SUMMARY Suppositories of sulphapyridine, 5-aminosalicylic acid, and placebo were used in 45 patients with idiopathic proctitis to determine the active part of sulphasalazine. Each patient used one of the suppositories twice daily for four weeks in a double-blind controlled trial. Complete clinical remission with normal rectal mucosa on sigmoidoscopy occurred in 60% of patients given 5-aminosalicylic acid, but in only 13% and 27% of those given sulphapyridine and placebo respectively. Twelve patients were included twice. tn eight of these patients 5-aminosalicylic acid was given one time and sulphapyridine (two patients) or placebo (six patients) another time. Clinical remission occurred in each patient with 5-aminosalicylic acid, but in only one patient during other therapy. The results suggest that 5-aminosalicylic acid is the active therapeutic moiety of sulphasalazine.Salicylazosulphapyridine (Salazopyrin, sulphasalazine, SASP) is widely used in the treatment of ulcerative colitis and Crohn's disease. Several controlled trials have established its value in mild and moderately active colitis ' and in maintenance therapy to prevent recurrence of the disease3 4. Its value in Crohn's disease has not yet been established. SASP is composed of sulphapyridine (SP) in azo linkage with 5-aminosalicylic acid (5-ASA). After an oral dose of SASP in man, only a small fraction is absorbed in the small bowel. Most of the drug reaches the colon and is almost completely split at the diazo bond by bacterial azo-reductases into SP and 5-ASA.5 6 SP is then mostly absorbed and partially metabolised in the liver (acetylation and glucuronidation) before excretion in the urine. Most of the 5-ASA moiety can be recovered in the faeces and only a small portion is found in the urine as the acetylated form.7The mode of action of SASP remains unknown.As SASP is particularly effective in the treatment of *Address for reprint requests: P A M van
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