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[奥美拉唑与肝脏细胞色素P450系统]

[Omeprazole and the cytochrome P450 system of the liver].

作者信息

Petersen K U

机构信息

Institut für Pharmakologie und Toxikologie der RWTH Aachen.

出版信息

Leber Magen Darm. 1993 Sep;23(5):186-92.

PMID:8412467
Abstract

Enzymes of the cytochrome P450 family play a key role in xenobiotic and thus drug metabolism. The H+,K(+)-ATPase blocker, omeprazole, has been reported to inhibit (subfamily P450IIC) or induce (P450IA) this system. The slower metabolic elimination of diazepam, warfarin und phenytoin is probably due to omeprazole competition for P450IIC; however, this effect was rather negligible in magnitude and not reproducible in each case. Also induction of P450IA was only minor; it resulted in no (theophylline) or trivial changes (caffeine) in elimination of drugs metabolized by this subfamily. Concerns about a possible increase in activation of procarcinogens by P450IA appear illfounded, given the fact that cruciferous vegetables such as broccoli and Brussels sprouts are potent inducers but may rather be associated with a lower incidence of certain types of cancer.

摘要

细胞色素P450家族的酶在异源物质以及药物代谢中起关键作用。据报道,H⁺,K⁺-ATP酶阻滞剂奥美拉唑可抑制(P450IIC亚家族)或诱导(P450IA)该系统。地西泮、华法林和苯妥英钠代谢消除减慢可能是由于奥美拉唑与P450IIC竞争;然而,这种效应在程度上相当微不足道,且并非在每种情况下都可重现。P450IA的诱导作用也很轻微;它对该亚家族代谢的药物消除没有影响(茶碱)或仅有轻微变化(咖啡因)。鉴于西兰花和抱子甘蓝等十字花科蔬菜是强效诱导剂,但可能与某些类型癌症的较低发病率相关,因此关于P450IA可能增加致癌物前体活化的担忧似乎没有根据。

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