reserpine (Serpasil, Apoplon)

Introduction

Tradename: Serpasil.

Indications

• management of mild to moderate hypertension

Dosage

• start 0.5 mg PO QD for 1-2 weeks
• maintenance: 0.1-0.25 mg/day

Tabs: 0.1, 0.25, 1 mg.

Pharmacokinetics

• full antihypertensive effects are delayed for 2-3 weeks
• distributed to many body tissues including adipose tissue
• metabolized to inactive components
• excreted in the urine & feces
• 1/2life is 11.3 days; increased in obese patients
• duration of action is 24 hours to 2-6 weeks

elimination via liver

elimination via kidney

Adverse effects

• common (> 10%)
  • dizziness, anorexia, diarrhea, dry mouth, nasal congestion, nausea/vomiting
• less common (1-10%)
  • peripheral edema, arrhythmias, melena, hematemesis, bradycardia, chest pain, headache, impotence
• uncommon (< 1%)
  • rash, difficulty urinating, trembling of hands & fingers, hypotension, drowsiness, fatigue, depression, parkinsonism, Na+ & water retention, increased gastric acid secretion
• other
  • lethargy
  • abdominal pain
  • activation of peptic ulcer disease
  • NO rebound hypertension on discontinuation

• drug adverse effects of antihypertensive agents

Drug interactions

• cardiac glycosides (digoxin): predisposition to cardiac arrhythmias
• MAO inhibitors: excitation & hypertension
• CNS depressants: additive CNS effects
• sympathomimetic agents: enhances pressor effects

• drug interaction(s) of NSAIDs & antihypertensives

Mechanism of action

• binds tightly to storage vesicles in central & peripheral adrenergic neurons
• storage vesicles become destroyed & nerve endings lose ability to concentrate & store norepinephrine & dopamine
• depletes norepinephrine from post-ganglionic adrenergic neurons
• reduces cardiac output & peripheral vascular resistance

More general terms

• adrenergic neuron inhibitor

Component of

• polythiazide/reserpine
• methyclothiazide/reserpine
• hydroflumethiazide/reserpine
• hydrochlorothiazide/reserpine
• chlorthalidone/reserpine
• chlorothiazide/reserpine
• reserpine/thiazide
• hydralazine/hydrochlorothiazide/reserpine; hydralazine/HCTZ/reserpine (Ser Ap Es)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5770
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5052
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5326170
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=121434
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3084265