Lähteenmäki P L, Lähteenmäki P
Fertil Steril. 1985 Jul;44(1):20-4.
We summarize the hormonal profiles of women at different stages of inhibition of ovarian function during sustained-release subcutaneous treatment with a progestin, ST-1435. In the highest release group of ST-1435, a decrease in the luteinizing hormone (LH)follicle-stimulating hormone (FSH) ratio was found; and in spite of follicular phase levels of plasma FSH, inhibition of folliculogenesis, as judged by plasma estradiol (E2) concentrations below 60 pg/ml, occurred during the entire treatment period of 230 days. This may be indicative of a direct action of ST-1435 on the ovaries. When the average plasma concentration of ST-1435 decreased below 100 pg/ml, follicle development had started in most of the study subjects. At that time, the LH/FSH ratio had normalized to that found during the follicular phase of the normal menstrual cycle. In spite of the E2 rise during follicular development, no midcycle gonadotropin surges or subsequent elevations in plasma progesterone concentrations were found, thus indicating that the positive feedback action of E2 on gonadotropins was blocked by this progestin. We infer that the mechanism of inhibition of ovulation by sustained parenteral treatment with the progestin ST-1435 is concentration dependent, in such a manner that lower plasma concentrations of ST-1435 act on the hypothalamus and/or pituitary, whereas at higher plasma concentrations of ST-1435, a direct effect on the ovaries is also achieved.
我们总结了在使用孕激素ST - 1435进行皮下缓释治疗期间，处于卵巢功能抑制不同阶段的女性的激素谱。在ST - 1435的最高释放组中，发现促黄体生成素（LH）与促卵泡生成素（FSH）的比值下降；尽管血浆FSH处于卵泡期水平，但根据血浆雌二醇（E2）浓度低于60 pg/ml判断，在整个230天的治疗期间卵泡生成受到抑制。这可能表明ST - 1435对卵巢有直接作用。当ST - 1435的平均血浆浓度降至100 pg/ml以下时，大多数研究对象开始出现卵泡发育。此时，LH/FSH比值已恢复至正常月经周期卵泡期的水平。尽管在卵泡发育过程中E2有所升高，但未发现中期促性腺激素高峰或随后血浆孕酮浓度升高，这表明E2对促性腺激素的正反馈作用被这种孕激素阻断。我们推断，通过孕激素ST - 1435进行持续非肠道治疗抑制排卵的机制是浓度依赖性的，即较低血浆浓度的ST - 1435作用于下丘脑和/或垂体，而在较高血浆浓度时，也会对卵巢产生直接作用。
