急性冠脉综合征抗血小板xx进展
关于急性冠脉综合征(ACS)抗血小板xx,以下10点需要记住:
1、阿司匹林和氯吡格雷(clopidogrel)双重抗血小板xx已被证明在许多情况下能够降低心血管事件。
2、为了进一步改善预后导致人们去研制更有力的抗血小板xx,但是代价是增加出血并发症。
3、寻找具有{zj0}缺血保护和可接受的出血风险的抗血小板xx仍然是抗血小板xx发展的最主要的方面。
4、普拉格雷(Prasugrel)是一种新的和更有效的噻吩并吡啶类xx。与氯吡格雷相似,不可逆转地结合并阻断ADP P2Y12受体。它比氯吡格雷显效更快,抑制作用更强。
5、替卡格雷(Ticagrelor)是一种口服活性xx,与P2Y12受体结合。不象氯吡格雷和普拉格雷,它不是一个噻吩并吡啶类xx,相反,它是一类新的抗血小板制剂,为环戊基三唑并嘧啶类化合物。更重要的是,它与P2Y12受体的结合是可逆的。与先前的试剂不同,它并不需要经过代谢转换或经过肝脏xx,本身就是活性形式。
6、氯吡格雷是{wy}的已经被批准用于非ST段抬高ACS患者xxxx的P2Y12拮抗剂。在P2Y12受体拮抗剂中,它好像也是具有{zj0}安全性的一种。因此,对于出血风险高危的患者(如老年人、低体重、短暂性脑缺血发作或卒中病史者)进行xx或介入xx时,应考虑选择性用氯吡格雷。
7、普拉格雷,因为其起效更快,STEMI直接PCI时应该{sx},因为这些患者进行氯吡格雷负荷的时间窗短,或者是尽管氯吡格雷xx,但患者仍持续有复发缺血事件,特别是支架内血栓形成。(所谓氯吡格雷抵抗患者)。
8、血栓事件高危的糖尿病患者,普拉格雷可能会提供更好的效果(尽管事后分析得出结论这个证据基础不强大)。
9、由于其可逆性抑制血小板的特性,对于冠脉解剖未知和/或紧急冠脉搭桥术不能推迟的患者,替卡格雷应该是{sx}。 对于急性严重呼吸困难或有严重呼吸困难/慢性阻塞性肺病、高尿酸血症、中至重度肾功能不全病史以及缓慢性心律失常且没有心脏起搏器保护的患者,不鼓励使用替卡格雷,或应小心使用。
10、普拉格雷和替卡格雷与氯吡格雷相比,有改善缺血性的益处。这些益处的代价就是出血增加。因此,仔细选择患者,权衡利弊,以{zy}化其临床应用。
【Date Posted: 5/28/2010; Author(s): Eshaghian S, Shah PK, Kaul S.;Heart 2010;96:656-661.】
Advances in Antiplatelet Treatment for Acute Coronary Syndromes
Perspective: The following are 10 points to remember about antiplatelet treatment for acute coronary syndromes (ACS).
1. Dual antiplatelet inhibition with aspirin and clopidogrel has
been shown to result in a reduction in cardiovascular events in a
variety of settings.
2. Attempts to improve outcomes further have led to the development of more potent antiplatelet agents, but at a cost of increased bleeding complications.
3. The search for an
antiplatelet agent with optimal ischemic protection and an
acceptable bleeding risk remains the holy grail of antiplatelet
drug development.
4. Prasugrel is a new and
more potent thienopyridine. Similar to clopidogrel, it irreversibly
binds and blocks the ADP P2Y12 receptor. It has a more rapid onset
of action and a stronger inhibitory effect than
clopidogrel.
5. Ticagrelor is an orally
active drug that binds the P2Y12 receptor. Unlike clopidogrel and
prasugrel, it is not a thienopyridine; rather, it is a new class of
antiplatelet agent termed cyclopentyl-triazolo-pyrimidine.?More importantly, its
binding to the P2Y12 receptor is reversible. Distinct from previous
agents, it does not require metabolic conversion or hepatic
activation to an active form.
6. Clopidogrel is the only
P2Y12 antagonist that has been approved for the medical management
of patients with non-ST-elevation ACS. It also appears to have the
best safety profile among the P2Y12 antagonists. Therefore,
clopidogrel should be considered the treatment of choice in
patients at high risk of bleeding (elderly, low body weight,
history of transient ischemic attack or strokes) undergoing medical
or invasive therapy.
7. Prasugrel, because of its
faster onset of action, should be the preferred agent in patients
with ST-elevation myocardial infarction undergoing primary
percutaneous coronary intervention because of short time window to
preload clopidogrel in these patients, or in patients who continue
to have recurrent ischemic events, particularly stent thrombosis,
despite treatment with clopidogrel (so-called clopidogrel-resistant patients).
8. Another group of patients
in whom prasugrel might provide superior efficacy are patients with
diabetes who are at high risk of thrombotic events (although the
evidence base is not robust, as it is derived from a post-hoc
analysis).
9. As a result of its
reversible nature of platelet inhibition, ticagrelor should be the
preferred agent in patients in whom coronary anatomy is unknown
and/or urgent coronary artery bypass grafting cannot be deferred.
Ticagrelor should be discouraged or used cautiously in patients who
develop acute severe
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