Research Article| Volume 38, ISSUE 4, P477-486, October 1988

Alterations in the serum levels of gestodene and SHBG during 12 cycles of treatment with 30 μg ethinylestradiol and 75 μg gestodene

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      The serum concentrations of gestodene have been measured radioimmunologically in 11 female volunteers on Day 1, 10, and 21 of the 1st, 3rd, 6th, and 12th cycle of treatment with an oral contraceptive containing 30 μg ethinylestradiol and 75 μg gestodene during the first 4 hours and 24 hours after intake.
      During the 1st cycle the maximal gestodene levels increased from 2.1 to 6.2 ng/ml on Day 1 to values between 7.5 and 22.0 ng/ml on Day 21. During the 3rd and 6th treatment cycle the levels were still higher with maxima between 10.1 and 26.3 ng/ml, while during the 12th cycle the gestodene concentrations were slightly lower.
      The serum levels of SHBG rose significantly during intake of the pill up to values between 210 and 240 nmol/l on Day 21 of each cycle, and were reduced to a certain degree during the pill-free interval. The SHBG concentrations correlated closely with the area under the gestodene concentration-versus-time curves (AUC) indicating a pronounced influence of serum protein binding upon the pharmacokinetics of gestodene.
      The gestodene levels of the individual women remained relatively constant during the 12 treatment cycles, although great interindividual differences were found. It is concluded that the relatively high serum concentrations of gestodene are not only based on the binding to SHBG, but probably also on an impeded metabolism of gestodene.
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        • März W.
        • Gross W.
        • Gahn G.
        • Romberg G.
        • Taubert H.-D
        • Kuhl H.
        A randomized crossover comparison of two low-dose contraceptives: Effects on serum lipids and lipoproteins.
        Am. J. Obstet. Gynecol. 1985; 153: 287-293
        • Orme M.L'E.
        • Back D.J.
        • Breckenridge A.M.
        Clinical pharmacokinetics of oral contraceptive steroids.
        Clin. Pharmacokinetics. 1983; 8: 95-136
        • Kuhl H.
        • Jung-Hoffmann C.
        • Heidt F.
        Serum levels of 3-keto-desogestrel and SHBG during 12 cycles of treatment with 30 ug ethinylestradiol and 150 ug desogestrel.
        Contraception. 1988; 38: 381-390
        • Hümpel M.
        • Wendt H.
        • Pommerenke G.
        • Weiβ C.
        • Speck U.
        Investigations of pharmacokinetics of levonorgestrel to specific consideration of a possible first-pass effect in women.
        Contraception. 1978; 17: 207-220
        • Lähteenmäki P.
        • Nilsson C.G.
        Plasma concentrations of ethinylestradiol and d-norgestrel during two immediate postabortal oral contraceptive cycles.
        Contraception. 1978; 17: 9-17
        • Back D.J.
        • Bates M.
        • Breckenridge A.M.
        • Hall J.M.
        • MacIver M.
        • Orme M.L'E.
        • Park B.K.
        • Rowe P.H.
        The pharamcokinetics of levonorgestrel and ethinylestradiol in women - studies with Ovran and Ovranette.
        Contraception. 1981; 23: 229-239
        • Back D.J.
        • Breckenridge A.M.
        • Crawford F.E.
        • McIver M.
        • Orme M.L'E.
        • Park B.K.
        • Rowe P.H.
        • Smith E.
        Kinetics of norethindrone in women. I. Radioimmunoassay and concentrations during multiple dosing.
        Clin. Pharmacol. Ther. 1978; 24: 439-447
        • Cekan S.Z.
        • Jia M.
        • Landgren B.-M.
        • Diczfalusy E.
        The interaction between sex hormone binding globulin and levonorgestrel released from vaginal rings in women.
        Contraception. 1985; 31: 431-439
        • Victor A.
        • Weiner E.
        • Johansson E.D.B.
        Sex hormone binding globulin: the carrier protein for d-norgestrel.
        J. Clin. Endocrinol. Metab. 1976; 43: 244-247
        • Anderson D.C.
        Sex-hormone-binding globulin.
        Clin. Endocrinology. 1974; 3: 69-95
        • Siiteri P.K.
        • Murai J.T.
        • Hammond G.L.
        • Nisker J.A.
        • Raymoure W.J.
        • Kuhn R.W.
        The serum transport of steroid hormones.
        Rec. Progr. Horm. Res. 1982; 38: 457-503
        • Hammond G.L.
        • Langley M.S.
        • Robinson P.A.
        • Nummi S.
        • Lund L.
        Serum steroid binding protein concentrations, distribution of progestogens, and bioavailability of testosterone during treatment with contraceptives containing desogestrel or levonorgestrel.
        Fertil. Steril. 1984; 42: 44-51
        • Bergink E.W.
        • Hamburger A.D.
        • de Jager E.
        • van der Vies J.
        Binding of a contraceptive progestogen Org 2969 and its metabolites to receptor proteins and human sex hormone binding globulin.
        J. Steroid Biochem. 1981; 14: 175-183
        • Jung-Hoffmann C.
        • Kuhl H.
        Divergent effects of two low-dose oral contraceptives on sex hormone-binding globulin and free testosterone.
        Am. J. Obstet. Gynecol. 1987; 156: 199-203
        • Pollow K.
        Endocrine-pharmacological profile of gestodene.
        (unpublished results; cited by Elger, W.:)in: XIth World Congress of Gynecology and Obstetrics, Berlin1985
        • Düsterberg B.
        • Tack J.-W.
        • Krause W.
        • Hümpel M.
        Pharmacokinetics and biotransformation of gestodene in man.
        in: Elstein M. Gestodene: Development of a new gestodene-containing low dose oral contraceptive. Proceedings of a Special Satellite Symposium held in conjunction with the XIth World Congress of Gynecology and Obstetrics. Parthenon Publishing, U.K1987: 35-44