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左旋布比卡因

Levobupivacaine.

作者信息

McClellan K J, Spencer C M

机构信息

Adis International Limited, Auckland, New Zealand.

出版信息

Drugs. 1998 Sep;56(3):355-62; discussion 363-4. doi: 10.2165/00003495-199856030-00005.

DOI:10.2165/00003495-199856030-00005
PMID:9777312
Abstract

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.

摘要

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。

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本文引用的文献

1
The local anaesthetic activity of levobupivacaine does not differ from racemic bupivacaine (Marcain): first clinical evidence.左旋布比卡因的局部麻醉活性与消旋布比卡因(耐乐品)无异:首个临床证据。
Expert Opin Investig Drugs. 1997 Dec;6(12):1883-5. doi: 10.1517/13543784.6.12.1883.
2
Extradural S(-)-bupivacaine: comparison with racemic RS-bupivacaine.硬膜外S(-)-布比卡因:与消旋RS-布比卡因的比较。
Br J Anaesth. 1998 Mar;80(3):289-93. doi: 10.1093/bja/80.3.289.
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Cardiovascular and central nervous system effects of intravenous levobupivacaine and bupivacaine in sheep.
A randomized-controlled, double-blind comparison of the postoperative analgesic efficacy of caudal bupivacaine and levobupivacaine in minor pediatric surgery.小儿短小手术中骶管布比卡因和左旋布比卡因术后镇痛效果的随机对照双盲比较。
Korean J Anesthesiol. 2014 Jun;66(6):457-61. doi: 10.4097/kjae.2014.66.6.457. Epub 2014 Jun 26.
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Epidural Infusion of Morphine and Levobupivacaine through a Subcutaneous Port for Cancer Pain Management.硬膜外输注吗啡和左布比卡因通过皮下港用于癌症疼痛管理。
Korean J Pain. 2014 Apr;27(2):139-44. doi: 10.3344/kjp.2014.27.2.139. Epub 2014 Mar 28.
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Intrathecal low-dose levobupivacaine and bupivacaine combined with fentanyl in a randomised controlled study for caesarean section: blockade characteristics, maternal and neonatal effects.鞘内注射低剂量左旋布比卡因和布比卡因联合芬太尼用于剖宫产的随机对照研究:阻滞特征、对母婴的影响
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A randomized comparison of different doses of intrathecal levobupivacaine combined with fentanyl for elective cesarean section: prospective, double-blinded study.一项比较鞘内不同剂量左旋布比卡因复合芬太尼用于择期剖宫产的随机对照研究:前瞻性、双盲研究。
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Levobupivacaine: a review of its pharmacology and use as a local anaesthetic.左旋布比卡因:其药理学及作为局部麻醉剂应用的综述
Drugs. 2000 Mar;59(3):551-79. doi: 10.2165/00003495-200059030-00013.
左旋布比卡因和布比卡因静脉注射对绵羊心血管及中枢神经系统的影响
Anesth Analg. 1998 Apr;86(4):797-804. doi: 10.1097/00000539-199804000-00023.
4
Myocardial uptake of bupivacaine: II. Pharmacokinetics and pharmacodynamics of bupivacaine enantiomers in the isolated perfused rabbit heart.布比卡因的心肌摄取:II. 布比卡因对映体在离体灌注兔心脏中的药代动力学和药效学
Anesth Analg. 1993 Sep;77(3):477-82.
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Stereoselective block of cardiac sodium channels by bupivacaine in guinea pig ventricular myocytes.布比卡因对豚鼠心室肌细胞中心脏钠通道的立体选择性阻滞作用。
Circulation. 1995 Nov 15;92(10):3014-24. doi: 10.1161/01.cir.92.10.3014.
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Stereoselective effects of the enantiomers of bupivacaine on the electrophysiological properties of the guinea-pig papillary muscle.布比卡因对映体对豚鼠乳头肌电生理特性的立体选择性作用。
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Reg Anesth. 1992 Nov-Dec;17(6):311-6.