雷洛昔芬在绝经后骨质疏松症中的应用综述。
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Clemett D, Spencer CM
雷洛昔芬在绝经后骨质疏松症中的应用综述。
药物。2000年8月;60(2):379-411。
- PubMed ID
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10983739 (PubMed视图］
- 摘要
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雷洛昔芬是一种选择性雌激素受体调节剂，部分模拟雌激素在骨骼和心血管系统中的作用，同时在子宫内膜和乳房组织中发挥抗雌激素的作用。在涉及绝经后妇女或骨质疏松症患者的随机安慰剂对照研究中，雷洛昔芬60 - 150mg /day在12- 36个月的周期内有效地增加骨密度(BMD)。在60 mg/天推荐剂量下，腰椎、股骨颈和全髋关节分别增加1.6 - 3.4%、0.9 - 2.3%和1.0 - 1.6%，而安慰剂组<或=0.5%。雷洛昔芬60或120毫克/天可降低绝经后骨质疏松症患者36个月的椎体骨折风险。与安慰剂组相比，无论基线时患者是否存在骨折，放射学骨折风险均显著降低(30%和50%)。尽管雷洛昔芬不影响非椎体骨折的总体发生率，但与安慰剂相比，踝关节骨折的发生率有所降低。在绝经后妇女中，与安慰剂相比，雷洛昔芬60mg /天显著降低了血清总胆固醇和低密度脂蛋白胆固醇水平。高密度脂蛋白胆固醇和甘油三酯水平未受影响。在无乳腺癌史的绝经后骨质疏松症患者中位40个月的随访中，雷洛昔芬60或120毫克/天可使浸润性乳腺癌的风险降低76%。雌激素受体阳性侵袭性乳腺癌的相对风险降低了90%; estrogen-receptor negative cancer risk was unaffected by raloxifene. Raloxifene was generally well tolerated in clinical trials at dosages up to 150 mg/day. Adverse events thought to be related to raloxifene treatment were hot flushes and leg cramps. Venous thromboembolism was the only serious adverse event thought to be related to raloxifene treatment and a relative risk of 3.1 compared with placebo treatment was reported in patients with osteoporosis. Vaginal bleeding occurred in < or =6.4% of raloxifene-treated women but was reported by 50 to 88% of those receiving estrogens or hormone replacement therapy (HRT). Raloxifene treatment was not associated with stimulatory effects on the endometrium. CONCLUSIONS: Raloxifene significantly increases BMD in postmenopausal women and reduces vertebral fracture risk in patients with osteoporosis. In clinical trials, raloxifene was generally well tolerated compared with placebo and HRT, although its propensity to cause hot flushes precludes use in women with vasomotor symptoms. In particular, the lack of stimulatory effects on the endometrium and the reduction in invasive breast cancer incidence indicate raloxifene as an attractive alternative to HRT for the management of postmenopausal osteonorosis.
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