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

Background: Tegaserod (HTF 919) is a selective 5-HT4 receptor partial agoni st 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 sample s were collected from 0 to 24 h postdose. Non-compartmental pharmacokinetic s 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-infinity) a nd AUC(0-tz); there was a statistically significant effect of age on these parameters. AUC(0-infinity) and AUC(0-tz) in the elderly were greater than in the young (AUC(0-infinity) 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 releva nt because it is within the variability in the pharmacokinetics parameters of tegaserod and because the dose-response relationship of tegaserod is rel atively shallow. Conclusions: No dose adjustment for age or gender is recommended in tegaser od therapy.