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Capacity-limited gut wall metabolism of 5-aminosalicylic acid, a therapeutically active metabolite of sulfasalazine, in rats.

H J Pieniaszek·T R Bates
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Abstract

The metabolic fate of 5-aminosalicylic acid (reported to be the active therapeutic moiety of sulfasalazine) was assessed in fasting rats as a function of dose (25-200 mg/kg) and administration route (oral, intraperitoneal, and intravenous). 5-Aminosalicylic acid is subject to both capacity-limited presystemic (apparently during first passage through the intestinal epithelium) and systemic acetylation. The possibility exists that 5-aminosalicylic acid also is acetylated presystemically after oral sulfasalazine administration to patients with inflammatory bowel disease. Any alteration in the absorption activity if N-acetyl-5-aminosalicylic acid is inactive or less active than 5-amino-salicylic acid.

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AcetylationAdministration, OralAminosalicylic AcidsAnimalsBiotransformationDose-Response Relationship, DrugInjections, IntraperitonealInjections, IntravenousIntestinal MucosaMaleRatsSulfasalazineJournal ArticleResearch Support, U.S. Gov't, P.H.S.

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H J Pieniaszek, T R Bates. 1979. Capacity-limited gut wall metabolism of 5-aminosalicylic acid, a therapeutically active metabolite of sulfasalazine, in rats.. https://doi.org/10.1002/jps.2600681036

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Increased acetylation of H3K14 in the genomic regions that encode trained immunity enzymes in lysophosphatidylcholine-activated human aortic endothelial cells - Novel qualification markers for chronic disease risk factors and conditional DAMPs.

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