氨基（羟乙氧基甲基）嘌呤：一种新的阿昔洛韦吸收良好的前药。

Amino (hydroxyethoxymethyl) purine: a new well-absorbed prodrug of acyclovir.

作者信息

Selby P, Powles R L, Blake S, Stolle K, Mbidde E K, McElwain T J, Hickmott E, Whiteman P D

出版信息

Lancet. 1984 Dec 22;2(8417-8418):1428-30. doi: 10.1016/s0140-6736(84)91624-6.

Abstract

Acyclovir is an effective treatment for herpes simplex and herpes zoster infections, but it is somewhat limited by low oral absorption. 2-amino-9-[(2hydroxyethoxy)methyl]-9H-purine (BW A515U), a new prodrug of acyclovir, when evaluated in 10 patients with haematological malignancies, was well tolerated, excellently absorbed, and produced high plasma concentrations of acyclovir which were comparable to those with intravenous acyclovir. The plasma concentrations after oral BW A515U were much higher than those after oral acyclovir.

摘要

阿昔洛韦是治疗单纯疱疹和带状疱疹感染的有效药物，但口服吸收较差，在一定程度上限制了其应用。阿昔洛韦的一种新前体药物2-氨基-9-[(2-羟基乙氧基)甲基]-9H-嘌呤（BW A515U），在10例血液系统恶性肿瘤患者中进行评估时，耐受性良好，吸收极佳，可产生与静脉注射阿昔洛韦相当的高血浆阿昔洛韦浓度。口服BW A515U后的血浆浓度远高于口服阿昔洛韦后的血浆浓度。