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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › AGENTS AGAINST LEISHMANIASIS AND TRYPANOSOMIASIS › Antimony compounds
meglumine antimonate
P01CB01
Forms & Strengths
- Solution for injection: 30% w/v in 5 mL ampoules (equivalent to 8.1% or 81 mg/mL pentavalent antimony)
Adult Dosing
- Cutaneous leishmaniasis: 20 mg Sb5+/kg/day intramuscularly for 20-25 days
- Visceral leishmaniasis: 20 mg Sb5+/kg/day intramuscularly or intravenously for 28-30 days
- Mucosal leishmaniasis: 20 mg Sb5+/kg/day intramuscularly for 30 days
Pediatric Dosing
- Cutaneous leishmaniasis: 20 mg Sb5+/kg/day intramuscularly for 20-25 days (same as adult mg/kg dosing)
- Visceral leishmaniasis: 20 mg Sb5+/kg/day intramuscularly or intravenously for 28-30 days
Indications
- Treatment of visceral leishmaniasis (kala-azar)
- Treatment of cutaneous leishmaniasis
- Treatment of mucocutaneous leishmaniasis
Mechanism of Action
- Pentavalent antimony prodrug converted intracellularly to active trivalent antimony
- Inhibits parasite glycolysis and fatty acid oxidation
- Decreases parasite intracellular ATP and GTP levels
Contraindications
- Severe hepatic impairment
- Severe renal impairment
- Severe cardiac disease or arrhythmias
- Hypersensitivity to meglumine antimonate or antimony compounds
Adverse Reactions
- Cardiotoxicity: ECG changes (T-wave inversion, QT prolongation), arrhythmias
- Gastrointestinal: abdominal pain, nausea, vomiting, anorexia
- Musculoskeletal: myalgia, arthralgia
- Neurological: headache, dizziness, malaise
- Hepatic and renal: transient elevation of transaminases and BUN/creatinine
- Injection site pain and local thrombophlebitis
Drug Interactions
- QT-prolonging drugs (e.g., antiarrhythmics, macrolides): increased risk of fatal cardiac arrhythmias
- Nephrotoxic drugs: increased risk of renal impairment
- Hepatotoxic drugs: potential for additive liver injury
Curated Content: Needs Vetting Before Put to Clinical Use