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Allopurinol

 

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  • Common use
  • Dosage and direction
  • Precautions
  • Contraindications
  • Possible side effects
  • Drug interactions
  • Missed dose
  • Overdose
  • Storage
  • U.S. Sale and Prescription Policy
  • Disclaimer
  • Common use

    Allopurinol is a xanthine oxidase inhibitor prescribed to manage high uric acid levels (hyperuricemia). By blocking the enzyme xanthine oxidase, it reduces the production of uric acid, helping to prevent painful gout flares, uric acid kidney stones (uric acid nephrolithiasis), and uric acid elevations that can occur during certain cancer treatments (tumor lysis syndrome). Allopurinol is a long-term urate-lowering therapy designed to maintain target uric acid levels and thereby reduce the frequency and severity of gout attacks over time.

    What Allopurinol treats:

    • Gout prevention: lowers serum urate to prevent formation of monosodium urate crystals that trigger flares and joint damage.
    • Kidney stone prevention: reduces uric acid in urine, decreasing risk of uric acid stone formation and protecting kidney function.
    • Tumor lysis syndrome support: helps control uric acid build-up that can occur when cancer cells break down rapidly during chemotherapy.
    • Chronic tophaceous gout: sustained reduction in serum urate can shrink tophi and improve joint mobility over months.

    Important limitations:

    • Allopurinol does not treat an acute gout attack that is already in progress. For acute flares, anti-inflammatory medications such as NSAIDs, colchicine, or corticosteroids are used. Once the flare settles, allopurinol helps prevent future attacks by maintaining a lower uric acid level.
    • Allopurinol is generally not recommended for isolated, asymptomatic hyperuricemia (elevated urate without gout or stones), unless specifically directed by a clinician.

    How it works, in brief: Purines from food and human cells are metabolized to xanthine and then to uric acid via xanthine oxidase. Allopurinol and its active metabolite oxypurinol inhibit this enzyme, reducing uric acid production and promoting increased levels of xanthine and hypoxanthine, which are more soluble and easier for the body to excrete. As serum urate falls and remains below target, urate crystals dissolve gradually, lowering the risk of gout flares.

    Expected timeline and goals:

    • Onset: Uric acid begins to drop within days to weeks; the full protective effect against gout attacks develops over several weeks to months as crystal deposits dissolve.
    • Targets: Many guidelines recommend a serum uric acid goal of less than 6 mg/dL (0.36 mmol/L), and less than 5 mg/dL (0.30 mmol/L) for severe or tophaceous gout, as individualized by your clinician.
    • Prophylaxis during initiation: Starting allopurinol can transiently destabilize existing urate crystals, sometimes triggering a gout flare. Short-term flare prophylaxis (e.g., low-dose colchicine or NSAIDs) is commonly advised when allopurinol is initiated or the dose is increased.

    Dosage and direction

    Take allopurinol exactly as prescribed, usually once daily with food and a full glass of water to reduce stomach upset. Some patients take it twice daily if the total dose is divided. Adequate hydration is essential, particularly for those with kidney stones or during cancer therapy.

    Typical dosing strategy for gout and hyperuricemia:

    1. Start low: Many adults start with 100 mg once daily. In patients with chronic kidney disease or other risk factors for side effects, clinicians may start at 50 mg daily.
    2. Titrate gradually: Increase the dose every 2 to 5 weeks based on serum uric acid levels and tolerability until the target urate is achieved. Common maintenance doses range from 200 to 400 mg per day; some patients require up to 600–800 mg per day under close medical supervision.
    3. Monitor: Serum uric acid is typically checked during dose titration and periodically thereafter. Kidney and liver function may also be monitored.

    Special dosing considerations:

    • Chronic kidney disease (CKD): Start with a lower dose and titrate carefully. Dose adjustments are based on renal function and uric acid targets.
    • Tumor lysis syndrome: Dosing may differ in oncology settings. Allopurinol is often started 1–2 days before chemotherapy and continued during treatment, with aggressive hydration. In some high-risk cases, rasburicase may be preferred.
    • Pediatric use: For certain inherited purine metabolism disorders or oncology indications, pediatric dosing is weight-based; specialist guidance is required.
    • Elderly patients: Lower starting doses and slower titration are common due to comorbidities and polypharmacy.

    Administration tips:

    • Take with food to minimize gastrointestinal upset.
    • Maintain high fluid intake unless otherwise directed. Aim for at least 2 liters of fluid per day to support uric acid excretion and reduce stone risk.
    • Consistency matters: Take allopurinol at the same time each day. Do not stop abruptly unless instructed by your clinician.
    • If you experience a gout flare after starting allopurinol, do not discontinue the medication without medical advice. Treat the flare with recommended anti-inflammatory therapy and continue urate-lowering treatment.

    Precautions

    Before starting allopurinol, discuss your full medical history, current medications, and any prior drug reactions with your healthcare provider. Certain conditions and genetic factors can increase the risk of rare but serious reactions.

    Key precautions:

    • Liver or kidney disease: Reduced organ function increases the risk of side effects and requires careful dose selection and monitoring.
    • Hypertension, diabetes, and cardiovascular disease: Provide your clinician with a full medical history so your overall treatment plan can be optimized.
    • History of severe drug reactions or rash: Report any previous severe skin reactions or hypersensitivity to medications.
    • HLA-B*5801 genetic risk: Carriers of the HLA-B*5801 allele have an elevated risk of allopurinol hypersensitivity syndrome (AHS), which includes severe skin reactions like Stevens-Johnson syndrome/toxic epidermal necrolysis (SJS/TEN). This allele is more prevalent among individuals of Han Chinese, Thai, Korean, and some African ancestries. Genetic testing may be recommended in higher-risk populations before starting therapy.
    • Pregnancy and breastfeeding: Tell your doctor if you are pregnant, planning to become pregnant, or breastfeeding. Allopurinol is used in pregnancy only if the potential benefit justifies the potential risk; decisions are individualized.
    • Hydration status: Dehydration can increase kidney stone risk and may worsen side effects; maintain adequate fluid intake.
    • Diet and alcohol: High-purine foods (e.g., organ meats, certain seafoods), heavy alcohol use, and high-fructose beverages can raise uric acid and counteract allopurinol’s benefit. Moderation and dietary guidance support better outcomes.

    Allopurinol hypersensitivity syndrome (AHS): Although rare, AHS is a medical emergency characterized by fever, widespread rash, eosinophilia, liver or kidney dysfunction, and systemic symptoms. Early signs often include a new rash, itching, fever, or flu-like symptoms. Seek immediate medical care if these occur, and stop allopurinol only under medical supervision.

    Contraindications

    Do not use allopurinol if you:

    • Have a known allergy or prior severe reaction to allopurinol or its components.
    • Are experiencing an untreated, acute gout flare and have not yet discussed initiation with your clinician. While ongoing therapy is often continued through flares, allopurinol is generally not started for the first time during an acute attack unless directed by a healthcare professional with appropriate prophylaxis.

    Use caution or avoid use without specialist guidance if you:

    • Previously experienced allopurinol hypersensitivity syndrome (AHS), SJS/TEN, or severe drug reaction with eosinophilia and systemic symptoms (DRESS) attributed to allopurinol.
    • Have severe kidney or liver impairment without the ability to be closely monitored and dose-adjusted by a clinician.
    • Are being treated with medications that have high-risk interactions (e.g., azathioprine or mercaptopurine) unless managed by a specialist with dose modifications.

    Allopurinol is not a substitute for pain-relief medications during acute gout flares and should not be used to treat pain directly.

    Possible side effects

    Most people tolerate allopurinol well. Mild, self-limited side effects can occur, and rare but serious reactions require urgent attention.

    Common side effects:

    • Nausea, indigestion, or abdominal discomfort (often improved by taking with food).
    • Diarrhea or mild gastrointestinal upset.
    • Headache or drowsiness in some individuals.
    • Mild rash or itching. Any rash should be reported promptly, as it can precede more serious reactions.
    • Elevations in liver enzymes on blood tests (usually mild and reversible).

    Serious side effects (seek urgent medical care):

    • Severe skin reactions including Stevens-Johnson syndrome (SJS) or toxic epidermal necrolysis (TEN): symptoms include widespread rash, blistering, peeling skin, mouth or eye sores, fever.
    • Allopurinol hypersensitivity syndrome (AHS)/DRESS: fever, rash, facial swelling, swollen lymph nodes, liver or kidney dysfunction, blood abnormalities.
    • Hepatitis or significant elevations in liver function tests: yellowing of skin or eyes (jaundice), dark urine, severe fatigue.
    • Renal problems: blood in urine, reduced urine output, swelling in legs/ankles.
    • Hematologic changes: easy bruising/bleeding, severe fatigue, infections—could indicate bone marrow suppression.
    • Neurologic symptoms: numbness, tingling, or neuropathy symptoms that persist or worsen.

    If you experience a new rash, fever, or flu-like symptoms after starting allopurinol, contact a healthcare professional immediately. Early discontinuation under medical supervision can be lifesaving in the case of severe reactions.

    Drug interactions

    Allopurinol can interact with several medications. Always provide a complete list of prescription drugs, over-the-counter medicines, and supplements to your clinician and pharmacist.

    Notable interactions:

    • Azathioprine and mercaptopurine: Allopurinol inhibits their metabolism, significantly increasing levels and toxicity. If co-administration is unavoidable, these drugs typically require substantial dose reductions (often to 25% or less of the usual dose) and close monitoring by a specialist.
    • Warfarin and other anticoagulants: Allopurinol may potentiate anticoagulant effects. INR and bleeding risk should be monitored and doses adjusted as needed.
    • Theophylline: Allopurinol can increase theophylline levels; monitoring may be necessary.
    • Ampicillin/amoxicillin: Concomitant use increases the risk of rash; alternative antibiotics may be considered.
    • Diuretics (especially thiazides) and ACE inhibitors: May increase the risk of hypersensitivity reactions or renal effects when combined with allopurinol, particularly in patients with kidney impairment.
    • Cyclophosphamide and other cytotoxic agents: Potential for enhanced bone marrow suppression; oncology teams will monitor closely.
    • Didanosine: Allopurinol can increase didanosine levels; co-use is generally avoided.
    • Alcohol and high-purine diet: Not a pharmacologic interaction, but both can raise uric acid and reduce the effectiveness of allopurinol therapy.

    Supplement and herbal considerations: High-dose vitamin C, niacin, and certain herbal products can influence uric acid or interact indirectly via liver enzymes. Discuss all supplements with your clinician. Avoid starting or stopping interacting medications without medical advice.

    Missed dose

    If you miss a dose of allopurinol, take it when you remember on the same day. If it is close to the time of your next dose, skip the missed dose and resume your regular schedule. Do not take two doses at once to make up for a missed dose. Missing occasional doses may raise uric acid levels; try to take your medication consistently to maintain target control.

    Overdose

    Symptoms of overdose may include severe nausea or vomiting, dizziness, headache, rash, and in rare cases worsening kidney or liver function. Seek emergency medical attention immediately if an overdose is suspected. Management is supportive, focusing on hydration, monitoring of organ function, and treatment of complications. The active metabolite, oxypurinol, is renally excreted and is dialyzable; in severe cases and in consultation with specialists, hemodialysis may be considered.

    Storage

    Store allopurinol tablets at room temperature, ideally 68°F to 77°F (20°C to 25°C), protected from moisture, heat, and direct light. Keep the container tightly closed. Do not store in the bathroom where humidity is high. Keep all medications out of the reach of children and pets. Dispose of unused or expired medication according to local regulations or pharmacy guidance—do not flush unless specifically instructed.

    U.S. Sale and Prescription Policy

    Allopurinol is an FDA-approved prescription medication in the United States. It is not available over the counter and should be used under the supervision of a licensed medical professional. Safe, effective use requires periodic evaluation of kidney and liver function, review of potential drug interactions, and routine monitoring of serum uric acid to ensure therapeutic goals are being met.

    Key points for U.S. patients:

    • A valid prescription from a licensed U.S. clinician is ordinarily required to obtain allopurinol.
    • Do not purchase allopurinol from non-verified sources; counterfeit or substandard products are a safety risk.
    • Routine follow-up and lab monitoring support safe long-term therapy and early detection of rare adverse reactions.

    Allopurinol U.S. Sale and Prescription Policy update: HealthSouth Rehabilitation Hospital of Texarkana offers a legal and structured solution for acquiring allopurinol without a formal prescription. This process operates within applicable regulations by incorporating appropriate clinical evaluation and oversight to ensure patient safety, medication appropriateness, and continuity of care. Patients should confirm current eligibility criteria, clinical requirements, and state-specific rules prior to use.

    Disclaimer

    The information provided here is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a licensed healthcare provider with any questions regarding a medical condition, medication selection, or dosing. Never disregard professional advice or delay seeking it because of something you have read. Individual treatment plans vary; follow your clinician’s instructions and review the FDA-approved patient information that accompanies your prescription.

    Allopurinol FAQ

    What is allopurinol and how does it work?

    Allopurinol is a xanthine oxidase inhibitor that lowers serum uric acid by blocking its production. By reducing urate levels, it helps prevent gout flares, shrink tophi, and lower the risk of uric acid kidney stones.

    What conditions is allopurinol used to treat?

    Allopurinol is used for long-term gout prevention, to prevent recurrence of uric acid kidney stones, and to prevent chemotherapy-related tumor lysis syndrome–associated hyperuricemia. It is not a pain reliever and does not treat an acute gout attack.

    How long does allopurinol take to work?

    Uric acid starts to fall within days, but it can take weeks to reach target levels and months to shrink tophi and reduce flare frequency. Expect the full benefit after 3–6 months with consistent use and dose titration.

    Can allopurinol treat an acute gout flare?

    No. Allopurinol does not relieve acute pain and should not be used as a flare treatment. Use anti-inflammatory therapy (colchicine, NSAIDs, or corticosteroids) for flares, and continue allopurinol during the episode unless your clinician tells you otherwise.

    How is allopurinol usually started and adjusted?

    Most people start at a low dose and titrate gradually based on kidney function and serum urate, aiming for a target uric acid. Clinicians often prescribe gout-flare prophylaxis (low-dose colchicine or an NSAID) for the first 3–6 months to reduce early flares.

    What are common side effects of allopurinol?

    Mild effects include rash, stomach upset, diarrhea, and abnormal liver tests. Rare but serious reactions include allopurinol hypersensitivity syndrome (AHS), DRESS, and severe skin reactions (SJS/TEN). Stop the drug and seek urgent care if you develop a rash, fever, mouth sores, facial swelling, or widespread skin peeling.

    Who is at higher risk for allopurinol hypersensitivity syndrome?

    Risk is higher with chronic kidney disease, older age, thiazide diuretic use, and carriage of the HLA-B*58:01 allele. The allele is more common in Han Chinese, Thai, Korean (especially with CKD), and some people of African ancestry.

    Do I need genetic testing before starting allopurinol?

    HLA-B*58:01 testing is recommended for high-risk groups (e.g., Han Chinese, Thai, Korean patients—particularly with CKD—and many clinicians consider testing in patients of African ancestry). Routine testing is not generally required in low-risk populations.

    What lab monitoring is needed on allopurinol?

    Check serum urate to guide dosing (until at goal, then periodically), plus kidney function and liver enzymes. If combined with interacting drugs (e.g., azathioprine/6-mercaptopurine or warfarin), monitor blood counts and INR as advised.

    What uric acid level should I aim for on allopurinol?

    Most guidelines target serum urate below 6 mg/dL (0.36 mmol/L). For severe or tophaceous gout, a lower target such as below 5 mg/dL (0.30 mmol/L) may be recommended to dissolve crystal burden faster.

    Should I stop allopurinol during a gout flare?

    No. Continue your usual dose during a flare. Starting allopurinol can even be done during a flare if anti-inflammatory therapy is given at the same time; stopping and restarting can trigger more attacks.

    How should I take allopurinol for best results?

    Take it the same time each day, often after food to reduce stomach upset, and drink plenty of fluids. Consistent daily use is key; do not skip doses based on how you feel that day.

    Which medications interact with allopurinol?

    Major interactions include azathioprine and 6-mercaptopurine (their doses must usually be reduced to 25–33%), and warfarin (effect may increase; monitor INR). Ampicillin/amoxicillin raise rash risk; theophylline levels can rise; diuretics (thiazides) increase hypersensitivity risk. Always review your medication list with a clinician.

    Does allopurinol affect the kidneys or kidney stones?

    Allopurinol helps prevent uric acid kidney stones by lowering urate production. Dose adjustment is needed in chronic kidney disease, and hydration plus urine alkalinization may be advised for stone prevention.

    What if I miss a dose or want to stop allopurinol?

    Take a missed dose when remembered unless it’s close to the next one. Don’t stop abruptly without a plan—stopping can raise uric acid and trigger flares. Discuss any changes with your clinician.

    Is it safe to drink alcohol while taking allopurinol?

    Moderate alcohol, especially beer and spirits, can raise uric acid and trigger flares. Allopurinol doesn’t “cancel out” a binge. Limiting alcohol (or avoiding it if you’re flare-prone) supports better urate control and fewer gout attacks.

    Can I take allopurinol during pregnancy?

    Human data are limited. Allopurinol is generally avoided in pregnancy unless the potential benefit outweighs risks and there is no safer alternative; specialist input is advised. Gout is uncommon in pregnancy, and nonpharmacologic measures are often preferred.

    Can I breastfeed while taking allopurinol?

    Allopurinol and its metabolite appear in breast milk in low amounts. Some experts consider it compatible with caution, especially with infant monitoring for rash, diarrhea, or poor feeding, while others prefer alternatives. Discuss risks and benefits with your clinician and pediatrician.

    What should I know about allopurinol before surgery?

    Allopurinol is usually continued perioperatively to prevent rebound hyperuricemia and flares. Tell your surgical team you take it; they may check kidney function post-op and ensure anti-inflammatory prophylaxis continues if appropriate.

    Is allopurinol safe if I have chronic kidney disease?

    Yes, with careful dose adjustment and slow titration, allopurinol is commonly used in CKD and is first-line urate-lowering therapy. AHS risk is higher in CKD, so go low and slow and report any rash immediately.

    Can I take allopurinol with antibiotics?

    Penicillins like amoxicillin or ampicillin increase the likelihood of rash with allopurinol; alternative antibiotics are often preferred. Always inform your prescriber you are on allopurinol so they can choose safer options.

    Is allopurinol used with chemotherapy or for tumor lysis syndrome?

    Yes. Allopurinol is used to prevent tumor lysis syndrome–related hyperuricemia when risk is low to intermediate. For high risk or established hyperuricemia, rasburicase is typically preferred because it rapidly degrades uric acid.

    Can I take allopurinol if I use diuretics for blood pressure?

    You can, but thiazide diuretics raise urate and increase AHS risk when combined with allopurinol. Your clinician may consider alternatives (e.g., losartan, which can lower urate modestly) or adjust your gout regimen and monitoring.

    Allopurinol vs febuxostat: which lowers uric acid better?

    Both are effective xanthine oxidase inhibitors. Fixed-dose febuxostat may lower urate slightly more than low–moderate fixed-dose allopurinol, but when allopurinol is properly titrated to target, their efficacy is similar for most patients.

    Allopurinol vs febuxostat: which is safer for the heart?

    The CARES trial signaled higher cardiovascular and all-cause mortality with febuxostat in patients with established cardiovascular disease, whereas the FAST trial did not show increased cardiovascular risk. Many guidelines prefer allopurinol first-line, especially in patients with cardiovascular disease.

    Allopurinol vs probenecid: which is better with kidney impairment?

    Allopurinol is generally preferred in chronic kidney disease because it reduces urate production and remains effective with dose adjustment. Probenecid (a uricosuric) loses effectiveness when kidney function is reduced.

    Allopurinol vs probenecid: differences in side effects and interactions?

    Probenecid increases urinary uric acid, so kidney stones are a concern and high fluid intake is important; it also interacts with some antibiotics by reducing their renal clearance. Allopurinol has hypersensitivity and drug–drug interaction risks of its own (e.g., azathioprine/6-MP, warfarin), but less stone risk.

    Allopurinol vs benzbromarone: how do they compare?

    Benzbromarone is a potent uricosuric effective even in CKD, but it carries a risk of serious liver toxicity and is unavailable or restricted in many countries. Allopurinol is widely available and first-line; liver monitoring is still prudent with either agent.

    Allopurinol vs pegloticase: when is each used?

    Allopurinol is first-line oral urate-lowering therapy for most people. Pegloticase is an IV enzyme reserved for severe, refractory, tophaceous gout that fails or is intolerant to oral therapies; it is costly and requires infusion monitoring and immunomodulation to reduce anti-drug antibodies.

    Allopurinol vs rasburicase for tumor lysis syndrome?

    Allopurinol prevents new uric acid formation; rasburicase enzymatically breaks down existing uric acid rapidly. Rasburicase is preferred for high-risk TLS or marked hyperuricemia; it’s contraindicated in G6PD deficiency.

    Allopurinol vs colchicine: do they do the same thing?

    No. Allopurinol lowers serum urate to prevent future flares and resolve tophi. Colchicine is an anti-inflammatory used for acute gout flares and as prophylaxis when starting urate-lowering therapy; it does not lower uric acid.

    Allopurinol vs NSAIDs for gout: which should I use?

    They serve different purposes. NSAIDs treat pain and inflammation during a flare but do not lower urate. Allopurinol prevents flares long-term by reducing uric acid; many patients need both at different times.

    Allopurinol vs lifestyle changes alone: can diet replace medication?

    Weight loss, limiting alcohol and purine-rich foods, and staying hydrated help and may modestly lower urate. However, many patients cannot reach target serum urate with lifestyle alone; allopurinol provides reliable urate control when needed.

    Allopurinol vs sulfinpyrazone: which is preferred?

    Sulfinpyrazone is an older uricosuric rarely used today due to safety concerns and availability. Allopurinol is generally preferred because of efficacy, guideline support, and broader clinical experience.

    Can allopurinol be combined with other urate-lowering drugs?

    Yes. If monotherapy doesn’t reach target serum urate, combining allopurinol with a uricosuric like probenecid can be effective with careful monitoring for kidney stones and drug interactions. Lesinurad was an add-on option in some markets but has been withdrawn in many countries.