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Pharmacology & Therapeutics in

Nursing
Introduction to Drug Therapy
Linda Self
Adapted by
Dr Michelle Russell
Grouping of Drugs
• Names may reflect the conditions for which
they are used (e.g. antidepressants)
• May reflect their chemical characteristics
(benzodiazepines)
• May reflect the effects on body systems
(central nervous system depressants)
Prototype Drugs
• Individual drugs that represent groups of
drugs are called Prototypes
• May be the first drugs of this group to be
developed (e.g., penicillin for antibiotics,
morphine for opioid analgesics)
Drug Names
• Generic Name is related to the chemical name
and is independent of the manufacturer (e.g.,
sertraline)
• Trade name is designated and patented by the
manufacturer (e.g., Zoloft)
Categories of Controlled Substances
• Schedule I—not approved for medical use and
have high abuse potentials; LSD, heroin,
peyote, ecstasy (3,4 methyenedioxy-
methamphetamine)
• Schedule II—used medically. High abuse
potential (methadone, meperidine, cocaine,
pentobarbital, Tylox)
Categories of Controlled Substances
continued
• Schedule III-less potential for abuse than I and
II but may lead to psychological or physical
dependence (Vicodin, Tylenol with codeine)
• Schedule IV-drugs have some potential for
abuse (Valium, Dalmane, Klonopin)
• Schedule V-contain moderate amounts of
controlled substances. An example is Lomotil
(atropine and diphenoxylate)
Pregnancy Categories
• Cat. A-studies in pregnant women failed to
show risk to the fetus
• Cat. B- animal studies have failed to show a
risk to the fetus but there are no adequate
studies in women
• Cat. C-animal studies have shown an adverse
effect on the fetus, no adequate human
studies, benefits may outweigh risks
Pregnancy Categories cont.
• Cat. D-positive evidence of human fetal risk
• Cat. X-animal or human studies have shown
fetal abnormalities or toxicity
Pharmacokinetics
• Involves drug movement through the body to
reach sites of action, metabolism, and
excretion
• Specific processes are absorption, distribution,
metabolism and excretion
Pharmacokinetics-Drug Transport Pathways

• Three main pathways of drug movement


across cell membrances
1. Most common is direct penetration by lipid
soluble drugs
2. 2nd pathway involves passage through
protein channels. Gates open and close
either by voltage gating or by assist of
chemical substances (Na+ and K+ ions
affecting some cardiac drugs)
Drug Transport Pathways cont.
3. 3rd is by carrier proteins that transport
molecules from one side of the cell
membrane to the other. An example would
be oral drugs that carry hormones to their
sites of action
(see text for details)
Pharmacokinetics
• Absorption-process that occurs from the time
a drug enters the body to the time it enters
the bloodstream to be circulated
• Factors affecting absorption include: dosage
form, route of administration, blood flow to
the site of administration, gastrointestinal
function, presence of food or other drugs
• For many medications, food in the stomach
slows absorption
Bioavailability
• Is the portion of a dose that reaches the
systemic circulation and is available to act on
body cells
• IV administration is 100% bioavailable
• Subcutaneous administrations has more rapid
absorption than does the oral route
• Mucous membranes allow for rapid and direct
absorption into the bloodstream
Distribution
• Involves the transport of drug molecules
within the body
• After the drug is absorbed into the
bloodstream, it is carried by the blood or
tissue fluids to its sites of pharmacologic
action, metabolism and excretion
• Protein binding is an important factor in drug
distribution
Distribution cont.
• Drug distribution into the CNS is limited because of
the blood-brain barrier
• Blood-brain barrier is composed of capillaries with
tight walls which limits movement of drug molecules
into brain tissue
• Only drugs that are lipid soluble or have a transport
system can cross the blood-brain barrier and reach
therapeutic concentrations in brain tissue
Distribution cont.
• Drug distribution during pregnancy and
lactation is unique as most drugs cross the
placenta or in the case of lactation, pass into
breast milk
Protein binding
• Most drugs form a compound with plasma proteins,
mainly albumin, which act as carriers
• Only the free or unbound portion of a drug acts on
body cells
• As unbound drug acts on cells, the decrease in
plasma drug level causes some of the bound drug to
be released
• Protein binding allows a part of a drug dose to be
stored and released as needed
Metabolism
• Method by which drugs are inactivated or
biotransformed by the body
• Some drugs yield metabolites that are also
active and exert effects on the body until they
are excreted (normeperidine)
• Most drugs are lipid soluble which aids their
passage across the cell membrane
Metabolism cont.
• Excretion usually is by kidneys. Need to be
water soluble for this to occur. Thus, one
function of metabolism is to convert fat
soluble medications to water soluble ones.
• Hepatic drug metabolism or clearance is a
major mechanism for terminating drug action
and eliminating drug molecules from the body
Metabolism cont.
• Most drugs are metabolized by the
cytochrome P450 enzymes in the liver
• Liver contains complex system of enzymes,
three of which are key in the metabolism of
medications/drugs
Cytochrome p450
• CYP enzymes catalyze the chemical reactions which
ultimately metabolize the medications
• With chronic administration (greater than 1-3
weeks), some drugs stimulate hepatocytes to
produce larger amounts of drug metabolizing
enzymes (inducers). Enzyme induction accelerates
drug metabolism. Result is that larger doses of the
drug may be need for therapeutic effects.
Cytochrome p450
• Enzyme inhibition may occur with concurrent
administration of two or more drugs that compete
for the same metabolizing enzymes (e.g., Dilantin,
EES, Tagamet)
• Oral meds are generally absorbed by the GI tract and
carried to the liver. Drug may undergo extensive
metabolism leaving little for systemic use. This is
called the first pass effect.
Excretion
• Refers to the elimination of a drug from the
body
• Most are excreted by the kidneys although
some are excreted in the bile then the feces
Serum Drug Levels
• Lab measurement of the amount of a drug in
the blood at a particular time
• Minimum effective concentration (MEC)-must
be present before a drug exerts its
pharmacologic action on body cells
• Duration of action-time during which serum
drug levels are at or above the MEC (may
measure serum drug levels when the drugs
have a low therapeutic index)
Pharmacodynamics--Receptors
• Involves drug actions on target cells and the
resulting alterations in cellular biochemical
reactions
• Most drugs chemically bind with receptors at
the cellular level
• Drug-receptor complex initiates
physiochemical reactions that stimulate or
inhibit cellular functions
Pharmacodynamics-receptors
• Receptors vary in type, location, number and
functional capacity
• When drug molecules chemically bind with
cell receptors, pharmacologic effects result
from agonism or antagonism
Pharmacodynamics-receptors
• Agonists-are drugs that produce effects similar to
those produced by naturally occurring hormones,
neurotransmitters and others. Agonists may
accelerate or slow normal cellular processes
depending on the type of receptor activated.
• Antagonists—drugs that inhibit cell function by
occupying receptor sites.
• Not all drugs act on receptors. Examples include:
antacids, osmotic diuretics, chelators.
Variables that affect drug actions
• Dosage
• Route
• Drug-diet interactions. Food may slow
absorption or foods may actually interact with
certain medications (tyramine and MAO
inhibitors; tetracycline and milk products;
ingestion when taking certain
antihypertensive medications)
Variables affecting drug actions
• Drug-drug interations-additive effects such as
seen with sedatives and ethanol. Synergism as
seen with acetaminophen and codeine.
• Antidote—drug can be given to antagonize the
toxic effects of another drug
Variables that affect drug actions
• Age
• Pregnancy
• Body weight
• Gender-hormonal effects
• Pathologic conditions
• Placebo response
• Temperature
Variables that affect drug actions
• Genetics-hepatic drug metabolizing
enzymes===acetyltransferase. Rapid acetylators may
need larger than usual dosages and conversely,
smaller doses if slow acetylators
• Glucose-6-phosphate deficiency—develop hemolytic
anemia if take antimalarials or sulfonamides
• Ethnicity—ACE inhibitors in African Americans
• Tolerance and cross tolerance
Adverse effects of drugs
• CNS
• GI
• Hematologic-anticonvulsants
• Hepatic-acetaminophen, INH
• Nephrotoxicity-aminoglycosides, NSAIDS
• Hypersensitivity
• Drug fever-fever associated w/administration of
some antimicrobials, atropine or TCAs
Adverse Drug Effects
• Drug dependency
• Idiosyncrasy
• Carcinogenicity
• Teratogenicity
Toxicology—Drug Overdosage
• General management
1. CPR
2. ETT
3. IV
4. Check blood sugar, drug screen, liver and kidney
function
5. Charcoal
6. Narcan or possible antidotes
7. May alkalinize the urine to prevent kidney damage
Antidotes for Selected Therapeutic Drugs

• Acetaminophen-mucomyst
• Digoxin-digibind
• Beta blockers-Glucagon (increases myocardial
contractility)
• Phenothiazines-benadryl (EPS)
• Coumadin-vitamin K
• Heparin-protamine sulfate
Antidotes cont.
• Benzodiazepines—flumazenil
• Cholinergics-atropine
• Calcium channel blockers—calcium gluconate
General Principles of accurate drug
administration
1. Right patient
2. Right drug
3. Right formulation
4. Right equipment
5. Right dose
6. Right route
7. Right time and frequency
8. Right storage
9. Right disposal
10. Right documentation
General Principles cont.
• Follow the ‘rights’ consistently
• Learn essential information about each drug
• Interpret prescriber’s orders correctly
• Read labels for right medication and
concentration
Drug Administration
• Minimize the use of abbreviations
• Calculate dosages correctly
• Measure doses accurately
• Use appropriate anatomic landmarks to
identify sites of IM injections-follow
manufacturers recommendations
• Verify client identity
Drug Administration
*****Seek information about the client’s
medical diagnoses and condition in relation to
drug administration
• Be especially vigilant with children to avoid
errors
• Ensure drug is safe for geriatric use
Legal Responsibilities
• Nurse is legally responsible for safe and accurate
administration of medications

• Nurse is expected to have sufficient drug knowledge


to recognize and question erroneous orders

• Unit dose wrappings of oral drugs should be left in


place until the nurse is in the presence of the client
and ready to administer the medication
Medication Orders
• Include the full name of the patient
• Generic or trade name of the drug
• The dose, the route and frequency of
administration
• Date, time and signature of the prescriber
Common abbreviations
• PO
• IM
• IV
• SL
• Sub q
Times of Drug Administration
• AC
• Ad lib
• bid, tid, qid
• HS
• PC
• PRN
• Stat
Drug Dosages
• cc/ml
• g
• Gr
• gtt
• mL
• oz
• Tsp
• tbsp
Routes of Administration
• Oral, buccal, sublingual
• Via GI tube
• Parenteral-IM, IV and sub q
• Topical
• Rectal
• Otic, nasally, ophthalmic
• vaginal
Sites for injections
• Sub q-abdomen, thighs, back ,belly and upper
arms
• IM-deltoid, dorsogluteal, ventrogluteal and
vastus lateralis muscles
• IV-antecubital, hands, arms, external jugular
• Others: intradermal, intra-articular, intra-
arterial and intrathecal
Equivalents
• Metric
• Apothecary
• Household
Drug administration cardinal rules
• Wash hands before giving meds
• Read MAR carefully. If ever in doubt, check the
original order
• Never give medications you are uncertain of
unless you have looked them up or have
consulted with pharmacy
Drug Administration Cardinal Rules
• Never give more than 3cc per IM injection
• Wear gloves with all injections
• For sub q injections, use 25G, 5/8” needles
• Do not give oral meds if patient is vomiting,
sedated, NPO or is unconscious
• Follow narcotic protocol for signing out of
narcotics
Nursing Process in Drug Therapy
• Is a systematic way of gathering and using
information to plan and provide individualized
client care and to evaluate the outcomes of care
• Five steps of the nursing process are:
1. assessment,
2. nursing diagnosis
3. planning,
4. interventions
5. evaluation
General Principles of Drug Therapy
• Expected benefits should outweigh potential
adverse effects
• Drug therapy should be individualized
• Drug effects on quality of life should be
considered in designing a drug therapy
regiment
Drug selection and dosage
• Use as few drugs as possible
• Fixed dose combinations increase compliance
• Lowest dose with therapeutic effect
• Follow guidelines but dosages must be
individualized
• Drugs with long half-lives may require loading
doses then titrated lower maintenance doses
Drug Therapy in special populations-
pediatrics
• Pediatrics-all aspects must be guided by the
child’s age, weight and level of growth and
development
• Safe therapeutic ranges are less well-defined
• Choice of drug is restricted because many
drugs used in adults have not been sufficiently
investigated
Pediatric physiologic characteristics
affecting pharmacokinetics
• Thin, permeable skin –increased absorption of
topicals
• Immature blood-brain barrier—increased
distribution into the CNS until age 2
• Altered protein binding until age 1
• Decreased activity of metabolizing enzymes in
infants, increased in children
Pediatric physiologic effects
• Increased percentage of body water
• Decreased GFR until one year of age
Pediatrics
• Oral route for meds is preferable
• For injections, may wish to use topical EMLA
(eutectic mixture of lidocaine and prilocaine,
local anesthetics)
• Site selection for injections—infants, use thigh
muscles; older than 18 months of age, use
deltoid; older than 3, use ventrogluteal muscle
Drug Therapy in Older Adults
Physiologic characteristics and
pharmacokinetic impact
• Decreased GI motility—slower absorption
• Decreased cardiac output—slower absorption
from site of administration, decreased
distribution to sites of action in tissues
• Decreased blood flow to liver and kidneys-
delayed metabolism and excretion
Drug Therapy in Older Adults
• Decreased total body water and lean body
mass-fat soluble meds stay with patient
longer, water soluble drugs are distributed in
smaller area, greater risk for toxicity
• Decreased blood flow to liver-slowed
metabolism and detox of drugs
Drug Therapy in Older Adults
• Decreased albumin-decreased availability of
protein for binding and transporting. Will also
have higher concentration of free active drug.
• Decreased blood flow to kidneys—impaired
drug excretion, potential toxicity
Older Adults
Renal Impairment
• Know baseline renal function
• Tailor dosages
• Avoid nephrotoxic medications
• Be aware of need for additional dosing if
patient is receiving renal replacement therapy
Older Adults
Hepatic Impairment
• Those with cirrhosis, hepatitis, receiving hepatotoxic
drugs, have heart failure, are undergoing major
surgery or have had trauma are at higher risk for
toxicities r/t medications
• Know drug effects on hepatic function
• Reduce dosages on medications that are extensively
metabolized by the liver such as: cimetidine,
phenytoin, ranitidine, theophylline
Older Adults
Critical Illnesses
• Be aware that all medications may have
variable effects in this scenario
• Know the actions, usual dosages and side
effects of medications
• Closely monitor renal and liver function tests
• Monitor serum protein and albumin levels
Older Adults
Critical Illness
• Most drugs will be given IV-for this reason,
medications may have faster onset
• Many factors may interfere with drug effects if
given orally
• Considerations when giving medications via
feeding tube
• Appropriate scheduling very important
Drug Therapy in Home Care
• On patient’s turf
• Schedule visit at convenient time for patient
and caregiver
• Assess patient’s ability to perform self-care or
if caregiver needed
• Assess patient’s understanding and attitude
regarding medication regimen
• Inquire if patient is taking any herbal
preparations or teas
Drug Therapy in Home Care
• Inquire if patient is taking any OTC meds
• Assess environment for safety
• Educate patient and caregiver indication,
proper administration and side effects of
administered medications
• Between visits, maintain contact with patient
to monitor progress and serve as a resource
Herbal and Dietary Supplements
• Black cohosh-used to relieve menopausal s/s
• Capsaicin-post-herpetic neuralgia
• Echinacea-anti-infective, for common cold
• Ginger—nausea. Not for morning sickness.
• Garlic-cholesterol lowering
• Moringa – cure all
• Guinea hen weed – prostate and cancers
• Turmeric – fibroids and antiinflamatory
Herbal and Dietary supplements
• Feverfew-for migraines, menstrual complaints.
Can cause withdrawal s/s.
• Ginseng-increase stamina, endurance and
mental acuity. Can affect bleeding time, BP,
increase hypoglycemia. No longer than 3
weeks use with Siberian ginseng.
Questions
• Define these Medical terms in your notes
• Antagonism
• Accumulation
• Habituation vs addiction
• Hypersensitivity
• Idiosyncrasy
• Poison
• Synergism - potentiation

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