A critical evaluation of the therapeutic benefits and side-effects of aminosalicylate analogues in the treatment of inflammatory bowel disease

Peppercorn MA. A critical evaluation of the therapeutic benefits and side-effects of aminosalicyiate analogues in the treatment of inflammatory bowel disease. Inflammopharmacology. 1993;2:263-276. Sulphasalazine, which consists of sulphapyridine linked to 5-amimosalicylic acid (5-ASA) via an azo bond, is efficacious in the therapy of active and remitted ulcerative colitis and active Crohn’s disease when the colon is involved. Its use is limited by a high incidence of adverse effects. Studies of sulphasalazine’s pharmacology suggested that it may be serving as a vehicle for delivery of its 5-ASA metabolite to distal disease sites. Toxicity studies revealed that most of the side-effects of sulphasalazine could be attributed to its sulpha moiety. These observations led to the development of a new group of agents, the aminosalicylates, based on sulphasalazine’s structure. Topical forms of 5-ASA have proved to be effective in active and remitted distal ulcerative colitis and proctitis. Oral forms of 5-ASA are as effective as sulphasalazine in active ulcerative colitis and in maintaining remission in ulcerative colitis and appear to be useful in active and remitted Crohn’s disease regardless of distribution. Eighty to ninety percent of patients intolerant of or allergic to sulphasalazine will tolerate an aminosalicyiate.