MODERIL
Clinical safety rating
cautionComprehensive clinical and safety monograph for MODERIL (MODERIL).
Reserpine is an alkaloid that depletes catecholamines (norepinephrine, dopamine) and serotonin from central and peripheral nerve endings by irreversibly binding to and inhibiting the vesicular monoamine transporter (VMAT), preventing storage and leading to degradation by monoamine oxidase.
| Metabolism | Extensively metabolized in the liver via hydrolysis and conjugation; cytochrome P450 (CYP) enzymes not majorly involved. |
| Excretion | Renal: 60% (mainly as unchanged drug); biliary/fecal: ~40% (includes glucuronide conjugates). |
| Half-life | Terminal elimination half-life: 2.5–3.5 hours; may be prolonged to 6–8 hours in severe renal impairment. |
| Protein binding | 50–70% bound to albumin and α1-acid glycoprotein. |
| Volume of Distribution | Vd: 2–4 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral: 50–70% (first-pass effect); IM: 100%; IV: 100%. |
| Onset of Action | IM: 15–30 minutes; IV: 5–10 minutes; oral: 30–60 minutes. |
| Duration of Action | IM/IV: 1–2 hours; oral: 4–6 hours; antihypertensive effect persists 6–12 hours with controlled-release formulation. |
| Molecular Weight | 608.68 |
1-10 mg orally twice daily, titrate to effect.
| Dosage form | TABLET |
| Renal impairment | GFR <30 mL/min: reduce dose by 50%; GFR <15 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: contraindicated. |
| Pediatric use | 0.1-0.5 mg/kg/day divided every 12 hours, max 10 mg/day. |
| Geriatric use | Initiate at 1 mg once daily, titrate slowly; monitor for hypotension and sedation. |
| 1st trimester | Reserpine is contraindicated in first trimester due to risk of fetal malformations including skeletal abnormalities and CNS defects; use only if no alternative. |
| 2nd trimester | Use with caution; may cause maternal hypotension leading to reduced placental perfusion, respiratory depression, and bradycardia in fetus. |
| 3rd trimester | Avoid near term because reserpine may cause severe neonatal adverse effects such as nasal congestion, respiratory depression, bradycardia, and hypothermia. |
Clinical note
Comprehensive clinical and safety monograph for MODERIL (MODERIL).
| Placental transfer | Reserpine crosses the placenta, with fetal concentrations up to 50% of maternal levels; CNS effects observed in animal studies. |
| Breastfeeding | Reserpine is excreted into breast milk; may cause infant diarrhea, nasal congestion, and lethargy. Avoid breastfeeding during therapy. |
| Lactation Rating | L5 |
| Teratogenic Risk | Category C. First trimester: insufficient data; animal studies show embryotoxicity at high doses. Second/third trimesters: risk of fetal hypotension and renal impairment due to maternal hypotension; may reduce uteroplacental perfusion. |
| Fetal Monitoring | Maternal: blood pressure (sitting and standing) q1-2h initially, heart rate, signs of hypotension/syncope. Fetal: serial ultrasound for growth restriction (if used in 2nd/3rd trimesters), nonstress test or biophysical profile if preeclampsia risk; monitor for fetal bradycardia after maternal dosing. |
| Fertility Effects | No formal studies; animal data show no impairment of fertility at therapeutic doses. Postulated: alpha-1 blockade may affect ejaculatory function in males, but no evidence of altered spermatogenesis or impact on female fertility. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to reserpine or any componentHistory of mental depression, especially with suicidal tendenciesActive peptic ulcerUlcerative colitisElectroconvulsive therapy (within 2 weeks)Concomitant use with MAO inhibitors
| Precautions | Mental depression, especially in patients with history of depression, Peptic ulcer disease exacerbation, Electroconvulsive therapy (ECT) use caution due to severe reactions, Biliary colic in patients with gallstones, Surgery: increased susceptibility to hypotension and bradycardia |
| Food/Dietary | Avoid tyramine-rich foods (aged cheeses, cured meats, fermented products) to prevent hypertensive crises. |
| Clinical Pearls | Moderil (reserpine) is an antihypertensive alkaloid. Onset is slow (3-6 days) and duration prolonged (1-6 weeks). Use with caution in patients with history of depression or peptic ulcer. Monitor for bradycardia and orthostatic hypotension. Discontinue at least 2 weeks before elective surgery to reduce risk of hypotension with anesthetics. |
| Patient Advice | Take exactly as prescribed; do not stop suddenly due to risk of severe hypertension. · May cause drowsiness, dizziness, or nasal congestion; avoid driving if affected. · Rise slowly from sitting or lying to prevent fainting. · Report any signs of depression, mood changes, or nightmares to your doctor. · Avoid alcohol and other CNS depressants. · Inform all healthcare providers you are taking this medication. |
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