Oxycodone/Naloxone

DEA Class; Rx

Common Brand Names; Targiniq ER

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

Naloxone: Antagonist of mu, kappa, and delta opioid receptors, with greatest affinity for the mu receptor; produces opioid withdrawal signs and symptoms in individuals physically dependent on full opioid agonists when administered parenterally

Significant respiratory depression

Acute or severe bronchial asthma

Known or suspected paralytic ileus and GI obstruction

Known hypersensitivity to oxycodone or naloxone

Moderate-to-severe hepatic impairment

• 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

Cases of serotonin syndrome, a potentially life-threatening condition, reported with concomitant use of serotonergic drugs; this may occur within the recommended dosage range; the onset of symptoms generally occur within several hours to a few days of concomitant use, but may occur later than that; discontinue therapy immediately if serotonin syndrome is suspected

While serious, life-threatening, or fatal respiratory depression can occur at any time during therapy, risk is greatest during initiation of therapy or following dosage increase; monitor patients closely for respiratory depression, especially within first 24 to 72 hr of initiating therapy with and following dosage increases; accidental ingestion of even one dose, especially by children, can result in respiratory depression and death due to overdose of opioid

Deaths have occurred in nursing infants exposed to high levels of opioid in breast milk because mothers were ultra-rapid metabolizers of opioid

Prolonged use of opioid analgesics during pregnancy can cause neonatal opioid withdrawal syndrome; there are no available data in pregnant women to inform a drug associated risk for major birth defects and miscarriage

Drug is present in breast milk; published lactation studies report variable concentrations of drug in breast milk with administration of immediate-release formulation to nursing mothers in early postpartum period