卡维地洛抗实验性心律失常作用  

Protective effects of carvedilol on experimental arrhythmias

作　　者：吕艳青[1] 周际安[1] 曾繁典[1] 

机构地区：[1]同济医科大学临床药理研究所

出　　处：《中国药理学通报》1999年第5期428-431,共4页Chinese Pharmacological Bulletin

摘　　要：目的　评价卡维地洛（ＣＶＤ）抗实验性心律失常作用，并与β受体阻断剂普萘洛尔（ＰＲＯ） 进行比较。方法　采用氯仿致小鼠室颤（ＶＦ） ， 哇巴因、乌头碱致豚鼠、大鼠心律失常，肾上腺素致豚鼠心律失常， 以及结扎大鼠冠状动脉诱发心律失常等５ 种模型。结果　与溶媒对照组相比， ＣＶＤ１ ｍｇ·ｋｇ－１ 显著降低氯仿诱发的小鼠ＶＦ 发生率〔１８－７５ ％（３／１６） ｖｓ８１－２５％ （１３／１６），Ｐ＜ ０－０１〕，此作用与ＰＲＯ 相似。１ ｍｇ·ｋｇ－１ ＣＶＤ 和ＰＲＯ 均显著提高致室早（ＶＥ） ， 室速（ＶＴ）， ＶＦ， 心搏停止（ＣＡ） 所需哇巴因和乌头碱用量（ Ｐ＜０－０１ ｖｓ 溶剂对照组） ；ＣＶＤ 对抗哇巴因的致心律失常作用较等剂量ＰＲＯ 显著（ Ｐ＜ ０－０１ ，ＣＶＤ ｖｓ ＰＲＯ）。ＣＶＤ 剂量依赖性地显著缩短ｉｖ 肾上腺素４０ μｇ·ｋｇ－ １ 所致心律失常持续时间，有效减少结扎冠脉诱发的缺血性心律失常ＶＴ，ＶＦ，ＣＡ 的发生率并缩短ＶＴ 的持续时间。结论　ＣＶＤ 具有抗多种实验性心律失常作用，该作用在等剂量时至少与ＰＲＯ 相近，或强于ＰＲＯ。ＣＶＤ的这种作用最终将有益于接受其治疗的原发性高血压、冠心病。AIM The aim was to evaluate the antiarrhythmic effects provided by carvedilol, and compared with propranolol in several arrhythmia animal models. METHODS Experiments were performed in 5 arrhythmic animal models, inhalation of chloroform to induce ventricular fibrillation (VF) in mice, ouabain induced or aconitine induced arrhythmia in guinea pigs or rats, adrenaline induced arrhythmia in guinea pigs and ligation of coronary artery of rats to induce arrhythmia. RESULTS Carvedilol 1 mg·kg -1 significantly reduced the chloroform induced VF incidence in mice[18 75% (3/16) vs 81 25%(13/16), carvedilol vs vehicle]. The effects were similar to which of propranolol. The doses of ouabain and aconitine to produce ventricular extrasystole (VE), ventricular tachycardia (VT), VF, cardiac arrest (CA) were significantly increased in 1 mg·kg -1 of carvedilol and of propranolol groups respectively ( P <0 01 vs vehicle). At the same dose, the effects of carvedilol on ouabain induced arrhythmia were greater than those of propranolol (P <0 01 vs vehicle, P< 0 01 vs propranolol). The duration of arrhythmia induced by 40 μg·kg -1 adrenaline were significantly reduced by carvedilol, in a dose dependent manner. Besides these, carvedilol also effectively reduced VT, VF, CA incidences and duration of VT in animals subjected to coronary artery ligation. CONCLUSIONS Carvedilol has antiarrhythmic effects in various animal models. At the same dose, 1 mg·kg -1 , its antiarrhythmic effects were at least equal to which of propranolol, or more potent. The antiarrhythmic effects provided by carvedilol may ultimately be beneficial to patients subjected to essential hypertension, coronary artery disease or congestive heart failure.

关 键 词：卡维地洛 抗心律失常药 

分 类 号：R972.2[医药卫生—药品]