Allopurinol

Allopurinol

DEA Class; Rx

Common Brand Names; Zyloprim, Aloprim

  • Xanthine Oxidase Inhibitors; 
  • Antigout Agents

Purine analog; a xanthine oxidase inhibitor (XOI)
Used in the chronic management of gout and gouty arthritis and prophylaxis of hyperuricemia due to radiation and chemotherapy
Commonly causes rash; fatal hypersensitivity may occur; persons with the HLA-B*5801 haplotype are at risk for serious side effects; must also adjust doses for renal dysfunction

Indicated for Gout and Antineoplastic-Induced Hyperuricemia

 

Patients with a history of severe reaction to any formulation of this drug

  • Rash (1.5%)
  • Nausea (1.3%)
  • Renal failure (1.2%)
  • Vomiting (1.2%)
  • Amblyopia
  • Arthralgias
  • Blood dyscrasias
  • Bronchospasm
  • Cardiovascular abnormalities
  • Cataracts
  • Confusion
  • Decrease in libido
  • Dizziness
  • Ecchymosis
  • Electrolyte abnormalities
  • Epistaxis
  • Foot drop
  • Hematuria
  • Hepatotoxicity
  • Hypotonia
  • Iritis
  • Kidney function abnormality
  • Macular retinitis
  • Malaise
  • Neuritis

Discontinue at first sign of allergic reactions (first sign of rash, vasculitis, or Stevens-Johnson syndrome, drug rash with eosinophilia and systemic symptoms (DRESS) and/or generalized vasculitis, irreversible hepatotoxicity)

The HLA-B*58:01 allele is a genetic marker for severe skin reactions indicative of hypersensitivity to allopurinol; patients who carry the HLA-B*58:01 allele are at a higher risk of allopurinol hypersensitivity syndrome (AHS); however, hypersensitivity reactions reported in patients who do not carry this allele; frequency of this allele is higher in individuals of African, Asian (e.g., Han Chinese, Korean, Thai), and Native Hawaiian/Pacific Islander ancestry; prior to starting therapy, consider testing for the HLA-B*58:01 allele in genetically at-risk populations; therapy not recommended in HLA-B*58:01 positive patients unless benefits clearly outweigh risks

Myelosuppression reported; use caution when administering other drugs known to cause myelosuppression

Hepatotoxicity (reversible) reported

Not for treatment of asymptomatic hyperuricemia

Use with caution in renal impairment

Available limited published data on allopurinol use in pregnant women do not demonstrate a clear pattern or increase in frequency of adverse developmental outcomes.

Adults

800 mg/day PO or 600 mg/day IV. Any single oral dose should not exceed 300 mg PO; higher daily dosages should be administered in divided doses.

Adolescents

300 mg/dose and 800 mg/DAY PO; 200 mg/m2/day (Max: 400 mg/day) IV.

Children

300 mg/dose and 800 mg/DAY PO; 200 mg/m2/day (Max: 400 mg/day) IV.

Allopurinol sodium

tablet

  • 100mg
  • 300mg

powder for injection

  • 500mg/vial
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