Oxycodone
Appearance
Oxycodone (hydrochloride)
OxyContin (ER), Roxicodone (IR), Oxaydo (IR abuse-deterrent), Xtampza ER (abuse-deterrent ER)
Experience
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Effects
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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
Common uses
Classification(s)
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)[2]
Bioavailability
~60-87% (oral; high and more consistent than codeine or hydrocodone, making efficacy less CYP2D6-genotype-dependent)[2]
Pregnancy
Chronic third-trimester exposure produces neonatal opioid withdrawal syndrome and respiratory depression at delivery.[citation needed]
Legal status
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[1].
References
- ↑ CPIC Guideline for CYP2D6, OPRM1, and COMT and Opioid Use, 2021. https://cpicpgx.org/guidelines/cpic-guideline-for-codeine-and-cyp2d6/
- ↑ 2.0 2.1 2.2 FDA Prescribing Information, OxyContin (oxycodone hydrochloride extended-release), Purdue Pharma, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022272s033lbl.pdf