Halofantrine hydrochloride

Halofantrine hydrochloride, a phenanthrene-methanol, is effective against erythrocytic (but not other) stages of all four human malaria species. Oral absorption is variable and is enhanced with food. Because of toxicity concerns, it should not be taken with meals. Plasma levels peak 16 hours after dosing, and the half-life is about 4 days. Excretion is mainly in the feces. The mechanism of action of halofantrine is unknown. The drug is not available in the USA (although it has been approved by the FDA), but it is widely available in malaria-endemic countries. 

Taillardat-Bertschinger, A. C.S. Perry A. Galland R.J. Prankerd W.N. Charman. Partitioning of halofantrine hydrochloride between water, micellar solutions, and soybean oil Effects on its apparent ionization constant./. Pharm. Sci. 2003, 92, 2217—2228. 

The recently introduced antimalanal halofantrine (6) is an orally active blood schizonucide reported to be more than 95% effective in the treatment of malaria [S] Mefloquine hydrochloride (7) contmues to be useful m the prophylaxis and treatment of malaria [9]... 

Porter, C.J.H., et al. 1996. Lymphatic transport of halofantrine in the conscious rat when administered as either the free base or the hydrochloride salt Effect of lipid class and lipid vehicle dispersion. J Pharm Sci 85 357. 

Anabwani G, Canfield CJ, Hutchinson DB. Combination atovaquone and proguanil hydrochloride vs. halofantrine for treatment of acute Plasmodium falciparum malaria in children. Pediatr Infect Dis J 1999 18(5) 456-61. 

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