Papadopoulos Dimitris P, Papademetriou Vasilios
Georgetown University Medical Center, Georgetown, Washington, D.C.; and Veterans Affairs Medical Center, Washington, DC 20422, USA.
Angiology. 2009 Oct-Nov;60(5):608-13. doi: 10.1177/0003319708326450. Epub 2008 Nov 24.
Metoprolol is a selective beta(1)-adrenergic antagonist extensively used since 1975. Metoprolol has proven its efficacy in reducing cardiovascular events and mortality in patients with hypertension and coronary heart disease. A recently developed controlled release/ extended-release formulation of metoprolol succinate was designed to provide relatively constant metoprolol plasma concentrations and beta(1)-blockade while retaining the convenience of once daily administration. A 100-mg metoprolol controlled/extended-release tablet contains 95 mg of metoprolol succinate and is considered to have equivalent activity of 100 mg metoprolol tartrate. After ingestion, the tablet disintegrates into individual pellets and each pellet acts as a diffusion cell releasing the drug at a relatively constant rate over a period of approximately 20 hours. The aim of this review was to determine the pharmacokinetic and pharmacodynamic properties of metoprolol succinate and to apply those properties in combination with other drugs mainly diuretics in the treatment of hypertension.
美托洛尔是一种选择性β(1)肾上腺素能拮抗剂,自1975年以来被广泛使用。美托洛尔已证明其在降低高血压和冠心病患者心血管事件及死亡率方面的疗效。最近开发的琥珀酸美托洛尔控释/缓释制剂旨在提供相对恒定的美托洛尔血浆浓度和β(1)受体阻滞作用,同时保持每日一次给药的便利性。一片100毫克美托洛尔控释/缓释片含有95毫克琥珀酸美托洛尔,被认为具有相当于100毫克酒石酸美托洛尔的活性。摄入后,片剂崩解成单个小丸,每个小丸作为一个扩散单元,在大约20小时的时间内以相对恒定的速率释放药物。本综述的目的是确定琥珀酸美托洛尔的药代动力学和药效学特性,并将这些特性与其他药物(主要是利尿剂)联合应用于高血压的治疗。