Allopurinol: Uses, Dosage & Side Effects

10 min read

Quick Facts

What Is Allopurinol?

Allopurinol is a xanthine oxidase inhibitor that decreases uric acid production by inhibiting the final steps of purine metabolism, effectively reducing serum and urinary uric acid levels.

How Allopurinol Works
Allopurinol inhibits xanthine oxidase, the enzyme responsible for converting hypoxanthine to xanthine and xanthine to uric acid. This reduces uric acid production by 60-80%, preventing gout attacks and hyperuricemia complications.

Indications

  • Chronic gout (prevention of attacks and management of tophaceous gout)
  • Asymptomatic hyperuricemia (serum urate >13 mg/dL or with risk factors)
  • Uric acid nephrolithiasis (kidney stones)
  • Tumor lysis syndrome prophylaxis
  • Secondary hyperuricemia (from chemotherapy, hemolytic anemia)

Dosage and Administration

Gout Prevention:

  • Initial: 50-100 mg daily (some clinicians use 100-200 mg)
  • Increase by 50-100 mg every 2-4 weeks until serum urate <6 mg/dL
  • Maintenance: 300-800 mg daily in 1-3 divided doses
  • Maximum: 800 mg daily (higher doses rarely used)

Tumor Lysis Syndrome:

  • 200-400 mg daily divided into 3-4 doses
  • Start 1-3 days before chemotherapy
Clinical Note
Colchicine or NSAIDs should be given concurrently for the first 3-6 months of allopurinol to prevent gout flares triggered by rapid uric acid lowering. Start low, go slow to minimize hypersensitivity reactions.

Side Effects

Common: Rash (maculopapular), GI upset, diarrhea, headache Serious: Allopurinol hypersensitivity syndrome (fever, rash, eosinophilia, organ dysfunction), hepatotoxicity, Stevens-Johnson syndrome, toxic epidermal necrolysis

Contraindications

  • Asymptomatic hyperuricemia without complications (not routinely indicated)
  • Acute gout attack (use colchicine or NSAIDs first; start allopurinol after attack resolves)
  • Severe hepatic disease
  • HLA-B*5801 allele positive patients (very high hypersensitivity risk, especially in Han Chinese and Thai populations)

Drug Interactions

  • Azathioprine/6-mercaptopurine: increased toxicity; reduce dose to 1/3-1/4
  • Theophylline: increased levels; monitor theophylline concentration
  • Warfarin: potential increased anticoagulant effect; monitor INR
  • Ampicillin: increased rash incidence
  • Thiazide diuretics: increased hyperuricemia risk; monitor urate levels

Key Clinical Evidence

Multiple RCTs demonstrate allopurinol effectively reduces gout attack frequency and resolves tophi. CARES trial (NEJM 2020) showed febuxostat (alternative xanthine oxidase inhibitor) increased cardiovascular events; allopurinol remains preferred agent.

Monitoring Parameters

  • Baseline assessment before initiating therapy
  • Regular clinical follow-up per indication
  • Laboratory parameters as specified in sections above
  • Drug interaction screening at each visit

Special Populations

Dosing adjustments may be necessary in:

  • Renal impairment
  • Hepatic impairment
  • Elderly patients
  • Pregnancy and lactation
  • Pediatric patients

Patient Counseling

  • Take exactly as directed; do not modify dose without consulting healthcare provider
  • Report any unusual symptoms or adverse effects
  • Maintain regular follow-up appointments
  • Store at room temperature away from moisture and light
  • Keep out of reach of children

Disclaimer: This information is for educational purposes only and should not substitute for professional medical advice. Always consult with a qualified healthcare provider before starting, stopping, or modifying any medication.

Sources

  1. [1]undefined. "PubMed Reference." undefined, undefined.
  2. [2]undefined. "PubMed Reference." undefined, undefined.

Medically reviewed by

,

Last updated: 2024-01-01Sources: 2

The content on Medical Atlas is for informational purposes only. It is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider.