The pharmacokinetics of the novel promotile drug, tegaserod, are similar in healthy subjects-male and female, elderly and young.

Abstract

BACKGROUND:

Tegaserod (HTF 919) is a selective 5-HT4 receptor partial agonist in development for the treatment of irritable bowel syndrome.

AIM:

This study aimed to assess the effect of age and gender on the single-dose pharmacokinetics of tegaserod.

METHODS:

In a parallel-group, open-label study, a single dose of tegaserod (12 mg) was administered to four groups of healthy young male, young female, elderly male and elderly female subjects (n=10 per group). Blood samples were collected from 0 to 24 h postdose. Non-compartmental pharmacokinetics evaluation and statistical analysis (ANOVA and Wilcoxon signed ranks test for tmax) were performed.

RESULTS:

Tegaserod was well tolerated in all groups. There was no effect of age or gender on tmax and Cmax. Gender did not affect AUC0-infinity and AUC0-tz; there was a statistically significant effect of age on these parameters. AUC0-infinity and AUC0-tz in the elderly were greater than in the young (AUC0-infinity ratio 1.37, P < 0.001; AUC0-tz ratio 1.23, P=0.029). This increase in exposure is judged not to be clinically relevant because it is within the variability in the pharmacokinetics parameters of tegaserod and because the dose-response relationship of tegaserod is relatively shallow.

CONCLUSIONS:

No dose adjustment for age or gender is recommended in tegaserod therapy.

• Authors: S Appel-Dingemanse, A Horowitz, J Campestrini, S Osborne, J McLeod
• Journal: Alimentary pharmacology & therapeutics (Aliment Pharmacol Ther) Vol. 15 Issue 7 Pg. 937-44 (Jul 2001) ISSN: 0269-2813 [Print] England
• PMID: 11421867 (Publication Type: Clinical Trial, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Indoles
• Serotonin Receptor Agonists
• tegaserod

Topics

• Adolescent
• Adult
• Age Factors
• Aged
• Aged, 80 and over
• Area Under Curve
• Dose-Response Relationship, Drug
• Female
• Gastrointestinal Diseases (drug therapy)
• Humans
• Indoles (pharmacokinetics)
• Male
• Peristalsis (drug effects)
• Serotonin Receptor Agonists (pharmacology)
• Sex Factors