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暴露前预防中的抗逆转录病毒药物:HIV 预防的新兴和先进趋势。

Antiretroviral agents in pre-exposure prophylaxis: emerging and advanced trends in HIV prevention.

机构信息

School of Health Sciences, International Medical University, Bukit Jalil, Kuala Lumpur, Malaysia.

Department of Life Sciences, School of Pharmacy, International Medical University, Bukit Jalil, Kuala Lumpur, Malaysia.

出版信息

J Pharm Pharmacol. 2019 Sep;71(9):1339-1352. doi: 10.1111/jphp.13107. Epub 2019 May 29.

Abstract

OBJECTIVES

Antiretroviral agents (ARVs) have been the most promising line of therapy in the management of human immunodeficiency virus (HIV) infections. Some of these ARVs are used in the pre-exposure prophylaxis (PrEP) to suppress the transmission of HIV. Prophylaxis is primarily used in uninfected people, before exposure, to effectively prevent HIV infection. Several studies have shown that ART PrEP prevents HIV acquisition from sexual, blood and mother-to-child transmissions. However, there are also several challenges and limitations to PrEP. This review focuses on the current antiretroviral therapies used in PrEP.

KEY FINDINGS

Among ARVs, the most common drugs employed from the class of entry inhibitors are maraviroc (MVC), which is a CCR5 receptor antagonist. Other entry inhibitors like emtricitabine (FTC) and tenofovir (TFV) are also used. Rilpivirine (RPV) and dapivirine (DPV) are the most common drugs employed from the Non-nucleoside reverse transcriptase inhibitor (NNRTIs) class, whereas, tenofovir disoproxil fumarate (TDF) is primarily used in the Nucleoside Reverse Transcriptase Inhibitor (NRTIs) class. Cabotegravir (CAB) is an analog of dolutegravir, and it is an integrase inhibitor. Some of these drugs are also used in combination with other drugs from the same class.

SUMMARY

Some of the most common pre-exposure prophylactic strategies employed currently are the use of inhibitors, namely entry inhibitors, non-nucleoside reverse transcriptase inhibitors, nucleoside reverse transcriptase inhibitors, integrase and protease inhibitors. In addition, we have also discussed on the adverse effects caused by ART in PrEP, pharmacoeconomics factors and the use of antiretroviral prophylaxis in serodiscordant couples.

摘要

目的

抗逆转录病毒药物(ARV)是治疗人类免疫缺陷病毒(HIV)感染最有希望的治疗方法。其中一些 ARV 用于暴露前预防(PrEP)以抑制 HIV 的传播。预防主要用于未感染的人,在暴露之前,以有效预防 HIV 感染。几项研究表明,ART PrEP 可预防性传播、血液和母婴传播获得 HIV。然而,PrEP 也存在一些挑战和局限性。本综述重点介绍了目前用于 PrEP 的抗逆转录病毒治疗方法。

主要发现

在 ARV 中,最常用的属于进入抑制剂类的药物是马拉维若(MVC),它是一种 CCR5 受体拮抗剂。其他进入抑制剂,如恩曲他滨(FTC)和替诺福韦(TFV)也有使用。利匹韦林(RPV)和地匹福韦(DPV)是最常用的非核苷类逆转录酶抑制剂(NNRTIs)类药物,而富马酸替诺福韦二吡呋酯(TDF)主要用于核苷类逆转录酶抑制剂(NRTIs)类。卡博特韦(CAB)是多拉韦林的类似物,它是一种整合酶抑制剂。这些药物中的一些也与来自同一类别的其他药物联合使用。

总结

目前使用的一些最常见的暴露前预防性策略是使用抑制剂,即进入抑制剂、非核苷类逆转录酶抑制剂、核苷类逆转录酶抑制剂、整合酶和蛋白酶抑制剂。此外,我们还讨论了 ART 在 PrEP 中引起的不良反应、药物经济学因素以及在血清不一致的夫妇中使用抗逆转录病毒预防。

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