Department of Neurology and Stroke Center, University Duisburg-Essen, Essen, Germany.
J Cell Mol Med. 2010 Oct;14(10):2371-80. doi: 10.1111/j.1582-4934.2010.01162.x.
Antiplatelet agents are a cornerstone in the treatment of acute arterial thrombotic events and in the prevention of thrombus formation. However, existing antiplatelet agents (mainly aspirin, the combination of aspirin and dipyridamole and clopidogrel) reduce the risk of vascular events only by about one quarter compared with placebo. As a consequence, more efficacious antiplatelet therapies with a reduced bleeding risk are needed. We give an overview of several new antiplatelet agents that are currently investigated in secondary stroke prevention: adenosine 5'-diphosphonate receptor antagonists, cilostazol, sarpogrelate, terutroban and SCH 530348. There are unique features in secondary stroke prevention that have to be taken into account: ischaemic stroke is a heterogeneous disease caused by multiple aetiologies and the blood-brain barrier is disturbed after stroke which may result in a higher intracerebral bleeding risk. Several small randomized trials indicated that the combination of aspirin and clopidogrel might be superior to antiplatelet monotherapy in the acute and early post-ischaemic phase. There is an ongoing debate about antiplatelet resistance. Decreasing response to aspirin is correlated independently with an increased risk of cardiovascular events. However, there is still no evidence from randomized trials linking aspirin resistance and recurrent ischaemic events. Similarly, randomized trials have not demonstrated a clinical significantly decreased antiplatelet effect by the concomitant use of clopidogrel and proton pump inhibitors. Nevertheless, a routine use of this drug combination is not recommended.
抗血小板药物是治疗急性动脉血栓栓塞事件和预防血栓形成的基石。然而，现有的抗血小板药物（主要是阿司匹林、阿司匹林和双嘧达莫联合用药以及氯吡格雷）与安慰剂相比，仅将血管事件的风险降低了约四分之一。因此，需要更有效的、出血风险更低的抗血小板治疗方法。我们概述了几种目前正在进行二级卒中预防研究的新型抗血小板药物：腺苷 5′-二磷酸受体拮抗剂、西洛他唑、沙格雷酯、替罗非班和 SCH 530348。二级卒中预防具有一些独特的特征需要考虑：缺血性卒中是一种由多种病因引起的异质性疾病，并且卒中后血脑屏障受到干扰，这可能导致颅内出血风险增加。几项小型随机试验表明，在急性和缺血后早期阶段，阿司匹林和氯吡格雷联合用药可能优于抗血小板单药治疗。目前仍在争论抗血小板抵抗的问题。对阿司匹林反应降低与心血管事件风险增加独立相关。然而，随机试验仍没有证据表明阿司匹林抵抗与复发性缺血事件有关。同样，随机试验也没有证明氯吡格雷和质子泵抑制剂同时使用会显著降低抗血小板作用。尽管如此，不推荐常规使用这种药物联合治疗。
