Oral contraceptives stimulate the excretion of clofibric acid glucuronide in women and female rats.
1. Glucuronidation of clofibric acid, the pharmacologically active form of the hypolipidemic drug clofibrate was investigated in a human population, either in vitro with liver homogenates from biopsies, or after ingestion of the drug and determination of the urinary metabolite. No difference in the glucuronidation rate according to age of the patients was observed. Bilirubin but not clofibric acid glucuronidation was significantly higher in women (106% increase), when expressed per gram of tissue. 2. The excretion of clofibryl glucuronide in women who took oral contraceptives was significantly enhanced by 25%. 3. In female rats, treatment with the contraceptive agent norethindrone also stimulated by 48% the formation of clofibrylglucuronide in liver microsomes.
Liu
H F
HF
Laboratoire de Chimie Analytique, U.R.A. CNRS 597, Faculté des Sciences Pharmaceutiques et Biologiques, Nancy, France.
Magdalou
J
J
Nicolas
A
A
Lafaurie
C
C
Siest
G
G
D000328:Adult; D000818:Animals; D001663:Bilirubin / Q000097:blood; D002995:Clofibric Acid / Q000031:analogs & derivatives / Q000652:urine*; D003278:Contraceptives, Oral, Hormonal / Q000494:pharmacology*; D004997:Ethinyl Estradiol / Q000494:pharmacology; D005260:Female; D014453:Glucuronosyltransferase / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D007527:Isoenzymes; D008099:Liver / Q000201:enzymology; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology; D008875:Middle Aged; D009640:Norethindrone / Q000494:pharmacology; D011506:Proteins / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains
D003278:Contraceptives, Oral, Hormonal; D007527:Isoenzymes; D011506:Proteins; D004997:Ethinyl Estradiol; D002995:Clofibric Acid; C030678:clofibric pyranoglucuronate; D014453:Glucuronosyltransferase; D001663:Bilirubin; D009640:Norethindrone