TROXYCA ER
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TROXYCA ER (TROXYCA ER).
TROXYCA ER is a fixed-dose combination of oxycodone hydrochloride, a mu-opioid receptor agonist, and naltrexone hydrochloride, a mu-opioid receptor antagonist. Naltrexone is sequestered in the core of the tablet and is not released if taken as directed; however, if crushed or chewed, naltrexone is released and blocks the effects of oxycodone, reducing abuse potential.
| Metabolism | Oxycodone is extensively metabolized in the liver via CYP3A4 and CYP2D6; naltrexone is metabolized primarily to 6β-naltrexol by dihydrodiol dehydrogenase. |
| Excretion | Renal: ~70% as unchanged drug and metabolites (tramadol, acetaminophen), biliary/fecal: ~30%. |
| Half-life | Tramadol: 5–6 hours; acetaminophen: 2–3 hours. Clinical context: Steady-state reached in ~1-2 days. |
| Protein binding | Tramadol: ~20% bound primarily to albumin; acetaminophen: negligible binding (<5%). |
| Volume of Distribution | Tramadol: ~2.6–3.0 L/kg; acetaminophen: ~0.9–1.0 L/kg. Indicates extensive tissue distribution for tramadol. |
| Bioavailability | Oral: ~75% (tramadol); acetaminophen: ~88%. |
| Onset of Action | Oral: ~30–60 minutes. |
| Duration of Action | Analgesic effect: 4–6 hours (due to acetaminophen component); tramadol component provides extended relief. |
| Molecular Weight | Oxycodone: 315.36 Da; Naltrexone: 341.4 Da; Naloxone: 327.37 Da |
One capsule orally once daily at approximately the same time each day. The dosage strength should be individualized based on prior opioid use and tolerance. For opioid-naive patients, initiate with the lowest available strength (e.g., 60 mg/3.2 mg). Titrate no more frequently than every 3-7 days as needed.
| Dosage form | CAPSULE, EXTENDED RELEASE |
| Renal impairment | For GFR 30-89 mL/min: No adjustment recommended. For GFR 15-29 mL/min: Initiate with 60 mg/3.2 mg once daily and titrate cautiously; monitor for respiratory depression. For GFR <15 mL/min: Not recommended due to accumulation of metabolites. |
| Liver impairment | For Child-Pugh Class A (mild impairment): No adjustment. For Child-Pugh Class B (moderate impairment): Initiate with 60 mg/3.2 mg once daily and titrate cautiously. For Child-Pugh Class C (severe impairment): Not recommended. |
| Pediatric use | Not approved for use in pediatric patients (safety and efficacy not established). |
| Geriatric use | Initiate with the lowest available strength (60 mg/3.2 mg) once daily and titrate cautiously due to increased sensitivity and risk of respiratory depression; consider renal function decline. |
| 1st trimester | Teratogenic risk: Fetal opioid dependence syndrome potential; use only if maternal benefit outweighs fetal risk. Limited human data; animal studies not available. |
| 2nd trimester | Risk of premature labor, low birth weight, and neonatal withdrawal; use only if clearly needed. |
| 3rd trimester | Risk of neonatal opioid withdrawal syndrome, respiratory depression at birth; avoid prolonged use near term. |
Clinical note
Comprehensive clinical and safety monograph for TROXYCA ER (TROXYCA ER).
| Placental transfer | Oxycodone readily crosses the placenta; naltrexone and naloxone cross to a lesser degree but detectable in fetal plasma. |
| Breastfeeding | TROXYCA ER is not recommended during breastfeeding. Oxycodone is excreted in breast milk; naltrexone and naloxone may be present in low amounts. Monitor infant for respiratory depression, sedation, and withdrawal. |
■ 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
| Serious Effects |
Hypersensitivity to oxycodone, naltrexone, naloxone, or any componentSignificant respiratory depressionAcute or severe bronchial asthma in unmonitored settings or without resuscitative equipmentParalytic ileusPatients receiving opioid agonists (e.g., methadone) for opioid use disorder
| Precautions | Addiction, abuse, and misuse, Life-threatening respiratory depression, Accidental ingestion (especially in children), Neonatal opioid withdrawal syndrome, Risks from concomitant use with benzodiazepines or other CNS depressants, Interaction with alcohol, Risk of severe hypotension, Risk of seizures in patients with seizure disorders, Avoid use in patients with gastrointestinal obstruction |
| Food/Dietary | Avoid alcohol and alcoholic beverages. No specific food restrictions; however, a high-fat meal may slightly increase oxycodone absorption, but no dose adjustment needed. |
Loading safety data…
| Lactation Rating | L4 (Hazardous) |
| Teratogenic Risk | First trimester: No adequate human data; animal studies show no teratogenicity at exposures up to 10 times MRHD. Second/third trimester: Prolonged use may cause neonatal opioid withdrawal syndrome (NOWS) and respiratory depression at birth. Avoid chronic use. |
| Fetal Monitoring | Monitor maternal respiratory rate, sedation, bowel function. Fetal: assess growth and amniotic fluid volume with chronic use; neonatal monitoring for NOWS if used near term. |
| Fertility Effects | No human data; animal studies show no impairment of fertility at doses up to 10 times MRHD. Opioid use may affect hormonal regulation; consider endocrine effects. |
| Clinical Pearls | TROXYCA ER is a fixed-dose combination of oxycodone and naltrexone designed for abuse deterrence. The naltrexone is sequestered and released only if the tablet is crushed, precipitating withdrawal in opioid-dependent individuals. It is not indicated for PRN use; only for around-the-clock management of severe chronic pain. Avoid in patients with opioid dependence due to risk of precipitated withdrawal. Do not administer with alcohol or other CNS depressants due to additive effects. Monitor for respiratory depression, especially in elderly or debilitated patients. |
| Patient Advice | Take exactly as prescribed; do not crush, chew, or dissolve tablets. · This medication contains an opioid that can be habit-forming; use only for your pain and do not share with others. · Do not drink alcohol while taking this medication; it can increase the risk of severe drowsiness and respiratory depression. · Common side effects include constipation, nausea, dizziness, and drowsiness; report severe or persistent symptoms. · Store safely out of reach of children and dispose of unused tablets via a take-back program or flushing (per FDA guidelines). · Do not stop abruptly without talking to your doctor to avoid withdrawal symptoms. |