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瑞马唑仑用于镇静的综合综述。

A comprehensive review of remimazolam for sedation.

作者信息

Noor Nazir, Legendre Rhorer, Cloutet Alexandra, Chitneni Ahish, Varrassi Giustino, Kaye Alan D

机构信息

Mount Sinai Medical Center, Miami Beach, FL.

Louisiana State University Health Sciences Center School of Medicine, Shreveport, LA.

出版信息

Health Psychol Res. 2021 Jun 11;9(1):24514. doi: 10.52965/001c.24514. eCollection 2021.

Abstract

Benzodiazepines are one of the most commonly used medications in the field of anesthesia. They offer excellent anxiolytic and amnestic properties ideal for the perioperative period when patient anxiety is understandably heightened. Remimazolam has presented a favorable alternative to some of the common intravenous anesthetic agents used given its fast onset of action, high safety profile, and reasonably short duration of action. The drugs within the four classes of benzodiazepines, 2-keto-benzodiazepines, 3-hydroxy-benzodiazepines, triazolo-benzodiazepines, and 7-nitro-benzodiazepines provide varying degrees of anxiolysis, sedation, and amnesia. This is provided by the benzodiazepine molecule binding and causing a conformational change to the chloride ion channel to cause hyperpolarization and thus inhibition of the central nervous system. Each type of benzodiazepine has a preferred role within the realm of medicine. For instance, diazepam is used for the treatment of seizures and anxiety. Midazolam's anxiolytic and anterograde amnestic properties are taking advantage of during the perioperative period. Lorazepam is beneficial for anxiety and status epilepticus. Remimazolam, currently in phase II and III clinical trials, has demonstrated a very short during of action and low context-sensitive half-time, allowing for its rapid removal even during a prolonged infusion. Much of its properties may be credited to being a soft drug, meaning it is a metabolically active drug that is rapidly inactivated in the body. This provides anesthesiologists and other practitioners administering it with a more predictable sedative. These properties have the potential to push it towards becoming the drug of choice for premedication during the perioperative period and sedation in the ICU. Furthermore, remimazolam does not seem to rely on any specific organ to be metabolized. The drug's ester moiety makes it a substrate for non-specific tissue esterase enzymes, meaning its metabolism and elimination are not impaired in patients with hepatic and/or renal disease. Its addictive potential closely resembles that of its parent compound, midazolam. Reports of its adverse reactions include headache and somnolence after an involuntary movement during infusion. Benzodiazepines are a great adjunct to anesthetic care. Remimazolam's safety profile, pharmacokinetics, pharmacodynamics, and potential practical use make it quite favorable in this regard. It has the potential to equip anesthesiologists and other medical practitioners with a more predictable medication that has a good safety profile. However, further large clinical trials will provide us with a better understanding of the advantages and disadvantages of remimazolam.

摘要

苯二氮䓬类药物是麻醉领域最常用的药物之一。它们具有出色的抗焦虑和遗忘特性,非常适合围手术期,因为在此期间患者焦虑情绪加剧是可以理解的。瑞马唑仑已成为一些常用静脉麻醉剂的有利替代品,因为它起效快、安全性高且作用时间合理较短。苯二氮䓬类药物的四个类别,即2-酮基-苯二氮䓬类、3-羟基-苯二氮䓬类、三唑并-苯二氮䓬类和7-硝基-苯二氮䓬类中的药物,提供不同程度的抗焦虑、镇静和遗忘作用。这是通过苯二氮䓬分子结合并引起氯离子通道构象变化,导致超极化从而抑制中枢神经系统来实现的。每种类型的苯二氮䓬类药物在医学领域都有其首选作用。例如,地西泮用于治疗癫痫和焦虑。咪达唑仑的抗焦虑和顺行性遗忘特性在围手术期得到了利用。劳拉西泮对焦虑和癫痫持续状态有益。瑞马唑仑目前正处于II期和III期临床试验,已证明其作用时间非常短且背景敏感半衰期低,即使在长时间输注期间也能快速清除。其许多特性可能归功于它是一种软药,这意味着它是一种在体内迅速失活的代谢活性药物。这为麻醉医生和其他使用它的从业者提供了一种更可预测的镇静剂。这些特性有可能使其成为围手术期术前用药和重症监护病房镇静的首选药物。此外,瑞马唑仑似乎不依赖任何特定器官进行代谢。该药物的酯部分使其成为非特异性组织酯酶的底物,这意味着在患有肝和/或肾病的患者中其代谢和消除不会受到损害。其成瘾潜力与母体化合物咪达唑仑非常相似。其不良反应报告包括输注期间非自主运动后出现头痛和嗜睡。苯二氮䓬类药物是麻醉护理的重要辅助药物。瑞马唑仑的安全性、药代动力学、药效学和潜在实际用途在这方面使其非常有利。它有可能为麻醉医生和其他医疗从业者提供一种更可预测且安全性良好的药物。然而,进一步的大型临床试验将使我们更好地了解瑞马唑仑的优缺点。

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