BLACK BOX WARNING
- addiction, abuse, and misuse with potential for overdose and death
- life-threatening respiratory depression
- accidental ingestion can be fatal to children
- neonatal opioid withdrawal syndrome
- interaction with benzodiazepines and CNS depressants
oxycodone
Brand: OxyContin, Roxicodone, Percocet (with acetaminophen)
⚠ BBW ISMP High Alert Prototype: morphine
Drug Class: opioid analgesic
Drug Family: opioid
Subclass: semi-synthetic mu-opioid agonist
Organ Systems: cns
Mechanism of Action
Full agonist at mu-opioid receptors; approximately 1.5 times more potent than oral morphine. Available in immediate-release (IR) and extended-release (ER) formulations; the ER formulation was at the center of the opioid epidemic when its misuse potential (crushing/snorting) was exploited.
mu-opioid receptor (MOR)kappa-opioid receptor (KOR)
Indications
- moderate to severe pain
Contraindications
- significant respiratory depression
- acute or severe asthma
- paralytic ileus
Adverse Effects
Common
- constipation
- nausea
- somnolence
- dizziness
- pruritus
Serious
- respiratory depression
- opioid use disorder
- overdose death
- neonatal opioid withdrawal syndrome
Pharmacokinetics (ADME)
| Absorption | oral bioavailability ~60-87%; food has minimal effect on IR; high-fat meal may increase ER peak concentration |
| Distribution | protein binding ~45%; Vd ~2.6 L/kg |
| Metabolism | primarily CYP3A4 (to inactive noroxycodone) and CYP2D6 (to active oxymorphone); CYP2D6 poor metabolizers may have reduced analgesia |
| Excretion | primarily renal |
| Half-life | IR: 3-5 hours; ER: 4.5 hours (but designed for 12-hour dosing) |
| Onset | IR: 10-30 minutes; ER: 1 hour |
| Peak | IR: 1-2 hours; ER: 4-5 hours |
| Duration | IR: 4-6 hours; ER: 12 hours |
| Protein Binding | 45% |
| Vd | 2.6 L/kg |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| CNS depressants (especially benzodiazepines) | additive respiratory depression; major contributor to overdose death | major |
| CYP3A4 inhibitors | increase oxycodone levels; increase respiratory depression risk | major |
| CYP3A4 inducers | decrease oxycodone levels; may precipitate withdrawal or inadequate pain control | major |
Nursing Considerations
- Extended-release oxycodone tablets must NOT be crushed, chewed, or dissolved — this destroys the controlled-release mechanism, causing rapid absorption of the full dose with potentially fatal respiratory depression.
- Combination products (Percocet) contain acetaminophen; verify total daily acetaminophen dose from all sources does not exceed 4000 mg/day (3000 mg/day in elderly or those with hepatic disease).
- Document pain scores, sedation level (Pasero Opioid-Induced Sedation Scale), and respiratory rate before each dose; hold and notify prescriber if sedation scale ≥3.
- The combination of oxycodone with benzodiazepines is the most common cause of prescription opioid overdose death — perform medication reconciliation and alert prescriber to concurrent use.
Clinical Pearls
- OxyContin's extended-release formulation, initially marketed as abuse-deterrent because the coating supposedly prevented crushing, was misused by dissolving — this contributed significantly to the opioid epidemic of the 2000s.
- Oxycodone's activation to oxymorphone via CYP2D6 is clinically less important than codeine's similar conversion; oxycodone itself is a potent analgesic independent of CYP2D6 metabolizer status.
Safety Profile
Pregnancy avoid
Lactation use-with-caution
Renal Adjustment Required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.