Biliary excretion of acetaminophen in ureter-ligated rats.
Over one fourth (28.4%) of a 100 mg/kg intravenous dose of acetaminophen (AA) is excreted into bile of conscious rats within 8 h. The main metabolite in bile was the glucuronide (14.3%), followed by the sulfate (8.2%), the glutathione conjugate (4.7%) and unchanged AA (1.2%). In rats with bilateral ligation of the ureters, the amount of total AA excreted into bile was significantly increased to 37.8% of the dose; this enhanced excretion was a consequence of augmented amounts of glucuronide (20.3%) and sulfate (12.0%) whereas the amount of the glutathione conjugate in bile was slightly diminished (4.2%). During renal failure, increased biliary elimination of AA conjugates, mainly as the sulfate, seems to partially compensate the lack of renal excretion.
D000082:Acetaminophen / Q000031:analogs & derivatives / Q000032:analysis* / Q000378:metabolism; D000818:Animals; D001646:Bile / Q000378:metabolism*; D007676:Kidney Failure, Chronic / Q000378:metabolism*; D008026:Ligation; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013464:Sulfuric Acids / Q000378:metabolism; D014513:Ureter / Q000502:physiology
D013464:Sulfuric Acids; D000082:Acetaminophen; C037386:acetaminophen glucuronide; C034780:3-(glutathion-S-yl)acetaminophen