Oxycodone

Opioidoral · inferred

Semi-synthetic opioid with intrinsic analgesic activity (unlike codeine). Metabolized to oxymorphone (14x more potent) by CYP2D6 and to noroxycodone by CYP3A4. Half-life ~3.5 hours for immediate release, 4.5 hours for extended release.

Projected serum levels — 5 mg, as needed (shown daily)

Oxycodone
Oxycodone modeled serum levels, 5 mg as needed (shown daily) over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 1 days. 0 1.3 2.5 3.8 5 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 1

Maintenance schedule: 5 mg as needed (shown daily) (oral).

Modeled steady state after ~1 days: peak ≈ 2.8 mg, trough ≈ 0.037 mg body load. Population-based estimate over 15 days for a 5 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Opioid
Route modeled
Oral
Model confidence
inferred
Half-life
3.5 h
Common dose
5 mg
Suggested maximum
60 mg/day
Reference dose range
2.5–60 mg (single dose)
Suggested cadence
as needed (shown daily)
Validated against
10 mg oral — Cmax 0.025 mg/L at 1.5 h

Documented interactions

  • contraindicated
    Efavirenz (Sustiva) + Oxycodone CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Oxycodone AUC by ~0.18x

  • contraindicated
    Rifampin + Oxycodone CYP induction

    Rifampin inducer of CYP3A4 predicted to change Oxycodone AUC by ~0.18x

  • danger
    1,4-BDO (1,4-Butanediol) + Oxycodone Contraindicated

    1,4-BDO converts to GHB, a potent CNS depressant. Combined with opioid respiratory depression, frequently fatal. Delayed 1,4-BDO peak makes timing especially treacherous.

  • danger
    7-Hydroxymitragynine (7-OH) + Oxycodone Contraindicated

    7-Hydroxymitragynine is ~10x more potent than morphine at mu-opioid receptors. Combined with oxycodone, additive mu-agonism creates extreme risk of fatal respiratory depression.

  • danger
    Carbamazepine (Tegretol) + Oxycodone CYP induction

    Carbamazepine (Tegretol) inducer of CYP3A4 predicted to change Oxycodone AUC by ~0.28x

  • danger
    Clarithromycin (Biaxin) + Oxycodone CYP inhibition

    Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Oxycodone AUC by ~2.37x

Serum checks 140 modeled interaction pairings for oxycodone across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Pharmacokinetics and Pharmacodynamics of Oral Oxycodone in Healthy Human Subjects: Role of Circulating Active Metabolites Lalovic B et al. · Clinical Pharmacology & Therapeutics, 2006 DOI

    Evaluated oxycodone and oxymorphone pharmacokinetics in healthy subjects, finding CYP2D6-generated oxymorphone has 40-fold higher mu-opioid affinity but low plasma concentrations.

  2. Updated Clinical Pharmacokinetics and Pharmacodynamics of Oxycodone Kinnunen M et al. · Clinical Pharmacokinetics, 2019 DOI

    Comprehensive update on oxycodone PK/PD covering absorption, distribution, CYP2D6/CYP3A4 metabolism to oxymorphone and noroxycodone, and genetic polymorphism effects on clinical outcomes.

  3. Effect of Opioid vs Nonopioid Medications on Pain-Related Function in Patients With Chronic Back Pain or Hip or Knee Osteoarthritis Pain: The SPACE Randomized Clinical Trial Krebs EE et al. · JAMA, 2018 DOI

    12-month RCT of 240 veterans found opioids (including oxycodone) were NOT superior to non-opioid therapy for pain-related function in chronic back/hip/knee pain; pain intensity was actually worse in the opioid group.

  4. CDC Clinical Practice Guideline for Prescribing Opioids for Pain - United States, 2022 Dowell D et al. · MMWR Recommendations and Reports, 2022 DOI

    Updated CDC guideline recommending non-opioid therapies as first-line for chronic pain, with individualised risk assessment if opioids used; reflects evidence that long-term opioid benefit for non-cancer pain is poorly…

4 published studies referenced in the app, each with a plain-language summary.