Plasma concentrations of the enantiomers of halofantrine and its main metabolite in malaria patients
Gimenez, F. ; Gillotin, C. ; Basco, L. K. ; Bouchaud, O. ; Aubry, A. -F. ; Wainer, I. W. ; Bras, J. ; Farinotti, R.
Springer
Published 1994
Springer
Published 1994
| ISSN: |
1432-1041
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|---|---|
| Keywords: |
Halofantrine ; Enantiomers ; Malaria ; stereoselectivity ; Plasmodium falciparum
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| Source: |
Springer Online Journal Archives 1860-2000
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| Topics: |
Chemistry and Pharmacology
Medicine
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| 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.
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| Type of Medium: |
Electronic Resource
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| URL: |