Department of Pediatrics, Asan Medical Center Children's Hospital, University of Ulsan College of Medicine, Seoul, Korea.
Department of Clinical Pharmacology and Therapeutics, Asan Medical Center, University of Ulsan College of Medicine, Seoul, Korea.
J Clin Pharmacol. 2018 Dec;58(12):1586-1596. doi: 10.1002/jcph.1282. Epub 2018 Jul 27.
This study aimed to evaluate the safety and tolerability of intravenous (IV) levetiracetam (LEV) as a monotherapy in children aged 1 month-16 years and to explore the pharmacokinetics (PK) of IV LEV and the time to seizure after IV then oral administration of LEV in pediatric children with epilepsy. Children diagnosed with acute unprovoked seizures requiring in-hospital IV LEV administration were included. After administration, the clinical seizure outcomes, side effects, and the Korean-Child Behavior Checklist were monitored and the PK and repeated time to seizure were analyzed via modeling using NONMEM software. Overall, 37 children with epilepsy were enrolled and underwent a PK analysis (median age, 4.6 years; median weight, 18.0 kg). Nine children (24.3%) had seizure recurrence during the follow-up period (median, 3.8 months) and 5 children (13.5%) experienced LEV-associated adverse events such as irritability (n = 2; 5.4%) and somnolence (n = 3; 8.1%). The plasma LEV concentrations after IV LEV were best described by a one-compartment linear PK model. Only body weight was associated with both the clearance and volume of distribution of LEV. The Weibull distribution model described the time to seizure recurrence well; no statistically significant predictor for the time to seizure was identified. Therefore, IV LEV was a well-tolerated and effective alternative in children with acute unprovoked seizures, and models for the PK and time to repeated seizure recurrence after LEV were successfully developed. In particular, the current use of a weight-based IV LEV dosing regimen in pediatric children is practical.
本研究旨在评估静脉内(IV)左乙拉西坦(LEV)单药治疗 1 个月至 16 岁儿童的安全性和耐受性,并探索 IV LEV 的药代动力学(PK)以及在儿科癫痫患儿中 IV 然后口服 LEV 后的癫痫发作时间。包括被诊断为需要住院 IV LEV 治疗的急性自发性癫痫发作的儿童。给药后,监测临床癫痫发作结果、副作用和韩国儿童行为检查表,并使用 NONMEM 软件通过建模分析 PK 和重复癫痫发作时间。总体而言,37 名癫痫患儿接受了 PK 分析(中位年龄 4.6 岁;中位体重 18.0 公斤)。9 名儿童(24.3%)在随访期间(中位时间为 3.8 个月)癫痫发作复发,5 名儿童(13.5%)出现与 LEV 相关的不良事件,如易怒(n=2;5.4%)和嗜睡(n=3;8.1%)。IV LEV 后 LEV 的血浆浓度最好用单室线性 PK 模型描述。只有体重与 LEV 的清除率和分布容积有关。威布尔分布模型很好地描述了癫痫发作复发的时间;未确定癫痫发作时间的统计学显著预测因子。因此,IV LEV 是急性自发性癫痫发作儿童的一种耐受良好且有效的替代药物,并且成功开发了 LEV 后 PK 和重复癫痫发作时间的模型。特别是,目前在儿科儿童中使用基于体重的 IV LEV 给药方案是实用的。