Prostigmin

Indikasi
Atonic constipation before radiographic
examinations; postoperative intestinal atony and
urine retention; myasthenia gravis
pseudoparalytica; curare antagonism (reversal of
the effects of curare and curare-like,
nondepolarizing muscle relaxants).
 Side effect
Prostigmin can have undesirable functional effects
on the autonomic nervous system (ANS).
Muscarinic effects can include nausea, vomiting,
diarrhea, stomach cramps, increased peristalsis
and bronchial secretion, salivation and
lacrimation, bradycardia and miosis. The primary
nicotinic effects are muscle spasms, fasciculations
and muscular weakness.
 Dosis
Standard Dosage: Atonic Constipation, Meteorism (eg,
before radiographic examination): Adults: to one 1 mL
ampule (0.25-0.5 mg) SC or IM. Children: - of a 1 mL
ampoule (0.125-0.25 mg) SC or IM. In children, it may be
advisable to administer a glycerin (50 mL, 10%) or saline (20
mL, 10%) enema a -hr after injection of Prostigmin.
Postoperative Intestinal Atony and Urine Retention:
Prophylaxis: of a 1 mL ampule (0.25 mg) SC or IM
immediately after surgery; repeat this dose every 4-6 hrs as
required.
Treatment: Adults: One 1 mL ampule (0.5 mg) SC, IM or by
very slow IV injection; if necessary, repeat this dose at 4- to
5-hr intervals. Children: - of a 1 mL ampule (0.125-2.5
mg) SC or IM.
 Myasthenia Gravis Pseudoparalytica: Parenteral doses
adjusted to the degree of disability. Oral co-medication with
Mestinon (pyridostigmine) may be advisable.
Curare Antagonism (reversal of the effects of curare and
curare-like, nondepolarizing muscle relaxants): 1-5 mg IM
and/or slow IV injection, possibly with prior combination of
0.4-1.2 mg atropine sulfate to reduce cholinergic side effects
eg, bradycardia and hypersecretion.
Atropine and neostigmine must not be injected with the
same syringe. (see Incompatibilities under Interactions).
The above doses must not be exceeded even in cases of
curare overdosage.
Special Dosage Instructions: Longer dosage intervals or
lower repeat doses may be indicated in patients with
impaired renal function.
 Onset : 2-5 menit
Durasi : 30 60 menit
 Lidocain
Dosis
Epidural
Epidural anaesthesia
Adult: 2-3 mL administered for each dermatome to be anaesthesised.
Recommended doses are: Lumbar epidural 250-300 mg (as 1% soln) for analgesia
and 225-300 mg (as 1.5% soln) or 200-300 mg (as 2% soln) for anaesth; for thoracic
epidural: 200-300 mg (as 1% soln). For obstetric caudal analgesia, 200-300 mg (as
1% soln); for surgical caudal anaesth: 225-300 mg (as 1.5% soln). For continuous
epidural or caudal anaesth, not to repeat max doses more frequently than 1.5 hrly.

Intramuscular
Emergency treatment of ventricular arrhythmias
Adult: 300 mg injected into the deltoid muscle, repeat after 60-90 min if necessary.
 Intraspinal
Spinal anaesthesia
Adult: As hyperbaric soln of 1.5% or 5% lidocaine
in 7.5% glucose soln. Normal vaginal delivery: Up
to 50 mg (as 5% soln) or 9-15 mg (as 1.5% soln).
Caesarian operation: Up to 75 mg (as 5% soln).
Other surgical procedures: 75-100 mg.
 Intravenous
Pulseless ventricular fibrillation or ventricular tachycardia
Adult: 1-1.5 mg/kg repeated as necessary. Max: 3 mg/kg. For
ventricular arrhythmias in more stable patients: Usual loading dose:
50-100 mg as an IV inj at 25-50 mg/min, may repeat once or twice
up to a max of 200-300 mg in 1 hr, followed by 1-4 mg/min via
continuous IV infusion. May need to reduce dose if the infusion is
longer than 24 hr.

Intravenous
Intravenous regional anaesthesia
Adult: As 0.5% soln w/o epinephrine: 50-300 mg. Max: 4 mg/kg.
 Topical/Cutaneous
Surface anaesthesia
Adult: As 5% oint: Max: 20 g in 24 hr for skin and mucous
membrane. As 2% gel: Approx 120-220 mg into urethra
several min before examination. As 4% foam: Apply 3-4
times daily for pain relief. As soln: Apply 40-200 mg to
affected area. As patch: Apply patch to painful area for up
to 12 hr w/in a 24-hr period. Max: 1 patch/24 hr.

Transdermal
Postherpetic neuralgia
Adult: As 5% patch: Apply to most painful area once daily
for up to 12 hr w/in a 24-hr period. Max: Up to 3 patches in
a single application.
 Kontraindikasi
Hypovolaemia, complete heart block, Adam-
Stokes syndrome, Wolff-Parkinson-White
syndrome. Must not be applied to inflamed or
injured skin.
 Description: Lidocaine is an amide type local
anaesth. It stabilises the neuronal membrane
and inhibits Na ion movements, which are
necessary for conduction of impulses. In the
heart, lidocaine reduces depolarisation of the
ventricles during diastole and automaticity in the
His-Purkinje system. Duration of action potential
and effective refractory period are also reduced.
Onset: 45-90 sec (IV); approx 4 hr (transdermal);
20 sec to 5 min (ophth). .
Duration: 10-20 min (IV); 5-30 min (ophth).
 Pharmacokinetics:
Absorption: Readily absorbed from the GI tract,
mucous membranes, damaged skin, inj sites, including
muscle; poor absorption through intact skin.
Distribution: Crosses the placenta, blood-brain barrier
and enters breast milk. Protein-binding: 66% (1-acid
glycoprotein).
Metabolism: Undergoes rapid metabolism and approx
90% is dealkylated to monoethylglycinexylidide and
glycinexylidide. First-pass metabolism is extensive.
Excretion: Via urine (<10% unchanged). Elimination
half-life: biphasic; initial: 7-30 min; terminal: 1.5-2 hr.
 Side effect
Arrhythmia, bradycardia, arterial spasms, CV collapse,
oedema, flushing, hert block, hypotension, sinus node
suppression, agitation, anxiety, coma, confusion, drowsiness,
hallucinations, euphoria, headache, hyperaesthesia,
hypoaesthesia, lightheadedness, lethargy, nervousness,
psychosis, seizure, slurred speech, unconsciousness,
somnolence, nausea, vomiting, metallic taste, tinnitus,
disorientation, dizziness, paraesthesia, resp depression and
convulsions. Patch: Bruising, depigmentation, petechiae,
irritation. Ophth: Conjunctival hyperaemia, corneal epithelial
changes, diplopia,visual changes.
 Marcain
Bupivacaine HCl

Indikasi
Surgical anesth eg, epidural block, field block
(minor & major nerve blocks & infiltration),
analgesia (minor nerve block & infiltration);
analgesia in post-op pain or labor pain.
 Dosis
Adult 400 mg single dose daily. Surgical anesth: Lumbar
epidural (abdominal, pelvic & lower limb surgery including
caesarean section) 75-150 mg (5 mg/mL); thoracic epidural
(upper abdominal) 12.5-37.5 mg (2.5 mg/mL); thoracic
surgery 25-50 mg (5 mg/mL); caudal epidural 37.5-100 mg
(2.5 mg/mL) &/or 75-125 mg (5 mg/mL); other blocks (local
infiltration) 12.5-150 mg (2.5 mg/mL) or 25-150 mg (5
mg/mL); intercostal (per segment) 10-20 mg (2.5 mg/mL) or
15-25 mg (5 mg/mL); brachial plexus 100-150 mg (5 mg/mL);
sciatic 3 in 1 (femoral obturator & lateral cutaneous) 50-100
mg (5 mg/mL); pudendal 7.5-100 mg (2.5-5 mg/mL).
 Dosis
Analgesia: Caudal epidural (post-op pain
management) 50-75 mg bolus (2.5 mg/mL); lumbar
epidural (bolus & continuous infusion) 15-60 mg
bolus (2.5-5 mg/mL) followed by 12.5-18.75 mg/hr
(1.25-2.5 mg/mL); thoracic epidural (continuous
infusion for post-op pain management) 6.25-12.5
mg/hr (1.25 mg/mL). Childn Calculate dose based
on wt up to 2 mg/kg, adrenaline may be added to
prolong duration of the block by 50-100%.
 Side effect
Pronounced acidosis, hypokalaemia or hypoxia
may increase the risk of severity of toxic reaction.
CNS, CV effects. Cutaneous lesions, urticaria,
edema or anaphylactoid reactions.
 Onset: 5 min
Durasi: 2-4 jam
 Buscopan
Dosis
Oral
Gastrointestinal tract spasm, Genitourinary spasm
Adult: As butylbromide: 20 mg 4 times daily.
Child: As butylbromide: 6-12 yr: 10 mg tid.

Parenteral
Gastrointestinal tract spasm, Genitourinary spasm
Adult: As butylbromide: 20 mg IM/IV repeated after 30 min
if needed. Max: 100 mg daily.
 Parenteral
Premedication before anaesthesia
Adult: As hydrobromide: 0.2-0.6 mg via SC or IM
inj 30-60 minutes before induction of anesth.
Child: As hydrobromide: 15 mcg/kg via SC or IM
inj, 30-60 minutes before induction of anesth.
 Subcutaneous
Preoperative sedation
Adult: As hydrobromide: 0.6 mg 3-4 times daily.

Subcutaneous
Prophylaxis of nausea and vomitting
Adult: As hydrobromide: 0.3-0.6 mg.
Child: As hydrobromide: 0.006 mg/kg.

Transdermal
Prophylaxis of motion sickness
Adult: As patch delivering 1 mg over 3 days: Apply 1 patch at
least 4 hr before exposure to motion. To be applied behind the
ear.
 Side effect
Flushing, postural hypotension, tachycardia, fibrillation. Rarely
psychotic reactions. Dizziness, drowsiness, fatigue, headache,
memory loss. Dry skin, erythema, increased sensitivity to light,
rash. Bloatedness, constipation, dry throat, dysphagia, nausea,
vomiting, xerostomia. Dysuria, urinary retention. Tremor,
weakness. Impaired accommodation, blurred vision, cycloplegia,
dryness, narrow-angle glaucoma, increased intraocular pain,
itching, photophobia, pupil dilation. Dry nose. Decreased
diaphoresis, heat intolerance. Ophthalmic: Somnolence,
dermatitis, oedema, exudate, follicular conjunctivitis, increased
IOP, local irritation, photophobia, vascular and respiratory
congestion.
 Potentially Fatal: CNS depression, coma, circulatory and
respiratory failure. Flushing, postural hypotension, tachycardia,
fibrillation. Rarely psychotic reactions. Dizziness, drowsiness,
fatigue, headache, memory loss. Dry skin, erythema, increased
sensitivity to light, rash. Bloatedness, constipation, dry throat,
dysphagia, nausea, vomiting, xerostomia. Dysuria, urinary
retention. Tremor, weakness. Impaired accommodation,
blurred vision, cycloplegia, dryness, narrow-angle glaucoma,
increased intraocular pain, itching, photophobia, pupil dilation.
Dry nose. Decreased diaphoresis, heat intolerance.
Ophthalmic: Somnolence, dermatitis, oedema, exudate,
follicular conjunctivitis, increased IOP, local irritation,
photophobia, vascular and respiratory congestion.
Potentially Fatal: CNS depression, coma, circulatory and
respiratory failure.
 Description: Hyoscine competitively blocks muscarinic receptors
and has central and peripheral actions. It relaxes smooth muscle
and reduces gastric and intestinal motility.
Onset: Oral, IM: 0.5-1 hr; IV: 10 min.
Duration: Oral, IM: 4-6 hr; IV: 2 hr.
Pharmacokinetics:
Absorption: Tertiary salts: Readily absorbed. Quaternary salts:
Poorly absorbed.
Distribution: Reversibly bound to plasma proteins.
Metabolism: Hepatic.
Excretion: Via urine (as metabolites); 4.8 hr (elimination half-life).
 Nifedipine
Dosis
Adult : PO HTN Immediate-release: Initial: 5 mg
tid. Maintenance: 10-20 mg tid. Extended- release:
10-40 mg bid or 20-90 mg once daily. Angina
pectoris Immediate-release: Initial: 5 mg tid.
Maintenance: 10-20 mg tid. Extended- release: 10-
40 mg bid or 30-90 mg once daily. Raynaud's
syndrome Immediate-release: 5-20 mg tid.
 Side effect
Dizziness, flushing, headache, hypotension, peripheral
oedema, tachycardia, palpitations, nausea, constipation,
other GI disturbances, increased micturition frequency,
lethargy, eye pain, visual disturbances, syncope, vertigo,
migraine, mood disturbances, rashes (including erythema
multiforme), liver function abnormalities (including
cholestasis), pruritus, gingival hyperplasia, myalgia,
gynaecomastia, tremor, impotence, fever. Paradoxical
increase in ischaemic chest pain during initiation of
treatment. GI obstruction in some tablets covered in
indigestible membrane.
 Description: Nifedipine prevents Ca ion from entering
the slow channels of cardiac and smooth muscles
during depolarisation, producing peripheral and
coronary vasodilatation. It reduces afterload,
peripheral resistance and BP; increases coronary
blood flow and causes reflex tachycardia. It has little
or no effect on cardiac conduction and rarely has
negative inotropic activity.
Onset: Immediate-release: 15-30 min; Approx 20 min.
Durasi: 6-8 hr
 Pharmacokinetics:
Absorption: Rapidly and almost completely absorbed from the GI
tract. Absorption may be affected by food, but result vary
depending on the preparation used. Bioavailability: 45-56% (liquid-
filled cap); 65-89% (extended-release). Time to peak plasma
concentration: 30-60 min (liquid-filled cap).
Distribution: Enters breast milk. Plasma protein binding: Approx
92-98%.
Metabolism: Extensively oxidised in the liver via CYP3A4
isoenzyme. Undergoes extensive hepatic first-pass metabolism.
Excretion: Via urine (80-95% as inactive metabolites) and faeces.
Elimination half-life: Approx 2 hr (liquid-filled cap).
 Norepineprine
Dosis
Adult : IV Acute hypotensive states Initial: 8-12
mcg/min, up to 8-30 mcg/min in refractory shock.
Adjust according to BP response. Maintenance: 2-
4 mcg/min. Injection Upper GI haemorrhage
Instill 8 mg in 100 mL of 0.9% sodium chloride
soln through a nasogastric tube hrly for 6-8 hr,
then 2 hrly for 4-6 hr. Withdraw drug gradually.

 Injection
Upper gastrointestinal haemorrhage
Adult: Intraperitoneal admin: 8 mg in 250 ml of
0.9% sodium chloride inj. Alternatively, instill 8 mg
in 100 ml of 0.9% sodium chloride solution
through a nasogastric tube every hr for 68 hr,
then every 2 hr for 46 hr. Withdraw drug
gradually.
 Intravenous
Acute hypotensive states
Adult: Initially, 8-12 mcg/minute, up to 8-30
mcg/minute in refractory shock. Infuse using a solution
of 4 mcg/ml in glucose 5%, or sodium chloride 0.9%
and glucose 5% at a rate of 2-3 ml/minute. Adjust
according to BP response. Average maintenance dose:
0.5-1 ml/minute (2-4 mcg/minute). Infuse via a central
venous catheter or into a large vein.
Child: Administer at a rate of 2 mcg/minute.
Alternatively, 2 mcg/m2/minute. Adjust rate according
to BP response and perfusion.
Elderly: Initial dose should be at low end of dose range.
 Side effect
Hypertension, headache, peripheral ischaemia,
bradycardia, arrhythmias, anxiety, skin necrosis
(with extravasation), dyspnoea, respiratory
difficulty.
 Description: Norepinephrine is a direct-acting
sympathomimetic which stimulates 1- and -
adrenergic receptors. Its -agonist effects cause
vasoconstriction, thereby raising systolic and
diastolic BP with reflex slowing of heart rate.
Onset: Rapid.
Duration: Short; stops within 1-2 min after
discontinuing the infusion.
 Pharmacokinetics:
Absorption: Oral: Destroyed in the GI tract; SC:
Poorly absorbed.
Distribution: Mainly localises in sympathetic
nervous tissue; crosses the placenta but not the
blood-brain barrier.
Metabolism: Metabolised in the liver and in other
tissues by the enzymes catechol-O-
methyltransferase (COMT) and monoamine
oxidase (MAO).
Excretion: Via urine (mainly as metabolites).
 Doburan
(Dobutamine)
Dosis
Adult : IV Acute heart failure 2.5-10 mcg/kg/min,
adjust according to response. Dose range of 0.5-40
mcg/kg/min may be given. Cardiac stress test 5
mcg/kg/min for 8 min via infusion pump. Increase
dose by increments of 5 mcg/kg/min up to max 20
mcg/kg/min, w/ each dose being infused for 8 min
before the next increase.
 Intravenous
Acute heart failure
Adult: 2.5-10 mcg/kg/min. Dose range of 0.5-40
mcg/kg/min may be given. Adjust according to
patient's BP, heart rate, cardiac and urine output.
Child: Neonates to 18 yr Initially, 5 mcg/kg/min,
adjust to 2-20 mcg/kg/min according to response.
 Intravenous
Cardiac stress test
Adult: 5 mcg/kg/min for 8 min via infusion pump
using a soln containing 1 mg/mL. Increase dose by
increments of 5 mcg/kg/min up to max 20
mcg/kg/min, w/ each dose being infused for 8 min
before the next increase.
 Side effect
Increased heart rate, ectopic heartbeats, angina,
chest pain, palpitation, elevations in BP, skin rash,
fever, eosinophilia, bronchospasm, paraesthesia,
nausea, vomiting, tingling sensation, dyspnoea,
fever, headache, mild leg cramps pruritus of the
scalp; phlebitis at the inj site. Rarely, ventricular
tachycardia, hypokalaemia.
 Description: Dobutamine exerts positive inotropic
effect on the myocardium by stimulating 1-
adrenergic receptors, thereby increasing myocardial
contractility, stroke vol and cardiac output.
Onset: Approx 2 min.
Duration: <10 min.
Pharmacokinetics:
Absorption: Inactivated when given orally.
Metabolism: Hepatically metabolised; converted to 3-O-
methyldobutamine by COMT and via conjugation by
glucuronic acid.
Excretion: Mainly via urine; via faeces (small amounts).
Elimination half-life: Approx 2 min.
 Ketamine
Dosis
Adult : IV 1-4.5 mg/kg as inj or infuse 0.5-2 mg/kg. IM
6.5-13 mg/kg
Intramuscular
Induction of anaesthesia
Adult: 6.5-13 mg/kg. A dose of 10 mg/kg produces surgical
anaesth w/in 3-4 min after inj lasting for 12-25 min.
Increments of half to the full induction dose may be
repeated as needed for maintenance of anesth. For
diagnostic or other procedures not involving intense pain: 4
mg/kg as initial dose.
 Intravenous
Induction of anaesthesia
Adult: 4.5 mg/kg via slow IV inj over 60 sec. A
dose of 2 mg/kg produces surgical anaesth w/in
30 sec after inj lasting for 5-10 min. Increments of
half to the full induction dose may be repeated as
needed for maintenance of anesthesia.
Alternatively, a total induction dose of 0.5-2 mg/kg
via infusion, given at an appropriate rat, and
maintained at 10-45 mcg/kg/min, adjusted
according to response.

 Side effect
Emergence reactions (e.g. vivid dreams,
hallucinations, confusion, irrational behaviour);
increased muscle tone sometimes resembling
seizures; temporary HTN and tachycardia,
hypotension, bradycardia, arrhythmias, apnoea,
laryngospasm, resp depression, diplopia,
nystagmus, nausea, vomiting, lacrimation,
hypersalivation, raised intraocular and CSF
pressure, transient rash and pain at inj site, cystitis.
 Description: Ketamine is a noncompetitive N-
methyl-D-aspartate receptor antagonist that
blocks glutamate. It has a direct action on the
cortex and limbic system. It produces a
cataleptic-like state wherein the patient is
withdrawn from the surrounding environment.
Onset: 30 sec (IV); 3-4 min (IM).
Duration: 5-10 min (IV); 12-25 min (IM).
 Pharmacokinetics:
Absorption: Rapidly absorbed following parenteral
admin.
Distribution: Crosses the placenta. Volume of
distribution: 3 L/kg.
Metabolism: Hepatic biotransformation to
norketamine (active metabolite). Other metabolic
pathways include hydroxylation of the cyclohexone
ring and conjugation w/ glucuronic acid.
Excretion: Via urine as metabolites. Elimination
half-life: 10-15 min (alpha phase); 2.5 hr (beta
phase).