Category: pharmacological
Aliases: Azulfidine
Sulfonamide-mesalamine prodrug — gut bacteria cleave the azo bond releasing 5-ASA (anti-inflammatory, mesalamine-active component) + sulfapyridine (mostly side-effect-driver). Used for IBD + rheumatoid arthritis (DMARD). PK (Azulfidine label, parent species): Absolute F < 15% for parent — most of a PO dose is cleaved by colonic bacteria to sulfapyridine (F 60%, well-absorbed) + 5-aminosalicylic acid (F 10–30%, poorly absorbed, locally active). Vdss 7.5 ± 1.6 L from IV data, t½ 7.6 ± 3.4 h. The "PK" recorded here is for the parent — the clinical effect is driven by 5-ASA topically in the colon for UC and by an undefined immunomodulatory mechanism for RA.
PO: 7.6h