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局部麻醉药的最新进展:以左旋布比卡因为例。

Update on local anesthetics: focus on levobupivacaine.

机构信息

Department of Anesthesia, Intensive Care and Pain Medicine, Mater Misericordiae, University Hospital Dublin, Ireland.

出版信息

Ther Clin Risk Manag. 2008 Apr;4(2):381-92. doi: 10.2147/tcrm.s1433.

Abstract

In recent years levobupivacaine, the pure S (-)-enantiomer of bupivacaine, emerged as a safer alternative for regional anesthesia than its racemic parent. It demonstrated less affinity and strength of depressant effects onto myocardial and central nervous vital centers in pharmacodynamic studies, and a superior pharmacokinetic profile. Clinically, levobupivacaine is well tolerated in a variety of regional anesthesia techniques both after bolus administration and continuous postoperative infusion. Reports of toxicity with levobupivacaine are scarce and occasional toxic symptoms are usually reversible with minimal treatment with no fatal outcome. Yet, levobupivacaine has not entirely replaced bupivacaine in clinical practice. In anesthesia and analgesia practice, levobupivacaine and bupivacaine produce comparable surgical sensory block with similar adverse side effects, and equal labor pain control with comparable maternal and fetal outcome. The equipotency of the two drugs has been recently questioned, prompting clinicians to increase the dose of levobupivacaine in an attempt to ensure adequate anesthesia and analgesia and offsetting, therefore, the advantages of less motor block with levobupivacaine. In this review we aim to discuss the pharmacological essentials of the safer profile of levobupivacaine, and analyze the evidence regarding the current clinical indications.

摘要

近年来,左旋布比卡因(布比卡因的纯 S(-)对映体)作为一种比其外消旋母体更安全的局部麻醉替代药物出现。在药效学研究中,它对心肌和中枢神经系统生命中枢的抑制作用的亲和力和强度较低,药代动力学特征也更好。在临床中,左旋布比卡因在各种局部麻醉技术中都具有良好的耐受性,无论是在单次推注后还是连续术后输注时。有关左旋布比卡因毒性的报告很少,偶尔出现的毒性症状通常在经过轻微治疗后即可逆转,没有致死后果。然而,左旋布比卡因在临床实践中并未完全取代布比卡因。在麻醉和镇痛实践中,左旋布比卡因和布比卡因产生类似的手术感觉阻滞,不良反应相似,且对分娩疼痛的控制效果相同,对母婴结局的影响也相似。这两种药物的等效性最近受到质疑,促使临床医生增加左旋布比卡因的剂量,以确保足够的麻醉和镇痛效果,从而抵消左旋布比卡因运动阻滞较少的优势。在这篇综述中,我们旨在讨论左旋布比卡因更安全的药理学要点,并分析当前临床适应证的相关证据。

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