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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Uloric
Generic Name
Febuxostat
Active Ingredient
FebuxostatCategory
Xanthine Oxidase Inhibitor [EPC]
Variants
2
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Uloric, you must consult a qualified healthcare professional.
Detailed information about Uloric
Febuxostat is a potent, non-purine selective xanthine oxidase inhibitor used for the chronic management of hyperuricemia in adult patients with gout who have an inadequate response to allopurinol.
The dosing of febuxostat must be individualized based on the patient's serum uric acid (sUA) levels and clinical response.
Febuxostat is currently NOT approved for use in pediatric patients (under 18 years of age). The safety and effectiveness of the drug in children have not been established in clinical trials. Parents and caregivers should consult a pediatric rheumatologist for alternative treatments for hyperuricemia in children.
No significant differences in safety or efficacy have been observed between elderly patients (65 years and older) and younger adults. No dose adjustment is generally required based solely on age, though clinicians should always consider the patient's overall renal and cardiovascular status.
If you miss a dose of febuxostat, take it as soon as you remember. If it is almost time for your next scheduled dose, skip the missed dose and resume your regular schedule. Do not take two doses at once to make up for a missed one.
In the event of an overdose, contact a poison control center or seek emergency medical attention immediately. While specific data on febuxostat overdose are limited, symptoms may include exaggerated side effects such as severe nausea, gastrointestinal distress, or signs of an allergic reaction. Treatment is primarily supportive, focusing on managing symptoms and maintaining hydration.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or stop taking this medication without medical guidance, as this can cause uric acid levels to spike and trigger severe gout flares.
While many patients tolerate febuxostat well, some experience side effects during the initial phases of treatment. The most common side effects reported in clinical trials include:
Febuxostat is a potent medication that requires careful clinical oversight. It is not a first-line treatment for gout and should be reserved for specific patient populations as defined by the FDA. Patients must be aware that this medication is for the long-term control of uric acid and will not provide immediate relief during an acute gout flare.
Cardiovascular Death: The FDA has issued its highest level of warning for Febuxostat. Clinical data indicates an increased risk of heart-related death in patients taking Febuxostat compared to those taking allopurinol. This warning is particularly relevant for patients with a history of heart disease, stroke, or heart failure. Patients should be monitored for signs and symptoms of cardiovascular events, such as chest pain or shortness of breath.
Febuxostat is a potent inhibitor of xanthine oxidase, which is the primary enzyme responsible for the metabolism of certain purine-based drugs. Using these drugs together can lead to toxic levels of the following medications:
There are specific scenarios where Febuxostat must NEVER be used because the risks far outweigh any potential benefits:
These are conditions where the drug should be used with extreme caution and only if no other options are available:
Pregnancy Category C (Previous FDA classification): There are no adequate and well-controlled studies of febuxostat in pregnant women. Animal reproduction studies using high doses did not show clear evidence of teratogenicity (birth defects), but animal data does not always predict human response. Febuxostat should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Most rheumatologists recommend attempting to control gout through diet or other means before using XO inhibitors during pregnancy.
It is not known whether febuxostat is excreted in human milk. In animal studies, febuxostat was found to be excreted in the milk of lactating rats and was associated with decreased development in the offspring. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing 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.
Safety and effectiveness in pediatric patients under the age of 18 have not been established. Gout is rare in children; however, for conditions like Lesch-Nyhan syndrome or secondary hyperuricemia, other treatments with better-established pediatric safety profiles are typically used.
Febuxostat is a non-purine selective inhibitor of xanthine oxidase. Its molecular structure is 2-[3-cyano-4-(2-methylpropoxy) phenyl]-4-methylthiazole-5-carboxylic acid. Unlike allopurinol, which is a purine analog that must be converted to its active metabolite oxypurinol, febuxostat is active in its parent form.
Xanthine oxidase exists in two interconvertible forms: xanthine dehydrogenase and xanthine oxidase. Febuxostat inhibits both forms. It works by creating a highly stable binding interaction with the molybdenum-pterin center of the enzyme, effectively 'plugging' the channel that leads to the active site. This prevents the substrate (hypoxanthine or xanthine) from entering, thus halting the production of uric acid. Because it is not a purine analog, it does not inhibit other enzymes in the purine/pyrimidine pathway, such as guanine deaminase or orotidine-5'-monophosphate decarboxylase.
Febuxostat produces a dose-dependent decrease in serum uric acid levels. A reduction in sUA is typically seen within 24 hours of the first dose. The maximum effect is usually observed within 2 weeks of consistent dosing. Studies have shown that febuxostat 40 mg is roughly equivalent to allopurinol 300 mg in uric acid-lowering potency, while febuxostat 80 mg is significantly more potent than the standard 300 mg dose of allopurinol.
Common questions about Uloric
Febuxostat is primarily used for the chronic management of high uric acid levels (hyperuricemia) in adults with gout. It is specifically reserved for patients who have not responded well to allopurinol or who cannot tolerate allopurinol due to side effects. By lowering uric acid, it helps prevent the formation of crystals in the joints that cause painful gout attacks. It is not intended for the treatment of acute gout flares that are already happening. Regular use can lead to a significant reduction in the frequency of gout episodes over time.
The most frequently reported side effects include liver function test abnormalities, nausea, joint pain, and skin rashes. Many patients also experience a temporary increase in gout flares when they first start the medication, which is why doctors often prescribe a second medicine like colchicine for the first few months. While most side effects are mild, the drug does carry a serious warning regarding cardiovascular risks. Patients should report any chest pain, shortness of breath, or signs of a stroke to their doctor immediately. Liver enzymes are usually monitored through blood tests to ensure the drug isn't causing hepatic stress.
There is no direct drug interaction between febuxostat and alcohol, but drinking alcohol is generally discouraged for people with gout. Alcohol, particularly beer and spirits, can increase the production of uric acid and trigger painful gout flares, potentially neutralizing the benefits of the medication. Additionally, both alcohol and febuxostat are processed by the liver, so combining them may increase the risk of liver strain. It is best to discuss your alcohol consumption with your healthcare provider to determine what is safe for your specific condition. Most experts recommend limiting alcohol to minimize gout recurrence.
Febuxostat is generally not recommended during pregnancy unless the potential benefits clearly outweigh the risks to the fetus. There are no adequate, well-controlled studies in pregnant women to confirm its safety. Animal studies have not shown direct birth defects, but data is insufficient to rule out risks in humans. If you are pregnant or planning to become pregnant, you should discuss alternative ways to manage your gout with your rheumatologist. Most doctors prefer to avoid this medication during pregnancy and breastfeeding if possible.
Febuxostat begins to lower serum uric acid levels within 24 hours of the first dose, but it takes about two weeks of consistent daily use to reach a stable, maximum effect. While your blood levels of uric acid will drop quickly, it may take several months (6 months or more) of treatment before you notice a decrease in the number of gout flares. This is because it takes time for the existing uric acid crystals in your joints to dissolve. Consistency is key, and you should not stop taking the medication if you don't feel immediate relief. Your doctor will monitor your blood work to confirm the drug is working.
You should not stop taking febuxostat suddenly without consulting your healthcare provider. Gout is a chronic condition, and stopping the medication will likely cause your uric acid levels to rise back to their previous high levels very quickly. This sudden spike can trigger a severe and painful gout flare. If you need to stop the medication due to side effects, your doctor will provide a plan to manage your uric acid levels through other means. Long-term adherence is necessary to prevent joint damage and tophi formation.
If you miss a dose of febuxostat, you should take it as soon as you remember on that same day. However, if it is almost time for your next scheduled dose, you should skip the missed dose and simply take the next one at your regular time. Never take two doses at once to 'catch up,' as this can increase the risk of side effects. To help remember your dose, try taking it at the same time every day, such as with breakfast. If you frequently miss doses, talk to your pharmacist about using a pill organizer or a reminder app.
Weight gain is not a commonly reported side effect of febuxostat in clinical trials. Most patients taking the medication do not experience significant changes in their body weight due to the drug itself. However, many people with gout are advised to make dietary changes and lose weight as part of their overall treatment plan, which can sometimes lead to confusion about the drug's effects. If you notice rapid or unusual weight gain while taking this medication, it could be a sign of fluid retention or another underlying issue, and you should consult your doctor. Monitoring your weight is a good practice for general health while managing gout.
Febuxostat has several important drug interactions that must be managed. It should never be taken with azathioprine or mercaptopurine, as it can cause these drugs to reach toxic, life-threatening levels in the blood. It may also interact with theophylline, requiring careful dose monitoring. However, it is commonly and safely taken alongside NSAIDs or colchicine, which are used to prevent flares during the start of therapy. Always provide your doctor and pharmacist with a complete list of all medications, including over-the-counter supplements, to ensure there are no dangerous interactions.
Yes, febuxostat is available as a generic medication, which makes it much more affordable than the original brand-name version, Uloric. Generic versions are required by the FDA to have the same active ingredient, strength, dosage form, and route of administration as the brand-name drug. They must also prove bioequivalence, meaning they work the same way in the body. Choosing the generic version can significantly lower your out-of-pocket costs while providing the same therapeutic benefit. Check with your pharmacist or insurance provider to see if the generic version is covered under your plan.
Other drugs with the same active ingredient (Febuxostat)
> Warning: Stop taking Febuxostat and call your doctor immediately if you experience any of these serious symptoms:
With prolonged use, the primary concern is the cumulative effect on the cardiovascular system and liver. Long-term studies, such as the CARES and FAST trials, have focused on these risks. Patients on long-term therapy should have periodic blood tests to ensure their liver and kidneys are functioning correctly and to monitor for any emerging cardiovascular symptoms.
Febuxostat carries a significant FDA Black Box Warning regarding Cardiovascular Death.
Summary of Warning:
In a large clinical safety study (the CARES trial), patients with gout and established cardiovascular disease who were treated with febuxostat had a higher rate of cardiovascular death compared to those treated with allopurinol. The study found that while the overall rate of major adverse cardiovascular events (MACE) was similar between the two drugs, the risk of death from a heart-related cause was significantly higher in the febuxostat group.
Because of this risk, febuxostat should only be used in patients who have not responded adequately to allopurinol, who are intolerant to allopurinol, or for whom allopurinol is not appropriate. Healthcare providers should consider the cardiovascular history of the patient before prescribing and monitor for signs of cardiovascular events during treatment.
Report any unusual symptoms to your healthcare provider immediately. Early intervention is key to managing drug-related complications.
To ensure the safe use of febuxostat, healthcare providers will typically order the following tests:
Febuxostat may cause dizziness or somnolence (sleepiness) in some individuals. Patients should observe how they react to the medication before driving, operating heavy machinery, or engaging in tasks that require mental alertness.
While there is no direct chemical interaction between febuxostat and alcohol, alcohol consumption (especially beer and hard liquor) is a well-known trigger for gout flares and can increase uric acid production. Limiting alcohol is a key component of gout management. Furthermore, both alcohol and febuxostat can stress the liver, so excessive drinking should be avoided.
Do not stop taking febuxostat without consulting your doctor. Sudden discontinuation can cause serum uric acid levels to rise rapidly, leading to a high risk of severe gout flares and the progression of joint damage. There is no known withdrawal syndrome, but the underlying condition (hyperuricemia) will return if the medication is stopped.
> Important: Discuss all your medical conditions, especially any history of heart disease or liver problems, with your healthcare provider before starting Febuxostat.
Febuxostat primarily affects serum uric acid tests. It does not typically interfere with common urine or blood chemistry panels, other than the intended effect on urate and the potential elevation of liver enzymes.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking. A simple interaction check can prevent serious medical complications.
There is evidence to suggest that patients who have experienced a skin reaction or hypersensitivity to allopurinol may also react to febuxostat. While they are chemically different (purine vs. non-purine), the underlying immune predisposition to react to XO inhibitors may overlap. Physicians should exercise extreme caution when switching a patient from allopurinol to febuxostat due to a previous rash.
> Important: Your healthcare provider will evaluate your complete medical history, including your heart health and previous drug allergies, before prescribing Febuxostat.
Clinical studies of febuxostat included a significant number of subjects aged 65 and over. No overall differences in safety or effectiveness were observed between these subjects and younger subjects. Pharmacokinetic studies have shown that age does not significantly alter the absorption or disposition of febuxostat. Therefore, no dose adjustment is necessary for elderly patients, provided their renal function is adequate.
No dose adjustment is necessary in patients with mild to moderate hepatic impairment (Child-Pugh Class A and B). For those with severe impairment, the drug has not been studied, and clinicians typically monitor liver enzymes more frequently if the drug is initiated.
> Important: Special populations require individualized medical assessment. Always inform your doctor if you are planning to become pregnant or if you have underlying kidney or liver issues.
| Parameter | Value |
|---|---|
| Bioavailability | ~84% |
| Protein Binding | 99.2% (primarily to albumin) |
| Half-life | 5–8 hours |
| Tmax | 1–1.5 hours |
| Metabolism | UGT conjugation and CYP1A2, 2C8, 2C9 oxidation |
| Excretion | Renal 49%, Fecal 45% |
Febuxostat belongs to the therapeutic class of Antigout Agents and the pharmacological class of Xanthine Oxidase Inhibitors. It is the first non-purine selective XOI to be approved for clinical use, providing a distinct chemical alternative to the older purine-analog inhibitors like allopurinol.