Aedo A R, Le Donne M, Landgren B M, Diczfalusy E
Department of Reproductive Endocrinology, Karolinska Institute and Hospital, Stockholm, Sweden.
Maturitas. 1989 Jun;11(2):147-57. doi: 10.1016/0378-5122(89)90007-8.
The gonadotrophin-suppressing effect of 4 peroral oestrogen regimens (A: 2.5 mg piperazine oestrone sulphate; B: 1.25 mg piperazine oestrone sulphate + 5.0 mg oestriol; C: 2.0 mg oestradiol valerate; D: 10.0 mg oestriol; all administered daily) was studied in 7 post-menopausal women, in the absence, and then in the presence of daily oral doses of 250 micrograms of levonorgestrel. A randomized, complete cross-over design was used, and from each volunteer 80 blood samples were drawn during a period of 252 days for the assay of immunoreactive follicle stimulating hormone (FSH), luteinizing hormone (LH) and bioactive LH levels. All 4 formulations significantly diminished pretreatment gonadotrophin levels. Combination with levonorgestrel enhanced the suppressive effects. Subsequent placebo administration for a week restored gonadotrophin levels to those found previously during oestrogen administration, but not to pretreatment levels. Regimen D exhibited the relatively weakest and regimens A and B the strongest suppression, both in the absence and in the presence of levonorgestrel. Treatment with all oestrogen formulations decreased, and the addition of levonorgestrel increased the ratio of bioactive (B) to immunoreactive (I) LH. Seven days of placebo administration abolished the effect of levonorgestrel, but not that of the various oestrogens on the B/I ratios.
在7名绝经后女性中研究了4种口服雌激素方案(A:2.5mg哌嗪雌酮硫酸盐;B:1.25mg哌嗪雌酮硫酸盐 + 5.0mg雌三醇;C:2.0mg戊酸雌二醇;D:10.0mg雌三醇;均每日给药)的促性腺激素抑制作用,先是在无每日口服250μg左炔诺孕酮的情况下,然后是在有该剂量左炔诺孕酮的情况下进行研究。采用随机、完全交叉设计,在252天的时间里从每位志愿者采集80份血样,用于检测免疫反应性促卵泡激素(FSH)、促黄体生成素(LH)和生物活性LH水平。所有4种制剂均显著降低了治疗前的促性腺激素水平。与左炔诺孕酮联合使用增强了抑制作用。随后给予一周安慰剂使促性腺激素水平恢复到雌激素给药期间之前的水平,但未恢复到治疗前水平。无论有无左炔诺孕酮,方案D的抑制作用相对最弱,方案A和B的抑制作用最强。所有雌激素制剂治疗均降低了生物活性(B)与免疫反应性(I)LH的比值,而添加左炔诺孕酮则增加了该比值。给予7天安慰剂消除了左炔诺孕酮的作用,但未消除各种雌激素对B/I比值的作用。