OPANA ER

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OPANA ER (OPANA ER).

How it works

Opana ER (oxymorphone hydrochloride) is a full opioid agonist with relative selectivity for the mu-opioid receptor, although it can interact with other opioid receptors at higher doses. The principal therapeutic action is analgesia via activation of mu-opioid receptors in the central nervous system, leading to altered perception and response to pain.

What the body does with it

Metabolism	Oxymorphone is extensively metabolized in the liver via conjugation to oxymorphone-3-glucuronide and, to a lesser extent, via reduction to 6-hydroxy-oxymorphone and conjugation. CYP450-mediated metabolism is minimal.
Excretion	Renal (primarily as glucuronide conjugates and unchanged drug): 85-90%; Fecal: <10%
Half-life	Terminal elimination half-life: 11.1–13.8 hours; clinically relevant as steady-state achieved in 2–3 days
Protein binding	Protein binding: ~80% bound; primarily to albumin
Volume of Distribution	Vd: 2.4–3.5 L/kg; indicates extensive tissue distribution
Bioavailability	Oral (extended-release): 80–87% (relative to immediate-release oxymorphone)
Onset of Action	Oral (extended-release): 1–2 hours; Peak effect: 6–8 hours
Duration of Action	12–24 hours; clinical note: dosing interval is 12 hours for most patients

Classification & Brands

Dosing & administration

Initial: 5 mg orally every 12 hours; titrate by 5-10 mg every 12 hours every 3-7 days; maximum 40 mg every 12 hours.

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	GFR 30-59 mL/min: initiate at 50% of usual dose; GFR <30 mL/min: avoid use (not recommended).
Liver impairment	Child-Pugh Class A: no adjustment; Child-Pugh Class B: initiate at 50% of usual dose; Child-Pugh Class C: avoid use.
Pediatric use	Not approved for use in pediatric patients (safety and efficacy not established).
Geriatric use	Initiate at 50% of usual dose; titrate cautiously; monitor for respiratory depression and cognitive impairment.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for OPANA ER (OPANA ER).

Breastfeeding	Oxymorphone is excreted in breast milk. M/P ratio unknown. Use caution; monitor infant for drowsiness, respiratory depression, and withdrawal symptoms. The American Academy of Pediatrics recommends use only if benefits outweigh risks.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: No adequate studies; animal studies show increased risk of neural tube defects at high doses. Second/third trimester: Prolonged use may cause neonatal opioid withdrawal syndrome (NOWS), respiratory depression, and low birth weight. Avoid during labor to prevent neonatal respiratory depression.

Warnings & precautions

■ FDA Black Box Warning

WARNING: ADDICTION, ABUSE, AND MISUSE; LIFE-THREATENING RESPIRATORY DEPRESSION; ACCIDENTAL INGESTION; NEONATAL OPIOID WITHDRAWAL SYNDROME; and RISKS FROM CONCOMITANT USE WITH BENZODIAZEPINES OR OTHER CNS DEPRESSANTS. See full prescribing information for complete boxed warning.

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 oxymorphone or any other ingredient in the formulation"]

Clinical Precautions

Precautions

["Addiction, abuse, and misuse","Life-threatening respiratory depression","Accidental ingestion","Neonatal opioid withdrawal syndrome","Risks from concomitant use with benzodiazepines or other CNS depressants","Adrenal insufficiency","Severe hypotension","Gastrointestinal effects (constipation, ileus)","Seizures","Use in patients with head injury or increased intracranial pressure"]

Clinical Tips & Counseling

Drug interactions

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OPANA ER

Clinical safety rating: caution

Comprehensive clinical and safety monograph for OPANA ER (OPANA ER).

How it works

What the body does with it

Metabolism	Oxymorphone is extensively metabolized in the liver via conjugation to oxymorphone-3-glucuronide and, to a lesser extent, via reduction to 6-hydroxy-oxymorphone and conjugation. CYP450-mediated metabolism is minimal.
Excretion	Renal (primarily as glucuronide conjugates and unchanged drug): 85-90%; Fecal: <10%
Half-life	Terminal elimination half-life: 11.1–13.8 hours; clinically relevant as steady-state achieved in 2–3 days
Protein binding	Protein binding: ~80% bound; primarily to albumin
Volume of Distribution	Vd: 2.4–3.5 L/kg; indicates extensive tissue distribution
Bioavailability	Oral (extended-release): 80–87% (relative to immediate-release oxymorphone)
Onset of Action	Oral (extended-release): 1–2 hours; Peak effect: 6–8 hours
Duration of Action	12–24 hours; clinical note: dosing interval is 12 hours for most patients

Classification & Brands

Dosing & administration

Initial: 5 mg orally every 12 hours; titrate by 5-10 mg every 12 hours every 3-7 days; maximum 40 mg every 12 hours.

Dosage form	TABLET, EXTENDED RELEASE
Renal impairment	GFR 30-59 mL/min: initiate at 50% of usual dose; GFR <30 mL/min: avoid use (not recommended).
Liver impairment	Child-Pugh Class A: no adjustment; Child-Pugh Class B: initiate at 50% of usual dose; Child-Pugh Class C: avoid use.
Pediatric use	Not approved for use in pediatric patients (safety and efficacy not established).
Geriatric use	Initiate at 50% of usual dose; titrate cautiously; monitor for respiratory depression and cognitive impairment.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for OPANA ER (OPANA ER).

Breastfeeding	Oxymorphone is excreted in breast milk. M/P ratio unknown. Use caution; monitor infant for drowsiness, respiratory depression, and withdrawal symptoms. The American Academy of Pediatrics recommends use only if benefits outweigh risks.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: No adequate studies; animal studies show increased risk of neural tube defects at high doses. Second/third trimester: Prolonged use may cause neonatal opioid withdrawal syndrome (NOWS), respiratory depression, and low birth weight. Avoid during labor to prevent neonatal respiratory depression.