Pharmacokinetics of naproxen, its metabolite O‐desmethylnaproxen, and their acyl glucuronides in humans

  title={Pharmacokinetics of naproxen, its metabolite O‐desmethylnaproxen, and their acyl glucuronides in humans},
  author={T. Vree and M. van den Biggelaar-Martea and C. P. Verwey-van Wissen and J. B. Vree and P. Guelen},
  journal={Biopharmaceutics & Drug Disposition},
  • T. Vree, M. van den Biggelaar-Martea, +2 authors P. Guelen
  • Published 1993
  • Chemistry, Medicine
  • Biopharmaceutics & Drug Disposition
  • The aim of this investigation was to assess the pharmacokinetics of naproxen in 10 human subjects after an oral dose of 500 mg using a direct HPLC analysis of the acyl glucuronide conjugates of naproxen and its metabolite O‐desmethylnaproxen. The mean t1/2 of naproxen in 9 subjects was 24.7 ± 6.4 h (range 16 to 36 h). The t1/2 of 7.4 as found in subject number 10 must, therefore, be regarded as an extraordinary case (p <0.0153). Naproxen acyl glucuronide accounts for 50.8 ± 7.32 per cent of the… CONTINUE READING
    45 Citations

    Topics from this paper.

    Disposition of naproxen, naproxen acyl glucuronide and its rearrangement isomers in the isolated perfused rat liver
    • 9
    Conjugation of desmethylnaproxen in the rat--a novel acyl glucuronide-sulfate diconjugate as a major biliary metabolite.
    • 24
    • Highly Influenced
    • PDF
    Clinical Pharmacokinetics of Naproxen
    • 91
    Sulphation of o-desmethylnaproxen and related compounds by human cytosolic sulfotransferases.
    • 19
    Stereoselective binding properties of naproxen glucuronide diastereomers to proteins
    • 27
    Acyl Glucuronide Drug Metabolites: Toxicological and Analytical Implications
    • 226
    Acyl glucuronides: the good, the bad and the ugly.
    • 117


    Negligible excretion of unchanged ketoprofen, naproxen, and probenecid in urine.
    • 111
    Studies on the fate of naproxen. II. Metabolic fate in various animals and man.
    • 34
    Interindividual and interethnic differences in the demethylation and glucuronidation of codeine.
    • 105
    Pharmacokinetics and metabolism of codeine in humans
    • 92