Reserpine

Therapeutic Class
Central Monoamine-Depleting Agent; Rauwolfia Alkaloid
Indications

Management of mild-to-moderate hypertension; treatment of agitated psychotic states (schizophrenia), Management of tardive dyskinesia.

Adult Doses

Usual dose range: 0.05-0.25 mg once daily; 0.1 mg every other day may be given to achieve 0.05 mg once daily

Hypertension: Initial: 0.1 mg once daily; adjust as necessary based on response.

Schizophrenia or tardive dyskinesia Dosing recommendations vary; initial dose recommendations generally range from 0.05-0.25 mg. May be increased in increments of 0.1-0.25 mg; maximum dose in tardive dyskinesia: 5 mg/day

Elderly: Oral: Initial: 0.05 mg once daily increasing by 0.05 mg every week as necessary; full antihypertensive effects may take as long as 3 weeks

Pediatric Doses

Hypertension:
0.01-0.02 mg/kg/24 hours divided every 12 hours;
maximum dose: 0.25 mg/day (not recommended in children)

Doses in Renal impairment

Not removed by hemo- or peritoneal dialysis; supplemental dose is not necessary

Clcr <10 mL/minute: Avoid use.

Contraindications

Active peptic ulcer or ulcerative colitis; depression; Parkinson's disease; pheochromocytoma; electroconvulsive therapy (ECT).

Warnings / Precautions

Elderly or debilitated patients; epilepsy; renal insufficiency; gallstones; allergic conditions; cardiac arrhythmias; MI. Maintain an interval of at least 7-14 days between the last dose of reserpine and start of ECT.

Adverse Reactions

Nasal congestion; headache; CNS disorders; GI disturbances; breast engorgement, galactorrhoea; gynaecomastia, decreased libido, impotence, Na retention, oedema, decreased or increased appetite; weight gain, miosis, dry mouth, sialorrhoea, dysuria, rashes, pruritus, thrombocytopaenic purpura.

Overdose Reactions

Signs include CNS depression ranging from drowsiness to coma.

Drug Interactions

Hypotensive effects enhanced by thiazide diuretics and other antihypertensives. May cause excitation and hypertension with MAOIs. May cause cardiac arrhythmias with digitalis or quinidine. Effects of CNS depressants may be enhanced. May decrease patient's response to levodopa.

Lab Interactions

May cause a slight increase in urinary 5-hydroxyindoleacetic acid excretion. May also interfere with colorimetric assay procedures for the determination of urinary 17-hydroxycorticosteroids by the Glenn-Nelson technique and 17-ketosteroids by the Holtorff Koch modification of the Zimmerman reaction.

Food Interactions

Ethanol: May increase CNS depression; monitor for increased effects with coadministration. Caution patients about effects.

Herb/Nutraceutical: Avoid dong quai if using for hypertension (has estrogenic activity). Avoid ephedra, yohimbe (may worsen hypertension). Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression). Avoid garlic (may have increased antihypertensive effect).

Mechanism of Actions

Reduces blood pressure via depletion of sympathetic biogenic amines (norepinephrine and dopamine); this also commonly results in sedative effects

Metabolism

Inhibits P-glycoprotein

Pharmacodynamics

Onset of action: Antihypertensive: 3-6 days

Duration: 2-6 weeks

Absorption: ~40%

Distribution: Crosses placenta; enters breast milk

Protein binding: 96%

Metabolism: Extensively hepatic (>90%)

Half-life elimination: 50-100 hours

Excretion: Feces (30% to 60%); urine (10%)

Monitoring

Blood pressure, standing and sitting/supine

Administration

Should be taken with food.

Pregnancy Category

C: Drug Pregnancy Category Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.

Lactation

Enters breast milk/use caution

Storage Conditions

Oral: Store at 20-25°C.

ATC Classification
C02AA02 - reserpine ; Belongs to the class of rauwolfia alkaloids, centrally-acting antiadrenergic agents. Used in the treatment of hypertension.
GenericPedia Classification
  • Storage

    Oral: Store at 20-25°C.

    Available As
  • Reserpine 0.1 mg
  • Reserpine 0.25 mg
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