Remimazolam: A New Ultra Short Acting Benzodiazepine

Remimazolam (CNS 7056) is a novel molecule, water soluble, ultra-short-acting intravenous BDZ under human research in protocols phase II-III. This new BDZ is a designed soft drug, ester-based, intended to undergo rapid hydrolysis by esterase enzymes to inactive metabolites. It acts on GABAA receptors containing gamma subunits, initiating cell membrane hyperpolarization and therefore inhibition of the neural activity via rising chloride influx. After intravenous infusion it rapidly induces sedation for a short period of time with no serious side effects. It has been investigated in the induction and maintenance of general anesthesia, for sedation in gastrointestinal endoscopies, and in the critically ill patient. Like other BDZs, remimazolam can be reversed with flumazenil in order to rapidly terminate sedation if necessary. Because of its organ-independent metabolism, rapid and predictable onset and recovery, remimazolam appears to be the next sedative drug.