title: Biliary excretion and choleretic effect of cefmetazole in rats.
abstract: The effect of cefmetazole, a broad-spectrum cephalosporin, on bile flow and composition in rats was studied. Intravenous injection of cefmetazole at doses ranging from 40 to 400 mumol/kg of body weight led to an increase in its biliary concentration and excretion rate, with a maximum at 30 min after injection. Excretion of cefmetazole into bile was associated with a marked choleresis. The magnitude of the increase in bile flow was dose dependent, with a maximal increase at a dose of 200 mumol/kg. Cefmetazole administration did not affect the secretion of bile acids or their osmotic activities, whereas the bile acid-independent bile flow increased by 49% at a dose of 200 mumol/kg. Cefmetazole administration at a dose of 200 mumol/kg significantly increased the biliary outputs of sodium, potassium, chloride, and bicarbonate (+36, +56, +28, and +31%, respectively) compared with outputs of controls. A linear relationship was observed between bile flow and cefmetazole excretion, 44 microliters of bile being produced per mumol of cefmetazole excreted into bile. Our results demonstrate that cefmetazole induces choleresis by stimulating bile acid-independent bile flow. This effect appears to be partly due to the osmotic properties of cefmetazole transported into bile.
authors.affiliation: Department of Physiology, Pharmacology, and Toxicology, University of León, Spain.
authors.forename: J
authors.initials: J
authors.lastname: Gonzalez
authors.forename: C
authors.initials: C
authors.lastname: Fernandez
authors.forename: E
authors.initials: E
authors.lastname: Marińo
authors.forename: A
authors.initials: A
authors.lastname: Morales
authors.forename: R
authors.initials: R
authors.lastname: Jimenez
mesh_terms: D000818:Animals; D001646:Bile / Q000187:drug effects / Q000378:metabolism*; D015311:Cefmetazole / Q000378:metabolism* / Q000494:pharmacology; D002756:Cholagogues and Choleretics; D007275:Injections, Intravenous; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains
chemical_list: D002756:Cholagogues and Choleretics; D015311:Cefmetazole