Melarsoprol
Mechanism :
Melarsoprol is a trivalent arsenical compound that irreversibly binds to vicinal sulfhydryl groups on pyruvate kinase, which disrupts energy production in the parasite.
Indication :
- African Trypanosomiasis (Sleeping Sickness):Used for the treatment of late stages of T. b. gambiense and T. b. rhodesiense infections involving the CNS.
Contraindications :
Glucose-6-phosphate dehydrogenase (G6PD) deficiency, hypersensitivity.
Dosing :
18-25 mg/kg total over 1 month. Initial 0.36 mg/kg IV followed by gradually increasing to 3.6 mg/kg IV at intervals of 1-5 days for total of 9-10 doses.
Adverse Effect :
Glucose-6-phosphate dehydrogenase (G6PD) deficiency, hypersensitivity.
Hypertension, myocardial damage, encephalopathy, peripheral neuropathy, colic, vomiting, albuminuria, herxheimer-type reaction, arsenic encephalopathy.
Hepatic Dose :
No dosage adjustments are recommended.