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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › AGENTS AGAINST LEISHMANIASIS AND TRYPANOSOMIASIS › Nitroimidazole derivatives
benznidazole
P01CA02
Forms & Strengths
- Tablets: 12.5 mg
- Tablets: 100 mg
Adult Dosing
- Chagas disease (American trypanosomiasis): 5 to 7 mg/kg/day orally divided into two doses for 60 days
- Maximum daily dose: 400 mg/day
Pediatric Dosing
- Pediatric patients 2 to 12 years: 5 to 10 mg/kg/day orally divided into two doses for 60 days
- Maximum daily dose: 300 mg/day
Indications
- Treatment of Chagas disease caused by Trypanosoma cruzi in pediatric patients aged 2 to 12 years
Mechanism of Action
- Nitroimidazole prodrug reduced by parasite-specific nitroreductase (NTR-1) to reactive intermediate metabolites
- Metabolites bind to parasite macromolecules, inducing DNA damage, lipid peroxidation, and oxidative stress leading to parasite death
Contraindications
- Hypersensitivity to benznidazole, other nitroimidazole derivatives, or excipients
- Concomitant use of alcohol (disulfiram-like reaction)
- Severe hepatic impairment
- Severe renal impairment
Adverse Reactions
- Dermatologic: Rash, dermatitis, pruritus, toxic epidermal necrolysis
- Nervous system: Peripheral neuropathy, paresthesia, headache, dizziness, insomnia
- Gastrointestinal: Nausea, vomiting, abdominal pain, anorexia
- Hematologic: Leukopenia, thrombocytopenia, agranulocytosis
- Psychiatric: Depression, irritability
Drug Interactions
- Alcohol: May cause disulfiram-like reactions (flushing, cramps, vomiting, tachycardia)
- Lithium: Potential for increased lithium toxicity
- CYP450 substrates: Potential interaction as a weak inhibitor or inducer, monitor closely
- Myelosuppressive agents: Increased risk of bone marrow suppression and hematologic toxicity
Curated Content: Needs Vetting Before Put to Clinical Use