Zyloprim: Advanced Uric Acid Control for Gout Management
Zyloprim
Zyloprim is used to treat gout and high uric acid levels in the blood or urine caused by certain types of cancer chemotherapy.
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Synonyms
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Zyloprim, with its active ingredient allopurinol, represents a cornerstone in the long-term pharmacological management of gout and conditions marked by elevated uric acid levels (hyperuricemia). As a xanthine oxidase inhibitor, it operates at the enzymatic source of uric acid production, offering a prophylactic approach rather than merely treating acute inflammatory episodes. This medication is prescribed for patients who experience frequent gout attacks, have tophi, or are at risk of uric acid kidney stone formation. Its efficacy is well-established in clinical practice, providing a strategic method for reducing serum urate concentrations and preventing the debilitating pain associated with crystal deposition.
Features
- Active Pharmaceutical Ingredient: Allopurinol.
- Dosage Form: Film-coated tablets for oral administration.
- Available Strengths: 100 mg and 300 mg tablets.
- Mechanism of Action: Potent inhibitor of the enzyme xanthine oxidase.
- Therapeutic Class: Xanthine Oxidase Inhibitor; Antigout agent.
- Prescription Status: Requires a prescription from a licensed healthcare provider.
Benefits
- Prophylaxis of Gout Attacks: Significantly reduces the frequency and severity of painful acute gout flares by maintaining lower uric acid levels.
- Prevention of Tophus Formation: Aids in the gradual dissolution of existing urate crystal deposits (tophi) and prevents the formation of new ones, protecting joint integrity.
- Reduces Risk of Uric Acid Nephrolithiasis: Lowers the urinary concentration of uric acid, thereby decreasing the likelihood of developing painful kidney stones.
- Management of Hyperuricemia Secondary to Cytotoxic Therapy: Crucial for preventing tumor lysis syndrome-related renal complications in patients undergoing treatment for certain cancers.
- Long-Term Disease Modification: Offers a sustainable, daily management strategy to control the underlying biochemical dysfunction causing gout.
Common use
Zyloprim (allopurinol) is primarily indicated for the management of:
- Chronic gout and recurrent gouty arthritis.
- Hyperuricemia secondary to blood cancers (e.g., leukemias, lymphomas) and their treatment.
- Patients with uric acid nephrolithiasis (kidney stones).
- Hyperuricemia associated with enzymatic disorders such as Lesch-Nyhan syndrome.
It is not intended for the treatment of an acute gout attack, as initiation of therapy can precipitate an acute episode. Anti-inflammatory prophylaxis (e.g., with NSAIDs or colchicine) is often co-administered during the initial months of treatment.
Dosage and direction
Dosage must be individualized based on serum uric acid levels and the specific condition being treated. The goal is to reduce and maintain serum uric acid levels below 6 mg/dL.
- Adults (Gout & Hyperuricemia): Starting dose is typically 100 mg once daily. The dose may be increased by 100 mg weekly until a serum uric acid level of <6 mg/dL is achieved. The average maintenance dose is 200-300 mg daily for mild gout, and 400-600 mg daily for moderate to severe tophaceous gout. Doses exceeding 300 mg should be administered in divided doses.
- Children (Secondary Hyperuricemia): 10 mg/kg/day, up to a maximum of 800 mg/day, administered in 2-3 divided doses.
- Renal Impairment: Dosage adjustment is mandatory. A lower initial dose (e.g., 100 mg every other day or 50-100 mg daily) is recommended, with slower titration and lower maintenance doses based on creatinine clearance.
- Administration: Tablets should be swallowed whole with a full glass of water. To minimize the risk of kidney stone formation, adequate hydration is essential (fluid intake of at least 2 liters daily). Administration after meals can help mitigate gastrointestinal upset.
Precautions
- Hypersensitivity Syndrome: A serious, potentially fatal multi-organ hypersensitivity reaction (Drug Reaction with Eosinophilia and Systemic Symptoms - DRESS) has been associated with allopurinol. Monitor for rash, fever, lymphadenopathy, eosinophilia, and hepatitis. Discontinue immediately at the first sign of rash or hypersensitivity.
- Renal Impairment: Use with extreme caution. Patients with impaired renal function are at increased risk of severe adverse reactions. Dose adjustment is critical.
- Hepatic Impairment: Use cautiously and monitor liver function tests periodically.
- Asymptomatic Hyperuricemia: Generally not recommended unless a patient is undergoing cytotoxic therapy with a high risk of tumor lysis syndrome.
- Pregnancy and Lactation: Use only if clearly needed and the potential benefit justifies the potential risk to the fetus or infant. Allopurinol crosses the placenta and is excreted in breast milk.
- Initial Gout Flare: Initiation of therapy may precipitate an acute gout attack due to the mobilization of urate from tissue deposits. This does not indicate treatment failure. Prophylactic anti-inflammatory therapy is advised for the first few months.
Contraindications
Zyloprim is contraindicated in patients with:
- A history of a severe hypersensitivity reaction to allopurinol or any component of the formulation.
- Patients who are currently experiencing an acute gout attack.
- Patients with a history of allopurinol-induced severe skin reactions, such as Stevens-Johnson Syndrome (SJS) or Toxic Epidermal Necrolysis (TEN).
Possible side effect
Common side effects may include:
- Skin rash (maculopapular) - monitor closely as it may be a precursor to a severe reaction.
- Nausea, vomiting, diarrhea.
- Drowsiness, dizziness.
- Headache.
- Changes in liver function tests.
Serious but less common side effects require immediate medical attention:
- Severe skin reactions: Stevens-Johnson Syndrome (SJS), Toxic Epidermal Necrolysis (TEN), DRESS syndrome.
- Hepatitis, jaundice.
- Eosinophilia, leukopenia, thrombocytopenia, agranulocytosis, aplastic anemia.
- Vasculitis, arthralgia.
- Acute kidney injury, interstitial nephritis.
Drug interaction
Allopurinol can interact with several medications, necessitating dose adjustments or increased monitoring:
- Azathioprine & Mercaptopurine: Allopurinol potently inhibits their metabolism, dramatically increasing their toxicity (myelosuppression). The dose of these drugs must be reduced to ¼ to ⅓ of the usual dose.
- Warfarin: Allopurinol may potentiate its anticoagulant effect, increasing the risk of bleeding. INR should be monitored closely.
- ACE Inhibitors (e.g., lisinopril, enalapril): Increased risk of hypersensitivity reactions, including Stevens-Johnson Syndrome.
- Diuretics (especially Thiazides): May increase the risk of allopurinol hypersensitivity reactions and can reduce the efficacy of allopurinol, requiring a higher dose.
- Ampicillin/Amoxicillin: Increased incidence of skin rash.
- Theophylline: Allopurinol may increase theophylline serum levels.
- Cyclophosphamide: May enhance bone marrow suppression.
- Didanosine: Plasma levels may be increased.
Missed dose
- If a dose is missed, it should be taken as soon as it is remembered.
- However, if it is almost time for the next scheduled dose, the missed dose should be skipped.
- Do not double the dose to make up for a missed one.
Overdose
- Symptoms: Severe nausea, vomiting, diarrhea, and dizziness. In large overdoses, acute renal failure and hepatotoxicity may occur.
- Management: There is no specific antidote. Treatment is supportive and symptomatic. Gastric lavage may be considered if presented early. Adequate hydration is crucial to promote excretion and prevent crystalluria. Hemodialysis may be effective in removing allopurinol and its primary metabolite, oxypurinol.
Storage
- Store at room temperature (20°C to 25°C or 68°F to 77°F), in a dry place, protected from light and moisture.
- Keep the container tightly closed.
- Keep all medications out of the reach of children and pets.
- Do not flush medications down the toilet or pour them into a drain unless instructed to do so.
Disclaimer
This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The information provided is based on the drug’s general profile and may not encompass all possible uses, directions, precautions, or interactions.
Reviews
- “As a rheumatologist with over 20 years of practice, allopurinol remains a first-line, foundational therapy for my patients with chronic gout. Its ability to reliably lower urate levels and prevent long-term joint damage is unparalleled when used correctly. The key is patient education on the prophylactic nature of the drug and careful management during the initiation phase.” – Dr. A. Sharma, MD, Rheumatology.
- “After suffering from debilitating gout attacks for years, starting Zyloprim changed my life. The first few months required patience and colchicine to manage flares, but I haven’t had a significant attack in over two years. My uric acid levels are consistently normal.” – Patient M., 58.
- “The risk of hypersensitivity, while rare, is serious. It mandates that we start low, go slow, and counsel our patients meticulously on the warning signs of a reaction. In patients with renal issues, dose adjustment is non-negotiable.” – Clinical Pharmacist, Renal Unit.
- “The interaction with azathioprine is a critical teaching point in oncology and transplant medicine. We automatically reduce the thiopurine dose by 75% when a patient requires allopurinol, preventing dangerous myelosuppression.” – Oncology Specialist, PharmD.