Background and Aims: Budesonide is a highly potent topical glucocorticosteroid that is characterized by low systemic availability as a result of high first-pass hepatic metabolism. The aim of this study was to evaluate the efficacy and safety of three doses of an enema preparation of budesonide in patients with active distal ulcerative colitis/proctitis. Methods: In a double-blind multicenter trial, 233 patients were randomized to receive either a placebo enema or budesonide enema at a dose of 0.5 mg/100 mL, 2.0 mg/100 mL, or 8.0 mg/100 mL. The primary efficacy variables were an improvement of sigmoidoscopic inflammation grade, total histopathology score, and remission rates. Effects on cortisol concentrations were also assessed. Results: After 6 weeks of treatment, there was significant improvement in sigmoidoscopy and histopathology scores in the budesonide 2.0-mg and 8.0-mg dose groups compared with placebo. Remission was achieved in 19% of patients in the 2.0-mg budesonide group (P ≤ 0.050) and 27% of patients in the 8.0- mg budesonide group (P ≤ 0.001) compared with 4% in the placebo group. More than 90% of all budesonide patients had a normal adrenocorticotropin (ACTH)- stimulated cortisol response at the last visit. The budesonide enemas were well tolerated. Conclusions: Budesonide enema is both effective and safe for the treatment of active distal ulcerative colitis/proctitis. A dose of 2.0 mg/100 mL budesonide is the lowest effective dose.
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