泛昔洛韦的药理学特征。

Seminars in dermatology Pub Date : 1996-06-01
C Crumpacker
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引用次数: 0

摘要

Famciclovir是喷昔洛韦的一种吸收良好的口服形式,喷昔洛韦是一种强效和选择性抗病毒药物,对疱疹病毒家族成员具有活性,包括水痘-带状疱疹病毒(VZV)、单纯疱疹病毒-1 (HSV-1)和单纯疱疹病毒-2。泛昔洛韦被迅速吸收并转化为喷昔洛韦。口服500mg泛环洛韦后,喷昔洛韦具有优良的生物利用度(77%)。与无环洛韦类似,泛环洛韦通过磷酸化转化为其活性代谢物——三磷酸喷昔洛韦。三磷酸喷昔洛韦在hsv -1和hsv -2感染的细胞中具有较长的体外细胞内半衰期,分别为10至20小时,在vzv感染的细胞中为9至14小时。相比之下,阿昔洛韦的体外细胞内半衰期明显缩短,在HSV-1和hsv -2感染细胞中分别为0.7和1小时,在vzv感染细胞中为0.8小时。泛昔洛韦主要通过肾脏排出。对于肾功能正常或轻度受损的老年患者,不需要调整famciclovir的剂量,并且penciclovir的可用程度不受食物的影响。良好的生物利用度确保了足够的药物到达病毒感染的细胞,并且泛环洛韦活性形式的细胞内半衰期延长导致持续的抗病毒活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The pharmacological profile of famciclovir.

Famciclovir is the well-absorbed oral form of penciclovir, a potent and selective antiviral agent, with activity against members of the herpesvirus family, including varicella-zoster virus (VZV), and herpes simplex virus-1 (HSV-1) and HSV-2. Famciclovir is rapidly absorbed and converted to penciclovir. Penciclovir has excellent bioavailability (77%) after oral administration of 500 mg of famciclovir. Similar to acyclovir, famciclovir is converted by phosphorylation to its active metabolite, penciclovir-triphosphate. Penciclovir-triphosphate has a prolonged in vitro intracellular half-life of 10 to 20 hours in HSV-1-and HSV-2-infected cells, respectively, and 9 to 14 hours in VZV-infected cells. In contrast, the in vitro intracellular half-life of acyclovir is substantially shorter at 0.7 and 1 hours in HSV-1- and HSV-2-infected cells, respectively, and 0.8 hours in VZV-infected cells. Famciclovir is eliminated primarily via the kidneys. Dosage adjustment is not required for famciclovir in elderly patients with normal or mildly impaired renal function, and the extent of penciclovir availability is not affected by food. The excellent bioavailability ensures that adequate drug reaches virus-infected cells, and the prolonged intracellular half-life of the active form of famciclovir results in persistent antiviral activity.

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