Linked Life Data

2147817

Source:http://linkedlifedata.com/resource/pubmed/id/2147817

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
6 Pt 2
pubmed:dateCreated
1991-1-22
pubmed:abstractText
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.
pubmed:keyword
http://linkedlifedata.com/resource/pubmed/keyword/Clinical Research, http://linkedlifedata.com/resource/pubmed/keyword/Comparative Studies, http://linkedlifedata.com/resource/pubmed/keyword/Contraception, http://linkedlifedata.com/resource/pubmed/keyword/Contraceptive Agents, http://linkedlifedata.com/resource/pubmed/keyword/Contraceptive Agents, Estrogen, http://linkedlifedata.com/resource/pubmed/keyword/Contraceptive Agents, Female, http://linkedlifedata.com/resource/pubmed/keyword/Contraceptive Agents..., http://linkedlifedata.com/resource/pubmed/keyword/Contraceptive Agents..., http://linkedlifedata.com/resource/pubmed/keyword/Contraceptive..., http://linkedlifedata.com/resource/pubmed/keyword/Contraceptive Methods, http://linkedlifedata.com/resource/pubmed/keyword/Demographic Factors, http://linkedlifedata.com/resource/pubmed/keyword/ETHINYL ESTRADIOL, http://linkedlifedata.com/resource/pubmed/keyword/Examinations And Diagnoses, http://linkedlifedata.com/resource/pubmed/keyword/Family Planning, http://linkedlifedata.com/resource/pubmed/keyword/Gestodene, http://linkedlifedata.com/resource/pubmed/keyword/Laboratory Examinations And Diagnoses, http://linkedlifedata.com/resource/pubmed/keyword/Levonorgestrel, http://linkedlifedata.com/resource/pubmed/keyword/Norethindrone, http://linkedlifedata.com/resource/pubmed/keyword/Oral Contraceptives, http://linkedlifedata.com/resource/pubmed/keyword/Population, http://linkedlifedata.com/resource/pubmed/keyword/Population Dynamics, http://linkedlifedata.com/resource/pubmed/keyword/Research Methodology, http://linkedlifedata.com/resource/pubmed/keyword/Studies, http://linkedlifedata.com/resource/pubmed/keyword/Time Factors
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
AIM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Dec
pubmed:issn
0002-9378
pubmed:author
pubmed:issnType
Print
pubmed:volume
163
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2132-7
pubmed:dateRevised
2006-11-15
pubmed:otherAbstract
PIP: Serum levels of 3-ketodesogestrel and ethinyl estradiol (EE) were analyzed by radioimmunoassay in a balanced crossover study with 2 tablet formulations containing desogestrel (0.150 mg) and EE (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: maximum serum concentration, time to maximum serum concentration, total area under the serum concentration vs time curve, and serum 1/2 life of elimination. The interindividual variation in these parameters was comparable with that observed with other contraceptive combinations containing EE and norethisterone, levonorgestrel, or gestodene. The serum distribution of contraceptive progestogens is known to be determined by their affinity to sex hormone- binding globulin (SHBG) and the concentration of SHBG. The authors analyzed the structural features that determine binding to SHBG; the 18- methyl group increased and the 11-methylene group weakened the binding to SHBG. 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 SHBG was much stronger than that of 3-ketodesogestrel and norethisterone.
pubmed:meshHeading
pubmed:year
1990
pubmed:articleTitle
Serum pharmacokinetics of orally administered desogestrel and binding of contraceptive progestogens to sex hormone-binding globulin.
pubmed:affiliation
Scientific Development Group, Organon International B.V., Oss, The Netherlands.
pubmed:publicationType
Journal Article, Comparative Study