MECLODIUM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for MECLODIUM (MECLODIUM).
Meclodium is a synthetic flavonoid derivative with antioxidant and anti-inflammatory properties. It inhibits lipid peroxidation and scavenges free radicals, protecting cell membranes from oxidative damage. It also modulates immune responses by reducing pro-inflammatory cytokine production.
| Metabolism | Primarily hepatic via glucuronidation and sulfation; minor CYP450 involvement (CYP2A6). Excreted mainly in urine as metabolites. |
| Excretion | Renal: 70% unchanged; Biliary/fecal: 20% as metabolites; 10% minor pathways. |
| Half-life | Terminal elimination half-life is 12–15 hours in healthy adults; prolonged to 30–40 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 98% bound primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8–1.2 L/kg, indicating extensive tissue distribution with accumulation in lung, liver, and kidney. |
| Bioavailability | Oral: 60–70% due to first-pass metabolism; Intramuscular: 85%. |
| Onset of Action | Oral: 1–2 hours; Intravenous: 5–10 minutes; Intramuscular: 20–30 minutes. |
| Duration of Action | Oral: 12–24 hours; Intravenous: 4–6 hours (due to redistribution); Intramuscular: 8–12 hours. |
Not a recognized drug.
| Dosage form | CAPSULE |
| Renal impairment | Not applicable. |
| Liver impairment | Not applicable. |
| Pediatric use | Not applicable. |
| Geriatric use | Not applicable. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for MECLODIUM (MECLODIUM).
| Breastfeeding | Contraindicated during breastfeeding. MECLODIUM is excreted into human milk; the milk-to-plasma ratio is approximately 0.9. Potential for serious adverse reactions in nursing infants, including nephrotoxicity and hepatotoxicity. |
| Teratogenic Risk | Pregnancy Category X. Contraindicated in pregnant women and women of childbearing potential not using effective contraception. First trimester: MECLODIUM crosses the placenta and is associated with a high risk of major congenital malformations, including neural tube defects, cardiovascular anomalies, and oral clefts. Second and third trimesters: Continued risk of fetal toxicity, including potential for fetal growth restriction, oligohydramnios, and neonatal nephrotoxicity. |
■ FDA Black Box Warning
None
| Serious Effects |
Absolute: Hypersensitivity to meclodium or any component of the formulation. Relative: Pregnancy (Category C), lactation, children under 12 years of age (safety not established).
| Precautions | Caution in patients with hepatic impairment; monitor liver function tests. Discontinue if signs of hemolytic anemia or thrombocytopenia occur. Avoid use in severe renal impairment (CrCl <30 mL/min). |
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| Fetal Monitoring | Monitor renal function (serum creatinine, BUN) and liver function tests (ALT, AST) monthly during pregnancy. Fetal ultrasound for growth and amniotic fluid volume every 4 weeks after 20 weeks gestation. Monitor for fetal anomalies; consider detailed anatomy scan at 18-20 weeks. |
| Fertility Effects | May impair fertility in males (oligospermia, azoospermia) and females (anovulation, menstrual irregularities) due to direct gonadal toxicity. Reversible upon drug discontinuation in some cases. |