神经肌肉阻滞与逆转的新药研发：甘他库铵、CW002、CW011和卡拉巴地翁。
New Drug Developments for Neuromuscular Blockade and Reversal: Gantacurium, CW002, CW011, and Calabadion.
作者信息
de Boer Hans Donald, Carlos Ricardo Vieira
机构信息
Department of Anesthesiology and Pain Medicine, Martini General Hospital Groningen, PO Box 30033, 9700 RM Groningen, the Netherlands.
2Department of Anesthesiology, Child Institute, Hospital das Clinicas, Sao Paulo University Medical School, Sao Paulo, Brazil.
出版信息
Curr Anesthesiol Rep. 2018;8(2):119-124. doi: 10.1007/s40140-018-0262-9. Epub 2018 Mar 22.
PURPOSE OF REVIEW
The purpose of this chapter is to provide a brief review of the literature on the recent developments in neuromuscular blockade and reversal agents.
RECENT FINDINGS
Novel drug development resulted in pharmacological advancements in neuromuscular management and led to a new series of compounds, chlorofumarates, such as gantacurium, CW002, and CW011. These drugs have a fast onset and rapid to intermediate duration of action and can be rapidly reversed by l-cysteine adduction without side effects that are commonly observed with anticholinesterase reversal drugs. Another new advancement is the development of a new class of reversal drugs, the calabadions. These drugs are able to reverse both steroidal and non-steroidal non-depolarizing neuromuscular blocking drugs rapidly.
SUMMARY
Recent advancements in neuromuscular blocking agents and reversal drugs have shown promise in improving safety of management of neuromuscular blockade. Preclinical and clinical studies are discussed. However, to date these new drugs are not yet available for clinical use.
综述目的
本章旨在简要回顾有关神经肌肉阻滞及逆转剂近期进展的文献。
近期研究结果
新型药物研发带来了神经肌肉管理方面的药理学进展，并催生了一系列新化合物，即氯富马酸盐，如甘氨酰环素、CW002和CW011。这些药物起效迅速，作用持续时间从快速到中等，并且可以通过L-半胱氨酸加成迅速逆转，而不会产生抗胆碱酯酶逆转药物常见的副作用。另一项新进展是一类新型逆转药物——卡拉巴多因的研发。这些药物能够迅速逆转甾体和非甾体非去极化神经肌肉阻滞药物的作用。
总结
神经肌肉阻滞剂和逆转药物的近期进展在提高神经肌肉阻滞管理安全性方面显示出前景。文中讨论了临床前和临床研究。然而，迄今为止，这些新药尚未可供临床使用。
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