Lønning P E, Kvinnsland S, Thorsen T, Ekse D
Breast Cancer Res Treat. 1986;7 Suppl:S77-82.
Using a [4-14C]estradiol bolus injection technique possible effects of AG administration on estrogen metabolism were studied in seven patients. No alterations in steroid disposition were seen after a short term AG treatment. Chronic AG administration produced no change in mean estradiol clearance value. Chronic AG treatment as a low- or high-dose drug schedule produced a consistent reduction in estrone sulfate production rate (mean reductions 24 and 42%) as well as an increased estrone sulfate elimination rate constant (mean increase 30 and 69%). Urinary estriol secretion rate was consistently increased during chronic treatment (mean increase 95%) with no difference between low- and high dose drug schedules. These findings are consistent with AG being a potent enzyme inducer stimulating estrogen metabolism, and this mechanism may be an important part of AG mechanism of action by reducing estrone sulfate bioavailability.
采用[4-¹⁴C]雌二醇推注技术，在7例患者中研究了给予AG对雌激素代谢的可能影响。短期AG治疗后未观察到类固醇处置的改变。长期给予AG后，雌二醇清除率均值未发生变化。以低剂量或高剂量给药方案长期给予AG，均可使硫酸雌酮生成率持续降低（平均降低24%和42%），同时使硫酸雌酮消除速率常数增加（平均增加30%和69%）。长期治疗期间，尿雌三醇分泌率持续增加（平均增加95%），低剂量和高剂量给药方案之间无差异。这些发现与AG是一种刺激雌激素代谢的强效酶诱导剂一致，并且这种机制可能是AG通过降低硫酸雌酮生物利用度发挥作用机制的重要组成部分。
