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Protein binding of the contraceptive steroids gestodene, 3-keto-desogestrel and ethinylestradiol in human serum.
J Steroid Biochem. 1990 Feb; 35(2):313-8.JS

Abstract

The protein binding of ethinylestradiol (EE2), gestodene (GEST) and 3-keto-desogestrel (KDG) has been determined by ultrafiltration in the serum of women who had either taken a gestodene (n = 37) or desogestrel (n = 28) containing oral contraceptive for a time period of at least 3 months. GEST and KDG were analyzed in individual serum pools whereas EE2 was repeatedly measured in two serum pools, each one representing one treatment group. The respective free fractions of the three steroids were 0.6 +/- 0.1% (GEST), 2.5 +/- 0.2% (KDG), 1.7 +/- 0.6% (EE2, in the gestodene-group) and 1.5 +/- 0.2% (EE2, in the desogestrel-group). EE2 was exclusively bound to albumin, whereas GEST and KDG were also bound to sex-hormone-binding globulin (SHBG). The distribution of the two progestins over the serum binding proteins was determined after heat-treatment of serum samples. For GEST, the contribution of albumin and SHBG was 24.1 +/- 9.1 and 75.3 +/- 9.1%, respectively and for KDG it was 65.9 +/- 11.9 and 31.6 +/- 12.0%, respectively. SHBG and corticosteroid-binding globulin (CBG) concentrations were measured in the serum samples obtained from both treatment groups. In the gestodene-group 180 +/- 61 nmol/l (SHBG) and 89 +/- 13 mg/l (CBG) were measured, the corresponding values in the desogestrel-group were 226 +/- 64 nmol/l (SHBG) and 93 +/- 14 mg/l (CBG). SHBG concentrations were correlated with the total concentration of GEST and its free fraction and a positive (r = 0.395) and negative (r = -0.491) correlation respectively was found. Only a weak negative correlation (r = -0.291) was found for SHBG and the free fraction of KDG in the serum. These data demonstrate that the three contraceptive steroids EE2, GEST and KDG were all bound extensively to serum proteins, however, with pronounced differences concerning their distribution over the various binding proteins.

Authors+Show Affiliations

Research Laboratories, Schering AG, Berlin, F.R.G.No affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

2308344

Citation

Kuhnz, W, et al. "Protein Binding of the Contraceptive Steroids Gestodene, 3-keto-desogestrel and Ethinylestradiol in Human Serum." Journal of Steroid Biochemistry, vol. 35, no. 2, 1990, pp. 313-8.
Kuhnz W, Pfeffer M, al-Yacoub G. Protein binding of the contraceptive steroids gestodene, 3-keto-desogestrel and ethinylestradiol in human serum. J Steroid Biochem. 1990;35(2):313-8.
Kuhnz, W., Pfeffer, M., & al-Yacoub, G. (1990). Protein binding of the contraceptive steroids gestodene, 3-keto-desogestrel and ethinylestradiol in human serum. Journal of Steroid Biochemistry, 35(2), 313-8.
Kuhnz W, Pfeffer M, al-Yacoub G. Protein Binding of the Contraceptive Steroids Gestodene, 3-keto-desogestrel and Ethinylestradiol in Human Serum. J Steroid Biochem. 1990;35(2):313-8. PubMed PMID: 2308344.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Protein binding of the contraceptive steroids gestodene, 3-keto-desogestrel and ethinylestradiol in human serum. AU - Kuhnz,W, AU - Pfeffer,M, AU - al-Yacoub,G, PY - 1990/2/1/pubmed PY - 1990/2/1/medline PY - 1990/2/1/entrez KW - Biology KW - Contraception KW - Contraceptive Agents, Estrogen--analysis KW - Contraceptive Agents, Female--analysis KW - Contraceptive Agents--analysis KW - Data Analysis KW - Endocrine System KW - Ethinyl Estradiol--analysis KW - Examinations And Diagnoses KW - Family Planning KW - Hematological Effects KW - Hemic System KW - Hormones--analysis KW - Laboratory Examinations And Diagnoses KW - Physiology KW - Research Methodology KW - Serum Protein Effects SP - 313 EP - 8 JF - Journal of steroid biochemistry JO - J Steroid Biochem VL - 35 IS - 2 N2 - The protein binding of ethinylestradiol (EE2), gestodene (GEST) and 3-keto-desogestrel (KDG) has been determined by ultrafiltration in the serum of women who had either taken a gestodene (n = 37) or desogestrel (n = 28) containing oral contraceptive for a time period of at least 3 months. GEST and KDG were analyzed in individual serum pools whereas EE2 was repeatedly measured in two serum pools, each one representing one treatment group. The respective free fractions of the three steroids were 0.6 +/- 0.1% (GEST), 2.5 +/- 0.2% (KDG), 1.7 +/- 0.6% (EE2, in the gestodene-group) and 1.5 +/- 0.2% (EE2, in the desogestrel-group). EE2 was exclusively bound to albumin, whereas GEST and KDG were also bound to sex-hormone-binding globulin (SHBG). The distribution of the two progestins over the serum binding proteins was determined after heat-treatment of serum samples. For GEST, the contribution of albumin and SHBG was 24.1 +/- 9.1 and 75.3 +/- 9.1%, respectively and for KDG it was 65.9 +/- 11.9 and 31.6 +/- 12.0%, respectively. SHBG and corticosteroid-binding globulin (CBG) concentrations were measured in the serum samples obtained from both treatment groups. In the gestodene-group 180 +/- 61 nmol/l (SHBG) and 89 +/- 13 mg/l (CBG) were measured, the corresponding values in the desogestrel-group were 226 +/- 64 nmol/l (SHBG) and 93 +/- 14 mg/l (CBG). SHBG concentrations were correlated with the total concentration of GEST and its free fraction and a positive (r = 0.395) and negative (r = -0.491) correlation respectively was found. Only a weak negative correlation (r = -0.291) was found for SHBG and the free fraction of KDG in the serum. These data demonstrate that the three contraceptive steroids EE2, GEST and KDG were all bound extensively to serum proteins, however, with pronounced differences concerning their distribution over the various binding proteins. SN - 0022-4731 UR - https://www.unboundmedicine.com/medline/citation/2308344/Protein_binding_of_the_contraceptive_steroids_gestodene_3_keto_desogestrel_and_ethinylestradiol_in_human_serum_ L2 - https://antibodies.cancer.gov/detail/CPTC-SERPINA6-1 DB - PRIME DP - Unbound Medicine ER -