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氟司洛尔(简称Fle)是继艾司洛尔后的又一个超短效作用的β阻滞剂。不同的是它对心脏无选择性,作用更强,半衰期更短。本文综述Fle的药效学和药动学。药效学 1.动物研究:Gorczynski等在豚鼠及麻醉狗的离体心脏及支气管组织中研究了Fle的β阻滞作用。测得Fle对心房的pA_2(拮抗激动剂产生的β作用所需摩尔浓度的负对数)为8.01,支气管组织的pA_2为8.16。因此它是个非心脏选择性β阻滞剂。浓度在pA_2的4倍以上时无内源性拟交感活性,但有直接的心脏抑制作用。在麻醉狗,Fle抑制异丙肾上腺素(ISO)引起的心动过速的50%所需剂量约为每分钟1μg/kg,其效能
Fluorolol (Fle) is after Esmolol is another ultra-short-acting beta blockers. The difference is that it is non-selective heart, stronger role, shorter half-life. This article reviews Fle’s pharmacodynamics and pharmacokinetics. Pharmacodynamics 1. Animal studies: Gorczynski et al. Studied the beta block of Fle in isolated hearts and bronchial tissues of guinea pigs and anesthetized dogs. The pA 2 of Fle (a negative logarithm of molar concentration required to antagonize agonist-produced β) was measured to be 8.01 for Fle and 8.16 for bronchial tissue. It is therefore a non-cardiac selective beta blocker. There was no intrinsic sympathomimetic activity at concentrations above 4-fold higher than pA2 but with direct cardiac inhibition. In anesthetized dogs, the dose required for 50% of Fle to inhibit isoproterenol (ISO) -induced tachycardia is about 1 μg / kg per minute, and its efficacy