KINETICS OF METAPRAMINE AND ITS DEMETHYLATED METABOLITES AFTER SINGLE AND CHRONIC ORAL-ADMINISTRATION IN MAN

被引:5
作者
BOUGEROLLE, AM
CHABARD, JL
DORDAIN, G
FRYDMAN, A
GAILLOT, J
PIRON, JJ
PETIT, J
BERGER, JA
机构
[1] FAC PHARM CLERMONT FERRAND, CHIM ANALYT LAB, PL H DUNANT, BP 38, F-63001 CLERMONT FERRAND, FRANCE
[2] CTR HOSP REG & UNIV CLERMONT FERRAND, HOP NORD, SERV NEUROL, CLERMONT FERRAND, FRANCE
[3] INSERM, U17, CLERMONT FERRAND, FRANCE
[4] RHONE POULENC, INST BIOPHARM, DEPT DIODYNAM, ANTONY, FRANCE
[5] SPECIA, DEPT PSYCHOTROPES, PARIS, FRANCE
关键词
D O I
10.1007/BF03189836
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The kinetics of metapramine and two of its demethylated metabolites were determined in six normal subjects after oral administration of a single 150 mg dose on day 1 and 3 .times. 50 mg dose on day 2-6. This study has shown that three demethylated metabolites were found in plasma beside metapramine. The monodemethylated metabolite I appeared to be the predominant one and the mean area under the plasma concentration curve .**GRAPHIC**. was 49% of the metapramine value. Its half-life was shorter (5,92 h) than that of metapramine (8,29 h). The kinetic profiles of metapramine and its major metabolites I and II were similar and data over 24 h could be fitted by a tri-exponential equation even though entero-hepatic cycles were observed. A high interindividual variability of data was found for both metapramine and its metabolites. There were no significant differences between men and women. The minimal plasma level (Cmin) seemed in agreement with the half-life of the drug.
引用
收藏
页码:113 / 118
页数:6
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