RAUSERPIN
Clinical safety rating: caution
Comprehensive 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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RAUSERPIN (RAUSERPIN).
| Breastfeeding | Reserpine is excreted into breast milk with an M/P ratio of approximately 1.0. Potential for significant effects in the nursing infant including bradycardia, sedation, and gastrointestinal disturbances. Use is contraindicated during breastfeeding. |
| 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. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to rauwolfia alkaloids","History of mental depression (especially suicidal ideation)","Active peptic ulcer","Ulcerative colitis","Electroconvulsive therapy (within 7 days)","Pheochromocytoma","Concomitant use with MAO inhibitors"]
| 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"] |
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| 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. |