Sharma G V
Am J Med. 1987 Aug 24;83(2A):2-5. doi: 10.1016/0002-9343(87)90879-5.
Early attempts to treat thromboembolic disorders focused on the prevention of thrombus formation, along with the prevention of extension and/or embolization of an existing thrombus. Antithrombotic therapy for these conditions included intravenous and oral anticoagulants and later antiplatelet agents, all of which remain in use today. Subsequent research sought a thrombolytic agent that could lyse a clot directly. Intravenously administered streptokinase and urokinase were found to act on the inactive proenzyme plasminogen to produce the active enzyme plasmin that could safely and effectively lyse fresh fibrin clots. These agents have proved effective for the treatment of myocardial infarction and pulmonary embolism, as well as peripheral arterial and venous thromboembolic conditions. Recent efforts have been directed toward a search for clot-specific agents that would avoid the systemic lytic state associated with the use of urokinase and streptokinase. Three clot-specific plasminogen activators are currently being evaluated: recombinant tissue-specific plasminogen activator, anisoylated streptokinase plasminogen activator complex, and pro-urokinase.
早期治疗血栓栓塞性疾病的尝试主要集中在预防血栓形成，以及预防现有血栓的扩展和/或栓塞。针对这些病症的抗血栓治疗包括静脉内和口服抗凝剂，以及后来的抗血小板药物，所有这些药物至今仍在使用。随后的研究寻求一种能够直接溶解血栓的溶栓剂。发现静脉注射的链激酶和尿激酶作用于无活性的酶原纤溶酶原，产生能够安全有效地溶解新鲜纤维蛋白凝块的活性酶纤溶酶。这些药物已被证明对治疗心肌梗死、肺栓塞以及外周动脉和静脉血栓栓塞病症有效。最近的努力一直致力于寻找能够避免与使用尿激酶和链激酶相关的全身溶解状态的血栓特异性药物。目前正在评估三种血栓特异性纤溶酶原激活剂：重组组织特异性纤溶酶原激活剂、茴香酰化链激酶纤溶酶原激活剂复合物和尿激酶原。
