febuxostat (Rx)

Brand and Other Names:Uloric
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 40mg
  • 80mg

Chronic Gout

Indicated for chronic management of hyperuricemia in patients who:

  • Responded inadequately to optimal allopurinol therapy
  • Are intolerant to allopurinol
  • Treatment with allopurinol not advisable

Initial dose: 40 mg PO qDay

May increase to 80 mg PO qDay after 2 wk if serum uric acid <6 mg/dL is not achieved

Dosage Modifications

Renal impairment

  • Mild to moderate (CrCl 30-89 mL/min): No dosage adjustment necessary
  • Severe (CrCl <30 mL/min): Not to exceed 40 mg/day

Hepatic impairment

  • Mild to moderate (Child-Pugh class A or B): Dosage adjustment not necessary
  • Severe (Child-Pugh class C): Data not available; use with caution

Prophylaxis for gout flares during treatment

  • Upon initiation, recommend for flare prophylaxis with a nonsteroidal anti-inflammatory drug (NSAID) or colchicine
  • Prophylactic therapy may be beneficial for up to 6 months
  • If a gout flare occurs, managed gout flare concurrently; treatment does not need to be discontinued

Dosing Considerations

Limitation of use: Not recommended for the treatment of asymptomatic hyperuricemia

Perform serum uric acid level as early as 2 weeks after initiating therapy

Safety and efficacy not established

Next:

Interactions

Interaction Checker

and febuxostat

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 

            Contraindicated (4)

            • azathioprine

              febuxostat increases levels of azathioprine by decreasing metabolism. Contraindicated.

            • didanosine

              febuxostat will increase the level or effect of didanosine by decreasing metabolism. Contraindicated.

            • mercaptopurine

              febuxostat increases levels of mercaptopurine by decreasing metabolism. Contraindicated. Potential for increased myelosuppression.

            • theophylline

              febuxostat increases levels of theophylline by decreasing metabolism. Contraindicated.

            Serious - Use Alternative (0)

              Monitor Closely (3)

              • apalutamide

                apalutamide will decrease the level or effect of febuxostat by increasing elimination. Use Caution/Monitor. Apalutamide induces UGT and may decrease systemic exposure of drugs that are UGT substrates.

              • dichlorphenamide

                dichlorphenamide and febuxostat both decrease serum potassium. Use Caution/Monitor.

              • ethambutol

                ethambutol decreases effects of febuxostat by Other (see comment). Use Caution/Monitor. Comment: Hyperuricemia reported with ethambutol and precipitation of gout reported; uric acid lowering agents may be require dosage adjustment.

              Minor (0)

                Previous
                Next:

                Adverse Effects

                1-10%

                Liver function abnormalities (4.6-6.6%)

                Rash (0.5-1.6%)

                Nausea (1.1-1.3%)

                Arthralgia (0.7-1.1%)

                >1%

                Blood and lymphatic system disorders: Anemia, idiopathic thrombocytopenic purpura, leukocytosis/leukopenia, neutropenia, pancytopenia, splenomegaly, thrombocytopenia

                Cardiac disorders: Angina pectoris, atrial fibrillation/flutter, cardiac murmur, ECG abnormal, palpitations, sinus bradycardia, tachycardia

                Ear and labyrinth disorders: Deafness, tinnitus, vertigo

                Eye disorders: Vision blurred

                Gastrointestinal disorders: Abdominal distention, abdominal pain, constipation, dry mouth, dyspepsia, flatulence, frequent stools, gastritis, gastroesophageal reflux disease, gastrointestinal discomfort, gingival pain, hematemesis, hyperchlorhydria, hematochezia, mouth ulceration, pancreatitis, peptic ulcer, vomiting

                General disorders and administration site conditions: Asthenia, chest pain/discomfort, edema, fatigue, feeling abnormal, gait disturbance, influenza-like symptoms, mass, pain, thirst

                Hepatobiliary disorders: Cholelithiasis/cholecystitis, hepatic steatosis, hepatitis, hepatomegaly

                Immune system disorder: Hypersensitivity

                Infections and infestations: Herpes zoster

                Procedural complications: Contusion

                Metabolism and nutrition disorders: Anorexia, appetite decreased/increased, dehydration, diabetes mellitus, hypercholesterolemia, hyperglycemia, hyperlipidemia, hypertriglyceridemia, hypokalemia, weight decreased/increased

                Musculoskeletal and connective tissue disorders: Arthritis, joint stiffness, joint swelling, muscle spasms/twitching/tightness/weakness, musculoskeletal pain/stiffness, myalgia

                Nervous system disorders: Altered taste, balance disorder, cerebrovascular accident, Guillain-Barré syndrome, headache, hemiparesis, hypoesthesia, hyposmia, lacunar infarction, lethargy, mental impairment, migraine, paresthesia, somnolence, transient ischemic attack, tremor

                Psychiatric disorders: Agitation, anxiety, depression, insomnia, irritability, libido decreased, nervousness, panic attack, personality change

                Renal and urinary disorders: Hematuria, nephrolithiasis, pollakiuria, proteinuria, renal failure, renal insufficiency, urgency, incontinence

                Reproductive system and breast changes: Breast pain, erectile dysfunction, gynecomastia

                Respiratory, thoracic and mediastinal disorders: Bronchitis, cough, dyspnea, epistaxis, nasal dryness, paranasal sinus hypersecretion, pharyngeal edema, respiratory tract congestion, sneezing, throat irritation, upper respiratory tract infection

                Skin and subcutaneous tissue disorders: Alopecia, angio edema, dermatitis, dermographism, ecchymosis, eczema, hair color changes, hair growth abnormal, hyperhidrosis, peeling skin, petechiae, photosensitivity, pruritus, purpura, skin discoloration/altered pigmentation, skin lesion, skin odor abnormal, urticaria

                Vascular disorders: Flushing, hot flush, hypertension, hypotension

                Laboratory parameters: Activated partial thromboplastin time prolonged, creatine increased, bicarbonate decreased, sodium increased, EEG abnormal, glucose increased, cholesterol increased, triglycerides increased, amylase increased, potassium increased, TSH increased, platelet count decreased, hematocrit decreased, hemoglobin decreased, MCV increased, RBC decreased, creatinine increased, blood urea increased, BUN/creatinine ratio increased, creatine phosphokinase increased, alkaline phosphatase increased, LDH increased, PSA increased, urine output increased/decreased, lymphocyte count decreased, neutrophil count decreased, WBC increased/decreased, coagulation test abnormal, low density lipoprotein increased, prothrombin time prolonged, urinary casts, urine positive for white blood cells and protein

                Postmarketing Reports

                Immunologic: Anaphylaxis, anaphylactic reaction

                Musculoskeletal: Rhabdomyolysis

                Hepatobiliary: Hepatic failure (some fatal), jaundice, serious cases of abnormal LFT results, liver disorders

                Psychiatric: Psychotic behavior, including aggressive thoughts

                Renal and urinary: Tubulointerstitial nephritis

                Dermatologic: Generalized rash, Stevens-Johnson syndrome, hypersensitivity skin reactions, drug reaction with eosinophilia and systemic symptoms (DRESS) and toxic epidermal necrolysis (TEN)

                Blood and lymphatic system disorders: Agranulocytosis, eosinophilia

                Previous
                Next:

                Warnings

                Black Box Warnings

                Cardiovascular death

                • Patients with established cardiovascular (CV) disease treated with febuxostat had a higher rate of CV death compared with those treated with allopurinol in a CV outcomes study
                • Evaluate risks and benefits when prescribing febuxostat or continuing treatment

                Contraindications

                Coadministration with azathioprine or mercaptopurine

                Cautions

                After initiation, an increase in gout flares is frequently observed; 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)

                Postmarketing 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

                Postmarketing 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 >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
                • 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 increased risk of CV death, 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 coadministered
                  • 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)
                Previous
                Next:

                Pregnancy & Lactation

                Pregnancy

                Limited available data in pregnant women are insufficient to inform a drug associated risk of adverse developmental outcomes

                Animal data

                • No adverse developmental effects observed in embryo-fetal development studies with oral administration of febuxostat to pregnant rats and rabbits during organogenesis at doses that produced maternal exposures up to 40 and 51 times, respectively, the exposure at the maximum recommended human dose (MRHD)
                • No adverse developmental effects observed in a pre- and postnatal development study with administration of febuxostat to pregnant rats from organogenesis through lactation at an exposure ~11 times the MRHD

                Lactation

                There are no data on presence of febuxostat in human milk, effects on breastfed infant, or on milk production; drug is present in rat milk

                Consider the developmental and health benefits of breastfeeding along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from therapy or from underlying maternal condition

                Pregnancy Categories

                A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                NA: Information not available.

                Previous
                Next:

                Pharmacology

                Mechanism of Action

                Xanthine oxidase inhibitor; inhibits conversion of hypoxanthine to xanthine to uric acid; at therapeutic dosages, decreases production of uric acid without disrupting synthesis of vital purines and pyrimidines

                Absorption

                Absorption: 49%

                Peak plasma concentration: ~1.6 mcg/mL (40-mg dose); 2.6 mcg/mL (80-mg dose)

                Peak plasma time: 1-1.5 hr

                Following multiple 80 mg qDay doses with a high fat meal, peak plasma concentration decreased by 49% and AUC decreased by 18%

                Distribution

                Protein bound: 99.2%

                Vd: 50 L

                Metabolism

                Metabolized by UGT1A1, UGT1A3, UGT1A9, and UGT2B7; oxidized by CYP1A2, CYP2C8, and CYP2C9; also metabolized by non-CYP450 enzymes

                Elimination

                Half-life: 5-8 hr

                Excretion: Feces (45%; 12% unchanged; 25% their conjugates; 7% other unknown metabolites), urine (49%; 3% unchanged)

                Previous
                Next:

                Administration

                Oral Administration

                Take without regard to food or antacid use

                Storage

                Protect from light

                Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F)

                Previous
                Next:

                Images

                BRAND FORM. UNIT PRICE PILL IMAGE
                Uloric oral
                -
                40 mg tablet
                Uloric oral
                -
                80 mg tablet
                febuxostat oral
                -
                40 mg tablet
                febuxostat oral
                -
                80 mg tablet
                febuxostat oral
                -
                80 mg tablet
                febuxostat oral
                -
                40 mg tablet
                febuxostat oral
                -
                80 mg tablet
                febuxostat oral
                -
                40 mg tablet
                febuxostat oral
                -
                40 mg tablet
                febuxostat oral
                -
                80 mg tablet

                Copyright © 2010 First DataBank, Inc.

                Previous
                Next:

                Patient Handout

                Patient Education
                febuxostat oral

                FEBUXOSTAT - ORAL

                (feb-UX-oh-stat)

                COMMON BRAND NAME(S): Uloric

                WARNING: Febuxostat may rarely cause very serious side effects including heart attack, stroke, or possibly fatal heart-related problems. Before taking this medication, tell your doctor if you have heart disease, chest pain (angina), or have had a heart attack or stroke in the past since these conditions may increase your risk. Discuss the risks and benefits of this medication and treatment options with your doctor. Get medical help right away if you have any of these very serious side effects: chest/jaw/left arm pain, unusual sweating, shortness of breath, fast/irregular heartbeat, dizziness, fainting, weakness on one side of the body, sudden vision changes, confusion, trouble speaking, sudden severe headache.

                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.

                HOW TO USE: Read the Medication Guide provided by your pharmacist before you start taking febuxostat and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with or without food as directed by your doctor, usually once daily.The dosage is based on your medical condition and response to treatment. Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day.You may have more gout attacks for several months after starting this medicine while the body removes extra uric acid. Febuxostat is not a pain reliever. Your doctor may prescribe medication (such as colchicine, NSAIDs such as ibuprofen, naproxen, or indomethacin) to prevent/treat a gout attack during the first several months you are taking febuxostat. Continue to take your prescribed medicines for gout attacks as directed by your doctor.Tell your doctor if your condition lasts or gets worse.

                SIDE EFFECTS: See also Warning section.Nausea may occur. If this effect lasts or gets worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Febuxostat may rarely cause serious (possibly fatal) liver disease. It may also cause an increase in liver enzymes. Your doctor will order blood tests to measure these enzymes. Keep all medical/lab appointments. Tell your doctor right away if you develop symptoms of liver disease, including nausea that doesn't stop, stomach/abdominal pain, dark urine, yellowing eyes/skin.Tell your doctor right away if you have any serious side effects, including: pink/bloody urine, painful urination.Febuxostat may cause a rash that could be a sign of a severe reaction. Get medical help right away if you develop any rash.A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: fever, swollen lymph nodes, rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

                PRECAUTIONS: See also Warning section.Before taking febuxostat, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: cancer, heart disease (such as heart attack, chest pain/angina), stroke, liver disease, kidney disease, organ transplant.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if febuxostat passes into breast milk. Consult your doctor before breast-feeding.

                DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: azathioprine, mercaptopurine.

                OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

                NOTES: Do not share this medication with others.Lab and/or medical tests (such as uric acid blood level, liver function tests) may be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.

                MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.

                STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.

                Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

                IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

                Previous
                Next:

                Formulary

                FormularyPatient Discounts

                Adding plans allows you to compare formulary status to other drugs in the same class.

                To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

                Adding plans allows you to:

                • View the formulary and any restrictions for each plan.
                • Manage and view all your plans together – even plans in different states.
                • Compare formulary status to other drugs in the same class.
                • Access your plan list on any device – mobile or desktop.

                The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                NC NOT COVERED – Drugs that are not covered by the plan.
                Code Definition
                PA Prior Authorization
                Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                QL Quantity Limits
                Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                ST Step Therapy
                Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                OR Other Restrictions
                Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
                Additional Offers
                Email to Patient

                From:

                To:

                The recipient will receive more details and instructions to access this offer.

                By clicking send, you acknowledge that you have permission to email the recipient with this information.

                Email Forms to Patient

                From:

                To:

                The recipient will receive more details and instructions to access this offer.

                By clicking send, you acknowledge that you have permission to email the recipient with this information.

                Previous
                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.