PLASMA-CONCENTRATIONS OF THE ENANTIOMERS OF HALOFANTRINE AND ITS MAIN METABOLITE IN MALARIA PATIENTS

被引：20

作者：

GIMENEZ, F

GILLOTIN, C

BASCO, LK

BOUCHAUD, O

AUBRY, AF

WAINER, IW

LEBRAS, J

FARINOTTI, R

机构：

[1] FAC PHARM CHATENAY MALABRY,DEPT CLIN PHARM,CHATENAY MALABRY,FRANCE

[2] HOP BICHAT CLAUDE BERNARD,SERV PARASITOL,PARIS,FRANCE

[3] HOP BICHAT CLAUDE BERNARD,DEPT MALAD INFECT & TROP,PARIS,FRANCE

[4] MCGILL UNIV,DIV ONCOL,MONTREAL,PQ,CANADA

来源：

EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY | 1994年 / 46卷 / 06期

关键词：

HALOFANTRINE; ENANTIOMERS; MALARIA; STEREOSELECTIVITY; PLASMODIUM FALCIPARUM;

D O I：

10.1007/BF00196116

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 mu g.ml(-1).h) than for (-)-halofantrine (6127 mu g.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.

引用

页码：561 / 562

页数：2

共 6 条

[1] INVITRO ACTIVITY OF THE ENANTIOMERS OF MEFLOQUINE, HALOFANTRINE AND ENPIROLINE AGAINST PLASMODIUM-FALCIPARUM [J].