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

Idrugs Pub Date : 2010-12-01
William Kirke Rogers, Thomas S McDowell
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引用次数: 0

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.

雷马唑仑,一种短效GABA(a)受体激动剂,用于日间手术和非手术过程中的静脉镇静和/或麻醉。
Remimazolam (CNS-7056)是一种短效GABA(a)受体激动剂,由PAION与日本Ono Pharmaceutical合作开发,作为静脉镇静剂,可用于日间手术,诱导和维持麻醉。作为苯二氮杂苯类药物的一员,雷马唑仑的结构经过修饰,可以产生一种不依赖器官代谢的药物。羧酸酯部分掺入雷马唑仑的苯二氮杂苯核心,使其对非特异性组织酯酶敏感,并迅速代谢成其无药理活性的代谢物CNS-7054。绵羊临床前研究表明,与咪达唑仑相比,雷马唑仑起效更快,作用持续时间更短。在一项评估雷马唑仑作为上消化道内镜患者程序性镇静剂的IIa期临床试验中,与咪达唑仑相比,雷马唑仑镇静恢复时间更短,且更一致。由于其不依赖于器官的代谢以及快速和可预测的起效和恢复,雷马唑仑似乎比其他目前可用的短效镇静剂具有潜在的优势。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Idrugs
Idrugs 医学-药学
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