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β受体阻滞剂卡替洛尔对犬心肺制备标本的心脏抑制作用研究。

A study on the cardiodepressant action of a beta-blocking agent carteolol in heart-lung preparation of the dog.

作者信息

Ono H, O'Hara N

出版信息

Jpn Circ J. 1984 Sep;48(9):1030-44. doi: 10.1253/jcj.48.1030.

Abstract

Direct cardiodepressant activities of three beta-blockers, carteolol, pindolol and propranolol, were estimated using heart-lung preparation of the dog. Beta-blocking doses of these drugs to inhibit the positive chronotropic effect of isoproterenol by 50% were 2.2 micrograms for carteolol, 4.0 micrograms for pindolol and 21 micrograms for propranolol. Cardiac performance of the preparation was not influenced by up to 1 mg of these three beta-blockers. After 10 mg of these drugs, the cardiac function curves were shifted rightward and downward indicating the heart failure. It was doubtful, however, that this result indicated the cardiodepressant action of beta-blockers, for the preparation showed spontaneous deterioration without beta-blocker treatment. The influences of these beta-blockers on the compromised heart-lung preparations showed essentially similar results. In conclusion, direct cardiodepressant activity of the beta-blocker, if any, was exerted with far more large doses than their beta-blocking doses. The implication of the results in clinical use of beta-blockers, especially in relation to heart failure, was discussed.

摘要

使用狗的心肺制备模型评估了三种β受体阻滞剂(卡替洛尔、吲哚洛尔和普萘洛尔)的直接心脏抑制活性。这些药物抑制异丙肾上腺素正性变时作用50%的β受体阻滞剂量分别为:卡替洛尔2.2微克、吲哚洛尔4.0微克、普萘洛尔21微克。高达1毫克的这三种β受体阻滞剂对该制备模型的心脏功能没有影响。给予10毫克这些药物后,心脏功能曲线向右下方移位,提示心力衰竭。然而,这一结果是否表明β受体阻滞剂的心脏抑制作用值得怀疑,因为该制备模型在未用β受体阻滞剂治疗时就出现了自发性恶化。这些β受体阻滞剂对受损心肺制备模型的影响基本相似。总之,β受体阻滞剂若有直接心脏抑制活性,其发挥作用的剂量要比其β受体阻滞剂量大得多。讨论了这些结果对β受体阻滞剂临床应用的意义,尤其是与心力衰竭相关的意义。

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