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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

Pharmacokinetics of sertindole in healthy young and elderly male and female subjects.

OBJECTIVE: The pharmacokinetic disposition of oral sertindole, a new selective antipsychotic compound, in young and elderly male and female subjects was investigated. STUDY DESIGN: A total of 46 subjects (12 young males, 11 elderly males, 11 young females, and 12 elderly females) received 4 mg/day sertindole (once a day; days 1 through 3) for 3 consecutive days, 8 mg/day sertindole for 3 consecutive days (days 4 through 6), and 12 mg/day sertindole for 10 consecutive days (days 7 through 16). RESULTS: Age and gender did not appear to have any effect on the plasma binding of sertindole, despite a lower albumin concentration in elderly subjects. After multiple dosing of 12 mg sertindole, the mean peak plasma concentration (Cmax) values for young and elderly female subjects were 20% and 31% higher than those observed for male subjects of comparable age (p < 0.05). The mean values for area under the plasma concentration-time curve [AUC(0-24)] of female subjects were 29% higher than those observed in male subjects of similar age (p < 0.05). There were no statistically significant age-related differences in Cmax and AUC(0-24) (or apparent total plasma clearance), and there were no gender- or age-related differences for the elimination rate constant or values for apparent volume of distribution during the terminal elimination phase after the last 12 mg dose on day 16 (p > 0.05). CONCLUSIONS: There are no differences between young and elderly subjects in the absorption and elimination of sertindole. The higher Cmax and AUC values in females may be a result of a higher extent of absorption or a dependence of sertindole clearance on lean body mass.[1]


  1. Pharmacokinetics of sertindole in healthy young and elderly male and female subjects. Wong, S.L., Cao, G., Mack, R.J., Granneman, G.R. Clin. Pharmacol. Ther. (1997) [Pubmed]
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