Oral contraceptives containing 20 or 30 micrograms ethinylestradiol and 150 micrograms desogestrel: pharmacokinetics and pharmacodynamic parameters.
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)
Jung-Hoffmann
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C
Department of Obstetrics and Gynecology, J.W. Goethe University, Frankfurt am Main, FRG.
Fitzner
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Kuhl
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H
D000328:Adult; D003277:Contraceptives, Oral, Combined / Q000493:pharmacokinetics* / Q000494:pharmacology; D017135:Desogestrel; D004997:Ethinyl Estradiol / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D005260:Female; D006801:Humans; D009652:Norpregnenes / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D045167:Progesterone Congeners / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology
D003277:Contraceptives, Oral, Combined; D009652:Norpregnenes; D045167:Progesterone Congeners; C044815:etonogestrel; D004997:Ethinyl Estradiol; D017135:Desogestrel