PMID: 2095343Jan 1, 1990Paper

Rapid and slow benzbromarone elimination phenotypes in man: benzbromarone and metabolite profiles

European Journal of Clinical Pharmacology
I Walter-SackE Weber

Abstract

Following oral administration of the uricosuric drug benzbromarone two major metabolites appear in the circulation. 1'-hydroxy-benzbromarone (M1), and a second product (M2) of unknown structure. The plasma concentrations of the parent drug and of M1 and M2 have now been compared in two different elimination phenotypes. 10 subjects who eliminated the drug rapidly (S1-10) and one individual (S11) whose elimination capacity was impaired, presumably due to genetic variation (S11). The AUC (0-96) of the parent drug in S11 was 145 micrograms.ml-1 h. and in the other individuals it averaged 18.3 (11.4-24.5) micrograms.ml-1 h. The plasma elimination half life of benzbromarone was 3.34 (1.77-5.24) h in the rapid eliminators, and 13.08 h in the subject with the elimination defect. The mean plasma elimination half life of the metabolites in S1-10 amounted to 20.1 (11.9-41.2) h for M1, and 17.2 (12.9-30.7) h for M2. In S11 the plasma elimination half life of M1 was prolonged to 76.6 h, and of M2 to 75.4 h. Thus, the elimination defect in S11 was not restricted to the parent drug, but it also involved the two major metabolites M1 and M2. This might be a consequence of a hepatic enzyme deficiency, or be due to impairment of drug excretion.

References

Jan 1, 1990·European Journal of Clinical Pharmacology·I Walter-SackN Zöllner
Jan 19, 1990·Klinische Wochenschrift·N ZöllnerI Walter-Sack
Dec 1, 1989·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·J X De VriesE Weber
Nov 1, 1988·Klinische Wochenschrift·I Walter-SackE Weber
Jul 1, 1987·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·S G WoodR F Lambe
Mar 1, 1986·Australian Veterinary Journal·R G WilsonS Groenendyk
Mar 1, 1972·European Journal of Clinical Pharmacology·J BroekhuysenM Van Hee
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Citations

Feb 1, 1996·Journal of Clinical Pharmacology·H ShimodairaT Kudo
Mar 1, 1994·Journal of Hepatology·M M van der KlauwP Spoelstra
Oct 22, 2010·Drug Metabolism and Pharmacokinetics·Shinya UchidaHiroshi Watanabe
Jan 11, 2013·Case Reports in Medicine·Simone FargettiRicardo Fuller
Aug 31, 2012·Biopharmaceutics & Drug Disposition·Kaoru KobayashiKan Chiba
Apr 17, 2015·Pharmacogenomics·Rebecca L Roberts, Lisa K Stamp
Jun 27, 2002·Journal of Gastroenterology and Hepatology·Makoto AraiHiromitsu Saisho
Jan 1, 1990·European Journal of Clinical Pharmacology·I Walter-SackN Zöllner
Mar 4, 2015·Pain·Yueming ZhengZhaobing Gao

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