Tetracycline Halofantrine

Chloroquine, quinine, mefloquine, halofantrine, proguanil, pyrimethamine, and tetracyclines blood schizontocides) kill these asexual forms. Drugs which act on this stage in the cycle of the parasite may be used for ... 

Huee antimalarial drags have polycyclic ring systems (Fig. 9-10) in common. The flrst is the common tetracycline anti biotic, doxycycline. The second is one of the newer drags luticated for malaria, halofantrine. The third is the discontinued agent used in the South Pacific, aminoacridine. 

Pyrimethamine-sulfadoxine or, plus Tetracycline or, plus Clindamycin Mefloquine Halofantrine... 

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. 

A study in 8 healthy subjects found that tetracycline 500 mg twice daily for 7 days increased the maximum plasma levels, AUC and elimination half-life of a single 500-mg dose of halofantrine by 146%, 99%, and 73%, respectively. Increases in the major metabolite of halofantrine also occurred in the presence of tetracycline. As both halofantrine and tetracycline are excreted into the bile, competition for this elimination route may result in increased plasma levels. There may be an increased risk of halofantrine toxicity if it is used with higher doses of tetracycline. In contrast, in vitro studies found that doxycycline does not inhibit the metabolism of halofantrine. ... 

Bassi PU, Onyeji CO, Ul onmwan OE. Effects of tetracycline on die pharmacokinetics of halofantrine in healthy volunteers. BrJ Clin Pharmacol (2004) 58, 52-5. 

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