Oxycodone

Opioid analgesic (semi-synthetic), Schedule II controlled substance, Analgesic

Oxycodone (hydrochloride)

OxyContin (ER), Roxicodone (IR), Oxaydo (IR abuse-deterrent), Xtampza ER (abuse-deterrent ER)

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Summary

Classes

Opioid analgesic (semi-synthetic), Schedule II controlled substance, Analgesic

Common uses

Moderate to severe acute pain (FDA)▲0▼, Postoperative pain (FDA)▲0▼, Cancer pain (FDA)▲0▼, Severe chronic pain unresponsive to non-opioid alternatives (FDA, with the CDC opioid prescribing guidance constraints)▲0▼

Pharmacy

Starting dose

IR opioid-naive: 5-10 mg PO every 4-6 hours as needed. ER opioid-naive: 10 mg PO every 12 hours (lowest available); titrate slowly to clinical effect

Preparations

IR tablets 5, 7.5, 10, 15, 20, 30 mg; IR oral solution 5 mg/5 mL; concentrated solution 20 mg/mL; OxyContin ER tablets 10, 15, 20, 30, 40, 60, 80 mg; Xtampza ER capsules

US FDA Max

No fixed ceiling; titrate to clinical effect and tolerability with CDC opioid prescribing guidance constraints on morphine-milligram-equivalent (MME) totals

Pharmacology

Routes

Oral

Onset

10-30 minutes (IR)

Duration

4-6 hours (IR); 12 hours (ER)

Half-life

3-5 hours (IR); 4.5 hours (ER)

Bioavailability

~60-87% (oral; high and more consistent than codeine or hydrocodone, making efficacy less CYP2D6-genotype-dependent)

Pregnancy

Chronic third-trimester exposure produces neonatal opioid withdrawal syndrome and respiratory depression at delivery.^{[citation needed]}

Legal status

Schedule II controlled substance in US

Purported mechanism

Semi-synthetic μ-opioid receptor agonist, intermediate in potency between hydrocodone and morphine. Metabolized via CYP3A4 N-demethylation to noroxycodone (largely inactive) and via CYP2D6 O-demethylation to oxymorphone (active, more potent at μ). Unlike codeine and hydrocodone, oxycodone itself is largely the analgesic agent, so efficacy is less CYP2D6-genotype-dependent than for codeine.▲0▼ CYP3A4 inhibitors (ketoconazole, ritonavir, clarithromycin, grapefruit juice) substantially raise plasma exposure. OxyContin's 2010 reformulation introduced an abuse-deterrent matrix that resists crushing and dissolution, a major harm-reduction intervention. CPIC provides CYP2D6 genotype-guided opioid selection guidance.