Document Type
Article
Publication Date
9-18-2025
Abstract
Remimazolam, an ultrashort-acting benzodiazepine, has emerged as a promising sedative agent for procedural sedation and general anesthesia. It combines the favorable properties of traditional benzodiazepines with a rapid onset and offset of action, largely due to its unique metabolism via hepatic carboxylesterases rather than cytochrome P450 enzymes. This metabolism allows for predictable pharmacokinetics, reducing the risk of prolonged sedation and drug accumulation, particularly in patients with hepatic or renal impairment. Clinically, remimazolam demonstrates non-inferiority to midazolam and propofol, with advantages including a lower incidence of hypotension and respiratory depression. Multiple randomized controlled trials have shown its efficacy in various procedural settings, including endoscopy and bronchoscopy, with high procedural success rates and faster recovery times compared to midazolam. Additionally, remimazolam is reversible with flumazenil, further enhancing its safety profile. Pharmacokinetic studies indicate a rapid distribution phase, a short terminal half-life of approximately 37–53 min, and a clearance rate significantly higher than midazolam. Pharmacodynamic analyses confirm dose-dependent sedation effects, making remimazolam suitable for tailored sedation levels across patient populations. Special population studies suggest minimal impact of age, renal function, or mild-to-moderate hepatic impairment on drug disposition. However, rare cases of anaphylaxis and re-sedation following flumazenil administration have been reported. Given its rapid onset, predictable clearance, and favorable safety profile, remimazolam represents a valuable alternative to existing sedatives in procedural and anesthetic applications. Further research is warranted to explore its long-term safety, expanded clinical applications, and potential role in high-risk populations.
Recommended Citation
Murrell, D.E., Harirforoosh, S. Clinical Pharmacokinetics, Pharmacodynamics, and Drug Interactions of Remimazolam. Eur J Drug Metab Pharmacokinet (2025). https://doi.org/10.1007/s13318-025-00963-2
Copyright
The authors
Creative Commons License
This work is licensed under a Creative Commons Attribution-Noncommercial 4.0 License
Included in
Anesthesia and Analgesia Commons, Medicinal and Pharmaceutical Chemistry Commons, Other Pharmacy and Pharmaceutical Sciences Commons
Comments
This article was originally published in European Journal of Drug Metabolism and Pharmacokinetics in 2025. https://doi.org/10.1007/s13318-025-00963-2