Ravid R, Jedwab G, Persitz E, David M P, Karni N, Gil S, Cordova T, Harell A, Ayalon D
Clin Endocrinol (Oxf). 1977 May;6(5):333-8. doi: 10.1111/j.1365-2265.1977.tb02019.x.
Administration of clomiphene citrate (150 mg/day) for 5 days to twenty-four ovariectomized patients and seven normal female patients evoked a significant release of FSH and LH in the normal control group and suppressed the gonadotrophin secretion in the castrated patients. A similar suppressive effect on gonadotrophin secretion was noted in eight ovariectomized patients treated for 10 days with low doses (50 microgram/day) of ethinyl oestradiol. It is suggested that in the ovariectomized hypoestrogenic patients, clomiphene acted as an oestrogen, suppressing by a negative feedback action gonadotrophin release in a way similar to ethinyl oestradiol. In the normal control group with an adequate steroid environment, clomiphene acted (probably at the hypothalamic level) as an oestrogen antagonist and stimulated gonadotrophin secretion. In view of our findings, it seems as if the ability of anovulatory patients to respond to clomiphene treatment by increased gonadotrophin secretion depends upon the absolute concentration of the compound in the different organs and by the quantitative relation of clomiphene to the endogenous oestrogens.
对24名卵巢切除患者和7名正常女性患者给予枸橼酸氯米芬(150毫克/天),持续5天,结果正常对照组促卵泡激素(FSH)和促黄体生成素(LH)显著释放,而阉割患者的促性腺激素分泌受到抑制。在用低剂量(50微克/天)乙炔雌二醇治疗10天的8名卵巢切除患者中,也观察到对促性腺激素分泌有类似的抑制作用。提示在卵巢切除的低雌激素患者中,氯米芬起到雌激素的作用,通过负反馈作用抑制促性腺激素释放,其方式类似于乙炔雌二醇。在具有足够类固醇环境的正常对照组中,氯米芬(可能在下丘脑水平)起到雌激素拮抗剂的作用,刺激促性腺激素分泌。鉴于我们的研究结果,似乎无排卵患者通过增加促性腺激素分泌来对氯米芬治疗作出反应的能力取决于该化合物在不同器官中的绝对浓度以及氯米芬与内源性雌激素的定量关系。