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

✍ Scribed by F. Gimenez; C. Gillotin; L. K. Basco; O. Bouchaud; A. -F. Aubry; I. W. Wainer; J. Bras; R. Farinotti

• Publisher: Springer
• Year: 1994
• Tongue: English
• Weight: 188 KB
• Volume: 46
• Category: Article
• ISSN: 0031-6970
• DOI: 10.1007/bf00196116

✦ Synopsis

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 x 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 gg. ml-i. h) than for ( -)-halofantrine (6127 gg-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.