Antiplatelet and Anticoagulant Therapy for Atherothrombotic Disease: The Role of Current and Emerging Agents

Coronary atherothrombotic disease, including chronic stable angina and acute coronary syndromes (ACS), is associated with significant global burden. The acute clinical manifestations of atherothrombotic disease are mediated by occlusive arterial thrombi that impair tissue perfusion and are composed of a core of aggregated platelets, generated by platelet activation, and a superimposed fibrin mesh produced by the coagulation cascade. Long-term antithrombotic therapies, namely oral antiplatelet agents and anticoagulants, have demonstrated variable clinical effects. Aspirin and P2Y₁₂ adenosine diphosphate (ADP) receptor antagonists have been shown to reduce the risk for thrombosis and ischaemic events by blocking the thromboxane (Tx) A₂ and platelet P2Y₁₂ activation pathways, respectively, whereas the benefits of oral anticoagulants have not been consistently documented. However, even in the presence of aspirin and a P2Y₁₂ receptor antagonist, the risk for ischaemic events remains substantial because platelet activation continues via pathways independent of TxA₂ and ADP, most notably the protease-activated receptor (PAR)-1 platelet activation pathway stimulated by thrombin. Emerging antithrombotic therapies include those targeting the platelet, such as the new P2Y₁₂ antagonists and a novel class of oral PAR-1 antagonists, and those inhibiting the coagulation cascade, such as the new direct factor Xa antagonists, the direct thrombin inhibitors, and a novel class of factor IX inhibitors. The role of emerging antiplatelet agents and anticoagulants in the long-term management of patients with atherothrombotic disease will be determined by the balance of efficacy and safety in large ongoing clinical trials.     

Oral Antiplatelet Therapy in the Secondary Prevention of Atherothrombotic Events

Atherothrombosis is the leading cause of death worldwide and has a large economic impact. It is a pathologic process related to atherosclerosis, which leads to adverse clinical manifestations, including acute coronary syndrome, cerebrovascular disease, and peripheral arterial disease. Patients with atherothrombosis are at heightened risk for recurrent ischemic events or death, and therefore, secondary prevention is an important goal in the treatment of these patients. Antiplatelet therapies available for long-term secondary prevention include aspirin (acetylsalicylic acid), extended-release dipyridamole plus aspirin, and clopidogrel. A number of clinical trials have demonstrated the benefit of combined antiplatelet therapy in secondary prevention, supporting the recommendations made in current published guidelines. Although the efficacy and safety of antiplatelet agents is well established and supported by clinical trials, their utilization rate in patients with atherothrombosis remains suboptimal. Quality improvement initiatives have demonstrated effectiveness in promoting the awareness and implementation of treatment guidelines. This article reviews the benefits and risks of antiplatelet therapy in patients with cardiovascular disease with the aim of spurring greater adherence to treatment recommendations and, thereby, better patient outcomes.     

Antiplatelet Agents for the Prevention of Cardiovascular Disease in Diabetes Mellitus

Patients with diabetes mellitus (DM) have accelerated atherothrombotic disease of coronary, cerebral, leg, and other vessels. The major cause of death is cardiovascular, and the risk for a myocardial infarction (MI) in a patient with DM who has never had a MI is the same as a nondiabetic individual who has already had one. In this paper, we review the major reasons for a prothrombotic state in patients with DM: alterations in the intrinsic coagulation and fibrinolytic systems and many abnormalities of platelet function. Increased platelet thromboxane production as well as activation of platelet receptors for fibrinogen and or adenosine diphosphate (ADP) are often present, and can be treated with aspirin (acetylsalicylic acid) and/or receptor blockers. Review of the major primary prevention trials in DM indicates that a significantly reduced risk for MI or major cardiovascular events may be obtained by enteric-coated aspirin, 81–325 mg/day. There is emerging consensus that this is recommended strategy in adult (aged >30 years) patients with DM who are at high vascular risk. Surveys suggest that this includes virtually every patient with type 2 DM in the US, as well as many patients with complicated type 1 DM. These recommendations are also appropriate for secondary prevention. Data supporting the use of clopidogrel as an alternative drug in the case of aspirin allergy or other contraindications are reviewed. Evidence is presented in support of using aspirin plus clopidogrel in acute coronary syndromes (ACS), and a meta-analysis of six trials of platelet glycoprotein (GP) IIb/IIIa inhibitors and aspirin in diabetic patients with ACS establishes this regimen as an effective choice. Although bleeding episodes are more common with combined antiplatelet therapy for ACS than for aspirin alone, the benefit of a significant reduction in 30-day mortality appears to outweigh the risk of major bleeding. It is concluded that major advances in our understanding of the prothrombotic state in DM have been made. Evidence from controlled clinical trials supports the use of enteric-coated aspirin, 81–325 mg/day, as a primary and a secondary prevention strategy in adults with DM with high vascular risk. In ACS, combination therapy with aspirin plus clopidogrel or alternatively, aspirin plus a platelet GP IIb/IIIa inhibitor is supported by prospective trial data. These approaches should be added to the other multifactorial preventive strategies directed at lowering the risk for major vascular events in patients with DM.     

抗血小板药物研究进展

近年来心脑血管疾病对人类健康已造成严重威胁,因而开发安全有效、价格低廉的抗血栓、抗血小板及抗凝血药已成当务之急。阿司匹林与氯吡格雷是目前抗血小板治疗的标准组合。但两药合用导致的出血发生率增加、以及日益受到关注的阿司匹林和氯吡格雷抵抗等问题,使得现有抗血小板治疗难以满足临床需要。本文从ADP受体抑制剂、凝血酶受体抑制剂、5-羟色胺受体抑制剂这四方面综述了近年来新的抗血小板药物的研究进展。     

Antiplatelet Agents in Patients Undergoing Percutaneous Coronary Intervention

Antiplatelet agents play a major role in patients undergoing percutaneous coronary intervention (PCI). Stent thrombosis and the demand for improved clinical outcomes have driven the need for aggressive antiplatelet and anticoagulant regimens and newer, more efficacious, therapies. The benefits of intravenous glycoprotein (GP) IIb/IIIa antagonists and clopidogrel in high-risk patients undergoing PCI appear complementary. In low- to intermediate-risk patients, clopidogrel pre-treatment and a maintenance dose of aspirin + clopidogrel for at least 1 year after PCI are supported by the data, although the optimal duration of clopidogrel treatment beyond 1 year remains hotly contested. The next generation of clinical trials will examine the benefits of antiplatelet and antithrombotic agents as adjunctive therapy with drug-eluting stents. A better understanding of our patients' overall risk will add to procedural success and more durable outcomes.     

口服抗血小板药物在冠心病52例治疗中的临床分析

目的:探讨口服不同的抗血小板药物治疗冠心病的临床效果。方法:选择某院2013年12月~2014年12月期间收治的冠心病患者共52例作为研究对象,并按数字表法随机分为两组。对照组患者(n=25)给予阿司匹林联合氟吡格雷进行治疗,而观察组患者则(n=27)给予阿司匹林联合普拉格雷进行治疗,观察两组患者治疗前后的血小板指标变化,比较两组治疗后的不良反应及临床事件发生情况差异。结果:治疗前两组患者的平均血小板聚集率(MPA)和平均血小板反应指数(PRI)差异均无统计学意义(P0.05),而治疗后两组的MPA和PRI均明显下降,并以观察组的降低程度更高;并且,观察组治疗后的不良反应发生率仅为7.41%(2/27),显著低于对照组的36.00%(9/25);而观察组的不良临床事件发生比率也较对照组低,两组间差异比较均具有统计学意义(P0.05)。结论:普拉格雷应用于冠心病的辅助治疗中,可有效发挥抗血小板作用,其效果要显著优于氟吡格雷辅助治疗,具有更较高的安全性,值得在临床上推广使用。     

家长口腔健康素养在学生牙病防治中的作用分析

目的:分析家长口腔健康素养在学生牙病防治中的作用。方法:于2013年5月~2015年5月期间选取当地同一所学校同一年级的300例学生作为研究对象,随机分成对照组和观察组,每组150例学生。对照组不对家长进行口腔健康知识教育,观察组对家长进行口腔健康知识教育。结果:观察组学生及其家长的口腔健康知识知晓率均明显高于对照组(P0.05),观察组学生龋齿患病率明显低于对照组(P0.05)。结论:家长口腔健康素养在学生牙病防治中具有积极影响作用,有效减少学生牙病的发生。     

成都市口服避孕药的销售及使用情况调查

目的:了解口服避孕药(OC)的市场前景并普及其基本知识。方法:运用文献研究和实地调查、问卷调查方法收集数据,分析OC的销售及使用现状,了解主要消费人群对于OC的基本知识了解情况。结果与结论:OC的主要消费群体为18～29岁的青年人,主要使用种类为紧急避孕药;主要消费人群对OC了解不多,药政部门及生产企业应采取措施加强OC的基本知识普及。     

2008年我院口服降糖药应用分析

目的：了解我院口服降糖药使用现状及发展趋势。方法：对我院2008年口服降糖药的销售金额、用药频度（DDDs）、日均费用（DDC）等进行回顾性分析。结果：我院2008年口服降糖药销售金额排序前3位的是阿卡波糖、瑞格列奈、二甲双胍;DDDs排序前3位的是阿卡波糖、二甲双胍、瑞格列奈;二甲双胍的DDC最低。结论：我院口服降糖药应用基本合理,新药用量呈上升趋势,老药仍占据相当地位。     

执业药师在疾病管理中的作用

疾病管理可提高医疗的服务质量,减少不必要的医疗费用,执业药师在疾病管理尤其是慢病管理中可发挥重要作用。本文介绍了执业药师在疾病管理中的作用,并提出执业药师在慢病管理中的策略。     

口服降血糖药的研究进展与临床应用

目的为临床合理应用口服降血糖药提供参考。方法介绍口服降血糖药的研究进展,对几种新型口服降血糖药进行临床应用评价。结果与结论提出了几点合理应用口服降血糖药的建议。糖尿病为慢性疾病,其所致的各种并发症已成为患者致残和早死的主要原因,而目前所有治疗中口服降血糖药是主要手段,因此其合理应用显得尤为重要。     

Deuterated Clopidogrel Analogues as a New Generation of Antiplatelet Agents

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