|Other names||Remimazolam besylate, CNS-7056|
|Main uses||Procedural sedation|
|Side effects||Low blood pressure, high blood pressure, low oxygen|
|Duration of action||10 min|
|Chemical and physical data|
|Molar mass||439.313 g·mol−1|
|3D model (JSmol)|
Remimazolam, sold under the brand name Byfavo, is a medication used for procedural sedation. Specifically it is used in adults for procedures lasting less than 30 minutes. It is given by injection into a vein. While onset of effects is similar, the duration is shorter than midazolam.
Common side effects include low blood pressure, high blood pressure, and low oxygen. Other side effects may include abuse and allergic reactions. Effectiveness is not altered in kidney problems, though lower doses may be used in those with liver problems. Effects can be revered with flumazenil. It is a benzodiazepine and works by attaching to gamma-amino butyric acid (GABA) receptors.
Remimazolam was approved for medical use in the United States in July 2020.
The U.S. Food and Drug Administration (FDA) approved remimazolam based on evidence from three clinical trials (Trial 1/NCT02290873, Trial 2/NCT02296892 and Trial 3/NCT02532647) in adults undergoing short procedures. Trials were conducted at 32 sites in the United States.
Trials 1 and 3 were conducted in participants undergoing colonoscopy and Trial 2 was conducted in participants undergoing bronchoscopy procedures.
In the trials, participants were randomly divided in three groups: one group received remimazolam, one group received placebo and one group received midazolam (similar, but approved drug). In the first two groups, neither participants nor investigators knew which medications were given and participants could also receive midazolam as a rescue drug when needed for sedation. In the third group, all participants received midazolam only Additionally, in all three trials participants received a medication for pain control
Trials 1 and 2 compared participants who received remimazolam to participants in the other two groups, measuring the success of sedation with the set of pre-determined criteria. Data from Trial 3 were used primarily to assess the side effects of remimazolam when multiple dosing is used.
Society and culture
On 28 January 2021, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Byfavo, intended for procedural sedation. The applicant for this medicinal product is PAION Netherlands B.V. Remimazolam (Byfavo) was approved for medical use in the European Union in March 2021.
Phase I and Ib dose-finding studies for procedural sedation with patients recovering faster from remimazolam than midazolam. Phase II trials comparing remimazolam to the standard anesthesia protocols for cardiac surgery and colonoscopy were presented at major conferences in October 2014.
A Phase IIa trial comparing remimazolam to midazolam for upper endoscopy was published in December 2014, finding a similar safety profile. Remimazolam was originally synthesized in the late 1990s at Glaxo Wellcome in their labs in Research Triangle Park, North Carolina.
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- Clinical trial number NCT02290873 for "A Phase III Study of the Efficacy and Safety of Remimazolam Compared to Placebo and Midazolam in Colonoscopy Patients" at ClinicalTrials.gov
- Clinical trial number NCT02296892 for "A Phase III Study of Remimazolam in Patients Undergoing Bronchoscopy" at ClinicalTrials.gov
- Clinical trial number NCT02532647 for "Safety and Efficacy of Remimazolam in ASA III and IV Patients Undergoing Colonoscopy" at ClinicalTrials.gov