Document Detail


The metabolic disposition of norgestrel in female rhesus monkeys.
MedLine Citation:
PMID:  35318     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Following single intragastric doses of d- and dl-[24C]norgestrel (Ng), rhesus monkeys excreted 29.5 +/- 2.0 (SE) and 52.6 +/- 5.4% of the administered radioactivity in urine. Fecal excretion accounted for 57.1 +/- 4.0 and 37.2 +/- 4.4%, respectively. Urinary radioactivity was separated into neutral, acidic, and conjugated fractions. The neutral and conjugated fractions contained Ng; 2 alpha, 16 alpha- and 16 beta-hydroxy-Ng; 3 alpha,5 beta-tetrahydro-Ng and 16 beta-hydroxy-3 alpha,5 beta-tetrahydro-Ng and their glucuronides. However, the bulk of the radioactivity in these fractions was associated with more polar metabolites. The acidic fraction contained unstable metabolies which lose 14CO2 at pH values below 5. The most abundant of these metabolites was isolated as its stable methyl ester. The structure of a 13-ethyl-D-homogon-4-ene-3,17 alpha-dione-17 carboxylic acid is proposed for the metabolite which decomposes to 13-ethyl-D-homogon-4-ene-3,17 alpha-dione [D-homo-G]. The probable mechanism of the metabolite's formation is postulated. Quantitative differences in urinary metabolite patterns were observed following the administration of d- and dl-Ng. Ng is the major identified drug-related entity in plasma. The d-Ng concentrations in plasma measured by radioimmunoassay were in good agreement with those determined by fractionation and radiometry. The latter method indicated the presence of D-homo-G and a glucuronide of 3 alpha,5 beta-tetrahydro-Ng following the administration of d- and dl-Ng.
Authors:
S F Sisenwine; H B Kimmel; A L Liu; H W Ruelius
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Drug metabolism and disposition: the biological fate of chemicals     Volume:  7     ISSN:  0090-9556     ISO Abbreviation:  Drug Metab. Dispos.     Publication Date:    1979 Jan-Feb
Date Detail:
Created Date:  1979-07-16     Completed Date:  1979-07-16     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  9421550     Medline TA:  Drug Metab Dispos     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1-6     Citation Subset:  IM    
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MeSH Terms
Descriptor/Qualifier:
Animals
Female
Haplorhini
Keto Acids / metabolism
Macaca mulatta
Norgestrel / metabolism*,  urine
Phenols / urine
Time Factors
Chemical
Reg. No./Substance:
0/Keto Acids; 0/Phenols; 6533-00-2/Norgestrel

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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