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  • Title: Oral contraceptives containing 20 or 30 micrograms ethinylestradiol and 150 micrograms desogestrel: pharmacokinetics and pharmacodynamic parameters.
    Author: Jung-Hoffmann C, Fitzner M, Kuhl H.
    Journal: Horm Res; 1991; 36(5-6):238-46. PubMed ID: 1823082.
    Abstract:
    The serum concentrations of ethinylestradiol (EE) and 3-keto-desogestrel (KDG) were compared during treatment with a combination of 20 micrograms EE + 150 micrograms DG (20EE/DG) or of 30 micrograms EE + 150 micrograms DG (30EE/DG). During intake of both preparations, the peak levels and the areas under the curve (AUC) of EE increased significantly by approximately 100% between days 1 and 10. In the steady state, the maximal EE levels were 75 +/- 34 pg/ml (20EE/DG) and 136 +/- 55 pg/ml (30EE/DG), and the AUC were 464 +/- 236 pg.h/ml and 840 +/- 492 pg.h/ml. The KDG levels, which were identical with both preparations, increased between days 1 and 21 by approximately 300% up to values of 4.5 +/- 1.6 ng/ml. There were large interindividual variations in the AUC of EE and KDG and no correlation between the levels of EE and KDG. On day 21 of intake of 30EE/DG, the serum concentrations of sex-hormone- and corticosteroid-binding globulin were higher by 16% and 12%, respectively than with 20EE/DG. Although the morning peak levels of cortisol did not differ, the decrease which occurred thereafter, according to the circadian rhythm, was slower with 30EE/DG. There was no relationship between the serum concentrations of EE and/or KDG and the occurrence of irregular bleedings, which was similar during treatment with both preparations. As most of the women who bled had bleedings both with 20EE/DG and 30EE/DG, an influence of predisposition can be assumed.(ABSTRACT TRUNCATED AT 250 WORDS) Gynecological endocrinologists at J.W. Goethe University in Frankfurt am Main, Germany, compared serum data on 34 20-39 year old women who used either the oral contraceptive Marvelon (30 mcg ethinyl estradiol [EE] and 150 mcg desogestrel [DG] or Lovelle (20 mcg EE and 150 mcg DG) to observe their pharmacokinetics and some pharmacodynamic parameters. Both formulations had the same DG levels. Between days 1 and 10, peak levels and areas under the curve (AUC) of EE rose by about 100% (p .05). During the washout cycle, EE levels were as high as 75 pg/ml (Lovelle) and 136 pg/ml (Marvelon). The corresponding AUC stood at 464 pg x h/ml and 840 pg x h/ml). Keto-DG (KDG) levels rose by almost 300% between day 1 and 21 (1.7 ng/ml vs. 4.5 ng/ml; p .01). Yet, considerable differences in the AUC of EE and KDG existed within the same women. Further, there was no association between EE levels and KDG levels. Marvelon resulted in 16% higher sex hormone-binding globulin levels and 12% higher corticosteroid-binding globulin levels than Lovelle on day 21 (p .05 and p .01, respectively). The decrease following the morning peak levels of cortisol was less pronounced in women taking Marvelon than in those taking Lovelle, resulting in a significantly higher AUC of cortisol (252 mcg x h/dl vs. 231 mcg x h/dl; p .05). No relationship between serum levels of EE and/or KDG existed between the 2 groups. In addition irregular bleeding patterns were similar for both treatment groups (44% for Lovelle and 50% for Marvelon). In fact, 7 of the 10 women who experienced irregular bleeding did so with both formulations, suggesting they were predisposed to irregular bleeding. In conclusion, the contraceptive steroids suppressed hepatic steroid metabolism, resulting in a rise in EE levels and some rise in progestogen levels.
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