Ivani G, Borghi B, van Oven H
Dept Anaesthesiology, Regina Margherita Children's, Hospital, Turin, Italy.
Minerva Anestesiol. 2001 Sep;67(9 Suppl 1):20-3.
Bupivacaine has been the most widely used local anaesthetic for years. Recent studies point out levobupivacaine, an S(-) isomer of the racemic bupivacaine. This review shows the properties of levobupivacaine describing the animal and human volunteers studies on toxicity and the first clinical studies in obstetrics, general surgery and paediatrics. In vitro animal studies show that, injected intravenously, levobupivacaine has less cardiotoxic effects and less toxic effects on the CNS in comparison with both R(+) bupivacaine and bupivacaine itself, caused by a minor affinity for brain tissue resulting in less CNS depressant effects as well as for myocardial tissue, which leads to a higher dose necessary before being lethal in comparison to bupivacaine. Studies in human volunteers confirm these results, adding a minor arrhythmogenic, and less negative inotropic effect. Clinical studies show no significant differences in onset, duration and sensory block, but complete regression of sensory block takes longer. Potency is equal for levo- and bupivacaine according to MLAC in labour analgesia. Studies in paediatrics confirm effective analgesia but show less intensity of motor block. The reduced toxicity of levobupivacaine gives wider safety margin in the daily clinical practice both for single shot and for continuous infusion, intraoperatively during various surgical procedures and for the postoperative pain control and analgesia in labour.
多年来,布比卡因一直是使用最广泛的局部麻醉剂。最近的研究指出了左旋布比卡因,它是消旋布比卡因的S(-)异构体。这篇综述展示了左旋布比卡因的特性,描述了关于其毒性的动物和人体志愿者研究以及在产科、普通外科和儿科的首批临床研究。体外动物研究表明,静脉注射时,与R(+)布比卡因和布比卡因本身相比,左旋布比卡因对心脏的毒性作用更小,对中枢神经系统的毒性作用也更小,这是因为它对脑组织的亲和力较小,导致中枢神经系统抑制作用较小,对心肌组织的亲和力也较小,这使得与布比卡因相比,其致死前所需剂量更高。人体志愿者研究证实了这些结果,还发现其致心律失常作用较小,负性肌力作用也较小。临床研究表明,在起效时间、持续时间和感觉阻滞方面没有显著差异,但感觉阻滞的完全消退所需时间更长。根据分娩镇痛中的半数有效浓度(MLAC),左旋布比卡因和布比卡因的效能相当。儿科研究证实了其有效的镇痛作用,但显示运动阻滞的强度较小。左旋布比卡因毒性的降低在日常临床实践中为单次注射和持续输注、各种手术过程中的术中应用以及术后疼痛控制和分娩镇痛都提供了更宽的安全范围。