Department of Anaesthesiology, Institut Mutualiste Montsouris, 42 Bd Jourdan, 75014, Paris, France.
Clinique Medipole Garonne, Toulouse, France.
Drugs. 2018 Aug;78(12):1229-1246. doi: 10.1007/s40265-018-0955-x.
Lidocaine is an amide local anaesthetic initially used intravenously as an antiarrhythmic agent. At some point it was proposed that intravenous lidocaine (IVL) had an analgesic effect that could be potentially beneficial in perioperative settings. Since these preliminary reports, a large body of evidence confirmed that IVL had anti-inflammatory and opiate-sparing effects, a combination of characteristics leading to an array of effects such as a decrease in postoperative pain and opiate consumption, and a reduction in the duration of digestive ileus. Additional studies demonstrated IVL to possess antithrombotic, antimicrobial and antitumoral effects. Beneficial effects of IVL have been characterized in abdominal surgery but remain controversial in other types of surgeries. Because the quality of evidence was limited, due to inconsistency, imprecision and study quality, recent conclusions from meta-analysis pooling together all types of surgery stated the uncertainty about IVL benefits. Additional indications such as the prevention of propofol-induced injection pain, prevention of hyperalgesia, protection against bronchial reactivity by bronchotracheal relaxation during surgery, and the increase in depth of general anaesthesia have since emerged. IVL is rapidly distributed in the body and metabolized by the liver. With the commonly recommended doses, lidocaine's therapeutic index remains very high and the plasma concentrations stay largely below the cardiotoxic and neurotoxic threshold levels, a notion that may be used by clinicians to draw conclusions on the benefit-risk profile of IVL in comparison to other analgesic strategies. The purpose of this review is to address the pharmacokinetic and pharmacodynamic properties of lidocaine in healthy and pathological conditions.
利多卡因是一种酰胺类局部麻醉剂,最初作为抗心律失常药物静脉内使用。在某个时候,有人提出静脉内利多卡因(IVL)具有镇痛作用,在围手术期可能有益。自这些初步报告以来,大量证据证实 IVL 具有抗炎和阿片类药物节约作用,这种组合的特点导致了一系列的效果,如术后疼痛和阿片类药物消耗减少,以及消化性肠梗阻持续时间缩短。其他研究表明 IVL 具有抗血栓形成、抗菌和抗肿瘤作用。IVL 在腹部手术中的有益作用已得到证实,但在其他类型手术中的作用仍存在争议。由于证据质量有限,由于不一致性、不精确性和研究质量,最近汇总所有类型手术的荟萃分析得出的结论对 IVL 益处存在不确定性。其他适应症如预防异丙酚引起的注射疼痛、预防痛觉过敏、通过支气管松弛术在手术期间保护支气管反应性以及增加全身麻醉深度等也相继出现。IVL 在体内迅速分布并被肝脏代谢。在常用推荐剂量下,利多卡因的治疗指数仍然很高,血浆浓度在很大程度上低于心脏毒性和神经毒性阈值水平,这一概念可能被临床医生用来比较 IVL 与其他镇痛策略的获益风险状况。本综述的目的是探讨利多卡因在健康和病理条件下的药代动力学和药效学特性。