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Allopurinol is an isomer of hypoxanthine that inhibits xanthine oxidoreductase (IC50 values between 0.2 and 50 μM, depending on assay and cell type).1,2 In vivo, allopurinol has been reported to effectively and safely lower serum and urinary uric acid levels and is also reported to be effective in the treatment of gout and hyperuricemia. Allopurinol is rapidly metabolized in vivo to the xanthine analog oxypurinol, which is a metabolite that clearly augments the therapeutic effect of allopurinol.3
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2. Therapeutic effects of xanthine oxidase inhibitors: Renaissance half a century after the discovery of allopurinol. Pharmacol. Rev. 58(1), 87-114 (2006).
3. Clinical pharmacokinetics and pharmacodynamics of allopurinol and oxypurinol. Clin. Pharmacokinet. 46(8), 623-644 (2007).