Wolff J P, Cachelou R, Guéritée N
Maturitas. 1982 Dec;4(4):239-46. doi: 10.1016/0378-5122(82)90054-8.
The women in this study were either post-menopausal or ovariectomised for at least 1 yr prior to the study. They had also been treated for cancer of the cervix (27 women), endometrium (5), ovaries (5) or breast (1). All women presented with sexual troubles, mainly genital discomfort (dyspareunia or vaginism). In a double-blind fashion, gynaecological capsules containing either an oestradiol diether (ICD: promestriene) or only the excipient were administered for 40 consecutive days. At the end of the treatment, the FSH, LH, oestrone (E1) and oestradiol (E2) plasma levels were not found to be significantly different from the pre-therapeutic values. These results suggest that promestriene acts on the vaginal mucosa, therefore not being converted back into the hormone from which it was derived. Also, in its dietheroxide form, promestriene is incapable of crossing the malpighian (vaginal or epidermal) epithelium and of reaching the general blood circulation. This discrepancy between the local anti-atrophic effects and the inability to exert systemic oestrogen activities singles out promestriene and justifies its therapeutic use when hormonally active oestrogens are contra-indicated, as in patients who have an oestrogen-sensitive cancer in their medical history.
本研究中的女性要么处于绝经后状态，要么在研究开始前至少已切除卵巢1年。她们还曾接受过宫颈癌（27名女性）、子宫内膜癌（5名）、卵巢癌（5名）或乳腺癌（1名）的治疗。所有女性均出现性问题，主要是生殖器不适（性交困难或阴道痉挛）。以双盲方式连续40天给予含有雌二醇二醚（国际化学标识符：普罗雌烯）或仅含辅料的妇科胶囊。治疗结束时，未发现促卵泡生成素（FSH）、促黄体生成素（LH）、雌酮（E1）和雌二醇（E2）的血浆水平与治疗前值有显著差异。这些结果表明，普罗雌烯作用于阴道黏膜，因此不会再转化回其来源的激素。此外，以其二醚形式存在时，普罗雌烯无法穿过马尔皮基（阴道或表皮）上皮并进入全身血液循环。局部抗萎缩作用与无法发挥全身雌激素活性之间的这种差异使普罗雌烯脱颖而出，并证明了在有雌激素敏感癌病史等激素活性雌激素禁忌的患者中其治疗用途的合理性。
