Ethinylestradiol (EE, 17a-ethynyl-l,3,5(lO)-estratriene-3,l'IP-diol) 30 pg daily, in combination with 150 pg per day of desogestrel (Org 2969, 17a-ethynyl-18-methyl-l lmethylene-4-estrene-17P-01) or levonorgestrel (17~-ethynyl-18-methyl-4-estrene-17P-ol-3-one), was administered to two groups of 10 healthy human women who had been without hormonal treatment during 3 months prior to the study. The preparations were given for three 21-day cycles with 7-day intervals. Blood samples were taken before treatment and at the end of the third treatment period. Serum sex-hormone binding globulin (SHBG), ceruloplasmin, ornsomucoid, Cl-esterase inhibitor and C4 were analyzed by electroimmunoassay and transcortin was assayed as cortisol-binding capacity. Serum testosterone was assayed by radioimmunoassay of methylenedichloride extracts using an antiserum with about 20% cross-reactivity for dihydrotestosterone (DHT).The increases in serum ceruloplasmin and transcortin concentrations were the same in both groups (about 80% and 100-140%, respectively), whereas no significant change was noted for the orosomucoid, C1-esterase inhibitor or C4 concentrations. The SHBG concentration, how-Res Commun 72:489, 1976.
Desogestrel (Org 2969, 17u-ethinyl-18-methyl-11methylene-4-estrene-17@-01) was given for 21 days to 6 female volunteers in daily doses of 15,30 or 60 pg until ovulation inhibition was achieved. Control cycles were studied before and after each treatment cycle. Blood samples for determinations of serum FSH, LH, unconjugated 170estradiol, progesterone, prolactin, ceruloplasmin, and orosomucoid were taken at intervals of 1-2 days. The karyopyknotic index and the amount of cervical mucus, ferning, Spinnbarkeit and sperm penetration were also assessed at 2-day intervals. An endometrial biopsy was taken on day 22 from 5 volunteers receiving the 30 p g dose.The results of FSH, LH, 170-estradiol and progesterone
A new progestational compound, desogestrel, was given orally to four otherwise healthy, ovariectomized volunteers who had first been treated for two cycles with ethinylestradiol and lynestrenol (given sequentially) and then primed with ethinylestradiol. The effects of decreasing doses of desogestrel(250 to 15 pg) in combination with 50 pg ethinylestradiol were compared with those of 1 mg lynestrenol plus 50 pg ethinylestradiol. Variables studied were basal body temperature, vaginal cytology (karyopyknotic index), cervical mucus (including Spinnbarkeit and ferning) and endometrial biopsies. In addition, body weight, blood pressure and selected biochemical variables were monitored.No side effects attributable to the treatment were noted. Progestational effects were observed on all variables in volunteers with adequate priming. Basal body temperature rose in all volunteers on desogestrel at doses down to 60 pg to the same extent as those with I mg lynestrenol. The karyopyknotic index did not react to estrogen priming in 2 volunteers, and the results with the 2 other volunteers were inconclusive. Cervical mucus became thick and scanty with reduced Spinnbarkeit at doses of desogestrel down to 60 pg as well as with 1 mg lynestrenol. Crystallization of mucus (ferning) ceased at a dose of 30 pg desogestrel and endometrial biopsies showed marked secretion at doses of desogestrel down to 30 pg; 60 pg was considered to be equipotent to 1 mg lynestrenol. The ovariectomized woman with her uterus intact appears to be a good model for the initial testing of progestational compounds.
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