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The pharmacokinetics of the novel promotile drug, tegaserod, are similar in healthy subjects—male and female, elderly and young
Author(s) -
AppelDingemanse S.,
Horowitz A.,
Campestrini J.,
Osborne S.,
Mcleod J.
Publication year - 2001
Publication title -
alimentary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 3.308
H-Index - 177
eISSN - 1365-2036
pISSN - 0269-2813
DOI - 10.1046/j.1365-2036.2001.00973.x
Subject(s) - tegaserod , medicine , pharmacokinetics , partial agonist , gastroenterology , agonist , irritable bowel syndrome , receptor
Background: Tegaserod (HTF 919) is a selective 5‐HT 4 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 t max ) were performed. Results: Tegaserod was well tolerated in all groups. There was no effect of age or gender on t max and C max . Gender did not affect AUC 0–∞ and AUC 0–tz ; there was a statistically significant effect of age on these parameters. AUC 0–∞ and AUC 0–tz in the elderly were greater than in the young ( AUC 0–∞ ratio 1.37, P < 0.001; AUC 0–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.