A Placebo- and Midazolam-Controlled Phase I Single Ascending-Dose Study Evaluating the Safety, Pharmacokinetics, and Pharmacodynamics of Remimazolam (CNS 7056)

Abstract

Remimazolam provided sedation with rapid onset and offset, and was well tolerated. There was no supplemental oxygen or ventilation required. On the basis of these data, further studies on the potential utility of remimazolam for sedation/anesthesia are warranted.

Enhancement of GABAergic Activity: Neuropharmacological Effects of Benzodiazepines and Therapeutic Use in Anesthesiology

“…Remimazolam has been administered for 1 min to healthy male volunteers, and a doserelated depression of bispectral index and a change in the sedation state was observed (Antonik et al, 2009 randomized, double-blind, dose-finding study of 100 patients undergoing upper gastrointestinal endoscopy has been completed and the results are to be published (Rogers and McDowell, 2010). According to the data published by the manufacturer Paion AG, the procedure was completed without assisted ventilation or supplementary sedation in 32, 56, and 64% of patients receiving remimazolam 0.1, 0.15, and 0.2 mg/kg, respectively, compared with 44% of patients receiving midazolam 0.075 mg/kg.…”

Determination of the Hypnotic Potency in Rats of the Novel Ketamine Ester Analogue SN 35210

“…Previous investigators have employed similar rationale in the development of such 'soft' designer drugs as remifentanil [23] , and more recently remimazolam [24] , and MOC-etomidate [25] , each designed to exhibit predictable elimination kinetics through rapid metabolism by esterases to inactive metabolites. By adopting this rationale, we have produced a drug with seemingly ketamine-like qualities (rapid onset hypnosis), yet with significantly lesser duration of action.…”

Total Intravenous Anesthesia and Anesthetic Outcomes

“…In phase 1 clinical trials, median time for return to a fully alert condition was 10 minutes compared with 40 minutes for midazolam. 57 Novel propofol and etomidate formulations are being developed in an effort to overcome drawbacks associated with current TOTAL INTRAVENOUS ANESTHESIA AND ANESTHETIC OUTCOMES S13 formulations, such as pain on injection (for propofol) and adrenal suppression (for etomidate). 58 Although these agents are in early stages of development, preliminary evidence is encouraging, and they may increase the popularity of TIVA in the future.…”