Remimazolam: The future of its sedative potential

Abstract

Remimazolam (CNS 7056) is a new drug innovation in anesthesia. It combines the properties of two unique drugs already established in anesthesia – Midazolam and remifentanil. It acts on GABA receptors like midazolam and has organ-independent metabolism like remifentanil. It is likely to be the sedative of the future, as preliminary phase II trials have shown minimal residual effects on prolonged infusions. It has potential to be used as a sedative in ICU and as a novel agent for procedural sedation. Unlike most rapidly acting intravenous sedatives available presently, the propensity to cause apnea is very low. Availability of a specific antagonist (flumazenil) adds to its safety even in cases of overdose. The present review discusses remimazolam's potential as a new drug in anesthesia along with the presently available literary evidence.

Effects of Vitamin D Receptor, Cytochrome P450 3A, and Cytochrome P450 Oxidoreductase Genetic Polymorphisms on the Pharmacokinetics of Remimazolam in Healthy Chinese Volunteers

“…Remimazolam is a new ultra‐short‐acting benzodiazepine used for sedation and anesthesia 1 . Remimazolam works on the gamma‐aminobutyric acid receptor, especially gamma‐aminobutyric acid‐α, 2 which is similar to midazolam. In addition, the compound structure of remimazolam is similar to that of midazolam (Figure 1).…”

Medical, Political, and Economic Considerations for the Use of MAC for Endoscopic Sedation: Big Price, Little Justification?

“…The drug is metabolized quickly when administered in the doses and durations typically used for endoscopic sedation. Remimazolam is a benzodiazepine and like propofol acts on GABA-alpha receptors [ 50 , 51 ]. In fact, it has a structure quite similar to midazolam, the very popular sedative in GI endoscopy.…”

Pharmacological sedation management in the paediatric intensive care unit

“…Apart from optimal dosing strategies, new products may also improve pharmacological sedation management. A promising example is the ultra‐rapid‐acting benzodiazepine remimazolam, which has a pharmacokinetic profile comparable to that of remifentanil, allowing for fast titration. It has only been studied in adults so far.…”