RAUWILOID
Clinical safety rating
cautionComprehensive clinical and safety monograph for RAUWILOID (RAUWILOID).
Rauwiloid (alseroxylon) is a rauwolfia alkaloid that depletes catecholamines and serotonin from postganglionic sympathetic nerve endings and the central nervous system by inhibiting vesicular monoamine transporter (VMAT). This leads to reduced peripheral vascular resistance and decreased sympathetic outflow, resulting in antihypertensive and antipsychotic effects.
| Metabolism | Primarily hepatic via cytochrome P450 enzymes (CYP2D6 and CYP3A4); undergoes extensive first-pass metabolism. |
| Excretion | Primarily renal excretion of metabolites; ~60–80% of a dose is eliminated in urine as metabolites, with <1% as unchanged drug. Biliary/fecal excretion accounts for ~15%. |
| Half-life | Terminal elimination half-life is approximately 10–12 hours. Clinical context: Requires twice-daily dosing for sustained antihypertensive effect; steady-state achieved in 2–3 days. |
| Protein binding | Approximately 90% bound to plasma proteins, primarily albumin and alpha1-acid glycoprotein. |
| Volume of Distribution | Approximately 1.6 L/kg. Clinical meaning: Indicates extensive tissue distribution beyond plasma volume; consistent with peripheral binding and accumulation in tissues. |
| Bioavailability | Oral: Approximately 30–50% due to first-pass metabolism. |
| Onset of Action | Oral: 1–2 hours for initial blood pressure reduction; peak effect at 2–4 hours. |
| Duration of Action | Oral: 8–12 hours. Clinical note: Duration may be shorter in some patients, necessitating twice-daily dosing; antihypertensive effect may persist for up to 24 hours at higher doses. |
| Molecular Weight | 478.63 |
2 mg orally twice daily, adjusted based on response; maximum 4 mg twice daily.
| Dosage form | TABLET |
| Renal impairment | Not recommended in patients with GFR <30 mL/min; for GFR 30-60 mL/min, reduce dose by 50%. |
| Liver impairment | Child-Pugh class B: reduce dose by 50%; Child-Pugh class C: use is contraindicated. |
| Pediatric use | Not recommended for pediatric use; safety and efficacy not established. |
| Geriatric use | Start at 1 mg orally once daily; increase slowly with close monitoring of blood pressure. |
| 1st trimester | Data are limited; use only if clearly needed. Potential risk of teratogenicity due to antiadrenergic effects. |
| 2nd trimester | Use with caution; may cause fetal bradycardia and hypotension. |
| 3rd trimester | Avoid in late pregnancy due to risk of neonatal bradycardia, hypotension, and respiratory depression. |
Clinical note
Comprehensive clinical and safety monograph for RAUWILOID (RAUWILOID).
| Placental transfer | Crosses placenta; detected in fetal plasma. |
| Breastfeeding | Excreted into breast milk; use with caution. Monitor infant for bradycardia and sedation. |
| Lactation Rating | L3 (Moderately Safe) |
| Teratogenic Risk | No adequate studies in pregnant women. Animal reproduction studies have not been conducted with Rauwiloid (alseroxylon). Use in first trimester: unknown risk. Second and third trimesters: may cause fetal bradycardia, hypotension, and hypothermia if used near term. Avoid use in pregnancy unless clearly needed. |
| Fetal Monitoring | Monitor maternal blood pressure and heart rate regularly. Assess fetal heart rate and growth if used in second or third trimester. Watch for signs of neonatal respiratory depression or bradycardia after delivery. |
| Fertility Effects | No human data on fertility. In animal studies, reserpine (closely related) may impair fertility. Possible effects on male and female reproductive function due to catecholamine depletion. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to rauwiloidActive peptic ulcerSevere hepatic impairmentSevere renal impairmentPheochromocytomaHistory of mental depressionConcurrent use of MAO inhibitors
| Precautions | May cause depression (including suicidal ideation), bradycardia, orthostatic hypotension, nasal congestion, and gastrointestinal disturbances. Use with caution in patients with history of depression, peptic ulcer disease, or colitis. Avoid abrupt discontinuation to prevent rebound hypertension. |
| Food/Dietary | Avoid excessive intake of tyramine-rich foods (e.g., aged cheeses, cured meats, fermented products) as Rauwiloid may potentiate pressor effects; limit sodium intake to enhance antihypertensive effect; avoid large amounts of caffeine. |
| Clinical Pearls | Rauwiloid (alseroxylon) is a rauwolfia alkaloid used for mild to moderate hypertension; its antihypertensive effect is due to depletion of catecholamines from peripheral sympathetic nerve endings; onset is slow (weeks) and prolonged; common side effects include nasal congestion, bradycardia, and depression; avoid in patients with history of depression or peptic ulcer disease; may cause sodium and water retention; taper dose to avoid rebound hypertension. |
| Patient Advice | Take this medication exactly as prescribed; do not stop suddenly as this may cause a rapid increase in blood pressure. · Avoid alcohol and other central nervous system depressants as they can worsen drowsiness or dizziness. · You may experience nasal congestion, dry mouth, or slowed heart rate; report any signs of depression or mood changes. · Rise slowly from sitting or lying positions to prevent dizziness or fainting. · This medication may take several weeks to achieve full effect; continue taking it even if you feel well. |
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