Leinonen P, Bolton N J, Kontturi M, Vihko R
Prostate. 1982;3(6):589-97. doi: 10.1002/pros.2990030608.
The short-term (6-day) endocrine effects of tamoxifen and testolactone were investigated in men with prostatic carcinoma. Tamoxifen treatment (20 mg/day) did not affect the gonadotropin levels, but it temporarily increased prolactin, induced sex hormone-binding globulin production, and suppressed peripheral serum progesterone, 17-hydroxyprogesterone, androstenedione, testosterone, and 5 alpha-dihydrotestosterone concentrations. These changes were attributed to the estrogenic properties of tamoxifen, since no changes in peripheral serum estradiol concentrations were observed. Testolactone (1000 mg/day) decreased peripheral estradiol concentrations by 50% and increased the concentrations of the neutral steroids measured. The increases in serum FSH and LH were very small. This study corroborates the early estrogen-like action of tamoxifen, and the experiment with testolactone further suggests that endogenous estradiol has physiological functions in man, regulating gonadotropin and androgen production.
对前列腺癌男性患者研究了他莫昔芬和睾酮内酯的短期（6天）内分泌效应。他莫昔芬治疗（20毫克/天）不影响促性腺激素水平，但它使催乳素暂时升高，诱导性激素结合球蛋白产生，并抑制外周血清孕酮、17-羟孕酮、雄烯二酮、睾酮和5α-双氢睾酮浓度。这些变化归因于他莫昔芬的雌激素特性，因为未观察到外周血清雌二醇浓度有变化。睾酮内酯（1000毫克/天）使外周雌二醇浓度降低50%，并使所测中性类固醇浓度升高。血清促卵泡激素（FSH）和促黄体生成素（LH）的升高非常小。本研究证实了他莫昔芬早期类似雌激素的作用，而睾酮内酯实验进一步表明内源性雌二醇在男性中具有生理功能，调节促性腺激素和雄激素的产生。
