Li Letao, Sassen Sebastiaan D T, van der Jagt Mathieu, Endeman Henrik, Koch Birgit C P, Hunfeld Nicole G M
Department of Hospital Pharmacy, Erasmus MC-University Medical Center, Doctor Molewaterplein 40, 3015 GD Rotterdam, The Netherlands.
Department of Intensive Care, Erasmus MC-University Medical Center, Doctor Molewaterplein 40, 3015 GD Rotterdam, The Netherlands.
Pharmaceutics. 2022 Feb 28;14(3):549. doi: 10.3390/pharmaceutics14030549.
Haloperidol is considered the first-line treatment for delirium in critically ill patients. However, clinical evidence of efficacy is lacking and no pharmacokinetic studies have been performed in intensive care unit (ICU) patients. The aim of this study was to establish a pharmacokinetic model to describe the PK in this population to improve insight into dosing. One hundred and thirty-nine samples from 22 patients were collected in a single-center study in adults with ICU delirium who were treated with low-dose intravenous haloperidol (3-6 mg per day). We conducted a population pharmacokinetic analysis using Nonlinear Mixed Effects Modelling (NONMEM). A one-compartment model best described the data. The mean population estimates were 51.7 L/h (IIV 42.1%) for clearance and 1490 L for the volume of distribution. The calculated half-life was around 22 h (12.3-29.73 h) for an average patient. A negative correlation between C-Reactive Protein (CRP) and haloperidol clearance was observed, where clearance decreased significantly with increasing CRP up to a CRP concentration of 100 mg/L. This is the first step towards haloperidol precision dosing in ICU patients and our results indicate a possible role of inflammation.
氟哌啶醇被认为是重症患者谵妄的一线治疗药物。然而,目前缺乏其疗效的临床证据,且尚未在重症监护病房(ICU)患者中进行药代动力学研究。本研究的目的是建立一个药代动力学模型来描述该人群的药代动力学特征,以提高对给药剂量的认识。在一项针对患有ICU谵妄的成年患者的单中心研究中,收集了22例患者的139份样本,这些患者接受低剂量静脉注射氟哌啶醇(每天3 - 6毫克)治疗。我们使用非线性混合效应模型(NONMEM)进行了群体药代动力学分析。单室模型能最好地描述数据。群体平均估计清除率为51.7 L/h(个体间变异42.1%),分布容积为1490 L。平均患者的计算半衰期约为22小时(12.3 - 29.73小时)。观察到C反应蛋白(CRP)与氟哌啶醇清除率之间呈负相关,即随着CRP升高至100 mg/L,清除率显著降低。这是朝着ICU患者氟哌啶醇精准给药迈出的第一步,我们的结果表明炎症可能起到一定作用。