Capacity-limited gut wall metabolism of 5-aminosalicylic acid, a therapeutically active metabolite of sulfasalazine, in rats
✍ Scribed by Henry J. Pieniaszek; Theodore R. Bates
- Publisher
- John Wiley and Sons
- Year
- 1979
- Tongue
- English
- Weight
- 393 KB
- Volume
- 68
- Category
- Article
- ISSN
- 0022-3549
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✦ Synopsis
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.