RAUDIXIN
Clinical safety rating: caution
Comprehensive 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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RAUDIXIN (RAUDIXIN).
| Breastfeeding | Raudixin (methamphetamine hydrochloride) is contraindicated during breastfeeding due to high secretion into breast milk, potential for infant toxicity (irritability, poor feeding, seizures), and unknown M/P ratio. Discontinue nursing or drug. |
| 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. |
■ FDA Black Box Warning
None.
| Serious Effects |
["History of depression (especially suicidal ideation)","Active peptic ulcer","Ulcerative colitis","Electroconvulsive therapy (within 7 days)","Hypersensitivity to reserpine","Concomitant use with MAOIs"]
| 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."] |
Loading safety data…
| 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. |