Effects of estradiol decanoate in ovariectomized women
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Estradiol decanoate (E2D) dissolved in ethyl oleate was given orally for 14 days in a daily dose of 0.25 mg to 6 ovariectomized women with the uterus left in situ. Effects on plasma estrone (E1), estradiol (E2), FSH, LH and prolactin (PRL), as well as on vaginal smears, cervical mucus Ferning and Spinnbarkeit, and endometrial proliferation were studied. Circulating plasma E1, E2, FSH, LH and PRL were measured by specific radioimmunoassays on days 0, 1, 2, 4, 7, 10, 15, 16 and 17 at 08:00 h. Plasma E1 and E2 were also frequently assayed on days 1 and 14. Determination of plasma estrogens was always done after isolation of the individual steroids by chromatography on Sephadex LH-20. For the statistical evaluation paired t-test was applied. After a single dose of E2D mean plasma E2 rose from 21.3 to 40.8 pg/ml (p <0.05) and to 57.7 pg/ml (p < 0.001) within 30 minutes and 1 hour, respectively. There was a further rise to 88.7 pg/ml after 10 hours. Mean plasma E1 rose slowly from 18.5 to a maximum of 57.3 pg/ml after a single dose of E2D. On repeated daily administration of E2D mean plasma E2 and E1, measured at 08:00 h, rose to 116.2 and 58.2 pg/ml, respectively. Frequent plasma sampling on day 14 revealed similar proportional increases of E2 and E1 levels, with mean peak values of 140.3 and 76.8 pg/ml, respectively. During treatment mean plasma E1:E2 ratio remained between 0,5 and 0.6. After discontinuation of E2D therapy plasma estrogen levels fell progressively within 48 hours. Suppression of plasma FSH and LH was weak, while mean PRL level increased 3-fold, although remaining within the range of normal menstruating women. Marked effects on vaginal epithelium and cervical mucus were recorded in all cases. Endometrial specimens showed moderate proliferative changes. No side-effects were reported. It was concluded that therapy with oral E2D dissolved in oil offers new possibilities for estrogen supplementation therapy.
Key-wordsEstradiol decanoate plasma estradiol estrone FSH LH PRL cervical mucus endometrial proliferation
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