Febuxostat 80mg Tablets
WARNING: A study showed that people with heart disease taking this drug had a higher rate of heart- related deaths compared to people taking allopurinol. This includes heart attack and stroke. Tell your doctor if you have ever had heart problems or a stroke. If you have questions, talk with your doctor.This drug is only for use when allopurinol cannot be taken or has not worked. If you have questions, talk with your doctor. @ COMMON USES: It is used to lower uric acid in the blood in people with gout.
Drug Class
Antigout agent
Pharmacologic Class
Xanthine oxidase inhibitor
Pregnancy Category
Category C
FDA Approved
Feb 2009
DEA Schedule
Not Controlled
Overview
What is this medicine?
Febuxostat is a medication used to lower high levels of uric acid in the blood, which causes gout. It works by blocking an enzyme in your body that makes uric acid. Lowering uric acid can prevent gout attacks and help dissolve uric acid crystals that have already formed.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. You can take this medication with or without food. Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication, store it at room temperature, protected from light, and in a dry place. Avoid storing it in a bathroom. Keep all medications in a secure location, out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist or healthcare provider. Instead, check with your pharmacist for guidance on the best disposal method, or look into local drug take-back programs.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
To get the most benefit from your medication, take it exactly as directed by your doctor. Carefully read all the information provided with your prescription, and follow the instructions closely. You can take this medication with or without food. Continue taking your medication as prescribed by your doctor or healthcare provider, even if you start to feel better.
Storing and Disposing of Your Medication
To maintain the effectiveness and safety of your medication, store it at room temperature, protected from light, and in a dry place. Avoid storing it in a bathroom. Keep all medications in a secure location, out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so by your pharmacist or healthcare provider. Instead, check with your pharmacist for guidance on the best disposal method, or look into local drug take-back programs.
What to Do If You Miss a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
Lifestyle & Tips
- Continue to take febuxostat daily as prescribed, even if you feel well or are not having gout attacks. It takes time to lower uric acid levels.
- You may experience more gout attacks when you first start taking febuxostat. This is normal as uric acid crystals dissolve. Your doctor may prescribe another medication (like colchicine or an NSAID) to help prevent these initial flares.
- Drink plenty of fluids (water) to help prevent kidney stones.
- Limit alcohol intake, especially beer and spirits.
- Avoid foods high in purines (e.g., organ meats, certain seafood like anchovies, sardines, mussels, scallops, and some red meats).
- Maintain a healthy weight.
- Do not stop taking febuxostat without talking to your doctor, as your uric acid levels may rise again.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
Initial: 40 mg once daily. If serum uric acid is not <6 mg/dL after 2 weeks, increase to 80 mg once daily.
Dose Range:
40 - 80 mg
Condition-Specific Dosing:
gout:
Initial: 40 mg once daily. If serum uric acid is not <6 mg/dL after 2 weeks, increase to 80 mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required (CrCl 30-89 mL/min)
Moderate:
No dose adjustment required (CrCl 30-89 mL/min)
Severe:
Use with caution; limited data (CrCl <30 mL/min)
Dialysis:
Not studied; use with caution
Hepatic Impairment:
Mild:
No dose adjustment required (Child-Pugh A)
Moderate:
No dose adjustment required (Child-Pugh B)
Severe:
Not studied; use with caution (Child-Pugh C)
Pharmacology
Mechanism of Action
Febuxostat is a non-purine selective inhibitor of xanthine oxidase (XO). It works by potently and selectively inhibiting both the oxidized and reduced forms of xanthine oxidase, thereby reducing the production of uric acid. By inhibiting XO, febuxostat decreases serum uric acid concentrations, which helps prevent the formation of uric acid crystals and dissolves existing crystals, thus treating and preventing gout flares.
Pharmacokinetics
Absorption:
Bioavailability:
49%
Tmax:
1-1.5 hours
FoodEffect:
No clinically significant effect on AUC or Cmax; can be taken with or without food.
Distribution:
Vd:
Approximately 50 L
ProteinBinding:
Approximately 99.2% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
5-8 hours
Clearance:
Not available (primarily hepatic metabolism)
ExcretionRoute:
Approximately 49% renal (primarily as acyl glucuronide metabolites, <5% unchanged), 45% fecal (primarily as unchanged drug and metabolites)
Unchanged:
Approximately 3% (renal), 11% (fecal)
Pharmacodynamics
OnsetOfAction:
Within 2 weeks (for significant uric acid reduction)
PeakEffect:
Approximately 2 weeks (for maximal uric acid reduction)
DurationOfAction:
Maintains reduced uric acid levels with once-daily dosing
Safety & Warnings
BLACK BOX WARNING
Cardiovascular Death: In a large, randomized, controlled cardiovascular outcomes study, febuxostat was shown to have a higher rate of cardiovascular death compared to allopurinol in patients with gout and established cardiovascular disease. Consider the risks and benefits of febuxostat when deciding to prescribe or continue treatment in patients with cardiovascular disease.
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Neurological symptoms, such as:
+ Weakness on one side of the body
+ Trouble speaking or thinking
+ Change in balance
+ Drooping on one side of the face
+ Blurred eyesight
Cardiovascular symptoms, such as:
+ Chest pain or pressure
+ Fast heartbeat
+ Abnormal heartbeat
Respiratory symptoms, such as:
+ Shortness of breath
Other severe symptoms, such as:
+ Dizziness or fainting
+ Headache
+ Fever
+ Swollen gland
+ Flu-like symptoms
Liver Problems: A Rare but Serious Side Effect
In rare cases, this medication can cause liver problems, which can be fatal. If you experience any of the following symptoms, contact your doctor immediately:
Dark urine
Tiredness
Decreased appetite
Upset stomach or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Rare but Serious Skin Reactions
In rare cases, this medication can cause severe and potentially life-threatening skin reactions, such as Stevens-Johnson syndrome or toxic epidermal necrolysis. If you experience any of the following symptoms, seek medical help right away:
Red, swollen, blistered, or peeling skin (with or without fever)
Red or irritated eyes
Sores in your mouth, throat, nose, or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor if you notice any of the following:
Joint pain
* Upset stomach
If you experience any side effects that bother you or do not go away, contact your doctor for advice. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Neurological symptoms, such as:
+ Weakness on one side of the body
+ Trouble speaking or thinking
+ Change in balance
+ Drooping on one side of the face
+ Blurred eyesight
Cardiovascular symptoms, such as:
+ Chest pain or pressure
+ Fast heartbeat
+ Abnormal heartbeat
Respiratory symptoms, such as:
+ Shortness of breath
Other severe symptoms, such as:
+ Dizziness or fainting
+ Headache
+ Fever
+ Swollen gland
+ Flu-like symptoms
Liver Problems: A Rare but Serious Side Effect
In rare cases, this medication can cause liver problems, which can be fatal. If you experience any of the following symptoms, contact your doctor immediately:
Dark urine
Tiredness
Decreased appetite
Upset stomach or stomach pain
Light-colored stools
Vomiting
Yellow skin or eyes
Rare but Serious Skin Reactions
In rare cases, this medication can cause severe and potentially life-threatening skin reactions, such as Stevens-Johnson syndrome or toxic epidermal necrolysis. If you experience any of the following symptoms, seek medical help right away:
Red, swollen, blistered, or peeling skin (with or without fever)
Red or irritated eyes
Sores in your mouth, throat, nose, or eyes
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor if you notice any of the following:
Joint pain
* Upset stomach
If you experience any side effects that bother you or do not go away, contact your doctor for advice. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Signs of a heart attack or stroke: chest pain, shortness of breath, sudden weakness or numbness on one side of the body, slurred speech, sudden severe headache.
- Signs of liver problems: unusual tiredness, loss of appetite, pain in the upper right side of your stomach, dark urine, yellowing of your skin or eyes (jaundice).
- Signs of severe allergic reaction: rash, hives, swelling of the face, lips, tongue, or throat, difficulty breathing.
- Signs of severe skin reactions: widespread rash, blistering, peeling skin, fever, swollen lymph nodes (Stevens-Johnson syndrome, Toxic Epidermal Necrolysis).
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you are currently being treated for cancer or have been diagnosed with Lesch-Nyhan syndrome, a specific health condition.
* If you are taking either of the following medications: Azathioprine or Mercaptopurine.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to discuss all of your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. Additionally, inform them about any existing health problems.
Remember, before starting, stopping, or modifying the dosage of any medication, including this one, you must consult with your doctor to confirm that it is safe to do so in conjunction with your other medications and health conditions.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you are currently being treated for cancer or have been diagnosed with Lesch-Nyhan syndrome, a specific health condition.
* If you are taking either of the following medications: Azathioprine or Mercaptopurine.
Please note that this is not an exhaustive list of all potential interactions. To ensure your safety, it is crucial to discuss all of your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. Additionally, inform them about any existing health problems.
Remember, before starting, stopping, or modifying the dosage of any medication, including this one, you must consult with your doctor to confirm that it is safe to do so in conjunction with your other medications and health conditions.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. Be sure to discuss any concerns or questions you have with your doctor.
When you first start taking this drug, you may experience an increase in gout attacks. It is crucial not to stop taking the medication. Your doctor may prescribe additional medications to help prevent these gout attacks. Consult with your doctor to discuss the best course of treatment.
A rare but potentially life-threatening reaction can occur, characterized by symptoms such as fever, rash, or swollen glands, accompanied by problems in various organs, including the liver, kidney, blood, heart, muscles and joints, or lungs. If you have any questions or concerns, it is vital to discuss them with your doctor.
If you are pregnant, planning to become pregnant, or are breastfeeding, inform your doctor. It is necessary to have a discussion about the potential benefits and risks of this medication to both you and your baby, to determine the best approach for your specific situation.
When you first start taking this drug, you may experience an increase in gout attacks. It is crucial not to stop taking the medication. Your doctor may prescribe additional medications to help prevent these gout attacks. Consult with your doctor to discuss the best course of treatment.
A rare but potentially life-threatening reaction can occur, characterized by symptoms such as fever, rash, or swollen glands, accompanied by problems in various organs, including the liver, kidney, blood, heart, muscles and joints, or lungs. If you have any questions or concerns, it is vital to discuss them with your doctor.
If you are pregnant, planning to become pregnant, or are breastfeeding, inform your doctor. It is necessary to have a discussion about the potential benefits and risks of this medication to both you and your baby, to determine the best approach for your specific situation.
Overdose Information
Overdose Symptoms:
- Limited information on specific overdose symptoms. Expected to be an exaggeration of known side effects, such as liver enzyme elevations, gastrointestinal upset, or cardiovascular events.
What to Do:
In case of suspected overdose, seek immediate medical attention or call a poison control center (e.g., 1-800-222-1222). Management is supportive and symptomatic.
Drug Interactions
Contraindicated Interactions
- Azathioprine
- Mercaptopurine
- Theophylline
Major Interactions
- Didanosine (concurrent use not recommended)
Moderate Interactions
- Warfarin (monitor INR)
- Colchicine (no dose adjustment needed, but monitor for adverse effects)
- Naproxen (no dose adjustment needed)
Monitoring
Baseline Monitoring
Serum Uric Acid (sUA)
Rationale: To establish baseline and guide initial dosing.
Timing: Prior to initiation of therapy
Liver Function Tests (LFTs) including ALT, AST, bilirubin
Rationale: Febuxostat is metabolized in the liver and can cause liver enzyme elevations.
Timing: Prior to initiation of therapy
Cardiovascular risk assessment
Rationale: Due to increased risk of cardiovascular death.
Timing: Prior to initiation of therapy
Routine Monitoring
Serum Uric Acid (sUA)
Frequency: Every 2 weeks initially, then monthly until target <6 mg/dL is reached, then periodically (e.g., every 6 months)
Target: <6 mg/dL
Action Threshold: If sUA remains >6 mg/dL after 2 weeks on 40 mg, increase to 80 mg. If sUA remains >6 mg/dL on 80 mg, consider alternative therapy.
Liver Function Tests (LFTs)
Frequency: Periodically (e.g., at 2 and 4 months, then annually or as clinically indicated)
Target: Within normal limits
Action Threshold: Discontinue if ALT or AST >3 times ULN or if signs/symptoms of liver injury develop.
Symptom Monitoring
- Signs of gout flares (pain, swelling, redness in joints), especially during initiation of therapy (prophylaxis with NSAIDs or colchicine is recommended)
- Signs of liver injury (unusual fatigue, anorexia, right upper quadrant pain, dark urine, jaundice)
- Symptoms of cardiovascular events (chest pain, shortness of breath, sudden weakness or numbness, slurred speech)
- Signs of severe skin reactions (rash, blistering, peeling skin)
Special Patient Groups
Pregnancy
Febuxostat is classified as Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Use only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Animal studies have shown adverse effects on fetal development at doses higher than human therapeutic doses. Risk in humans is unknown.
Second Trimester:
Risk in humans is unknown.
Third Trimester:
Risk in humans is unknown.
Lactation
It is not known whether febuxostat is excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
L3 - Moderate risk. Potential for adverse effects on the infant is possible; weigh benefits of drug to mother vs. risks to infant.
Pediatric Use
Safety and effectiveness in pediatric patients (<18 years of age) have not been established. Febuxostat is not recommended for use in this population.
Geriatric Use
No dose adjustment is necessary based on age. However, elderly patients may be more sensitive to the effects of the drug, and monitoring for adverse effects, particularly cardiovascular events, is important.
Clinical Information
Clinical Pearls
- Febuxostat is a good alternative for patients who are intolerant to allopurinol or who do not achieve target uric acid levels with allopurinol.
- Prophylaxis with an NSAID or colchicine is recommended for the first 6 months of febuxostat therapy to prevent gout flares, as initiation of uric acid-lowering therapy can precipitate acute attacks.
- The Black Box Warning regarding increased cardiovascular death risk, particularly in patients with established cardiovascular disease, is crucial. Carefully assess patient cardiovascular history before prescribing.
- Monitor serum uric acid levels regularly to ensure the therapeutic target of <6 mg/dL is achieved.
- Febuxostat can be taken with or without food.
- Unlike allopurinol, febuxostat does not require dose adjustment for mild to moderate renal impairment, making it a potentially preferred option for some patients with kidney disease.
Alternative Therapies
- Allopurinol (another xanthine oxidase inhibitor)
- Probenecid (uricosuric agent)
- Lesinurad (selective uric acid reabsorption inhibitor, often used in combination)
- Pegloticase (recombinant uricase enzyme, for refractory gout)
Cost & Coverage
Average Cost:
$100 - $300 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (may require prior authorization)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others or take someone else's medication. This medication is accompanied by a Medication Guide, which provides crucial information for patients. Please read this guide carefully and review it again whenever you receive a refill of this medication. If you have any questions or concerns about this medication, consult your doctor, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call the poison control center or seek emergency medical attention. Be prepared to provide detailed information about the overdose, including the substance taken, the amount, and the time it occurred.