Hoffmann H, Moore C, Zimmermann H, Elger W, Schwarz S, Gräser T, Oettel M
Jenapharm & Co. KG, Department R & D, Jena, Germany.
Exp Toxicol Pathol. 1998 Sep;50(4-6):458-64. doi: 10.1016/s0940-2993(98)80034-1.
The strong hepatic estrogenic actions of ethinylestradiol (EE) are very likely to be the cause of the cardiovascular morbidity related to the use of combined oral contraceptives (COCs). This survey presents results of EE replacement in COCs with natural 17beta-estradiol (E2) in the following stages: reduction of EE to daily doses of 0.01 mg and concomitant replacement with E2 (as valerate, EV), complete replacement of EE with E2 using a novel multiphasic combination containing EV and the progestin dienogest (DNG), and the use of natural E2 to develop estrogen sulfamates (J 995) showing sufficient dissociation of uterine from liver estrogenicity. Recent data from preclinical and clinical studies show that these approaches seem to be promising.
乙炔雌二醇（EE）强大的肝脏雌激素作用很可能是与使用复方口服避孕药（COC）相关的心血管疾病的病因。本调查展示了在以下阶段用天然17β-雌二醇（E2）替代COC中EE的结果：将EE减至每日剂量0.01 mg并同时用E2（戊酸酯，EV）替代，使用含EV和孕激素地诺孕素（DNG）的新型多相组合完全用E2替代EE，以及使用天然E2开发显示子宫与肝脏雌激素活性充分解离的雌激素硫酸酯（J 995）。临床前和临床研究的最新数据表明，这些方法似乎很有前景。
