Schrör K
Institut für Pharmakologie und Klinische Pharmakologie, Universitätsklinikum Düsseldorf, Germany.
Internist (Berl). 2005 Aug;46(8):873-8, 880-1. doi: 10.1007/s00108-005-1452-3.
The design and development of new antithrombotics, i.e. anticoagulants and antiplatelet drugs, is a rapidly expanding area of pharmacological research. New anticoagulants, i.e. inhibitors of thrombin formation and action have been developed and some of them are already in clinical use. This includes hirudin and its analogs, such as bivalirudin. In contrast to heparins, these compounds as well as low-molecular weight inhibitors of thrombin and factor Xa directly inhibit thrombus-associated generation and action of thrombin, eventually associated with a reduced bleeding tendency. Orally active compounds are available and currently subject of clinical trials. It appears possible that these new agents may replace cumarins as oral anticoagulants, specifically in long-term use, in the near future. The introduction of clopidogrel marks another important development in the field of antiplatelet drugs. Synergistic actions of this compound with acetylsalicylic acid and GP-IIb/IIIa-antagonists because of their different mode of action enhance the antithrombotic potential considerably and have been clinically confirmed. Despite of this optimistic outlook, the individual risk/benefit ratio of these new drugs, in particular in the area of anticoagulants, still needs to be defined.
新型抗栓药物,即抗凝剂和抗血小板药物的设计与开发,是药理学研究中一个迅速发展的领域。新型抗凝剂,即凝血酶形成和作用的抑制剂已被研发出来,其中一些已投入临床使用。这包括水蛭素及其类似物,如比伐卢定。与肝素不同,这些化合物以及凝血酶和Xa因子的低分子量抑制剂直接抑制与血栓相关的凝血酶生成和作用,最终使出血倾向降低。口服活性化合物已可供使用,目前正处于临床试验阶段。在不久的将来,这些新型药物有可能取代香豆素类作为口服抗凝剂,尤其是在长期使用方面。氯吡格雷的引入标志着抗血小板药物领域的另一项重要进展。由于其不同的作用方式,该化合物与乙酰水杨酸和糖蛋白IIb/IIIa拮抗剂的协同作用显著增强了抗栓潜力,并已得到临床证实。尽管前景乐观,但这些新药的个体风险/效益比,尤其是在抗凝剂领域,仍有待确定。