Booij L H
Dept. Anaesthesiology, Catholic University Nijmegen, The Netherlands.
Pharm World Sci. 1997 Feb;19(1):13-34. doi: 10.1023/a:1008641427473.
Clinically, neuromuscular blockade is induced with either depolarizing or non-depolarizing relaxants. Suxamethonium is the only depolarizing relaxant still in use. It is hydrolysed in the plasma by pseudo-cholinesterase (plasma cholinesterase). In some patients and in particular diseases the plasma cholinesterase activity is low and hence the effect of suxamethonium prolonged. Suxamethonium is characterized by side-effects such as myalgia, fasciculations and increase in intraocular, intracranial and intragastric pressure. More serious adverse reactions are masseter muscle spasm and potassium release, in patients with some neuromuscular diseases and increase in extrajunctional acetylcholine receptors. As non-depolarizing muscle relaxants benzylisoquinolines and steroidal compounds are mainly used. Each relaxant has its own pharmacological characteristics. The effect of most relaxants depends on liver and renal function because the pharmacokinetic behaviour is strongly dependent on these organs. Also, acid base balance disturbances, change in temperature, and neurological diseases have an effect on the profile of the relaxants. A number of drugs (anaesthetics, antibiotics, antiepileptics, etc.) have an effect on neuromuscular transmission, and thus interact with the relaxants. Some non-depolarizing relaxants cause histamine release and cardiovascular effects.
临床上，神经肌肉阻滞可通过去极化或非去极化肌松药诱导产生。琥珀胆碱是仍在使用的唯一一种去极化肌松药。它在血浆中被假性胆碱酯酶（血浆胆碱酯酶）水解。在一些患者及特定疾病中，血浆胆碱酯酶活性较低，因此琥珀胆碱的作用时间会延长。琥珀胆碱具有诸如肌痛、肌束震颤以及眼内压、颅内压和胃内压升高等副作用。在患有某些神经肌肉疾病且终板外乙酰胆碱受体增加的患者中，更严重的不良反应是咬肌痉挛和钾离子释放。作为非去极化肌松药，主要使用苄异喹啉类和甾体类化合物。每种肌松药都有其自身的药理学特性。大多数肌松药的作用取决于肝肾功能，因为其药代动力学行为强烈依赖于这些器官。此外，酸碱平衡紊乱、体温变化和神经系统疾病也会对肌松药的作用产生影响。许多药物（麻醉药、抗生素、抗癫痫药等）会对神经肌肉传递产生影响，从而与肌松药相互作用。一些非去极化肌松药会引起组胺释放和心血管效应。
