University Hospitals of Cleveland, Cleveland, Ohio, USA.
Antimicrob Agents Chemother. 2010 May;54(5):2032-41. doi: 10.1128/AAC.01508-09. Epub 2010 Feb 16.
A multicenter, open-label study evaluated the single-dose pharmacokinetics and safety of a pediatric oral famciclovir (prodrug of penciclovir) formulation in infants aged 1 to 12 months with suspicion or evidence of herpes simplex virus infection. Individualized single doses of famciclovir based on the infant's body weight ranged from 25 to 175 mg. Eighteen infants were enrolled (1 to <3 months old [n = 8], 3 to <6 months old [n = 5], and 6 to 12 months old [n = 5]). Seventeen infants were included in the pharmacokinetic analysis; one infant experienced immediate emesis and was excluded. Mean C(max) and AUC(0-6) values of penciclovir in infants <6 months of age were approximately 3- to 4-fold lower than those in the 6- to 12-month age group. Specifically, mean AUC(0-6) was 2.2 microg h/ml in infants aged 1 to <3 months, 3.2 microg h/ml in infants aged 3 to <6 months, and 8.8 microg h/ml in infants aged 6 to 12 months. These data suggested that the dose administered to infants <6 months was less than optimal. Eight (44.4%) infants experienced at least one adverse event with gastrointestinal events reported most commonly. An updated pharmacokinetic analysis was conducted, which incorporated the data in infants from the present study and previously published data on children 1 to 12 years of age. An eight-step dosing regimen was derived that targeted exposure in infants and children 6 months to 12 years of age to match the penciclovir AUC seen in adults after a 500-mg dose of famciclovir.
一项多中心、开放性研究评估了单剂量儿童口服泛昔洛韦(喷昔洛韦前体药物)制剂在 1 至 12 个月龄、疑似或有单纯疱疹病毒感染证据的婴儿中的药代动力学和安全性。根据婴儿体重,个体化的单剂量泛昔洛韦范围为 25 至 175 毫克。共纳入 18 名婴儿(1 至<3 个月龄[8 名]、3 至<6 个月龄[5 名]和 6 至 12 个月龄[5 名])。17 名婴儿纳入药代动力学分析;1 名婴儿出现即刻呕吐,被排除。6 个月龄以下婴儿的喷昔洛韦 C(max)和 AUC(0-6)值约为 6 至 12 个月龄组的 3-4 倍。具体而言,1 至<3 个月龄婴儿的 AUC(0-6)均值为 2.2 微克 h/ml,3 至<6 个月龄婴儿为 3.2 微克 h/ml,6 至 12 个月龄婴儿为 8.8 微克 h/ml。这些数据表明,6 个月龄以下婴儿的给药剂量不足。8 名(44.4%)婴儿发生至少 1 次不良事件,最常见的是胃肠道事件。进行了更新的药代动力学分析,纳入了本研究和之前发表的 1 至 12 岁儿童研究中的婴儿数据。得出了一个 8 步剂量方案,旨在使 6 个月至 12 岁婴儿和儿童的暴露量与 500 毫克泛昔洛韦后成人的喷昔洛韦 AUC 相匹配。