Reserpine

Reserpine
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Gerald Chi

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Overview

Reserpine is a catecholamine-depleting sympatholytic that is FDA approved for the {{{indicationType}}} of mild essential hypertension. Common adverse reactions include abdominal pain, diarrhea, nausea, vomiting, xerostomia, dizziness, headache, lethargy, somnolence, vertigo, depression, and nasal congestion.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Mild Essential Hypertension

• Dosing Information

• Initial Dosage

• In the average patient not receiving other antihypertensive agents, the usual initial dosage is 0.5 mg daily for 1 or 2 weeks.

• Maintenance Dosage

• For maintenance, reduce to 0.1–0.25 mg daily.
• Higher dosages should be used cautiously, because occurrence of serious mental depression and other side effects may increase considerably.

Psychiatric Disorders

• Dosing Information

• Dosage

• The usual initial dosage is 0.5 mg daily, but may range from 0.1 mg to 1.0 mg. Adjust dosage upward or downward according to the patient's response.

• Reserpine is also useful as adjunctive therapy with other antihypertensive agents in the more severe forms of hypertension; relief of symptoms in agitated psychotic states (e.g., schizophrenia), primarily in those individuals unable to tolerate phenothiazine derivatives or in those who also require antihypertensive medication.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Reserpine in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Reserpine in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

• Reserpine is not recommended for use in children.

• If it is to be used in treating a child, the usual recommended starting dose is 20 µg/kg daily. The maximum recommended dose is 0.25 mg (total) daily.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Reserpine in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Reserpine in pediatric patients.

Contraindications

• Hypersensitivity
• Mental depression or history of mental depression (especially with suicidal tendencies)
• Active peptic ulcer
• Ulcerative colitis
• Electroconvulsive therapy

Warnings

• Extreme caution should be exercised in treating patients with a history of mental depression. Reserpine may cause mental depression. Recognition of depression may be difficult because this condition may often be disguised by somatic complaints (masked depression). The drug should be discontinued at first signs of depression such as despondency, early morning insomnia, loss of appetite, impotence, or self-deprecation. Drug-induced depression may persist for several months after drug withdrawal and may be severe enough to result in suicide.

Precautions

• General

• Since reserpine increases gastrointestinal motility and secretion, it should be used cautiously in patients with a history of peptic ulcer, ulcerative colitis, or gallstones (biliary colic may be precipitated).

• Caution should be exercised when treating hypertensive patients with renal insufficiency, since they adjust poorly to lowered blood pressure levels.

• Preoperative withdrawal of reserpine does not assure that circulatory instability will not occur. It is important that the anesthesiologist be aware of the patient’s drug intake and consider this in the overall management, since hypotension has occurred in patients receiving rauwolfia preparations. Anticholinergic and/or adrenergic drugs (e.g., metaraminol, norepinephrine) have been employed to treat adverse vagocirculatory effects.

Adverse Reactions

Clinical Trials Experience

There is limited information regarding Clinical Trial Experience of Reserpine in the drug label.

Postmarketing Experience

• The following adverse reactions have been observed with rauwolfia preparations, but there has not been enough systematic collection of data to support an estimate of their frequency. Consequently the reactions are categorized by organ system and are listed in decreasing order of severity and not frequency.

Neurologic

Rare parkinsonian syndrome and other extrapyramidal tract symptoms; dizziness; headache; paradoxical anxiety; depression; nervousness; nightmares; dull sensorium; drowsiness.

Cardiovascular

Arrhythmias (particularly when used concurrently with digitalis or quinidine), syncope, angina-like symptoms, bradycardia, edema.

Respiratory

Dyspnea, epistaxis, nasal congestion.

Gastrointestinal

Vomiting, diarrhea, nausea, anorexia, dryness of mouth, hypersecretion.

Musculoskeletal

Muscular aches.

Genitourinary

Pseudolactation, impotence, dysuria, gynecomastia, decreased libido, breast engorgement.

Metabolic

Weight gain.

Hypersensitive Reactions

Purpura, rash, pruritus.

Special Senses

Deafness, optic atrophy, glaucoma, uveitis, conjunctival injection.

Drug Interactions

• MAO inhibitors

• MAO inhibitors should be avoided or used with extreme caution.

• Tricyclic antidepressants

• Concurrent use of tricyclic antidepressants may decrease the antihypertensive effect of reserpine.

• Reserpine and sympathomimetics

• Concurrent use of reserpine and direct-or-indirect acting sympathomimetics should be closely monitored. The action of direct-acting amines (epinephrine, isoproterenol, phenylephrine, metaraminol) may be prolonged when given to patients taking reserpine. The action of indirect-acting amines (ephedrine, tyramine, amphetamines) is inhibited.
• Reserpine should be used cautiously with digitalis and quinidine, since cardiac arrhythmias have occurred with rauwolfia preparations.
• Concomitant use of reserpine with other antihypertensive agents necessitates careful titration of dosage with each agent.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

• Pregnancy Category

Pregnancy Category (AUS):

• Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Reserpine in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Reserpine during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Reserpine with respect to nursing mothers.

Pediatric Use

There is no FDA guidance on the use of Reserpine with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Reserpine with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Reserpine with respect to specific gender populations.

Race

There is no FDA guidance on the use of Reserpine with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Reserpine in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Reserpine in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Reserpine in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Reserpine in patients who are immunocompromised.

Administration and Monitoring

Administration

• Oral

• Intravenous

Monitoring

There is limited information regarding Monitoring of Reserpine in the drug label.

Condition1

• Description

IV Compatibility

There is limited information regarding IV Compatibility of Reserpine in the drug label.

Overdosage

Acute Overdose

Signs and Symptoms

• Description

Management

• Description

Chronic Overdose

There is limited information regarding Chronic Overdose of Reserpine in the drug label.

Pharmacology

Reserpine
Systematic (IUPAC) name
Methyl (3β,16β,17α,18β,20α)-11,17-dimethoxy-18-[(3,4,5-trimethoxybenzoyl)oxy]yohimban-16-carboxylate
Identifiers
CAS number	50-55-5
ATC code	C02AA02
PubChem	5770
DrugBank	DB00206
Chemical data
Formula	Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox
Mol. mass	608.68 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	50%
Metabolism	gut/liver
Half life	phase 1 = 4.5h, phase 2 = 271h, average = 33h
Excretion	62% feces / 8% urine
Therapeutic considerations
Licence data	US
Pregnancy cat.	C Risk cannot be ruled out, US
Legal status	Rx-only (some countries banned/discontinued)
Routes	oral

Mechanism of Action

• Reserpine depletes stores of catecholamines and 5-hydroxytryptamine in many organs, including the brain and adrenal medulla. Most of its pharmacological effects have been attributed to this action. Depletion is slower and less complete in the adrenal medulla than in other tissues. The depression of sympathetic nerve function results in a decreased heart rate and a lowering of arterial blood pressure. The sedative and tranquilizing properties of reserpine are thought to be related to depletion of catecholamines and 5-hydroxytryptamine from the brain.

Structure

• Reserpine, USP is an antihypertensive, available as 0.1 mg and 0.25 mg tablets for oral administration. Its chemical name is methyl 18β-hydroxy-11,17 α-dimethoxy-3β, 20α-yohimban-16β-carboxylate 3,4,5-trimethoxybenzoate (ester) and its structural formula is:

This image is provided by the National Library of Medicine.

• Reserpine USP, a pure crystalline alkaloid of rauwolfia, is a white or pale buff to slightly yellowish, odorless crystalline powder. It darkens slowly on exposure to light, but more rapidly when in solution. It is insoluble in water, freely soluble in acetic acid and in chloroform, slightly soluble in benzene, and very slightly soluble in alcohol and in ether. Its molecular weight is 608.69.

• Inactive Ingredients: Acacia, confectioner’s sugar, corn starch, lactose monohydrate, magnesium stearate.

Pharmacodynamics

• Reserpine, like other rauwolfia compounds, is characterized by slow onset of action and sustained effects. Both cardiovascular and central nervous system effects may persist for a period of time following withdrawal of the drug.
• Mean maximum plasma levels of plasma concentrations after a single dose of 0.5 mg of reserpine, administered as two 0.25 mg tablets or as an aqueous solution, peaked after 2.5 hours. The mean peak level was approximately 1.1 ng/ml. The two formulations were found to be bioequivalent. Absolute bioavailability of reserpine, as established by comparison to an intravenous dose, has been reported to be approximately 50%.

Pharmacokinetics

• Reserpine is extensively bound (95%) to plasma proteins. Reserpine is almost completely metabolized in the body, and only about 1% is excreted as unchanged drug in the urine. No definitive studies on the human metabolism of reserpine have been made. After oral administration, an initial half-life of approximately 5 hours is followed by a terminal half-life of the order of 200 hours. Plasma levels may be measurable 14 days after a single dose. The clinical significance of the long terminal half-life is unknown.

Nonclinical Toxicology

There is limited information regarding Nonclinical Toxicology of Reserpine in the drug label.

Clinical Studies

There is limited information regarding Clinical Studies of Reserpine in the drug label.

Condition1

• Description

How Supplied

Storage

There is limited information regarding Reserpine Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

• Patients should be informed of possible side effects and advised to take the medication regularly and continuously as directed.

Precautions with Alcohol

• Alcohol-Reserpine interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

• Resa®

• Serpalan®

Look-Alike Drug Names

• N/A

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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