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中国临床药理学与治疗学 ›› 2005, Vol. 10 ›› Issue (7): 721-725.

• 综述 •    下一篇

CYP3A4 和P 糖蛋白与药物的肠道处置

辛华雯   

  1. 广州军区武汉总医院临床药理科, 武汉430070, 湖北
  • 收稿日期:2005-05-08 修回日期:2005-06-20 出版日期:2005-07-26 发布日期:2020-11-10
  • 通讯作者: 辛华雯, 女, 医学博士, 副主任医师, 主要从事临床药理学研究。Tel:027-68878689 E-mail: huawenxin2005@hotmail.com
  • 基金资助:
    湖北省自然科学基金资助课题(NO2002AB114)

Impact of CYP3A4 and P-glycoprotein on drug disposition in intestine

XIN Hua-wen   

  1. Department of Clinical Pharmacology, Wuhan General Hospital, Wuhan 430070, Hubei, China
  • Received:2005-05-08 Revised:2005-06-20 Online:2005-07-26 Published:2020-11-10

摘要: 肠CYP3A4 介导的生物转化和P 糖蛋白介导的药物主动泵出肠细胞是决定口服药物生物利用度的主要因素。有证据显示CYP3A4 和P 糖蛋白在小肠不是共同调节的, 但两者在药物肠道处置中的协同作用已得到体外试验和动物体内试验的证实。进一步了解两者的相互作用有助于改善CYP3A4 /P 糖蛋白底物的生物利用度。

关键词: CYP3A4, P 糖蛋白, 药物代谢, 肠道, 肝脏首过代谢, 生物利用度, 相互作用

Abstract: Intestinal CYP3A4-mediated biotransformation and active efflux of absorbed drug by P-glycoprotein are major determinants of bioavailability of orally administered drugs. The expression of CYP3A4 and P-glycoprotein in the intestine is not co-ordinately regulated. However, synergistic actions of CYP3A4 and P-glycoprotein in intestinal drug disposition have been confirmed by in vitro and animal studies. Further understanding of this interaction would be potentially useful to improve oral bioavailability of CYP3A4 /-glycoprotein substrates.

Key words: CYP3A4, P-glycoprotein, drug metabolism, intestine, liver, first-pass metabolism, bioavailability, drug interaction

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