Tacrolimus is a macrolide immunosuppressant that is structurally similar to rapamycin and has been found to have potent immunosuppressive properties, showing 10- to 100-fold higher potency for inhibiting lymphocyte activation than cyclosporine A (CsA). Because less variability in absorption and serum levels is observed among patients treated with tacrolimus compared with those who receive oral CsA, tacrolimus has been suggested to be more easily and safely administered to patients with refractory ulcerative colitis (UC) than CsA. However, because oral tacrolimus has a slower onset of action than intravenous CsA and food intake is known to reduce tacrolimus serum trough levels due to its low absorption rate, the proper method for administration of oral tacrolimus has not been determined. Moreover, the long-term effects of oral tacrolimus also remain unclear. In this chapter, key issues regarding the use of oral tacrolimus in patients with UC are reviewed.
Part of the book: New Insights into Inflammatory Bowel Disease