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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Coadministration of acetaminophen and troglitazone: pharmacokinetics and safety.
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Coadministration of acetaminophen and troglitazone: pharmacokinetics and safety.

机译：对乙酰氨基酚和曲格列酮的共同给药：药代动力学和安全性。

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摘要

Troglitazone, a PPAR-gamma agonist, enhances the actions of insulin on muscle and liver. It is metabolized predominantly in the liver to a sulfate conjugate and a quinone metabolite. Acetaminophen also undergoes metabolism by conjugation. This three-way crossover study in 12 healthy male volunteers was conducted to investigate the effects of acetaminophen on the metabolism of troglitazone and vice versa. No statistically or clinically relevant differences in area under the concentration-time curve extrapolated to infinity (AUCinfinity) were observed for troglitazone, its quinone metabolite, or acetaminophen. A statistically significant decrease in troglitazone sulfate conjugate during administration with acetaminophen was not clinically relevant. No statistically or clinically relevant differences were observed in maximum concentration (Cmax), time to Cmax (tmax), or elimination half-life of troglitazone, its two main metabolites, and acetaminophen or in acetaminophen urinary sulfate excretion, although there was a slight decrease in acetaminophen glucuronide excretion during administration with troglitazone. Adverse events were minor and similar between treatments. These findings suggest that troglitazone and acetaminophen can be coadministered without adverse clinical consequences.
机译：曲格列酮是一种PPAR-γ激动剂，可增强胰岛素对肌肉和肝脏的作用。它主要在肝脏中代谢为硫酸盐结合物和醌代谢物。对乙酰氨基酚也可以通过结合而代谢。这项针对12名健康男性志愿者的三项交叉研究旨在研究对乙酰氨基酚对曲格列酮代谢的影响，反之亦然。对于曲格列酮，其醌代谢产物或对乙酰氨基酚，未观察到浓度-时间曲线外推至无穷大（AUCinfinity）下面积的统计或临床相关差异。在对乙酰氨基酚给药期间，硫酸曲格列酮缀合物的统计学显着减少与临床无关。在最大浓度（Cmax），达到Cmax的时间（tmax）或曲格列酮，其两种主要代谢产物和对乙酰氨基酚或对乙酰氨基酚尿硫酸盐排泄的消除半衰期方面，未观察到统计学或临床相关差异，尽管略有降低曲格列酮给药期间对乙酰氨基酚葡糖苷酸排泄的作用。治疗之间的不良事件较小且相似。这些发现表明曲格列酮和对乙酰氨基酚可以并用而不会产生不利的临床后果。

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