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Pronunciation
(re SER peen)
Generic Available (U.S.)
Yes
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Management of mild-to-moderate hypertension; treatment of agitated psychotic states (schizophrenia)
Use: Unlabeled/Investigational
Management of tardive dyskinesia
Pregnancy Risk Factor
C
Lactation
Enters breast milk/use caution
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
Special handling:
• Hazardous agent: Use appropriate precautions for handling and disposal.
Concerns related to adverse effects:
• CNS effects: At high doses, significant mental depression, anxiety, or psychosis may occur (uncommon at dosages <0.25 mg/day).
• Orthostatic hypotension: 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).
Disease-related concerns:
• Asthma: Use with caution in patients with asthma.
• Gallstones: Use with caution in patients with gallstones.
• Gastrointestinal disease: Use with caution in patients with inflammatory bowel disease or history of peptic ulcer disease.
• Parkinson's disease: Use with caution in patients with Parkinson's disease.
• Renal impairment: Use with caution in patients with renal impairment.
Concurrent drug therapy issues:
• MAO inhibitors: Avoid concurrent use of MAO inhibitors and/or drugs with MAO-inhibiting properties.
Special populations:
• Elderly: Not recommended for use in the elderly due to potential for impotence, depression, sedation, and orthostatic hypotension. Avoid using doses >0.25 mg daily of reserpine (Beers Criteria).
Dosage form specific issues:
• Tartrazine: Some products may contain tartrazine.
Other warnings/precautions:
• Electroshock therapy: Discontinue reserpine 7 days before electroshock therapy.
Adverse Reactions
Frequency not defined.
Cardiovascular: Arrhythmia, bradycardia, chest pain, hypotension, peripheral edema, PVC, syncope
Central nervous system: Dizziness, drowsiness, dull sensorium, fatigue, headache, mental depression, nightmares, nervousness, parkinsonism, paradoxical anxiety
Dermatologic: Flushing of skin, pruritus, purpura, rash
Endocrine & metabolic: Gynecomastia, weight gain
Gastrointestinal: Anorexia, diarrhea, dry mouth, gastric acid secretion increased, nausea, salivation increased, vomiting
Genitourinary: Impotence, libido decreased
Hematologic: Thrombocytopenia purpura
Neuromuscular & skeletal: Muscle ache
Ocular: Blurred vision, optic atrophy
Respiratory: Dyspnea, epistaxis, nasal congstion
Metabolism/Transport Effects
Inhibits P-glycoprotein
Drug Interactions
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Amifostine: Antihypertensives may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, antihypertensive medications should be withheld for 24 hours prior to amifostine administration. If antihypertensive therapy can not be withheld, amifostine should not be administered. Risk D: Consider therapy modification
Amphetamines: Gastrointestinal Acidifying Agents may decrease the serum concentration of Amphetamines. Risk C: Monitor therapy
Antihypertensives: May enhance the hypotensive effect of other Antihypertensives. Risk C: Monitor therapy
Beta-Blockers: Reserpine may enhance the hypotensive effect of Beta-Blockers. Risk C: Monitor therapy
Cardiac Glycosides: Reserpine may enhance the adverse/toxic effect of Cardiac Glycosides. Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Exceptions: Levocabastine (Nasal). Risk C: Monitor therapy
Colchicine: P-Glycoprotein Inhibitors may increase the serum concentration of Colchicine. Colchicine distribution into certain tissues (e.g., brain) may also be increased. Management: Colchicine is contraindicated in patients with impaired renal or hepatic function who are also receiving a p-glycoprotein inhibitor. In those with normal renal and hepatic function, reduce colchicine dose as directed. Risk D: Consider therapy modification
Dabigatran Etexilate: P-Glycoprotein Inhibitors may increase serum concentrations of the active metabolite(s) of Dabigatran Etexilate. Management: Dabigatran dose reductions may be needed. According to Canadian labeling, dabigatran dose for prevention of venous thromboembolism post hip or knee replacement should be reduced to 150 mg/day in patients receiving amiodarone, verapamil, or quinidine. Risk D: Consider therapy modification
Diazoxide: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Risk D: Consider therapy modification
Everolimus: P-Glycoprotein Inhibitors may increase the serum concentration of Everolimus. Management: Everolimus dose reductions are required for patients being treated for subependymal giant cell astrocytoma or renal cell carcinoma. See prescribing information for specific dose adjustment and monitoring recommendations. Risk D: Consider therapy modification
Herbs (Hypertensive Properties): May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Herbs (Hypotensive Properties): May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Management: For patients being treated with hydroxyzine, a reduction in the dose of any other CNS depressants that are to be used in combination is recommended. With concurrent use, monitor patients closely for excessive response to the combination. Risk D: Consider therapy modification
Hypotensive Agents: May enhance the adverse/toxic effect of other Hypotensive Agents. Risk C: Monitor therapy
Iobenguane I 123: Reserpine may diminish the therapeutic effect of Iobenguane I 123. Risk X: Avoid combination
MAO Inhibitors: May enhance the adverse/toxic effect of Reserpine. Existing MAOI therapy can result in paradoxical effects of added reserpine (e.g., excitation, hypertension). Management: Monoamine oxidase inhibitors (MAOIs) should be avoided or used with great caution in patients who are also receiving reserpine. Risk D: Consider therapy modification
MAO Inhibitors: May enhance the orthostatic hypotensive effect of Orthostatic Hypotension Producing Agents. Risk C: Monitor therapy
Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Risk D: Consider therapy modification
Methylphenidate: May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Pentoxifylline: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
P-Glycoprotein Substrates: P-Glycoprotein Inhibitors may increase the serum concentration of P-Glycoprotein Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). Risk C: Monitor therapy
Phosphodiesterase 5 Inhibitors: May enhance the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Prostacyclin Analogues: May enhance the hypotensive effect of Antihypertensives. Risk C: Monitor therapy
QuiNIDine: Reserpine may enhance the adverse/toxic effect of QuiNIDine. Risk C: Monitor therapy
RiTUXimab: Antihypertensives may enhance the hypotensive effect of RiTUXimab. Risk D: Consider therapy modification
Rivaroxaban: P-Glycoprotein Inhibitors may increase the serum concentration of Rivaroxaban. Risk C: Monitor therapy
Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Risk C: Monitor therapy
Silodosin: P-Glycoprotein Inhibitors may increase the serum concentration of Silodosin. Risk X: Avoid combination
Tetrabenazine: Reserpine may enhance the adverse/toxic effect of Tetrabenazine. Risk X: Avoid combination
Topotecan: P-Glycoprotein Inhibitors may increase the serum concentration of Topotecan. Risk X: Avoid combination
Yohimbine: May diminish the antihypertensive effect of Antihypertensives. Risk C: Monitor therapy
Ethanol/Nutrition/Herb 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).
Storage
Protect oral dosage forms from light.
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%)
Dosage
Note: When used for management of hypertension, full antihypertensive effects may take as long as 3 weeks.
Oral:
Children: Hypertension: 0.01-0.02 mg/kg/24 hours divided every 12 hours; maximum dose: 0.25 mg/day (not recommended in children)
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.
Elderly: Initial: 0.05 mg once daily, increasing by 0.05 mg every week as necessary (Beers Criteria: Avoid doses >0.25 mg daily)
Dosing adjustment in renal impairment: Clcr <10 mL/minute: Avoid use
Dialysis: Not removed by hemo or peritoneal dialysis; supplemental dose is not necessary
Monitoring Parameters
Blood pressure, standing and sitting/supine
Patient Education
May take up to 2 weeks to see effects of therapy. Avoid alcohol and maintain recommended diet. May cause nervousness, dizziness, fatigue, nausea, loss of appetite, constipation, nasal stuffiness, or impotence (will resolve when medication is discontinued). Report chest pain, palpitations, respiratory difficulty, sudden increase in weight, swelling in ankles or hands, depression, or alteration in gait or balance.
Geriatric Considerations
Some studies advocate the use of reserpine because of its low cost, long half-life, and efficacy, but it is generally not considered a first-line drug.
This medication is considered to be potentially inappropriate in this patient population (Beers Criteria severity: Low).
Additional Information
Adverse effects are usually dose related, mild, and infrequent when administered for the management of hypertension.
Anesthesia and Critical Care Concerns/Other Considerations
Clinical Pearls/Comments: Currently, reserpine is used only infrequently for treatment of hypertension. Nasal congestion, sedation, depression, and activation of peptic ulcer are important adverse effects.
Cardiovascular Considerations
Currently, reserpine is used only infrequently for treatment of hypertension. An important side effect is drowsiness. It is important that reserpine be discontinued at least 1 week before elective electroshock therapy.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia and changes in salivation (normal salivary flow resumes upon discontinuation).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause dizziness, nightmares, and drowsiness; high dose may cause depression, anxiety, or psychosis
Mental Health: Effects on Psychiatric Treatment
Contraindicated in depression and with MAO inhibitors. Discontinue reserpine 7 days before ECT. Combined use with CNS depressants may produce additive effects. TCAs may diminish reserpine's antihypertensive effects.
Nursing: Physical Assessment/Monitoring
Use caution and monitor closely with a history of depression, PUD, or gallstones. Assess blood pressure and cardiac status prior to starting therapy, during first doses, when changing dose, and regularly thereafter. Monitor for hypotension, CNS changes (nervousness, depression), rash, diarrhea, nausea, and vomiting.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, oral: 0.1 mg, 0.25 mg
Pricing: U.S. (www.drugstore.com)
Tablets (Reserpine)
0.25 mg (30): $56.86
References
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, 289(19):2560-71.
International Brand Names
Lexi-Comp.com
Last full review/revision May 2011
Content last modified May 2011
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