Reserpine

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Some people taking reserpine have developed depression. Stop taking reserpine and call your doctor right away if you have:

• unusual changes in mood or behavior;
• sudden lack of energy or feelings of low self-worth;
• loss of interest in things you once enjoyed;
• new sleep problems, such as nightmares or early morning insomnia; or
• thoughts about hurting yourself.

Keep taking reserpine but call your doctor at once if you have:

• chest pain, slow heartbeats, trouble breathing;
• swelling in your hands or feet;
• a light-headed feeling, like you might pass out;
• painful or difficult urination;
• vision or hearing problems; or
• uncontrolled muscle movements or tremors.

Common side effects may include:

• nausea, vomiting, diarrhea, loss of appetite;
• headache, dizziness, drowsiness;
• breast tenderness or swelling;
• itching or rash;
• stuffy nose, nosebleeds;
• weight gain; or
• impotence, decreased interest in sex.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Reserpine is a prescription medication used to treat high blood pressure. 

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Reserpine is part of the drug class:

• Rauwolfia alkaloids

You should not use reserpine if you are allergic to it, or if you have:

• a history of depression;

• a history of suicidal thoughts or actions;

• a stomach ulcer;

• ulcerative colitis; or

• a condition for which you are being treated with electroconvulsive (shock) therapy.

To make sure reserpine is safe for you, tell your doctor if you have:

• gallstones;

• kidney disease; or

• a history of stomach problems or slow digestion.

It is not known whether this medicine will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant while taking reserpine.

Reserpine can pass into breast milk and may harm a nursing baby. You should not breast-feed while using this medicine.

Reserpine is not approved for use by anyone younger than 18 years old.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include redness or warmth under your skin, tingly feeling, diarrhea, feeling light-headed, shallow breathing, weak pulse, slow heartbeats, pinpoint pupils, extreme drowsiness, or loss of consciousness.

This medicine may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.

Drinking alcohol with this medicine can cause side effects.

Usual Adult Dose for Hypertension:

Initial dose: 0.5 mg orally once a day for 1 to 2 weeks.
Maintenance dose: 0.1 to 0.25 mg orally once a day.

Usual Adult Dose for Schizophrenia:

Initial dose: 0.5 mg orally once a day, but may range from 0.1 to 1 mg.
Maintenance dose: Adjust dose upward or downward according to patient response.

Usual Adult Dose for Hyperthyroidism:

The value of orally administered reserpine during thyrotoxic crisis is not known.

Limited data in which seven patients with thyrotoxic crisis received reserpine 1 to 5 mg intramuscularly, then 0.07 to 0.3 mg per kg in the first 24 hours reveal significant, dose-related improvement in symptoms within four to eight hours of drug administration.

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:

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 sugar1, corn starch, lactose monohydrate, magnesium stearate.

This product complies with Dissolution Test #2.

In 0.25 mg tablets only.

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.

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%.

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.

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.

Information for Patients

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

Drug Interactions

MAO inhibitors should be avoided or used with extreme caution.

Concurrent use of tricyclic antidepressants may decrease the antihypertensive effect of Reserpine.

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.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Rodent studies have shown that Reserpine is an animal tumorigen, causing an increased incidence of mammary fibroadenomas in female mice, malignant tumors of the seminal vesicles in male mice, and malignant adrenal medullary tumors in male rats. These findings arose in 2-year studies in which the drug was administered in the feed at concentrations of 5 to 10 ppm – about 100 to 300 times the usual human dose. The breast neoplasms are thought to be related to Reserpine’s prolactin-elevating effect. Several other prolactin-elevating drugs have also been associated with an increased incidence of mammary neoplasia in rodents.

The extent to which these findings indicate a risk to humans is uncertain. Tissue culture experiments show that about one third of human breast tumors are prolactin-dependent in vitro, a factor of considerable importance if the use of the drug is contemplated in a patient with previously detected breast cancer. The possibility of an increased risk of breast cancer in Reserpine users has been studied extensively; however, no firm conclusion has emerged. Although a few epidemiologic studies have suggested a slightly increased risk (less than twofold in all studies except one) in women who have used Reserpine, other studies of generally similar design have not confirmed this. Epidemiologic studies conducted using other drugs (neuroleptic agents) that, like Reserpine, increase prolactin levels and therefore would be considered rodent mammary carcinogens have not shown an association between chronic administration of the drug and human mammary tumorigenesis. While long-term clinical observation has not suggested such as association, the available evidence is considered too limited to be conclusive at this time. An association of Reserpine intake with pheochromocytoma or tumors of the seminal vesicles has not been explored.

Pregnancy Category C

Reserpine administered parenterally has been shown to be teratogenic in rats at doses up to 2 mg/kg and to have an embryocidal effect in guinea pigs given dosages of 0.5 mg daily.

There are no adequate and well-controlled studies of Reserpine in pregnant women. Reserpine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Reserpine crosses the placental barrier, and increased respiratory tract secretions, nasal congestion, cyanosis, and anorexia may occur in neonates of Reserpine-treated mothers.

Nursing Mothers

Reserpine is excreted in maternal breast milk, and increased respiratory tract secretions, nasal congestion, cyanosis, and anorexia may occur in breast-fed infants. Because of the potential for adverse reactions in nursing infants and the potential for tumorigenicity shown for Reserpine in animal studies, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use

Safety and effectiveness in children have not been established by means of controlled clinical trials, although there is experience with the use of Reserpine in children (see DOSAGE AND ADMINISTRATION.) Because of adverse effects such as emotional depression and lability, sedation, and stuffy nose, Reserpine is not usually recommended as a step-2 drug in the treatment of hypertension in children.

Hypertension

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

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.

Children

Reserpine is not recommended for use in children (see PRECAUTIONS: Pediatric Use). 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.