Abstract
Studies on the metabolism and pharmacokinetics of allopurinol have shown that the principal metabolic product, oxipurinol (4,6-dihydroxypyrazolo(3,4-d)pyrimidine), is formed rapidly and has a prolonged plasma half-life1. The plasma half-life of allopurinol is in the range of 0.5–1 hour, while that of oxipurinol has been reported to range from 18 to 30 hours1,2. Since oxipurinol binds very tightly to the reduced form of xanthine oxidase3,4 and inactivates the enzyme, its inhibitory effects on urate synthesis are apparent long after allopurinol itself has been cleared from the body.
This is a preview of subscription content, log in via an institution.
Buying options
Tax calculation will be finalised at checkout
Purchases are for personal use only
Learn about institutional subscriptionsPreview
Unable to display preview. Download preview PDF.
References
G.B. Elion, A. Kovensky, G.H. Hitchings, E. Metz and R.W. Rundles, Metabolic studies of allopurinol, an inhibitor of xanthine oxidase, Biochem. Pharmacol. 15:863 (1966).
G.B. Elion, T.-F. Yü, A.B. Gutman and G.H. Hitchings, Renal clearance of oxipurinol, the chief metabolite of allopurinol, Amer. J. Med. 45:69 (1968).
V.Massey, H. Komai, G. Palmer and G.B. Elion, On the mechanism of inactivation of xanthine oxidase by allopurinol and other pyrazolo(3,4-d)pyrimidines, J. Biol. Chem. 245:2837 (1970).
T. Spector and D.G. Johns, Stoichiometric inhibition of reduced xanthine oxidase by hydroxypyrazolo(3,4-d)pyrimidines, J. Biol. Chem. 245:5079 (1978).
R.W. Rundles, J.B. Wyngaarden, G.H. Hitchings, G.B. Elion and H.R. Silberman, Effects of a xanthine oxidase inhibitor on thiopurine metabolism, hyperuricemia, and gout, Trans. Assoc. Amer. Physicians 76:126 (1963).
G.P. Rodnan, J.A. Robin, S.F. Tolchin and G.B. Elion, Allopurinol and gouty hyperuricemia. Efficacy of a single daily dose, J. Amer. Med. Assoc. 231:1143 (1975).
C.P. Hayes, Jr., E.N. Metz, R.R. Robinson, and R.W. Rundles, Use of allopurinol (HPP) to control hyperuricemia in patients on chronic intermittent dialysis. Trans. Amer. Soc. Artif. Intern. Organs 11:247 (1965).
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1980 Plenum Press, New York
About this chapter
Cite this chapter
Elion, G.B., Benezra, F.M., Beardmore, T.D., Kelley, W.N. (1980). Studies with Allopurinol in Patients with Impaired Renal Function. In: Rapado, A., Watts, R.W.E., De Bruyn, C.H.M.M. (eds) Purine Metabolism in Man-III. Advances in Experimental Medicine and Biology, vol 122A. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-9140-5_43
Download citation
DOI: https://doi.org/10.1007/978-1-4615-9140-5_43
Publisher Name: Springer, Boston, MA
Print ISBN: 978-1-4615-9142-9
Online ISBN: 978-1-4615-9140-5
eBook Packages: Springer Book Archive