Antimetabolite Therapy in Ulcerative Colitis: Azathioprine, 6-Mercaptopurine, and Methotrexate

Abstract

Ulcerative colitis (UC) is a lifelong, immune-mediated inflammatory condition of the colonic mucosa, which is characterized by a relapsing and remitting course (Sandborn, Gastroenterology 135(5):1442–1447, 2008). The primary goals of therapy in the treatment of UC are to induce remission of patient’s symptoms as rapidly as possible and to maintain remission on a long-term basis. By reducing the episodes of relapse, it is possible to reduce the risk of long-term complications and improve patient quality of life. Corticosteroids remain one of the most effective therapies for inducing remission in patients with moderate to severe UC. However, approximately 50–80 % of patients in whom corticosteroids are prescribed will experience a rapid relapse of symptoms. Antimetabolite therapy has found widespread use for corticosteroid-dependent patients in clinical practice, although the data supporting the use of thiopurines—azathioprine and mercaptopurine—and methotrexate are more robust in steroid-dependent Crohn’s disease than in UC. This chapter will review the current state of the art regarding the thiopurine drugs and methotrexate for the treatment of UC.