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阿昔洛韦概述概述

Author
Kimon C Zachary, MD
Section Editor
Martin S Hirsch, MD
Deputy Editor
Jennifer Mitty, MD, MPH

引言

阿昔洛韦广泛用于治疗疱疹病毒感染，特别是单纯疱疹病毒(herpes simplex virus, HSV)和水痘-带状疱疹病毒(varicella-zoster virus, VZV)。本文将对阿昔洛韦的作用机制、耐药机制及其主要临床应用进行概述。

阿昔洛韦用于特定临床综合征的给药和治疗，将在相关专题中作更详细的介绍。

伐昔洛韦和泛昔洛韦是较新一代的药物，作用机制与阿昔洛韦类似；这两种药物的应用将在别处讨论。 (参见“Valacyclovir: An overview”和“泛昔洛韦的概述”)

作用机制

阿昔洛韦[9-(2-羟甲基)鸟嘌呤]是一种核苷类似物，能选择性抑制1型和2型HSV(HSV-1、HSV-2)及VZV的复制。阿昔洛韦被摄取到细胞内后，通过病毒编码的胸苷激酶转化为单磷酸阿昔洛韦。在未感染细胞中，不会明显发生上述步骤，因此该药物的活性具有特异性。随后这种单磷酸衍生物被细胞酶转换为三磷酸阿昔洛韦。

三磷酸阿昔洛韦作为三磷酸脱氧鸟苷(deoxyguanosine triphosphate, dGTP)的类似物，竞争性地抑制病毒DNA聚合酶。三磷酸阿昔洛韦掺入DNA中，由于缺乏3'羟基基团，阻止更多的核苷附着，导致DNA链复制终止。与细胞DNA聚合酶相比，三磷酸阿昔洛韦对病毒DNA聚合酶的亲和力要高得多，因此治疗比率较高[1,2]。

               

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Literature review current through: 2017-06 . | This topic last updated: 2016-07-25.
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