OPANA ER
Clinical safety rating
cautionComprehensive clinical and safety monograph for OPANA ER (OPANA ER).
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.
| 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 |
| Molecular Weight | 337.37 |
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. |
| 1st trimester | Limited human data; animal studies show increased risk of neural tube defects at high doses; use only if benefit outweighs risk. |
| 2nd trimester | May cause fetal dependence and withdrawal; use only if clearly needed. |
| 3rd trimester | Prolonged use may result in neonatal opioid withdrawal syndrome; avoid in late pregnancy unless necessary. |
Clinical note
Comprehensive clinical and safety monograph for OPANA ER (OPANA ER).
| Placental transfer | Oxymorphone crosses the placenta; detected in fetal plasma in animal studies. |
| Breastfeeding | Oxymorphone is excreted in breast milk in low concentrations; monitor infant for sedation and respiratory depression. Consider risk vs benefit. |
| Lactation Rating | L3 (Moderately Safe) |
| 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. |
| Fetal Monitoring | Monitor maternal respiratory rate, sedation level, and bowel function. Fetal: ultrasound for growth restriction (prolonged use), non-stress test and biophysical profile in third trimester, and neonatal monitoring for withdrawal symptoms post-delivery. |
| Fertility Effects | Chronic opioid use may cause menstrual irregularities, anovulation, and reduced fertility. In males, may decrease libido and cause erectile dysfunction. Effects are reversible upon discontinuation. |
■ 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.
| Serious Effects |
Hypersensitivity to oxymorphone or any componentSignificant respiratory depressionAcute or severe bronchial asthmaKnown or suspected paralytic ileusModerate to severe hepatic impairmentConcurrent use of MAOIs or within 14 days
| 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 |
| Food/Dietary | Avoid alcohol as it potentiates CNS depression and increases risk of respiratory depression. Grapefruit juice may increase oxymorphone absorption; consumption should be limited. High-fat meals may delay or decrease absorption; take consistently with or without food to maintain stable levels. |
| Clinical Pearls | OPANA ER is an extended-release formulation of oxymorphone, a mu-opioid agonist. It should only be used for opioid-tolerant patients requiring around-the-clock analgesia. Do not crush, chew, or dissolve tablets, as this leads to rapid release and potential fatal overdose. Conversion from other opioids requires careful dose titration due to incomplete cross-tolerance. Use with caution in elderly, cachectic, or debilitated patients due to increased risk of respiratory depression. Concomitant use with CNS depressants (e.g., benzodiazepines, alcohol) increases risk of profound sedation and respiratory depression. |
| Patient Advice | Take exactly as prescribed; do not alter the tablet's integrity (crushing, chewing, dissolving) as it can cause life-threatening overdose. · Avoid alcohol and other CNS depressants (e.g., sedatives, tranquilizers) while taking this medication. · Do not stop abruptly; withdrawal symptoms may occur. Taper under medical supervision. · Store securely away from children and others; accidental ingestion can be fatal. · Report difficulty breathing, excessive sedation, or signs of allergic reaction immediately. · This medication has abuse potential and should be monitored closely. |
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