Antiplatelet Drug Resistance

Platelet activation plays an important role in arteried thrombosis. Therefore, several million individuals worldwide take antiiplatelet drugs, including aspirin or clopidogrel.     

围术期的抗血小板治疗

心血管病患者需不中断地终生使用阿司匹林.植入裸金属支架后6周、心肌梗死后3～6个月及植入药物洗脱支架后至少12个月必须使用氯吡格雷(Clopidogrel)治疗.持续用双联抗血小板治疗的支架植入患者,由于手术导致的易凝状态,早期停用用作心血管病二级预防的抗血小板治疗,使术后心肌梗死及死亡风险增加5～10倍.血运重建与手术间隔时间越短,严重心脏事件发生的风险就越高.择期手术应迟于这些时段,挽救生命的、半紧急或紧急手术需在连续使用双联抗血小板治疗的情况下完成.单用阿司匹林或氯吡格雷使手术出血风险增加约20%,而双联抗血小板治疗使手术出血风险增加约50%.现有的临床数据提示,除了密闭腔(如颅内、眼后房)或大出血及止血困难的手术,围术期停用抗血小板药的心血管事件风险要高于继续使用这些药的手术出血风险[1].     

New Antiplatelet Drugs

ADP-receptor antagonistPrasugrel is a thienopyridine of the third generation and needs conversion into an active drug metabolite(R-138727).Preclinical and clinical studies showed a more rapid,potent and consistent inhibition of patelet function for prasugrel compared to clopidogrel.Prasugrel has been shown to be of particular benefit in patients with diabetes,especially those on insulin [30% rel     

Advances in Antiplatelet Therapy

Platelets play a central role in hemostasis and throm- bosis but also in the initation of atherosclerosis making platelet receptors and there intracellular signaling path- ways important molecular targets for antithrombotic and anti-inflammatory therapy.Therapeutic targeting of plate- lets has two objectives:prevention of vessel occlusion and inhibition of the platelet contribution to lesion progres- sion.     

血小板功能检测及其临床应用

血小板检测方法可归纳为出血、血栓和药物监测3大类。虽则有些方法能应用于多种检测目的,但为特殊目的而创建的方法亦有重要价值。故在检测时应合理地运用。     

Antiplatelet use in interventional cardiology

Thrombosis within the target vessel is one of the most feared complications associated with coronary intervention, as it is often associated with severe adverse clinical sequelae. This thrombosis is mediated via the activation and aggregation of platelets and therefore considerable effort has been directed at ways of inhibiting platelet function. It is now mandatory to consider the use of two and often three different antiplatelet agents, particularly when intracoronary stents are inserted. Using these regimes, many of the adverse clinical outcomes associated with platelet activation can be reduced.     

Antiplatelet therapy in cardiovascular disease

Platelet activation and aggregation are considered to be central to arterial thrombus formation. Antiplatelet therapy is therefore important for both the treatment and prevention of cardiovascular disease. Aspirin, the most widely used antiplatelet agent, inhibits platelet cyclo-oxygenase and the conversion of arachidonic acid to the potent platelet agonist thromboxane A(2) but does not prevent platelet activation occurring via various signalling pathways that are independent of thromboxane A(2) release. Therefore a number of other compounds have been developed to complement aspirin's beneficial effect. These include the thienopyridines (clopidogrel and ticlopidine), dipyridamole, and the alpha(IIb)beta(3) (glycoprotein IIb/IIIa) receptor inhibitors.     

抗血小板药物抵抗的研究进展

抗血小板药物从20世纪60年代问世一直应用至今,是治疗心血管疾病、预防血栓事件的主要手段。随着药物的广泛应用,人们发现,部分接受抗血小板药物治疗的患者仍然发生血栓事件,被称为"抗血小板药物抵抗"。这一现象与药物的剂量、药物间的相互作用、基因的多态性、基础血小板的反应性、药物吸收的个体差异、患者依从性等多个因素密切相关。联合使用药物或加大剂量是目前最主要应对药物抵抗的措施,但也增加了出血并发症的危险。     

Bleeding Complications in Antiplatelet Therapy

Antipatelet therapy paly a vital role in preventing atherothrombotic events in patients with coronary artery disease and in those underging revascularization procedures.How,the therapy may occur at the expense of increase risk of bleeding.With a stronger antiplatelet treatment in clinical application,the risk of bleeding causedby antiplatelet agents has become a new and important     

血管紧张素转换酶抑制剂抗血小板作用的研究

目的评估心血管病患者在分别接受血管紧张素转换酶抑制剂（ACEI）、阿司匹林、氯吡格雷加阿司匹林或不用上述药物时血小板的凝血活性。方法对303例心血管病患者进行全血血小板聚集功能测定。血小板聚集功能（Pag）由血小板对聚集剂ADP或胶原产生反应，通过电极的阻抗增加判定。结果在ACEI、阿司匹林、阿司匹林加氯吡格雷组Pag减弱，表现为与非治疗组相比有较低的阻抗增加。ACEI组，ADP介导的Pag下降33％（P=0．041）；阿司匹林组未见到有意义的抗血栓形成作用（17％，P=1．0）；阿司匹林加氯吡格雷组下降85％（P=0．001）。胶原介导的Pag在ACEI组下降16％（P=0．018）；在阿司匹林组和阿司匹林加氯吡格雷组分别下降23％（P=0．004）和35％（P=0．016）。结论ACEI降低Pag；阿司匹林加氯吡格雷有确切的抗血栓作用。ACEI对血小板的作用可能是该类药物在临床心血管病试验主要终点获益的原因。     

新型抗血小板药物的研究进展

我国人口逐步老龄化,动脉硬化性血栓相关疾病是致死和致残的关键原因,特别是心血管疾病,其中脑卒中的危害亦逐年增加。动脉粥样硬化性卒中的发病原因为细胞因素,故抗血小板治疗为关键,是缺血性卒中二级预防及治疗的基石。环加氧酶Ⅰ受体抑制剂阿司匹林及噻吩吡啶类P2Y12受体拮抗剂氯吡格雷是临床上常用的抗血小板药物,但各有缺陷,且阿司匹林抗血小板作用相对较弱;氯吡格雷为前体药物,起效慢,而且疗效受多种药物影响,导致不同患者对药物的反应存在差异性。因此降低出血风险及提高疗效是研发新型抗血小板药物的目标。     

Antiplatelet Effects and Mechanisms of Berberine

ＡｎｔｉｐｌａｔｅｌｅｔＥｆｆｅｃｔｓａｎｄＭｅｃｈａｎｉｓｍｓｏｆＢｅｒｂｅｒｉｎｅＣＨＵＺｈｏｎｇ－ｌｕ（储钟禄）；ＨＵＡＮＧＣａｉ－ｇｕｏ（黄才国）ａｎｄＸＵＺｈｉ－ｐｉｎｇ（徐志平）（ＳｅｃｏｎｄＭｉｌｉｔａｒｙＭｅｄｉｃａｌＵｎｉｖｅｒｓｉ...     

瓜蒌的抗血小板聚集活性成分研究

目的研究瓜蒌的抗血小板聚集活性成分。方法利用抗血小板聚集的活性追踪方法，采用Sephadex LH-20柱色谱、反复硅胶柱色谱分离，通过IR、^1H—NMR、^13C-NMR、MS等波谱分析手段研究化学结构。结果分离得到7个化合物，分别鉴定为棕榈酸(Ⅰ)，5，5‘-双氧甲基呋喃醛(Ⅱ)，N-苯基苯二甲酰亚胺(Ⅲ)，4-羟基-2-甲氧基苯甲酸(Ⅳ)，4-羟基-烟酸(Ⅴ)，香叶木素-7-O-β-D-葡萄糖苷(Ⅵ)，腺苷(Ⅶ)。结论化合物Ⅳ、Ⅵ、Ⅵ均具有很强的抗血小板聚集作用，化合物Ⅲ为首次从植物中分离得到的天然产物，化合物Ⅴ～Ⅵ为首次从该属植物中分离获得，化合物Ⅱ、Ⅳ为首次从该种植物中分离得到。     

抗血小板类抗血栓药物的研究进展

抗血小板治疗是抗凝血治疗的重要方法,在治疗心脑血管凝血性疾病中占有重要地位,该文对近年来抗血小板类抗凝血药物的开发研究进展进行综述,旨在为我国新型抗血栓药物的研发,以及在临床上科学、安全的使用抗血栓药物提供一定价值的借鉴.     

Antiplatelet aggregation effect of Andregraphis paniculata

This article deals with the antiplatelet aggregation effect of Andregraphis paniculata (AP), 61 blood samples and 8 volunteers were investigated to observe the effect of AP on platelet function in vitro and in vivo respectively. The results showed that the crude extract of AP could inhibit significantly one-phase and two-phase platelet aggregation induced by ADP (P less than 0.001, 0.01). The potency of AP crude extract seemed to be somewhat stronger than Ligustrazine and Persantin injection in vitro, but the difference was not statistically significant (P greater than 0.05). A dose-effect relationship of AP was demonstrated also (r = 0.93). The rapid effect of this drug on platelet aggregation in vivo suggested that AP could be absorbed quickly, but the effect lasted for only a short time. 12 hours after with-drawing of AP, the 1 minute and 5 minutes aggregation rates increased by 18.67%, 36.63% respectively, as compared with the lowest aggregation rate after administration. The activating effect of AP on fibrinolysis was also detected by shortened euglobulinlysis time (211.50 vs 182.50 min in vitro, 219.38 vs 149.38 min in vivo, P less than 0.001). In addition, the influence of AP upon coagulation and thrombelastogram was determined. This study suggested that AP in a promising antithrombogenic agent. This drug might be beneficial in preventing and treating arterial thrombotic diseases.     

急性冠状动脉综合征抗血小板和抗凝治疗

急性冠状动脉综合征(ACS)包括非ST段抬高的ACS(主要为不稳定性心绞痛和非Q波心肌梗死)和ST段抬高的ACS(Q波心肌梗死)以及心源性猝死。其共同的发病机制是斑块破裂,     

经皮冠状动脉介入治疗术后抗血小板治疗依从性调查分析

目的 分析经皮冠状动脉介入治疗(PCI)术后抗血小板治疗依从性的现状、影响因素和对策.方法 采用回顾性方法,调查和分析患者接受PCI后抗血小板治疗的用药情况及其影响因素.结果 187例PCI术后患者,双重抗血小板依从性好的在术后3个月占89.9%,术后1年降至82.3%.药品副作用、患者的用药知识、对冠心病的了解及医师指导等因素是影响患者用药依从性的主要因素.结论 PCI术后抗血小板药物治疗依从性不理想,药师和医师应共同肩负起提高术后二级预防用药依从性的重任.     

Antiplatelet therapy in non-ST-segment elevation acute coronary syndromes

Acute coronary syndromes are a frequent cause of hospital admission for patients with coronary artery disease. The pathophysiology of acute coronary syndromes often involves plaque rupture or fissure with platelet aggregation. Recognition of the importance of platelet aggregation resulted in several large randomized trials testing 3 types of platelet antagonists, aspirin, glycoprotein IIb/IIIa inhibitors, and adenosine diphosphate inhibitors. A thorough understanding of the data, risks, and benefits of these therapies is important to optimize treatment of the patient with an acute coronary syndrome. Recognition that there is a great deal of interpatient variability in response to these antiplatelet therapies highlights the need for future research in this area.