Plasma and brain pharmacokinetics of amitriptyline and its demethylated and hydroxylated metabolites after one and six half-life repeated administrations to rats

被引：23

作者：

Coudore, F

Besson, A

Eschalier, A

Lavarenne, J

Fialip, J

机构：

[1] FAC PHARM CLERMONT FERRAND, PHARMACOL LAB, F-63001 CLERMONT FERRAND, FRANCE

[2] FAC MED, LAB PHARMACOL MED, F-63001 CLERMONT FERRAND, FRANCE

来源：

GENERAL PHARMACOLOGY-THE VASCULAR SYSTEM | 1996年 / 27卷 / 02期

关键词：

amitriptyline; acute and repeated administration; rat demethylated and hydroxylated metabolites;

D O I：

10.1016/0306-3623(95)02008-X

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The purposes of the present study were as follows: 1. After an acute intraperitoneal (IP) administration of amitriptyline (AMI) to male Sprague-Dawley rats we found that: (i) its absorbtion rate is rapid; (ii) its elimination half life is muck shorter than in humans; and (iii) its levels largely exceeded those of its metabolites. The most important metabolites being 10-hydroxynortriptyline and nortriptyline in plasma and brain, respectively. 2. After six (every half life) repeated IP administrations: (i) AMI kinetic parameters were unchanged; and (ii) amounts of metabolites were significantly increased and the levels of AMI were lowered both in plasma and brain.

引用

页码：215 / 219

页数：5

共 25 条

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