超长效局麻药的研究进展

Research progress of ultra⁃long⁃acting local anesthetics

多模式镇痛是术后疼痛管理的金标准,以超声引导下的神经阻滞为基础辅以少阿片类药物和足量全程使用的非甾体类抗炎药是目前最主流的多模式镇痛方案。但超声引导下神经阻滞受限于局麻药作用时间,往往为外科手术患者提供不超过8 h的有效术后镇痛,使外科手术患者术后镇痛满意率不高。随着快速康复理念的不断深入研究,如何延长局麻药的作用时间是研究的重点和热点。超长效局麻药包括已经应用于临床的布比卡因脂质体、HTX-011,以及仍处于研究阶段的季铵盐类衍生物等。本文将从具有缓释系统的超长效局麻药、超长效局麻药的新作用通路及靶点、开发全新化合物形式的超长效局麻药进行综述,为后续超长效局麻药的研究与临床应用提供新的思路。

Multimodal analgesia is the gold standard for postoperative pain management,and ultrasound-guided nerve block as the cornerstone supplemented with fewer opioids and a sufficient amount of non-steroidal anti-inflammatory drugs(NSAIDs)throughout the entire course of the procedure is the most mainstream multimodal analgesic regimen at present.However,ultrasound-guided nerve blocks are limited by the duration of action of local anesthetics and often provide effective analgesia for surgical patients for no more than 8 hours,resulting in a low satisfaction rate of postoperative analgesia in surgical patients.With the continuous research on the concept of rapid rehabilitation,how to extend the duration of action of local anesthetics is the focus and hotspot of research.Ultra-long-acting local anesthetics include liposomal bupivacaine and HTX-011,which have been applied in clinical practice,and quaternary ammonium derivatives,which are still in the research stage.In this paper,we will review the existing ultra-long-acting local anesthetics in terms of ultra-long-acting local anesthetics with extended-release systems,new pathways and targets of ultra-long-acting local anesthetics,and the development of ultra-long-acting local anesthetics in the form of brand-new compounds,so as to provide new ideas for the subsequent research and clinical application of ultra-long-acting local anesthetics.