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2'-[2-羟基-3-(丙氨基)-丙氧基]-3-苯基苯丙酮(普罗帕酮,SA 79)盐酸盐的药理学

[Pharmacology of 2'-[2-hydroxy-3-(propylamino)-propoxy]-3-phenylpropiophenone (Propafenone, SA 79)-hydrochloride].

作者信息

Hapke H J, Prigge E

出版信息

Arzneimittelforschung. 1976;26(10):1849-57.

PMID:1037204
Abstract

The pharmacologic actions of 2'-[2-hydroxy-3-(propylamino)-propoxy]-3-phenylpropiophenone (propafenone, SA 79) hydrochloride were investigated in animal experiments. The drug showed antiarrhythmic action in anesthetized dogs, cats and rabbits after i.v. (1 mg/kg) and oral (2-10 mg/kg) application. The model arrhythmias were induced by epinephrine infusion plus chloroform inhalation or by infusion of digoxin, calciumchloride or aconitine or by occlusion of the left coronary artery. Propafenon prolonged the refractory period in isolated atria of guinea pigs and elevated the electrical fluttering level of the ventricle in anesthetized guinea pigs or conscious rabbits. It showed local-anesthetic action on the cornea of the guinea pigs. In doses of 3-10 mg/kg i.v. it lowered blood pressure, inhibited contraction force of the heart ventricle and dilated coronary arteries. Heart rate was unchanged by anti-arrhythmic doses. With higher doses (more than 7 mg/kg i.v.) ECG was altered. The autonomic nervous system was unaffected but bronchial adrenergic beta-receptors appeared to be inhibited. The results show, that propafenon has a specific antiarrhythmic action on the heart. The doses to be used have no influences on other circulatory parameters. Propafenon acts after oral application too.

摘要

在动物实验中研究了盐酸2'-[2-羟基-3-(丙氨基)-丙氧基]-3-苯基苯丙酮(普罗帕酮,SA 79)的药理作用。静脉注射(1毫克/千克)和口服(2 - 10毫克/千克)后,该药物在麻醉的狗、猫和兔子身上显示出抗心律失常作用。模型心律失常通过输注肾上腺素加吸入氯仿或输注地高辛、氯化钙或乌头碱或结扎左冠状动脉诱导。普罗帕酮延长了豚鼠离体心房的不应期,并提高了麻醉豚鼠或清醒兔子心室的电颤动水平。它对豚鼠角膜显示出局部麻醉作用。静脉注射剂量为3 - 10毫克/千克时,它降低血压,抑制心室收缩力并扩张冠状动脉。抗心律失常剂量下心率不变。较高剂量(静脉注射超过7毫克/千克)时心电图会改变。自主神经系统未受影响,但支气管肾上腺素β受体似乎受到抑制。结果表明,普罗帕酮对心脏具有特异性抗心律失常作用。所用剂量对其他循环参数无影响。口服普罗帕酮也有作用。

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引用本文的文献

1
Effects of propafenone on calcium current in guinea-pig ventricular myocytes.普罗帕酮对豚鼠心室肌细胞钙电流的影响。
Br J Pharmacol. 1993 Mar;108(3):721-7. doi: 10.1111/j.1476-5381.1993.tb12868.x.
2
Effects of propafenone on TEA-induced action potentials in vascular smooth muscle of canine coronary arteries.普罗帕酮对犬冠状动脉血管平滑肌中TEA诱导的动作电位的影响。
Experientia. 1980 Sep 15;36(9):1082-3. doi: 10.1007/BF01965982.
3
Beta-blocking and electrophysiological effects of propafenone in volunteers.
Eur J Clin Pharmacol. 1983;25(6):831-3. doi: 10.1007/BF00542530.
4
[Electrophysiological classification of newer antiarrhythmic drugs (author's transl)].新型抗心律失常药物的电生理分类(作者译)
Klin Wochenschr. 1980 Sep 15;58(18):907-18. doi: 10.1007/BF01477048.
5
Electrophysiological effects of propafenone in untreated and propafenone-pretreated guinea-pig atrial and ventricular muscle fibres.普罗帕酮对未经处理及经普罗帕酮预处理的豚鼠心房和心室肌纤维的电生理效应。
Br J Pharmacol. 1985 Dec;86(4):765-75. doi: 10.1111/j.1476-5381.1985.tb11098.x.
6
Propafenone. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in the treatment of arrhythmias.普罗帕酮。对其药效学和药代动力学特性以及在心律失常治疗中的治疗用途的综述。
Drugs. 1987 Dec;34(6):617-47. doi: 10.2165/00003495-198734060-00001.
7
Effects of propafenone on 45Ca movements and contractile responses in vascular smooth muscle.普罗帕酮对血管平滑肌中45Ca转运及收缩反应的影响。
Br J Pharmacol. 1991 Jun;103(2):1453-7. doi: 10.1111/j.1476-5381.1991.tb09810.x.