reserpine

Reserpine is a medication used to treat high blood pressure (hypertension), a major risk factor for cardiovascular diseases.

Reserpine is one of the earliest antihypertensive agents to be developed and was initially used as a first-line treatment. With the development of newer drugs with better side effect profile, reserpine is rarely prescribed anymore and is no longer available in the U.S. Reserpine was previously used to also treat schizophrenia, and tardive dyskinesia, movement disorders associated with long-term antipsychotic therapy, but no longer.

Reserpine is a compound (indole alkaloid) extracted from the roots of a plant, Rauwolfia serpentina. Reserpine depletes the tissue stores of norepinephrine, dopamine, and serotonin, chemicals (neurotransmitters) that nerve cells (neurons) use to communicate. These neurotransmitters regulate the heart rate, force of cardiac contraction, and blood pressure, in addition to regulating many body functions including emotions, digestion, and movement.

Reserpine binds to storage vesicles of neurons and prevents the uptake of dopamine, norepinephrine, and serotonin. The neurotransmitters not contained in the vesicles are broken down (metabolized) naturally by the enzyme monoamine oxidase, depleting their stores. This slows down the activity of the nervous system, lowering blood pressure as well as producing sedative effects. Reserpine exerts its effects on the cardiovascular system, central nervous system and gastrointestinal system.

• Do not use in patients with hypersensitivity to reserpine or any of its components.
• Do not use reserpine in the following conditions:
  • Active peptic ulcer
  • Ulcerative colitis
  • History of depression, especially with suicidal tendencies
• Do not use reserpine in patients undergoing electroconvulsive therapy. Discontinue reserpine at least a week before, and do not restart for at least a week after treatment.
• Use reserpine with caution in the following conditions:
  • History of peptic ulcer disease
  • Inflammatory bowel disease
  • History of gallstones
  • Impaired kidney function
  • Parkinson’s disease
  • Asthma
• High doses of reserpine may cause significant mental depression, anxiety, or psychosis. Exercise caution.
• Reserpine may cause postural (orthostatic) hypotension. Use with caution in patients at risk of hypotension, particularly those with cardiovascular or cerebrovascular disease.
• Some formulations of reserpine may contain tartrazine. Avoid use in patients with tartrazine allergy and use with caution in patients who have a history of allergic reactions.

Common side effects of reserpine include:

• Irregular heart rate (arrhythmia)
• Slow heart rate (bradycardia)
• Premature ventricular contractions
• Chest pain (angina)
• Low blood pressure (hypotension)
• Fainting (syncope)
• Flushing
• Swelling of extremities (peripheral edema)
• Paradoxical anxiety
• Nervousness
• Depression
• Reduced mental acuity
• Drowsiness
• Nightmares
• Dizziness
• Headache
• Fatigue
• Drug-induced Parkinson’s disease
• Muscle pain (myalgia)
• Nausea
• Vomiting
• Excessive salivation (sialorrhea) or dry mouth (xerostomia)
• Hyperacidity
• Diarrhea
• Loss of appetite (anorexia)
• Impotence
• Reduced libido
• Breast tissue growth in males (gynecomastia)
• Weight gain
• Nasal congestion
• Nasal bleeding (epistaxis)
• Shortness of breath (dyspnea)
• Blurred vision
• Optic nerve damage (optic atrophy)
• Skin rash
• Itching (pruritus)
• Immune-mediated drop in platelet count (immune thrombocytopenia)
• Bruising (purpura)

Call your doctor immediately if you experience any of the following symptoms or serious side effects while using this drug:

• Serious heart symptoms include fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness;
• Severe headache, confusion, slurred speech, severe weakness, vomiting, loss of coordination, feeling unsteady;
• Severe nervous system reaction with very stiff muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, and feeling like you might pass out; or
• Serious eye symptoms include blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.

This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.

Tablets

• 0.1 mg
• 0.25 mg

Adult:

Hypertension

Initial

• 0.5 mg daily for 1 or 2 weeks

Maintenance

• 0.1-0.25 mg orally once daily
• Use higher dosages cautiously occurrence of mental depression or other adverse reactions may increase

Psychiatric Disorders

• 0.5 mg daily, but may range from 0.1 to 1 mg; titrate dose according to patient response

Tardive Dyskinesia

• 0.25 mg every 6 hours; may increase by 0.1-0.25 mg to a total of 5 mg daily

Geriatric:

Hypertension

• Adverse central nervous system (CNS) effects; may cause slow heart rate and dizziness on standing (orthostatic hypotension); not recommended as routine treatment for hypertension (Beers criteria)
• 0.05 mg orally once daily; may increase by 0.05 mg after 1 week as needed; not to exceed 0.1 mg/day

Pediatric

Hypertension

• 0.02 mg/kg/day orally once daily or divided every 12 hours, not to exceed 0.25 mg/day

Overdose

• Reserpine overdose can cause nausea, vomiting, hypotension, sedation, and coma, and rarely, cardiovascular collapse and death. Overdose treatment is symptomatic and supportive and may include elimination of undigested drug from the gastrointestinal tract.

Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.

• Reserpine has no listed severe interactions with other drugs.
• Serious interactions of reserpine include:
  • deutetrabenazine
• Moderate interactions of reserpine include:
  • berotralstat
  • esketamine intranasal
  • ganaxolone
  • lemborexant
• Reserpine has no listed mild interactions with other drugs.

The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.

It is important to always tell your doctor, pharmacist, or health care provider of all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.

• Animal reproductive studies indicate reserpine may cause fetal harm if used during pregnancy. Use reserpine with caution in pregnant women, if benefits clearly outweigh potential risks to the fetus.
• Reserpine is present in breast milk, avoid use in nursing mothers.

• Take reserpine exactly as prescribed.
• Store safely out of reach of children.
• In case of overdose, seek medical help or contact Poison Control.
• Reserpine is no longer available in the United States. If you have been taking reserpine, contact your doctor for switching to another therapy.