remimazolam mesylate

Remimazolam mesylate is a novel, ultra-short acting, water-soluble benzodiazepine sedative and anesthetic. It acts as a positive allosteric modulator and agonist at the gamma-aminobutyric acid type A (GABAA) receptor, enhancing GABA-mediated inhibitory neurotransmission in the central nervous system. This results in sedation, hypnosis, anxiolysis, anticonvulsant effects, and muscle relaxation. Its unique structure incorporates an ester bond that allows for rapid hydrolysis by non-specific tissue esterases into an inactive metabolite (CNS7054), leading to fast onset and offset of action with minimal accumulation even after prolonged infusion. The drug’s metabolism does not depend on hepatic or renal function—making it suitable for patients with organ impairment—and its effects can be rapidly reversed by flumazenil if needed. Developed as a safer alternative to existing sedatives like propofol and midazolam, remimazolam mesylate is approved in China for procedural sedation during endoscopy/colonoscopy as well as induction and maintenance of general anesthesia[1][2][3][5][7].

Brand names

瑞倍宁

Other names

甲磺酸瑞马唑仑注射用甲磺酸瑞马唑仑Remimazolam tosylate (alternate salt form, but not the mesylate)Remimazolam (parent compound)