title: Interaction between drug acetylation and ethanol, acetate, pyruvate, citrate, and L(-) carnitine in isolated rat liver parenchymal cells.
abstract: The acetylation of sulfanilamide and procainamide in suspensions of isolated rat parenchymal cells was studied in absence and presence of ethanol (33mM), citrate (4 mM), pyruvate (4 mM), and L(-)carnitine (2 mM). Ethanol treatment enhanced the sulfanilamide acetylation whereas the acetylation of procainamide was considered to be unchanged. Acetate (1-5 mM), citrate, and pyruvate treatment enhanced the acetylation of both sulfanilamide and procainamide. Acetate (4 mM) increased both Km and Vmax of both sulfanilamide and procainamide acetylation. Combined treatment with L(-)carnitine and either acetate, pyruvate, or citrate enhanced the acetylation rate of sulfanilamide more than acetate, pyruvate, or citrate, respectively alone. In cell suspensions treated with L(-) carnitine and acetate or pyruvate, the acetylation kinetics of sulfanilamide changed from zero-to apparent first-order. With procainamide as test drug, a further increase of the acetylation rate was found when L(-) carnitine was added to citrate pyruvate. Acetyl-CoA increased the rate of sulfanilamide acetylation in rat liver homogenates in a dose dependent manner.
mesh_terms: D000085:Acetates / Q000494:pharmacology; D000107:Acetylation; D000123:Acetyltransferases / Q000378:metabolism; D000818:Animals; D002331:Carnitine / Q000494:pharmacology; D002951:Citrates / Q000494:pharmacology; D004347:Drug Interactions; D000431:Ethanol / Q000494:pharmacology; D066298:In Vitro Techniques; D008099:Liver / Q000187:drug effects* / Q000378:metabolism; D008297:Male; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D011342:Procainamide / Q000378:metabolism; D011773:Pyruvates / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013424:Sulfanilamides / Q000378:metabolism
chemical_list: D000085:Acetates; D002951:Citrates; D004364:Pharmaceutical Preparations; D011773:Pyruvates; D013424:Sulfanilamides; D000431:Ethanol; D000123:Acetyltransferases; D011342:Procainamide; D002331:Carnitine