RAUSERPIN
Clinical safety rating
cautionComprehensive clinical and safety monograph for RAUSERPIN (RAUSERPIN).
Rauwolfia alkaloid (reserpine) depletes catecholamines (norepinephrine, dopamine, serotonin) from sympathetic nerve endings and brain by irreversibly binding to vesicular monoamine transporter (VMAT). This results in reduced sympathetic outflow, decreased heart rate, and vasodilation.
| Metabolism | Hepatic via CYP2D6; undergoes extensive first-pass metabolism; metabolites excreted in urine and feces. |
| Excretion | Primarily renal (60-70% as unchanged drug and metabolites); biliary/fecal (15-20%) |
| Half-life | Terminal elimination half-life: 4-8 hours; clinical context: requires multiple daily dosing to maintain therapeutic levels. |
| Protein binding | 80-90% bound primarily to albumin |
| Volume of Distribution | 1.0-2.0 L/kg; clinical meaning: indicates extensive tissue distribution, including CNS. |
| Bioavailability | Oral: 80-90%; Intramuscular: 100% |
| Onset of Action | Oral: 30-60 minutes; Intramuscular: 15-30 minutes. |
| Duration of Action | Oral: 6-8 hours; Intramuscular: 8-12 hours; clinical notes: duration may be prolonged in hepatic impairment. |
| Molecular Weight | 334.33 Da |
Initial: 0.1-0.25 mg orally once daily; increase gradually to 0.5-1 mg per day in 2 divided doses. Maximum: 3 mg/day.
| Dosage form | TABLET |
| Renal impairment | GFR 30-50 mL/min: reduce dose by 25%. GFR 15-29 mL/min: reduce dose by 50%. GFR <15 mL/min: avoid use. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: reduce dose by 50%. Child-Pugh C: contraindicated. |
| Pediatric use | Not approved for pediatric use; safety and efficacy not established. |
| Geriatric use | Initiate at 0.05 mg orally once daily; increase slowly. Maximum 1.5 mg/day. Monitor for orthostatic hypotension and sedation. |
| 1st trimester | Avoid; risk of fetal harm based on animal data and limited human studies. Antipsychotic use associated with congenital malformations, especially during first trimester. |
| 2nd trimester | Use only if benefit outweighs risk; may cause extrapyramidal symptoms in neonate. |
| 3rd trimester | Use only if benefit outweighs risk; risk of neonatal withdrawal or extrapyramidal symptoms; monitor neonate for abnormal movements. |
Clinical note
Comprehensive clinical and safety monograph for RAUSERPIN (RAUSERPIN).
| Placental transfer | Rauserpin crosses the placenta; detectable in fetal serum with a maternal-to-fetal ratio of approximately 0.5-0.7 based on limited human data. |
| Breastfeeding | Rauserpin is excreted into breast milk in small amounts; however, not recommended due to potential for adverse effects in the infant, including sedation, extrapyramidal symptoms, and impact on neurodevelopment. |
| Lactation Rating | L4 (Possibly Hazardous) |
| Teratogenic Risk | Rauserpin (reserpine) crosses the placenta. First trimester: Increased risk of congenital malformations including skeletal and cardiovascular anomalies based on animal studies; human data limited but avoid use. Second and third trimesters: Fetal bradycardia, hypothermia, and respiratory depression due to catecholamine depletion. Neonatal withdrawal: Lethargy, nasal congestion, and poor feeding. Avoid use throughout pregnancy. |
| Fetal Monitoring | Monitor maternal: blood pressure, heart rate, and signs of depression. Fetal: ultrasound for growth and anomalies, fetal heart rate monitoring. Neonatal: assess for bradycardia, respiratory depression, and withdrawal symptoms after delivery. |
| Fertility Effects | Reserpine may cause hyperprolactinemia via dopamine depletion, leading to menstrual irregularities, galactorrhea, and reduced fertility. It may also impair spermatogenesis in males. Effects are reversible upon discontinuation. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to rauserpin or any component of the formulationSevere CNS depressionComatose statesHistory of neuroleptic malignant syndrome (NMS)Concurrent use with other antipsychotics that prolong QTc interval
| Precautions | May cause severe depression with high risk of suicide, Electroconvulsive therapy (ECT) should be discontinued at least 7 days prior, Use cautiously in patients with history of peptic ulcer disease (increased gastric acid secretion), May precipitate biliary colic in patients with gallstones, Monitor for hypotension and bradycardia |
| Food/Dietary | Avoid high-tyramine foods (e.g., aged cheeses, cured meats, pickled fish, ferments) as RAUSERPIN may potentiate their pressor effects, leading to hypertensive crisis. Limit alcohol intake due to increased risk of hypotension and sedation. |
| Clinical Pearls | RAUSERPIN (rauwolfia alkaloid) is an antihypertensive that depletes catecholamines from postganglionic sympathetic nerve endings. Onset of effect is slow (weeks), and it may cause significant bradycardia and sedation. Avoid in patients with history of depression, peptic ulcer disease, or pheochromocytoma. Use with caution in patients receiving MAOIs or other antihypertensives due to additive effects. |
| Patient Advice | Take this medication exactly as prescribed, usually once daily at the same time each day. · It may take several weeks to see the full benefit; do not stop abruptly as this may cause rapid increase in blood pressure. · This drug may cause drowsiness, dizziness, or nasal congestion; avoid driving or operating machinery until you know how it affects you. · Avoid alcohol and sedatives as they may worsen drowsiness. · Contact your doctor if you experience depression, slow heart rate, fainting, or signs of stomach ulcer (e.g., black stools, stomach pain). |
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