Oxycodone: Difference between revisions
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{{MedTemplate | {{MedTemplate | ||
| generic = Oxycodone | | generic = Oxycodone (hydrochloride) | ||
| brand = OxyContin | | brand = OxyContin (ER), Roxicodone (IR), Oxaydo (IR abuse-deterrent), Xtampza ER (abuse-deterrent ER) | ||
| classes = Opioid, Analgesic | | structure = | ||
| mechanism = | | classes = [[:Category:Opioid analgesics|Opioid analgesic (semi-synthetic)]], [[:Category:Schedule II controlled substances|Schedule II controlled substance]], [[:Category:Analgesics|Analgesic]] | ||
| uses = <vote slug="moderate-severe-acute-pain-use">Moderate to severe acute pain (FDA)</vote>, <vote slug="post-surgical-pain-use">Postoperative pain (FDA)</vote>, <vote slug="cancer-pain-use">Cancer pain (FDA)</vote>, <vote slug="severe-chronic-pain-use">Severe chronic pain unresponsive to non-opioid alternatives (FDA, with the CDC opioid prescribing guidance constraints)</vote> | |||
| 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 | |||
| fda_max = No fixed ceiling; titrate to clinical effect and tolerability with CDC opioid prescribing guidance constraints on morphine-milligram-equivalent (MME) totals | |||
| pill_id = | |||
| routes = Oral | |||
| onset = 10-30 minutes (IR) | |||
| duration = 4-6 hours (IR); 12 hours (ER) | |||
| halflife = 3-5 hours (IR); 4.5 hours (ER)<ref name="oxycontin-label">FDA Prescribing Information, OxyContin (oxycodone hydrochloride extended-release), Purdue Pharma, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/022272s033lbl.pdf</ref> | |||
| bioavailability = ~60-87% (oral; high and more consistent than codeine or hydrocodone, making efficacy less CYP2D6-genotype-dependent)<ref name="oxycontin-label" /> | |||
| pregnancy = Chronic third-trimester exposure produces neonatal opioid withdrawal syndrome and respiratory depression at delivery.{{citation needed}} | |||
| legal = [[USLegal:Schedule II|Schedule II controlled substance]] in US<ref name="oxycontin-label" /> | |||
| mechanism = <vote slug="oxycodone-mech-claim">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.</vote> 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<ref name="cpic-opioid-cyp2d6">CPIC Guideline for CYP2D6, OPRM1, and COMT and Opioid Use, 2021. https://cpicpgx.org/guidelines/cpic-guideline-for-codeine-and-cyp2d6/</ref>. | |||
}} | }} | ||
== References == | |||
<references /> | |||
[[Category:Opioid analgesics]] | |||
[[Category:Schedule II controlled substances]] | |||
[[Category:Analgesics]] | [[Category:Analgesics]] | ||
Latest revision as of 06:37, 23 May 2026
Oxycodone (hydrochloride)
OxyContin (ER), Roxicodone (IR), Oxaydo (IR abuse-deterrent), Xtampza ER (abuse-deterrent ER)
Experience
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Summary
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)[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