Ranney R E
J Toxicol Environ Health. 1977 Sep;3(1-2):139-66. doi: 10.1080/15287397709529555.
The metabolism of mestranol, ethynylestradiol, norethynodrel, norethindrone, ethynodiol diacetate, lynestrenol, and norgestrel is reviewed. The estrogenic components of the oral contraceptives, mestranol or ethynylestradiol, have nearly identical metabolic pathways since mestranol is rapidly and almost completely converted to ethynylestradiol The major fraction of the drugs plus metabolites is excreted in the urine as conjugated materials. All of the 17beta-ethynyl progestins reviewed follow similar metabolic paths. For three of these, norethynodrel, ethynodiol diacetate and lynestrenol, a principal metabolite is norethindrone. Biotransformation to more polar metabolites and conjugation proceed rapidly for these three precursor drugs and norethindrone. Norgestrel follows metabolic paths similar to those of norethindrone. However, the ethyl moiety at the C-13 position appears to slow the metabolism of this steroid so that biotransformation to more polar metabolites and the conjugation of these steroids does not proceed as rapidly as that of the other progestins. The high progestational potency of norgestrel may be attributed to this slow rate of biotransformation. Some of the pharmacokinetic parameters derived from the research reports reviewed here are summarized. The compounds appear to be readily absorbed, and they and their metabolites are excreted to a greater extent in the urine than in the feces.
本文综述了炔雌醇甲醚、炔雌醇、异炔诺酮、炔诺酮、双醋炔诺醇、利奈孕酮和左炔诺孕酮的代谢情况。口服避孕药中的雌激素成分，即炔雌醇甲醚或炔雌醇，具有几乎相同的代谢途径，因为炔雌醇甲醚能迅速且几乎完全转化为炔雌醇。药物及其代谢产物的主要部分以结合物的形式经尿液排出。本文所综述的所有17β - 乙炔基孕激素都遵循相似的代谢途径。对于其中三种，即异炔诺酮、双醋炔诺醇和利奈孕酮，主要代谢产物是炔诺酮。这三种前体药物和炔诺酮向极性更强的代谢产物的生物转化以及结合过程进行得很快。左炔诺孕酮的代谢途径与炔诺酮相似。然而，C - 13位的乙基部分似乎减缓了这种甾体的代谢，因此向极性更强的代谢产物的生物转化以及这些甾体的结合过程不像其他孕激素那样迅速。左炔诺孕酮的高孕激素活性可能归因于这种缓慢的生物转化速率。本文总结了从所综述的研究报告中得出的一些药代动力学参数。这些化合物似乎易于吸收，并且它们及其代谢产物经尿液排泄的程度比经粪便排泄的程度更大。
