Heppolette Chantal A A, Brunnen Derek, Bampoe Sohail, Odor Peter M
Centre of Anaesthesia and Perioperative Medicine, University College Hospital, London, UK.
Centre for Perioperative Medicine, University College London, London, UK.
Clin Pharmacokinet. 2020 Jun;59(6):715-745. doi: 10.1007/s40262-020-00868-0.
Levobupivacaine is a long-acting amide local anaesthetic used in analgesia and anaesthesia. Like other local anaesthetic drugs, levobupivacaine exhibits effects on motor and sensory nerves by inhibiting the opening of voltage-gated sodium channels, and hence propagation of neuronal action potentials. Levobupivacaine is the S(-) stereoisomer of dextrobupivacaine, although both are used commercially in the racemic form bupivacaine. A favourable safety and drug effect profile for levobupivacaine has led to widespread use. Levobupivacaine is generally well tolerated but dose adjustment is important in populations such as paediatrics and the elderly. The pharmacokinetic properties of levobupivacaine are similar to that of bupivacaine; both extensively metabolised in the liver, and excreted in the urine and faeces. In vitro, animal model and human studies confirm a lower risk of cardiac and central nervous system toxicity with levobupivacaine compared with bupivacaine. Clinical trials of relative potency are impaired by the variability in chosen endpoints for sensory and motor function blockade, but clinically significant differences in potency are minor, with most clinical trials showing similar duration and quality of anaesthesia between levo- and racemic bupivacaine. In practice, levobupivacaine is most commonly used in regional anaesthesia, neuraxial anaesthesia and local infiltration analgesia. This review includes an appraisal of evidence from clinical trials of the pharmacokinetic and pharmacodynamic properties of levobupivacaine.
左旋布比卡因是一种长效酰胺类局部麻醉药，用于镇痛和麻醉。与其他局部麻醉药一样，左旋布比卡因通过抑制电压门控钠通道的开放，从而抑制神经元动作电位的传播，对运动神经和感觉神经产生作用。左旋布比卡因是布比卡因的S(-)立体异构体，尽管两者在商业上均以消旋形式布比卡因使用。左旋布比卡因良好的安全性和药物效应使其得到广泛应用。左旋布比卡因一般耐受性良好，但在儿科和老年人等人群中调整剂量很重要。左旋布比卡因的药代动力学特性与布比卡因相似；两者均在肝脏中广泛代谢，并通过尿液和粪便排泄。体外、动物模型和人体研究证实，与布比卡因相比，左旋布比卡因引起心脏和中枢神经系统毒性的风险更低。由于感觉和运动功能阻滞所选终点的变异性，相对效价的临床试验受到影响，但效价的临床显著差异较小，大多数临床试验表明左旋布比卡因和消旋布比卡因之间的麻醉持续时间和质量相似。在实践中，左旋布比卡因最常用于区域麻醉、神经轴麻醉和局部浸润镇痛。本综述包括对左旋布比卡因药代动力学和药效学特性临床试验证据的评估。
