Department of Gynaecology, Obstetrics and Reproductive Medicine, Second University of Naples, Largo Madonna delle Grazie 1, Naples, Italy.
Int J Womens Health. 2010 Aug 9;1:11-20. doi: 10.2147/ijwh.s3894.
The integrity of bone tissue and its remodeling that occurs throughout life requires a coordinated activity of osteoblasts and osteoclasts. The decreased estrogen circulating level during postmenopausal transition, with a prevalence of osteoclastic activity over osteoblastic activity, represents the main cause of bone loss and osteoporosis. Osteoporosis is a chronic disease requiring long-term therapy and it is important to evaluate the efficacy and safety of treatments over several years, as the fear of health risks is a common reason for discontinuing therapy. Raloxifene is a selective estrogen receptor modulator (SERM) leading to estrogen-agonist effects in some tissues and estrogen-antagonist effects in others. Raloxifene is effective to prevent and treat postmenopausal vertebral osteoporosis, with reduction of spine fractures and, in post-hoc analyses, non-spine fractures in high-risk subjects. Moreover, raloxifene reduces the risk of invasive breast cancer and improves the levels of serum lipoprotein but with an increased risk of venous thromboembolism and fatal stroke, without significant change in the incidence of coronary events. For these reasons the overall risk-benefit profile is favorable. Therefore, when considering the use of raloxifene in a postmenopausal woman, we should take into account the osteoporosis-related individual risk and weigh the potential benefits, skeletal and extra-skeletal, against the health risks.
骨骼组织的完整性及其在整个生命周期中的重塑需要成骨细胞和破骨细胞的协调活动。绝经后过渡期循环雌激素水平下降，破骨细胞活性超过成骨细胞活性，这是导致骨丢失和骨质疏松症的主要原因。骨质疏松症是一种需要长期治疗的慢性疾病，评估多年治疗的疗效和安全性非常重要，因为对健康风险的担忧是停止治疗的常见原因。雷洛昔芬是一种选择性雌激素受体调节剂（SERM），在某些组织中具有雌激素激动作用，在其他组织中具有雌激素拮抗作用。雷洛昔芬可有效预防和治疗绝经后椎体骨质疏松症，降低脊柱骨折风险，在高危人群中也可降低非脊柱骨折风险。此外，雷洛昔芬降低了浸润性乳腺癌的风险，并改善了血清脂蛋白水平，但增加了静脉血栓栓塞和致命性中风的风险，而冠心病事件的发生率没有显著变化。基于这些原因，整体风险效益比是有利的。因此，在考虑绝经后妇女使用雷洛昔芬时，我们应考虑与骨质疏松症相关的个体风险，并权衡骨骼和骨骼外的潜在益处与健康风险。
