Therapeutic benefits of budesonide in gastroenterology

Abstract

Budesonide is a synthetic steroid of the glucocorticoid family with a high topical antiinflammatory activity. Enteric-coated formulations resist gastric-acid degradation, delivering active drug to the small intestine and proximal colon. Budesonide has a high first-pass metabolism with minimal systemic absorption. It is therefore felt to cause fewer side effects than traditional glucocorticosteroids and to be generally well tolerated. The aim of this paper is to examine the utility of this medication in frequently encountered gastrointestinal conditions: Crohn's disease, ulcerative colitis, microscopic colitis and eosinophilic oesophagitis. A Medline search was performed to find published original research and review articles relating to the use budesonide in common gastroenterological conditions. The results showed that budesonide is efficacious in the induction and short-term maintenance of Crohn's disease. Budesonide is the best-documented treatment for microscopic colitis. It is well proven to be effective in the induction of remission in collagenous colitis but its use in lymphocytic colitis remains less well documented. In conclusion, budesonide is an effective glucocorticosteroid therapy for many chronic gastrointestinal diseases. In combination with its efficacy, the low incidence of serious side effects associated with this drug should keep it at the forefront in the therapeutic arsenal of any gastroenterologist.

p38 Mitogen activated protein kinase (MAPK): a new therapeutic target for reducing the risk of adverse pregnancy outcomes

“…This technique may thus be designed to exert a specific effect at the drug administration site, and then be rapidly metabolized to inactive compounds upon circulation [124,129]. One of the most successful therapeutic agents for IBD was shown to be highly metabolized to inactive forms in the liver [130]. This technique minimizes systemic off-target effects of the parent drug and thus raises the question as to whether it can be designed for PTB or pPROM, i.e., can the drug be targeted to the placenta or fetal membranes cells considering its rapid degradation (or metabolism to an inactive form) by maternal tissues.…”

FK506-Binding Protein 5 mRNA Levels in Ileal Mucosa Are Associated with Pouchitis in Patients with Ulcerative Colitis

“…Even the use of steroids has been advocated in the treatment of primary or persistent pouchitis [33][34][35]. FK506 has also been reported as being effective in refractory pouchitis [4][5][6].…”

Long-term safety and efficacy of budesonide in the treatment of ulcerative colitis

“…The reason for budesonide’s minimal systemic absorption lies in the high first-pass effect (over 90%) which is carried out by hepatic cytochrome P450 (CYP3A4 and CYP3A5) enzymes. Once metabolized, it is transforms into two metabolites, 6β-hydroxybudesonide and 16α-hydroxyprednisolone, with negligible glucocorticoid activity (less than 1%) which does not contribute to budesonide’s therapeutic action 3,13,20…”

“…Budesonide’s efficacy in treating microscopic colitis in both histological forms, collagenous colitis, and lymphocytic colitis, has been demonstrated in several reviews2,3 and in the European Consensus 10. There has been a recent publication demonstrating budesonide’s higher response rate and lower risk of recurrence when compared to prednisone in patients with microscopic colitis 11…”

“…Budesonide (9 mg per day) was the preferred treatment because it was associated with fewer side effects and demonstrated usefulness in replacing conventional systemic glucocorticoids in CD patients. However, budesonide’s efficacy in maintaining remission is controversial and published studies conclude that although this drug may delay relapse after medically induced remission, it is not effective at maintaining remission for 12 months 3,5–7…”