Zink Wolfgang, Graf Bernhard M
Department of Anesthesiology, Emergency and Intensive Care Medicine, University of Goettingen, Goettingen, Germany.
Curr Opin Anaesthesiol. 2008 Oct;21(5):645-50. doi: 10.1097/ACO.0b013e32830c214c.
Ropivacaine and levobupivacaine were developed after evidence of bupivacaine-related severe toxicity. Despite a comparable analgesic profile, quantitative differences become evident with regard to their specific rate of systemic toxicity. The present article provides a concise review of the toxic potencies of levobupivacaine and ropivacaine.
As lipophilicity is known to be a major determinant in local anesthetic toxicity, the clinical safety profile of ropivacaine seems to be more favorable than that of levobupivacaine. Experimental studies and case reports confirm this hypothesis, showing that ropivacaine is characterized by fewer (cardio) toxic effects and, most probably, a greater margin of safety. Both agents also may dose dependently damage neurons and skeletal muscle tissue at the injection site. Although their specific rate of neurotoxicity appears to be rather low, levobupivacaine is characterized by an outstanding myotoxic potential.
Compared with bupivacaine, both agents may be considered as 'more well tolerated' but not as 'totally well tolerated', as they are still capable of inducing systemic and local toxicity. However, ropivacaine seems to have the greatest margin of safety of all long-acting local anesthetics at present.
在有证据表明布比卡因存在严重毒性后,罗哌卡因和左旋布比卡因被研发出来。尽管它们的镇痛效果相当,但在全身毒性的具体发生率方面,定量差异变得明显。本文对左旋布比卡因和罗哌卡因的毒性强度进行简要综述。
由于已知亲脂性是局部麻醉药毒性的主要决定因素,罗哌卡因的临床安全性似乎比左旋布比卡因更有利。实验研究和病例报告证实了这一假设,表明罗哌卡因的(心脏)毒性作用较少,而且很可能具有更大的安全边际。两种药物在注射部位也可能剂量依赖性地损伤神经元和骨骼肌组织。尽管它们的神经毒性发生率似乎相当低,但左旋布比卡因具有显著的肌毒性潜力。
与布比卡因相比,这两种药物都可被认为“耐受性更好”,但并非“完全耐受性良好”,因为它们仍能引起全身和局部毒性。然而,罗哌卡因似乎是目前所有长效局部麻醉药中安全边际最大的。