Centre Hospitalier Universitaire de Rennes, Hôpital de Pontchaillou, France.
Expert Opin Drug Metab Toxicol. 2009 Nov;5(11):1455-68. doi: 10.1517/17425250903321514.
Atazanavir (ATV) is a potent and safe protease inhibitor (PI) initially approved in adult HIV-1 infected patients in combination with other antiretroviral drugs with once daily administration. In combination with nucleoside reverse transcriptase inhibitors (NRTIs) and boosted with ritonavir, it has been established as the preferred initial regimen in published guidelines.
This article reviews relevant pharmacodynamic, pharmacokinetic, efficacy and safety data of ATV, administered boosted with ritonavir or unboosted, in comparison with other PIs and/or non-NRTIs, with special focus on recent studies.
Review articles, recent primary literature and scientific meeting reports were analyzed.
Compared to most PIs with similar efficacy, the advantages of ATV are a once daily administration with only 100 mg ritonavir when boosted, a good gastrointestinal tolerance with limited diarrhea, a neutral effect on cholesterol and triglycerides, and a favorable resistance profile. However, highly frequent hyperbilirubinemia is observed resulting in some cases in clinical jaundice. Unboosted ATV must be cautiously used because increased resistances have been described.
The combination of a similar efficacy, a better tolerance and a low pill burden, as compared to other PIs, makes boosted ATV one of the best options, in combination with NRTIs, in PI-naive HIV-1 infected patients.
阿扎那韦（ATV）是一种强效且安全的蛋白酶抑制剂（PI），最初在成年 HIV-1 感染患者中与其他抗逆转录病毒药物联合使用，每日一次给药。与核苷类逆转录酶抑制剂（NRTIs）联合，并与利托那韦增效，已被确立为已发表指南中首选的初始方案。
本文综述了阿扎那韦与利托那韦增效或未增效时，与其他 PI 和/或非 NRTIs 相比的相关药效学、药代动力学、疗效和安全性数据，特别关注最近的研究。
分析了综述文章、最新的原始文献和科学会议报告。
与大多数具有相似疗效的 PI 相比，阿扎那韦的优势在于增效时每日只需服用 100mg 利托那韦，且胃肠道耐受性良好，腹泻有限，对胆固醇和甘油三酯影响中性，耐药谱良好。然而，频繁出现高胆红素血症，导致一些患者出现临床黄疸。未增效的阿扎那韦必须谨慎使用，因为已经描述了耐药性增加的情况。
与其他 PI 相比，阿扎那韦具有相似的疗效、更好的耐受性和更低的药物负担，与 NRTIs 联合使用，是初治 HIV-1 感染患者的最佳选择之一。
