Halofantrine Foods

Humberstone AJ, Porter CJ and Charman WN (1996) A Physicochemical Basis for the Effect of Food on the Absolute Oral Bioavailability of Halofantrine. J Pharm Sci 85 pp 525-529. 

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. 

Among potential malarial treatments attributable to the program are 1) mefloquine, 2) halofantrine, 3) artemisinin, and 4) a compound currently known as WR238605. Mefloguine was developed jointly by Walter Reed, WHO, and Hoffman-LaRoche, Inc., and was recently approved for U.S. marketing by the U.S. Food and Drug Administration (FDA). Halofantrine is a potential prophylactic jointly developed by Walter Reed and SmithKline Beecham that may be effective... 

Pyrimethamine/sulfadoxine and tetracycline have been shown to increase halofantrine levels, and may therefore increase its toxicity. Diltiazem, erythromycin, ketoconazole, mefloquine, quinine, and quinidine might also increase the toxicity of halofantrine because they have been shown to inhibit its metabolism in vitro. The manufacturer has therefore recommended caution with the concurrent use of potent CYP3A4 inhibitors. Fatty food markedly increases halofantrine levels, consequently it is recommended that halofantrine is taken on an empty stomach. Grapefruit juice has a similar effect Note that halofantrine is no longer widely marketed. 

Milton K, Edwards G, Ward SA, Orme ML E, Breckenridge AM. Pharmacokinetics of halofantrine in man effects of food and dose size. BrJ Clin Pharmacol (1989) 28, 71-7. 

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