ENANTIOSELECTIVE PHARMACOKINETICS OF HOMOCHLORCYCLIZINE .2. DISPOSITION AND METABOLISM OF (+)-, (-)- AND RACEMIC HOMOCHLORCYCLIZINE AFTER ORAL-ADMINISTRATION TO MAN

被引：6
作者：
NISHIKATA, M
NOMURA, A
ISEKI, K
MIYAZAKI, K
NAKAI, A
FUSHIDA, H
MIYAKE, K
ARITA, T
机构：
[1] HOKKAIDO UNIV,SCH MED,DEPT CARDIOVASC MED,SAPPORO,HOKKAIDO 060,JAPAN
[2] MUKOGAWA WOMENS UNIV,FAC PHARMACEUT SCI,NISHINOMIYA,HYOGO 663,JAPAN
来源：
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY | 1992年 / 43卷 / 05期
关键词：
HOMOCHLORCYCLIZINE; ENANTIOSELECTIVE; METABOLISM; PHARMACOKINETICS; PROTEIN BINDING; SIDE EFFECTS;
D O I：
10.1007/BF02285097
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
The pharmacokinetics of a single oral dose of 20 mg (+)-, (-)- and racemic homochlorcyclizine (HCZ) have been studied in humans. The formation of the quarternary ammonium-linked glucuronide was an important metabolic pathway, and the metabolic process was enantioselective as a result of differing urinary excretion rates of (+)-, (-)- and racemic glucuronide. There were significant differences between (+)-, (-)- and racemic HCZ in AUC (0-14 h) and plasma protein binding, but all HCZ enantiomers were slowly absorbed and eliminated (elimination half-lives about 11 h). The results shows help to establish a more efficient dosage regimen for HCZ therapy.
引用
收藏
页码：533 / 538
页数：6
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