Febuxostat

Febuxostat is a prescription medication used to treat Chronic Gout.

• Febuxostat is available under the following different brand names: Uloric

Dosages of Febuxostat:

Adult dosage

Tablet

• 40mg
• 80mg

Chronic Gout

• Initial dose: 40 mg orally once a day
• May increase to 80 mg orally once daily after 2 weeks if serum uric acid less than 6 mg/dL is not achieved

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”.

Common side effects of Febuxostat include:

• gout flares, 
• joint pain, 
• nausea, 
• mild rash, and 
• liver problems

Serious side effects of Febuxostat include:

• hives, 
• difficulty breathing, 
• swelling of the face, lips, tongue, or throat, 
• fever, 
• sore throat, 
• burning in your eyes, 
• skin pain, 
• red or purple skin rash that spreads and causes blistering and peeling, 
• skin rash, 
• fever, 
• swollen glands, 
• flu-like symptoms, 
• muscle aches, 
• severe weakness, 
• unusual bruising, 
• yellowing of the skin or eyes (jaundice), 
• lightheadedness, 
• chest pain or pressure, 
• pain spreading to the jaw or shoulder, 
• fast heartbeats, 
• shortness of breath, 
• stomach pain (upper right side), 
• unusual tiredness, 
• dark urine, 
• sudden numbness, 
• weakness (especially on one side of the body), 
• sudden severe headache, 
• slurred speech, and
• problems with vision or balance

Rare side effects of Febuxostat include:

• none 

This is not a complete list of side effects and other serious side effects or health problems may occur as a result of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them.  Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first

• Febuxostat has severe interactions with the following drugs:
  • azathioprine
  • didanosine
  • mercaptopurine
  • theophylline
• Febuxostat has serious interactions with no other drugs. 
• Febuxostat has moderate interactions with the following drugs:
  • apalutamide
  • dichlorphenamide
  • ethambutol
• Febuxostat has minor interactions with at least 51 other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drugs interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use.  Keep a list of all your medications with you, and share this information with your doctor and pharmacist.  Check with your health care professional or doctor for additional medical advice, or if you have health questions, concerns.

Contraindications

• Coadministration with azathioprine or mercaptopurine 

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Febuxostat?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Febuxostat?”

Cautions

• After initiation, an increase in gout flares is frequently observed; the increase is due to reduction in serum uric acid levels, resulting in mobilization of urate from tissue deposits
• Not tested for secondary hyperuricemia; not recommended in patients whose rate of urate formation is greatly increased (eg, malignant disease and its treatment, Lesch-Nyhan syndrome)
• Post-marketing reports of serious skin and hypersensitivity reactions reported; discontinue if serious skin reactions are suspected; caution in patients who reported previous similar skin reactions to allopurinol
• Post-marketing reports of fatal and nonfatal hepatic failure; may increase liver enzyme activity; obtain LFTs at baseline, and do not initiate if alanine aminotransferase is 3x ULN with total bilirubin greater than 2x ULN
• Serious skin and hypersensitivity reactions, including Stevens-Johnson Syndrome, drug reaction with eosinophilia and systemic symptoms (DRESS) and toxic epidermal necrolysis (TEN) reported; discontinue therapy if serious skin reactions suspected; many patients reported previous similar skin reactions to allopurinol; use caution in these patients

Cardiovascular death

• A cardiovascular (CV) outcome study (ClinicalTrials.gov identifier NCT01101035) in patients with a history of major CV disease, cerebrovascular disease, or diabetes mellitus with micro-and/or macrovascular disease showed that febuxostat had a significantly higher incidence of CV deaths compared with allopurinol
• The most common cause of adjudicated CV deaths in the febuxostat group was sudden cardiac death compared with the allopurinol group; similar results to allopurinol were observed for nonfatal MI, nonfatal stroke, and unstable angina with urgent coronary revascularization (see Black Box Warnings)
• Because of the increased risk of CV death, the drug should only be used in patients who have an inadequate response to a maximally titrated dose of allopurinol, who are intolerant to allopurinol, or for whom treatment with allopurinol is not advisable

Drug interaction overview

• Xanthine oxidase substrates
  • Febuxostat inhibits xanthine oxidase (XO)
  • Based on a drug interaction study in healthy patients, febuxostat altered the metabolism of theophylline in humans; caution if co-administered
  • Other drugs that are metabolized by XO (eg, mercaptopurine and azathioprine) have not been conducted; XO inhibition may increase plasma concentrations of these drugs leading to toxicity (see Contraindications)

Pregnancy and Lactation

• Limited available data in pregnant women are insufficient to inform a drug-associated risk of adverse developmental outcomes
• There are no data on the presence of febuxostat in human milk, effects on the breastfed infant, or milk production; the drug is present in rat milk
• Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for therapy and any potential adverse effects on the breastfed child from therapy or underlying maternal condition