Drug information of Febuxostat
Mechanism of effect
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.
Febuxostat is a xanathine oxidase (XO) inhibitor indicated in patients with gout suffering from hyperuricemia and is used in its chronic management.
Absorption:≥49%. Metabolism:Extensive conjugation via uridine diphosphate glucuronosyltransferases (UGTs) 1A1, 1A3, 1A9, and 2B7 and oxidation via cytochrome P450 (CYP) 1A2, 2C8, and 2C9 as well as non-P450 enzymes. Oxidation leads to formation of active metabolites (67M-1, 67M-2, 67M-4). Excretion:Urine (~49% mostly as metabolites, 3% as unchanged drug); feces (~45% mostly as metabolites, 12% as unchanged drug). Time to Peak:Plasma: 1 to 1.5 hours. Half-Life Elimination:~5 to 8 hours. Protein Binding:~99%, primarily to albumin.
Usual Adult Dose for Gout
Initial dose: 40 mg orally once a day
-If serum uric acid level is greater than 6 mg/dL after 2 weeks, increase the dose to 80 mg orally once a day
Maintenance dose: 40 to 80 mg orally once a day
Drug contraindicationshypersensitivity to drug or its components.
Side effectsnausea , Hepatic dysfunction , rash , Arthralgia
InteractionsTheophyline G , Didanosine , Mipomersen , mercaptopurine
1-Use with caution in patients with severe hepatic impairment
2-Use with caution in patients with severe renal impairment
3-Use in secondary hyperuricemia has not been studied; avoid use in patients at increased risk of urate formation (eg, malignancy and its treatment; Lesch-Nyhan syndrome).
Points of recommendation
1-Oral: Administer with or without meals or antacids.
2-Liver function tests at baseline and then periodically, serum uric acid levels (as early as 2 weeks after initiation); signs/symptoms of MI or stroke, signs/symptoms of hypersensitivity or severe skin reactions
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