De Leo V, la Marca A, Morgante G, Lanzetta D, Setacci C, Petraglia F
Department of Obstetrics and Gynecology, University of Siena, Italy.
Am J Obstet Gynecol. 2001 Feb;184(3):350-3. doi: 10.1067/mob.2001.111065.
OBJECTIVE(S): Raloxifene, a selective estrogen receptor modulator, has beneficial estrogen agonist effects on bone and cardiovascular risk factors and estrogen antagonist effects on the breast and uterus. Limited clinical data have shown a sustained decrease in total cholesterol, low-density lipoprotein cholesterol, and homocysteine levels; an elevated homocysteine level is an independent risk factor for atherosclerosis. All of these studies were conducted in relatively young populations of women (mean age, 52-54 years). Raloxifene does not affect hot flushes, a major immediate symptom of menopause. This drug may therefore be useful in older women to prevent osteoporosis and cardiovascular disease. The aim of this clinical study was to evaluate the effects of raloxifene on plasma lipids and homocysteine in older women.
The subjects were 45 healthy postmenopausal women, aged 60 to 70 years. The women were randomly assigned to therapy with raloxifene or placebo, 60 mg/d for 1 year. Twenty-six women received raloxifene and 19 received placebo. Checkups were performed every 3 months. At baseline and after 3, 6, 9, and 12 months of treatment we measured homocysteine, total serum cholesterol, triglycerides, and both high-density lipoprotein and low-density lipoprotein cholesterol.
An effect on lipids was evident by 3 months with no significant additional modification at 12 months. Mean low-density lipoprotein cholesterol levels were lowered by 15% and total cholesterol was lowered by 8.5%. No reduction in high-density lipoprotein cholesterol or triglycerides was observed. After 3 months of therapy, homocysteine was significantly lower than at baseline (9.9 +/- 1.6 vs 11 +/- 2.1 micromol/L; P < .05). The greatest reduction with respect to baseline was reached after 6 months of therapy (-19.5% +/- 3%; P < .05).
CONCLUSION(S): The results of our study show that raloxifene at a dose of 60 mg/d reduces serum concentrations of low-density lipoprotein cholesterol and total cholesterol in healthy older women. Our study shows that in older women raloxifene leads to a 19.5% +/- 3% reduction in fasting homocysteine levels. Raloxifene may have a favorable effect on the incidence of cardiovascular disease in older women.
雷洛昔芬是一种选择性雌激素受体调节剂，对骨骼和心血管危险因素具有有益的雌激素激动剂作用，对乳腺和子宫具有雌激素拮抗剂作用。有限的临床数据显示，总胆固醇、低密度脂蛋白胆固醇和同型半胱氨酸水平持续下降；同型半胱氨酸水平升高是动脉粥样硬化的独立危险因素。所有这些研究均在相对年轻的女性人群（平均年龄52 - 54岁）中进行。雷洛昔芬不影响潮热，潮热是绝经的主要即时症状。因此，这种药物可能对老年女性预防骨质疏松症和心血管疾病有用。本临床研究的目的是评估雷洛昔芬对老年女性血脂和同型半胱氨酸的影响。
研究对象为45名年龄在60至70岁之间的健康绝经后女性。这些女性被随机分配接受雷洛昔芬或安慰剂治疗，剂量为60 mg/d，为期1年。26名女性接受雷洛昔芬治疗，19名女性接受安慰剂治疗。每3个月进行一次检查。在基线以及治疗3、6、9和12个月后，我们测量了同型半胱氨酸、血清总胆固醇、甘油三酯以及高密度脂蛋白和低密度脂蛋白胆固醇。
3个月时对血脂的影响明显，12个月时无显著进一步变化。平均低密度脂蛋白胆固醇水平降低了15%，总胆固醇降低了8.5%。未观察到高密度脂蛋白胆固醇或甘油三酯降低。治疗3个月后，同型半胱氨酸显著低于基线水平（9.9±1.6对11±2.1 μmol/L；P < 0.05）。治疗6个月后相对于基线的降幅最大（-19.5%±3%；P < 0.05）。
我们的研究结果表明，60 mg/d剂量的雷洛昔芬可降低健康老年女性的血清低密度脂蛋白胆固醇和总胆固醇浓度。我们的研究表明，在老年女性中，雷洛昔芬可使空腹同型半胱氨酸水平降低19.5%±3%。雷洛昔芬可能对老年女性心血管疾病的发病率产生有利影响。
