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reserpine (Serpasil, Apoplon)
Tradename: Serpasil.
Indication:
- management of mild to moderate hypertension
Dosage:
1) start 0.5 mg PO QD for 1-2 weeks
2) maintenance: 0.1-0.25 mg/day
Tabs: 0.1, 0.25, 1 mg.
Pharmacokinetics:
1) full antihypertensive effects are delayed for 2-3 weeks
2) distributed to many body tissues including adipose tissue
3) metabolized to inactive components
4) excreted in the urine & feces
5) 1/2life is 11.3 days; increased in obese patients
6) duration of action is 24 hours to 2-6 weeks
Adverse effects:
1) common (> 10%)
- dizziness, anorexia, diarrhea, dry mouth, nasal congestion, nausea/vomiting
2) less common (1-10%)
- peripheral edema, arrhythmias, melena, hematemesis, bradycardia, chest pain, headache, impotence
3) uncommon (< 1%)
- rash, difficulty urinating, trembling of hands & fingers, hypotension, drowsiness, fatigue, depression, parkinsonism, Na+ & water retention, increased gastric acid secretion
4) other
- lethargy
- abdominal pain
- activation of peptic ulcer disease
- NO rebound hypertension on discontinuation [5]
Drug interactions:
1) cardiac glycosides (digoxin): predisposition to cardiac arrhythmias
2) MAO inhibitors: excitation & hypertension
3) CNS depressants: additive CNS effects
4) sympathomimetic agents: enhances pressor effects
Mechanism of action:
1) binds tightly to storage vesicles in central & peripheral adrenergic neurons
2) storage vesicles become destroyed & nerve endings lose ability to concentrate & store norepinephrine & dopamine
3) depletes norepinephrine from post-ganglionic adrenergic neurons
4) reduces cardiac output & peripheral vascular resistance
Interactions
drug interactions
drug adverse effects of antihypertensive agents
General
adrenergic neuron inhibitor
Properties
MISC-INFO: elimination route LIVER
KIDNEY
pregnancy-category C
safety in lactation -
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 8th ed.
Gilman et al, eds. Permagon Press/McGraw Hill
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Medical Knowledge Self Assessment Program (MKSAP) 11, American
College of Physicians, Philadelphia 1998
- Deprecated Reference
Component-of
chlorothiazide/reserpine
chlorthalidone/reserpine
hydralazine/hydrochlorothiazide/reserpine; hydralazine/HCTZ/reserpine (Ser Ap Es)
hydrochlorothiazide/reserpine
hydroflumethiazide/reserpine
methyclothiazide/reserpine
polythiazide/reserpine
reserpine/thiazide