Allopurinol
Allopurinol
Zyloprim, Aloprim (IV)
Experience
No personal reports yet
No clinical reports yet
Log in to add your own experience.
Problems
No problems yet. Be the first to suggest one.
+ Add a problemTitration strategies
No titration strategies yet. Be the first to suggest one.
Effects
No effects listed yet. Be the first to suggest one.
Relevant anecdote
No anecdotes yet. Share a relevant one.
Relevant Literature
No literature entries yet.
Log in to submit relevant literature.
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