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Serum pharmacokinetics of orally administered desogestrel and binding of contraceptive progestogens to sex hormone-binding globulin.
Am J Obstet Gynecol. 1990 Dec; 163(6 Pt 2):2132-7.AJ

Abstract

Serum levels of 3-ketodesogestrel and ethinyl estradiol were analyzed by radioimmunoassay in a balanced crossover study with two tablet formulations containing desogestrel (0.150 mg) and ethinyl estradiol (0.030 mg) in 25 women under steady-state conditions after 21 days of treatment. The pharmacokinetic properties of desogestrel were characterized by the following parameters: (1) maximum serum concentration, (2) time to maximum serum concentration, (3) total area under the serum concentration versus time curve, and (4) serum half-life of elimination. The interindividual variation in these parameters was comparable with that observed with other contraceptive combinations containing ethinyl estradiol and norethisterone, levonorgestrel, or gestodene. The serum distribution of contraceptive progestogens is known to be determined by their affinity to sex hormone-binding globulin and the concentration of sex hormone-binding globulin. We analyzed the structural features that determine binding to sex hormone-binding globulin. The 18-methyl group increased and the 11-methylene group weakened the binding to sex hormone-binding globulin. The double bond at C-15 reinforced the binding only when combined with an 18-methyl group. Therefore, the binding of levonorgestrel (the 18-methyl derivative of norethisterone) and gestodene (the delta-15,18 methyl derivative of norethisterone) to sex hormone-binding globulin was much stronger than that of 3-keto-desogestrel and norethisterone.

Authors+Show Affiliations

Scientific Development Group, Organon International B.V., Oss, The Netherlands.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

2147817

Citation

Bergink, W, et al. "Serum Pharmacokinetics of Orally Administered Desogestrel and Binding of Contraceptive Progestogens to Sex Hormone-binding Globulin." American Journal of Obstetrics and Gynecology, vol. 163, no. 6 Pt 2, 1990, pp. 2132-7.
Bergink W, Assendorp R, Kloosterboer L, et al. Serum pharmacokinetics of orally administered desogestrel and binding of contraceptive progestogens to sex hormone-binding globulin. Am J Obstet Gynecol. 1990;163(6 Pt 2):2132-7.
Bergink, W., Assendorp, R., Kloosterboer, L., van Lier, W., Voortman, G., & Qvist, I. (1990). Serum pharmacokinetics of orally administered desogestrel and binding of contraceptive progestogens to sex hormone-binding globulin. American Journal of Obstetrics and Gynecology, 163(6 Pt 2), 2132-7.
Bergink W, et al. Serum Pharmacokinetics of Orally Administered Desogestrel and Binding of Contraceptive Progestogens to Sex Hormone-binding Globulin. Am J Obstet Gynecol. 1990;163(6 Pt 2):2132-7. PubMed PMID: 2147817.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Serum pharmacokinetics of orally administered desogestrel and binding of contraceptive progestogens to sex hormone-binding globulin. AU - Bergink,W, AU - Assendorp,R, AU - Kloosterboer,L, AU - van Lier,W, AU - Voortman,G, AU - Qvist,I, PY - 1990/12/1/pubmed PY - 1990/12/1/medline PY - 1990/12/1/entrez KW - Clinical Research KW - Comparative Studies KW - Contraception KW - Contraceptive Agents KW - Contraceptive Agents, Estrogen KW - Contraceptive Agents, Female KW - Contraceptive Agents, Female--pharmacodynamics KW - Contraceptive Agents, Progestin--pharmacodynamics KW - Contraceptive Agents--pharmacodynamics KW - Contraceptive Methods KW - Demographic Factors KW - Desogestrel--pharmacodynamics KW - Ethinyl Estradiol KW - Examinations And Diagnoses KW - Family Planning KW - Gestodene KW - Laboratory Examinations And Diagnoses KW - Levonorgestrel KW - Norethindrone KW - Oral Contraceptives KW - Population KW - Population Dynamics KW - Research Methodology KW - Studies KW - Time Factors SP - 2132 EP - 7 JF - American journal of obstetrics and gynecology JO - Am J Obstet Gynecol VL - 163 IS - 6 Pt 2 N2 - Serum levels of 3-ketodesogestrel and ethinyl estradiol were analyzed by radioimmunoassay in a balanced crossover study with two tablet formulations containing desogestrel (0.150 mg) and ethinyl estradiol (0.030 mg) in 25 women under steady-state conditions after 21 days of treatment. The pharmacokinetic properties of desogestrel were characterized by the following parameters: (1) maximum serum concentration, (2) time to maximum serum concentration, (3) total area under the serum concentration versus time curve, and (4) serum half-life of elimination. The interindividual variation in these parameters was comparable with that observed with other contraceptive combinations containing ethinyl estradiol and norethisterone, levonorgestrel, or gestodene. The serum distribution of contraceptive progestogens is known to be determined by their affinity to sex hormone-binding globulin and the concentration of sex hormone-binding globulin. We analyzed the structural features that determine binding to sex hormone-binding globulin. The 18-methyl group increased and the 11-methylene group weakened the binding to sex hormone-binding globulin. The double bond at C-15 reinforced the binding only when combined with an 18-methyl group. Therefore, the binding of levonorgestrel (the 18-methyl derivative of norethisterone) and gestodene (the delta-15,18 methyl derivative of norethisterone) to sex hormone-binding globulin was much stronger than that of 3-keto-desogestrel and norethisterone. SN - 0002-9378 UR - https://www.unboundmedicine.com/medline/citation/2147817/Serum_pharmacokinetics_of_orally_administered_desogestrel_and_binding_of_contraceptive_progestogens_to_sex_hormone_binding_globulin_ L2 - https://linkinghub.elsevier.com/retrieve/pii/0002-9378(90)90553-J DB - PRIME DP - Unbound Medicine ER -