摘要
由于对乙酰氨基酚用药普遍性和广泛性,其肝毒性问题日益引起人们的关注。本文介绍对乙酰氨基酚肝脏代谢、转运以及与Keap1-Nrf2通路有关的生理性调控机制,阐述对乙酰氨基酚的肝毒性机理,包括代谢损伤和氧化应激损伤两大理论。并以此为基础从吸收、代谢、转运等方面对其治疗靶点及干预药物加以综述。其中,Keap1-Nrf2抗氧化解毒通路和转运蛋白环节与对乙酰氨基酚肝毒性关系的研究在近几年逐渐增多,有望发现新的治疗靶点和对乙酰氨基酚肝毒性的有效治疗药物。
Because of the wide use of non-steroidal anti-inflammatory drugs acetaminophen,its hepatotoxicity is paid more and more attention.This review introduces its metabolism,disposition in liver and endogenous regulation mechanism related to Keap1-Nrf2 pathway;explains its mechanisms of hepatotoxicity involving two theories： metabolic injury and oxidative stress injury.Important of all,we focus on its intervention targets related to absorption,metabolism and transport of drugs.Recent studies are interested in the relationships between acetaminophen toxicity and Keap1-Nrf2 detoxifying pathway especially hepatobiliary transporters,which is expected to search for new therapeutic targets and effective drugs.
出处
《药学与临床研究》
2011年第3期247-252,共6页
Pharmaceutical and Clinical Research
