RAUWILOID
Clinical safety rating: caution
Comprehensive 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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RAUWILOID (RAUWILOID).
| Breastfeeding | Not known whether alseroxylon is excreted in human milk. Due to potential for serious adverse reactions in nursing infants, a decision should be made whether to discontinue nursing or discontinue the drug. M/P ratio not available. |
| 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. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to rauwolfia alkaloids, history of depression (especially with suicidal tendencies), active peptic ulcer disease, ulcerative colitis, pheochromocytoma, and concurrent use with 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. |
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| 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. |