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Clopidogrel pathway.

机译:氯吡格雷途径。

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摘要

After oral- administration, clopidogrel is rapidly absorbed. Owing to its extensive metabolism, clopidogrel is not detected in human plasma. Clopidogrel is a prodrug that is absorbed in the intestine [3,4] and activated in the liver [5]. The conversion of clopidogrel to its active metabolite requires two sequential oxidative steps. As shown in Fig. 1, the first step leads to formation of 2-oxo-clopidogrel, followed by the conversion of 2-oxo-clopidogrel to the active metabolite. GYP1A2, GYP2B6, CYP2C9, CYP2G19, and CYP3A4/5 are implicated as cytochrome P450 enzymes involved in the metabolism of clopidogrel.
机译:口服给药后,氯吡格雷被迅速吸收。由于其广泛的新陈代谢,在人血浆中未检测到氯吡格雷。氯吡格雷是一种前药,可在肠道[3,4]中吸收并在肝脏中激活[5]。氯吡格雷向其活性代谢物的转化需要两个连续的氧化步骤。如图1所示,第一步导致形成2-氧代氯吡格雷,然后将2-氧代氯吡格雷转化为活性代谢物。 GYP1A2,GYP2B6,CYP2C9,CYP2G19和CYP3A4 / 5与参与氯吡格雷代谢的细胞色素P450酶有关。

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