大鼠体内丙咪嗪 - N - 氧化物的动力学

The kinetics of imipramine-N-oxide in rats.

作者信息

Nagy A

出版信息

Acta Pharmacol Toxicol (Copenh). 1978 Jan;42(1):68-72. doi: 10.1111/j.1600-0773.1978.tb02170.x.

DOI:10.1111/j.1600-0773.1978.tb02170.x

Abstract

Rats were given imipramine-N-oxide as single intramuscular injection and then as repeated oral doses. Imipramine-N-oxide and the metabolites imipramine and desipramine were analysed in the blood cells, plasma and brain tissue. The concentration of imipramine-N-oxide increased simultaneously in the brain and blood, reaching a peak 45 minutes after a single dose. Imipramine was the quantitatively predominant metabolite in the blood cells and brain, while desipramine reached a higher concentration than imipramine in the plasma. Samples taken at different times after oral doses during continuous treatment showed fairly constant concentrations of imipramine-N-oxide and desipramine in the brain, whereas the concentration of imipramine was more fluctuating.

摘要

给大鼠单次肌内注射氧化丙咪嗪，然后重复口服给药。对血细胞、血浆和脑组织中的氧化丙咪嗪及其代谢产物丙咪嗪和地昔帕明进行分析。氧化丙咪嗪在脑和血液中的浓度同时升高，单次给药后45分钟达到峰值。丙咪嗪是血细胞和脑中含量占优势的代谢产物，而地昔帕明在血浆中的浓度高于丙咪嗪。在连续治疗期间口服给药后不同时间采集的样本显示，脑中氧化丙咪嗪和地昔帕明的浓度相当恒定，而丙咪嗪的浓度波动较大。