Department of Clinical Pharmacy, Faculty of Pharmaceutical Sciences, Prince of Songkla University, Hat Yai, Songkhla, Thailand.
Division of Internal Medicine of Internal Medicine, Faculty of Medicine, Prince of Songkla University, Hat Yai, Songkhla, Thailand.
J Clin Pharmacol. 2024 Nov;64(11):1343-1350. doi: 10.1002/jcph.6102. Epub 2024 Jul 29.
Our goal is to create a population pharmacokinetic (PK) model and identify the best loading dose (LD) of intravenous valproic acid for hospitalized Thai patients. Data from patients who received intravenous valproic acid and underwent measurement of serum valproic acid concentrations during hospitalization were collected retrospectively. A nonlinear mixed-effects modeling approach was conducted to estimate the PK parameters of valproic acid. Covariates affecting the PK parameters of valproic acid were examined and ranked based on their impact on the model's performance. Monte Carlo simulations of 1000 patients were conducted to estimate the optimal LD of valproic acid. A total of 120 hospitalized patients (51.7% male) with 167 valproic acid concentrations were included in the study. A linear one-compartment model with constant residual error was the best base model. An age-covariate model was the best predictor of valproic acid clearance (CL). The typical values of CL and volume of distribution for valproic acid were 0.77 L/h and 14.56 L, respectively. The LD of 1000-1200 mg intravenous was identified as the pragmatic option as an empirical regimen for hospitalized Thai patients. The recommended time to initiate maintenance dose (MD) is 4-8 h following the LD. The population PK model and optimal LD of valproic acid in hospitalized Thai patients has been established, and it may be advisable to initiate the MD at a later time for the elderly.
我们的目标是建立一个群体药代动力学(PK)模型,并确定静脉用丙戊酸在泰国住院患者中的最佳负荷剂量(LD)。回顾性收集了接受静脉用丙戊酸治疗并在住院期间测量血清丙戊酸浓度的患者数据。采用非线性混合效应建模方法估算丙戊酸的 PK 参数。考察了影响丙戊酸 PK 参数的协变量,并根据其对模型性能的影响进行了排序。对 1000 名患者进行了 Monte Carlo 模拟,以估算丙戊酸的最佳 LD。共有 120 名住院患者(51.7%为男性),167 次丙戊酸浓度纳入研究。线性一室模型和恒定残差是最佳基础模型。年龄协变量模型是预测丙戊酸清除率(CL)的最佳模型。丙戊酸 CL 和分布容积的典型值分别为 0.77 L/h 和 14.56 L。1000-1200mg 静脉 LD 被确定为泰国住院患者的实用选择,作为经验性治疗方案。建议在 LD 后 4-8 小时开始维持剂量(MD)。已建立了泰国住院患者丙戊酸的群体 PK 模型和最佳 LD,对于老年人,可能需要延迟开始 MD。