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ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS › ANTIPROTOZOALS › AGENTS AGAINST LEISHMANIASIS AND TRYPANOSOMIASIS › Nitroimidazole derivatives
fexinidazole
P01CA03
Adult Dosing
- Human African Trypanosomiasis (Trypanosoma brucei gambiense): 1800 mg (three 600 mg tablets) once daily for 4 days, followed by 1200 mg (two 600 mg tablets) once daily for 6 days, taken with food.
Pediatric Dosing
- Children weighing >= 6 kg and >= 6 years of age: Dosed based on body weight and surface area following specific weight-band guidelines once daily for 10 days (4 days loading, 6 days maintenance), taken with food.
Indications
- Treatment of first-stage and non-severe second-stage human African trypanosomiasis (sleeping sickness) due to Trypanosoma brucei gambiense.
Mechanism of Action
- Nitroimidazole pro-drug that undergoes activation by parasite nitroreductases (such as Trypanosoma brucei NTR1) to generate reactive intermediates that inhibit DNA synthesis and disrupt cellular functions of the trypanosome.
Contraindications
- Hypersensitivity to fexinidazole or any component of the formulation
- Pre-existing prolongation of the QT interval
- Severe hepatic impairment
- Concomitant use of drugs known to prolong the QT interval or strong CYP3A4 inhibitors/inducers
Adverse Reactions
- Nausea
- Vomiting
- Decreased appetite
- Headache
- Insomnia
- Asthenia
- QT interval prolongation
- Psychiatric disorders (including psychotic disorder and anxiety)
Drug Interactions
- Avoid coadministration with QT-prolonging drugs (e.g., antiarrhythmics, fluoroquinolones, macrolides) due to additive risk of cardiac arrhythmias.
- Avoid concurrent use with strong CYP3A4 inducers or inhibitors which may alter fexinidazole exposure.
- Potential risk of additive CNS toxicity when used with other neurotoxic agents.
Curated Content: Needs Vetting Before Put to Clinical Use