RAU-SED
Clinical safety rating
cautionComprehensive clinical and safety monograph for RAU-SED (RAU-SED).
Reserpine depletes catecholamines (norepinephrine, dopamine) from adrenergic nerve endings by binding to and inhibiting the vesicular monoamine transporter (VMAT), preventing neurotransmitter storage and leading to depletion of catecholamines.
| Metabolism | Extensively metabolized in the liver via ester hydrolysis; major metabolite is trimethoxybenzoic acid; not fully characterized in humans. |
| Excretion | Renal (60-70% as unchanged drug and metabolites); fecal (20-30% via biliary elimination) |
| Half-life | Terminal elimination half-life: 45-90 hours (average 60 hours); clinical context: requires 5-7 days to reach steady-state; prolonged half-life may lead to cumulative effects |
| Protein binding | 96% bound, primarily to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | 8-10 L/kg; clinical meaning: extensive tissue distribution, high affinity for adipose tissue and brain |
| Bioavailability | Oral: 40-50% (first-pass metabolism); Intramuscular: 100% (complete absorption) |
| Onset of Action | Oral: 2-4 weeks for therapeutic effect (antihypertensive); Intramuscular: 1-2 hours for antipsychotic effect; Intravenous: 30-60 minutes for hypertensive crisis |
| Duration of Action | Oral: up to 2-3 weeks after discontinuation due to enterohepatic circulation; antihypertensive effect persists for 8-12 hours per dose; antipsychotic effects may last 1-2 weeks after single IM dose |
| Molecular Weight | 608.68 |
Initial: 0.5 mg orally once daily; maintenance: 0.1-0.25 mg orally once daily.
| Dosage form | TABLET |
| Renal impairment | Contraindicated in severe renal impairment (CrCl <30 mL/min). For moderate impairment (CrCl 30-60 mL/min), reduce dose by 50%. No adjustment needed for CrCl >60 mL/min. |
| Liver impairment | Contraindicated in severe hepatic impairment (Child-Pugh Class C). For moderate impairment (Child-Pugh Class B), reduce dose by 50% and monitor for excessive sedation. No adjustment for mild (Child-Pugh Class A). |
| Pediatric use | Not recommended due to lack of safety and efficacy data. Avoid use in children. |
| Geriatric use | Initiate with 0.1 mg orally once daily; titrate slowly based on response and tolerability. Monitor for orthostatic hypotension and sedation. |
| 1st trimester | Avoid: Reserpine crosses placenta; risk of fetal bradycardia, respiratory depression, and hypothermia. Associated with congenital malformations in animal studies. |
| 2nd trimester | Avoid: Continued risk of adverse fetal effects, including electrolyte imbalance and altered autonomic regulation. |
| 3rd trimester | Avoid: May cause neonatal nasal congestion, respiratory depression, and bradycardia if used near term. |
Clinical note
Comprehensive clinical and safety monograph for RAU-SED (RAU-SED).
| Placental transfer | Reserpine crosses the placenta readily, achieving fetal plasma concentrations similar to maternal levels. |
| Breastfeeding | Reserpine is excreted into human milk. May cause infant sedation, lethargy, and GI disturbances. Breastfeeding is not recommended during therapy. |
| Lactation Rating | L5 (Contraindicated) |
| Teratogenic Risk | Reserpine crosses placenta. First trimester: Increased risk of congenital malformations (cardiac defects, CNS anomalies) in animal studies; human data limited but risk considered elevated. Second/third trimesters: Risk of neonatal respiratory depression, bradycardia, hypothermia, and nasal congestion due to catecholamine depletion. Avoid use throughout pregnancy unless essential. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and signs of depression or extrapyramidal symptoms. For fetus: Ultrasound for growth and anatomy; fetal heart rate monitoring in third trimester. Neonatal: Assess for respiratory depression, bradycardia, hypothermia, and nasal congestion at birth. |
| Fertility Effects | May impair fertility due to inhibition of gonadotropin secretion and possible hyperprolactinemia. Reports of decreased libido and erectile dysfunction in males; menstrual irregularities in females. Reversible upon discontinuation. |
■ FDA Black Box Warning
Reserpine may increase the risk of suicide; patients should be monitored for depression. It should not be used in patients with a history of mental depression.
| Serious Effects |
History of depressionHypersensitivity to reserpineActive peptic ulcerUlcerative colitisPheochromocytomaConcurrent MAO inhibitor therapy
| Precautions | May cause severe depression, especially in patients with psychiatric history; may cause bradycardia, electrolyte imbalance, and gastrointestinal effects; caution in patients with peptic ulcer disease or gallstones due to increased gastric acid secretion. |
| Food/Dietary | Avoid tyramine-rich foods (aged cheese, cured meats, fermented products, soy sauce) as rauwolfia alkaloids can potentiate hypertensive crises. Limit caffeine intake. High-fiber diets may reduce absorption separate doses. |
| Clinical Pearls | RAU-SED (rauwolfia serpentina) is an antihypertensive and antipsychotic alkaloid. Onset of action is slow (2-3 weeks) for hypertension. Monitor for bradycardia, nasal congestion, and depression. Do not use with MAOIs or electroconvulsive therapy. Taper to avoid withdrawal hypertension. |
| Patient Advice | Take exactly as prescribed; do not stop suddenly as this may cause severe hypertension. · May cause drowsiness, dizziness, or nasal congestion; avoid driving if affected. · Report signs of depression, nightmares, or extrapyramidal symptoms (muscle stiffness, tremors). · Avoid alcohol and over-the-counter cold medications containing decongestants. · Rise slowly from sitting or lying to minimize postural hypotension. |
Loading safety data…