ROXICODONE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ROXICODONE (ROXICODONE).

How it works

Oxycodone is a full opioid agonist with high affinity for mu-opioid receptors, also binding to kappa and delta receptors. It acts primarily on the central nervous system and gastrointestinal tract.

What the body does with it

Metabolism	Hepatic, primarily via CYP3A4 and CYP2D6; major metabolites include noroxycodone and oxymorphone.
Excretion	Renal excretion: 70-80% as unchanged drug and metabolites (oxymorphone, noroxycodone); fecal: 10-20%.
Half-life	3.5-5 hours for immediate-release; 4.5-5.5 hours for extended-release. Accumulation may occur with repeated dosing, especially in elderly or hepatic impairment.
Protein binding	45% bound to albumin.
Volume of Distribution	2.0-2.5 L/kg. Large Vd indicates extensive tissue distribution, including to brain and adipose tissue.
Bioavailability	Oral immediate-release: 60-87%; oral extended-release: 40-60% (first-pass metabolism); intravenous: 100%; intramuscular: ~80%.
Onset of Action	Oral immediate-release: 10-15 min; oral extended-release: 60-120 min; intravenous: 2-3 min; intramuscular: 10-15 min.
Duration of Action	Immediate-release: 4-6 hours; extended-release: 8-12 hours. Duration may be shorter with acute pain or longer with chronic use.

Classification & Brands

Dosing & administration

5-15 mg orally every 4-6 hours as needed for pain; immediate-release formulation. Maximum 60 mg total daily dose for opioid-naive patients.

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	For eGFR 30-59 mL/min: administer at 50-75% of usual dose; for eGFR 10-29 mL/min: 50% of usual dose; for eGFR <10 mL/min: avoid use or use 25% of usual dose with extended intervals.
Liver impairment	Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: avoid use or reduce dose by 75% with extended dosing intervals.
Pediatric use	Children aged 11 years and older: 0.1-0.2 mg/kg per dose orally every 4-6 hours as needed; maximum 10 mg per dose. Not recommended for children under 11 years due to limited data.
Geriatric use	Initiate at 3-5 mg orally every 4-6 hours; titrate cautiously. Avoid in patients with severe renal or hepatic impairment. Monitor for respiratory depression, constipation, and falls.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for ROXICODONE (ROXICODONE).

Breastfeeding	Roxicodone (oxycodone) is excreted in breast milk; relative infant dose (RID) is approximately 2.5-5% of maternal weight-adjusted dose. M/P ratio: approximately 3.2:1. Use with caution; monitor infant for respiratory depression, sedation, and withdrawal. If used, lowest effective dose and shortest duration.
Teratogenic Risk	First trimester: Increased risk of neural tube defects and congenital heart defects (odds ratio 2.0-3.0 for any opioid). Second and third trimesters: Risk of fetal growth restriction, preterm birth, and neonatal opioid withdrawal syndrome (NOWS). Considered low to moderate teratogenic risk; no specific malformation pattern identified.

Warnings & precautions

■ FDA Black Box Warning

Risk of addiction, abuse, and misuse; life-threatening respiratory depression; accidental ingestion; neonatal opioid withdrawal syndrome; risks from concomitant use with benzodiazepines or other CNS depressants; interaction with alcohol.

Side Effect Profile

Serious Effects

Absolute Contraindications

Significant respiratory depression; acute or severe bronchial asthma in an unmonitored setting or in absence of resuscitative equipment; known or suspected gastrointestinal obstruction, including paralytic ileus; hypersensitivity to oxycodone or any component of the product.

Clinical Precautions

Precautions

Addiction, abuse, and misuse; life-threatening respiratory depression; neonatal opioid withdrawal syndrome; risks from concomitant use with benzodiazepines; severe hypotension; adrenal insufficiency; seizures; risks in patients with head injuries, increased intracranial pressure; severe hypertension; gastrointestinal obstruction; impaired renal or hepatic function; elderly and debilitated patients; pregnancy; lactation.

Clinical Tips & Counseling

Drug interactions

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ROXICODONE

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ROXICODONE (ROXICODONE).

How it works

Oxycodone is a full opioid agonist with high affinity for mu-opioid receptors, also binding to kappa and delta receptors. It acts primarily on the central nervous system and gastrointestinal tract.

What the body does with it

Metabolism	Hepatic, primarily via CYP3A4 and CYP2D6; major metabolites include noroxycodone and oxymorphone.
Excretion	Renal excretion: 70-80% as unchanged drug and metabolites (oxymorphone, noroxycodone); fecal: 10-20%.
Half-life	3.5-5 hours for immediate-release; 4.5-5.5 hours for extended-release. Accumulation may occur with repeated dosing, especially in elderly or hepatic impairment.
Protein binding	45% bound to albumin.
Volume of Distribution	2.0-2.5 L/kg. Large Vd indicates extensive tissue distribution, including to brain and adipose tissue.
Bioavailability	Oral immediate-release: 60-87%; oral extended-release: 40-60% (first-pass metabolism); intravenous: 100%; intramuscular: ~80%.
Onset of Action	Oral immediate-release: 10-15 min; oral extended-release: 60-120 min; intravenous: 2-3 min; intramuscular: 10-15 min.
Duration of Action	Immediate-release: 4-6 hours; extended-release: 8-12 hours. Duration may be shorter with acute pain or longer with chronic use.

Classification & Brands

Dosing & administration

5-15 mg orally every 4-6 hours as needed for pain; immediate-release formulation. Maximum 60 mg total daily dose for opioid-naive patients.

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	For eGFR 30-59 mL/min: administer at 50-75% of usual dose; for eGFR 10-29 mL/min: 50% of usual dose; for eGFR <10 mL/min: avoid use or use 25% of usual dose with extended intervals.
Liver impairment	Child-Pugh Class A: no adjustment; Child-Pugh Class B: reduce dose by 50%; Child-Pugh Class C: avoid use or reduce dose by 75% with extended dosing intervals.
Pediatric use	Children aged 11 years and older: 0.1-0.2 mg/kg per dose orally every 4-6 hours as needed; maximum 10 mg per dose. Not recommended for children under 11 years due to limited data.
Geriatric use	Initiate at 3-5 mg orally every 4-6 hours; titrate cautiously. Avoid in patients with severe renal or hepatic impairment. Monitor for respiratory depression, constipation, and falls.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for ROXICODONE (ROXICODONE).

Breastfeeding	Roxicodone (oxycodone) is excreted in breast milk; relative infant dose (RID) is approximately 2.5-5% of maternal weight-adjusted dose. M/P ratio: approximately 3.2:1. Use with caution; monitor infant for respiratory depression, sedation, and withdrawal. If used, lowest effective dose and shortest duration.
Teratogenic Risk	First trimester: Increased risk of neural tube defects and congenital heart defects (odds ratio 2.0-3.0 for any opioid). Second and third trimesters: Risk of fetal growth restriction, preterm birth, and neonatal opioid withdrawal syndrome (NOWS). Considered low to moderate teratogenic risk; no specific malformation pattern identified.