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Remimazolam: A Review in Procedural Sedation

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Remimazolam (Byfavo™) is a benzodiazepine sedative that is indicated for the induction and maintenance of procedural sedation in adults. Remimazolam was efficacious in three phase III trials in patients requiring endoscopies. Significantly higher procedure success rates (composite of the completion of the procedure, top-up doses of study drug within predefined limits and no requirement for rescue therapy) were observed with remimazolam than with placebo, with the majority of placebo recipients requiring rescue midazolam. Furthermore, remimazolam significantly reduced times to onset of sedation and recovery in comparison with placebo (plus rescue). Remimazolam is generally well tolerated, with hypotension and hypertension the most common adverse drug reactions. Higher doses of concomitant fentanyl with remimazolam may increase the incidence of adverse drug reactions and deep sedation events. However, no correlation was observed between depth of sedation and vital signs. In summary, remimazolam is a useful option for the induction and maintenance of procedural sedation. Although pharmacoeconomic analyses for remimazolam are not yet available, the rapid induction of sedation and short recovery times with remimazolam may be beneficial in improving patient throughput in clinics.

Plain Language Summary

Procedural sedation may be administered to patients to improve their comfort during diagnostic or therapeutic procedures. Remimazolam (Byfavo™) is a rapidly metabolised, intravenously administered benzodiazepine sedative, which induces sedation by binding to specific neurotransmitter receptors in the brain. It is approved for the induction and maintenance of procedural sedation in adults. Remimazolam had superior efficacy to placebo in three clinical trials in patients requiring an endoscopy. Most (> 80%) remimazolam recipients successfully completed their endoscopy (≥ 97% of patients) within a predefined dosage regimen of remimazolam (≥ 84%), without requiring midazolam as a rescue sedative (≥ 90%). Conversely, the vast majority (≥ 90%) of placebo recipients required rescue sedation. Times until the onset of sedation and until the patient was ready for discharge post procedure were significantly shorter with remimazolam than with placebo plus rescue. Remimazolam is generally well tolerated, with hypotension and hypertension being the most common adverse drug reactions. Overall, remimazolam is a fast-acting option for procedural sedation and is associated with short recovery times, which has the potential to improve patient throughput in clinics.

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During the peer review process, the manufacturer of remimazolam was also offered an opportunity to review this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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Correspondence to Arnold Lee.

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The preparation of this review was not supported by any external funding.

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Arnold Lee and Matt Shirley are salaried employees of Adis International Ltd/Springer Nature, and declare no relevant conflicts of interest. All authors contributed to the review and are responsible for the article content.

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The manuscript was reviewed by: B. Goudra, Departments of Anesthesiology and Critical Care Medicine, Hospital of the University of Pennsylvania, Philadelphia, PA, USA; B. J. Sweitzer, Perioperative Medicine, Inova Health Systems, Falls Church, VA, USA; S. Amornyotin, Department of Anesthesiology, Faculty of Medicine Siriraj Hospital, Mahidol University, Bangkok, Thailand.

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Lee, A., Shirley, M. Remimazolam: A Review in Procedural Sedation. Drugs 81, 1193–1201 (2021).

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