BUDESONIDE - A REVIEW OF ITS PHARMACOLOGICAL PROPERTIES AND THERAPEUTIC EFFICACY IN INFLAMMATORY BOWEL-DISEASE

Budesonide is a glucocorticoid with high topical activity; but low sys temic bioavailability which results in reduced systemic effects in com parison with other glucocorticoids. To date, it has been evaulated for use in patients with inflammatory bowel disease when administered eit her orally as a controlled ileal release formulation or rectally as an enema. In comparative trials, daily treatment with budesonide enema 2 mg/100ml for 4 weeks produced endoscopic remission or improvement in 46 to 84% of patients with active distal ulcerative colitis and/or pro ctitis and histological remission or improvement in 45 to 68%. In gene ral, this regimen was a effective as regimens of hydrocortisone, methy lprednisolone, prednisolone or mesalazine (5-amino-salicylic acid, mes alamine) enemas, but caused less suppression of plasma cortisol levels than the other glucocarticoids. Oral treatment with controlled releas e budesonide 9 mg/day for 8 weeks produces clinical remission in 42 to 67% of patients with active Crohn's disease of the ileum, ileocaecal region and/or ascending colon and significantly reduces Crohn's diseas e activity index scores compared with baseline and placebo. Results of a quality-of-life questionnaire reflected these clinical improvements . Budesonide has similar efficacy to prednisolone. Response to budeson ide is maintained after dosage tapering at 8 weeks. Compared with plac ebo, maintenance treatment with oral budesonide 3 or 6 mg/day increase s the duration of remission in patients with Crohn's disease, but does not appear to affect the 1-year relapse rate. Thus, budesonide, admin istered rectally to patients with distal ulcerative colitis or proctit is or orally to patients with Crohn disease of the ileum, ileocaecal r egion and/or ascending colon, is a favourable option for the treatment of acute exacerbations of inflammatory bowel disease. Because of the low incidence of adverse glucocorticoid-related effects associated wit h oral budesonide, it may also be a useful agent for longer term maint enance therapy if further clinical trials confirm its efficacy in this indication.