Clinical pharmacology of mesalazine (5-aminosalicylic acid) in chronic inflammatory bowel disease

Abstract

Several new salicylate compounds have been developed in recent years as a result of intensive clinical research with sulphasalazine (SZ). Since its discovery in 1941 SZ has been used as a kind of standard drug in the treatment of chronic inflammatory bowel disease (IBD); especial benefit has been obtained in the management of ulcerative colitis patients. However, therapy with this azo-compound is often limited by dose-dependent side effects and intolerance (for review see references 1 and 2). The mode of action of SZ is still unknown but metabolic and clinical studies have raised the question of whether it is the entire molecule or a metabolite that is the therapeutic principal. In the first controlled clinical trials it was realized that 5-aminosalicylic acid, a major primary metabolite of SZ (now renamed mesalazine) represents the active therapeutic moiety 3–5. During the last few years these initial studies have been confirmed by numerous investigations and clinical experience with mesalazine has been accumulating. Nowadays this salicylate has a well-established place in the treatment of IBD, especially for such patients as are sensitive to SZ6–9.