Department of Respiratory Sciences, College of Life Sciences, University of Leicester, Leicester, UK.
Jenny Lind Children's Hospital, Norfolk and Norwich University Hospital NHS Trust, Norwich, UK.
Pharmacol Res Perspect. 2022 Oct;10(5):e01004. doi: 10.1002/prp2.1004.
Altered physiology caused by critical illness may change midazolam pharmacokinetics and thereby result in adverse reactions and outcomes in this vulnerable patient population. This study set out to determine which critical illness-related factors impact midazolam pharmacokinetics in children using population modeling. This was an observational, prospective, controlled study of children receiving IV midazolam as part of routine care. Children recruited into the study were either critically-ill receiving continuous infusions of midazolam or otherwise well, admitted for elective day-case surgery (control) who received a single IV bolus dose of midazolam. The primary outcome was to determine the population pharmacokinetics and identify covariates that influence midazolam disposition during critical illness. Thirty-five patients were recruited into the critically ill arm of the study, and 54 children into the control arm. Blood samples for assessing midazolam and 1-OH-midazolam concentrations were collected opportunistically (critically ill arm) and in pre-set time windows (control arm). Pharmacokinetic modeling demonstrated a significant change in midazolam clearance with acute inflammation (measured using C-Reactive Protein), cardio-vascular status, and weight. Simulations predict that elevated C-Reactive Protein and compromised cardiovascular function in critically ill children result in midazolam concentrations up to 10-fold higher than in healthy children. The extremely high concentrations of midazolam observed in some critically-ill children indicate that the current therapeutic dosing regimen for midazolam can lead to over-dosing. Clinicians should be aware of this risk and intensify monitoring for oversedation in such patients.
危重病引起的生理改变可能会改变咪达唑仑的药代动力学,从而导致这一脆弱患者群体出现不良反应和结局。本研究旨在使用群体建模确定哪些与危重病相关的因素会影响儿童咪达唑仑的药代动力学。这是一项观察性、前瞻性、对照研究,纳入了接受 IV 咪达唑仑作为常规治疗一部分的儿童。入组研究的儿童要么是危重病患者,正在接受咪达唑仑持续输注,要么是情况良好,因择期日间手术入院(对照),接受单次 IV 咪达唑仑推注。主要结局是确定咪达唑仑的群体药代动力学,并确定影响危重病期间咪达唑仑处置的协变量。35 名儿童被纳入危重病组,54 名儿童被纳入对照组。采集血样以评估咪达唑仑和 1-OH-咪达唑仑浓度,机会性采集(危重病组)和在预设时间窗口采集(对照组)。药代动力学模型显示,咪达唑仑清除率与急性炎症(使用 C 反应蛋白测量)、心血管状态和体重有显著变化。模拟预测,危重病儿童的 C 反应蛋白升高和心血管功能受损会导致咪达唑仑浓度比健康儿童高 10 倍。一些危重病儿童中观察到的咪达唑仑极高浓度表明,目前咪达唑仑的治疗剂量方案可能导致用药过量。临床医生应该意识到这种风险,并在这些患者中加强对过度镇静的监测。