Pharmacodynamic
Febuxostat is a xanthine oxidase inhibitor which 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: ≥ 49 %
- Distribution: Protein Binding: 99.2 % (primarily to albumin)
- Metabolism: Extensively metabolized by conjugation via uridine diphosphate glucuronosyltransferase (UDPGT) enzyme system and oxidation via cytochrome P450 (CYP) system.
- Elimination: Eliminated by both hepatic and renal pathways
Indication
For the chronic management of hyperuricemia in patients with gout.
Dose
For Chronic Gout
Initial Dose: 40 mg OD
Increased to 80 mg OD after 2 weeks if serum uric acid
Gout flare prophylaxis of at least 6 months is recommended.
Patient Group
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Dose Consideration
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No dose adjustment required
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No dose adjustment is necessary in patients with mild or moderate renal impairment.
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Mild hepatic impairment: 80 mg.
Moderate hepatic impairment: limited information available
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Safety and efficacy in children aged below the age of 18 years have not been established.
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Side Effects
Nausea, Arthralgia, Rash & Liver function abnormalities
Pregnancy Category : C
Contraindications
Contraindicated in patient being treated with azathioprine or mercaptopurine
Warning & Precautions:
- History of Major Cardiovascular Disease A higher rate of cardiovascular thromboembolic events was observed in patients treated with febuxostat who has history of major cardiovascular disease. Monitor for signs and symptoms of MI and stroke
- Gout flares Increase in gout flares can be observed frequently during the initiation of febuxostat. In order to prevent this concurrent prophylactic treatment with an NSAID or colchicine is recommended
- Hepatic Effects Liver enzymes can be elevated significantly. Measure liver tests promptly in patients who report symptoms that may indicate liver injury, including fatigue, anorexia, right upper abdominal discomfort, dark urine or jaundice
Storage
Store below 25◦C
Missed Dose
- Take the missed dose as soon as you remember.
- Skip the missed dose if it is almost time for your next scheduled dose.
- Do not take extra medicine to make up the missed dose.
Presentation:
- Febumin 40 Each box contains: 10 strips X 10 Tabs. ALU-ALU Packing
- Febumin 80 Each box contains: 10 strips X 10 Tabs. ALU-ALU Packing