Clopidogrel is a mainstay in the treatment of patients with acute coronary syndromes or those receiving endovascular prostheses.However,its efficacy has been challenged in the recent past by studies suggesting variabl...Clopidogrel is a mainstay in the treatment of patients with acute coronary syndromes or those receiving endovascular prostheses.However,its efficacy has been challenged in the recent past by studies suggesting variable individual responsiveness and by new,more potent competitors,such as prasugrel and ticagrelor. But what is the actual body of evidence in support of clopidogrel?Is there any dark side of the moon?What is the role of prasugrel,which has already been approved in Europe and in the United States?And what will be the future role of ticagrelor,when approved for routine clinical practice?We hereby concisely summarize the scope of this clinical choice,providing arguments in favor and against each of the three antiplatelet agents:clopidogrel,prasugrel,and ticagrelor.展开更多
Aim To evaluate the time-effect and dose-effect of prasugrel hydrobromide acetic acid compound （PHAAC） inhibiting platelet aggregation. Methods For the time-effect study, 190 Sprague-Dawley （SD） rats were devided ...Aim To evaluate the time-effect and dose-effect of prasugrel hydrobromide acetic acid compound （PHAAC） inhibiting platelet aggregation. Methods For the time-effect study, 190 Sprague-Dawley （SD） rats were devided into 19 groups （n- 10）： the vehicle control group, the PHAAC groups （0.5, 1, 2, 4, 6, 24, 48, 72, 96 h） and the prasugrel hydrochloride groups （0.5, 1, 2, 4, 6, 24, 48, 72, 96 h）. Rats were singly intra- gastic administration of the vehicle, the PHAAC （5 mg·kg^-1） or the prasugrel hydrochloride （5 mg · kg^-1 ）, re- spectively. Blood samples were taken at each time point for the determination of platelet aggregation rate （PAR）. For the dose-effect study, 110 SD rats were devided into 11 groups （n= 10）： the vehicle control group, the PHAAC groups （10, 5, 2.5, 1, 0.5 mg · kg^-1, dosage of prasugrel） and the prasugrel hydrochloride groups （ 10, 5, 2.5, 1, 0.5 mg · kg^-1, dosage of prasugrel） . Blood samples were taken at 4 h after drug administration for the determination of PAR. Results Compared with the vehicle group, PHAAC has significant anti-platelet ag- gregative effects （P 〈 0.05） at the time of 0.5, 1, 2, 4, 6, 24, 48 h, and the effect at the time of 4 h was the strongest. There were no obvious differences between the effect of PHAAC （5 mg · kg^-1） and prasugrel hydrochlo- ride （5 mg · kg^-1） at each time point. Compared with the vehicle group, intragastic administration of PHAAC at the doses of 10, 5, 2.5, 1, 0.5 mg · kg^-1 could obviously inhibite the platelet aggregation, and showed a dose- dependent manner. There were no significant differences between the effect of PHAAC and prasugrel hydrochloride at the same dose. Conclusion PHAAC can inhibit platelet aggregation in a dose-dependent manner, and the effect at 4 h after drug administration is the strongest. The action strength and duration of PHAAC are similar with that of the prasugrel hydrochloride.展开更多
Dual antiplatelet therapy consisting of low-dose aspirin (LDA) and other antiplatelet medications is recommended in patients with coronary heart disease, but it may increase the risk of esophageal lesion and bleeding....Dual antiplatelet therapy consisting of low-dose aspirin (LDA) and other antiplatelet medications is recommended in patients with coronary heart disease, but it may increase the risk of esophageal lesion and bleeding. We describe a case of esophageal mucosal lesion that was difficult to distinguish from malignancy in a patient with a history of ingesting LDA and prasugrel after implantation of a drug-eluting stent. Multiple auxiliary examinations were performed to make a definite diagnosis. The patient recovered completely after concomitant acid-suppressive therapy. Based on these findings, we strongly argue for the evaluation of the risk of gastrointestinal mucosal injury and hemorrhage if LDA therapy is required, and we stress the paramount importance of using drug combinations in individual patients.展开更多
Background Clopidogrel is beneficial after acute coronary syndrome. Recent studies suggest the superiority of prasugrel compared with clopidogrel. The enhanced platelet inhibition with prasugrel lead to a reduction in...Background Clopidogrel is beneficial after acute coronary syndrome. Recent studies suggest the superiority of prasugrel compared with clopidogrel. The enhanced platelet inhibition with prasugrel lead to a reduction in major adverse cardiovascular events in patients with moderate to high risk acute coronary syndrome scheduled for PCI. However, prasugrel showed signs of increased bleeding potential. We performed a meta-analysis to assess clinical safety and efficacy of prasugrel in patients with acute coronary syndrome. Methods We systematically searched PubMed, ISI Web of Knowledge, Cochrane Central Register of Controlled Trials, clinicaltrials. gov, proceedings of major US and European cardiology meetings, China National Knowledge Infrastructure （CNKI） databases 2000-2010 and reviews, reference lists of relevant articles. The search strategy paired the term ＂prasugrel＂ ＂clopidogrel＂ with the following： ＂acute coronary syndrome＂ ＂percutaneous coronary intervention＂ We conducted a meta-analysis of randomized double-blind trials that evaluated clinical outcomes in patients with acute coronary syndrome. Two reviewers independently assessed the trials. Differences were resolved by consensus. Results A total of 2 trials with 14512 patients were available for analysis. Overall, prasugrel appeared significantly superior to clopidogrel for the risk of MACE （OR = 0.820.74-0.90, P ﹤0.0001）, stent thrombosis （OR = 0.470.35-0.62, P 0.00001）, death（OR = 0.850.78-0.93, P = 0.0003）, and myocardial infarction （OR = 0.760.68-0.85, P﹤0.00001）, without any significant difference in stroke （P = 0.85）. However, major bleeding associated with non coronary artery bypass grafting Thrombolysis in Myocardial Infarction related to prasugrel （OR = 1.321.03-1.67, P = 0.03）. Conclusions Prasugrel is superior to clopidogrel for acute coronary syndrome, while causing more bleedings.展开更多
The authors report the first case of thrombolysis in a patient already receiving both aspirin and prasugrel following a recent ischemic coronary event. A 55-year-old gentleman was treated for inferior wall myocardial ...The authors report the first case of thrombolysis in a patient already receiving both aspirin and prasugrel following a recent ischemic coronary event. A 55-year-old gentleman was treated for inferior wall myocardial infarction with aspirin, prasugrel and percutaneous angioplasty of right coronary artery. Three days following the procedure he developed acute ischemic stroke due to a left middle cerebral artery infarction with a National Institute of Health Stroke Scale (NIHSS) of 24 and was treated with alteplase. Therapy was interrupted after completion of 29 mg (for a body weight of 65 kg) dose due to oral bleeding. Fifteen minutes post thrombolysis NIHSS was 5 and dropped to zero after 12 h. This report highlights the benefits of alteplase in the context of several relative contraindications like the setting of acute myocardial infarction treated with percutaneous intervention and high NIHSS.展开更多
目的:系统评价替格瑞洛对比普拉格雷对血小板反应性的影响,以为临床治疗提供循证参考。方法:计算机检索Pub Med、中国期刊全文数据库和万方数据库,收集替格瑞洛对比普拉格雷对血小板反应性影响的随机对照试验(RCT)和对照试验,对符合纳...目的:系统评价替格瑞洛对比普拉格雷对血小板反应性的影响,以为临床治疗提供循证参考。方法:计算机检索Pub Med、中国期刊全文数据库和万方数据库,收集替格瑞洛对比普拉格雷对血小板反应性影响的随机对照试验(RCT)和对照试验,对符合纳入标准的临床研究进行资料提取,并采用Cochrane系统评价员手册5.1.0进行质量评价,再采用Rev man 5.1统计软件进行Meta分析。结果:共纳入17项RCT,合计2 757例患者。Meta分析结果显示,负荷剂量下,无论采用Verify Now P2Y12(VN)检测法[MD=15.43,95%CI(-0.39,31.25),P=0.06]或血管扩张刺激磷酸蛋白(VASP)检测法[MD=-3.04,95%CI(-8.98,2.90),P=0.32],替格瑞洛与普拉格雷对血小板反应性的效果相当,两组比较差异均无统计学意义;维持剂量下,无论采用VN检测法[MD=-48.94,95%CI(-58.04,-39.84),P<0.001]或VASP检测法[MD=-14.32,95%CI(-20.45,-8.20),P<0.001],替格瑞洛对血小板反应性的效果均优于普拉格雷,两组比较差异均有统计学意义。结论:在初期负荷剂量使用抗血小板药物时,选用替格瑞洛或普拉格雷对血小板反应性的影响没有显著差异,而后期维持剂量使用抗血小板药物时,替格瑞洛对血小板反应性的效果优于普拉格雷。展开更多
Antiplatelet therapy with aspirin or clopidogrel or both is the standard care for patients with proven coronary or peripheral arterial disease,especially those undergoing endovascular revascularization procedures. How...Antiplatelet therapy with aspirin or clopidogrel or both is the standard care for patients with proven coronary or peripheral arterial disease,especially those undergoing endovascular revascularization procedures. However,despite the administration of the antiplatelet regiments,some patients still experience recurrent cardiovascular ischemic events. So far,it is well documented by several studies that in vitro response of platelets may be extremely variable. Poor antiplatelet effect of clopidogrel or high on-treatment platelet reactivity(HTPR) is under investigation by numerous recent studies. This review article focuses on methods used for the ex vivo evaluation of HTPR,as well as on the possible underlying mechanisms and the clinical consequences of this entity. Alternative therapeutic options and future directions are also addressed.展开更多
文摘Clopidogrel is a mainstay in the treatment of patients with acute coronary syndromes or those receiving endovascular prostheses.However,its efficacy has been challenged in the recent past by studies suggesting variable individual responsiveness and by new,more potent competitors,such as prasugrel and ticagrelor. But what is the actual body of evidence in support of clopidogrel?Is there any dark side of the moon?What is the role of prasugrel,which has already been approved in Europe and in the United States?And what will be the future role of ticagrelor,when approved for routine clinical practice?We hereby concisely summarize the scope of this clinical choice,providing arguments in favor and against each of the three antiplatelet agents:clopidogrel,prasugrel,and ticagrelor.
文摘Aim To evaluate the time-effect and dose-effect of prasugrel hydrobromide acetic acid compound （PHAAC） inhibiting platelet aggregation. Methods For the time-effect study, 190 Sprague-Dawley （SD） rats were devided into 19 groups （n- 10）： the vehicle control group, the PHAAC groups （0.5, 1, 2, 4, 6, 24, 48, 72, 96 h） and the prasugrel hydrochloride groups （0.5, 1, 2, 4, 6, 24, 48, 72, 96 h）. Rats were singly intra- gastic administration of the vehicle, the PHAAC （5 mg·kg^-1） or the prasugrel hydrochloride （5 mg · kg^-1 ）, re- spectively. Blood samples were taken at each time point for the determination of platelet aggregation rate （PAR）. For the dose-effect study, 110 SD rats were devided into 11 groups （n= 10）： the vehicle control group, the PHAAC groups （10, 5, 2.5, 1, 0.5 mg · kg^-1, dosage of prasugrel） and the prasugrel hydrochloride groups （ 10, 5, 2.5, 1, 0.5 mg · kg^-1, dosage of prasugrel） . Blood samples were taken at 4 h after drug administration for the determination of PAR. Results Compared with the vehicle group, PHAAC has significant anti-platelet ag- gregative effects （P 〈 0.05） at the time of 0.5, 1, 2, 4, 6, 24, 48 h, and the effect at the time of 4 h was the strongest. There were no obvious differences between the effect of PHAAC （5 mg · kg^-1） and prasugrel hydrochlo- ride （5 mg · kg^-1） at each time point. Compared with the vehicle group, intragastic administration of PHAAC at the doses of 10, 5, 2.5, 1, 0.5 mg · kg^-1 could obviously inhibite the platelet aggregation, and showed a dose- dependent manner. There were no significant differences between the effect of PHAAC and prasugrel hydrochloride at the same dose. Conclusion PHAAC can inhibit platelet aggregation in a dose-dependent manner, and the effect at 4 h after drug administration is the strongest. The action strength and duration of PHAAC are similar with that of the prasugrel hydrochloride.
文摘Dual antiplatelet therapy consisting of low-dose aspirin (LDA) and other antiplatelet medications is recommended in patients with coronary heart disease, but it may increase the risk of esophageal lesion and bleeding. We describe a case of esophageal mucosal lesion that was difficult to distinguish from malignancy in a patient with a history of ingesting LDA and prasugrel after implantation of a drug-eluting stent. Multiple auxiliary examinations were performed to make a definite diagnosis. The patient recovered completely after concomitant acid-suppressive therapy. Based on these findings, we strongly argue for the evaluation of the risk of gastrointestinal mucosal injury and hemorrhage if LDA therapy is required, and we stress the paramount importance of using drug combinations in individual patients.
文摘Background Clopidogrel is beneficial after acute coronary syndrome. Recent studies suggest the superiority of prasugrel compared with clopidogrel. The enhanced platelet inhibition with prasugrel lead to a reduction in major adverse cardiovascular events in patients with moderate to high risk acute coronary syndrome scheduled for PCI. However, prasugrel showed signs of increased bleeding potential. We performed a meta-analysis to assess clinical safety and efficacy of prasugrel in patients with acute coronary syndrome. Methods We systematically searched PubMed, ISI Web of Knowledge, Cochrane Central Register of Controlled Trials, clinicaltrials. gov, proceedings of major US and European cardiology meetings, China National Knowledge Infrastructure （CNKI） databases 2000-2010 and reviews, reference lists of relevant articles. The search strategy paired the term ＂prasugrel＂ ＂clopidogrel＂ with the following： ＂acute coronary syndrome＂ ＂percutaneous coronary intervention＂ We conducted a meta-analysis of randomized double-blind trials that evaluated clinical outcomes in patients with acute coronary syndrome. Two reviewers independently assessed the trials. Differences were resolved by consensus. Results A total of 2 trials with 14512 patients were available for analysis. Overall, prasugrel appeared significantly superior to clopidogrel for the risk of MACE （OR = 0.820.74-0.90, P ﹤0.0001）, stent thrombosis （OR = 0.470.35-0.62, P 0.00001）, death（OR = 0.850.78-0.93, P = 0.0003）, and myocardial infarction （OR = 0.760.68-0.85, P﹤0.00001）, without any significant difference in stroke （P = 0.85）. However, major bleeding associated with non coronary artery bypass grafting Thrombolysis in Myocardial Infarction related to prasugrel （OR = 1.321.03-1.67, P = 0.03）. Conclusions Prasugrel is superior to clopidogrel for acute coronary syndrome, while causing more bleedings.
文摘The authors report the first case of thrombolysis in a patient already receiving both aspirin and prasugrel following a recent ischemic coronary event. A 55-year-old gentleman was treated for inferior wall myocardial infarction with aspirin, prasugrel and percutaneous angioplasty of right coronary artery. Three days following the procedure he developed acute ischemic stroke due to a left middle cerebral artery infarction with a National Institute of Health Stroke Scale (NIHSS) of 24 and was treated with alteplase. Therapy was interrupted after completion of 29 mg (for a body weight of 65 kg) dose due to oral bleeding. Fifteen minutes post thrombolysis NIHSS was 5 and dropped to zero after 12 h. This report highlights the benefits of alteplase in the context of several relative contraindications like the setting of acute myocardial infarction treated with percutaneous intervention and high NIHSS.
文摘目的:系统评价替格瑞洛对比普拉格雷对血小板反应性的影响,以为临床治疗提供循证参考。方法:计算机检索Pub Med、中国期刊全文数据库和万方数据库,收集替格瑞洛对比普拉格雷对血小板反应性影响的随机对照试验(RCT)和对照试验,对符合纳入标准的临床研究进行资料提取,并采用Cochrane系统评价员手册5.1.0进行质量评价,再采用Rev man 5.1统计软件进行Meta分析。结果:共纳入17项RCT,合计2 757例患者。Meta分析结果显示,负荷剂量下,无论采用Verify Now P2Y12(VN)检测法[MD=15.43,95%CI(-0.39,31.25),P=0.06]或血管扩张刺激磷酸蛋白(VASP)检测法[MD=-3.04,95%CI(-8.98,2.90),P=0.32],替格瑞洛与普拉格雷对血小板反应性的效果相当,两组比较差异均无统计学意义;维持剂量下,无论采用VN检测法[MD=-48.94,95%CI(-58.04,-39.84),P<0.001]或VASP检测法[MD=-14.32,95%CI(-20.45,-8.20),P<0.001],替格瑞洛对血小板反应性的效果均优于普拉格雷,两组比较差异均有统计学意义。结论:在初期负荷剂量使用抗血小板药物时,选用替格瑞洛或普拉格雷对血小板反应性的影响没有显著差异,而后期维持剂量使用抗血小板药物时,替格瑞洛对血小板反应性的效果优于普拉格雷。
文摘Antiplatelet therapy with aspirin or clopidogrel or both is the standard care for patients with proven coronary or peripheral arterial disease,especially those undergoing endovascular revascularization procedures. However,despite the administration of the antiplatelet regiments,some patients still experience recurrent cardiovascular ischemic events. So far,it is well documented by several studies that in vitro response of platelets may be extremely variable. Poor antiplatelet effect of clopidogrel or high on-treatment platelet reactivity(HTPR) is under investigation by numerous recent studies. This review article focuses on methods used for the ex vivo evaluation of HTPR,as well as on the possible underlying mechanisms and the clinical consequences of this entity. Alternative therapeutic options and future directions are also addressed.
