摘要
替格瑞洛为新型多效性的P_2Y_(12)受体拮抗剂,可通过与血小板上的P_2Y_(12)受体可逆结合,抑制二磷酸腺苷(ADP)诱导的血小板活化与聚集作用,并可抑制红细胞上腺苷ENT1通道载运体,抑制细胞利用腺苷,致使细胞外腺苷浓度增加,从而发挥扩血管、抗炎、抗血小板聚集及心肌保护等药理作用。但患者用药时由于体内腺苷浓度发生变化,会发生呼吸困难、心律失常、尿酸升高等不良反应,这可能与替格瑞洛刺激并导致支气管收缩,抑制红细胞摄取腺苷造成心肌缺血缺氧,腺苷浓度增加导致其代谢产物尿素增加有关。
Ticagrelor is a novel multi potent P2Y12 receptor antagonist,it can inhibit adenosine diphosphate(ADP)-induced platelet activation and aggregation by reversible binding to the P2Y12 receptor on platelets,it also can inhibit the adenosine ENT1 channel carrier on red blood cells,inhibit adenosine utilization by cells.It can increase the concentration of extracellular adenosine and exert its pharmacological effects such as vasodilation,anti-inflammation,anti-platelet aggregation and myocardial protection.However,the adverse reactions such as dyspnea,arrhythmia and elevated uric acid may occur due to the changes in adenosine concentration in the patient's body.These may be related to bronchoconstriction induced by ticagrelor stimulating bronchus,myocardial ischemia and hypoxia induced by inhibition of adenosine uptake by red blood cells,and the increase of adenosine concentration leading to the increase of its metabolite urea.
作者
李悦
陶娌娜
曹雪
宋燕青
张文锐
LI Yue;TAO Lina;CAO Xue;SONG Yanqing;ZHANG Wenrui(Department of Pharmacy,The First Hospital of Jilin University,Changchun,Jilin,China 130031)
出处
《中国药业》
CAS
2019年第8期94-96,共3页
China Pharmaceuticals
基金
吉林省科技发展计划项目[201501011133YY]
关键词
替格瑞洛
腺苷
P2Y12受体拮抗剂
生物学效应
药理作用
临床应用
不良反应
进展
ticagrelor
adenosine
P2Y12 receptor antagonist
biological effect
pharmacological action
clinical application
adverse reactions
progress
