Lippert T H, Seeger H, Mueck A O
Section of Clinical Pharmacology, University of Tuebigen, Germany.
Horm Metab Res. 1998 Sep;30(9):598-600. doi: 10.1055/s-2007-978940.
The metabolism of estradiol was investigated in postmenopausal women after 4 weeks' treatment with oral or transdermal unopposed estradiol. The urinary excretion of the metabolites was examined. With both administration routes, 2-hydroxyestrone, the main A-ring metabolite, and 16alpha-hydroxyestrone, the main D-ring metabolite, were excreted in higher amounts than estradiol and estrone. The ratio of 2-hydroxyestrone to 16alpha-hydroxyestrone remained the same for both administration routes. It has been suggested that dominance of D-ring metabolism, i.e. increase of 16alpha-hydroxyestrone production, is associated with an increased risk of breast cancer. The present study indicates that neither oral nor transdermal estradiol substitution shift this ratio to a higher level of possible risk. Oral estradiol substitution, however, in our study leads to higher metabolite concentrations which may be regarded as hazardous for women with diseases favoring D-ring metabolism.
在绝经后女性中，对口服或经皮使用单纯雌二醇治疗4周后的雌二醇代谢情况进行了研究。检测了代谢产物的尿排泄情况。两种给药途径下，主要的A环代谢产物2-羟雌酮和主要的D环代谢产物16α-羟雌酮的排泄量均高于雌二醇和雌酮。两种给药途径下，2-羟雌酮与16α-羟雌酮的比例保持不变。有人提出，D环代谢占优势，即16α-羟雌酮生成增加，与乳腺癌风险增加有关。本研究表明，口服或经皮雌二醇替代治疗均未使该比例升至更高的潜在风险水平。然而，在我们的研究中，口服雌二醇替代治疗会导致代谢产物浓度更高，这对于存在有利于D环代谢疾病的女性可能被视为有害。
