Febuxostat 40mg 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; Uric acid reducer
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 helps prevent gout attacks. It works by blocking an enzyme in the body that makes uric acid.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, it's essential to 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 feeling 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 the missed one.
To get the most benefit from your medication, it's essential to 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 feeling 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 the missed one.
Lifestyle & Tips
- Drink plenty of water to help flush uric acid from your body.
- Limit or avoid foods high in purines (e.g., red meat, organ meats, certain seafood like anchovies, sardines).
- Limit alcohol intake, especially beer.
- Maintain a healthy weight.
- Continue taking febuxostat daily as prescribed, even if you feel well, to keep uric acid levels low and prevent gout flares.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
40 mg orally once daily. If serum uric acid is >6 mg/dL after 2 weeks, increase to 80 mg orally once daily.
Dose Range:
40 - 80 mg
Condition-Specific Dosing:
gout:
Initial: 40 mg once daily. If target serum uric acid (<6 mg/dL) is not achieved 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; generally not recommended due to lack of data.
Hepatic Impairment:
Mild:
No dose adjustment required (Child-Pugh A).
Moderate:
No dose adjustment required (Child-Pugh B).
Severe:
Not studied; avoid use (Child-Pugh C).
Pharmacology
Mechanism of Action
Febuxostat is a non-purine selective inhibitor of xanthine oxidase (XO). It inhibits both the oxidized and reduced forms of XO, thereby decreasing uric acid synthesis. By inhibiting XO, febuxostat reduces serum uric acid concentrations, which helps prevent the formation of uric acid crystals and reduces the frequency of gout flares.
Pharmacokinetics
Absorption:
Bioavailability:
49%
Tmax:
1-1.5 hours
FoodEffect:
No clinically significant effect on AUC or Cmax.
Distribution:
Vd:
Approximately 50 L
ProteinBinding:
Approximately 99.2% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
5-8 hours
Clearance:
Not available
ExcretionRoute:
Approximately 49% renal (11% as unchanged drug), 45% fecal (12% as unchanged drug).
Unchanged:
Approximately 3% (urine), 12% (feces)
Pharmacodynamics
OnsetOfAction:
Uric acid lowering begins within 2 weeks.
PeakEffect:
Maximum uric acid lowering typically achieved within 2 weeks.
DurationOfAction:
Sustained uric acid lowering with once-daily dosing.
Safety & Warnings
BLACK BOX WARNING
Increased risk of cardiovascular death. In a large, randomized, controlled cardiovascular outcomes study (CARES trial) in patients with gout and established cardiovascular disease, febuxostat was associated with a higher rate of cardiovascular death compared to allopurinol. Consider the risks and benefits of febuxostat when deciding to prescribe it to patients with cardiovascular disease.
Side Effects
Serious Side Effects: Seek Medical Help Immediately
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 medical attention right away:
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 attention 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 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 other 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 medical attention right away:
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 attention 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 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 other 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:
- Gout flares (paradoxical increase in flares can occur during the first few months of treatment; continue medication and consult doctor).
- Signs of liver problems (yellowing of skin or eyes, dark urine, severe stomach pain, unusual tiredness, nausea, vomiting).
- Signs of a heart attack or stroke (chest pain, shortness of breath, sudden numbness or weakness on one side of the body, sudden severe headache, slurred speech). Seek emergency medical attention immediately if these occur.
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 allergic reaction and its symptoms.
If you are currently being treated for cancer or have been diagnosed with Lesch-Nyhan syndrome, a rare genetic disorder.
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 disclose all of your:
Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
* Health problems
Your doctor and pharmacist need this information to assess potential interactions and determine whether it is safe for you to take this medication with your existing treatments and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting 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 allergic reaction and its symptoms.
If you are currently being treated for cancer or have been diagnosed with Lesch-Nyhan syndrome, a rare genetic disorder.
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 disclose all of your:
Prescription and over-the-counter (OTC) medications
Natural products
Vitamins
* Health problems
Your doctor and pharmacist need this information to assess potential interactions and determine whether it is safe for you to take this medication with your existing treatments and health conditions. Never start, stop, or adjust the dosage of any medication without first consulting your doctor.
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. 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 attacks. Be sure to discuss this with your doctor.
A severe and potentially life-threatening reaction can occur, characterized by symptoms such as fever, rash, or swollen glands, along with problems in various organs, including the liver, kidney, blood, heart, muscles and joints, or lungs. If you have any questions or concerns, consult your doctor.
If you are pregnant, planning to become pregnant, or are breastfeeding, inform your doctor. It is necessary to discuss the potential benefits and risks of this medication to both you and your baby to make an informed decision.
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 attacks. Be sure to discuss this with your doctor.
A severe and potentially life-threatening reaction can occur, characterized by symptoms such as fever, rash, or swollen glands, along with problems in various organs, including the liver, kidney, blood, heart, muscles and joints, or lungs. If you have any questions or concerns, consult your doctor.
If you are pregnant, planning to become pregnant, or are breastfeeding, inform your doctor. It is necessary to discuss the potential benefits and risks of this medication to both you and your baby to make an informed decision.
Overdose Information
Overdose Symptoms:
- Symptoms of overdose are not well-defined. In clinical studies, patients tolerated doses up to 300 mg daily for 7 days without dose-limiting toxicities. Higher doses may lead to increased side effects.
What to Do:
In case of suspected overdose, contact a poison control center immediately (e.g., 1-800-222-1222 in the US) or seek emergency medical attention. Treatment is supportive and symptomatic.
Drug Interactions
Contraindicated Interactions
- Azathioprine
- Mercaptopurine
Major Interactions
- Didanosine
Moderate Interactions
- Theophylline
Monitoring
Baseline Monitoring
Serum Uric Acid (sUA)
Rationale: To establish baseline level and guide initial dosing.
Timing: Prior to initiation of therapy.
Liver Function Tests (ALT, AST, Bilirubin)
Rationale: To assess baseline hepatic function as febuxostat is hepatically metabolized and can cause liver enzyme elevations.
Timing: Prior to initiation of therapy.
Renal Function (Serum Creatinine, eGFR)
Rationale: To assess baseline renal function, although dose adjustment is not typically needed for mild-moderate impairment.
Timing: Prior to initiation of therapy.
Routine Monitoring
Serum Uric Acid (sUA)
Frequency: Every 2 weeks initially until target <6 mg/dL is achieved, then periodically (e.g., every 6 months or as clinically indicated).
Target: <6 mg/dL
Action Threshold: If sUA remains >6 mg/dL after 2 weeks on 40 mg, increase dose to 80 mg. If sUA remains >6 mg/dL on 80 mg, consider alternative therapy.
Liver Function Tests (ALT, AST)
Frequency: Periodically (e.g., at 2 and 4 months after initiation, then annually or as clinically indicated).
Target: Within normal limits
Action Threshold: Discontinue febuxostat if ALT or AST >3 times the upper limit of normal (ULN) or if signs/symptoms of liver injury develop.
Symptom Monitoring
- Signs of gout flares (joint pain, swelling, redness, warmth), especially during initiation of therapy.
- Symptoms of liver injury (unusual fatigue, nausea, vomiting, dark urine, yellowing of skin or eyes, severe stomach pain).
- Cardiovascular symptoms (chest pain, shortness of breath, palpitations, numbness or weakness on one side of the body, slurred speech).
Special Patient Groups
Pregnancy
Febuxostat is Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Limited human data; animal studies showed skeletal abnormalities at high doses.
Second Trimester:
Limited human data.
Third Trimester:
Limited human data.
Lactation
It is unknown 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. Generally advised to avoid.
Infant Risk:
Risk cannot be ruled out (L3 - Moderately Safe, but lack of data suggests caution).
Pediatric Use
Safety and effectiveness in pediatric patients (under 18 years of age) have not been established.
Geriatric Use
No dose adjustment is necessary based on age alone. However, elderly patients may have reduced renal function, which should be considered. Monitor renal function and adverse effects.
Clinical Information
Clinical Pearls
- Febuxostat is typically reserved for patients who are intolerant to allopurinol or for whom allopurinol is contraindicated, especially in patients with pre-existing cardiovascular disease, due to the Black Box Warning regarding increased cardiovascular death.
- Prophylactic anti-inflammatory therapy (e.g., colchicine or NSAIDs) should be initiated concurrently with febuxostat for at least the first 6 months to prevent gout flares, which can paradoxically increase during the initial phase of uric acid lowering.
- The target serum uric acid level is generally <6 mg/dL (or <5 mg/dL for patients with tophi or severe gout).
- Patients should be educated on the importance of adherence and the potential for initial gout flares, as well as symptoms of serious adverse events, particularly cardiovascular and liver-related issues.
Alternative Therapies
- Allopurinol (first-line xanthine oxidase inhibitor)
- Probenecid (uricosuric agent)
- Pegloticase (recombinant uricase enzyme, for refractory chronic gout)
- Lesinurad (selective uric acid reabsorption inhibitor, used in combination with a xanthine oxidase inhibitor)
Cost & Coverage
Average Cost:
Varies widely, typically $30-$100+ per 30 tablets (generic 40mg)
Generic Available:
Yes
Insurance Coverage:
Generic often Tier 2 or 3; Brand often Tier 3 or 4.
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication.
This medication is accompanied by a Medication Guide, a patient fact sheet that provides crucial information. It is vital to read this guide carefully and review it again whenever your prescription is refilled. If you have any questions or concerns about this medication, consult your doctor, pharmacist, or other healthcare provider for guidance.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the quantity, and the time it occurred.
This medication is accompanied by a Medication Guide, a patient fact sheet that provides crucial information. It is vital to read this guide carefully and review it again whenever your prescription is refilled. If you have any questions or concerns about this medication, consult your doctor, pharmacist, or other healthcare provider for guidance.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the quantity, and the time it occurred.