Oxycodone/Naltrexone

DEA Class; Rx

Common Brand Names; Troxyca ER

Opioid agonist/opioid antagonist combination product

Oxycodone: Opioid agonist; relatively selective for the mu receptor, but it can bind to other opioid receptors at higher doses; inhibits ascending pain pathways, thus altering response to pain; produces analgesia, respiratory depression, and sedation

Naltrexone: Opioid competitive receptor antagonist; shows highest affinity for mu receptors

Patients with significant respiratory depression

Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment

Known or suspected GI obstruction, including paralytic ileus

Hypersensitivity (eg, anaphylaxis) to oxycodone or naltrexone or any other components of the formulation

• Nausea (7-8%)
• Vomiting (2-5%)
• Headache (3-4%)
• Constipation (3%)
• Abdominal pain (3%)
• Back pain (3%)
• Anxiety (1-3%)
• Pruritus (2%)
• Insomnia (1-2%)
• Gastrointestinal disorders: Abdominal pain, constipation, diarrhea, nausea, and vomiting
• General disorders and administration site conditions: Drug withdrawal syndrome, fatigue, pain, malaise, and drug ineffective
• Injury, poisoning, and procedural complications: Inadequate analgesia
• Neoplasms benign, malignant, and unspecified (including cysts and polyps): Malignant neoplasm progression
• Nervous system disorders: Dizziness, headache, tremor, and somnolence
• Psychiatric disorders: Restlessness, confusional state, and anxiety
• Respiratory, thoracic, and mediastinal disorders: Dyspnea
• Skin and subcutaneous tissue disorders: Hyperhidrosis and pruritus

Contains oxycodone, a Schedule II controlled drug; as an opioid, oxycodone/naltrexone exposes users to the risks of addiction, abuse, and misuse; as extended-release products (eg, Troxyca ER) deliver the opioid over an extended period, there is a greater risk for overdose and death owing to the larger amount of oxycodone present (see Black Box Warnings)

Prolonged use during pregnancy can result in neonatal withdrawal syndrome that may be fatal if not recognized and managed by neonatal experts (see Black Box Warnings)

Adrenal insufficiency reported with opioid use (greater incidence if used >1 month); if adrenal insufficiency diagnosed, treat with physiologic replacement of corticosteroids, and wean patient off of the opioid

Severe hypotension reported, including orthostatic hypotension and syncope in ambulatory patients; risk increases in patients whose ability to maintain blood pressure has already been compromised by a reduced blood volume or concurrent administration of certain CNS depressant drugs (eg, phenothiazine, general anesthetics); monitor for severe hypotension during dosage initiation and titration; avoid use with circulatory shock

Oxycodone/naltrexone may further reduce respiratory drive and exacerbate CO2 retention in patients with increased ICP or brain tumors; may also obscure the clinical course in a patient with a head injury; avoid use with impaired consciousness or coma

Pregnancy

Prolonged use during pregnancy may cause neonatal opioid withdrawal syndrome (see Black Box Warnings)

Lactation

Oxycodone is present in breast milk; because of the potential for serious adverse reactions, including excess sedation and respiratory depression in a breastfed infant, breastfeeding is not recommended during treatment with oxycodone/naltrexone