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亚急性给药以及苯巴比妥和3-甲基胆蒽预处理对大鼠对乙酰氨基酚代谢的影响。

Effect of subacute dosing and phenobarbital and 3-methylcholanthrene pretreatment on the metabolism of acetaminophen in rats.

作者信息

Thomas B H, Zeitz W, Beaubien A R

出版信息

Can J Physiol Pharmacol. 1977 Feb;55(1):77-83. doi: 10.1139/y77-011.

Abstract

The metabolism of 14C-ring-labelled acetaminophen was studied in male Wistar rats. Pretreatment with phenobarbital increased the initial rate of elimination of 14C from the blood and increased the amount of acetaminophen glucuronide excreted in the urine. Pretreatment with 3-methylcholanthrene did not significantly affect the rate of elimination from the blood and decreased the amount of acetaminophen glucuronide in the urine. Daily dosing with acetaminophen for up to 3 weeks increased the rate of elimination of 14C from the blood after 4 h, and increased the urinary excretion of both total 14C and the glucuronide and sulfate conjugates. Subacute dosing with acetaminophen had a diuretic effect but this did not correlate with the increased excretion of the drug. It is concluded that acetaminophen elimination is increased by phenobarbital pretreatment and by subacute dosing with acetaminophen, but by different mechanisms.

摘要

在雄性Wistar大鼠中研究了14C环标记对乙酰氨基酚的代谢。用苯巴比妥预处理可提高血液中14C的初始消除速率,并增加尿中对乙酰氨基酚葡萄糖醛酸苷的排泄量。用3-甲基胆蒽预处理对血液中的消除速率没有显著影响,并降低了尿中对乙酰氨基酚葡萄糖醛酸苷的含量。连续3周每日给予对乙酰氨基酚,4小时后可提高血液中14C的消除速率,并增加总14C以及葡萄糖醛酸苷和硫酸盐结合物的尿排泄量。对乙酰氨基酚亚急性给药具有利尿作用,但这与药物排泄增加无关。得出的结论是,苯巴比妥预处理和对乙酰氨基酚亚急性给药均可增加对乙酰氨基酚的消除,但机制不同。

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