Inducing and maintaining remission in ulcerative colitis: role of high-dose, extended-release mesalamine.

In mild-to-moderate inflammatory bowel disease, particularly ulcerative colitis, 5-aminosalicylic acid (5-ASA) remains a cornerstone of therapy. Sulfasalazine, originally synthesized in 1940 as an arthritis treatment for Sweden's King Gustaf V, is an azo-linked compound between 5-ASA and sulfapyridine. This medication was soon discovered to be effective in treating ulcerative colitis. However, dose-related side effects of the sulfapyridine moiety led to considerable effort in developing medications to deliver 5-ASA to the desired parts of the intestine. The newest generation of 5-ASA medications allows high-dose medication delivery with decreased pill burden, thereby improving patient compliance. This review will describe the pharmacokinetics of various 5-ASA preparations, particularly focusing on high-dose formulations and their role in therapy; will examine current scientific literature; and will review clinical outcomes and safety profiles.