Sáez-Llorens X, Yogev R, Arguedas A, Rodriguez A, Spigarelli M G, De León Castrejón T, Bomgaars L, Roberts M, Abrams B, Zhou W, Looby M, Kaiser G, Hamed K
Hospital del Niño, Panama City, Panama.
Antimicrob Agents Chemother. 2009 May;53(5):1912-20. doi: 10.1128/AAC.01054-08. Epub 2009 Mar 9.
Two multicenter, open-label, single-arm, two-phase studies evaluated single-dose pharmacokinetics and single- and multiple-dose safety of a pediatric oral famciclovir formulation (prodrug of penciclovir) in children aged 1 to 12 years with suspicion or evidence of herpes simplex virus (HSV) or varicella-zoster virus (VZV) infection. Pooled pharmacokinetic data were generated after single doses in 51 participants (approximately 12.5 mg/kg of body weight [BW] for children weighing < 40 kg and 500 mg for children weighing > or = 40 kg). The average systemic exposure to penciclovir was similar (6- to 12-year-olds) or slightly lower (1- to < 6-year-olds) than that in adults receiving a 500-mg dose of famciclovir (historical data). The apparent clearance of penciclovir increased with BW in a nonlinear manner, proportional to BW(0.696). An eight-step weight-based dosing regimen was developed to optimize exposure in smaller children and was used in the 7-day multiple-dose safety phases of both studies, which enrolled 100 patients with confirmed/suspected viral infections. Twenty-six of 47 (55.3%) HSV-infected patients who received famciclovir twice a day and 24 of 53 (45.3%) VZV-infected patients who received famciclovir three times a day experienced at least one adverse event. Most adverse events were gastrointestinal in nature. Exploratory analysis following 7-day famciclovir dosing regimen showed resolution of symptoms in most children with active HSV (19/21 [90.5%]) or VZV disease (49/53 [92.5%]). Famciclovir formulation (sprinkle capsules in OraSweet) was acceptable to participants/caregivers. In summary, we present a weight-adjusted dosing schedule for children that achieves systemic exposures similar to those for adults given the 500-mg dose.
两项多中心、开放标签、单臂、两阶段研究评估了一种儿科口服泛昔洛韦制剂(喷昔洛韦的前体药物)在1至12岁疑似或确诊感染单纯疱疹病毒(HSV)或水痘带状疱疹病毒(VZV)的儿童中的单剂量药代动力学以及单剂量和多剂量安全性。在51名参与者中进行单剂量给药后生成了汇总药代动力学数据(体重<40 kg的儿童约为12.5 mg/kg体重[BW],体重≥40 kg的儿童为500 mg)。喷昔洛韦的平均全身暴露量与接受500 mg泛昔洛韦剂量的成年人相似(6至12岁儿童)或略低(1至<6岁儿童)(历史数据)。喷昔洛韦的表观清除率随体重以非线性方式增加,与BW(0.696)成比例。制定了一个基于体重的八步给药方案,以优化较小儿童的药物暴露,并在两项研究的7天多剂量安全性阶段中使用,这两项研究共纳入了100名确诊/疑似病毒感染的患者。每天接受两次泛昔洛韦治疗的47名HSV感染患者中有26名(55.3%),每天接受三次泛昔洛韦治疗的53名VZV感染患者中有24名(45.3%)经历了至少一次不良事件。大多数不良事件为胃肠道性质。对7天泛昔洛韦给药方案后的探索性分析表明,大多数活动性HSV(19/21 [90.5%])或VZV疾病患儿(49/53 [92.5%])的症状得到缓解。泛昔洛韦制剂(OraSweet中的散剂胶囊)为参与者/护理人员所接受。总之,我们提出了一种针对儿童的体重调整给药方案,该方案实现的全身暴露量与给予500 mg剂量的成年人相似。