Ottosson U B, Carlström K, Johansson B G, von Schoultz B
Gynecol Obstet Invest. 1984;18(3):140-6. doi: 10.1159/000299069.
The antiestrogenic effects of tamoxifen and estriol were compared in 39 postmenopausal women during estrogen replacement therapy. Subfractions of HDL cholesterol and its apolipoproteins and the serum levels of two estrogen sensitive liver proteins were followed during three cycles of unopposed estrogen therapy with 10 micrograms ethinyl estradiol daily. During the last 10 days of the following three cycles the women received sequential addition of either 10 mg tamoxifen twice daily or 2 mg estriol twice daily. Tamoxifen clearly reduced the estrogen-induced increase of apolipoprotein AI, HDL2 cholesterol and total HDL cholesterol. In comparison the pregnancy zone protein and sex hormone-binding globulin were more sensitive to the estrogenic as well as to the antiestrogenic effect than the lipoproteins. Tamoxifen also counteracted the therapeutic effect on climacteric symptoms and it seems unlikely that this compound may be clinically useful as an alternative to progestogens during estrogen replacement therapy. The sequential addition of estriol had no apparent effects as compared to unopposed estrogen treatment.
在39名绝经后妇女接受雌激素替代治疗期间，对他莫昔芬和雌三醇的抗雌激素作用进行了比较。在三个周期的每日10微克乙炔雌二醇单一雌激素治疗过程中，监测了高密度脂蛋白胆固醇及其载脂蛋白亚组分以及两种雌激素敏感肝脏蛋白的血清水平。在接下来三个周期的最后10天，这些女性每天两次序贯添加10毫克他莫昔芬或每天两次2毫克雌三醇。他莫昔芬明显降低了雌激素诱导的载脂蛋白AI、HDL2胆固醇和总HDL胆固醇的升高。相比之下，妊娠区蛋白和性激素结合球蛋白对雌激素以及抗雌激素作用比脂蛋白更敏感。他莫昔芬还抵消了对更年期症状的治疗效果，在雌激素替代治疗期间，这种化合物似乎不太可能作为孕激素的替代品在临床上发挥作用。与单一雌激素治疗相比，雌三醇的序贯添加没有明显效果。
