McClellan K J, Spencer C M
Adis International Limited, Auckland, New Zealand.
Drugs. 1998 Sep;56(3):355-62; discussion 363-4. doi: 10.2165/00003495-199856030-00005.
Levobupivacaine is an enantiomer of the long-acting local anaesthetic bupivacaine, which, although currently the most widely used agent in surgery and obstetrics, is associated with potentially fatal cardiotoxicity. Levobupivacaine 75 to 122 mg was less arrhythmogenic than the same dose range of bupivacaine in healthy volunteers. Its effects on the corrected QT interval were significantly weaker than those of bupivacaine, and it tended to have a weaker effect on QRS duration. The CNS depressant effect of intravenous levobupivacaine 40 mg was less than that of bupivacaine 40 mg in healthy volunteers, both in terms of the magnitude of the effect and the regions of the cortex affected. Clinical studies have demonstrated that epidural levobupivacaine produces a sensory and motor block clinically similar to that of bupivacaine in patients requiring anaesthesia during surgery. However, the duration of sensory block was significantly longer with levobupivacaine 0.75% than with levobupivacaine 0.5% or bupivacaine 0.5% or 0.75% in one study. Levobupivacaine 0.25% was as effective as bupivacaine 0.25% in women requiring epidural anaesthesia during labour with respect to time to onset of pain relief, overall quality of analgesia, extent of sensory blockade and number of patients reporting motor block. Levobupivacaine is as well tolerated as bupivacaine. In a clinical study involving 88 patients who received either drug, intraoperative hypotension was the most commonly reported adverse event with levobupivacaine and no serious arrhythmias occurred.
左旋布比卡因是长效局部麻醉药布比卡因的一种对映体,布比卡因虽然是目前外科手术和产科中使用最广泛的药物,但存在潜在致命的心脏毒性。在健康志愿者中,75至122毫克的左旋布比卡因比相同剂量范围的布比卡因致心律失常性更低。其对QT间期校正值的影响明显弱于布比卡因,并且对QRS波时限的影响往往也较弱。在健康志愿者中,静脉注射40毫克左旋布比卡因的中枢神经系统抑制作用在作用强度和受影响的皮质区域方面均小于40毫克布比卡因。临床研究表明,在手术期间需要麻醉的患者中,硬膜外注射左旋布比卡因产生的感觉和运动阻滞在临床上与布比卡因相似。然而,在一项研究中,0.75%的左旋布比卡因产生的感觉阻滞持续时间明显长于0.5%的左旋布比卡因或0.5%或0.75%的布比卡因。在分娩期间需要硬膜外麻醉的女性中,0.25%的左旋布比卡因在疼痛缓解开始时间、总体镇痛质量、感觉阻滞程度以及报告运动阻滞的患者数量方面与0.25%的布比卡因效果相同。左旋布比卡因与布比卡因的耐受性相当。在一项涉及88名接受这两种药物之一的患者的临床研究中,术中低血压是左旋布比卡因最常报告的不良事件,且未发生严重心律失常。