FAST, PREDICTABLE, REVERSIBLE: A COMPREHENSIVE REVIEW OF REMIMAZOLAM

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.