Plasma concentrations of the enantiomers of halofantrine and its main metabolite in malaria patients.
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.
Gimenez
F
F
Service Pharmacie-Pharmacocinétique, Hôpital Pitié Salpétrière, Paris, France.
Gillotin
C
C
Basco
L K
LK
Bouchaud
O
O
Aubry
A F
AF
Wainer
I W
IW
Le Bras
J
J
Farinotti
R
R
D000328:Adult; D000962:Antimalarials / Q000493:pharmacokinetics*; D006801:Humans; D008288:Malaria / Q000188:drug therapy / Q000378:metabolism*; D008875:Middle Aged; D010616:Phenanthrenes / Q000493:pharmacokinetics* / Q000627:therapeutic use; D013237:Stereoisomerism
D000962:Antimalarials; D010616:Phenanthrenes; C023768:halofantrine