Stege R, Gunnarsson P O, Johansson C J, Olsson P, Pousette A, Carlström K
Department of Urology, Karolinska Institutet, Huddinge University Hospital, Sweden.
Prostate. 1996 May;28(5):307-10. doi: 10.1002/(SICI)1097-0045(199605)28:5<307::AID-PROS6>3.0.CO;2-8.
The pharmacokinetics and endocrine effects of polyestradiol phosphate (PEP; Estradurin) were studied by determination of the concentrations of estradiol (E2), unconjugated (E1) and total estrone (tE1; > or = 85% estrone sulfate), and testosterone in serum from 11 prostatic cancer patients after administration of a single intramuscular injection (320 mg). After injection of PEP, serum concentrations of E2, E1, and tE1 increased during 2-3 weeks. Thereafter serum E2 declined monophasically with a mean half-life of 70 days. The elimination of E1 and tE1 seemed to be governed by the formation of E2. The testosterone concentration decreased inversely to the raising E2 level and reached castration levels within 3 weeks and remained at this level for about 2 weeks, whereafter it increased inversely to the decreasing E2 concentrations.
通过测定11例前列腺癌患者单次肌内注射（320mg）多聚磷酸雌二醇（PEP；Estradurin）后血清中雌二醇（E2）、未结合雌酮（E1）和总雌酮（tE1；≥85%硫酸雌酮）以及睾酮的浓度，研究了PEP的药代动力学和内分泌效应。注射PEP后，血清E2、E1和tE1浓度在2 - 3周内升高。此后，血清E2呈单相下降，平均半衰期为70天。E1和tE1的消除似乎受E2形成的影响。睾酮浓度与升高的E2水平呈反比下降，并在3周内达到去势水平，在此水平维持约2周，此后又与下降的E2浓度呈反比升高。
