title: Plasma concentrations of the enantiomers of halofantrine and its main metabolite in malaria patients.
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.
authors.affiliation: Service Pharmacie-Pharmacocinétique, Hôpital Pitié Salpétrière, Paris, France.
authors.forename: F
authors.initials: F
authors.lastname: Gimenez
authors.forename: C
authors.initials: C
authors.lastname: Gillotin
authors.forename: L K
authors.initials: LK
authors.lastname: Basco
authors.forename: O
authors.initials: O
authors.lastname: Bouchaud
authors.forename: A F
authors.initials: AF
authors.lastname: Aubry
authors.forename: I W
authors.initials: IW
authors.lastname: Wainer
authors.forename: J
authors.initials: J
authors.lastname: Le Bras
authors.forename: R
authors.initials: R
authors.lastname: Farinotti
mesh_terms: 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
chemical_list: D000962:Antimalarials; D010616:Phenanthrenes; C023768:halofantrine