RAUDIXIN
Clinical safety rating
cautionComprehensive clinical and safety monograph for RAUDIXIN (RAUDIXIN).
Raudixin (reserpine) is an indole alkaloid that depletes catecholamines (norepinephrine, dopamine) and serotonin from central and peripheral neuronal storage granules by inhibiting vesicular monoamine transporter (VMAT). This leads to prolonged sympathetic blockade and reduced blood pressure.
| Metabolism | Extensively metabolized in the liver via hydrolysis to reserpic acid and methyl reserpate; also undergoes glucuronidation. |
| Excretion | Primarily renal (80-90% as unchanged drug), minor biliary/fecal (10-20%). |
| Half-life | Terminal elimination half-life 50-100 hours; clinical context: once-daily dosing achieves steady state in 1-2 weeks. |
| Protein binding | 90-95% bound mainly to albumin and alpha-1 acid glycoprotein. |
| Volume of Distribution | 10-30 L/kg; large Vd indicates extensive tissue distribution, including adipose and brain. |
| Bioavailability | Oral: 35-50% due to first-pass metabolism; IM: 100%. |
| Onset of Action | Oral: 24-48 hours for antipsychotic effect; IM: 15-30 minutes for sedation, 24-48 hours for antipsychotic effect. |
| Duration of Action | Oral: 24-48 hours after last dose; IM: effects persist for 2-4 weeks due to long-acting depot formulation. |
| Molecular Weight | 608.6 Da (reserpine, active alkaloid) |
Usual adult dose: 400–1600 mg orally per day in divided doses; maximum 2400 mg/day; for severe agitation: 50–100 mg intramuscularly every 4–6 hours.
| Dosage form | TABLET |
| Renal impairment | No dose adjustment necessary for mild-to-moderate renal impairment (GFR ≥30 mL/min); severe renal impairment (GFR <30 mL/min): reduce dose by 25–50% and titrate cautiously. |
| Liver impairment | Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 30–50%; Child-Pugh Class C: avoid use or use with extreme caution at reduced doses. |
| Pediatric use | Children 6–12 years: initial dose 0.2 mg/kg/day orally in divided doses, increase gradually up to 0.4–0.6 mg/kg/day; maximum 1.0 mg/kg/day. Not recommended for children <6 years. |
| Geriatric use | Elderly patients: start at 10–50% of adult dose (e.g., 100–200 mg/day orally), titrate slowly due to increased sensitivity and higher risk of sedation, anticholinergic effects, and orthostatic hypotension. |
| 1st trimester | Avoid; risk of teratogenicity due to anticholinergic and dopamine-blocking effects. |
| 2nd trimester | Use only if benefit outweighs risk; may cause extrapyramidal symptoms in neonate. |
| 3rd trimester | Avoid near term; risk of neonatal respiratory depression, hypotonia, and withdrawal. |
Clinical note
Comprehensive clinical and safety monograph for RAUDIXIN (RAUDIXIN).
| Placental transfer | Crosses placenta; detectable in fetal plasma. |
| Breastfeeding | Raudixin (rauwolfia serpentina) is excreted into breast milk; may cause galactorrhea, gynecomastia, and sedation in infant. Avoid breastfeeding or discontinue drug. |
| Lactation Rating | L4 (Possibly Hazardous) |
| Teratogenic Risk | First trimester: Known human teratogen; may cause major congenital malformations (e.g., neural tube defects, cardiovascular anomalies). Second and third trimesters: Associated with neonatal withdrawal syndrome, respiratory depression, hypotonia, and feeding difficulties after prolonged exposure. Avoid use in pregnancy unless no safer alternative exists. |
| Fetal Monitoring | Pregnancy test prior to initiation (negative test required). During pregnancy: serial fetal ultrasound for anomalies, growth scans (monthly), nonstress tests (weekly starting at 32 weeks), and maternal blood pressure monitoring (risk of hypertension). Neonatal monitoring for withdrawal symptoms for at least 48 hours postpartum. |
| Fertility Effects | May impair female fertility via disruption of ovulation; male fertility may be reduced by impaired sperm motility and count. Reversible upon discontinuation. Advise contraception during therapy. |
■ FDA Black Box Warning
None.
| Serious Effects |
History of depressionActive peptic ulcer diseaseUlcerative colitisPheochromocytomaConcurrent electroconvulsive therapy
| Precautions | May cause severe depression, especially in patients with a history of depression., Use with caution in patients with peptic ulcer disease due to increased gastric acid secretion., Risk of biliary colic in patients with gallstones., Avoid use with MAOIs., May cause withdrawal symptoms (e.g., severe hypertension) upon abrupt discontinuation. |
| Food/Dietary | Avoid tyramine-rich foods (aged cheese, cured meats, fermented products) due to risk of hypertensive crisis. Grapefruit juice may increase reserpine levels. Take with food to reduce gastric irritation. |
| Clinical Pearls | RAUDIXIN (reserpine) is a rauwolfia alkaloid that depletes catecholamines from central and peripheral nerve endings. It causes significant sedation, increased gastric acid secretion (caution in peptic ulcer disease), and nasal congestion. Use is limited due to risk of depression and extrapyramidal symptoms. Monitor for hypotension, especially orthostatic. Avoid concurrent use with MAOIs and tricyclic antidepressants. |
| Patient Advice | Do not stop taking abruptly; withdrawal can cause severe hypertension. · You may feel drowsy or dizzy; avoid driving until you know how the drug affects you. · Report any symptoms of depression, unusual dreams, or suicidal thoughts immediately. · Avoid alcohol and over-the-counter cold medications containing decongestants. · Rise slowly from sitting or lying to prevent falls due to blood pressure drop. |
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