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对乙酰氨基酚代谢及其相关的遗传差异。

Paracetamol metabolism and related genetic differences.

机构信息

Institute of Clinical Pharmacology, Sun Yat-Sen University, Guangzhou, China.

出版信息

Drug Metab Rev. 2011 Feb;43(1):41-52. doi: 10.3109/03602532.2010.527984. Epub 2010 Nov 25.

Abstract

Paracetamol (acetaminophen) is a worldwide used analgesic and antipyretic drug. It is metabolised via several metabolic pathways, including glucuronidation, sulfation, oxidation, hydroxylation, and deacetylation: Hepatic and other organ damage may occur, especially in overdose, because of the accumulation of a toxic metabolite. Intersubject and ethnic differences have been reported in paracetamol metabolism activation, suggesting possible differences in susceptibility to toxicity and in pain alleviation, linked to different pharmacogenetic profiles. This article aims at reviewing, in the literature, the links between paracetamol metabolism and enzyme genotypes in the context of toxic side effects and efficacy of paracetamol in therapeutics.

摘要

对乙酰氨基酚(acetaminophen)是一种在全球范围内使用的止痛和退热药物。它通过多种代谢途径代谢,包括葡萄糖醛酸化、硫酸化、氧化、羟化和脱乙酰化:由于有毒代谢物的积累,肝和其他器官损伤可能发生,尤其是在过量用药的情况下。据报道,对乙酰氨基酚代谢激活存在个体间和种族差异,这表明对毒性的易感性和对疼痛缓解的效果可能存在差异,这与不同的药物遗传学特征有关。本文旨在回顾文献中对乙酰氨基酚代谢与酶基因型之间的联系,探讨其在毒性副作用和治疗效果方面的作用。

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