European Journal of Clinical Pharmacology

, Volume 19, Issue 6, pp 431–435 | Cite as

Pharmacokinetics and biotransformation of benzbromarone in man

  • H. Ferber
  • H. Vergin
  • G. Hitzenberger


After administration of a single oral dose of benzbromarone 100 mg to 7 subjects, the maximum serum level was 1.84±0.87 mg/l, and the elimination halflife was 2.77±1.07 h. The major metabolite, benzarone, could be detected in serum 3 h after administration of benzbromarone, and the maximum serum benzarone level of 0.79±0.21 mg/l occurred after 6 h. Benzarone had an elimination half-life from serum of 13.52±2.18 h. Both substances were excreted mainly via the liver and bile. In urine only benzarone β-glucuronide could be detected; it amounted to 1.55% of the benzbromarone dose.

Key words

benzbromarone benzarone blood levels pharmacokinetics biotransformation excretion 


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  1. 1.
    Zöllner N, Griebsch A, Fink JK (1970) On the effect of benzbromarone on serum uric acid levels and uric acid excretion in patients with gout. Dtsch Med Wochenschr 95: 2405–2412Google Scholar
  2. 2.
    Jain AK, Ryan JR, McMahon FG, Novek RJ (1974) Effect of single oral doses of benzbromarone on Serum and Urinary uric acid. Arthritis Rheum 17: 149Google Scholar
  3. 3.
    Kramp R, Lenoix R (1975) Distal permeability of urate and effects of benzofuran derivatives in the rat kidney. Am J Physiol 228: 875–883Google Scholar
  4. 4.
    Delbarre F, Auscher C, Oliver J, Rose A (1967) Traitement des hyperuricemics et de lagoutte par des clerives du benzofuranne. Sem Hop Paris 43: 1127–1133Google Scholar
  5. 5.
    Yu T (1976) Pharmacokinetics and clinical studies of a new uricosuric agent-benzbromarone. J Rheumatol 3: 305–312Google Scholar
  6. 6.
    Broekhuysen J, Pacco R, Sion L, Demeulenaese M, van Hel (1972) Metabolism of benzbromarone in man. Eur J Clin Pharmacol 4: 125–130Google Scholar
  7. 7.
    Rothe W, Schellhorn J (1977) Vorschlag einer Arzneibuchmethode zur Prüfung der Auflösungsrate von Wirkstoffen. Pharm Ind 39: 801–806Google Scholar
  8. 8.
    Vergin H, Bishop GB (1980) High-performance liquid chromatography determination of benzbromarone and its major metabolite benzarone in Serum. Chromatogr Biomed Appl 183: 383–386Google Scholar
  9. 9.
    Diamond HS (1978) Uricosuric drugs. In: Handbook of experimental pharmacology, Vol. 51, Chap 20. Springer, Berlin Heidelberg New York, pp 459–484Google Scholar
  10. 10.
    Broekhuysen J, Bekaert J, Rozenblum C, Deltour G (1965) Arch Int Pharmacodyn Ther 158: 165Google Scholar
  11. 11.
    Heel RC, Brodgen RN, Speight TM, Avery GS (1977) Benzbromarone: A review of its pharmacological properties and therapeutic use in gout and hyperurikaemia. Drugs 14: 349–366Google Scholar

Copyright information

© Springer-Verlag 1981

Authors and Affiliations

  • H. Ferber
    • 1
  • H. Vergin
    • 1
  • G. Hitzenberger
    • 1
  1. 1.Klinische Pharmakologie1. Medizinische UniversitätsklinikViennaAustria

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