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将布比卡因和利多卡因的心脏电生理特性与一种新型酰胺类局部麻醉药罗哌卡因的特性进行比较。

Cardiac electrophysiologic properties of bupivacaine and lidocaine compared with those of ropivacaine, a new amide local anesthetic.

作者信息

Moller R, Covino B G

机构信息

Department of Anesthesia, Brigham and Women's Hospital, Boston, Massachusetts 02115.

出版信息

Anesthesiology. 1990 Feb;72(2):322-9. doi: 10.1097/00000542-199002000-00019.

Abstract

Ropivacaine is a new amino-amide local anesthetic whose anesthetic profile appears similar to that of bupivacaine. Moreover, in intact animals ropivacaine was reportedly less arrhythmogenic than bupivacaine. These experiments evaluated the cardiac transmembrane electrophysiologic effects of ropivacaine compared with those of lidocaine and bupivacaine in an isolated rabbit Purkinje fiberventricular muscle preparation. Only bupivacaine (3-5 micrograms/ml, 0.92-1.5 x 10(-5) m) significantly decreased Purkinje fiber maximum diastolic potential. Action potential amplitude and maximal rate of depolarization (Vmax) were significantly decreased by all agents in the following order: bupivacaine, ropivacaine, lidocaine. High concentrations of bupivacaine and ropivacaine caused premature depolarizations during phase 3 in some preparations. In addition, bupivacaine altered the action potential configuration by producing "notching" not seen with either ropivacaine or lidocaine. This may reflect effects caused by changes in Ca2+, K+, or electrotonic effects. Ropivacaine and bupivacaine (30 micrograms/ml, 9.2 x 10(-5) m) and lidocaine (100 micrograms/ml, 3.74 x 10(-4) m) caused Purkinje fiber inexcitability and Purkinje fiber-ventricular muscle conduction block. However, the duration of PF inexcitability following exposure to ropivacaine and lidocaine was significantly shorter than in bupivacaine-treated preparation. Duration of PF-VM conduction block also tended to be shorter for ropivacaine than bupivacaine, but significantly longer than lidocaine. In general, ropivacaine is less potent than bupivacaine but more potent than lidocaine in terms of its depressant effect on cardiac excitation and conduction.

摘要

罗哌卡因是一种新型的氨基酰胺类局部麻醉药,其麻醉特性似乎与布比卡因相似。此外,据报道,在完整动物中,罗哌卡因致心律失常的作用比布比卡因小。这些实验在离体兔浦肯野纤维 - 心室肌标本中评估了罗哌卡因与利多卡因和布比卡因相比对心脏跨膜电生理的影响。只有布比卡因(3 - 5微克/毫升,0.92 - 1.5×10⁻⁵摩尔)能显著降低浦肯野纤维最大舒张电位。所有药物均能显著降低动作电位幅度和最大去极化速率(Vmax),其顺序为:布比卡因、罗哌卡因、利多卡因。在某些标本中,高浓度的布比卡因和罗哌卡因在第3期引起过早去极化。此外,布比卡因通过产生罗哌卡因和利多卡因均未出现的“切迹”改变了动作电位形态。这可能反映了由Ca²⁺、K⁺变化或电紧张效应引起的作用。罗哌卡因、布比卡因(30微克/毫升,9.2×10⁻⁵摩尔)和利多卡因(100微克/毫升,3.74×10⁻⁴摩尔)均可导致浦肯野纤维兴奋性丧失和浦肯野纤维 - 心室肌传导阻滞。然而,暴露于罗哌卡因和利多卡因后浦肯野纤维兴奋性丧失的持续时间明显短于布比卡因处理的标本。罗哌卡因引起的浦肯野纤维 - 心室肌传导阻滞持续时间也倾向于比布比卡因短,但明显长于利多卡因。总体而言,就对心脏兴奋和传导的抑制作用而言,罗哌卡因的效力比布比卡因弱,但比利多卡因强。

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