Febuxostat (febuxostat)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Febuxostat is a xanthine oxidase inhibitor.
Febuxostat inhibits xanthine oxidase, the enzyme that catalyzes the conversion of hypoxanthine to xanthine and xanthine to uric acid. By blocking uric acid production, febuxostat decreases serum concentrations of uric acid. Febuxostat has minimal effects on other enzymes involved in purine and pyrimidine synthesis and metabolism.
Febuxostat is extensively metabolized by conjugation by uridine diphosphate-glucuronosyltransferase (UGT) enzymes, including UGT 1A1, 1A3, 1A9, and 2B7, as well as by oxidation by cytochrome P-450 (CYP) isoenzymes, including CYP 1A2, 2C8, and 2C9, and non-CYP enzymes. The drug is eliminated in urine (49%) and feces (45%), principally in the form of various metabolites and their conjugates; 3 and 12% of an administered dose is recovered as unchanged drug in urine and feces, respectively.
USES: Febuxostat is used to lower uric acid levels in people with gout. Febuxostat works by reducing the amount of uric acid made by the body. An increased uric acid level can cause gout.
Because of the risk of very serious heart-related problems and stroke with febuxostat (see also Warning section), febuxostat should be used only after treatment with a medication called allopurinol did not work to lower your uric acid level, caused serious side effects, or is not recommended by your doctor. Febuxostat should be used only if you have symptoms caused by a high blood uric acid level.
Generic name: febuxostat
Pronunciation: (feb-UX-oh-stat)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Febuxostat
Indications
The following indications are listed for Febuxostat:
- Prevention Of Acute Gout Attack
Also known as: Acute Gout Attack Prophylaxis, Prevention Of Acute Gout Flare.
Dosing
The recommended initial dosage of febuxostat for the management of hyperuricemia in patients with gout is 40 mg once daily. The dosage of febuxostat may be increased to 80 mg once daily in patients who do not achieve serum urate concentrations of less than 6 mg/dL following 2 weeks of therapy with febuxostat 40 mg once daily.
Febuxostat is administered orally without regard to meals or antacids.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
Concomitant therapy with azathioprine or mercaptopurine. (See Drug Interactions: Drugs Metabolized by Xanthine Oxidase.)
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
Adverse effects reported in 1% or more of patients receiving febuxostat include liver function abnormalities, nausea, arthralgia, and rash.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy have not been established in pediatric patients.
Data are inadequate regarding use of febuxostat in pregnant women.
Animal reproduction studies using febuxostat have not revealed evidence of fetal harm at exposures greater than those attained with the maximum recommended human dosage.
Febuxostat is distributed into milk in rats at concentrations up to approximately 7 times plasma concentrations of the drug. It is not known whether febuxostat distributes into human milk, affects the breast-fed infant, or affects milk production.
The benefits of breast-feeding and the importance of febuxostat to the woman should be considered along with the potential adverse effects on the breast-fed child from the drug or from the underlying maternal condition.
No substantial differences in safety and efficacy have been observed in geriatric patients relative to younger adults, but increased sensitivity of some older patients cannot be ruled out.
Pharmacokinetic values in geriatric adults were similar to those in younger adults. Dosage adjustment based on age is not needed.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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