Reserpine: Drug information
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(For additional information see "Reserpine: Patient drug information")
PHARMACOLOGIC CATEGORY
Central Monoamine-Depleting Agent
Rauwolfia Alkaloid
DOSING: ADULTS
Hypertension:
**Manufacturer's labeling: Initial: 0.5 mg/day for 1-2 weeks; maintenance: 0.1-0.25 mg/day
**Note: Clinically, the need for a "loading" period (as recommended by the manufacturer) is not well supported, and alternative dosing is preferred.
**Alternative dosing (unlabeled): Initial: 0.1 mg once daily; adjust as necessary based on response.
**Usual dose range (JNC 7): 0.05-0.25 mg once daily; 0.1 mg every other day may be given to achieve 0.05 mg once daily
Schizophrenia (labeled use) or tardive dyskinesia (unlabeled use): Dosing recommendations vary; initial dose recommendations generally range from 0.05-0.25 mg (although manufacturer recommends 0.5 mg once daily initially in schizophrenia). May be increased in increments of 0.1-0.25 mg; maximum dose in tardive dyskinesia: 5 mg/day.
DOSING: PEDIATRIC — Children: Hypertension: 0.01-0.02 mg/kg/24 hours divided every 12 hours; maximum dose: 0.25 mg/day (not recommended in children)
DOSING: 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).
DOSING: RENAL IMPAIRMENT
Clcr <10 mL/minute: Avoid use.
Not removed by hemo- or peritoneal dialysis; supplemental dose is not necessary.
DOSAGE FORMS — Tablet: 0.1 mg, 0.25 mg
DOSAGE FORMS: CONCISE
Tablet: 0.1 mg, 0.25 mg
GENERIC EQUIVALENT AVAILABLE — Yes
USE — Management of mild-to-moderate hypertension; treatment of agitated psychotic states (schizophrenia)
USE - UNLABELED / INVESTIGATIONAL — Management of tardive dyskinesia
ADVERSE REACTIONS SIGNIFICANT — Frequency not defined.
Cardiovascular: Peripheral edema, arrhythmia, bradycardia, chest pain, PVC, hypotension, syncope
Central nervous system: Dizziness, headache, nightmares, nervousness, drowsiness, fatigue, mental depression, parkinsonism, dull sensorium, paradoxical anxiety
Dermatologic: Rash, pruritus, flushing of skin, purpura
Endocrine & metabolic: Gynecomastia, weight gain
Gastrointestinal: Anorexia, diarrhea, dry mouth, nausea, vomiting, increased salivation, increased gastric acid secretion
Genitourinary: Impotence, decreased libido
Hematologic: Thrombocytopenia purpura
Neuromuscular & skeletal: Muscle ache
Ocular: Blurred vision, optic atrophy
Respiratory: Nasal congestion, dyspnea, epistaxis
CONTRAINDICATIONS — Hypersensitivity to reserpine or any component of the formulation; active peptic ulcer disease, ulcerative colitis; history of mental depression (especially with suicidal tendencies); patients receiving electroconvulsive therapy (ECT)
WARNINGS / PRECAUTIONS — Use with caution in patients with impaired renal function, inflammatory bowel disease, asthma, Parkinson's disease, gallstones, or history of peptic ulcer disease, and the elderly. At high doses, significant mental depression, anxiety, or psychosis may occur (uncommon at dosages <0.25 mg/day). May cause orthostatic hypotension; use with caution in patients at risk of hypotension or in patients where transient hypotensive episodes would be poorly tolerated (cardiovascular disease or cerebrovascular disease). Avoid concurrent use of MAO inhibitors and/or drugs with MAO-inhibiting properties. Some products may contain tartrazine.
DRUG INTERACTIONS
Antihypertensives: Hypotensive effects may be increased.
CNS depressants, ethanol: Additive CNS effects may occur.
Digitalis glycosides: Concomitant administration may predispose some patients to cardiac arrhythmias.
MAO inhibitors: Reserpine may cause hypertensive reactions; concurrent use is not recommended. Theoretically, risk is decreased if reserpine is initiated several days prior to MAO inhibitors.
Quinidine, procainamide: Reserpine may increase the risk of cardiac arrhythmias effects.
Sympathomimetics: The effects of direct-acting sympathomimetics (eg, epinephrine, norepinephrine) may be modestly increased/prolonged. However, the effects of indirect-acting sympathomimetics (amphetamines, dopamine) may be blocked by reserpine.
ETHANOL / NUTRITION / HERB INTERACTIONS
Ethanol: Avoid ethanol (may increase CNS depression).
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).
PREGNANCY RISK FACTOR — C (show table)
LACTATION — Enters breast milk/use caution
PRICING — (data from drugstore.com)
Tablets (Reserpine)
**0.25 mg (30): $11.90
MONITORING PARAMETERS — Blood pressure, standing and sitting/supine
INTERNATIONAL BRAND NAMES — Hiposerpil® (RO); Raunevril® (RO); Raupasil® (PL); Resapin® (ID); Reserpina® (BR); Reserpin® (BG); Serpasil® (ID)
MECHANISM OF ACTION — Reduces blood pressure via depletion of sympathetic biogenic amines (norepinephrine and dopamine); this also commonly results in sedative effects
PHARMACODYNAMICS / KINETICS
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%)
Use of UpToDate is subject to the Subscription and License Agreement. REFERENCES 1.*Chobanian, AV, Bakris, GL, Black, HR, et al. The Seventh Report of the Joint National Committee on Prevention, Detection, Evaluation, and Treatment of High Blood Pressure: The JNC 7 Report. JAMA 2003;