静脉血栓部分10.ppt

* The number of patients affected by venous thromboembolism (VTE) has been estimated to be: - Deep venous thrombosis (DVT) – up to 145 patients per 100 000 population (age- and sex adjusted to the US 1980 white population) 1,2 - Pulmonary embolism (PE) – up to 69 patients per 100 000 population (Olmsted Country (USA), white population only) 3 Venous thrombosis is an important cause of morbidity and mortality, and is responsible for 300,000–600,000 hospitalisations in the USA alone each year. PE is potentially the most serious complication of VTE. 1. Gillum RF. Am Heart 1987. 1987;114:1262-1264 2. Anderson F Jr, Wheeler HB, Goldberg RJ, et al. A Population-based perspective of the hospital incidence and case-fatality rates of deep-vein thrombosis and pulmonary embolism: the Worcester study. Arch Intern Med 1991;151:933-938 3. Silverstein MD, Heit JA, Mohr DN, et al. Trends in the incidence of deep vein thrombosis and pulmonary embolism. Archives of Internal Medicine 1998;158:585-593 从20世纪30年代普通肝素的发明以来，抗凝药物已经经历近80年的发展。其研发开始朝向口服、特异性和直接作用的方向发展，因为这些特点可以降低副反应的发生和拥有较宽的治疗窗。 口服直接Xa因子抑制剂即为整个发展方向中的一部分，因为这类抗凝剂直接、特异性地抑制Xa因子。 Anticoagulant agents have evolved over the last 80 years. Drugs are being aimed at more specific targets in the coagulation pathway. The goal has been to develop agents that are able to target factors and enzymes involved in coagulation more directly, ideally producing fewer triggers of the feedback loop. 肝素类抗凝药物主要就是通过强化抗凝血酶Ⅲ的作用来达到抗凝效果的，它们与凝血酶Ⅲ结合使其结构改变，从而使抗凝血酶Ⅲ灭活凝血因子的速度明显增加。肝素类作用于此凝血瀑布图中蓝色标记的多个凝血因子。但主要是Xa和IIa因子。 * 普通肝素起效很快，但是需要注射或输注；个体差异大，治疗窗窄，有发生肝素诱导的血小板减少的风险（发生率约为3％），并需要进行血小板监测。长期应用还有导致骨质疏松的风险。 Although UFH has many side effects, it is still considered to have an acceptable safety and efficacy balance, as reflected by its recommended use in practice guidelines.1 Heparin is indicated for the treatment of deep vein thrombosis, pulmonary embolism, unstable angina pectoris, and acute peripheral arterial occlusion.2 REFERENCES 1. Geerts WH, et al. Che