCP),
Urinary tract infections, Traveler’s diarrhea.
Prevention of PCP in HIV-positive patients.
Unlabeled Use: Biliary tract infections,
osteomyelitis, burn and wound infections,
chlamydial infections, endocarditis,
gonorrhea, intra-abdominal infections,
nocardiosis, rheumatic fever prophylaxis,
sinusitis, eradication of meningococcal
carriers, prophylaxis of urinary tract
infections, and an alternative agent in the
treatment of chancroid. Prevention of
bacterial infections in immunosuppressed
patients.
Contraindications: Hypersensitivity to
sulfonamides or trimethoprim; History of
drug-induced immune thrombocytopenia
due to sulfonamides or trimethoprim;
Megaloblastic anemia secondary to folate
deficiency; Severe hepatic or renal
impairment; OB, Lactation, Pedi:
Pregnancy, lactation, or children 2 mo (can
cause kernicterus in neonates). Exception:
neonates born to HIV-infected mothers
(prophylaxis should be initiated at 4– 6
weeks of age).
Side Effects:
CV: hypotension. CNS: fatigue,
hallucinations, headache, insomnia, mental
depression, kernicterus in neonates. F and
E: hyperkalemia, hyponatremia. GI:
nausea, vomiting, diarrhea, stomatitis,
hepatitis, cholestatic jaundice, pancreatitis.
GU: crystalluria. Derm: rash,
photosensitivity. Endo: hypoglycemia.
Hemat: hemolytic anemia, leukopenia,
megaloblastic anemia, thrombocytopenia.
Local: phlebitis at IV site. Misc: fever.
Adverse Reaction:
GI: PSEUDOMEMBRANOUS COLITIS,
HEPATIC NECROSIS Derm: ERYTHEMA
MULTIFORME, STEVENS-JOHNSON
SYNDROME, TOXIC EPIDERMAL
NECROLYSIS Hemat:
AGRANULOCYTOSIS, APLASTIC ANEMIA
Nursing Responsibilities:
Assessment:
● Assess for infection (vital signs;
appearance of wound, sputum, urine,
and stool; WBC) at beginning of and
during therapy.
● Obtain specimens for culture and
sensitivity before initiating therapy. First
dose may be given before receiving
results.
● Inspect iv site frequently. Phlebitis is
common.
● Assess patient for allergy to
sulfonamides.
● Monitor intake and output ratios. Fluid
intake should be sufficient to maintain a
urine output of at least 1200– 1500 ml
daily to prevent crystalluria and stone
formation.
Diagnosis:
 Risk for infection (indications) (side
effects)
Planning:
 Pt. Will be able to have resolution of
signs and symptoms of infection.
Implementation:
 Medication should be administered
around the clock.
Page | 150
 Direct iv: reconstitute to a 10% solution
by adding 10 ml of sterile water for
injection or d5w to each 1 g. Do not use
preparations containing benzyl alcohol in
neonates.concentration: final
concentration should not exceed 100
mg/ml. Rate: inject slowly over at least 1
min
Evaluation:
 Assess daily for signs of bone marrow
depression (petechiae, sore throat,
fatigue, unusual bleeding, bruising).
Patients who have impaired liver or renal
function, infants, children, and the elderly
are at the greatest risk of developing
adverse effects.
 Monitor therapeutic blood levels
periodically during therapy. Timing of
blood levels is important in interpreting
results. Draw blood for peak levels 1 hr
after IM injection and 30 min after a 30-
min IV infusion is completed.Trough
levels should be drawn just before next
dose. Peak level range 20–30 mcg/mL;
trough level 10 mcg/mL.
Classification: URINARY
ANTISEPTICS
Brand Name: Furadantin,
Macrodantin, Macrobid
Generic Name: Nitrofurantoin
Recommended Dosage, Route, and
Frequency:
PO (Adults): Treatment of active infection—
50– 100 mg q 6– 8 hr or 100 mg q 12 hr as
extended-release product. Chronic
suppression—50– 100 mg single evening
dose.
PO (Children 1 mo): Treatment of active
infection—5– 7 mg/kg/day divided q 6 hr;
maximum dose: 400 mg/day. Chronic
suppression—1– 2 mg/kg/day as a single
dose at bedtime; maximum dose: 100
mg/day (unlabeled).
Drug Action: Interferes with bacterial
enzymes. Therapeutic Effects: Bactericidal
or bacteriostatic action against susceptible
organisms. Spectrum: Many gram-negative
and some gram-positive organisms,
specifically: Citrobacter, Corynebacterium,
Enterobacter, Escherichia coli, Klebsiella,
Neisseria, Salmonella, Shigella,
Staphylococcus aureus, Staphylococcus
epidermidis, Enterococcus.
Pharmacokinetics:
Absorption: Readily absorbed after oral
administration. Absorption is slower but
more complete with macrocrystals
(Macrodantin).
Distribution: Crosses placenta; enters
breast milk.
Metabolism and Excretion: Partially
metabolized by the liver; 30– 50% excreted
unchanged by the kidneys.
Half-life: 20 min (increase in renal
impairment). Onset: unknown Peak: 30 min
Duration: 6–12 hr
Drug-Drug and Drug-Food Interactions:
Drug-Drug: Probenecid prevents high
urinary concentrations; may decrease
effectiveness. Antacids may decrease
absorption. Increase risk of neurotoxicity
with neurotoxic drugs. Increase the risk of
hepatotoxicity with hepatotoxic drugs.
Increase risk of pneumonitis with drugs
having pulmonary toxicity.
Indications: Prevention and treatment of
urinary tract infections caused by
susceptible organisms; not effective in
systemic bacterial infections.
Contraindications: Hypersensitivity;
Hypersensitivity to parabens (suspension);
Oliguria, anuria, or significant renal
impairment (CCr 60 mL/min); History of
cholestatic jaundice or hepatic impairment
with previous use of nitrofurantoin;
Pregnancy near term and infants 1 mo
Side Effects:
CNS: dizziness, drowsiness, headache.
EENT: nystagmus. CV: chest pain. GI:
anorexia, nausea, vomiting, abdominal pain,
diarrhea. GU: rust/brown discoloration of
urine. Derm: photosensitivity. Hemat:
blood dyscrasias, hemolytic anemia. Neuro:
peripheral neuropathy. Misc:
hypersensitivity reactions.
Adverse Reaction:
Resp: PNEUMONITIS, PULMONARY
FIBROSIS GI: HEPATOTOXICITY,
PSEUDOMEMBRANOUS COLITIS
Nursing Responsibilities:
Assessment:
● Assess for signs and symptoms of
urinary tract infection (frequency,
urgency, pain, and burning on urination;
fever; cloudy or foul-smelling urine)
before and periodically during therapy.
● Obtain specimens for culture and
sensitivity before and during drug
administration.
Page | 151
● Monitor intake and output ratios. Report
significant discrepancies in totals.
● Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to health care
professional promptly as a sign of
pseudomembranous colitis. May begin
up to several weeks following cessation
of therapy.
● Assess for signs and symptoms of
pulmonary reactions periodically during
therapy. Acute reactions (fever, chills,
cough, chest pain, dyspnea, pulmonary
infiltration with consolidation or pleural
effusion on x-ray, eosinophilia) usually
occur within first week of treatment and
resolve when therapy is discontinued.
Chronic reactions (malaise, dyspnea on
exertion, cough, altered pulmonary
function) may indicate pneumonitis or
pulmonary fibrosis and are more
common in patients taking nitrofurantoin
for 6 mo or longer.
● Lab Test Considerations: Monitor CBC
routinely with patients on prolonged
therapy.
Diagnosis:
● Risk for infection (Indications)
Planning/Implementation:
● PO: Administer with food or milk to
minimize GI irritation, to delay and
increase absorption, to increase peak
concentration, and to prolong duration of
therapeutic concentration in the urine.
● Do not crush tablets or open capsules.
● Administer liquid preparations with
calibrated measuring device. Shake well
before administration. Oral suspension
may be mixed with water, milk, fruit
juices, or infant formula. Rinse mouth
with water after administration of oral
suspension to avoid staining teeth.
Evaluation:
● Resolution of the signs and symptoms of
infection. Therapy should be continued
for a minimum of 7 days and for at least 3
days after the urine has become sterile.
● Decrease in the frequency of infections in
chronic suppressive therapy
Classification: ANTITUBERCULARS
(FIRST LINE)
Brand Name: Isotamine
Generic Name: Isoniazid
Recommended Dosage, Route, and
Frequency:
Treatment of Active Tuberculosis
Adult: PO/IM 5 mg/kg (max: 300 mg/d)
Child: PO/IM 10–20 mg/kg (max: 300–500
mg/d)
Preventive Therapy
Adult: PO 300 mg/d
Child: PO 10 mg/kg up to 300 mg/d or 15
mg/kg 3 times/wk
Drug Action:
Inhibits mycobacterial cell wall synthesis and
interferes with metabolism.
Therapeutic Effects: Bacteriostatic or
bactericidal action against susceptible
mycobacteria.
Pharmacokinetics:
Absorption: Well absorbed the following
PO/IM administration.
Distribution: Widely distributed; readily
crosses the blood-brain barrier. Crosses the
placenta; enters breast milk in
concentrations equal to plasma. Protein
Binding: 10– 15%.
Metabolism and Excretion: 50%
metabolized by the liver by N-
acetyltransferase (rate of acetylation is
genetically determined [slow acetylators
have increased isoniazid levels and
increased risk of toxicity; fast acetylators
have decrease isoniazid levels and increase
the risk for treatment failure]); 50% excreted
unchanged by the kidneys.
Half-life: 1– 4 hr in patients with normal
renal and hepatic function; 0.5– 1.6 hr in fast
acetylators; 2– 5 hr in slow acetylators.
Drug-Drug and Drug-Food Interactions:
Drug-Drug: Additive CNS toxicity with other
antitubercular. BCG vaccine may not be
effective during isoniazid therapy. Isoniazid
inhibits the metabolism of phenytoin.
Aluminum-containing antacids may
decrease absorption. Psychotic reactions
and coordination difficulties may result with
disulfiram. Concurrent administration of
pyridoxine may prevent neuropathy.
Increase risk of hepatotoxicity with other
hepatotoxic agents including alcohol,
acetaminophen and rifampin. Isoniazid may
decrease blood levels and the effectiveness
of ketoconazole. Concurrent use with
carbamazepine blood levels and the risk of
hepatotoxicity. May decrease effectiveness
of clopidogrel (avoid concurrent use).
Drug-Food: Severe reactions may occur
with ingestion of foods containing high
concentrations of tyramine
Indications: First-line therapy of active
tuberculosis, in combination with other
agents. Prevention of tuberculosis in
patients exposed to active disease (alone).
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Contraindications: Hypersensitivity; Acute
liver disease; previous hepatitis from
isoniazid.
Side Effects:
CNS: psychosis, seizures. EENT: visual
disturbances. Nausea, vomiting. Derm:
rashes. Endo: gynecomastia. Hemat: blood
dyscrasias. Misc: fever.
Adverse Reaction:
GI: Drug-induces hepatitis Neuro:
Peripheral neuropathy
Nursing Responsibilities:
Assessment:
● Mycobacterial studies and susceptibility
tests should be performed prior to and
periodically throughout therapy to detect
possible resistance. About 50% to 65%
of Caucasians, Black, South Indians and
Mexicans are slow acetylators at risk for
toxicity, while 80 to 90% of Eskimos,
Japanese, and Chinese are rapid
acetylators at risk for decreased levels
and treatment failure.
● Lab Test Considerations: Hepatic
function should be evaluated prior to and
monthly throughout therapy. Increased
AST, ALT, and serum bilirubin may
indicate drug-induced hepatitis. Black
and Hispanic women, postpartal women,
and patients 50 yr are at highest risk. The
risk is lower in children; therefore, liver
function tests are usually ordered less
frequently for children.
● Toxicity and Overdose: If isoniazid
overdosage occurs, treatment with
pyridoxine (vitamin B) is instituted.
Potential Nursing Diagnoses:
● Risk for infection (Indications)
● Noncompliance (Patient/Family
Teaching)
Implementation:
● PO: May be administered with food or
antacids if GI irritation occurs, although
antacids containing aluminum should not
be taken within 1 hr of administration.
● IM: Medication may cause discomfort
at the injection site. Massage site after
administration and rotate injection sites.
● Solution may form crystals at low
temperatures; crystals will re dissolve
upon warming to room temperature.
Evaluation/Desired Outcomes
● Resolution of signs and symptoms of
tuberculosis.
● Negative sputum cultures.
● Prevention of activation of tuberculosis
in persons known to have been exposed.
Classification: FLUOROQUINILONES
(SECOND-LINE ANTITUBERCULAR
DRUGS)
Brand Name: Levaquin
Generic Name: Levofloxacin
Recommended Dosage, Route, and
Frequency:
PO, IV (Adults): Most infections 250– 750
mg q 24 hr; Inhalational anthrax (post-
exposure) 500 mg daily for 60 days.
PO, IV (Children>50 kg): Inhalational
anthrax (post-exposure) 500 mg daily for 60
days; Plague 500 mg daily for 10– 14 days.
PO, IV (Children 50 kg and 6 mo.):
Inhalational anthrax (post-exposure) 8
mg/kg (max: 250 mg/dose) every 12 hr for
60 days. Plague 8 mg/kg (max: 250
mg/dose) every 12 hr for 10– 14 days; Other
infections 10 mg/kg/dose every 24 hr (max:
500 mg/dose).
Renal Impairment
PO, IV (Adults): Normal renal function
dosing of 750 mg/day: CCr 20– 49 mL/ min
750 mg q 48 hr; CCr 10– 19 mL/min 750 mg
initially, then 500 mg q 48 hr; Normal renal
function dosing of 500 mg/day: CCr 20– 49
mL/min 500 mg initially then 250 mg q 24 hr;
CCr 10– 19 mL/min 500 mg initially then 250
mg q 48 hr. Normal renal function dosing of
250 mg/day: CCr 10– 19 mL/min 250 mg q
48 hr.
Drug Action:
Inhibits bacterial DNA synthesis by inhibiting
DNA gyrase enzyme.
Therapeutic Effects: Death of susceptible
bacteria.
Spectrum: Active against gram-positive
pathogens, including: Staphylococcus
aureus, Staphylococcus epidermidis,
Staphylococcus saprophyticus,
Streptococcus pyogenes, Streptococcus
pneumoniae, Enterococcus faecalis, and
Bacillus anthracis. Gram-negative spectrum
notable for activity against: Escherichia coli,
Klebsiella pneumoniae, Enterobacter
cloacae, Proteus mirabilis, Pseudomonas
aeruginosa, Serratia marcescens,
Haemophilusinfluenzae, Moraxella
catarrhalis. Additional spectrum includes:
Chlamydophila pneumoniae, Legionella
pneumoniae, Mycoplasma pneumoniae, and
Yersinia pestis
PHARMACOKINETICS: Absorption: Well
absorbed (99%) after oral administration; IV
administration results in complete
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bioavailability. Distribution: Widely
distributed. High tissue and urinary levels
are achieved. Appears to cross the placenta.
Metabolism and Excretion: 87% excreted
unchanged in urine, small amounts
metabolized. Half-life: 8 hr
Drug-Drug and Drug-Food Interactions:
Drug-Drug: Concurrent use of amiodarone,
disopyramide, procainamide, quinidine,
dofetilide, or sotalol increase risk of torsade
de pointes in susceptible individuals (avoid
concurrent use). Administration with
antacids, iron salts, bismuth subsalicylate,
sucralfate, and zinc salts decrease
absorption. May increase the effects of
warfarin. Serum levels may be decrease by
antineoplastic agents. Cimetidine may
interfere with elimination. Probenecid
preanal elimination. May increase the risk of
nephrotoxicity from cyclosporine. Concurrent
therapy with corticosteroids may increase
the risk of tendon rupture.
Drug-Food: Absorption is impaired by
concurrent enteral feeding (because of
metal cations).
Indications: Treatment of the following
bacterial infections: Urinary tract infections,
including cystitis, pyelonephritis, and
prostatitis, Respiratory tract infections,
including acute sinusitis, acute
exacerbations of chronic bronchitis,
community-acquired pneumonia, and
nosocomial pneumonia, Uncomplicated and
complicated skin and skin structure
infections. Post-exposure treatment of
inhalational anthrax. Treatment and
prophylaxis of plague.
Contraindications: Hypersensitivity (cross-
sensitivity within class may exist); QTc
interval prolongation; Uncorrected
hypokalemia or hypomagnesemia;
Concurrent use of Class IA antiarrhythmics
(disopyramide, quinidine, procainamide) or
Class III antiarrhythmics (amiodarone,
sotalol) (increased risk of QTc interval
prolongation and torsade de pointes);
History of myasthenia gravis (may worsen
symptoms including muscle weakness and
breathing problems);OB: Pregnancy;
Lactation: Not recommended.
Side Effects:
CNS: agitation, anxiety, confusion,
depression, dizziness, drowsiness,
hallucinations, headache, insomnia,
nightmares, paranoia, tremor. GI: nausea,
abdominal pain, diarrhea, vomiting. GU:
vaginitis. Derm: Photosensitivity, rash.
Endo: hyperglycemia, hypoglycemia. Local:
phlebitis at IV site. Neuro: peripheral
neuropathy. MS: arthralgia, tendinitis,
tendon rupture. Misc: hypersensitivity
reactions.
Adverse Reaction:
CNS: ELEVATED INTRACRANIAL
PRESSURE (including pseudotumor
cerebri), SEIZURES. CV: TORSADE DE
POINTES, QT interval prolongation. GI:
HEPATOTOXICITY,
PSEUDOMEMBRANOUS COLITIS. DERM:
STEVENS-JOHNSON SYNDROME. Misc:
ANAPHYLAXIS
Nursing Responsibilities:
Assessment:
● Assess for infection (vital signs;
appearance of wound, sputum, urine,
and stool; WBC; urinalysis; frequency
and urgency of urination; cloudy or foul-
smelling urine) at the beginning of and
during therapy.
● Obtain specimens for culture and
sensitivity before initiating a therapy. First
dose may be given before receiving
results.
● Assess for rash periodically during
therapy. May cause Stevens-Johnson
syndrome. Discontinue therapy if severe
or if accompanied with fever, general
malaise, fatigue, muscle or joint aches,
blisters, oral lesions, conjunctivitis,
hepatitis and/or eosinophilia.
● Assess for signs and symptoms of
peripheral neuropathy (pain, burning,
tingling, numbness, and/or weakness or
other alterations of sensation including
light touch, pain, temperature, position
sense, and vibratory sensation)
periodically during therapy. Symptoms
may be irreversible; discontinue
levofloxacin if symptoms occur.
Potential Nursing Diagnoses:
● Risk for infection (Patient/Family
Teaching
Implementation:
● Do not confuse levofloxacin with
levetiracetam.
● PO: May be administered without
regard to meals. Products or foods
containing calcium, magnesium,
aluminum, iron, zinc should not be
ingested for 4 hr before and 2 hr after
administration.
IV Administration:
>pH: 3.8– 5.8.
>Intermittent Infusion: Diluent: Dilute to a
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 with 0.9% NaCl, D5W, D5/0.9% NaCl,
D5/0.45% NaCl, or D5/LR.
Concentration: 5 mg/mL. Also available
in premixed bottles and flexible
containers with D5W, which need no
further dilution. Discard unused solution.
Diluted solution is stable for 72 hr at
room temperature and 14 days if
refrigerated. Rate: Administer by infusion
over at least 60 min for 250–mg or 500–
mg doses and over 90 min for 750–mg
dose. Avoid rapid bolus injection to
prevent hypotension.
>Y-Site Compatibility & Y-Site
Incompatibility:
Evaluation/Desired Outcomes
● Resolution of the signs and symptoms
of bacterial infection. Time for complete
resolution depends on an organism and
site of infection.
● Avoidance of signs and symptoms of
inhalational anthrax (postexposure
treatment).
● Prevention and treatment of plague.
Classification: MULTIBACILLARY
LEPROSY DRUGS
Brand Name: Rifadin, Rofact
Generic Name: Rifampin
Recommended Dosage, Route, and
Frequency:
Tuberculosis
PO, IV (Adults): 600 mg/day or 10
mg/kg/day (up to 600 mg/day) single dose;
may also be given twice weekly.
PO, IV (Children and Infants): 10– 20
mg/kg/day single dose or divided q 12 h (not
to exceed 600 mg/day); may also be given
twice weekly.
Asymptomatic Carriers of
Meningococcus
PO, IV (Adults): 600 mg q 12 hr for 2 days.
PO, IV (Children 1 mo): 10 mg/kg q 12 hr for
2 days (max: 600 mg/dose).
PO (Infants 1 mo): 5 mg/kg q 12 hr for 2
days.
H. influenzae Prophylaxis
PO (Adults): 600 mg/day for 4 days. PO
(Children): 20 mg/kg/day for 4 days (max:
600 mg/dose).
PO (Neonates): 10 mg/kg/day for 4 days.
Synergy for S.aureus infections
PO (Adults): 300– 600 mg BID. PO
(Children and Neonates): 5– 20 mg/kg/day
divided q 12 h (max: 600 mg/ dose)
Drug Action:
Inhibits RNA synthesis by blocking RNA
transcription in susceptible organisms.
Therapeutic Effects: Bactericidal action
against susceptible organisms.
PHARMACOKINETICS:
Absorption: Well absorbed following oral
administration.
Distribution: Widely distributed; enters
CSF. Crosses placenta; enters breast milk.
Protein Binding: 80%. Metabolism and
Excretion: Mostly metabolized by the liver;
60% eliminated in feces via biliary
elimination.
Half-life: 3 hr.
Drug-Drug and Drug-Food Interactions:
Drug-Drug: Increase risk of hepatotoxicity
with ritonavir-boosted saquinavir; concurrent
use contraindicated. Significantly decrease
blood levels of atazanavir, darunavir, fosam
decrease renavir, saquinavir, and tipranavir;
concurrent use contraindicated. Increase
risk of hepatotoxicity with other hepatotoxic
agents, including alcohol, ketoconazole,
isoniazid, pyrazinamide (concurrent use with
pyrazinamide may result in potentially fatal
hepatotoxicity and should be avoided).
Significantly decrease blood levels of
delavirdine, indinavir, and nelfinavir.
Rifampin stimulates liver enzymes, which
may increase metabolism and decrease
effectiveness of other drugs, including
ritonavir, nevirapine, and efavirenz (dose
adjustment may be necessary),
ciprofloxacin, clarithromycin, corticosteroids,
cyclosporine, diazepam, diltiazem,
disopyramide, doxycycline, levothyroxine,
methadone, c, quinidine, opioid analgesics,
oral hypoglycemic agents, warfarin,
estrogens, phenytoin, phenobarbital,
tacrolimus, verapamil, fluconazole,
ketoconazole, itraconazole, quinidine,
theophylline, zidovudine, chloramphenicol,
and hormonal contraceptive agents.
Indications: Active tuberculosis (with other
agents). Elimination of meningococcal
carriers. Unlabeled Use: Prevention of
disease caused by Hemophilus influenzae
type B in close contacts. Synergy with other
antimicrobial agents for S.aureus infections.
Contraindications: Hypersensitivity;
Concurrent use of atazanavir, darunavir,
fosamprenavir, saquinavir, tipranavir, or
ritonavir-boosted saquinavir.
Side Effects:
CNS: ataxia, confusion, drowsiness, fatigue,
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headache, weakness. Derm: rash, pruritus.
EENT: red discoloration of the tears. GI:
abdominal pain, diarrhea, flatulence,
heartburn, nausea, vomiting, increase liver
enzymes, red discoloration of saliva. GU:
red discoloration of urine. Hemat: hemolytic
anemia, thrombocytopenia. MS: arthralgia,
muscle weakness, myalgia. Misc: flu-like
syndrome.
Adverse Reaction: Unknown
Nursing Responsibilities:
Assessment:
● Perform mycobacterial studies and
susceptibility tests prior to and
periodically during therapy to detect
possible resistance.
● Assess lung sounds and character and
amount of sputum periodically during
therapy.
● Lab Test Considerations: Evaluate
renal function, CBC, and urinalysis
periodically and during therapy.
● Monitor hepatic function at least
monthly during therapy. May cause
increase BUN, AST, ALT, and serum
alkaline phosphatase, bilirubin, and uric
acid concentrations.
● May cause false-positive direct
Coombs’ test results. May interfere with
folic acid and vitamin B assays. ● May
interfere with dexamethasone
suppression test results; discontinue
rifampin 15 days prior to test.
● May interfere with methods for
determining serum folate and vitamin B
levels and with urine tests based on color
reaction.
● May delay hepatic uptake and
excretion of sulfobromophthalein (SBP)
during SBP uptake and excretion tests;
perform the test prior to a daily dose of
rifampin.
Potential Nursing Diagnoses:
● Risk for infection (Indications)
● Noncompliance (Patient/Family
Teaching)
PLANNING:
 Pt. will be able to have resolution of signs
and symptoms of infection.
Implementation:
● Do not confuse rifampin with rifabutin.
● PO: Administer medication on an
empty stomach at least 1 hr before or 2
hr after meals with a full glass (240 mL)
of water. If GI irritation becomes a
problem, may be administered with food.
Antacids may also be taken 1 hr prior to
administration. Capsules may be opened
and contents mixed with applesauce or
jelly for patients with difficulty swallowing.
● Pharmacist can compound a syrup for
patients unable to swallow solids.
Evaluation/Desired Outcomes:
● Decreased fever and night sweats.
● Diminished cough and sputum
production.
● Negative sputum cultures.
● Increased appetite.
● Weight gain.
● Reduced fatigue.
● Sense of well-being in patients with
tuberculosis.
● Prevention of meningococcal
meningitis.
● Prevention of H. influenzae type B
infection. Prophylactic course is usually
short term.
Classification: PAUCIBACILLARY
LEPROSY DRUGS
Brand Name: Aczone, Avlosulfon
Generic Name: Dapsone
Recommended Dosage, Route, and
Frequency:
Leprosy
PO (Adults): 50– 100 mg/day for 3– 10 yrs.
PO (Children): 1– 2 mg/kg/day, up to 100
mg/day.
Dermatitis Herpetiformis
PO (Adults): Initiate therapy with 50 mg/day,
up to 300 mg/day may be required.
Acne Vulgaris Topical
(Adults and Children 12 yrs): Apply a small
amount twice daily.
Pneumocystis jirovecii Pneumonia
PO (Adults): Prophylaxis—100 mg/day;
Treatment—100 mg/day (in combination
with trimethoprim) for 21 days.
PO (Children 1 mo): Prophylaxis—2
mg/kg/day (up to 100 mg/day) once daily, or
4 mg/kg once weekly (up to 200 mg/dose).
Drug Action:
Interferes with folate synthesis in susceptible
organisms.
Therapeutic Effects: Bacteriostatic action.
Pharmacokinetics:
Absorption: Slowly absorbed (70– 80%)
following an oral administration; acidic
environment promotes absorption.
Distribution: Widely distributed; crosses the
placenta and enters breast milk in significant
concentrations.
Metabolism and Excretion: Mostly
metabolized by the liver to monoacetyl
Page | 156
dapsone (MADDS), its major metabolite,
which is then metabolized back to dapsone.
Half-life: 10– 50 hr.
Drug-Drug and Drug-Food Interactions:
Concurrent administration with didanosine or
antacids may decrease absorption of
dapsone (separate administration times by 2
hr). Blood levels may be increase
byamiodarone, fluconazole, ketoconazole,
itraconazole, clarithromycin, erythromycin,
quinidine, verapamil, or diltiazem. Blood
levels may be a decrease by rifampin,
phenytoin, phenobarbital, or carbamazepine.
Coadministration with trimethoprim results in
increased levels of both agents. Concurrent
use with agents causing blood dyscrasias or
hemolytic anemia may increase the risk of
these adverse effects.
Indications: Treatment of leprosy (in
combination with other agents). Treatment
of dermatitis herpetiformis. Treatment of
acne vulgaris (topical). Unlabeled Use:
Prevention (as monotherapy) and treatment
of Pneumocystis jirovecii pneumonia (with
trimethoprim or other agents).
Contraindications: Hypersensitivity (cross-
sensitivity with sulfonamides may occur);
Lactation
Side Effects:
CNS: headache, insomnia, mood changes,
tonic-clonic movements (topical), vertigo.
EENT: blurred vision, tinnitus, pharyngitis
(topical). GI: abdominal pain, nausea,
pancreatitis, vomiting. Derm: exfoliative
dermatitis, hypersensitivity reactions
including erythema nodosum leprosum,
photosensitivity, systemic lupus
erythematosus. Hemat: hemolytic anemia,
reticulocytosis. Neuro: peripheral
neuropathy.
Adverse Reaction:
GI: Hepatotoxicity. Derm: Stevens-Johnson
Syndrome. Hemat: Agranulocytosis,
Methemoglobinemia
Nursing Responsibilities:
Assessment:
● Leprosy: Assess skin lesions prior to
and periodically throughout therapy.
● Assess the skin for new or toxic
dermatologic reactions during therapy.
Unless dermatologic reaction is leprosy
reactional state, dapsone should be
discontinued promptly. Large doses of
corticosteroids should be given if severe
reactions or neuritis occurs.
● Pneumocystis jirovecii pneumonia:
Assess the patient for infection (vital
signs, sputum, WBC) and monitor
respiratory status (rate, character, lung
sounds, dyspnea, sputum) at beginning
of and throughout therapy.
● Obtain specimens for culture and
sensitivity prior to initiating therapy. First
dose may be given before receiving
results.
● Monitor patients for hemolysis. Screen
patients at higher risk for G6PD
deficiency (patients of African American
or Mediterranean ancestry) prior to oral
therapy. If hemolysis occurs, discontinue
and do not restart dapsone.
Potential Nursing Diagnoses:
● Risk for infection (Indications)
● Deficient knowledge, related to
medication regimen (Patient/Family
Teaching)
● Noncompliance (Patient/Family
Teaching)
Implementation:
● PO: May be taken with food if GI upset
occurs.
● Do not administer concurrently with
alkaline drugs (e.g. antacids,
didanosine); separate administration
times by 2 hrs.
● Topical: Apply to clean, dry skin and
rub in thoroughly. Wash hands after
application.
Evaluation/Desired Outcomes
● Healing of skin lesions in patients with
leprosy or dermatitis. May require 6 mo–
3 yr or more in patients with
indeterminate and tuberculoid leprosy, 2–
10 yr in borderline (dimorphous) leprosy,
and 2 yr to life in lepromatous leprosy.
● Prevention and resolution of symptoms
of Pneumocystis jirovecii pneumonia.
● Decrease in acne lesions. If no
improvement after 12 weeks, reassess
treatment
Classification: SINGLE-LESION
PAUBACILLARY LEPROSY DRUGS
Brand Name: Floxin
Generic Name: Ofloxacin
Recommended Dosage, Route, and
Frequency:
PO (Adults): Most infections 400 mg q 12 hr
(for 3– 10 days depending infection).
Urethritis/cervicitis 300 mg q 12 hr (for 7
days). Prostatitis 300 mg q 12 hr (for 6
Page | 157
weeks). Urinary tract infections 200 mg q 12
hr. Gonorrhea 400 mg single dose.
Renal Impairment
PO (Adults): CCr 20– 50 mL/min 100% of
the usual dose q 24 hr; CCr 20 mL/ min 50%
of the usual dose q 24 hr.
Otic (Adults and Children 6 mo): Otitis
externa 6 mo to 13 yr: 5 drops instilled into
affected ear once daily for 7 days; Otitis
externa 13 yr 10 drops instilled into the
affected ear once daily for 7 days. Acute
otitis media in patients 1– 12 yr old with
tympanostomy tubes: 5 drops instilled into
the affected ear twice daily for 10 days.
Chronic suppurative otitis media with
perforated tympanic membranes in patients
12 yr: 10 drops instilled into the affected ear
twice daily for 14 days.
Drug Action:
Inhibits bacterial DNA synthesis by inhibiting
DNA gyrase enzyme.
Therapeutic Effects: Death of susceptible
bacteria.
Pharmacokinetics:
Absorption: Well absorbed (98%) following
oral administration.
Distribution: Widely distributed. High tissue
and urinary levels are achieved. Appears to
cross the placenta; enters breast milk.
Metabolism and Excretion: 70– 80%
excreted unchanged by the kidneys.
Half-life: 5– 7 hr.
Interactions:
Drug-Drug: Concurrent use of amiodarone,
disopyramide, procainamide, dofetilide,
quinidine, or sotalol increase the risk of
potentially dangerous arrhythmias in
susceptible individuals (avoid concurrent
use). Increase serum theophylline levels and
may lead to toxicity. Administration with
antacids, iron salts, bismuth subsalicylate,
sucralfate, and zinc salts decrease
absorption. May increase the effects of
warfarin. Serum levels may be a decrease
by antineoplastic agents. Cimetidine may
interfere with elimination. Probenecid
decrease renal elimination. May increase
the risk of nephrotoxicity from cyclosporine.
Concurrent corticosteroid therapy may
increase the risk of tendon rupture.
Drug-Food: Absorption is impaired by
concurrent enteral feeding (because of
metal cations). Absorption of ofloxacin is the
decrease by foods and/or dairy products.
Indications: PO: Treatment of the following
bacterial infections: Urinary tract and
gynecologic infections, including cystitis,
gonorrhea, nongonococcal urethritis and
cervicitis, acute pelvic inflammatory disease,
and prostatitis, Respiratory tract infections,
including acute exacerbations of chronic
bronchitis, and community-acquired
pneumonia, Uncomplicated skin and skin
structure infections. Otic Otitis externa or
otitis media.
Contraindications: Hypersensitivity (cross-
sensitivity within class may exist); QTc
interval prolongation; Uncorrected
hypokalemia or hypomagnesemia;
Concurrent use of Class IA antiarrhythmics
(disopyramide, quinidine, procainamide) or
Class III antiarrhythmics (amiodarone,
sotalol) (increase risk of QTc interval
prolongation and torsade de pointes);
History of myasthenia gravis (may worsen
symptoms including muscle weakness and
breathing problems); Pedi: Children (safety
and effectiveness not established);OB:
Pregnancy.
Side Effects:
CNS: dizziness, drowsiness, headache,
insomnia, agitation, confusion, peripheral
neuropathy.
CV: QT interval prolongation.
GI: abdominal pain, diarrhea, nausea,
vomiting.
GU: vaginitis. Derm: photosensitivity, rash.
Endo: hyperglycemia, hypoglycemia.
MS: tendinitis, tendon rupture.
Neuro: peripheral neuropathy.
Misc: hypersensitivity reactions
Adverse Reaction:
CNS: SEIZURES.
CV: TORSADE DE POINTES.
GI: PSEUDOMEMBRANOUS COLITIS.
Derm: STEVENS-JOHNSON SYNDROME.
Misc: ANAPHYLAXIS.
Nursing Responsibilities:
Assessment:
● Observe patient for signs and
symptoms of anaphylaxis (rash, pruritus,
laryngeal edema, wheezing). Discontinue
drug and notify physician or other health
care professional immediately if these
problems occur. Keep epinephrine, an
antihistamine, and resuscitation
equipment close by in case of an
anaphylactic reaction.
● Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to health care
professional promptly as a sign of
pseudomembranous colitis. May begin
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 up to several weeks following cessation
of therapy.
● Assess for a rash periodically during
therapy. May cause Stevens-Johnson
syndrome. Discontinue therapy if severe
or if accompanied with fever, general
malaise, fatigue, muscle or joint aches,
blisters, oral lesions, conjunctivitis,
hepatitis and/or eosinophilia.
Potential Nursing Diagnoses:
● Risk for infection (Indications)
Implementation:
● PO: Administer on an empty stomach 1
hr before or 2 hr after meals, with a full
glass of water. Products or foods
containing calcium, magnesium,
aluminum, iron, or zinc should not be
ingested for 4 hr before and 2 hr after
administration.
● Otic: Warm solution by holding a bottle
in hand for 1– 2 min to avoid dizziness
from instillation of cold solution. Patient
should lie with the affected ear upward,
before instilling drops. Maintain position
for 5 minutes. Repeat for opposite ear, if
necessary. For otitis media: Pump the
tragus 4 times by pushing inward to
facilitate penetration into the middle ear
after instillation.
Evaluation/Desired Outcomes:
● Resolution of the signs and symptoms
of bacterial infection. Time for complete
resolution depends on the organism and
site of infection.
Drug Classification: RIFAMPIN-
RESISTANT LEPROSY DRUGS
(FIRST 6 MONTHS)
Brand Name: Dynacin, Minocin,
Solodyn
Generic Name: Minocycline
Recommended Dosage, Route, and
Frequency:
PO (Adults): 100– 200 mg initially, then 100
mg q 12 hr or 50 mg q 6 hr.
PO (Children 8 yr): 4 mg/kg initially, then 2
mg/kg q 12 hr.
PO (Adults and Children 12 yrs [Solodyn]):
126– 136 kg—135 mg once daily for 12 wks;
111– 125 kg—115 mg once daily for 12 wks;
97– 110 kg—105 mg once daily for 12 wks;
85– 96 kg—90 mg once daily for 12 wks;
72– 84 kg—80 mg once daily for 12 wks;
60– 71 kg—65 mg once daily for 12 wks;
50– 59 kg—55 mg once daily for 12 wks;
45– 49 kg—45 mg once daily for 12 wks.
Drug Action:
Inhibit bacterial protein synthesis at the level
of the 30S bacterial ribosome.
Therapeutic Effects: Bacteriostatic action
against susceptible bacteria.
Spectrum: Include activity against some
gram-positive pathogens: Bacillus anthracis,
Clostridium perfringens, Clostridium tetani,
Listeria monocytogenes, Nocardia,
Propionibacterium acnes, Actinomyces
israelii. Active against some gram-negative
pathogens: Haemophilus influenzae,
Legionella pneumophila, Yersinia
entercolitica, Yersinia pestis, Neisseria
gonorrhoeae, Neisseria meningitidis. Also
active against several other pathogens,
including: Mycoplasma, Treponema
pallidum, Chlamydia, Rickettsia.
Pharmacokinetics:
Absorption: Well absorbed from the GI
tract.
Distribution: Widely distributed, some CSF
and good bone penetration; crosses the
placenta and enters breast milk.
Metabolism and Excretion: 5– 20%
excreted unchanged by the urine; some
metabolism by the liver with enterohepatic
circulation and excretion in bile and feces.
Half-life: 11– 26 hr
Drug-Drug and Drug-Food Interactions:
Drug-Drug: May increase the effect of
warfarin. May decrease the effectiveness of
estrogen containing oral contraceptives.
Antacids, calcium, iron supplements, and
magnesium salts form insoluble compounds
(chelates) and decrease absorption of
tetracyclines. Sucralfate may bind to
tetracycline and prevent its absorption from
the GI tract. Cholestyramine or colestipol
decrease an oral absorption of tetracyclines.
Adsorbent anti-diarrheas may decrease
absorption.
Drug-Food: Calcium in foods or dairy
products decrease absorption by forming
insoluble compounds (chelates).
Indications: Treatment of various infections
caused by unusual organisms, including:
Mycoplasma, Chlamydia, Rickettsia.
Treatment of gonorrhea and syphilis in
penicillin allergic patients. Prevention of
exacerbations of chronic bronchitis.
Treatment of acne. Inflammatory lesions of
non-nodular acne vulgaris (Solodyn and
Ximino).
Contraindications: Hypersensitivity; Some
products contain alcohol or bisulfites and
should be avoided in patients with known
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hypersensitivity or intolerance;
Pedi: Children 8 yr (permanent staining of
teeth)
OB: Risk of permanent staining of teeth in
the infant if used during last half of
pregnancy
Lactation: Lactation. Use Cautiously in:
Cachectic or debilitated patients; Renal
impairment; Hepatic impairment;
Nephrogenic diabetes insipidus.
Side Effects:
CNS: benign intracranial hypertension
(increase risk in children), dizziness. EENT:
vestibular reactions. GI: diarrhea, nausea,
vomiting, esophagitis, pancreatitis. Derm:
photosensitivity, rash, pigmentation of skin
and mucous membranes. Endo: thyroid
disorders. Hemat: blood dyscrasias. MS:
lupus-like syndrome. Misc: hypersensitivity
reactions, superinfection.
Adverse Reaction:
GI: Hepatotoxicity, Pseudomembranous
Colitis. Derm: Drug Rash With Eosinophilia
And Systemic Symptoms Syndrome,
Erythema Multiforme, Stevens-Johnson
Syndrome, Toxic Epidermal Necrolysis
Nursing Responsibilities:
Assessment:
● Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to health care
professional promptly as a sign of
pseudomembranous colitis. May begin
up to several weeks following cessation
of therapy.
● Assess for rash periodically during
therapy. May cause Stevens-Johnson
syndrome or toxic epidermal necrolysis.
Discontinue therapy if severe or if
accompanied with fever, general malaise,
fatigue, muscle or joint aches, blisters,
oral lesions, conjunctivitis, hepatitis
and/or eosinophilia.
Potential Nursing Diagnoses:
● Risk for infection (Indications) (Side
Effects)
● Noncompliance (Patient/Family
Teaching)
Implementation:
● Do not confuse Dynacin with Dynacirc.
● May cause yellow-brown discoloration
and softening of teeth and bones if
administered prenatally or during early
childhood. Not recommended for children
under 8 yr of age or during pregnancy or
lactation. ● Solodyn product should only
be used to treat acne, not to treat
infections.
● PO: Administer around the clock. May
be taken with food or milk if GI irritation
occurs. Administer with a full glass of
liquid at least 1 hr before going to bed to
avoid esophageal ulceration. Swallow
extended-release tablets and capsules
(Solodyn) whole; do not open, crush,
break, or chew. Do not administer within
1– 3 hr of other medications.
● Avoid administration of calcium,
antacids, magnesium-containing
medications, sodium bicarbonate, or iron
supplements within 1– 3 hr of
minocycline.
Evaluation/Desired Outcomes:
● Resolution of the signs and symptoms
of infection. Length of time for complete
resolution depends on the organism and
site of infection.
● Decrease in acne lesions.
Classification: DRUGS FOR
MYCOBACTERIUM AVIUM COMPLEX
INFECTION
Brand Name: Zithromax, Zmax
Generic Name: Azithromycin
Recommended Dosage, Route, and
Frequency:
Most Respiratory and Skin Infections
PO (Adults): 500 mg on 1st day, then 250
mg/day for 4 more days (total dose of 1.5 g);
Acute bacterial sinusitis—500 mg once daily
for 3 days or single 2-g dose of extended-
release suspension (Zmax).
PO (Children 6 mo): Pneumonia/Pertussis—
10 mg/kg (not 500 m g/dose) on 1st day,
then 5 mg/kg (not 250 m g/dose) for 4 more
days. Pharyngitis/tonsillitis—12 mg/kg once
daily for 5 days (not 500 m g/dose); Acute
bacterial sinusitis—10 mg/kg/day for three
days.
PO (Neonates): Pertussis, treatment and
post-exposure prophylaxis—10 mg/ kg/dose
once daily for 5 days.
Otitis media
PO (Children 6 mo): 30 mg/kg single dose
(not 1500 mg/dose) or 10 mg/kg/ day as a
single dose (not 500 m g/dose) for 3 days or
10 mg/kg as a single dose (not 500 m
g/dose) on 1st day, then 5 mg/kg as a single
dose (not 250 m g/dose) daily for 4 more
days.
Acute bacterial exacerbations of chronic
bronchitis
PO (Adults): 500 mg on 1st day, then 250
mg/day for 4 more days (total dose of 1.5 g)
or 500 mg daily for 3 days.
Page | 160
Community-Acquired Pneumonia
IV, PO (Adults): More severe—500 mg IV q
24 hr for at least 2 doses, then 500 mg PO q
24 hr for a total of 7– 10 days; less severe—
500 mg PO, then 250 mg/day PO for 4 more
days or 2 g single dose as extended-release
suspension (Zmax).
PO (Children >6 mo): 10 mg/kg on 1st day,
then 5 mg/kg for 4 more days.
Pelvic Inflammatory Disease
IV, PO (Adults): 500 mg IV q 24 hr for 1– 2
days, then 250 mg PO q 24 hr for a total of 7
days.
Endocarditis Prophylaxis
PO (Adults): 500 mg 1 hr before procedure.
PO (Children): 15 mg/kg 1 hr before
procedure.
Nongonococcal Urethritis, Cervicitis,
Chancroid, Chlamydia
PO (Adults): Single 1-g dose.
PO (Children): Chancroid:Single 20-mg/kg
dose (not >1000 mg/dose). Urethritis or
cervicitis:Single 10-mg/kg dose (not 1000
mg/dose).
Gonorrhea
PO (Adults): Single 2-g dose.
Prevention of Disseminated MAC Infection
PO (Adults): 1.2 g once weekly (alone or
with rifabutin).
PO (Children): 5 mg/kg once daily (not 250
m g/dose) or 20 mg/kg (not 1200 mg/dose)
once weekly (alone or with rifabutin).
Cystic Fibrosis
PO (Children 6 yrs, weight 25 kg to 40 kg):
250 mg q MWF. 40 kg: 500 mg q MWF.
Drug Action:
Inhibits protein synthesis at the level of the
50S bacterial ribosome.
Therapeutic Effects: Bacteriostatic action
against susceptible bacteria.
Spectrum: Active against the following gram-
positive aerobic bacteria: Staphylococcus
aureus, Streptococcus pneumonias.
pyogenes(group A strep). Active against
these gram-negative aerobic bacteria:
Hemophilus influenzae, Moraxella
catarrhalis, Neisseria gonorrhoeae. Also
active against: Bordetella pertussis,
Mycoplasma, Legionella, Chlamydia
pneumoniae, Ureaplasma urealyticum,
Borrelia burgdorferi, M. avium. Not active
against methicillin-resistant S. aureus.
PHARMACOKINETICS:
Absorption: Rapidly absorbed (40%) after
oral administration. IV administration results
in complete bioavailability.
Distribution: Widely distributed to body
tissues and fluids. Intracellular and tissue
levels exceed those in serum; low CSF
levels. Protein Binding: 7– 51%.
Metabolism and Excretion: Mostly
excreted unchanged in bile; 4.5% excreted
unchanged in urine.
Half-life: 11– 14 hr after single dose; 2– 4
days after several doses; 59 hr after
extended release suspension.
Drug-Drug and Drug-Food Interactions:
Drug-Drug: Quinidine, procainamide,
dofetilide, sotalol, and amiodarone may
increase the risk of QT interval prolongation;
concurrent use should be avoided.
Aluminum- and magnesium-containing
antacids decrease peak levels. Nelfinavir
increase levels (monitor carefully);
azithromycin also decrease nelfinavir levels.
Efavirenz increase levels. May increase the
effects and risk of toxicity of warfarin and
zidovudine. Other macrolide anti- infectives
have been known to increase levels and
effects of digoxin, theophylline, ergotamine,
dihydroergotamine, triazolam,
carbamazepine, cyclosporine, tacrolimus,
and phenytoin; careful monitoring of
concurrent use is recommended.
Indications: Treatment of the following
infections due to susceptible organisms:
Upper respiratory tract infections, including
streptococcal pharyngitis, acute bacterial
exacerbations of chronic bronchitis and
tonsillitis, Lower respiratory tract infections,
including bronchitis and pneumonia, Acute
otitis media, Skin and skin structure
infections, Nongonococcal urethritis,
cervicitis, gonorrhea, and chancroid.
Prevention of disseminated Mycobacterium
avium complex (MAC) infection in patients
with advanced HIV infection. Extended-
release suspension (ZMax) Acute bacterial
sinusitis and community-acquired
pneumonia in adults. Unlabeled Use:
Prevention of bacterial endocarditis.
Treatment of cystic fibrosis lung disease.
Treatment and postexposure prophylaxis of
pertussis in infants.
Contraindications: Hypersensitivity to
azithromycin, erythromycin, or other
macrolide anti-infectives; History of
cholestatic jaundice or hepatic dysfunction
with prior use of azithromycin.; QT interval
prolongation, hypokalemia,
hypomagnesemia, or bradycardia.;
Concurrent use of quinidine, procainamide,
dofetilide, amiodarone, or sotalol.
Side Effects:
CNS: dizziness, seizures, drowsiness,
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fatigue, headache. CV: chest pain, containing magnesium or aluminum
hypotension, palpitations, QT interval hydroxide.
prolongation. GI: abdominal pain, diarrhea, Evaluation/Desired Outcomes:
nausea, cholestatic jaundice, increase liver ● Resolution of the signs and symptoms
enzymes, dyspepsia, flatulence, melena, of infection. Length of time for complete
oral candidiasis, pyloric stenosis. GU: resolution depends on the organism and
nephritis, vaginitis. Hemat: anemia, site of infection.
leukopenia, thrombocytopenia. Derm:
photosensitivity, rash. EENT: ototoxicity. F
and E: hyperkalemia. Drug Classification:
METRONIDAZOLE
Adverse Reaction: Brand Name: Flagyl
Cv: Torsades De Pointes. Derm: Stevens- Generic Name: Metronidazole
Johnson Syndrome, Toxic Epidermal
Necrolysis. Misc: Angioedema. Gi:
Recommended Dosage, Route, and
Hepatotoxicity, Pseudomembranous Colitis,
Frequency:
PO (Adults): Anaerobic infections 7.5 mg/kg
Nursing Responsibilities:
q 6 hr (not to exceed 4 g/day).
Assessment:
Trichomoniasis 250 mg q 8 hr for 7 days or
● Observe for signs and symptoms of
a single 2-g dose or 1 g twice daily for 1 day.
anaphylaxis (rash, pruritus, laryngeal
Amebiasis 500– 750 mg q 8 hr for 5– 10
edema, wheezing). Notify health care
days. H. pylori 250 mg 4 times daily or 500
professional immediately if these occur.
mg twice daily for 1– 2 wk (with other
● Assess patient for skin rash frequently
agents). Bacterial vaginoses 750 mg once
during therapy. Discontinue azithromycin
daily as ER tablets for 7 days. Antibiotic
at first sign of rash; may be life-
associated pseudomembranous colitis 50–
threatening. Stevens-Johnson syndrome
500 mg 3– 4 times/day for 10– 14 days.
or toxic epidermal necrolysis may
PO (Infants and Children): Anaerobic
develop. Treat symptomatically; may
infections 30 mg/kg/day divided q 6 hr,
recur once treatment is stopped.
maximum dose: 4 g/day Trichomoniasis 15–
● Lab Test Considerations: May cause
30 mg/kg/day divided q 8 hr for 7– 10 days.
increase serum bilirubin, AST, ALT, LDH,
Amebiasis 35– 50 mg/kg/day divided q 8 hr
and alkaline phosphatase concentrations.
for 5– 10 days (not to exceed 750 mg/dose).
Potential Nursing Diagnoses:
Antibiotic associated pseudomembranous
● Risk for infection (Indications) (Side
colitis 30 mg/ kg/day divided q 6 hr for 7– 10
Effects)
days. H. pylori 15– 20 mg/kg/day divided
● Noncompliance (Patient/Family
twice daily for 4 weeks.
Teaching)
IV, PO (Neonates 0– 4 weeks, 1200 g): 7.5
Implementation:
mg/kg q 48 hr. Postnatal age 7 days, 1200–
● Zmax extended release oral
2000 g 7.5 mg/kg/day q 24 hr. Postnatal age
suspension is not bioequivalent or
7 days, 2000 g 15 mg/kg/day divided q 12
interchangeable with azithromycin oral
hr. Postnatal age 7 days, 1200– 2000 g 15
suspension.
mg/kg/ day divided q 12 hr. Postnatal age 7
● PO: Administer 1 hr before or 2 hr after
days, 2000 g 30 mg/kg/day divided q 12 hr.
meals.
IV (Adults): Anaerobic infections Initial dose
● For administration of single 1-g packet,
15 mg/kg, then 7.5 mg/kg q 6– 8 hr or 500
thoroughly mix entire contents of packet
mg q 6– 8 hr (not to exceed 4 g/day).
with 2 oz (60 mL) of water. Drink entire
Perioperative prophylaxis Initial dose 15
contents immediately; add an additional 2
mg/kg 1 hr before surgery, then 7.5 mg/kg 6
oz of water, mix and drink to assure
and 12 hr later. Amebiasis 500– 750 mg q 8
complete consumption of dose. Do not
hr for 5– 10 days.
use the single packet to administer doses
IV (Children): Anaerobic infections 30
other than 1000 mg of azithromycin.
mg/kg/day divided q 6 hr, maximum dose: 4
Pedi: 1-g packet is not for pediatric use.
g/day.
● For Zmax, shake suspension well and
Topical (Adults): Acne rosacea Apply thin
drink entire contents of bottle. Use within
film to affected area bid.
12 hr of reconstitution. If patient vomits
Vag (Adults): Bacterial vaginosis One
within 1 hr of administration, contact
applicatorful (5 g) 2 times daily for 5 days.
prescriber for instructions. Zmaxmay be
taken without regard to antacids

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Drug Action:
Disrupts DNA and protein synthesis in
susceptible organisms.
Therapeutic Effects: Bactericidal,
trichomonacidal, or amoebicidal action.
Pharmacokinetics:
Absorption: 80% absorbed after oral
administration. Minimal absorption after
topical or vaginal application.
Distribution: Widely distributed into most
tissues and fluids, including CSF. Crosses
the placenta and enters fetal circulation
rapidly; enters breast milk in concentrations
equal to plasma levels.
Metabolism and Excretion: Partially
metabolized by the liver (30– 60%), partially
excreted unchanged in the urine, 6– 15%
eliminated in the feces.
Half-life: Neonates: 25– 75 hr; Children and
adults: 6– 12 hr.
Drug-Drug and Drug-Food Interactions:
Drug-Drug: Cimetidine may decrease
metabolism. Phenobarbital and rifampin
increase metabolism and may decrease
effectiveness. Metronidazole increase the
effects of phenytoin, lithium, and warfarin.
Disulfiram-like reaction may occur with
alcohol ingestion. May cause acute
psychosis and confusion with a disulfiram.
Increase risk of leukopenia with fluorouracil
or azathioprine.
Indications: PO, IV: Treatment of the
following anaerobic infections: Intra-
abdominal infections (may be used with a
cephalosporin), Gynecologic infections, Skin
and skin structure infections, Lower
respiratory tract infections, Bone and joint
infections, CNS infections, Septicemia,
Endocarditis. IV Perioperative prophylactic
agent in colorectal surgery. PO: Amebicide
in the management of amebic dysentery,
amebic liver abscess, and trichomoniasis:
Treatment of peptic ulcer disease caused by
Helicobacter pylori. Topical Treatment of
acne rosacea. Vag: Management of
bacterial vaginosis.
Unlabeled Use: Treatment of giardiasis.
Treatment of anti-infective associated
pseudomembranous colitis.
Contraindications: Hypersensitivity;
Hypersensitivity to parabens (topical only);
OB: First trimester of pregnancy.
Side Effects:
CNS: dizziness, headache, aseptic
meningitis (IV), encephalopathy (IV). EENT:
optic neuropathy, tearing (topical only). GI:
abdominal pain, anorexia, nausea, diarrhea,
dry mouth, furry tongue, glossitis,
unpleasant taste, vomiting. Derm: rash,
urticaria topical only, burning, mild dryness,
skin irritation, transient redness. Hemat:
leukopenia. Local: phlebitis at IV site.
Neuro: peripheral neuropathy. Misc:
superinfection.
Adverse Reaction:
CNS: SEIZURES. Derm: STEVENS-
JOHNSON SYNDROME.
Nursing Responsibilities:
Assessment:
● Assess for infection (vital signs;
appearance of wound, sputum, urine, and
stool; WBC) at the beginning of and
throughout therapy.
● Obtain specimens for culture and
sensitivity before initiating a therapy. First
dose may be given before receiving results.
● Monitor neurologic status during and after
IV infusions. Inform health care professional
if numbness, paresthesia, weakness, ataxia,
or seizures occur.
● Monitor intake and output and daily
weight, especially for patients on sodium
restriction. Each 500 mg of premixed
injection or dilution contains 14 mEq of
sodium.
● Assess for a rash periodically during
therapy. May cause Stevens-Johnson
syndrome. Discontinue therapy if severe or if
accompanied with fever, general malaise,
fatigue, muscle or joint aches, blisters, oral
lesions, conjunctivitis, hepatitis and/or
eosinophilia.
● Giardiasis: Monitor three stool samples
taken several days apart, beginning 3– 4 wk
after treatment
Potential Nursing Diagnoses:
● Risk for infection (Indications)
● Diarrhea (Indications)
Implementation:
● Do not confuse metronidazole with
metformin.
● PO: Administer on an empty stomach, or
may administer with food or milk to minimize
GI irritation. Tablets may be crushed for
patients with difficulty swallowing. Swallow
extended-release tablets whole; do not
break, crush, or chew.
Evaluation/Desired Outcomes
● Resolution of the signs and symptoms of
infection. Length of time for complete
resolution depends on an organism and a
site of infection.
● Significant results should be seen within 3
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wk of application of topical gel. Application
may be continued for 9 wk.
Drug Classification: POLYENES
Brand Name: Fungizone
Generic Name: Amphoterecin B
Recommended Dosage, Route, and
Frequency:
Specific dosage and duration of therapy
depend on the nature of infection being
treated.
Amphotericin Deoxycholate
IV (Adults): Give test dose of 1 mg. If test
dose tolerated, initiate therapy with 0.25
mg/kg/day (doses up to 1.5 mg/kg/day may
be used, depending on type of infection)
(alternate-day dosing may also be used);
Bladder irrigation Instill 50 mcg/mL solution
into bladder daily for 5–10 days.
IV (Infants and Children): Give test dose of
0.1 mg/kg (maximum dose 1 mg) or may
administer initial dose of 0.25– 1 mg/kg/day
over 6 hr (without test dose) (some
infections may require 1.5 mg/kg/day;
alternate-day dosing may be used).
IT (Adults): 25– 300 mcg q 48– 72 hr
increase to 500 mcg– 1 mg as tolerated
(maximum total dose 15 mg).
IT (Children): 25– 100 mcg q 48– 72 hr
increase to 500 mcg as tolerated.
Amphotericin B Cholesteryl Sulfate
(Amphotec)
IV (Adults and Children): 3– 4 mg/kg q 24 hr
(no test dose needed).
Amphotericin B Lipid Complex (Abelcet)
IV (Adults and Children): 2.5– 5 mg/kg q 24
hr (no test dose needed).
Amphotericin B Liposome (AmBisome)
IV (Adults and Children): Empiric therapy—3
mg/kg q 24 hr; Documented infections 3– 5
mg/kg q 24 hr; Visceral leishmaniasis
(immunocompetent patients) 3 mg/kg q 24
hr on days 1– 5, then 3 mg/kg q 24 hr on
days 14 and 21; Visceral leishmaniasis
(immunosuppressed patients) 4 mg/kg q 24
hr on days 1– 5, then 4 mg/kg q 24 hr on
days 10, 17, 24, 31, and 38; Cryptococcal
meningitis in HIV patients 6 mg/kg q 24 hr.
Drug Action:
Binds to fungal cell membrane, allowing the
leakage of cellular contents. Toxicity
(especially acute infusion reactions and
nephrotoxicity) is less with lipid formulations.
Therapeutic Effects: Can be fungistatic or
fungicidal (depends on a concentration
achieved and susceptibility of organism).
Absorption: IV administration results in
complete bioavailability.
Distribution: Extensively distributed to body
tissues and fluids. Poor penetration into
CSF. Metabolism and Excretion:
Elimination is very prolonged. Detectable in
urine up to 7 wk after discontinuation.
Half-life: Biphasic initial phase, 24– 48 hr;
terminal phase, 15 days. Cholesteryl sulfate
28 hr.Lipid complex 174 hr. Liposomal 100–
153 hr.
Drug-Drug and Drug-Food Interactions:
Increase the risk of nephrotoxicity,
bronchospasm, and hypotension with
antineoplastic. Concurrent use with
corticosteroids increases the risk of
hypokalemia. Concurrent use with
zidovudine may increase the risk of
myelotoxicity and nephrotoxicity. Concurrent
use with flucytosine increase antifungal
activity but may increase the risk of toxicity
from flucytosine. Combined use with azole
antifungals may induce fungal resistance.
Increase the risk of nephrotoxicity with other
nephrotoxic agents such as
aminoglycosides, cyclosporine, or
tacrolimus. Hypokalemia from amphotericin
increase the risk of digoxin toxicity.
Hypokalemia may enhance the curariform
effects of neuromuscular blocking agents.
Indications: IV: Treatment of progressive,
potentially fatal fungal infections. The
cholesteryl sulfate, lipid complex, and
liposome formulations should be considered
for patients who are intolerant (e.g., renal
dysfunction) or refractory to amphotericin B
deoxycholate? Amphotericin B liposome:
Management of suspected fungal infections
in febrile neutropenic patients: Treatment of
visceral leishmaniasis, Treatment of
cryptococcal meningitis in HIV patients.
Contraindications: Hypersensitivity;
Lactation: Potential for distribution into
breast milk and toxicity in infant; discontinue
nursing.
Side Effects:
CNS: anxiety, confusion, headache,
insomnia. Resp: dyspnea, hypoxia,
wheezing. CV: chest pain, hypotension,
tachycardia, edema, hypertension. GI:
diarrhea, hyperbilirubinemia, increase liver
enzymes, nausea, vomiting, abdominal pain.
GU: nephrotoxicity, hematuria. F and E:
hyperglycemia, hypocalcemia, hypokalemia,
hypomagnesemia. Hemat: anemia,
leukopenia, thrombocytopenia. Derm:
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pruritis, rashes. Local: phlebitis.MS:
arthralgia, myalgia. Misc: chills, fever, acute
infusion reactions.
Adverse Reaction:
Misc: HYPERSENSITIVITY REACTIONS.
Nursing Responsibilities:
Assessment:
● Monitor patient closely during test dose
and the first 1– 2 hr of each dose for
fever, chills, headache, anorexia,
nausea, or vomiting. Premedicating with
antipyretics, corticosteroids,
antihistamines, meperidine, and
antiemetics may decrease these
reactions. Febrile reaction usually
subsides within 4 hr after the infusion is
completed.
● Assess the injection site frequently for
thrombophlebitis or leakage. Drug is very
irritating to tissues.
● Monitor vital signs every 15 min during
test dose and every 30 min for 2– 4 hr
after administration. Meperidine and
dantrolene have been used to prevent
and treat rigors. Assess respiratory
status (lung sounds, dyspnea) daily. If
respiratory distress occurs, discontinue
infusion immediately; anaphylaxis may
occur. Equipment for cardiopulmonary
resuscitation should be readily available.
● Monitor intake and output and weigh
daily. Adequate hydration (2000– 3000
mL/ day) and maintaining sodium
balance may minimize nephrotoxicity.
Potential Nursing Diagnoses:
● Risk for infection (Indications)
Implementation:
● Do not confuse amphotericin B
cholesteryl sulfate (Amphotec) with
amphotericin deoxycholate, amphotericin
B lipid complex (Abelcet), or
amphotericin B liposome (AmBisome);
they are not interchangeable.
● This drug should be administered IV
only to hospitalized patients or those
under close supervision. Diagnosis
should be confirmed before
administration.
Evaluation/Desired Outcomes:
● Resolution of signs and symptoms of
infection. Several weeks to months of
therapy may be required to prevent
relapse.
Drug Classification: AZOLE CLASS
Brand Name: Canesoral, Diflucan,
Monicure
Generic Name: Fluconazole
Recommended Dosage, Route, and
Frequency:
Oropharyngeal Candidiasis
PO, IV (Adults): 200 mg initially, then 100
mg daily for at least 2 wk.
PO, IV (Children > 14 days): 6 mg/kg
initially, then 3 mg/kg/day for at least 2 wk.
PO, IV (Neonates< 14 days, 30– 36 weeks'
gestation): same dose as older children
except frequency is q 48 hr; Premature
neonates 29 weeks' gestation: 5– 6 mg/
kg/dose q 48– 72 hr.
Esophageal Candidiasis
PO, IV (Adults): 200 mg initially, then 100
mg once daily for at least 3 wk (up to 400
mg/day).
Drug-Drug and Drug-Food Interactions:
PO, IV (Children 1>4 days): 6 mg/kg initially,
then 3– 12 mg/kg/day for at least 3 wk.
PO, IV (Neonates <14 days, 30– 36 weeks'
gestation): same dose as older children
except frequency is q 48 hr; Premature
neonates 29 weeks' gestation: 5– 6 mg/
kg/dose q 48– 72 hr.
Vaginal Candidiasis
PO (Adults): 150-mg single dose; prevention
of recurrence (unlabeled) 150 mg daily for 3
days then weekly for 6 mo.
Systemic Candidiasis
PO, IV (Adults): 400 mg/day initially, then
200– 800 mg/day for 28 days.
PO, IV (Children 14 days): 6– 12 mg/kg/day
for 28 days.
PO, IV (Neonates 14 days, 30– 36 weeks'
gestation): same dose as older children
except frequency is q 48 hr; Premature
neonates 29 weeks' gestation: 5– 6 mg/
kg/dose q 48– 72 hr.
Cryptococcal Meningitis
PO, IV (Adults): Treatment 400 mg once
daily until favorable clinical response, then
200– 800 mg once daily for at least 10– 12
wks. after a clearing of CSF; change to oral
therapy as soon as possible. Suppressive
therapy 200 mg once daily.
PO, IV (Children 14 days): 12 mg/kg/day
initially, then 6– 12 mg/kg/day for at least
10– 12 wk. after clearing of CSF; change to
oral therapy as soon as possible.
Suppressive therapy—6 mg/kg/day.
PO, IV (Neonates 14 days, 30– 36 weeks'
gestation): same dose as older children
except the frequency is q 48 hr.; Premature
neonates 29 weeks' gestation: 5– 6 mg/
kg/dose q 48– 72 hr.
Page | 165
Prevention of Candidiasis after Bone
Marrow Transplant
PO, IV (Adults): 400 mg once daily; begin
several days before the procedure if severe
neutropenia is expected, and continue for 7
days after ANC 1000 /mm3.
PO, IV (Children 14 days): 10– 12
mg/kg/day, not to exceed 600 mg/day.
Renal Impairment
PO, IV (Adults): CCr 11– 50 mL/min 50% of
the usual dose.
Drug Action:
Inhibits synthesis of fungal sterols, a
necessary component of the cell membrane.
Therapeutic Effects: Fungistatic action
against susceptible organisms. May be
fungicidal in higher concentrations.
Spectrum: Cryptococcus neoformans.
Candida spp.
PHARMACOKINETICS:
Absorption: Well absorbed after oral
administration.
Distribution: Widely distributed, good
penetration into CSF, saliva, sputum,
vaginal fluid, skin, eye, and peritoneum.
Excreted in breast milk.
Metabolism and Excretion: 80% excreted
unchanged by the kidneys; 10%
metabolized by the liver.
Half-life: Premature neonates: 46– 74 hr;
Children: 19– 25 hr (PO) and 15– 17 hr (IV);
Adults: 30 hr (increase in renal impairment).
Drug-Drug and Drug-Food Interactions:
Drug-Drug: Increase activity of warfarin.
Rifampin, rifabutin, and isoniazid decrease
the levels. Fluconazole at doses 200 mg/day
may inhibit the CYP3A4 enzyme system and
effect the activity of drugs metabolized by
this system. Increase hypoglycemic effects
of tolbutamide, glyburide, or glipizide.
Increase levels and the risk of toxicity from
cyclosporine, rifabutin, tacrolimus,
theophylline, zidovudine, alfentanil, and
phenytoin. Increase levels and effects of
benzodiazepines, zolpidem, buspirone,
nisoldipine, tricyclic antidepressants, and
losartan. Increase levels of the tofacitinib;
decrease dose of tofacitinib to 5 mg once
daily. May increase the risk of bleeding with
warfarin. May antagonize effects of
amphotericin B. May increase voriconazole
levels; avoid concurrent use.
Indications: PO, IV: Fungal infections
caused by susceptible organisms, including:
Oropharyngeal or esophageal candidiasis,
Serious systemic candida infections, Urinary
tract infections, Peritonitis, Cryptococcal
meningitis. Prevention of candidiasis in
patients who have undergone bone marrow
transplantation. PO Single-dose oral
treatment of vaginal candidiasis. Unlabeled
Use: Prevention of recurrent vaginal yeast
infections
Contraindications: Hypersensitivity to
fluconazole or other azole antifungals;
Concurrent use with pimozide or
voriconazole.
Side Effects:
Incidence of adverse reactions is increased
in HIV patients
CNS: headache, dizziness, seizures. GI:
Abdominal discomfort, diarrhea, nausea,
vomiting. Derm: exfoliative skin disorders
including. En: hypokalemia,
hypertriglyceridemia.
Adverse Reaction:
GI: HEPATOTOXICITY. Derm: STEVENS-
JOHNSON SYNDROME and the patients
has NAPHYLAXIS Responsibilities.
Nursing Responsibilities:
Assessment:
● Assess the infected area and monitor
CSF cultures before and periodically
during therapy.
● Specimens for culture should be taken
before instituting therapy. Therapy may
be started before results are obtained.
● Assess patient for rash (mild to
moderate rash usually occurs in the 2nd
wk of therapy and resolves within 1– 2
wk of continued therapy). If rash is
severe (extensive erythematous or
maculopapular rash with moist
desquamation or angioedema) or
accompanied by systemic symptoms
(serum sickness-like reaction, Stevens-
Johnson syndrome, toxic epidermal
necrolysis), therapy must be discontinued
immediately.
● Monitor liver function tests before and
periodically during therapy. May cause
increase AST, ALT, serum alkaline
phosphate, and bilirubin concentrations.
Potential Nursing Diagnoses
● Risk for infection (Indications)
Implementation
● Do not confuse Diflucan (fluconazole)
with Diprivan (propofol).
● PO: Shake oral suspension well before
the administration.
Evaluation/Desired Outcomes
● Resolution of clinical and laboratory
indications of fungal infections. Full
Page | 166
 course of therapy may require weeks or
months of treatment after resolution of
symptoms.
● Prevention of candidiasis in patients
who have undergone bone marrow
transplantation.
● Decrease in skin irritation and vaginal
discomfort in patients with vaginal
candidiasis. Diagnosis should be
reconfirmed with smears or cultures
before a second course of therapy to rule
out other pathogens associated with
vulvovaginitis. Recurrent vaginal
infections may be a sign of systemic
illness
Drug Classification: Antimetabolite
Brand Name: Ancobon
Generic Name: Flucytosine
Recommended Dosage, Route, and
Frequency:
PO (Adults): 12.5– 37.5 mg/kg every 6 hr.
PO (Children): 12.5– 37.5 mg/kg every 6 hr.
Renal Impairment
PO (Adults): CCr 20– 40 mL/min 12.5 mg/kg
every 12 hr; CCr 10– 20 mL/ min 12.5 mg/kg
every 24 hr; CCr 10 mL/min 12.5 mg/kg
every 24– 48 hr.
Drug Action:
Following penetration into fungi, converted
to fluorouracil, which interferes with fungal
DNA and RNA synthesis. Synergistic action
with amphotericin B against some fungi.
Therapeutic Effects: Fungicidal action
against susceptible organisms.
Pharmacokinetics:
Absorption: Well absorbed (80– 90%) from
the GI tract following oral administration.
Distribution: Widely distributed. Crosses
the blood-brain barrier.
Metabolism and Excretion: 80– 90%
excreted unchanged by the kidneys.
Half-life: 2.5– 5 hr (qin renal impairment).
Drug-Drug and Drug-Food Interactions:
Drug-Drug: Additive bone marrow
depression with other bone marrow
depressant drugs, including antineoplastic
and radiation therapy. Amphotericin B may
increase toxicity of flucytosine but may also
increase its antifungal activity. Cytarabine
may decrease its antifungal activity.
Indications: Treatment of serious fungal
infections including: Endocarditis,
Meningitis, Septicemia, Urinary tract
infections, Pulmonary infections.
Contraindications: Hypersensitivity,
Lactation: Pregnancy or lactation.
Side Effects:
CNS: ataxia, confusion, dizziness,
drowsiness, fatigue, headache.
CV: chest pain.
EENT: hearing loss.
GI: diarrhea, nausea, vomiting, abdominal
pain, dry mouth.
Derm: photosensitivity, pruritis, rash,
urticaria.
Endo: hypoglycemia.
F and E: hypokalemia.
GU: azotemia.
Hemat: eosinophilia, leukopenia,
pancytopenia, anemia, thrombocytopenia.
Neuro: peripheral neuropathy.
Resp: dyspnea.
Misc: fever.
Adverse Reaction:
CNS: Seizures.
Hemat: Aplastic Anemia.
Nursing Responsibilities:
Assessment:
● Assess the patient for signs and
symptoms of systemic fungal infection
prior to and periodically throughout
therapy.
● Obtain specimens for culture prior to
initiating a therapy. First dose may be
given before receiving results.
● Monitor hematologic function
periodically during therapy. May cause
anemia, leukopenia, or
thrombocytopenia.
● Toxicity and Overdose: Therapeutic
peak serum flucytosine levels range from
25– 100 mcg/mL. Peak levels should be
obtained 2 hours after a dose.
Potential Nursing Diagnoses:
● Risk for infection (Indications)
● Risk for deficient fluid volume (Adverse
Reactions)
● Deficient knowledge, related to
medication regimen (Patient/Family
Teaching)
Implementation:
● The number 5 in 5-FC is part of the
drug name and not the dose.
● PO: To reduce nausea and vomiting,
administer capsules a few at a time over
15 min.
Evaluation/Desired Outcomes:
● Resolution of the signs and symptoms
Page | 167
 of fungal infection. Duration of therapy is should be considered in patients who are
generally 4– 6 wk but may continue for not clinically responding.
several months.
Indications: Invasive aspergillosis
refractory to, or intolerant of, other therapies.
Drug Classification: Candidemia and associated serious
ECHINOCANDINS infections (intra-abdominal abscesses,
Brand Name: Cancidas peritonitis, pleural space infections).
Generic Name: Caspofungin Esophageal candidiasis. Suspected fungal
infections in febrile neutropenic patients.
Recommended Dosage, Route, and
Contraindications: Hypersensitivity;
Frequency:
Concurrent use with cyclosporine
IV (Adults): 70 mg initially followed by 50 mg
daily, duration determined by the clinical
Side Effects:
situation and response; Esophageal
CNS: headache, chills.GI: diarrhea, increase
candidiasis—50 mg daily, duration
liver enzymes, nausea, vomiting. Resp:
determined by clinical situation and
bronchospasm. GU: increase creatinine.
response.
Derm: flushing, pruritis, rash. Local: venous
IV (Children > 3 mo): 70 mg/m2 (max: 70
irritation at injection site. Misc: allergic
mg) initially followed by 50 mg/m2 daily
reactions, fever.
(max: 70 mg/day), duration determined by
clinical situation and response.
Adverse Reaction:
IV (Infants 1 to 3 mo and Neonates): 25
Misc: Anaphylaxis, Angioedema.
mg/m2 /dose once daily.
Hepatic Impairment
Nursing Responsibilities:
IV (Adults): Moderate hepatic impairment—
Assessment:
70 mg initially followed by 35 mg daily,
● Assess the patient for signs and
duration determined by clinical situation and
symptoms of fungal infections prior to
response.
and periodically during therapy.
● Monitor patient for signs of anaphylaxis
Drug Action:
(rash, dyspnea, stridor) during therapy.
Inhibits the synthesis of (1, 3)-D-glucan, a
● Lab Test Considerations: May cause
necessary component of the fungal cell wall.
increase serum alkaline phosphatase,
Therapeutic Effects: Death of susceptible
serum creatinine, AST, ALT, eosinophils,
fungi.
and urine protein and RBCs. May also
Pharmacokinetics:
cause decrease serum potassium,
Absorption: IV administration results in
hemoglobin, hematocrit, and WBCs.
complete bioavailability.
Potential Nursing Diagnoses:
Distribution: Widely distributed to tissues.
● Risk for infection (Indications)
Metabolism and Excretion: Slowly and
Implementation:
extensively metabolized; 1.5% excreted
IV Administration
unchanged in urine.
● pH: 6.6.
Half-life: Polyphasic: phase 9– 11 hr; phase
● Intermittent Infusion: Diluent: Allow
40– 50 hr.
refrigerated the vial to reach room
temperature. For a 70-mg or 50-mg dose
Drug-Drug and Drug-Food Interactions:
● Y-Site Compatibility: alfentanil,
Drug-Drug: Concurrent use with
allopurinol, amifostine, amikacin,
cyclosporine is not recommended due
aminophylline, amiodarone,
toqrisk of hepatic toxicity. May decrease
anidulafungin, atracurium, aztreonam,
blood levels and effects of tacrolimus. Blood
bleomycin, bumetanide, busulfan,
levels and effectiveness may be decrease
butorphanol, calcium acetate, calcium
by rifampin; maintenance dose should be
chloride, calcium gluconate, carboplatin,
increase to 70 mg (in patients with normal
carmustine, chlorpromazine, cimetidine.
liver function). Blood levels and
● Y-Site Incompatibility: amphotericin B
effectiveness also may be decrease by
colloidal, amphotericin B lipid complex,
efavirenz, nelfinavir, nevirapine, phenytoin,
amphotericin B liposome, ampicillin,
dexamethasone, or carbamazepine; an
ampicillin/sulbactam, bivalirudin,
increase in the maintenance dose to 70 mg
cefazolin, cefepime, cefoperazone,
cefotaxime, cefotetan, cefoxitin,

Page | 168
 ceftazidime, ceftriaxone, cefuroxime,
chloramphenicol.
● Solution Incompatibility: Solutions
containing dextrose.
Evaluation/Desired Outcomes:
● Decrease in signs and symptoms of
fungal infections. Duration of therapy is
determined based on the severity of
underlying disease, recovery from
immunosuppression, and clinical
response.
decrease blood levels and may decrease
the effectiveness. May decrease the
effectiveness of warfarin or hormonal
contraceptive agents.
Drug-Food: Absorption is an increase by
fatty foods.
Indications: Treatment of various tinea
infections. Should not be used for superficial
infections that may respond to topical
antifungals.

Classification: TUBULIN-INHIBITING Contraindications: Hypersensitivity;

AGENT Severe liver disease or porphyria.
Brand Name: Grosovin-FP Side Effects:
Generic Name: Griseofulvin CNS: headache, dizziness. EENT: hearing
loss. GI: diarrhea, epigastric distress,
extreme thirst, flatulence, nausea,
Recommended Dosage, Route, and
vomiting.Derm: photosensitivity, rashes.
Frequency:
Hemat: leukopenia. Misc: hypersensitivity
Microsize
reactions, lupus-like syndrome.
PO (Adults): Tinea pedis, onychomycosis
500 mg q 12 hr. Tinea capitis, corporis, or
Adverse Reaction:
cruris 250 mg q 12 hr or 500 mg once daily.
GI: Hepatotoxicity. Derm: Erythema
PO (Children 23 kg): 125– 250 mg q 12 hr or
Multiforme, Stevens-Johnson Syndrome,
250– 500 mg once daily.
Toxic Epidermal Necrolysis. Misc: Serum
PO (Children 14– 23 kg): 62.5– 125 mg q 12
Sickness.
hr or 125– 250 mg once daily.
Ultramicrosize
Nursing Responsibilities:
PO (Adults): Tinea pedis, onychomycosis
Assessment:
375 mg q 12 hr. Tinea capitis, corporis, or
● Assess skin at the site of fungal
cruris 187.5 mg q 12 hr or 375 mg once
infection routinely throughout course of
daily.
therapy.
PO (Children 27 kg): 187.5– 375 mg once
● Assess the patient for allergy to
daily.
penicillin; potential cross-sensitivity
PO (Children 16– 27 kg): 125– 187.5 mg
exists.
once daily.
● Assess for rash periodically during
therapy. May cause Stevens-Johnson
Drug Action:
syndrome or toxic epidermal necrolysis.
Inhibits mitosis of fungal cells. Deposits in
Discontinue therapy if severe or if
precursor cells of hair, skin, and nails,
accompanied with fever, general malaise,
making them resistant to fungal invasion.
fatigue, muscle or joint aches, blisters,
Therapeutic Effects: Growth of new cells
oral lesions, conjunctivitis, hepatitis
that is resistant to invasion by fungi.
and/or eosinophilia.
Pharmacokinetics:
● Lab Test Considerations: CBC, serum
Absorption: Micro size preparations are
creatinine, and hepatic functions should
variably (25– 70%) absorbed after oral
be monitored periodically throughout
administration. Ultramicro size products are
treatment.
almost completely absorbed.
● Monitor urinalysis periodically during
Distribution: Mostly deposited in the keratin
therapy. May rarely cause proteinuria.
layer of skin; also found in liver, fat, and
Potential Nursing Diagnoses:
skeletal muscle. Metabolism and
● Risk for impaired skin integrity
Excretion: Metabolized by the liver, some
(Indications)
excreted in feces and perspiration. Half-
● Risk for infection (Indications) (Side
life: 9– 24 hr.
Effects)
● Deficient knowledge, related to
Drug-Drug and Drug-Food Interactions:
medication regimen (Patient/Family
Drug-Drug: Tachycardia, flushing, and
Teaching)
increase CNS depression may result if taken
Implementation:
concurrently with alcohol. Phenobarbital
● Concurrent use of a topical agent is

Page | 169
 usually required.
● Ultra micro size griseofulvin 250 mg
provides serum concentrations equal to
that of micro size griseofulvin 500 mg.
● PO: Administer with or after meals,
preferably meals with high fat content, to
minimize GI irritation and increase
absorption.
Evaluation/Desired Outcomes:
● Resolution of signs and symptoms of
fungal infection. To prevent relapse,
treatment may take weeks to months and
should continue until organism is
completely eradicated as determined by
clinical or laboratory testing. Tinea capitis
usually requires treatment for 8– 10 wk;
tinea corporis, 2– 4 wk; tinea pedis, 4– 8
wk; onychomycosis, at least 4 mo for
fingernails and at least 6 mo for toenails
(recurrence rates for toenails are very
high).
Classification: POLYMYXINS
Brand Name: Aerosporin
Generic Name: Polymyxin B
Recommended Dosage, Route, and
Frequency:
Infections
Adult:
IV 15,000–25,000 U/kg/d divided q12h
IM 25,000–30,000 U/kg/d divided q4–6h
GU 1 mL/L NS q24h
Topical 1–2 drops in the eye q1h
Child:
IV 15,000–25,000 U/kg/d divided q12h
IM 25,000–30,000 U/kg/d divided q4–6h
Drug Action:
Antibiotic derived from strains of Bacillus
polymyxa. Binds to lipid phosphates in
bacterial membranes and, through cationic
detergent action, changes permeability to
permit leakage of the cytoplasm.
Therapeutic Effects: Bactericidal against
susceptible gram-negative organisms,
particularly most strains of Escherichia coli,
Haemophilus influenzae, Enterobacter
aerogenes, and Klebsiella pneumoniae.
Most species of Proteus and Neisseria are
resistant, as are all gram-positive organisms
and fungi.
Pharmacokinetics:
Absorption: Well absorbed from the GI
tract.
Distribution: Widely distributed. Crosses
the blood-brain barrier and placenta and
enters breast milk. Protein Binding: TMP:
45%; SMX: 68%.
Metabolism and Excretion: Some
metabolism by the liver (20%); remainder
excreted unchanged by the kidneys.
Half-life: Trimethoprim 6– 11 hr;
sulfamethoxazole 9– 12 hr, both prolonged
in renal failure.
Drug-Drug and Drug-Food Interactions:
Drug: Anesthetics and Neuromuscular
Blocking Agents may prolong skeletal
muscle relaxation. Aminoglycosides and
amphotericin B have additive nephrotoxic
potential.
Indications: Topically and in combination
with other anti-infective or corticosteroids for
various superficial infections of eye, ear,
mucous membrane, and skin. Concurrent
systemic anti-infective therapy may be
required for treatment of intraocular infection
and severe progressive corneal ulcer. Used
parenterally only in hospitalized patients for
treatment of severe acute infections of
urinary tract, bloodstream, and meninges;
and in combination with Neosporin for
continuous bladder irrigation to prevent
bacteremia associated with use of indwelling
catheter.
Contraindications: Hypersensitivity to
polymyxin antibiotics; concurrent and
sequential use of other nephrotoxic and
neurotoxic drugs; concurrent use of skeletal
muscle relaxants, ether, or sodium citrate.
Safety during pregnancy (category B) or
children <2 mo is not established.
Side Effects: Body as a Whole: Irritability,
facial flushing, ataxia, circumoral, lingual,
and peripheral paresthesia (stocking-glove
distribution); severe pain (IM site),
thrombophlebitis (IV site), superinfections,
electrolyte disturbances (prolonged use;
also reported in patients with acute
leukemia); local irritation and burning
(topical use), anaphylactoid reactions (rare).
CNS: Drowsiness, dizziness, vertigo,
convulsions, coma; neuromuscular blockade
(generalized muscle weakness, respiratory
depression or arrest); meningeal irritation,
increased protein and cell count in
cerebrospinal fluid, fever, headache, stiff
neck (intrathecal use). Special Senses:
Blurred vision, nystagmus, slurred speech,
dysphagia, ototoxicity (vestibular and
auditory) with high doses. GI: GI
disturbances. Urogenital: Albuminuria,
cylindruria, azotemia, hematuria.
Page | 170
Adverse Reaction: Unknown discomfort in patients with vaginal
candidiasis. Diagnosis should be
Nursing Responsibilities: reconfirmed with smears or cultures
Assessment & Drug Effects before a second course of therapy to rule
● Lab tests: Obtain C&S tests prior to the out other pathogens associated with
first dose and periodically thereafter to vulvovaginitis. Recurrent vaginal
determine continuing sensitivity of infections may be a sign of systemic
causative organisms. Perform baseline illness
serum electrolytes and kidney function
tests before parenteral therapy. Frequent
monitoring of kidney function and serum
drug levels is advised during therapy.
Monitor electrolytes at regular intervals
during prolonged therapy.
● Review electrolyte results. Patients Drug Classification: BACITRACIN
with low serum calcium and low Brand Name: BACiiM, Baciject,
intracellular potassium are particularly Bacitin
prone to develop neuromuscular Generic Name: Bacitracin
blockade.
● Inspect tongue every day. Assess for
Recommended Dosage, Route, and
S&S of superinfection (see Appendix F).
Frequency:
Polymyxin therapy supports the growth of
Topical (Adults and Children): Apply 1– 5
opportunistic organisms. Report
times daily.
symptoms promptly.
IM (Infants 2.5 kg): 1000 units/kg/day in 2– 3
● Monitor I&O. Maintain fluid intake
divided doses.
sufficient to maintain daily urinary output
IM (Infants 2.5 kg): 900 units/kg/day in 2– 3
of at least 1500 mL. Some degree of
divided doses.
renal toxicity usually occurs within first 3
or 4 d of therapy even with therapeutic
Drug Action:
doses. Consult a physician.
Inhibits bacterial cell wall synthesis by
● Withhold drug and report findings to a
preventing the transfer of mucopeptides into
physician for any of the following:
growing cell wall. Therapeutic Effects:
Decreases in urine output (change in I&O
Bactericidal action.
ratio), proteinuria, cellular casts, rising
Spectrum: Notable for activity against:
BUN, serum creatinine, or serum drug
Staphylococci,Streptococci .
levels (not associated with dosage
Pharmacokinetics:
increase). All can be interpreted as signs
Absorption: Well absorbed after IM
of nephrotoxicity.
administration. Poorly absorbed from
● Nephrotoxicity is generally reversible,
mucous membranes. Distribution: Poor
but it may progress even after the drug is
penetration into CSF.
discontinued. Therefore, close monitoring
Metabolism and Excretion: 10– 40%
of kidney function is essential, even
excreted in urine within 24 hr.
following termination of therapy.
Half-life: Unknown.
Potential Nursing Diagnoses
● Risk for infection (Indications)
Drug-Drug and Drug-Food Interactions:
Implementation
Drug-Drug: Increase incidence of
● Do not confuse Diflucan (fluconazole)
nephrotoxicity with other nephrotoxic drugs;
with Diprivan (propofol).
avoid concurrent use.
● PO: Shake oral suspension well before
the administration.
Indications: IM: Treatment of infants with
Evaluation/Desired Outcomes
pneumonia and empyema caused by
● Resolution of clinical and laboratory
susceptible Staphylococci. Topical, Ophth:
indications of fungal infections. Full
Treatment of localized infections due to
course of therapy may require weeks or
susceptible organisms.
months of treatment after resolution of
symptoms.
Contraindications: Hypersensitivity; Renal
● Prevention of candidiasis in patients
impairment
who have undergone bone marrow
transplantation.
● Decrease in skin irritation and vaginal

Page | 171
Side Effects:
Derm: rash. GI: nausea, vomiting. GU: renal
failure. Local: pain at the injection site.
Adverse Reaction:
GI: Pseudomembranous Colitis.
Nursing Responsibilities:
Assessment:
● IM: Monitor signs and symptoms of
infection (fever, chills, respiratory status,
mucous secretions) prior to and
periodically during therapy.
● Topical: Assess lesions prior to and
periodically during therapy.
● Monitor bowel function. Diarrhea,
abdominal cramping, fever, and bloody
stools should be reported to health care
professional promptly as a sign of
pseudomembranous colitis. May begin
up to several weeks following cessation
of therapy.
● Lab Test Considerations: Monitor CBC
periodically during therapy.
● Monitor renal function prior to and daily
during IM therapy.
Potential Nursing Diagnoses:
● Risk for infection (Indications)
Implementation:
● IM: Reconstitute with 0.9% NaCl
containing 2% procaine hydrochloride.
Do not use diluents containing parabens.
Store in refrigerator. Concentration: Not
less than 5,000 U/mL or more than
10,000 U/mL.
● Topical: Apply small amount of
ointment to affected area; may be
covered with a sterile bandage.
Evaluation/Desired Outcomes:
● Resolution of infection.
Drug Classification: ANTIMALARIALS
Brand Name: Aralen
Generic Name: Chloroquine
Hydrochloride
Recommended Dosage, Route, and
Frequency:
Doses below expressed as chloroquine
base: 1 mg of chloroquine base 1.67 mg
chloroquine phosphate or 1.25 mg
chloroquine hydrochloride.
Suppression/Prophylaxis of Malaria
PO (Adults): 300 mg once weekly, starting 2
wk prior to entering endemic areas and for 8
wk afterward. If suppressive therapy is not
initiated prior to entering endemic area,
initial dose should be 300 mg followed by
another 300 mg dose 6 hr later, followed by
the usual dosage regimen.
PO (Children): 5 mg/kg once weekly,
starting 2 wk prior to entering endemic areas
and for 8 wk afterward (not to exceed 300
mg/day).If suppressive therapy is not
initiated prior to entering endemic area,
initial dose should be 5 mg/kg followed by
another 5 mg/kg dose 6 hr later, followed by
the usual dosage regimen.
Treatment of Acute Attack of Malaria
PO (Adults): 600 mg initially, then 300 mg at
6– 8 hr, 24 hr, and 48 hr after initial dose.
PO (Children): 10 mg/kg initially (not to
exceed 600 mg), then 5 mg/kg at 6 hr, 24 hr,
and 48 hr after initial dose (not to exceed
300 mg/day).
Extraintestinal Amebiasis
PO (Adults): 600 mg daily for 2 days, then
300 mg daily for at least 2– 3 wk (in
combination with other antiprotozoals).
PO (Children): 10 mg/kg (not to exceed 300
mg/day for 2– 3 wk.
Rheumatoid Arthritis/Systemic Lupus
Erythematosus
PO (Adults): 150 mg once daily; reduce
dosage following maximal response.
Drug Action:
Inhibits protein synthesis in susceptible
organisms by inhibiting DNA and RNA
polymerase.
Therapeutic Effects: Death of plasmodia
responsible for causing malaria. Death of
amoeba responsible for causing amebiasis.
Improvement in inflammation in rheumatoid
arthritis and systemic lupus erythematosus.
Pharmacokinetics:
Absorption: Well absorbed following oral
administration.
Distribution: Widely distributed; high tissue
concentrations achieved. Crosses the
placenta, enters breast milk.
Metabolism and Excretion: 30%
metabolized by the liver. Metabolite also has
antiplasmodial activity; 70% excreted
unchanged by the kidneys.
Half-life: 3– 5 days.
Drug-Drug and Drug-Food Interactions:
Drug-Drug: Antacids may decrease
absorption (separate administration of these
agents by at least 4 hr). Blood levels may be
increase by cimetidine, fluconazole,
ketoconazole, clarithromycin, erythromycin,
fluoxetine, nefazodone, paroxetine, protease
inhibitors, quinidine, ritonavir, and verapamil
(concurrent use with cimetidine, should be
avoided). May decrease absorption of
ampicillin (separate administration of these
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agents by at least 2 hr). May increase blood
levels of cyclosporine, fluoxetine, lidocaine,
mirtazapine, nefazodone, paroxetine,
risperidone, ritonavir, thioridazine, tricyclic
antidepressants, and venlafaxine. Blood
levels may be decrease by carbamazepine,
nevirapine, phenobarbital, phenytoin, and
rifampin. May increase the risk of
hepatotoxicity when administered with other
hepatotoxic agents. Urinary acidifiers may
increase renal excretion and decrease
effectiveness. Concurrent use with
mefloquine may increase risk of seizures.
Drug-Food: Foods that acidify urine may
increase excretion and decrease
effectiveness.
Indications: Prophylaxis and treatment of
acute attacks of malaria. Treatment of
extraintestinal amebiasis. Unlabeled Use:
Treatment of severe rheumatoid arthritis.
Treatment of systemic lupus erythematosus.
Contraindications:
Hypersensitivity; Hypersensitivity to other 4-
aminoquinolones (hydroxychloroquine);
Visual damage caused by chloroquine or
other 4-aminoquinolones; Lactation:
Potential for serious adverse reactions in
nursing infants. Use Cautiously in: Liver
disease; Alcoholism; Patients receiving
hepatotoxic drugs; Porphyria (may
exacerbate condition); Psoriasis; G6PD
deficiency (increased risk of severe
hemolysis); Bone marrow depression;
Hearing impairment; Epilepsy; OB: Although
safety not established, has been used; Pedi:
Extremely sensitive to chloroquine effects;
Geri: May be predisposed to adverse
effects.
Side Effects:
CNS: anxiety, agitation, confusion, delirium,
depression, hallucinations, headache,
insomnia, personality changes, polyneuritis,
psychosis. EENT: corneal opacities
(reversible), hearing impairment,
retinopathy, tinnitus, visual disturbances.
CV: cardiomyopathy, ECG changes (T-wave
abnormalities, QRS prolongation),
hypotension. GI: abdominal cramps,
anorexia, diarrhea, hepatitis, increase liver
enzymes, nausea, vomiting. Derm:
alopecia, dermatoses, photosensitivity,
pigmentary changes, pruritus, skin
eruptions, urticaria. Hemat:
thrombocytopenia. Euro: neuromyopathy,
peripheral neuritis, weakness.
Adverse Reaction:
CNS: Seizures. Derm: Stevens-Johnson
Syndrome, Toxic Epidermal Necrolysis.
Hemat: Agranulocytosis, Aplastic Anemia,
Leukopenia.
Nursing Responsibilities:
Assessment:
● Determine a baseline for future
reference that includes current symptoms
of disease prior to administration.
● Assess deep tendon reflexes
periodically to determine muscle
weakness. If weakness occurs,
discontinue therapy.
● Discontinue therapy immediately if
hearing impairment develops.
● Perform ophthalmologic exam initially
and periodically during therapy;
discontinue therapy immediately if visual
disturbances develop.
● Observe for development of rash.
Discontinue chloroquine at the first sign
of skin reactions. Serious adverse
reactions such as Stevens-Johnson
syndrome or toxic epidermal necrolysis
preclude further use.
Potential Nursing Diagnoses:
● Risk for infection (Indications)
● Chronic pain (Indications)
● Deficient knowledge, related to
medication regimen (Patient/Family
Teaching)
Implementation:
● For malaria suppression/prophylaxis,
chloroquine therapy should be started 2
wk prior to potential exposures and
continued for 8 wk after leaving the area.
● PO: Administer with meals to minimize
GI distress.
Evaluation/Desired Outcomes:
● Prevention of or improvement in signs
and symptoms of malaria.
● Regression of extraintestinal amebic
disease.
● Decrease in the symptoms and
progression of rheumatoid arthritis and
systemic lupus erythematosus.
Drug Classification: ANTHELMINTICS
Brand Name: Albenza
Generic Name: Albendazole
Recommended Dosage, Route, and
Frequency:
Hydatid Disease
PO (Adults and Children 60 kg): 400 mg
twice daily with meals for 28 days, followed
by 14 days off, for a total of 3 cycles.
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PO (Adults and Children 60 kg): 15
mg/kg/day given in 2 divided doses with
meals (maximum daily dose 800 mg) for 28
days, followed by 14 days off, for a total of 3
cycles.
Neurocysticercosis
PO (Adults and Children 60 kg): 400 mg
twice daily with meals for 8– 30 days.
PO (Adults and Children 60 kg): 15
mg/kg/day given in 2 divided doses with
meals (maximum daily dose 800 mg) for 8–
30 days.
Drug Action:
Inhibits tubulin polymerization, resulting in
the loss of cytoplasmic microtubules.
Therapeutic Effects: Death of the affected
larval form of susceptible parasites.
Spectrum: Echinococcus granulosus (dog
tapeworm). Taenia solium (pork tapeworm).
PHARMACOKINETICS:
Absorption: Poorly absorbed following oral
administration because of extensive first-
pass hepatic metabolism, resulting in rapid
conversion to albendazole sulfoxide, the
active metabolite.
Distribution: Widely distributed. Protein
Binding: 70% bound to plasma proteins.
Metabolism and Excretion: After
conversion to the sulfoxide metabolite,
further hepatic metabolism to inactive
compounds occurs. 1% excreted in urine;
excretion is primarily via bile.
Half-life: Albendazole sulfoxide—8– 12 hr.
Drug-Drug and Drug-Food Interactions:
Drug-Drug: Blood levels of albendazole
sulfoxide are increased by concurrent
dexamethasone and praziquantel.
Albendazole may decrease blood levels of
theophylline.
Drug-Food: Blood levels of albendazole
sulfoxide are increased by concurrent
ingestion of a high-fat meal.
Indications:
Treatment of: Neurocysticercosis, Hydatid
disease.
Contraindications: Hypersensitivity;
Hepatic dysfunction; Patients with
neurocysticercosis involving the retina; OB:
Due to the potential for birth defects, women
of childbearing age should be cautioned
against becoming pregnant while on
albendazole or within 1 mo of completing
treatment.
Side Effects:
CNS: headache (increased in
neurocysticercosis), dizziness/vertigo,
increased intracranial pressure (increased in
neurocysticercosis). GI: abnormal liver
function tests (increased in hydatid disease),
abdominal pain (hydatid disease only),
nausea/ vomiting (increased in
neurocysticercosis). Derm: reversible
alopecia. Neuro: meningeal signs (in
neurocysticercosis only) Misc: fever
(hydatid disease only).
Adverse Reaction:
Hemat: Granulocytopenia, Agranulocytosis,
Pancytopenia
Nursing Responsibilities:
Assessment:
● Neurocysticercosis: Corticosteroids
should be administered for 1– 2 days
prior to starting albendazole to minimize
inflammatory reactions. Concurrent
corticosteroid and anticonvulsant therapy
should be administered during the first
week of albendazole therapy to prevent
cerebral hypertension and potential
seizures.
● Ophthalmic examinations should be
performed before therapy to determine
presence of retinal lesions.
● Lab Test Considerations: Monitor liver
function tests before the start of each
treatment and at least every 2 weeks
during treatment. If enzymes are
significantly elevated, discontinue
albendazole; may be reinstituted when
levels have returned to pretreatment
levels.
● Monitor WBC count before each 28-
day cycle and every 2 weeks during each
28– day cycle. Decrease in WBC count is
usually reversible upon discontinuation of
therapy. Therapy may be continued if a
decrease is moderate and does not
progress.
Potential Nursing Diagnoses:
● Risk for infection (Indications) Deficient
knowledge (Patient/Family Teaching)
Implementation:
● Therapy can be started following a
negative pregnancy test in women of
childbearing age. Administer with food
(preferably high in fat content).
Evaluation/Desired Outcomes:
● Resolution of cysts in
neurocysticercosis or hydatid disease.
Classification: NUCLEOSIDE REVERSE
TRANCRIPTASE INHIBITORS (NRTIs)
Brand Name: AZT, Retrovir
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Generic Name: Zidovudine
Recommended Dosage, Route, and
Frequency:
Management of HIV Infection
PO (Adults): 100 mg q 4 hr while awake
or 200 mg 3 times daily or 300 mg twice
daily (depends on combination and
clinical situation).
PO (Children 4 wk– 18 yr): 4– 8.9 kg– 12
mg/kg twice daily or 8 mg/kg 3 times daily;
9– 29.9 kg– 9 mg/kg twice daily or 6 mg/kg 3
times daily; 30 kg– 300 mg twice daily or
200 mg 3 times daily.
IV (Adults and Children 12 yr): 1 mg/kg
infused over 1 hr q 4 hr. Change to oral
therapy as soon as possible.
IV (Children): 120 mg/m2 q 6 hr (not to
exceed 160 mg/dose) or 20 mg/m2 /hr as a
continuous infusion.
Prevention of Maternal/Fetal
Transmission of HIV Infection
PO (Adults > 14 wk Pregnant): 100 mg 5
times daily until the onset of labor.
IV (Adults during Labor and Delivery): 2
mg/kg over 1 hr, then continuous infusion of
1 mg/kg/hr until umbilical cord is clamped.
IV (Infants): 1.5 mg/kg q 6 hr until able to
take PO.
PO (Infants): 2 mg/kg q 6 hr, started
within 12 hr of birth and continued for 6
wk.
PO (Neonates premature 30 wk
gestational age at birth): 2 mg/kg q 12 hr
then increase to q 8 hr at 4 wk of age.
PO (Neonates premature 30 wk
gestational age at birth): 2 mg/kg q 12 hr
then increase to q 8 hr at 2 wk of age.
IV (Neonates premature 30 wk gestational
age at birth): 1.5 mg/kg q 12 hr then
increase to q 8 hr at 4 wk of age.
IV(Neonates premature 30 wk gestational
age at birth): 1.5 mg/kg q 12 hr then
increase to q 8 hr at 2 wk of age.
Drug Action:
Following intracellular conversion to its
active form, inhibits viral RNA synthesis by
inhibiting the enzyme DNA polymerase
(reverse transcriptase). Prevents viral
replication.
Therapeutic Effects: Virustatic action against
selected retroviruses. Slowed progression
and decreased sequelae of HIV infection.
Decreased viral load and improved CD4
cell counts. Decreased transmission of
HIV to infants born to HIV infected
mothers.
Drug-Drug and Drug-Food Interactions:
Drug-Drug: Increase bone marrow
depression with other agents having bone
marrow–depressing properties,
antineoplastic, radiation therapy, or
ganciclovir. Increase neurotoxicity may
occur with acyclovir. Toxicity may be
increased by concurrent administration of
probenecid or fluconazole. Levels are
decreased by clarithromycin.
Indications:
HIV infection (with other antiretrovirals).
Reduction of maternal/fetal transmission of
HIV. Unlabeled Use: Chemoprophylaxis
after occupational exposure to HIV.
Contraindications: Hypersensitivity;
Lactation: Breast feeding not recommended
in HIV-infected patients.
Side Effects: CNS: headache, weakness,
anxiety, confusion, decreased mental acuity,
dizziness, insomnia, mental depression,
restlessness, syncope.GI: abdominal pain,
diarrhea, nausea, anorexia, drug-induced
hepatitis, dyspepsia, oral mucosa
pigmentation. Derm: nail pigmentation.
Endo: fat redistribution, gynecomastia.
Hemat: anemia, granulocytopenia, pure red-
cell aplasia, thrombocytosis.MS: back pain,
myopathy. Neuro: tremor's: immune
reconstitution syndrome.
Adverse Reaction: CNS: Seizures. Gi:
Hepatomegaly (with Steatosis),
Pancreatitis. F And E: Lactic Acidosis.
Nursing Responsibilities:
Assessment:
● Assess the patient for change in
severity of symptoms of HIV and for
symptoms of opportunistic infections
during therapy.
● May cause increase serum AST, ALT,
and alkaline phosphatase levels. Lactic
acidosis may occur with hepatic toxicity,
causing hepatic steatosis; may be fatal,
especially in women.
● Monitor serum amylase, lipase, and
triglycerides periodically during therapy.
Elevated serum levels may indicate
pancreatitis and require discontinuation.
● Monitor CBC every 2 wk during the first
8 wk of therapy in patients with advanced
HIV disease, and decrease to every 4 wk
after the first 2 mo if zidovudine is well
tolerated or monthly during the first 3 mo
and every 3 mo thereafter unless
indicated in patients who are
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 asymptomatic or have early symptoms.
Commonly causes granulocytopenia and
anemia. Anemia may occur 2– 4 wk after
initiation of therapy. Anemia may respond
to epoetin administration (see epoetin
monograph). Granulocytopenia usually
occurs after 6– 8 wk of therapy. Consider
dose reduction, discontinuation of
therapy, or blood transfusions if
hemoglobin is 7.5 g/dL or reduction of
25% from baseline and/or granulocyte
count is 750/ mm3 or reduction of 50%
from baseline. Therapy may be gradually
resumed when bone marrow recovery is
evident.
Potential Nursing Diagnoses:
● Risk for infection (Indications) (Side
Effects)
Implementation:
● Do not confuse Retrovir (zidovudine)
with ritonavir.
● PO: Administer doses around the
clock.
● IV: Patient should receive the IV
infusion only until oral therapy can be
administered.
Evaluation/Desired Outcomes:
● Decrease in viral load and an increase
in CD4 counts in patients with HIV.
● Delayed progression of AIDS and
decreased opportunistic infections in
patients with HIV.
● Reduction of maternal/fetal
transmission of HIV.

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