Haczynski J, Jakimiuk A
Medical Department, Eli Lilly Polska, Warsaw, Poland.
Med Sci Monit. 2001 Sep-Oct;7(5):1108-17.
Osteoporosis is a progressive skeletal disease, which in many cases remains silent and asymptomatic until a fracture occurs. Vertebral fractures are the earliest and most common osteoporotic fractures. The prevalence of vertebral fractures increases steadily with age, ranging between 20% for 50-year-old postmenopausal women to 64.5% for older women. The majority of vertebral fractures are not connected with severe trauma, and only one in three is diagnosed clinically. Usually vertebral fractures are associated with such clinical symptoms as back pain, posture change, loss of height, functional impairment, disability, and diminished quality of live. Women with the most severe vertebral fractures are the most likely to incur further fractures, with as much as 3.4 times the risk of hip fracture, and 12.6 times the risk of new vertebral fractures. Almost 20% of women will experience another fracture within 1 year after a vertebral fracture. Vertebral fractures are accompanied by increased mortality. The relative risk of death following vertebral fracture is almost 9 times higher. The most important purpose of osteoporosis management in postmenopausal women is prevention of the first vertebral fracture. Raloxifene (Evista) is the only SERM approved by the American FDA for the treatment and prevention of osteoporosis. It is the first compound with selective estrogen agonist activity in bone and in the cardiovascular system, but with estrogen antagonist activity or no activity in reproductive tissues and breast. Raloxifene reduces the risk of positive estrogen receptor breast cancer, decreases total cholesterol and LDL cholesterol, increases HDL cholesterol, does not increase the risk of endometrial cancer or cause bleeding and spotting. After 3 years of treatment Raloxifene reduces the risk of first vertebral fracture by 55%. The fracture risk within one year is reduced by as much as 68%. Continued observation has proved its sustained efficacy in the further reduction of fracture risk by 49% in the fourth year. Raloxifene treatment does not change the physiological structure of bone quality and does not cause fibrosis, osteomalacia or other toxic effects.
骨质疏松症是一种进行性骨骼疾病，在许多情况下，在骨折发生之前一直处于隐匿且无症状状态。椎体骨折是最早且最常见的骨质疏松性骨折。椎体骨折的患病率随年龄稳步上升，50岁绝经后女性的患病率为20%，老年女性则为64.5%。大多数椎体骨折与严重创伤无关，临床上仅三分之一能得到诊断。通常椎体骨折会伴有背痛、姿势改变、身高降低、功能障碍、残疾以及生活质量下降等临床症状。椎体骨折最严重的女性最有可能发生进一步骨折，髋部骨折风险高达3.4倍，新发椎体骨折风险高达12.6倍。近20%的女性在椎体骨折后1年内会再次发生骨折。椎体骨折会导致死亡率上升。椎体骨折后的相对死亡风险几乎高出9倍。绝经后女性骨质疏松症管理的最重要目的是预防首次椎体骨折。雷洛昔芬（易维特）是美国食品药品监督管理局（FDA）批准用于治疗和预防骨质疏松症的唯一选择性雌激素受体调节剂（SERM）。它是第一种在骨骼和心血管系统中具有选择性雌激素激动剂活性，但在生殖组织和乳腺中具有雌激素拮抗剂活性或无活性的化合物。雷洛昔芬可降低雌激素受体阳性乳腺癌的风险，降低总胆固醇和低密度脂蛋白胆固醇水平，升高高密度脂蛋白胆固醇水平，不会增加子宫内膜癌风险或引起出血和点滴出血。经过3年治疗，雷洛昔芬可将首次椎体骨折风险降低55%。1年内的骨折风险可降低多达68%。持续观察证明其在第4年可继续有效降低骨折风险49%。雷洛昔芬治疗不会改变骨质的生理结构，也不会引起纤维化、骨软化或其他毒性作用。
