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Serum was sampled for 12\u2003h post\u2010dose to measure alosetron concentrations.<\/jats:p><jats:p><jats:bold>Results\u2002<\/jats:bold> Serum concentrations of alosetron were higher in females than in males, resulting from a sex difference in clearance by metabolism. Mean clearance values were 504 <jats:italic>vs<\/jats:italic> 677\u2003ml\u2003min<jats:sup>\u22121<\/jats:sup> in young females <jats:italic>vs<\/jats:italic> males (mean ratio 0.75), and 461 <jats:italic>vs<\/jats:italic> 670\u2003ml\u2003min<jats:sup>\u22121<\/jats:sup> in elderly females <jats:italic>vs<\/jats:italic> males (mean ratio 0.69). The sex difference in alosetron pharmacokinetics achieved statistical significance in the elderly, but not in the young. Irrespective of sex, alosetron clearance was increased by smoking. Serum concentrations tended to be higher in the elderly, although the effect of age was generally not significant. 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