FAST, PREDICTABLE, REVERSIBLE: A COMPREHENSIVE REVIEW OF REMIMAZOLAM
DOI:
https://doi.org/10.31435/ijitss.1(49).2026.5111Keywords:
Remimazolam, Benzodiazepines, GABA-A, Procedural Sedation, General Anesthesia, PropofolAbstract
Remimazolam is a new, ultra–short-acting benzodiazepine whose unique chemical structure—the introduction of an ester moiety into the benzodiazepine core—enables rapid hydrolysis by non-specific tissue esterases to an inactive metabolite (CNS7054). This modification, analogous to that used in remifentanil, ensures an exceptionally rapid onset and equally rapid offset of sedation, organ-independent metabolism, and a highly predictable pharmacokinetic profile. The drug is intended exclusively for intravenous administration, which—according to the summary of product characteristics—eliminates gastrointestinal absorption and avoids the first-pass effect.
Pharmacodynamically, remimazolam exerts its sedative effect through allosteric enhancement of the inhibitory action of GABA at the GABA-A receptor. Remimazolam may be administered as a bolus or continuous infusion, and its dosing varies depending on the indication, country, patient condition, and concomitant medications. Compared with midazolam, it is characterized by a faster onset, deeper sedative effect, and shorter duration of action.
In comparison with propofol, remimazolam does not shorten recovery time but offers a more favorable safety profile—it significantly less frequently causes post-induction hypotension, bradycardia, respiratory depression, or injection pain. An additional advantage is the availability of a specific antidote—flumazenil. Although remimazolam reduces the risk of postoperative nausea and vomiting (PONV) compared with inhalational anesthetics, it may be associated with a higher incidence of vomiting when compared directly with propofol. However, the drug may offer benefits in terms of postoperative patient comfort.
Methodology: This review paper is based on data derived from peer-reviewed scientific articles and reports published in recognized databases and journals, including PubMed, Clinical Pharmacokinetics, and Anaesthesiology Intensive Therapy. It includes clinical studies and review articles published between 2015 and 2025 in English or Polish.
References
Zhang, H., Li, H., Zhao, S., & Bao, F. (2024). Remimazolam in general anesthesia: A comprehensive review of its applications and clinical efficacy. Drug Design, Development and Therapy, 18, 3487–3498. https://doi.org/10.2147/DDDT.S474854
Hu, Q., Liu, X., Wen, C., Li, D., & Lei, X. (2022). Remimazolam: An updated review of a new sedative and anaesthetic. Drug Design, Development and Therapy, 16, 3957–3974. https://doi.org/10.2147/DDDT.S384155
Kim, S. H., & Fechner, J. (2022). Remimazolam: Current knowledge on a new intravenous benzodiazepine anesthetic agent. Korean Journal of Anesthesiology, 75(4), 307–315. https://doi.org/10.4097/kja.22297
Kim, K. M. (2022). Remimazolam: Pharmacological characteristics and clinical applications in anesthesiology. Anesthesia and Pain Medicine, 17(1), 1–11. https://doi.org/10.17085/apm.21115
Kilpatrick, G. J. (2021). Remimazolam: Non-clinical and clinical profile of a new sedative/anesthetic agent. Frontiers in Pharmacology, 12, 690875. https://doi.org/10.3389/fphar.2021.690875
Pesic, M., Schippers, F., Saunders, R., Webster, L., Donsbach, M., & Stoehr, T. (2020). Pharmacokinetics and pharmacodynamics of intranasal remimazolam: A randomized controlled clinical trial. European Journal of Clinical Pharmacology, 76(11), 1505–1516. https://doi.org/10.1007/s00228-020-02984-z
Pesic, M., Stöhr, T., Ossig, J., Borkett, K., Donsbach, M., Dao, V. A., Webster, L., & Schippers, F. (2020). Remimazolam has low oral bioavailability and no potential for misuse in drug-facilitated sexual assaults, with or without alcohol: Results from two randomised clinical trials. Drugs in R&D, 20(3), 267–277. https://doi.org/10.1007/s40268-020-00317-0
Schmalix, W., Petersen, K. U., Pesic, M., & Stöhr, T. (2024). The metabolism of the new benzodiazepine remimazolam. Current Drug Metabolism, 25(2), 164–173. https://doi.org/10.2174/0113892002301026240318060307
Zhou, Y., Hu, P., & Jiang, J. (2017). Metabolite characterization of a novel sedative drug, remimazolam, in human plasma and urine using ultra high-performance liquid chromatography coupled with synapt high-definition mass spectrometry. Journal of Pharmaceutical and Biomedical Analysis, 137, 78–83. https://doi.org/10.1016/j.jpba.2017.01.016
Stöhr, T., Colin, P. J., Ossig, J., Pesic, M., Borkett, K., Winkle, P., Struys, M. M. R. F., & Schippers, F. (2021). Pharmacokinetic properties of remimazolam in subjects with hepatic or renal impairment. British Journal of Anaesthesia, 127(3), 415–423. https://doi.org/10.1016/j.bja.2021.05.027
Petersen, K. U., Schmalix, W., Pesic, M., & Stöhr, T. (2024). Drug-drug interaction potential of remimazolam: CYP 450, transporters, and protein binding. Current Drug Metabolism, 25(4), 266–275. https://doi.org/10.2174/0113892002300657240521094732
de Jong, B. T., Eleveld, D. J., Mason, K. P., & Struys, M. M. R. F. (2025). Clinical pharmacokinetics and pharmacodynamics of remimazolam. Clinical Pharmacokinetics, 64(9), 1263–1282. https://doi.org/10.1007/s40262-025-01548-7
Aszkiełowicz, A., Kapłan, C., Kapica, P., & Marszałek, R. (2025). Remimazolam: A comprehensive review. Anaesthesiology Intensive Therapy, 57(1), 257–266. https://doi.org/10.5114/ait/210611
Schüttler, J., Eisenried, A., Lerch, M., Fechner, J., Jeleazcov, C., & Ihmsen, H. (2020). Pharmacokinetics and pharmacodynamics of remimazolam (CNS 7056) after continuous infusion in healthy male volunteers: Part I. Pharmacokinetics and clinical pharmacodynamics. Anesthesiology, 132(4), 636–651. https://doi.org/10.1097/ALN.0000000000003103
Eisenried, A., Schüttler, J., Lerch, M., Ihmsen, H., & Jeleazcov, C. (2020). Pharmacokinetics and pharmacodynamics of remimazolam (CNS 7056) after continuous infusion in healthy male volunteers: Part II. Pharmacodynamics of electroencephalogram effects. Anesthesiology, 132(4), 652–666. https://doi.org/10.1097/ALN.0000000000003102
Fechner, J., El-Boghdadly, K., Spahn, D. R., Motsch, J., Struys, M. M. R. F., Duranteau, O., Ganter, M. T., Richter, T., Hollmann, M. W., Rossaint, R., Bercker, S., Rex, S., Drexler, B., Schippers, F., Morley, A., Ihmsen, H., Kochs, E., & Surgery Under Remimazolam - Total IntraVenous Anaesthesia (SURE-TIVA) Trial Group. (2024). Anaesthetic efficacy and postinduction hypotension with remimazolam compared with propofol: A multicentre randomised controlled trial. Anaesthesia, 79(4), 410–422. https://doi.org/10.1111/anae.16205
Doi, M., Morita, K., Takeda, J., Sakamoto, A., Yamakage, M., & Suzuki, T. (2020). Efficacy and safety of remimazolam versus propofol for general anesthesia: A multicenter, single-blind, randomized, parallel-group, phase IIb/III trial. Journal of Anesthesia, 34(4), 543–553. https://doi.org/10.1007/s00540-020-02788-6
Wu, X., Wang, C., Gao, H., Bai, X., Zhang, Z., Chen, R., Huang, X., An, L., Yi, J., & Tong, R. (2023). Comparison of remimazolam and propofol about safety outcome indicators during general anesthesia in surgical patients: A systematic review and meta-analysis. Minerva Anestesiologica, 89(6), 553–564. https://doi.org/10.23736/S0375-9393.23.17034-9
Chang, Y., Huang, Y. T., Chi, K. Y., & Huang, Y. T. (2023). Remimazolam versus propofol for procedural sedation: A meta-analysis of randomized controlled trials. PeerJ, 11, e15495. https://doi.org/10.7717/peerj.15495
Zhao, M. J., Hu, H. F., Li, X. L., Li, X. M., Wang, D. C., & Kuang, M. J. (2023). The safety and efficacy between remimazolam and propofol in intravenous anesthesia of endoscopy operation: A systematic review and meta-analysis. International Journal of Surgery, 109(11), 3566–3577. https://doi.org/10.1097/JS9.0000000000000638
Ko, C. C., Hung, K. C., Illias, A. M., Chiu, C. C., Yu, C. H., Lin, C. M., Chen, I. W., & Sun, C. K. (2023). The use of remimazolam versus propofol for induction and maintenance of general anesthesia: A systematic review and meta-analysis. Frontiers in Pharmacology, 14, 1101728. https://doi.org/10.3389/fphar.2023.1101728
Mao, Y., Guo, J., Yuan, J., Zhao, E., & Yang, J. (2022). Quality of recovery after general anesthesia with remimazolam in patients undergoing urologic surgery: A randomized controlled trial comparing remimazolam with propofol. Drug Design, Development and Therapy, 16, 1199–1209. https://doi.org/10.2147/DDDT.S359496
Ri, H. S., Jeon, S., Yeo, J., Jung, H., Kang, C., & Choo, H. (2025). Efficacy of remimazolam in preventing postoperative nausea and vomiting: A systematic review and meta-analysis. Scientific Reports, 15(1), 29236. https://doi.org/10.1038/s41598-025-14976-z
Yang, J. J., Lei, L., Qiu, D., Chen, S., Xing, L. K., Zhao, J. W., Mao, Y. Y., & Yang, J. J. (2023). Effect of remimazolam on postoperative delirium in older adult patients undergoing orthopedic surgery: A prospective randomized controlled clinical trial. Drug Design, Development and Therapy, 17, 143–153. https://doi.org/10.2147/DDDT.S392569
Downloads
Published
Issue
Section
License
Copyright (c) 2026 Agata Juchniewicz, Jakub Sapikowski, Julita Jagodzińska, Maria Janiszewska, Martyna Grześkowiak, Iga Kuba, Jakub Idziński, Anna Lubomska, Mikołaj Góralczyk

This work is licensed under a Creative Commons Attribution 4.0 International License.
All articles are published in open-access and licensed under a Creative Commons Attribution 4.0 International License (CC BY 4.0). Hence, authors retain copyright to the content of the articles.
CC BY 4.0 License allows content to be copied, adapted, displayed, distributed, re-published or otherwise re-used for any purpose including for adaptation and commercial use provided the content is attributed.

