恩卡胺、劳卡胺和ORG 6001与利多卡因相比在兔和豚鼠离体心脏中的抗纤颤疗效。
Antifibrillatory efficacy of encainide, loracainide and ORG 6001 compared with lignocaine in isolated hearts of rabbits and guinea-pigs.
作者信息
Almotrefi A A, Baker J B
出版信息
Br J Pharmacol. 1981 Jun;73(2):373-7. doi: 10.1111/j.1476-5381.1981.tb10431.x.
Abstract
1 In Langendorff-perfused rabbit hearts, electrical stimulation threshold and ventricular fibrillation threshold (VFT) were measured by applying rectangular impulses of 3 ms duration and increasing current at frequencies of 4 and 20 Hz respectively. 2 Perfusion with lignocaine or one of three new antiarrhythmic drugs, encainide, lorcainide and ORG 6001, produced significant, dose-dependent increases in both thresholds. 3 On a dosage basis, encainide was seven times, lorcainide fourteen times and ORG 6001 twice as potent as lignocaine in raising VFT. 4 In Langendorff-perfused guinea-pig hearts, only lorcainide provided complete protection against ouabain-induced ventricular fibrillation, while 6 of 6, 3 of 6 and 2 of 6 hearts fibrillated in the presence of encainide, lignocaine and ORG 6001 respectively, but with infusion durations significantly higher than control. 5 These results indicate the potential antifibrillatory activity of these new antiarrhythmic agents.
摘要
- 在Langendorff灌注兔心脏中，通过分别施加持续时间为3毫秒的矩形脉冲并以4赫兹和20赫兹的频率增加电流，测量电刺激阈值和心室颤动阈值（VFT）。2. 用利多卡因或三种新的抗心律失常药物之一恩卡尼、劳卡尼和ORG 6001进行灌注，可使两种阈值显著且呈剂量依赖性增加。3. 以剂量为基础，恩卡尼提高VFT的效力是利多卡因的7倍，劳卡尼是14倍，ORG 6001是2倍。4. 在Langendorff灌注豚鼠心脏中，只有劳卡尼能完全预防哇巴因诱导的心室颤动，而在恩卡尼、利多卡因和ORG 6001存在的情况下，分别有6只中的6只、6只中的3只和6只中的2只心脏发生颤动，但输注持续时间明显高于对照组。5. 这些结果表明这些新的抗心律失常药物具有潜在的抗颤动活性。
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