Remimazolam, a short-acting GABA(A) receptor agonist for intravenous sedation and/or anesthesia in day-case surgical and non-surgical procedures

William Kirke Rogers; Thomas S McDowell

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Journal article

Remimazolam, a short-acting GABA(A) receptor agonist for intravenous sedation and/or anesthesia in day-case surgical and non-surgical procedures

William Kirke Rogers and Thomas S McDowell

IDrugs : the investigational drugs journal, Vol.13(12), pp.929-937

12/2010

PMID: 21154153

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Abstract

Remimazolam (CNS-7056) is a short-acting GABA(A) receptor agonist, under development by PAION, in collaboration with Japanese licensee Ono Pharmaceutical, as an intravenous sedative agent for potential use in day-case procedures, and the induction and maintenance of anesthesia. A member of the benzodiazapene class of drugs, the structure of remimazolam was modified to produce a drug that displays organ-independent metabolism. The incorporation of a carboxylic ester moiety into the benzodiazapene core of remimazolam renders it susceptible to non-specific tissue esterases and it is rapidly metabolized into its pharmacologically inactive metabolite CNS-7054. Preclinical studies in sheep demonstrated that remimazolam produced a more rapid onset of action, and a shorter duration of action, compared with midazolam. In a phase IIa clinical trial evaluating remimazolam as a procedural sedative for upper gastrointestinal endoscopy in patients, the time to recovery from sedation was shorter and more consistent with remimazolam, relative to midazolam. Because of its organ-independent metabolism and rapid and predictable onset and recovery, remimazolam appears to have potential advantages over other currently available short-acting sedatives.

Anesthetics, Intravenous - adverse effects

Drugs, Investigational - adverse effects

Drugs, Investigational - pharmacology

Anesthetics, Intravenous - therapeutic use

Hypnotics and Sedatives - adverse effects

Humans

Drugs, Investigational - pharmacokinetics

Drugs, Investigational - therapeutic use

Hypnotics and Sedatives - therapeutic use

Anti-Anxiety Agents - pharmacokinetics

Anesthetics, Intravenous - pharmacology

GABA-A Receptor Agonists - pharmacology

Anti-Anxiety Agents - adverse effects

Anti-Anxiety Agents - therapeutic use

GABA-A Receptor Agonists - pharmacokinetics

GABA-A Receptor Agonists - therapeutic use

Benzodiazepines - pharmacology

GABA-A Receptor Agonists - adverse effects

Hypnotics and Sedatives - pharmacokinetics

Anti-Anxiety Agents - pharmacology

Benzodiazepines - pharmacokinetics

Animals

Ambulatory Surgical Procedures

Anesthetics, Intravenous - pharmacokinetics

Benzodiazepines - adverse effects

Hypnotics and Sedatives - pharmacology

Benzodiazepines - therapeutic use

Details

Title: Subtitle: Remimazolam, a short-acting GABA(A) receptor agonist for intravenous sedation and/or anesthesia in day-case surgical and non-surgical procedures
Creators: William Kirke Rogers - University of Wisconsin-Madison, Department of Anesthesiology, School of Medicine and Public Health B6/319 Clinical Sciences Center, 600 Highland Avenue, Madison WI 53792-3272, USA
Thomas S McDowell
Resource Type: Journal article
Publication Details: IDrugs : the investigational drugs journal, Vol.13(12), pp.929-937
PMID: 21154153
ISSN: 1369-7056
eISSN: 2040-3410
Language: English
Date published: 12/2010
Academic Unit: Anesthesia
Record Identifier: 9984083868802771

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