Duschek Erik J J, Gooren Louis J, Netelenbos Coen
Department of Endocrinology, VU University Medical Centre, Amsterdam, The Netherlands.
Eur J Endocrinol. 2004 Apr;150(4):539-46. doi: 10.1530/eje.0.1500539.
To explore effects on serum lipids, pituitary-gonadal axis, prostate and bone turnover of the administration of the mixed oestrogen agonist/antagonist raloxifene in healthy elderly men.
Thirty healthy men aged 60-70 years randomly received raloxifene 120 mg/day (n=15) or placebo (n=15) for 3 months.
In this double-blind, placebo-controlled study, serum gonadotrophins, sex hormones, prostate specific antigen (PSA), a marker of bone turnover, urinary hydroxyproline (OHPro) and cholesterol were measured at baseline and after 3 months.
Raloxifene significantly increased serum concentrations of LH and FSH (by 29% and 21%), total testosterone (20%), free testosterone (16%) and bioavailable testosterone (not bound to sex hormone-binding globulin (SHBG; 20%). In parallel with testosterone, 17 beta-oestradiol also increased by 21%. SHBG increased by 7%. Total cholesterol (TChol) decreased significantly, from 5.7 to 5.5 mmol/l (P=0.03). Low-density lipoprotein cholesterol (LDL-c) and high-density lipoprotein cholesterol (HDL-c) showed a trend to decrease. Overall, there was no change in urinary OHPro/creatinine ratio as a marker for bone resorption. However, the raloxifene-induced increases in both serum testosterone and 17 beta-oestradiol were significantly related to a lower OHPro/creatinine ratio. Total PSA increased by 17% without significant changes in free PSA or free/total PSA ratio. Participants reported no side effects and raloxifene was well tolerated.
In healthy elderly man, raloxifene 120 mg/day for 3 months increased LH, FSH and sex steroid hormones. Potentially beneficial effects were the small but significant decrease in TChol and the trend towards a decrease in LDL-c. Negative effects were the trend towards a decrease in HDL-c and the significant increase in serum PSA. A decrease in markers of bone resorption during raloxifene treatment was found only in men with relatively high increases in serum testosterone and 17 beta-oestradiol. Overall, there were no clear beneficial effects of administration of raloxifene to ageing men in this preliminary investigation.
探讨混合雌激素激动剂/拮抗剂雷洛昔芬对健康老年男性血脂、垂体-性腺轴、前列腺及骨转换的影响。
30名年龄在60 - 70岁的健康男性随机接受雷洛昔芬120毫克/天（n = 15）或安慰剂（n = 15）治疗3个月。
在这项双盲、安慰剂对照研究中，在基线和3个月后测量血清促性腺激素、性激素、前列腺特异性抗原（PSA）、骨转换标志物尿羟脯氨酸（OHPro）和胆固醇。
雷洛昔芬显著提高血清促黄体生成素（LH）和促卵泡生成素（FSH）浓度（分别提高29%和21%）、总睾酮（20%）、游离睾酮（16%）和生物可利用睾酮（未与性激素结合球蛋白（SHBG）结合；20%）。与睾酮平行，雌二醇也升高了21%。SHBG升高7%。总胆固醇（TChol）显著降低，从5.7降至5.5毫摩尔/升（P = 0.03）。低密度脂蛋白胆固醇（LDL - c）和高密度脂蛋白胆固醇（HDL - c）呈下降趋势。总体而言，作为骨吸收标志物的尿OHPro/肌酐比值无变化。然而，雷洛昔芬诱导的血清睾酮和雌二醇升高均与较低的OHPro/肌酐比值显著相关。总PSA升高17%，游离PSA或游离/总PSA比值无显著变化。参与者未报告副作用，雷洛昔芬耐受性良好。
在健康老年男性中，每天服用120毫克雷洛昔芬3个月可提高LH、FSH和性类固醇激素水平。潜在的有益作用是TChol有小幅度但显著的降低以及LDL - c有下降趋势。负面影响是HDL - c有下降趋势以及血清PSA显著升高。仅在血清睾酮和雌二醇升高相对较高的男性中发现雷洛昔芬治疗期间骨吸收标志物有所下降。总体而言，在这项初步研究中，给老年男性服用雷洛昔芬没有明显的有益效果。
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