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[关于β2-肾上腺素能支气管舒张剂克仑特罗(喘舒平)的心脏和血流动力学副作用]

[On the cardiac and hemodynamic side-effects of the beta 2-adrenergic broncholytic agent clenbuterol (Contraspasmin)].

作者信息

Femmer K, Heer S

出版信息

Pharmazie. 1982 Aug;37(8):584-6.

PMID:7146067
Abstract

Clenbuterol was tested for cardiac and haemodynamic side-effects by administering cumulative broncholytically efficient doses (continuous infusion) to anaesthetized dogs. The application of a dose of 1.25 micrograms/kg produced increased heart rate (+ 18%), increased maximum pressure-rise rate dp/dt max (+ 44%), increased heart time volume (+ 43%) and decreased total peripheral resistance (- 30%). The circulatory action of an isoprenaline dose of equivalent broncholytic efficacy (0.1875 micrograms/kg/min) led to more considerably marked changes of + 75%, - 117%, + 51% and - 33%, respectively. Parallel to the cardiovascular changes, Clenbuterol causes only a slight and non-significant increase of free fatty acids in the serum (+ 23%), whereas isoprenaline (with + 107%) has a strong beta 1-mimetic effect. In contrast to this, Clenbuterol stimulates the mobilization of glucose to a greater extent than isoprenaline. These findings show that Clenbuterol must be considered as a broncholytic agent of great beta 2-specificity; due to its long duration of action and its easy enteral absorption, it constitutes a true enrichment of therapeutics.

摘要

通过向麻醉犬输注累积支气管溶解有效剂量(持续输注)来测试克仑特罗的心脏和血流动力学副作用。给予1.25微克/千克的剂量可使心率增加(+18%)、最大压力上升速率dp/dt max增加(+44%)、每搏输出量增加(+43%)以及总外周阻力降低(-30%)。同等支气管溶解效力的异丙肾上腺素剂量(0.1875微克/千克/分钟)的循环作用分别导致更为显著的变化,即+75%、-117%、+51%和-33%。与心血管变化平行,克仑特罗仅使血清中游离脂肪酸略有增加且无统计学意义(+23%),而异丙肾上腺素(增加107%)具有强烈的β1拟交感神经效应。与此相反,克仑特罗比异丙肾上腺素更能刺激葡萄糖的动员。这些发现表明,克仑特罗必须被视为一种具有高度β2特异性的支气管溶解剂;由于其作用持续时间长且易于肠道吸收,它是治疗学上的一项真正进展。

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