Budesonide for the treatment of ulcerative colitis

Abstract

Budesonide is a synthetic corticosteroid characterized by enhanced topical potency and limited systemic bioavailability. Its use in ulcerative colitis (UC) was limited to rectal preparations until recently when the new oral budesonide formulation incorporating the multi-matrix system technology was introduced. The purpose of this review is to evaluate the current role of oral and rectal budesonide in managing UC patients Areas covered: In this paper, we described the chemical structure and pharmacologic characteristics of the different oral and rectal budesonide preparations, provided a summary of the published trials that evaluated the efficacy and safety of budesonide in UC, and discussed the current status of its use in this population Expert opinion: Budesonide is effective in inducing remission in a subset of patients with mild-moderate UC. Nevertheless, the current evidence suggests inferiority of oral budesonide to 5-aminosalisylates (5-ASA) and systemic steroids, whereas rectal applications are comparable to other rectal steroid preparations, but still inferior to rectal 5-ASA. In clinical practice, several issues need clarification including, its exact position in the line of induction agents; the role of combining budesonide and 5-ASAs; the role of combining oral and rectal budesonide; and the role of budesonide in maintenance therapy.

Keywords: Ulcerative colitis; budesonide; inflammatory bowel disease; steroids.

Figure 1. Molecular structure of Budesonide and its two metabolites

Figure adapted with permission from: G Jönsson, A Aström, and P Andersson, Budesonide is metabolized by cytochrome P450 3A (CYP3A) enzymes in human liver, Drug Metab Dispos January 1995 23:137-14218

Figure 2

Rates of remission (clinical and endoscopic) reported from combined CORE I and CORE II trials and Rubin et al study