CYP3A4介导的HIV-1蛋白酶抑制剂的增效作用  

CYP3A4-mediated synergistic effects on HIV-1 protease inhibitors

作　　者：姚瑶[1] 胡卓汉[1,2,3] 

机构地区：[1]上海医药工业研究院,上海201203 [2]瑞德肝脏疾病研究(上海)有限公司,上海201203 [3]上海中医药大学,上海201203

出　　处：《中国新药杂志》2010年第13期1124-1127,共4页Chinese Journal of New Drugs

摘　　要：HIV蛋白酶抑制剂(PIs)作为治疗艾滋病的有效药物,是肝药酶CYP3A4的底物。它们有生物利用度低、半衰期短、药物在个体之间药动学差异较大等缺点。利托那韦(ritonavir)可以抑制CYP3A4对PIs的代谢作用,因而被用于多种PIs的增效治疗。文中综述了ritonavir的药动学增效作用,重点阐述了ritonavir与各种PIs联合使用在临床上的发展现状、疗效特征以及适应症,并介绍了ritonavir作为增效剂的不足以及未来新的增效剂的发展前景。近几年来关于天然药物对PIs的增效作用也有报道,文中简要介绍了几种具有增效潜力的天然药物。HIV protease inhibitors（PIs）,as effective medications for AIDS treatment,are substrates of CYP3A4.They have low bioavailability,short half-life and large interindividual variability.As we discovered,ritonavir is the most potent inhibitor of CYP3A4,and has been widely used to boost other PIs.In this article,we reviewed the clinical use of ritonavir for pharmacokinetic synergy,and mainly focused on the development,effect and indication of clinical use of various PIs.We also showed the perspectives of new synergists in the future.In recent years,there have been reports on pharmacokinetic synergy of medical herbs,which were introduced briefly in this review.

关 键 词：人类免疫缺陷病毒蛋白酶抑制剂 耐药性 增效作用 

分 类 号：R96[医药卫生—药理学] R978.7[医药卫生—药学]