Pharmacokinetic properties of zolpidem in elderly and young adults: possible modulation by testosterone in men

Aims  The influence of ageing on the pharmacokinetics of zolpidem, an extensively prescribed hypnotic medication, was evaluated in healthy human volunteers. Methods  A series of 16 elderly (age: 61–85 years) and 24 young (age: 22–42 years) volunteers received single 5 mg oral doses of zolpidem tartr...

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Veröffentlicht in:British journal of clinical pharmacology 2003-09, Vol.56 (3), p.297-304
Hauptverfasser: Olubodun, Joel O., Ochs, Hermann R., Von Moltke, Lisa L., Roubenoff, Ronenn, Hesse, Leah M., Harmatz, Jerold S., Shader, Richard I., Greenblatt, David J.
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Sprache:eng
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Zusammenfassung:Aims  The influence of ageing on the pharmacokinetics of zolpidem, an extensively prescribed hypnotic medication, was evaluated in healthy human volunteers. Methods  A series of 16 elderly (age: 61–85 years) and 24 young (age: 22–42 years) volunteers received single 5 mg oral doses of zolpidem tartrate. Serum zolpidem concentrations were determined by HPLC with fluorescence detection in samples drawn during 8 h after dosage. The effect of testosterone on zolpidem biotransformation was evaluated in vitro using human liver microsomes. Possible induction of CYP3A protein expression and function was studied in cultured human hepatocytes. Results  Among men, apparent oral clearance of zolpidem was decreased in elderly compared to young subjects (3.8 vs 11.0 ml min−1 kg−1, P 
ISSN:0306-5251
1365-2125
DOI:10.1046/j.0306-5251.2003.01852.x