磷酸二酯酶Ⅲ抑制剂——奥普力农的研究新进展  

Advanced progress in olprinone,a phosphodiesterase Ⅲ inhibitor

作　　者：包娜仁[1] 唐冰[1] 王俊科[1] 

机构地区：[1]中国医科大学附属第一医院麻醉科,辽宁沈阳110001

出　　处：《中国新药与临床杂志》2011年第9期657-662,共6页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：奥普力农(olprinone)是由日本开发的治疗急性心力衰竭(心衰)注射剂,选择性地阻碍环磷酸腺苷的特异的磷酸二酯酶Ⅲ抑制剂。适用于治疗急性心衰或心脏外科手术后早期心衰。近年来,许多学者发现奥普力农的其他药理作用,如可选择性扩张脑动脉、颈动脉、肾动脉等,并可应用于治疗哮喘、增强呼吸衰竭时的膈肌收缩力。最新研究表明,由于其增加环磷酸腺苷,抑制炎症细胞聚集以及炎症因子的产生,因此还具有抗炎和器官保护的作用,预防各种病理生理情况下各脏器缺血-再灌注损伤。本文简述其化学特性、药理机制以及临床药理学,并重点就其研究新进展及作用机制做一综述。Olprinone, a specific phosphodiesterase （PDE） III inhibitor, was developed in Japan for the treatment of acute heart failure or early heart failure following cardiac surgery. In recent years, more attention was paid to the other pharmacological effects of olprinone besides heart failure treatment. Olprinone could dilate brain, carotid or renal arteries, etc., and could be used in treating asthma, increasing diaphragmatic contractility. Recent researches showed that olprinone could inhibit the accumulation of inflammatory cells and inflammatory cytokine production, because it could increase cAMP. Olprinone can provide anti-inflammation effect and organ protection and can be used to prevent ischemia-reperfusion injury of organs under a variety of pathophysiological situations.In this article, we reviewed the chemical properties, pharmacological mechanism and clinical pharmacology of olprinone, and focused on its progress and mechanisms.

关 键 词：磷酸二酯酶抑制剂 奥普力农 心力衰竭 充血性 抗炎 器官保护 

分 类 号：R972[医药卫生—药品]