Allopurinol

Class

  • Xanthine Oxidase Inhibitor

Indications

  • Chronic management of gout to reduce uric acid levels.
  • Prevention of recurrent kidney stones (uric acid stones).
  • Treatment of hyperuricemia associated with cancer chemotherapy or radiation therapy.

Mechanism of Action

  • Inhibits xanthine oxidase, an enzyme responsible for converting hypoxanthine and xanthine into uric acid.
  • Reduces uric acid production, lowering serum and urinary uric acid levels.

Dosage and Administration

For Gout

  • Starting dose: 100 mg daily.
  • Maintenance dose: 200–600 mg daily (mild gout) or up to 800 mg daily (severe gout).
  • Maximum dose: 800 mg daily, divided into 2–3 doses.

For Hyperuricemia in Cancer Therapy

  • Starting dose: 600–800 mg daily, starting 1–2 days before chemotherapy.

For Kidney Stones

  • Typical dose: 200–300 mg daily.

Administration

  • Take after meals to reduce gastrointestinal upset.
  • Drink plenty of fluids to prevent kidney stones and maintain hydration.
  • Doses above 300 mg should be divided to reduce gastrointestinal side effects.

Forms Available

  • Tablets: 100 mg, 300 mg
  • Injectable form (for hospital use): 500 mg vial

Brand Names and Manufacturers

  • Zyloprim (Prometheus Laboratories)
  • Aloprim (injectable form)
  • Generic versions widely available.

Cost

  • Generally affordable, ranging from $10–$50 for a monthly supply, depending on brand and dosage.

Contraindications

  • Hypersensitivity to allopurinol or any component of the formulation.
  • Current acute gout attack (use may worsen symptoms if initiated during an attack).

Precautions

  • Start at a low dose to minimize risk of gout flares when initiating therapy.
  • Use with caution in patients with renal or liver impairment; dosage adjustment may be required.
  • Discontinue immediately if a rash or other hypersensitivity reactions occur.
  • Risk of severe skin reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis.

Side Effects

Common

  • Rash
  • Diarrhea
  • Nausea

Less Common

  • Liver enzyme elevations
  • Drowsiness
  • Acute gout flares (especially when starting therapy)

Rare but Serious

  • Hypersensitivity syndrome (fever, rash, kidney/liver dysfunction)
  • Stevens-Johnson syndrome or toxic epidermal necrolysis
  • Bone marrow suppression

Drug Interactions

  • Azathioprine and Mercaptopurine: Increased toxicity; reduce their dose significantly if used together.
  • Warfarin: Enhanced anticoagulant effect; monitor INR closely.
  • Diuretics (e.g., thiazides): Increased risk of hypersensitivity reactions.
  • Antibiotics (e.g., amoxicillin): Increased risk of rash.

Monitoring Parameters

  • Uric acid levels: Aim for a target of <6 mg/dL in gout patients.
  • Liver and kidney function tests, especially in long-term use.
  • Signs of hypersensitivity or severe skin reactions.

Patient Counseling Points

  • Take after meals with plenty of fluids to reduce stomach upset.
  • Do not stop taking allopurinol during a gout flare; continue as directed by your doctor.
  • Inform your doctor of any rash, fever, or flu-like symptoms, as these may indicate a serious reaction.
  • Avoid alcohol and high-purine foods (e.g., red meat, seafood) to help control uric acid levels.
  • Be patient; full benefits may take weeks to months of consistent use.
  • Always inform healthcare providers about allopurinol use before starting new medications.

FAQs About Allopurinol

Q1: How long does it take for allopurinol to work?

  • It may take 1–2 weeks to lower uric acid levels and longer for gout symptoms to improve.

Q2: Can allopurinol be used during an acute gout attack?

  • No, it should not be started during an acute attack as it may worsen symptoms. It is used for long-term prevention.

Q3: What happens if I miss a dose?

  • Take it as soon as you remember, but skip it if it’s close to the next dose. Do not double doses.

Q4: Can I drink alcohol while taking allopurinol?

  • Alcohol can increase uric acid levels and reduce the effectiveness of allopurinol; it’s best to limit or avoid it.

Q5: Is allopurinol safe during pregnancy?

  • Use only if clearly needed and prescribed by a doctor; discuss risks and benefits with your healthcare provider.

Q6: What should I do if I develop a rash while taking allopurinol?

  • Stop taking allopurinol immediately and contact your doctor, as it may indicate a serious allergic reaction.

Q7: Can I eat a normal diet while on allopurinol?

  • A low-purine diet (avoiding red meat, seafood, and certain alcohols) may help enhance its effectiveness.

Q8: How is allopurinol different from febuxostat?

  • Both lower uric acid levels, but febuxostat may be preferred in patients who cannot tolerate allopurinol.

Q9: Are there natural alternatives to allopurinol?

  • Lifestyle changes like diet modification and hydration can help but are not substitutes for medication.

Q10: Can allopurinol prevent kidney stones?

  • Yes, it can prevent uric acid kidney stones by lowering uric acid levels in the urine.

Q11: Is allopurinol safe for long-term use?

  • Yes, but regular monitoring of kidney and liver function is recommended.

Q12: Can I stop allopurinol if my symptoms improve?

  • No, stopping may cause uric acid levels to rise and trigger gout attacks; always consult your doctor.

Q13: Does allopurinol cause weight gain?

  • No, weight gain is not a known side effect.

Q14: Can children take allopurinol?

  • Yes, in certain conditions like hyperuricemia due to cancer treatment, but under strict medical supervision.

Q15: What are high-purine foods to avoid while on allopurinol?

  • Red meat, organ meats, shellfish, anchovies, and beer

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