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口服阿昔洛韦疗法的评估。

Evaluation of oral acyclovir therapy.

作者信息

Fletcher C, Bean B

出版信息

Drug Intell Clin Pharm. 1985 Jul-Aug;19(7-8):518-24. doi: 10.1177/106002808501900703.

Abstract

Acyclovir is a specific antiviral agent. The triphosphate form inhibits viral DNA replication by competing for incorporation into the replicating DNA chain or by inhibiting viral DNA polymerase. Cells not infected with herpesvirus are generally unaffected. Oral acyclovir inhibits most herpes simplex virus types 1 and 2, and varicella-zoster virus at concentrations used clinically. Oral acyclovir has an average plasma half-life of three hours and is eliminated primarily by renal mechanisms. Peak plasma concentrations occur 1.5 to 2.5 hours after administration and the oral bioavailability is 15 to 30 percent. Acyclovir distributes into most body tissues, including vesicular fluid and the central nervous system. Oral acyclovir is effective treatment of initial and recurrent genital herpes and can suppress frequently recurring genital herpes in both immunocompetent and immunocompromised patients. It is also effective for acute herpes zoster in the immunocompetent and possibly immunocompromised patient. No role is established in either Epstein-Barr virus or cytomegalovirus infections. Oral acyclovir appears to be effective and relatively safe, nontoxic therapy when administered in doses of 1-4 g/d. Oral acyclovir represents a major therapeutic advance in the treatment of herpesvirus infections.

摘要

阿昔洛韦是一种特异性抗病毒药物。其三磷酸盐形式通过竞争掺入复制的DNA链或抑制病毒DNA聚合酶来抑制病毒DNA复制。未感染疱疹病毒的细胞通常不受影响。口服阿昔洛韦在临床使用浓度下可抑制大多数1型和2型单纯疱疹病毒以及水痘-带状疱疹病毒。口服阿昔洛韦的血浆平均半衰期为3小时,主要通过肾脏机制消除。给药后1.5至2.5小时出现血浆峰值浓度,口服生物利用度为15%至30%。阿昔洛韦分布于大多数身体组织,包括水疱液和中枢神经系统。口服阿昔洛韦是初发性和复发性生殖器疱疹的有效治疗方法,并且可以抑制免疫功能正常和免疫功能低下患者频繁复发的生殖器疱疹。它对免疫功能正常以及可能免疫功能低下患者的急性带状疱疹也有效。在EB病毒或巨细胞病毒感染中未证实其作用。当以1 - 4g/天的剂量给药时,口服阿昔洛韦似乎是一种有效且相对安全、无毒的治疗方法。口服阿昔洛韦代表了疱疹病毒感染治疗方面的一项重大治疗进展。

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