Allopurinol
Xanthine oxidase inhibitor first-line for gout urate-lowering therapy and tumor lysis prophylaxis. Parent drug rapidly converted to the active, long-lived metabolite oxypurinol (t1/2 18-30 h), which drives sustained urate lowering. Increasing interest in cardiovascular and longevity applications via reduced oxidative stress. Typical dose 100-600 mg/day titrated to serum urate target.
Projected serum levels — 300 mg, once daily
Maintenance schedule: 300 mg once daily (oral).
Modeled steady state after ~1 days: peak ≈ 178 mg, trough ≈ 2.0 mg body load. Population-based estimate over 15 days for a 300 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.
Key facts
- Category
- Metabolic
- Route modeled
- Oral
- Model confidence
- inferred
- Half-life
- 1.5 h
- Common dose
- 300 mg
- Suggested maximum
- 800 mg/day
- Reference dose range
- 150–800 mg (single dose)
- Suggested cadence
- once daily
- Validated against
- 300 mg oral — Cmax 2.6 mg/L at 1.5 h
Documented interactions
-
moderate
Azathioprine (Imuran) + Allopurinol
Allopurinol mechanism_based of xanthine_oxidase predicted to change Azathioprine (Imuran) AUC by ~1.68x
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moderate
Pyrazinamide (PZA) + Allopurinol
Allopurinol mechanism_based of xanthine_oxidase predicted to change Pyrazinamide (PZA) AUC by ~1.82x
Serum checks 2 modeled interaction pairings for allopurinol across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
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2012 American College of Rheumatology guidelines for management of gout. Part 1: Systematic nonpharmacologic and pharmacologic therapeutic approaches to hyperuricemia
ACR gout guideline establishing allopurinol as first-line urate-lowering therapy with titration to serum urate target <6 mg/dL, including HLA-B*5801 testing in high-risk populations.
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Allopurinol use and risk of fatal cardiovascular disease: a propensity score-matched analysis
Propensity-matched cohort study showed allopurinol use was associated with reduced fatal cardiovascular events in gout patients, supporting broader CV interest beyond urate lowering.
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Clinical pharmacokinetics of allopurinol and oxypurinol
PK review characterizing allopurinol's ~90% oral bioavailability, 1-2 hour parent half-life, rapid conversion to oxypurinol (active metabolite with 18-30 hour half-life), and renal elimination of oxypurinol.
3 published studies referenced in the app, each with a plain-language summary.