Schepens Tom, Cammu Guy
Acta Anaesthesiol Belg. 2014;65(4):151-9.
Non-depolarizing neuromuscular blocking agents (NMBAs) produce neuromuscular blockade by competing with acetylcholine at the neuromuscular junction, whereas depolarizing NMBAs open receptor channels in a manner similar to that of acetylcholine. Problems with NMBAs include malignant hyperthermia caused by succinylcholine, anaphylaxis with the highest incidence for succinylcholine and rocuronium, and residual neuromuscular blockade. To reverse these blocks, anticholinesterases can act indirectly by increasing the amount of acetylcholine in the neuromuscular junction; sugammadex is the only selective relaxant binding agent (SRBA) in clinical use. At all levels of blockade, recovery after sugammadex is faster than after neostigmine. Sugammadex potentially also has some other advantages over neostigmine that are related to neostigmine's increase in the amount of acetylcholine and the necessity of co-administering anticholinergics. However, hypersensitivity reactions, including anaphylaxis, have occurred in some patients and healthy volunteers after sugammadex and remain an issue for the FDA. In the near future, we may see the emergence of new SRBAs and of easier-to-use technologies that can routinely monitor neuromuscular transmissions in daily practice. The nature of the effect of sugammadex on freeing nicotinic acetylcholine receptors located outside the neuromuscular junction from NMBAs is unknown. Moreover, it is uncertain whether the full removal of the competing antagonists (by SRBAs) at the neuromuscular junction impacts the efficiency of acetylcholine transmission. In a recent pilot study in healthy volunteers, we demonstrated increased electromyographic diaphragm activity after sugammadex, compared to neostigmine. Further research is needed to elucidate the role of NMBAs and their reversal agents in the central control of breathing, respiratory muscle activity, and respiratory outcomes.
非去极化神经肌肉阻滞剂（NMBAs）通过在神经肌肉接头处与乙酰胆碱竞争产生神经肌肉阻滞，而去极化NMBAs则以类似于乙酰胆碱的方式打开受体通道。NMBAs的问题包括琥珀胆碱引起的恶性高热、琥珀胆碱和罗库溴铵发生率最高的过敏反应以及残余神经肌肉阻滞。为了逆转这些阻滞，抗胆碱酯酶可通过增加神经肌肉接头处乙酰胆碱的量间接发挥作用；舒更葡糖是临床使用的唯一选择性肌松药结合剂（SRBA）。在所有阻滞水平上，舒更葡糖后的恢复都比新斯的明快。舒更葡糖相对于新斯的明可能还有其他一些优势，这与新斯的明增加乙酰胆碱的量以及联合使用抗胆碱能药物的必要性有关。然而，在一些患者和健康志愿者使用舒更葡糖后发生了包括过敏反应在内的超敏反应，这仍然是美国食品药品监督管理局（FDA）关注的问题。在不久的将来，我们可能会看到新型SRBAs的出现以及更易于使用的技术，这些技术能够在日常实践中常规监测神经肌肉传递。舒更葡糖从NMBAs中释放位于神经肌肉接头外的烟碱型乙酰胆碱受体的作用性质尚不清楚。此外，神经肌肉接头处竞争性拮抗剂（通过SRBAs）的完全清除是否会影响乙酰胆碱传递的效率也不确定。在最近一项针对健康志愿者的初步研究中，我们证明与新斯的明相比，舒更葡糖后肌电图显示的膈肌活动增强。需要进一步研究以阐明NMBAs及其逆转剂在呼吸中枢控制、呼吸肌活动和呼吸结局中的作用。
