Kuhl H
Abteilung für Gynäkologische Endokrinologie, Univ.-Frauenklinik, Johann-Wolfgang-Goethe Universität, Frankfurt/Main, BRD.
Wien Med Wochenschr. 1987 Oct 15;137(18-19):433-40.
The different spectrum of biological actions of the various synthetic progestogens is compared on the basis of their chemical structure, pharmacokinetics and interaction with the multiple receptors. In detail, the mechanism of action of the progesterone derivatives (medroxyprogesterone acetate, chlormadinone acetate and cyproterone acetate), the norethisterone-related (norethisterone, ethynodiol diacetate, lynestrenol and norethynodrel) and the norgestrel-related progestogens (levonorgestrel, desogestrel, gestodene and norgestimate), and a possible influence of some metabolites upon the biological profile are discussed. With regard to the progestogenic activity, the time-course of the serum concentrations of the steroids after the application (pharmacokinetics) which is dependent upon absorption, metabolization in the gastro-intestinal tract and liver (first-pass effect), distribution and storage in fat and other tissues, binding to serum proteins, inactivation, and conjugation, is of particular importance. The various side-effects of the progestogens are mainly based on their influence upon hepatic metabolism (lipids, lipoproteins, serum proteins) and upon other organs which is dependent on their different estrogenic, antiestrogenic, androgenic, antiandrogenic, glucocorticoid and antimineralocorticoid actions.
基于各种合成孕激素的化学结构、药代动力学以及与多种受体的相互作用，对它们不同的生物学作用谱进行了比较。详细讨论了孕激素衍生物（醋酸甲羟孕酮、醋酸氯地孕酮和醋酸环丙孕酮）、炔诺酮相关（炔诺酮、醋酸炔诺二醇、利奈孕酮和异炔诺酮）以及左炔诺孕酮相关孕激素（左炔诺孕酮、去氧孕烯、孕二烯酮和诺孕酯）的作用机制，以及某些代谢产物对生物学特性的可能影响。关于孕激素活性，应用后类固醇血清浓度的时间进程（药代动力学）尤为重要，它取决于吸收、胃肠道和肝脏中的代谢（首过效应）、在脂肪和其他组织中的分布与储存、与血清蛋白的结合、失活以及结合反应。孕激素的各种副作用主要基于它们对肝脏代谢（脂质、脂蛋白、血清蛋白）以及其他器官的影响，这取决于它们不同的雌激素、抗雌激素、雄激素、抗雄激素、糖皮质激素和抗盐皮质激素作用。
