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氟哌隆(一种抗精神病丁酰苯类药物)的实验性抗心律失常特性

Experimental anti-arrhythmic properties of melperone, a neuroleptic butyrophenone.

作者信息

Petersen E N

出版信息

Acta Pharmacol Toxicol (Copenh). 1978 May;42(5):388-94. doi: 10.1111/j.1600-0773.1978.tb02222.x.

Abstract

The neuroleptic butyrophenone, melperone, has been compared with antiarrhythmics, neuroleptics, alpha-blockers and beta-blockers in various experimental arrhythmias. Melperone 0.01--1 mg/kg intravenously antagonized ouabain-induced arrhythmias in conscious rabbits to the same degree as propranolol 2 mg/kg and quinidine 10 mg/kg intravenously probably mainly via s CNS depressive effect. It was found to be considerably weaker than propranolol 2 mg/kg, when anaesthetized guinea pigs were used. Melperone 0.1--10 mg/kg was inactive against aconitine-induced arrhythmias. Melperone 1--5 mg/kg antagonized adrenaline-induced arrhythmias in halothane-sensitized guinea pigs like phentolamine 1--5 mg/kg intravenously and was more potent than chlorpromazine, propranolol and quinidine. This study and an electrophysiological study suggest that melperone might be a type III anti-arrhythmic drug, which at the same time depresses CNS and reduces afterload.

摘要

抗精神病药丁酰苯类药物美哌隆,已在各种实验性心律失常中与抗心律失常药、抗精神病药、α受体阻滞剂和β受体阻滞剂进行了比较。静脉注射0.01 - 1毫克/千克的美哌隆,对清醒家兔哇巴因诱发的心律失常的拮抗作用程度与静脉注射2毫克/千克的普萘洛尔和10毫克/千克的奎尼丁相同,这可能主要是通过中枢神经系统抑制作用实现的。当使用麻醉豚鼠时,发现其作用比2毫克/千克的普萘洛尔弱得多。0.1 - 10毫克/千克的美哌隆对乌头碱诱发的心律失常无活性。1 - 5毫克/千克的美哌隆对氟烷致敏豚鼠肾上腺素诱发的心律失常的拮抗作用与静脉注射1 - 5毫克/千克的酚妥拉明相似,且比氯丙嗪、普萘洛尔和奎尼丁更有效。这项研究和一项电生理研究表明,美哌隆可能是一种III类抗心律失常药物,同时具有抑制中枢神经系统和降低后负荷的作用。

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