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Oxypurinol, allopurinol and allopurinol-1-riboside in plasma following an acute overdose of allopurinol in a patient with advanced chronic kidney disease.

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RCT (the Allopurinol and Placebo-Controlled, Efficacy Study of Febuxostat (APEX) trial) including 1072 participants, with gout as per ARA criteria, and compared allopurinol 100 or 300 mg daily based on renal function with febuxostat 80, 120 or 240 mg daily or placebo.

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Up to 20% of the active drug is excreted by the kidneys.

Allopurinol and its active metabolite, oxypurinol, inhibits the enzyme xanthine oxidase, blocking the conversion of the oxypurines hypoxanthine and xanthine to uric acid.

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However, no improvement in leukemia response was noted with mercaptopurine-allopurinol co-therapy, so that work turned to other compounds and the team then started testing allopurinol as a potential for gout.

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