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Pharmacology: Pharmacodynamics: Selectively inhibits xanthine oxidase, the enzyme responsible for the conversion of hypoxanthine to xanthine to uric acid thereby decreasing uric acid. At therapeutic concentration does not inhibit other enzymes involved in purine and pyrimidine synthesis.
Pharmacokinetics: Absorption: The oral bioavailability is approximately 75% to 85%.
Cmax decrease by 49% and AUC decrease by 19% when taken with food. However. no clinically significant effect over time.
Distribution: Febuxostat is highly bound, 98% to 99% to plasma proteins, primarily albumin.
Volume of distribution is 41 to 50 L.
Metabolism: Febuxostat is extensively metabolized by conjugation via uridine diphosphate glucuronosyltransferases (UGTs) 1A1, 1A8, and 1A9 and oxidation via cytochrome P450 (CYP) 1A1, 1A2, 2C8, and 2C9 as well as non-P450 enzymes.
Excretion: Renal Excretion: Approximately 49% of the dose was excreted in the urine as unchanged Febuxostat (3%), the acyl glucuronide metabolite (30%), other known oxidative metabolites and conjugates (13%), and unknown metabolites (3%).
Feces: Approximately 45% of the dose was excreted in the feces as unchanged Febuxostat (12%), the acyl glucuronide metabolite (1%), other known oxidative metabolites and conjugates (25%), and unknown metabolites (7%).
Elimination Half-life: Febuxostat elimination half-life is 5 to 8 hours.
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