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泛昔洛韦的药理学特征。

The pharmacological profile of famciclovir.

作者信息

Crumpacker C

机构信息

Division of Infectious Diseases, Beth Israel Hospital, Boston, MA 02215, USA.

出版信息

Semin Dermatol. 1996 Jun;15(2 Suppl 1):14-26.

PMID:8840412
Abstract

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.

摘要

泛昔洛韦是喷昔洛韦的口服剂型,吸收良好。喷昔洛韦是一种强效且具有选择性的抗病毒药物,对疱疹病毒科成员具有活性,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(HSV-2)。泛昔洛韦吸收迅速并转化为喷昔洛韦。口服500mg泛昔洛韦后,喷昔洛韦具有出色的生物利用度(77%)。与阿昔洛韦类似,泛昔洛韦通过磷酸化转化为其活性代谢产物喷昔洛韦三磷酸盐。在HSV-1和HSV-2感染的细胞中,喷昔洛韦三磷酸盐的体外细胞内半衰期分别延长至10至20小时,在VZV感染的细胞中为9至14小时。相比之下,阿昔洛韦在HSV-1和HSV-2感染细胞中的体外细胞内半衰期分别短得多,为0.7小时和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泄。肾功能正常或轻度受损的老年患者使用泛昔洛韦时无需调整剂量,食物不影响喷昔洛韦的可利用程度。出色的生物利用度确保有足够的药物到达病毒感染细胞,泛昔洛韦活性形式延长的细胞内半衰期导致持续的抗病毒活性。

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