Sobbrio G A, Granata A, Granese D, D'Arrigo F, Panacea A, Nicita R, Pullè C, Trimarchi F
University of Messina, School of Medicine, Institute of Clinica Medica I, Italy.
Clin Exp Obstet Gynecol. 1991;18(1):43-5.
It is generally assumed that the oral contraceptives cause the carrier proteins to change. Notoriously this effect is used to evaluate indirectly their estrogenicity/gestagenicity ratio. In order to assess the residual intrinsic androgenic activity of two new 19-nor-derivative components, Desogestrel (DG) 150 micrograms and Gestodene (GD) 75 micrograms, both in association with Ethinylestradiol (EE) 30 micrograms, Sex Hormone Binding Globulin, Thyroxine Binding Globulin, Ceruloplasmin and Free Androgen Index (FAI), were studied in 40 young normally cycling healthy volunteers, matched for body mass index and age. The participants were randomly assigned to either EE-DG or EE-GD treatment. A marked significant increase in all the carrier proteins was found. Conversely, the values for FAI decreased significantly. The changes in the two groups were substantially of the same magnitude. These results are an indirect confirmation of the well-known negligible receptor binding affinity of the two progestogen in vitro, also supporting for these compounds the lack of relevant androgenic effects.
一般认为口服避孕药会导致载体蛋白发生变化。众所周知，这种效应被用于间接评估它们的雌激素/孕激素比例。为了评估两种新的19-去甲衍生物成分，即150微克去氧孕烯（DG）和75微克孕二烯酮（GD）与30微克炔雌醇（EE）联合使用时的残余内在雄激素活性，对40名体重指数和年龄匹配的正常月经周期的年轻健康志愿者进行了性激素结合球蛋白、甲状腺素结合球蛋白、铜蓝蛋白和游离雄激素指数（FAI）的研究。参与者被随机分配接受EE-DG或EE-GD治疗。发现所有载体蛋白均有显著明显增加。相反，FAI值显著下降。两组的变化幅度基本相同。这些结果间接证实了这两种孕激素在体外众所周知的可忽略不计的受体结合亲和力，也支持了这些化合物缺乏相关雄激素作用的观点。
