Tegaserod maleate in the treatment of irritable bowel syndrome: A clinical review

Background: Approved in July 2002, tegaserod maleate is a partial 5-hydroxytryptamine 4-receptor agonist used to improve symptoms of constipation-predominant irritable bowel syndrome (IBS). The physiologic actions of tegaserod relate to its ability to stimulate gastric and intestinal motility. Objective: This article reviews available data on the pharmacokinetic and pharmacodynamic properties and clinical efficacy of tegaserod. Methods: Searches of MEDLINE and PubMed from 1966 to the present were conducted using the search terms tegaserod, tegaserod maleate, irritable bowel syndrome, and Rome criteria. Abstracts presented at national meetings between 1997 and 2002 were reviewed and included if perceived to be reliable and relevant. Results: In clinical trials, tegaserod was associated with significantly better scores on the subject's global assessment of relief compared with placebo (P < 0.05). The absolute efficacy of tegaserod compared with placebo varied between trials and averaged 10% to 12%. Tegaserod had a good safety profile; diarrhea was the only adverse effect that occurred more often in tegaserod recipients than in placebo recipients. No electrocardiographic changes were observed at therapeutic concentrations of tegaserod. Long-term (1-year) treatment with tegaserod appeared to be well tolerated. The recommended dosage for patients aged >18 years with constipation-predominant IBS is 6 mg PO BID before meals for 4 to 6 weeks, with an additional 4 to 6 weeks of treatment if initial therapy is partially effective. Conclusions: The addition of tegaserod to the arsenal of moderately effective medications currently used in the treatment of IBS may be helpful in patients with constipation-predominant IBS. Continuous postmarketing surveillance and reporting of adverse reactions are essential to further characterize the safety profile of this new agent. Copyright (C) 2003 Excerpta Medica, Inc.