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  • Title: Plasma concentrations of the enantiomers of halofantrine and its main metabolite in malaria patients.
    Author: Gimenez F, Gillotin C, Basco LK, Bouchaud O, Aubry AF, Wainer IW, Le Bras J, Farinotti R.
    Journal: Eur J Clin Pharmacol; 1994; 46(6):561-2. PubMed ID: 7995326.
    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 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. AUC(0)84h values were higher for (+)halofantrine (9917 micrograms.ml-1.h) than for (-)-halofantrine (6127 micrograms.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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