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替格瑞洛与氯吡格雷的安全性特征和出血风险比较。

Safety profile and bleeding risk of ticagrelor compared with clopidogrel.

机构信息

Department of Cardiovascular Medicine, Cleveland Clinic, 9500 Euclid Avenue/J2-3, Cleveland, OH 44195, USA.

出版信息

Expert Opin Drug Saf. 2012 Nov;11(6):959-67. doi: 10.1517/14740338.2012.720972. Epub 2012 Sep 5.

Abstract

INTRODUCTION

Ticagrelor is a novel, non-thienopyridine ADP inhibitor that reversibly blocks the P2Y(12) receptor, preventing platelet activation and aggregation. It is the first ADP inhibitor to show a mortality benefit in patients with acute coronary syndromes (ACS). Its major safety concern, as with the other ADP blockers, is bleeding. Other common adverse effects of ticagrelor such as dyspnea and ventricular pauses appear to be mild and self-limited.

AREAS COVERED

The pharmacological properties of ticagrelor compared with clopidogrel are explored in this article. In addition, the relevant clinical trials in which ticagrelor was investigated are described, with an emphasis on efficacy and safety end points.

EXPERT OPINION

Although some patients suffer from dyspnea when administered with ticagrelor, there is no evidence of any untoward effects on the cardiovascular or pulmonary systems. Given that the majority of these episodes are mild to moderate and self-limiting, patients should be encouraged to continue the medication, as symptoms may resolve. Furthermore, patients with underlying heart failure or lung disease do not appear to be at an increased risk of developing ticagrelor-induced dyspnea. Its overall mortality benefit among patients with ACS, along with its ability to inhibit platelet aggregation more rapidly and consistently, makes it the preferred agent over clopidogrel.

摘要

简介

替格瑞洛是一种新型、非噻吩吡啶类 ADP 受体拮抗剂,可可逆性阻断 P2Y(12)受体,从而抑制血小板激活和聚集。它是首个在急性冠脉综合征(ACS)患者中显示出死亡率获益的 ADP 抑制剂。与其他 ADP 阻滞剂一样,其主要的安全性问题是出血。替格瑞洛的其他常见不良反应,如呼吸困难和室性停搏,似乎较为轻微且呈自限性。

涵盖的领域

本文探讨了替格瑞洛与氯吡格雷的药理学特性。此外,还描述了替格瑞洛相关的临床试验,重点介绍了疗效和安全性终点。

专家意见

虽然一些患者在服用替格瑞洛时会出现呼吸困难,但没有证据表明其对心血管或肺部系统有任何不良影响。鉴于这些症状大多为轻度至中度且呈自限性,应鼓励患者继续服药,因为症状可能会缓解。此外,患有基础心力衰竭或肺部疾病的患者似乎不会增加发生替格瑞洛引起的呼吸困难的风险。在 ACS 患者中,替格瑞洛具有总体死亡率获益,且能够更迅速和一致地抑制血小板聚集,使其成为优于氯吡格雷的首选药物。

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