Research Progress on the Application of Remimazolam as a Novel Sedative-Anesthetic Agent

Ziqing Zhu; Aidong Li; Yukang Gong; Baichi Chen; Qian Li

doi:10.54097/0t5r5q22

Authors

Ziqing Zhu
Aidong Li
Yukang Gong
Baichi Chen
Qian Li

DOI:

https://doi.org/10.54097/0t5r5q22

Keywords:

Remimazolam, Novel Sedative-Anesthetic Agent, γ-aminobutyric Acid Type A

Abstract

Remimazolam is a novel, ultra-short-acting benzodiazepine characterized by its rapid onset of action. It has been approved for procedural sedation and general anesthesia, exhibiting typical pharmacodynamic profiles akin to other benzodiazepines, such as midazolam. The drug demonstrates high organ-independent clearance and acts primarily on the γ-aminobutyric acid type A (GABA-A) receptors. It is rapidly metabolized by nonspecific esterases, predominantly carboxylesterases, into inactive metabolites with significantly reduced binding affinity—approximately 300 to 400 times lower for GABA-A receptors compared to the parent compound. Following administration, plasma concentrations of remimazolam decline predictably and rapidly; at adequate doses, no prolonged sedative effects are observed. Currently, remimazolam has been successfully employed in endoscopic procedures as well as for the induction and maintenance of general anesthesia, offering rapid and predictable onset and recovery, minimal impact on respiratory and hemodynamic parameters, and an absence of severe drug-related adverse events. Moreover, its effects can be reversed by flumazenil. Although remimazolam holds considerable potential for sedation in patients requiring anesthesia, further research is needed to evaluate its efficacy and safety in broader sedative applications. This review aims to outline the pharmacokinetic profile of remimazolam, its current clinical utility, and future directions in clinical practice.

Downloads

Download data is not yet available.

References

[1] MASHOUR G A, KELZ M B. Systems Neuroscience: The Exciting Journey to Oblivion [J]. Current Biology, 2018, 28(5): R223-R4.

[2] LAMP K, HUMENY A, NIKOLIC Z, et al. The murine GABA(B) receptor 1: cDNA cloning, tissue distribution, structure of the Gabbr1 gene, and mapping to chromosome 17 [J]. Cytogenetic & Genome Research, 2001, 92(1-2): 116-21.

[3] ZHANG Y Y. Etomidate-propofol combination in painless gastrointestinal endoscopy for elderly patients:A comparative study [J]. World Journal of Gastrointestinal Surgery, 2025, 17(7): 275-83.

[4] BOUCHEZ S. Faculty Opinions recommendation of Multimodal general anesthesia: theory and practice [J]. Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature, 2019.

[5] GOUDRA B, MASON K P. Emerging Approaches in Intravenous Moderate and Deep Sedation [J]. Journal of Clinical Medicine, 2021, 10(8): 1735.

[6] DAO V A, SCHIPPERS F, STHR T. Efficacy of remimazolam versus midazolam for procedural sedation: post hoc integrated analyses of three phase 3 clinical trials [J]. Endoscopy International Open.

[7] KIM S H, CHO J Y, KIM M, et al. Safety and efficacy of remimazolam compared with midazolam during bronchoscopy: a single-center, randomized controlled study [J]. Scientific Reports, 2023, 13(1).

[8] WESOLOWSKI, ALEXANDRA, M, et al. Remimazolam: Pharmacologic Considerations and Clinical Role in Anesthesiology [J]. Pharmacotherapy, 2016.

[9] DESSAI S, NINAVE S, BELE A. The Rise of Remimazolam: A Review of Pharmacology, Clinical Efficacy, and Safety Profiles [J]. Cureus, 2024, 16(3): 7.

[10] SANDER K, TOM G H, MARC V D V. Remimazolam and serious adverse events: A scoping review [J]. European journal of anaesthesiology, 2023, 40(11): 841-53.

[11] DENG B R, ZHANG Y, XIE Z F, et al. Comparative Analysis of Hemodynamic Effects of Remimazolam and Propofol Combined with Esketamine in Colonoscopic Procedures in the Elderly [J]. Drug Design, Development & Therapy, 2024, 18.

[12] KIM J, LEE S, JEONG J S, et al. Capnography-detected respiratory depression during procedural sedation with remimazolam versus propofol: a randomised trial [J]. Scientific Reports, 2025, 15(1).

[13] SHINTANI R, ICHINOMIYA T, TASHIRO K, et al. Comparison of Hemodynamic Effects of Remimazolam and Midazolam During Anesthesia Induction in Patients Undergoing Cardiovascular Surgery: A Single-Center Retrospective and Exploratory Study [J]. Cureus, 2024.

[14] NIELSEN S, MCAULEY A. Etizolam: A rapid review on pharmacology, non-edical use and harms [J]. Drug and Alcohol Review, 2020, 39(4).

[15] WILTSHIRE H R, KILPATRICK G J, TILBROOK G S, et al. A Placebo- and Midazolam-Controlled Phase I Single Ascending-Dose Study Evaluating the Safety, Pharmacokinetics, and Pharmacodynamics of Remimazolam (CNS 7056) [J]. Anesthesia and analgesia, 2012, 115(2): 284-96.

[16] Li L, Zhou Y. Effects of Remimazolam on Hemodynamics and Postoperative Cognitive Function in Elderly Patients Undergoing Total Hip Arthroplasty under General Anesthesia [J]. Modern Medicine and Health Research (Electronic Edition), 2024, (22).

[17] Cheng HH, Ge Y, Wang H. Effects of Remimazolam on Recovery Quality and Cognitive Function in Elderly Patients Undergoing Total Hip Arthroplasty under General Anesthesia [J]. Systems Medicine, 2025, 10(5): 89-92.

[18] Zhuo M, Liu JL, Zhong ML, et al. Effects of Remimazolam on Postoperative Recovery Quality and Cognitive Function in Patients Undergoing Hepatectomy [J]. Chinese Medical Innovations, 2024, 21(5): 46-50.

[19] Ye XQ. Application Effect of Different Doses of Remimazolam Combined with Propofol and Its Impact on Delirium in Elderly Patients Undergoing Painless Gastrointestinal Endoscopy [J]. Northern Pharmacy, 2024, 21(10): 44-7.

[20] Xu FM, Mao ZH, Ye YJ, et al. Study on Hemodynamic Stability of Tolisate Remimazolam versus Propofol for Anesthetic Sedation during Endoscopic Submucosal Dissection of the Esophagus [J]. China Medicine and Pharmacy, 2023, 13(21): 167-70.