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Allopurinol is the drug most widely used to lower the blood concentrations of urate and, therefore, to decrease the number of repeated attacks of gout. Allopurinol is rapidly and extensively metabolised to oxypurinol (oxipurinol), and the hypouricaemic efficacy of allopurinol is due very largely to this metabolite.

The pharmacokinetic parameters of allopurinol after oral dosage include oral bioavailability of 79 ± 20% (mean ± SD), an elimination half-life (t_1/2) of 1.2 ± 0.3 hours, apparent oral clearance (CL/F) of 15.8 ± 5.2 mL/min/kg and an apparent volume of distribution after oral administration (V_d/F) of 1.31 ± 0.41 L/kg. Assuming that 90mg of oxypurinol is formed from every 100mg of allopurinol, the pharmacokinetic parameters of oxypurinol in subjects with normal renal function are a t1/2 of 23.3 ± 6.0 hours, CL/F of 0.31 ± 0.07 mL/min/kg, V_d/F of 0.59 ± 0.16 L/kg, and renal clearance (CL_R) relative to …