The effects of tegaserod (HTF 919) on oesophageal acid exposure in gastro-oesophageal reflux disease

Aliment Pharmacol Ther. 2000 Nov;14(11):1503-9. doi: 10.1046/j.1365-2036.2000.00854.x.


Background: Tegaserod (HTF 919), a 5-HT4 receptor partial agonist, has prokinetic effects that might be useful in decreasing acid reflux in gastro-oesophageal reflux disease (GERD).

Methods: To investigate the potential clinical utility of tegaserod in GERD, a five-period crossover study (balanced Latin square) was designed to evaluate the efficacy of 4 b.d. doses of tegaserod vs. placebo. Four-hour manometry (1 h fasting and 3 h postprandial) with continuous recording of lower oesophageal sphincter pressure and distal oesophageal pH, was performed at the end of each 2-week treatment period in 19 patients with mild-to-moderate GERD. Recordings were scored for mean lower oesophageal sphincter pressure, number of transient lower oesophageal sphincter relaxations, and distal oesophageal acid exposure.

Results: Tegaserod (1 mg/day and 4 mg/day) caused a more than 50% decrease in acid exposure in the postprandial period in patients with abnormal acid exposure, although only the 1 mg/day tegaserod treatment elicited statistically significant decreasing (P < 0.05) for the entire treatment group (percentage time for which pH < 4: placebo=13%; 1 mg/day dose=5%; 4 mg/day dose=8%). A decreased number of reflux episodes was demonstrated with both the 1 mg/day and 4 mg/day tegaserod doses. There was no apparent effect on mean lower oesophageal sphincter pressure, whilst transient lower oesophageal sphincter relaxations frequency decreased in the 1-2.5 h post-dose.

Conclusions: Tegaserod in a dose of 1 mg/day causes a significant decrease in postprandial oesophageal acid exposure. The reduction in oesophageal acid exposure with tegaserod treatment may result from enhanced oesophageal acid clearance, improved gastric emptying, and/or reduced transient lower oesophageal sphincter relaxations.

Publication types

  • Clinical Trial
  • Multicenter Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Cross-Over Studies
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Esophagogastric Junction / drug effects*
  • Female
  • Gastric Acid / metabolism
  • Gastroesophageal Reflux / drug therapy*
  • Gastrointestinal Agents / administration & dosage
  • Gastrointestinal Agents / therapeutic use*
  • Humans
  • Indoles / administration & dosage
  • Indoles / therapeutic use*
  • Male
  • Manometry
  • Postprandial Period
  • Pressure
  • Treatment Outcome


  • Gastrointestinal Agents
  • Indoles
  • tegaserod