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首页> 外文期刊>Prescrire international >Ticagrelor. Acute coronary syndromes: nothing new.
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Ticagrelor. Acute coronary syndromes: nothing new.

机译：替卡格雷洛。急性冠状动脉综合征：没有什么新鲜事。

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摘要

Several revascularisation methods are effective in patients with acute coronary syndromes. Standard antithrombotic treatment combines heparin and aspirin during the acute phase, followed by long-term aspirin therapy. The only proven advantage of adding clopidogrel is for patients who undergo angioplasty with stenting. Ticagrelor is an antiplatelet drug belonging to a different chemical class than clopidogrel. Its chemical structure resembles that of adenosine. Ticagrelor has been authorised in the European Union for patients with acute coronary syndromes, in combination with aspirin. Clinical evaluation is mainly based on a double-blind randomised trial comparing ticagrelor + aspirin versus clopidogrel + aspirin in 18 624 patients who underwent angioplasty (64% of patients), coronary artery bypass grafting (10%), or who received medical treatment only. Half of the patients were treated for at least 9 months. After 12 months of treatment, compared to the clopidogrel group, overall mortality appeared to be significantly lower in the ticagrelor group (4.5% versus 5.9%), along with cardiovascular mortality (4.0% versus 5.1%). Symptomatic myocardial infarction was also less frequent (5.8% versus 6.9%), but not stroke (about 1.4% in both groups). Ticagrelor did not statistically significantly reduce overall mortality in patients who had angioplasty with stenting, but stent thrombosis was less frequent than with clopidogrel (2.9% versus 3.8%). In combination with aspirin, ticagrelor provoked more bleeding than clopidogrel, based on the definition used in the trial (16.1% versus 14.6%). In contrast, the rate of major bleeding was similar in the two groups (11.5%), including fatal bleeding (0.3%). The adverse effect profile of ticagrelor resembles that of adenosine in certain respects. For example, dyspnoea was more frequent with ticagrelor than with clopidogrel (13.8% versus 7.8%), as were conduction disorders and ventricular pauses at the beginning of treatment (5.8% versus 3.6%). There were also more cases of hyperuricaemia and elevated creatinine levels with ticagrelor. Ticagrelor and its active metabolite are substrates and inhibitors of cytochrome P450 isoenzymes and P-glycoprotein, creating a risk of multiple pharmacokinetic interactions. Pharmacodynamic interactions are also likely to occur, especially with antithrombotic agents and heart-rate-lowering drugs. In practice, in patients with an acute coronary syndrome treated with angioplasty and stenting, and who are also receiving aspirin, it remains to be shown whether the harm-benefit balance of ticagrelor is clearly better than that of clopidogrel. In other settings, there is no firm evidence that ticagrelor is better than aspirin alone.
机译：几种血运重建方法对急性冠脉综合征的患者有效。在急性期，标准的抗血栓形成治疗将肝素和阿司匹林联合使用，然后进行长期的阿司匹林治疗。经证实，添加氯吡格雷的唯一优势是对那些接受支架置入术的患者。替卡格雷是一种抗血小板药物，与氯吡格雷属于不同的化学类别。它的化学结构类似于腺苷。 Ticagrelor与阿司匹林联用已获欧盟批准用于患有急性冠脉综合征的患者。临床评估主要基于一项双盲随机试验，该试验对ticagrelor +阿司匹林与氯吡格雷+阿司匹林对18 624例行血管成形术（占64％），冠状动脉搭桥术（10％）或仅接受药物治疗的患者进行了比较。一半的患者接受了至少9个月的治疗。与氯吡格雷组相比，治疗12个月后，替卡格雷组的总死亡率似乎显着降低（4.5％对5.9％）以及心血管疾病死亡率（4.0％对5.1％）。有症状的心肌梗塞的发生率也较低（5.8％比6.9％），但没有中风（两组均约为1.4％）。替卡格雷洛没有在统计学上显着降低支架置入血管成形术患者的总死亡率，但支架血栓形成的发生率低于氯吡格雷（2.9％比3.8％）。根据试验中的定义，替卡格雷与阿司匹林合用比氯吡格雷引起更多的出血（16.1％比14.6％）。相反，两组的大出血发生率相似（11.5％），包括致命性出血（0.3％）。替卡格雷的不良反应在某些方面类似于腺苷。例如，替卡格雷比氯吡格雷的呼吸困难发生率更高（分别为13.8％和7.8％），以及治疗开始时的传导障碍和心室停顿（分别为5.8％和3.6％）。替卡格雷对高尿酸血症和肌酐水平升高的病例也更多。替卡格雷及其活性代谢物是细胞色素P450同工酶和P-糖蛋白的底物和抑制剂，存在多重药代动力学相互作用的风险。药效相互作用也很可能发生，特别是在抗血栓药和降低心率的药物中。在实践中，在接受了血管成形术和支架置入术治疗的急性冠状动脉综合征患者中，同时也接受阿司匹林治疗的患者，替卡格洛的利弊平衡是否明显优于氯吡格雷，尚待证实。在其他情况下，没有确凿的证据表明替格瑞洛比单独使用阿司匹林更好。

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