de Jong Bas T, Eleveld Douglas J, Mason Keira P, Struys Michel M R F
Department of Anesthesiology, University of Groningen, University Medical Center Groningen, P.O. Box 30001, 9700 RB, Groningen, The Netherlands.
Department of Anesthesiology, Boston Children's Hospital, Harvard Medical School, Boston, MA, USA.
Clin Pharmacokinet. 2025 Jul 21. doi: 10.1007/s40262-025-01548-7.
Remimazolam is a benzodiazepine with a high affinity for the γ-aminobutyric acid type A-receptor thereby inducing sedation and amnesia. It is a short-acting drug, has a fast onset, short duration of action, and a predictable recovery profile. Remimazolam is metabolized mainly into CNS7054. In recent years, numerous population pharmacokinetic and combined pharmacokinetic/pharmacodynamic studies have been published. This narrative review aims to give an overview of and insight into pharmacokinetic/pharmacodynamic models and related clinical effects. Body weight, age and American Society of Anesthesiologists classification, sex, hepatic function, and extracorporeal circulation have been shown to significantly impact remimazolam pharmacokinetics. Body mass index, race, concomitant opioid administration, and a CNS7054-induced tolerance effect may be covariates. The labeling of remimazolam is not consistent worldwide as it has been approved for general anesthesia and/or sedation in different countries. To date, remimazolam is only approved by the intravenous route. Remimazolam has been approved for general anesthesia and/or sedation. The incidence of postoperative nausea and vomiting seems higher compared with propofol, yet pain on injection is less common. One study has published population pharmacokinetics in children. Reports on alternative methods to intravenous administration have been sparse.
瑞米唑仑是一种对γ-氨基丁酸A型受体具有高亲和力的苯二氮䓬类药物，从而可诱导镇静和失忆。它是一种短效药物，起效快，作用持续时间短，恢复情况可预测。瑞米唑仑主要代谢为CNS7054。近年来，已发表了大量群体药代动力学以及联合药代动力学/药效学研究。本叙述性综述旨在概述并深入了解药代动力学/药效学模型及相关临床效应。已证明体重、年龄和美国麻醉医师协会分级、性别、肝功能及体外循环对瑞米唑仑的药代动力学有显著影响。体重指数、种族、同时使用阿片类药物以及CNS7054诱导的耐受效应可能是协变量。瑞米唑仑在全球的标签并不一致，因为它在不同国家已被批准用于全身麻醉和/或镇静。迄今为止，瑞米唑仑仅被批准通过静脉途径给药。瑞米唑仑已被批准用于全身麻醉和/或镇静。与丙泊酚相比，术后恶心和呕吐的发生率似乎更高，但注射痛较少见。一项研究发表了儿童群体药代动力学。关于静脉给药替代方法的报道很少。
