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利托那韦增效的蛋白酶抑制剂在 HIV 治疗中的应用。

Ritonavir-boosted protease inhibitors in HIV therapy.

机构信息

Division of AIDS, Department of Medicine, University of British Columbia, Vancouver, Canada.

出版信息

Ann Med. 2011 Aug;43(5):375-88. doi: 10.3109/07853890.2011.572905. Epub 2011 Apr 18.

Abstract

The advent of combination antiretroviral therapy has led to significant improvement in the care of HIV-infected patients. Originally designed as a protease inhibitor (PI), ritonavir is currently exclusively used as a pharmacokinetic enhancer of other protease inhibitors, predominantly due to ritonavir's potent inhibition of the cytochrome P450 3A4 isoenzyme. Ritonavir-boosting of PIs decrease pill burden and frequency of dosing. Boosted PIs are recommended for first-line therapy in treatment and play a key role in the management of treatment-experienced patients. Potential problems associated with PIs include metabolic abnormalities (e.g. dyslipidemia), increased cardiovascular risk, and drug interactions.

摘要

联合抗逆转录病毒疗法的出现显著改善了 HIV 感染患者的治疗效果。利托那韦最初被设计为一种蛋白酶抑制剂(PI),但目前仅作为其他蛋白酶抑制剂的药代动力学增强剂使用,主要是因为利托那韦对细胞色素 P450 3A4 同工酶有很强的抑制作用。利托那韦增强 PI 可减少药物负担和给药频率。增强后的 PI 推荐用于一线治疗,在治疗中发挥着重要作用,在治疗经验丰富的患者的管理中也起着关键作用。与 PI 相关的潜在问题包括代谢异常(如血脂异常)、心血管风险增加和药物相互作用。

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