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Ulcerative Colitis Therapy: Maximizing the Use of 5-ASA Agents


These agents remain the mainstay of therapy for the majority of patients with the disease.

The 5-ASA agents (sulfasalazine, mesalamine, and balsalazide, all derivatives of salicylic acid) remain the mainstay of therapy for the majority of patients with ulcerative colitis, suggested Sunanda V. Kane, MD, MSPH, Mayo Clinic College of Medicine, Rochester, Minnesota, in a presentation at 2012 Advances in Inflammatory Bowel Diseases, the Crohn’s & Colitis Foundation’s Clinical & Research Conference, in Hollywood, Florida.

Dr Kane’s discussion was a welcome reality check in the midst of a conference that tended to focus on the newest, most expensive biologic agents (anti–tumor necrosis factor [anti-TNF] agents). Cost and concerns about life-threatening adverse effects (malignancy and infection) limit more widespread use of the anti-TNF agents and, in general, have prevented their use as first-line agents.

No evidence exists to support any claim of superiority of one 5-ASA agent over any other, although there may be some value in combining two 5-ASA agents to maximize absorption, Dr Kane noted.

Given therapeutic equivalency, insurance considerations often determine the preferred 5-ASA for a given patient, and e-Prescribing systems may simplify the process by preemptively alerting physicians to insurance-approved formulary.

Still, the 5-ASA agents, which are effective for mild to moderate ulcerative colitis, may be limited by noncompliance because of adverse effects, most frequently GI symptoms.

Historically, this led to recommendations for bid or qid dosing with food; no evidence base supported the recommendation, and recent studies have shown that it is unnecessary.

Dr Kane reviewed the pharmacokinetic literature on 5-ASA at some length. Comparing single doses with multiple doses, the weight of evidence suggests no significant difference in maximum drug delivery over the entire colon or individual colonic segments.

Further, there is no evidence for differences in efficacy or safety when comparing bid, tid, and qid dosing and no evidence to support claims of a superior adverse-effect profile for delayed-release preparations.

Dr Kane asked the audience, “Are you finding that the 5-ASA preparation you prescribed isn’t working?” Consider whether there may be concurrent infection. “Are you treating symptoms not attributable to inflammatory activity?” “Irritable bowel syndrome or other functional condition?” “Incorrect diagnosis?” Finally, “consider whether this patient has more severe disease than your original assessment indicated-at that point, consider second-line agents or combination therapy.”

Dr Kane disclosed that she is a consultant to Shire Pharmaceuticals, manufacturer of Pentasa® (mesalamine).

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