Efficacy of Rebamipide Enemas in Active Distal Ulcerative Colitis and Proctitis: A Prospective Study Report

Abstract

Rebamipide has a broad spectrum of pharmacological actions that include suppression of neutrophil functions and stimulation of mucosal epithelial cell regeneration by increasing the expression of epithelial growth factor (EGF) and the EGF receptor. Sixteen patients with active ulcerative colitis (UC; mild in 1 patient, moderate in 11, and severe in 4) were recruited. Enemas containing 150 mg rebamipide per dosing were administered during the daytime after passage of stool, twice a day for 4 weeks. UC disease activity index (UC-DAI), endoscopic activity index (EAI), and Floren's grading (FG) of mucosal biopsy specimens were measured at entry and at 4 weeks. Five of 16 patients did not complete the study, and therefore, final efficacy assessment was done on 11 patients who completed the 4 weeks of treatment. Improvements were observed in UC-DAI (P = 0.0049), EAI (P = 0.0043), and FG (P = 0.0084). There was no serious rebamipide-related side effect in any of the 16 patients. In conclusion, rebamipide topical therapy appears to be effective for the treatment of mildly to moderately active distal UC. Further controlled studies are warranted for this promising drug.

Novel topical therapies for distal colitis

“…Histological improvement and clinical remission in 9 patients was demonstrated after 12 wk of twice daily administration of 150 mg rebamipide in 1.5% carboxymethylcellulose at pH 6.34. A further open-labelled study demonstrated clinical remission in 5 of 16 patients while another 2 demonstrated a marked improvement after 4 wk of therapy [68] . The final open-labelled study treated 20 patients for 3 wk with 11 achieving clinical remission and 16 responding endoscopically [69] .…”

Ulcerative proctitis: an update on the pharmacotherapy and management

“…Rebamipide, an agent suppressing neutrophil function and stimulating epithelial cell regeneration, induced significant clinical, endoscopical and histological improvement when administered as enemas in patients with proctitis or distal colitis [56]. Case series have shown that elective appendectomy can be associated with clinical improvement or complete resolution of symptoms [57,58].…”

Current and Future Biological Treatments in Inflammatory Bowel Disease

“…It aids mucosal healing by stimulating local prostaglandin synthesis and epithelial cell regeneration via up-regulation of EGF and its receptor, neutrophil suppression, and decreased production of inflammatory cytokines stimulated by NSAIDs and/or H pylori [46]. A small open-label trial in which twice daily Rebamipide enemas were given to patients with UC proctitis for one month demonstrated significant clinical, endoscopic and histopathologic improvement [47].…”