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药动学与药效学 Esmolol具有β受体阻滞剂的共同结构特点,同时还含有一个酯基,因而易被酯酶水解,红细胞浆中的酯酶水解作用最强。水解产物为甲醇和3.4二羟基—3异丙胺丙氧基苯丙酸,简称ASL—8123。治疗量所产生的甲醇浓度与未用Esmolol时接近。该药清除半衰期为10min,远短于心得安的清除半衰期3.5～6h。停药后2min作用明显减退,18min完全消失。主要以代谢产物形式经肾迅速排泄。该药的优点是心脏β受体(β_1)选择性强,作用时间短。故可用于冠心病伴支气管哮喘患者;对病情变化迅速的病人;比其他β受体阻滞剂易于掌握剂量;静脉用该药后还可在短时间内再用钙通道阻滞剂。
Pharmacokinetics and pharmacodynamics Esmolol β-blockers with the common structural features, but also contains an ester group, which is easily esterase hydrolysis, the strongest red blood cell plasma esterase hydrolysis. Hydrolyzate is methanol and 3.4 dihydroxy-3 isopropylamine propoxyphenylpropionic acid, referred to as ASL-8123. The amount of methanol produced by treatment was similar to that obtained without Esmolol. The drug clearance half-life of 10min, much shorter than the safe clearance half-life 3.5 ~ 6h. 2min after stopping the role of significant decline, 18min completely disappeared. Mainly in the form of metabolites by the rapid renal excretion. The advantage of this medicine is the strong selectivity of cardiac β receptor (β_1) and short acting time. It can be used in patients with coronary heart disease and bronchial asthma; patients with rapidly changing conditions; easy to grasp the dose than other beta-blockers; intravenous use of the drug can be re-used in a short time calcium channel blockers.