Metabolic Studies of High Doses of Allopurinol in Humans

  • Donald J. Nelson
  • Gertrude B. Elion
Part of the Advances in Experimental Medicine and Biology book series (AEMB, volume 165)


Allopurinol has been used for 16 years at doses ranging from 200 to 800 mg/day for the control of primary and secondary hyperuricemia. At the most commonly used doses of allopurinol (300–400 mg/ day) about 70% of the allopurinol is oxidized to oxipurinol, which is excreted in the urine. Urinary allopurinol and allopurinol riboside each account for about 10% of the dose. Since the degree of xanthine oxidase inhibition is dose-related, not only the oxidation of hypoxanthine and xanthine to uric acid, but also the oxidation of allopurinol to oxipurinol might be expected to be strongly inhibited at high doses of allopurinol. This would lead to increased levels of allopurinol, as well as allopurinol riboside, in plasma and urine. The extent to which this phenomenon occurs was investigated in several laboratory animal species and in man.


Uric Acid Xanthine Oxidase Metabolic Study Single Daily Dose Aldehyde Oxidase 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. 1.
    Elion, G. B., Kovensky, A. K., Hitchings, G. H., Metz, E., Rundles, W., Biochem. Pharm. 15: 863 (1966).PubMedCrossRefGoogle Scholar
  2. 2.
    Hitchings, G., Arth. and Rheum. 18: 863 (1975).CrossRefGoogle Scholar
  3. 3.
    Kelly, W. N., Beardmore, T. D., Science 169: 388 (1970).CrossRefGoogle Scholar
  4. 4.
    Krenitsky, T. A., Tuttle, J. V., Cattau, E. L., Wang, P., Comp. Biochem. and Physiol. 49B: 687 (1974).Google Scholar
  5. 5.
    Rundles, R. W., Metz, E. N., Silberman, H. R., Annals of Int. Med., 64: 229 (1966).Google Scholar
  6. 6.
    Schwartz, P. M., Dunigan, J. M., Marsh, J. C. Handschumacher, R. E., Cancer Research 40: 1885 (1980).PubMedGoogle Scholar
  7. 7.
    Sweetman, L., Fed. Proc. 27: 1055 (1968).PubMedGoogle Scholar
  8. 8.
    Weissman, S. M., Eisen, A. Z., Fallow, H. J., Lewis, M., Karon, M. J. Clin. Invest. 41: 1546 (1962).CrossRefGoogle Scholar

Copyright information

© Plenum Press, New York 1984

Authors and Affiliations

  • Donald J. Nelson
    • 1
  • Gertrude B. Elion
    • 1
  1. 1.Wellcome Research LaboratoriesBurroughs Wellcome Co.USA

Personalised recommendations