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    DEA Class; Rx

    Common Brand Names; Targiniq ER

    • Opioid Analgesics
    • Opioid Reversal Agents

    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

    Indicated for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate

    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


    Use as first opioid analgesic or in non-opioid tolerant patients

    • Starting dose: 10 mg/5 mg PO q12hr
    • Use of higher starting doses in patients who are not opioid tolerant may cause fatal respiratory depression

    Titration and maintenance

    • May be up-titrated from current dose by increasing by 10 mg/5 mg q12hr q1-2 days as needed based on efficacy, safety, and tolerability
    • Not to exceed daily dose of 80 mg/40 mg (ie, 40 mg/20 mg q12hr)
    • If breakthrough pain experienced, assess need for a dosage increase or a rescue dose of an immediate-release analgesic

    Opioid tolerant patients

    • Patients who are opioid tolerant are those receiving the following for ≥1 week:
    • -≥60 mg/day PO morphine
    • -≥25 mcg/hr transdermal fentanyl
    • -≥30 mg/day PO oxycodone
    • -≥8 mg/day PO hydromorphone
    • -≥25 mg/day PO oxymorphone, OR
    • -Equianalgesic dose of another opioid


    <18 years: Safety and efficacy not established


    <18 years: Safety and efficacy not established

    Oxycodone Hydrochloride/naloxone

    extended-release tablet: Schedule II

    • 10 mg/5 mg
    • 20 mg/10 mg
    • 40 mg/20 mg