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Esmolol(ASL-8052)为一种新的超短时作用的β-受体阻滞剂,尤其对心脏β-受体具有选择性阻滞作用。其注射剂主要用于静脉滴注,生物利用度高,起效快,因其药动学半衰期短,故作用持续时间短,易于控制。一、药动学 Esmolol为苯氧丙醇胺类化合物,在苯氧丙醇胺的对位含有一个丙酸甲酯链,可被血浆或组织中的酯酶(主要是红细胞胞质中的酯酶)水解代谢而失活。Esmolol的主要代谢产物是ASL-8123和甲醇;ASL-8123为
Esmolol (ASL-8052) is a novel β-blocker with ultra-short-duration action, which has selective block on cardiac β-receptor. Its injection is mainly used for intravenous infusion, high bioavailability, rapid onset, because of its short half-life pharmacokinetic, so the role of short duration, easy to control. Pharmacokinetics Esmolol is a phenoxy propanolamine compound containing a methyl propionate in the para-position of phenoxypropanolamine that can be activated by esterases in the plasma or tissue (predominantly in the cytoplasm of erythrocytes Enzyme) is hydrolytically metabolized and inactivated. The major metabolites of Esmolol are ASL-8123 and methanol; ASL-8123 is