用（S）-1-（3-羟基-2-膦酰甲氧基丙基）胞嘧啶对病毒性视网膜炎进行长效治疗。

Long-acting therapy of viral retinitis with (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine.

作者信息

Flores-Aguilar M, Huang J S, Wiley C A, De Clercq E, Vuong C, Bergeron-Lynn G, Chandler B, Munguia D, Freeman W R

机构信息

Department of Ophthalmology, University of California, School of Medicine, San Diego, La Jolla.

出版信息

J Infect Dis. 1994 Mar;169(3):642-7. doi: 10.1093/infdis/169.3.642.

DOI:10.1093/infdis/169.3.642

PMID:8158041

Abstract

(S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine (HPMPC), a high-potency antiherpes and anticytomegalovirus (CMV) drug was evaluated in the treatment of experimental retinitis caused by preretinal herpes simplex virus (HSV-1) injection in rabbits. HPMPC (100 micrograms/0.1 mL) was intravitreally injected 10, 15, 21, 30, or 46 days before, concurrently, or 3, 5, or 7 days after viral inoculation. Ganciclovir (200 micrograms/0.1 mL) was intravitreally injected 3, 7, or 10 days before HSV-1 inoculation, concurrent with viral inoculation, or 3, 5, or 7 days after viral inoculation. Eyes pretreated with HPMPC were protected from retinitis for 15-21 days. Ganciclovir did not protect completely even if administered 3 days before inoculation. Early treatment of established retinitis with HPMPC markedly delayed the progression of the infection. However, with ganciclovir there was delayed progression only in rabbits treated 3 days after viral inoculation. HPMPC had a remarkably potent and prolonged (< or = 1 month) antiviral effect in this retinitis model and may prove more useful than ganciclovir in local treatment of CMV retinitis.

摘要

（S）-1-（3-羟基-2-膦酰甲氧基丙基）胞嘧啶（HPMPC）是一种高效抗疱疹和抗巨细胞病毒（CMV）药物，在兔视网膜前注射单纯疱疹病毒1型（HSV-1）所致的实验性视网膜炎治疗中进行了评估。HPMPC（100微克/0.1毫升）在病毒接种前10、15、21、30或46天、同时或接种后3、5或7天玻璃体内注射。更昔洛韦（200微克/0.1毫升）在HSV-1接种前3、7或10天、与病毒接种同时或接种后3、5或7天玻璃体内注射。用HPMPC预处理的眼睛可预防视网膜炎15 - 21天。即使在接种前3天给药，更昔洛韦也不能完全起到保护作用。用HPMPC对已确立的视网膜炎进行早期治疗可显著延缓感染进展。然而，使用更昔洛韦时，仅在病毒接种后3天治疗的兔中感染进展出现延缓。在该视网膜炎模型中，HPMPC具有显著强效且持久（≤1个月）的抗病毒作用，在CMV视网膜炎的局部治疗中可能比更昔洛韦更有用。