Freysz M, Béal J L, Timour Q, Bertrix L, Faucon G
Département d'Anesthésie-Réanimation, Hôpital Général, Dijon.
Ann Fr Anesth Reanim. 1988;7(3):181-8. doi: 10.1016/s0750-7658(88)80109-6.
Local anaesthetics can have systemic adverse effects, mostly affecting the central nervous system and the heart. The physicochemical characteristics of the different local anaesthetics are recalled, for they determine the relationship between structure, activity and toxicity. The pharmacokinetic factors involved in the toxic effects of local anaesthetics, whether the drug is given in a single extravascular dose or, accidentally, within a blood vessel, are discussed. The toxic effects of repeated administrations of local anaesthetics depend on the metabolism of the drug as well as on pharmacokinetic factors. Possible maximal doses and drug interactions are also discussed. The mechanism of action of local anaesthetics, which block the sodium channel, explains their tissue toxicity and, more specifically, their central nervous and cardiovascular toxicities, which are more pronounced for the more potent local anaesthetic agents (bupivacaine, etidocaine). Systemic maternal effects and transplacental passage probably explain their foetal toxicity. Specific toxic effects are seen with some drugs, such as methaemoglobinaemia and allergic reactions (rarely for amide agents). Overall, local anaesthetic accidents are rare, but they must be prevented.
局部麻醉药可产生全身不良反应，主要影响中枢神经系统和心脏。回顾了不同局部麻醉药的理化特性，因为它们决定了结构、活性和毒性之间的关系。讨论了局部麻醉药产生毒性作用时涉及的药代动力学因素，无论药物是单次血管外给药，还是意外注入血管内。局部麻醉药重复给药的毒性作用取决于药物的代谢以及药代动力学因素。还讨论了可能的最大剂量和药物相互作用。局部麻醉药通过阻断钠通道发挥作用的机制，解释了它们的组织毒性，更具体地说，解释了它们的中枢神经和心血管毒性，对于更强效的局部麻醉药（布比卡因、依替卡因）而言，这些毒性更为明显。母体的全身效应和经胎盘转运可能解释了它们对胎儿的毒性。某些药物会出现特定的毒性作用，如高铁血红蛋白血症和过敏反应（酰胺类药物很少见）。总体而言，局部麻醉意外很少见，但必须加以预防。
