Serum concentrations of ethinylestradiol, 3-keto-desogestrel, SHBG, CBG and gonadotropins during treatment with a biphasic oral contraceptive containing desogestrel
Abstract
During a cross-over study, the pharmacokinetics of ethinylestradiol (EE) and 3-keto-desogestrel (KDG) were investigated on days 7 and 22 of one cycle of treatment with two biphasic formulations containing 50 micrograms EE (7 tablets) and 50 micrograms EE + 125 micrograms desogestrel (DG) (15 tablets) (50/50 EE) or 40 micrograms EE + 25 micrograms DG (7 tablets) and 30 micrograms EE + 125 micrograms DG (15 tablets) (40/30 EE). Peak serum levels and areas under the curve of EE increased significantly by 50% between days 7 and 22 of those taking 50/50 EE, while during treatment with 40/30 EE, no difference was found between days 7 and 22. Both formulations caused identical KDG levels on day 22. There were only slight differences in the effects of both preparations on sex-hormone-binding globulin (SHBG; +150 to +160%) and on corticosteroid-binding globulin (CBG; +130 to +150%) on day 7. On day 22, the changes were more pronounced with 50/50 EE (SHBG, +310%; CBG, +240%) than with 40/30 EE (SHBG, +250%; CBG, +180%). On day 22 after discontinuation of treatment, the SHBG and CBG levels were still significantly above the control values. Using both formulations, LH and FSH levels were significantly suppressed on day 22, while on day 7 no significant reduction was observed. The rise in the EE levels between days 7 and 22 of 50/50 EE intake and the time course of the EE concentrations during treatment with 40/30 EE appear to be due to an inhibition of hepatic metabolism by the contraceptive steroids, as EE is nearly exclusively bound to albumin which does not change.
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The COC-induced increase of CBG plateaus after just over a week of COC use and weans off 4 to 6 weeks after discontinuation.
“This COC-induced increase of CBG plateaus after just over a week of COC use and weans off 4 to 6 weeks after discontinuation (11, 13-17).”
From Salivary Cortisol and Cortisone Can Circumvent Confounding Effects of Oral Contraceptives in the Short Synacthen Test (2024) · cites this paper as [15]
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White, T., Özel, B. Z., Jain, J. K., & Stanczyk, F. Z. (2006) · Contraception · doi:10.1016/j.contraception.2006.04.005 · Cited by 66 · see citing works
“Sex-hormonebinding globulin (SHBG) has been studied extensively in OC users; it appears that the EE-stimulated increase is counterbalanced by the dose and type of progestin [4–8].”
BackgroundPharmacokinetics and Pharmacodynamics of a Transdermal Contraceptive Patch and an Oral Contraceptive
Devineni, D., Skee, D. M., Vaccaro, N. M., Massarella, J. W., Janssens, L., LaGuardia, K. D., & LEUNG, A. T. (2007) · The Journal of Clinical Pharmacology · doi:10.1177/0091270006297919 · Cited by 62 · see citing works
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Aden, U., Jung-Hoffmann, C., & Kühl, H. (1998) · Contraception · doi:10.1016/s0010-7824(98)00071-7 · Cited by 63 · see citing works
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“Eligible subjects for inclusion were healthy females aged between 18 and 45 years with mild to moderate acne vulgaris [13].”
BackgroundSchuder, S. (2005) · Annals of the New York Academy of Sciences · doi:10.1196/annals.1356.036 · Cited by 16 · see citing works
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Kränzlin, H. T., & Nap, M. A. (2006) · The European Journal of Contraception & Reproductive Health Care · doi:10.1080/13625180500252638 · Cited by 11 · see citing works
van den Ende, A., Geurts, T. B. P., & Kloosterboer, H. J. (1997) · The European Journal of Contraception & Reproductive Health Care · doi:10.3109/13625189709167473 · Cited by 9 · see citing works
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Present Role of Hormonal Contraception in Family Planning
Benagiano, G., Bastianelli, C., Farris, M., & Brosens, I. (2018) · Reproductive medicine for clinicians · doi:10.1007/978-3-319-78009-2_11
- Authors
- Jung-Hoffmann, C., Storch, A., & Kuhl, H.
- Affiliations
- Goethe University Frankfurt (DE)
- Venue
- Hormone Research
- Publisher
- S. Karger AG
- Published
- 2008-12-03
- Volume
- 38
- Issue
- 3-4
- Pages
- 184-189
- ISSN
- 0301-0163 (ISSN-L)
- 1423-0046
- OpenAlex
- W2025984032
- Cited by
- 15
- References
- 0
- Citations by year
- 2024: 1 · 2020: 1 · 2018: 1 · 2014: 1 · 2012: 1
- FWCI
- 0.00
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Hormone Research (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Reproductive Health and Contraception
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
- Health Sciences › Medicine › Reproductive Medicine › Hypothalamic control of reproductive hormones
- Keywords
- ethinyl estradiol, desogestrel, pharmacokinetics, sex hormone-binding globulin, corticosteroid-binding globulin, gonadotropins, luteinizing hormone, follicle-stimulating hormone, albumin binding, contraceptive formulations
- MeSH terms
- Adult, Contraceptives, Oral, Hormonal, Ethinyl Estradiol, Female, Follicle Stimulating Hormone, Humans, Kinetics, Luteinizing Hormone, Sex Hormone-Binding Globulin, Transcortin, Desogestrel
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