Allopurinol
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Allopurinol
Zyloprim, Aloprim (IV)
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Summary
Pharmacy
Starting dose
100 mg PO once daily; titrate by 100 mg every 2-4 weeks to a serum urate target (typically <6 mg/dL, or <5 in tophaceous disease)
Preparations
100 mg, 300 mg tablets; IV 500 mg vial
US FDA Max
800 mg/d (rarely needed)
Pharmacology
Routes
Oral, IV
Onset
Serum urate falls gradually over days to weeks; acute flare prevention requires colchicine cover during initiation
Duration
24 hours
Half-life
1-2 hours (parent); 18-30 hours for active metabolite oxypurinol[2]
Bioavailability
~80% (oral)[2]
Pregnancy
Limited safety data; weigh benefit individually.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Allopurinol is a purine analog that competitively inhibits xanthine oxidase (and is itself metabolized by the enzyme to oxypurinol, also a xanthine oxidase inhibitor), blocking the conversion of hypoxanthine to xanthine and xanthine to uric acid.0 HLA-B*58:01 carriage is strongly associated with severe cutaneous adverse reactions (Stevens-Johnson syndrome, toxic epidermal necrolysis, DRESS), with the strongest risk signal in Han Chinese, Thai, and Korean populations; CPIC and several regulators recommend pre-prescription HLA-B*58:01 testing in those populations[1].
References
- ↑ CPIC Guideline for HLA-B and Allopurinol, 2016 (update). https://cpicpgx.org/guidelines/guideline-for-allopurinol-and-hla-b/
- ↑ 2.0 2.1 FDA Prescribing Information, Zyloprim (allopurinol), Casper Pharma, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/016084s048lbl.pdf