陈维洲, 董月丽, 丁光生. 抗心律失常新药——常咯啉的心血管作用J. 药学学报, 1979, 14(12): 710-714.
引用本文: 陈维洲, 董月丽, 丁光生. 抗心律失常新药——常咯啉的心血管作用J. 药学学报, 1979, 14(12): 710-714.
Chen Weizhou, Dong Yueli , Ding Guangsheng, . CARDIOVASCULAR EFFECT OF A NEW ANTIARRHYTHMIC DRUG——CHANGROLINJ. Acta Pharmaceutica Sinica, 1979, 14(12): 710-714.
Citation: Chen Weizhou, Dong Yueli , Ding Guangsheng, . CARDIOVASCULAR EFFECT OF A NEW ANTIARRHYTHMIC DRUG——CHANGROLINJ. Acta Pharmaceutica Sinica, 1979, 14(12): 710-714.

抗心律失常新药——常咯啉的心血管作用

CARDIOVASCULAR EFFECT OF A NEW ANTIARRHYTHMIC DRUG——CHANGROLIN

  • 摘要: 常咯啉是我所发现的一个新的抗心律失常药。麻醉狗静注常咯啉30mg/kg(2mg/kg/min),对总外周血管阻力减低不显著,血压、左心室内收缩压和心输出量显著降低,左心室作功亦减弱。心电图出现QRS增宽,P-R和Q-Tc间期延长。但停药后一些指标能趋于回复。常咯啉具有心脏迷走神经阻滞作用,而无肾上腺素能受体的阻滞作用。麻醉狗静脉滴注4mg/min共120分钟,可使哇巴因所引起的室性心动过速转为室上性或窦性节律。常咯啉的有效剂量为4.5±2.1mg/kg((?)±SD),血浆中的有效浓度为0.61±0.29μg/ml。滴注15分钟血浆中的浓度升至0.89±0.23μg/ml,至120分钟为2.19±0.16μg/ml。本文结果提示常咯啉对心电图和血流动力学作用基本上与奎尼丁的作用相似。

     

    Abstract: Changrolin is 4-3', 5'-bis (N-pyrrolidinyl) methyl-4'-hydroxyanilino-quinazoline. It was found in our Institute to be a new antiarrhythmic drug. In anesthetized dogs, intravenous injection of 30 mg/kg (2mg/kg/min) did not cause a significant reduction of the total peripheral resistance, but the blood pressure, left ventricular systolic pressure and cardiac output were lowered significantly, The work of the left ventricle was weakened. A widening of the QRS complex and a prolongation of the P-R and Q-Tc intervals on EKG were observed. After cessation of the medication these indices tended to restore. Ghangrolin exhibited a cardio-vagal blocking effect but showed no adrenergic blocking action. Ouabain induced ventricular tachycardia in anesthetized dogs could be reverted to supra-ventricular or sinus rhythm, by intravenous drip of changrolin 4 mg/min for 120 minutes. This reversion occurred when the dose reached 4.5±2.1 mg/kg (±SD) while the concentration of changrolin in plasma was about 0.61±0.29 μg/ml. The concentration of changrolin in plasma rose to 0.89±0.23 μg/ml at 15 minutes and to 2.19±0.16 μg/ml at 120 minutes.The cardiovascular actions of changrolin were thus similar to that of quinidine.

     

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