Eflornithine, (DL-alpha-difluoromethylornithine) is a fluorinated analogue of the uncommon amino acid ornithine.
Eflornithine is highly effective against Trypanosoma brucei gambiense and, when available, is the drug of choice in late-stage Gambian human African trypanosomiasis. Eflornithine is not effective against Trypanosoma brucei rhodesiense.
Eflornithine is an irreversible suicide inhibitor of ornithine decarboxylase, the first enzyme in the biosynthesis of the polyamines putrescine and spermidine.
The mechanisms of eflornithine resistance for T.b. gambiense have not yet been elucidated.
Eflornithine is about 50% orally bioavailable. Its elimination half-life is 3.3 h and 81% is excreted unchanged.
The recommended dosage for new cases of late-stage Gambian trypanosomiasis is 100 mg/kg every 6h IV for 14 days.
Reduce dosage in renal failure.
Hematological: anemia (up to 40%), leukopenia (20-30%) or thrombocytopenia (50%).
Seizures associated with high CSF concentrations
Diarrhea (12% IV, 50% po)
Abortion in pregnant women
Studies with eflornithine have not been done in pregnant women.
No data.
Ornidyl™ (Aventis)