Moller R A, Covino B G
Department of Anesthesia Research, Brigham and Women's Hospital, Boston, Massachusetts 02115.
Anesth Analg. 1993 Jun;76(6):1266-73. doi: 10.1213/00000539-199306000-00014.
Articaine is a local anesthetic structurally different from lidocaine and bupivacaine in that it contains a thiophene ring. We compared its cardiodepressant effects with those of lidocaine and bupivacaine in a randomized, blinded study using the isolated rabbit heart preparation. The hearts were removed quickly from thiamylal anesthetized/killed animals. The right septal wall was placed in a warm, aerated, Tyrode's solution-perfused chamber. The effects of the three local anesthetics on action potentials from the Purkinje fiber (PF) and ventricular muscle (VM) tissues were determined. Bupivacaine (17.4 microM) and articaine (141 microM) depressed action potential overshoot, amplitude, and maximal rate of depolarization (Vmax) by similar amounts. Bupivacaine's effects persisted significantly longer than articaine and lidocaine (P < 0.05). Rate-dependent decreases in steady-state (SS) Vmax were obtained with all three drugs. At their highest concentrations, bupivacaine (17 microM) and lidocaine (85 microM) produced decreases in SS Vmax from the first Vmax response. However, articaine (141 microM) increased SS Vmax at 1 and 2 Hz and only decreased SS Vmax at 3 Hz. During superfusion of a "bolus concentration" of the local anesthetics, bupivacaine blocked PF-VM conduction significantly longer than either articaine or lidocaine (P < 0.001). Articaine, at ten times its observed clinical blood concentration was significantly less cardiodepressant in these in vitro experiments than bupivacaine at five times its observed clinical blood concentration.
阿替卡因是一种局部麻醉药,其结构与利多卡因和布比卡因不同,因为它含有一个噻吩环。在一项使用离体兔心标本的随机、盲法研究中,我们比较了它与利多卡因和布比卡因的心脏抑制作用。心脏迅速从硫喷妥钠麻醉/处死的动物身上取出。右间隔壁被置于一个温暖、通气、用台氏液灌注的腔室中。测定了三种局部麻醉药对浦肯野纤维(PF)和心室肌(VM)组织动作电位的影响。布比卡因(17.4微摩尔)和阿替卡因(141微摩尔)使动作电位的超射、幅度和最大去极化速率(Vmax)降低的程度相似。布比卡因的作用持续时间明显长于阿替卡因和利多卡因(P<0.05)。所有三种药物均导致稳态(SS)Vmax呈速率依赖性降低。在最高浓度时,布比卡因(17微摩尔)和利多卡因(85微摩尔)从第一个Vmax反应开始就使SS Vmax降低。然而,阿替卡因(141微摩尔)在1Hz和2Hz时增加了SS Vmax,仅在3Hz时降低了SS Vmax。在局部麻醉药“推注浓度”的灌注过程中,布比卡因阻断PF-VM传导的时间明显长于阿替卡因或利多卡因(P<0.001)。在这些体外实验中,阿替卡因在其观察到的临床血药浓度的10倍时,其心脏抑制作用明显小于布比卡因在其观察到的临床血药浓度的5倍时。