Gallus A S
Drugs. 1979 Dec;18(6):439-77. doi: 10.2165/00003495-197918060-00002.
Because platelets are so important in thrombus formation, drugs which inhibit platelet function (the 'antiplatelet drugs') have considerable potential as antithrombotic agents. Among the antiplatelet drugs, only aspirin, sulphinpyrazone, dipyridamole, hydroxychloroquine, and clofibrate have had wide clinical trial. Their effects on platelet metabolism differ. Aspirin prevents platelet prostaglandin synthesis by acetylating and irreversibly inactivating platelet prostaglandin synthetase, while sulphinpyrazone is a reversible inhibitor of the same enzyme. Both aspirin and sulphinpyrazone impair the platelet release reaction and reduce platelet aggregation, but neither prevents platelet adhesion to the subendothelium or to foreign surfaces. On the other hand, dipyridamole reduces platelet adhesion as well as aggregation, probably by inhibiting phosphodiesterase and so raising platelet cyclic AMP levels. The effects of hydroxychloroquine and clofibrate have been less well defined. As the antiplatelet drugs form a diverse group of substances with differing effects on platelet function, it is hardly surprising that every potential clinical application of each antiplatelet drug or drug combination has had to be tested separately, and that these drugs have not proved to be equally effective. One or more antiplatelet drugs have now been evaluated in each of the following situations.
由于血小板在血栓形成中非常重要，抑制血小板功能的药物（“抗血小板药物”）作为抗血栓形成剂具有相当大的潜力。在抗血小板药物中，只有阿司匹林、磺吡酮、双嘧达莫、羟氯喹和氯贝丁酯进行过广泛的临床试验。它们对血小板代谢的影响各不相同。阿司匹林通过乙酰化并不可逆地使血小板前列腺素合成酶失活来阻止血小板前列腺素的合成，而磺吡酮是同一酶的可逆抑制剂。阿司匹林和磺吡酮都损害血小板释放反应并减少血小板聚集，但两者都不能阻止血小板黏附于内皮下或异物表面。另一方面，双嘧达莫可能通过抑制磷酸二酯酶从而提高血小板环磷酸腺苷水平来减少血小板黏附和聚集。羟氯喹和氯贝丁酯的作用还不太明确。由于抗血小板药物是一组对血小板功能有不同影响的多种物质，因此每种抗血小板药物或药物组合的每一种潜在临床应用都必须单独进行测试，而且这些药物并未被证明具有同等疗效，这也就不足为奇了。现在，在以下每种情况下都对一种或多种抗血小板药物进行了评估。
