Tegaserod for Constipation-Predominant Irritable Bowel Syndrome

Authors

  • Pramodini B. Kale-Pradhan Pharm.D.,

    Corresponding author
    1. Department of Pharmacy Practice, Wayne State University
    2. Department of Pharmacy, St. John Hospital and Medical Center and the Department of Pharmacy, Harper University Hospital Detroit, Michigan.
    Search for more papers by this author
  • Sheila M. Wilhelm Pharm.D.

    1. Department of Pharmacy Practice, Wayne State University
    2. Department of Pharmacy, Harper University Hospital Detroit, Michigan.
    Search for more papers by this author

Pramodini Kale-Pradhan, Pharm.D., Department of Pharmacy Practice, Wayne State University, 22101 Moross Road, Detroit, MI 48236–2172; e-mail: pkale@wayne.edu.

Abstract

Tegaserod, a selective and partial agonist at the 5-hydroxytryptamine (5-HT [serotonin]) receptor subtype 4 (5-HT4), is the only United States Food and Drug Administration–approved drug for the treatment of constipation-predominant irritable bowel syndrome (IBS) in women. The drug's stimulation of 5-HT4 receptors on intestinal enterocytes increases peristaltic activity and fluid secretion into the gut lumen, facilitating stool passage. In addition, affinity of tegaserod for 5-HT4 receptors modulates visceral sensitivity, which helps alleviate abdominal pain associated with constipation-predominant IBS. The drug's pharmacokinetic and pharmacodynamic parameters do not differ significantly with age or sex. Tegaserod safely and effectively relieves overall gastrointestinal symptoms and abdominal discomfort and normalizes bowel habits in patients with constipation-predominant IBS. It is associated with few drug interactions. In clinical studies, tegaserod was well tolerated, and its adverse-effect profile was similar to that of placebo. Severe diarrhea, as well as abdominal pain, flatulence, headache, and nausea, were the most commonly reported events. Patients who experience severe diarrhea should discontinue the drug. With the data available, tegaserod remains an option for patients with constipation-predominant IBS.

Ancillary