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Related Experiment Videos

Review article: tegaserod.

M Camilleri1

  • 1Enteric Neuroscience Program, Gastroenterology Research Unit, Mayo Clinic and Mayo Foundation, Rochester, MN 55905, USA. camilleri.michael@mayo.edu

Alimentary Pharmacology & Therapeutics
|February 24, 2001
PubMed
Summary

Tegaserod, a selective 5-HT4 receptor agonist, effectively treats constipation-predominant irritable bowel syndrome by improving bowel function and reducing abdominal pain. This drug demonstrated safety and tolerability in clinical trials, with transient diarrhea as the main side effect.

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Area of Science:

  • Pharmacology
  • Gastroenterology

Background:

  • Tegaserod is a serotonin derivative and a selective partial agonist for the 5-HT4 receptor.
  • It exhibits high affinity for the 5-HT4 receptor and is absorbed rapidly after oral administration.

Purpose of the Study:

  • To evaluate the efficacy and safety of tegaserod in patients with constipation-predominant irritable bowel syndrome (IBS-C).
  • To assess the drug's pharmacokinetic and pharmacodynamic properties.

Main Methods:

  • Three large, randomized, double-blind, placebo-controlled Phase III trials were conducted, primarily in female patients with IBS-C.
  • Pharmacokinetic studies analyzed absorption, distribution, metabolism, and excretion.
  • Pharmacodynamic studies investigated effects on gastrointestinal motility and sensation in animals and humans.

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Main Results:

  • Tegaserod demonstrated efficacy in improving global assessment of relief and secondary endpoints like abdominal pain, bowel frequency, and consistency in IBS-C patients.
  • Pharmacokinetic studies showed linear absorption and excretion mainly via bile as N-glucuronides.
  • Pharmacodynamic studies confirmed stimulation of peristalsis, increased motility, and accelerated transit in the gastrointestinal tract.

Conclusions:

  • Tegaserod is an effective and well-tolerated treatment for constipation-predominant irritable bowel syndrome.
  • The drug's safety profile is favorable, with transient diarrhea being the most common adverse event.