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与硝普钠和硝酸甘油相比,新型α阻滞剂尼麦角林对开胸麻醉犬的一些血流动力学效应。

Some haemodynamic effects of nicergoline, a new alpha-blocking agent, in the closed-chest anaesthetized dog as compared with nitroprusside and nitroglycerin.

作者信息

Moore N D, Cazor J L, Leclerc J L, Saligaut C, Boismare F

出版信息

Arzneimittelforschung. 1981;31(10):1693-8.

PMID:6797441
Abstract

Considering the recent rediscovery of the use of alpha-blocking agents in the treatment of hypertension and heart failure, we have studied the haemodynamic effects of 10-methyl-1,6-dimethyl-ergoline-8 beta-methanol-(5-bromonicotinate (nicergoline, Sermion), a new alpha-blocking ergot derivative, on the closed-chest anesthetized dog. For comparative reasons, the effects of nitroglycerin and nitroprusside were studied on the same model. The doses were adjusted to give an identical decrease in blood pressure after 30 min infusion (nearly 30%). Nicergoline did not change the heart rate, decreased total and femoral arterial resistance, did not change the cardiac output or the femoral flow, as opposed to nitroglycerin which decreased the cardiac output and systolic volume, causing a reflex tachycardia and femoral constriction, confirming its predominantly venous effect. Nitroprusside did not cause tachycardia, and the femoral resistances were increased, though less so than with nitroglycerin. Both nitroglycerin and nitroprusside apparently had no direct effect on myocardial performance, whilst nicergoline seemed to increase the myocardial compliance (by a decrease of the sympathetic tone). This drug merits further attention in that it is readily soluble and can easily be administered i.v., for treatment of acute heart failure, for example.

摘要

鉴于近期重新发现α受体阻滞剂在高血压和心力衰竭治疗中的应用,我们研究了一种新型α受体阻断麦角衍生物10-甲基-1,6-二甲基麦角灵-8β-甲醇-(5-溴烟酸酯)(尼麦角林,Sermion)对开胸麻醉犬的血流动力学影响。出于比较目的,在同一模型上研究了硝酸甘油和硝普钠的作用。调整剂量以使输注30分钟后血压有相同程度的下降(近30%)。与硝酸甘油降低心输出量和收缩容积、引起反射性心动过速和股动脉收缩从而证实其主要为静脉作用不同,尼麦角林不改变心率,降低总动脉和股动脉阻力,不改变心输出量或股动脉血流量。硝普钠不引起心动过速,股动脉阻力增加,但其增加程度小于硝酸甘油。硝酸甘油和硝普钠显然对心肌功能无直接影响,而尼麦角林似乎增加了心肌顺应性(通过降低交感神经张力)。例如,这种药物易于溶解且可通过静脉注射轻松给药,在治疗急性心力衰竭方面值得进一步关注。

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