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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TROXYCA ER (TROXYCA ER).
| Breastfeeding | M/P ratio unknown. Oxycodone and naltrexone enter breast milk in low amounts; monitor infant for sedation and respiratory depression. Benefits may outweigh risks with short-term use. |
| 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 |
■ 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 |
["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)","Concurrent use of monoamine oxidase inhibitors (MAOIs) or use within 14 days of such therapy","Hypersensitivity to oxycodone, naltrexone, or any component of the product"]
| 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"] |
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| 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. |