ISSN:
1432-1041
Keywords:
Halofantrine
;
Enantiomers
;
Malaria
;
stereoselectivity
;
Plasmodium falciparum
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
,
Medicine
Notes:
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.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00196116