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Plasma concentrations of the enantiomers of halofantrine and its main metabolite in malaria patients

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Abstract

The plasma concentrations of the enantiomers of halofantrine and its N-desbutyl metabolite in six patients with malaria were measured after oral administration of 3×750 mg doses of micronised, racemic halofantrine hydrochloride given at 6-hour intervals.

Significant differences were observed between the plasma concentrations of the enantiomers both of halofantrine and its N-monodesbutyl metabolite. AUC084h values were higher for (+)halofantrine (9917 μg·ml−1·h) than for (-)-halofantrine (6127 μg·ml−1·h).

The clinical significance of these observations is not known. The isomers have equipotent activity in vitro but their relative toxicity has not yet been assessed.

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Gimenez, F., Gillotin, C., Basco, L.K. et al. Plasma concentrations of the enantiomers of halofantrine and its main metabolite in malaria patients. Eur J Clin Pharmacol 46, 561–562 (1994). https://doi.org/10.1007/BF00196116

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  • DOI: https://doi.org/10.1007/BF00196116

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