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  • Title: Furosemide pharmacokinetics and pharmacodynamics following gastroretentive dosage form administration to healthy volunteers.
    Author: Klausner EA, Lavy E, Stepensky D, Cserepes E, Barta M, Friedman M, Hoffman A.
    Journal: J Clin Pharmacol; 2003 Jul; 43(7):711-20. PubMed ID: 12856384.
    Abstract:
    The objective of this study was to evaluate the pharmacokinetic and pharmacodynamic properties of furosemide following gastroretentive dosage from (GRDF) administration. A furosemide (60 mg) GRDF, releasing the drug during 6 hours in vitro, or an immediate-release tablet was administered to healthy male volunteers (N = 14) in a crossover design. Food and liquid intake were standardized; urine was collected, weighed, and assayed for furosemide and sodium concentrations. Pharmacokinetics of furosemide following the GRDF administration, as compared to the tablet, showed lower Cmax and indicated a prolonged absorption phase leading to longer mean residence time in the stomach. The sustained input of the drug significantly improved diuretic and natriuretic efficiencies during the first 5 hours and thereby increased the total effects measured over 24 hours. The unfolding controlled-release GRDF of furosemide improved the pharmacodynamic actions due to the sustained absorption in the stomach and jejunum, which delayed the body's counteractivity to the drug effect.
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