Klinik für Anaesthesiologie und Intensivmedizin, Technische Universität München, Klinikum Rechts der Isar, Ismaninger Straße, München, Germany.
Curr Opin Anaesthesiol. 2020 Aug;33(4):490-498. doi: 10.1097/ACO.0000000000000891.
The present review provides a summary of the literature on recent development of new neuromuscular blocking agents and presents clinically well established and new reversal agents.
Anesthesiologists are still waiting for the ideal neuromuscular blocking agent with a succinylcholine-like rapid onset and offset without side effects. Recent drug development led to a new series of neuromuscular compounds, called the chlorofumarates such as gantacurium, CW002, and CW011. These drugs have a promising pharmacodynamic profile; importantly, they can rapidly be reversed by L-cysteine adduction without relevant side effects. In addition, a new spectrum of reversal agents are currently examined in preclinical studies: adamgammadex sodium, a modified γ-cyclodextrin derivate that forms an inactive tight inclusion complex with rocuronium or vecuronium and calabadions, capable of reversing both benzylisoquinolines and steroidal neuromuscular blocking agents.
Although the recent advancements in neuromuscular research are very promising, to date, the presented drugs are currently not available for clinical use. Clinical studies will determine the role of these developments in anesthesia practice. Therefore, well established combinations such as rocuronium-sugammadex are popular in clinical practice to offer quick paralysis for intubation and to optimize surgical conditions, while providing a fast neuromuscular recovery at the end of surgery.
本综述总结了近年来新型神经肌肉阻断剂的研究进展，并介绍了临床上已确立的和新的逆转剂。
麻醉师仍在等待具有琥珀胆碱样快速起效和消除作用而无副作用的理想神经肌肉阻断剂。最近的药物开发导致了一系列新的神经肌肉化合物，称为氯代富马酸盐，如加丹曲林、CW002 和 CW011。这些药物具有有前途的药效学特征；重要的是，它们可以通过 L-半胱氨酸加成快速逆转，而没有相关的副作用。此外，目前正在临床前研究中检查一系列新的逆转剂：纳曲胺，一种改良的γ-环糊精衍生物，与罗库溴铵或维库溴铵和 calabadions 形成无活性的紧密包含复合物，能够逆转苯并异喹啉类和甾体神经肌肉阻断剂。
尽管神经肌肉研究的最新进展非常有前景，但迄今为止，所提出的药物目前尚未临床应用。临床研究将确定这些进展在麻醉实践中的作用。因此，罗库溴铵- sugammadex 等已确立的组合在临床实践中很受欢迎，可提供快速插管的麻痹作用，并优化手术条件，同时在手术结束时提供快速的神经肌肉恢复。
