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OpioidCalc

Oxycodone conversion and pharmacology

A semi-synthetic opioid widely used for acute and chronic pain management.

Agonist
Oral
Parenteral
Rectal

Equianalgesic estimate

20mg Oral ≈ 30mg Oral Morphine

Published equianalgesic ratios vary between references and with clinical context. Read how to interpret conversion results before applying an estimate.

Mechanism of action

Agonist at mu, kappa, and delta opioid receptors, with the strongest affinity for mu receptors.

Brand names: OxyContin, Roxicodone, Percocet (w/ APAP)

Pharmacokinetics

Protein binding
38-45%
Volume of distribution
2.6 L/kg
Half-life
3-5 hours (IR), ~4.5 hours (ER)
Oxycodone pharmacokinetic parameters by route
RouteFormBioavailabilityOnsetPeakDuration
OralIR60-87%10-30 min1-2 hours3-6 hours
OralER~1 hour~3 hours12 hours

Metabolism

  • CYP3A4/5 (N-demethylation)
  • CYP2D6 (O-demethylation)

Metabolites

  • Oxymorphone Potent analgesic (formed via CYP2D6).
  • Noroxycodone Weak activity (formed via CYP3A4/5); major circulating metabolite.

Major CYP3A4 substrate. CYP3A4 inhibitors (e.g., clarithromycin, ketoconazole) significantly increase oxycodone levels. CYP3A4 inducers (e.g., rifampin) decrease levels. Oxymorphone contribution depends on CYP2D6 status.

Renal and hepatic impairment

Renal

Use with caution. Parent compound and metabolites accumulate. Dose reduction recommended (e.g., 25-50% reduction depending on severity).

Hepatic

Clearance significantly reduced. Start with 1/3 to 1/2 the usual dose and titrate carefully.

Clinical cautions

  • Higher oral bioavailability than morphine.
  • Often combined with acetaminophen; monitor total daily APAP dose (max 4g/day).

For qualified healthcare professionals. This page is an educational reference, not prescribing advice. Check medicine information and conversion factors against a current clinical source and local guidance.

Other opioids in this reference

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Last updated 30 August 2026. Read how to interpret conversion results and the Terms of Service.