氯喹去乙基代谢物在大鼠体内的分布及尿排泄情况。

Distribution and urinary excretion of the desethylmetabolites of chloroquine in the rat.

作者信息

Salako L A, Ajayi F O

机构信息

Department of Pharmacology & Therapeutics, University of Ibadan, Nigeria.

出版信息

J Pharm Pharmacol. 1987 Oct;39(10):859-60. doi: 10.1111/j.2042-7158.1987.tb05136.x.

DOI:10.1111/j.2042-7158.1987.tb05136.x

PMID:2891831

Abstract

The tissue distribution of desethylchloroquine and bisdesethylchloroquine has been studied in rats after single intraperitoneal administration of the drugs at a dose of 10 mg kg-1. Concentrations of the chloroquine metabolites in the liver, heart, lungs, kidney and spleen were 34 to 250 times higher than their plasma concentrations 24 h after the drugs had been injected. Urinary excretion of the drugs was studied in rats after single intravenous administration of 2.5, 5 or 10 mg kg-1 doses. The total estimated urinary excretion of desethylchloroquine and bisdesethylchloroquine was 25 and 64% respectively of the administered dose, with the maximum urinary excretion occurring on the first day. The results show that the desethylmetabolites of chloroquine are concentrated in the tissues in the same manner as the parent compound.

摘要

在大鼠腹腔注射剂量为10 mg kg-1的药物后，研究了去乙基氯喹和双去乙基氯喹的组织分布。注射药物24小时后，肝脏、心脏、肺、肾脏和脾脏中氯喹代谢物的浓度比血浆浓度高34至250倍。在大鼠单次静脉注射2.5、5或10 mg kg-1剂量后，研究了药物的尿排泄情况。去乙基氯喹和双去乙基氯喹的总尿排泄量分别估计为给药剂量的25%和64%，最大尿排泄量出现在第一天。结果表明，氯喹的去乙基代谢物与母体化合物一样以相同的方式在组织中富集。