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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › AGENTS AGAINST LEISHMANIASIS AND TRYPANOSOMIASIS › Arsenic compounds
melarsoprol
P01CD01
Forms & Strengths
- Injectable solution: 3.6% (180 mg in 5 mL ampoules)
Adult Dosing
- Human African Trypanosomiasis (Trypanosoma brucei rhodesiense): 3.6 mg/kg/day IV (max 200 mg/day) for 3-4 days, repeat after 7-10 days; alternative courses exist depending on protocol.
Pediatric Dosing
- Human African Trypanosomiasis: Safety and efficacy not formally established in children; dosing follows weight-based regimens (e.g., 3.6 mg/kg/day total cumulative dose scaling) under expert tropical disease guidance.
Indications
- Treatment of second-stage Human African Trypanosomiasis (sleeping sickness) caused by Trypanosoma brucei rhodesiense or late-stage T. b. gambiense refractory to eflornithine.
Mechanism of Action
- Arsenical compound that reacts with sulfhydryl groups of trypanosomal enzymes (such as trypanothione reductase), inhibiting parasite metabolism and causing parasite death.
Contraindications
- Glucose-6-phosphate dehydrogenase (G6PD) deficiency
- Current acute infections other than trypanosomiasis
- Hypersensitivity to melarsoprol
Adverse Reactions
- Reactive encephalopathy (potentially fatal)
- Myocardial damage and heart failure
- Peripheral neuropathy
- Albuminuria and hypertension
- Injection site thrombophlebitis and pain
- Gastrointestinal distress (nausea, vomiting, abdominal pain)
- Hemolysis in G6PD-deficient patients
Drug Interactions
- Increased risk of neurotoxicity when used with other neurotoxic drugs
- Additive cardiotoxicity with other QT-prolonging or cardiotoxic medications
- Caution with concomitant medications metabolized by or affecting hepatic function due to high drug toxicity profile
Curated Content: Needs Vetting Before Put to Clinical Use