Oxycodone-Naloxone

Oxycodone-Naloxone is a prescription medication used to relieve chronic pain. 

• Oxycodone-Naloxone is available under the following different brand names: Targiniq ER

Common side effects of Oxycodone-Naloxone include:

• Nausea,
• Headache,
• Constipation,
• Abdominal pain,
• Vomiting,
• Itching,
• Anxiety,
• Insomnia,
• Back pain, or
• Drug withdrawal syndrome.
• High blood pressure (hypertension).

Serious side effects of Oxycodone-Naloxone include:

• Hives,
• Difficulty breathing,
• Swelling of the face, lips, tongue, or throat,
• Lightheadedness,
• Chest pain,
• Fast or slow heartbeats,
• Shallow breathing,
• Cold or clammy skin,
• Seizures,
• Confusion,
• Severe drowsiness,
• Missed menstrual periods,
• Impotence,
• Loss of interest in sex,
• Nausea,
• Vomiting,
• Loss of appetite,
• Dizziness,
• Worsening tiredness,
• Weakness,
• Agitation,
• Hallucinations,
• Fever,
• Sweating,
• Shivering,
• Muscle stiffness,
• Twitching,
• Loss of coordination, and
• Diarrhea
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms such as fast, irregular, or pounding heartbeats; fluttering in your chest; shortness of breath; and sudden dizziness, lightheartedness, or passing out.
• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors.

Rare side effects of Oxycodone-Naloxone include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult dosage

Extended-release tablet: Schedule II

10 mg/5 mg

• 20 mg/10 mg
• 40 mg/20 mg

Chronic Pain

Adult dosage

• Use as a first opioid analgesic or in non-opioid tolerant patients
• Starting dose: 10 mg/5 mg orally every 12 hours
• Use of higher starting doses in patients who are not opioid tolerant may cause fatal respiratory depression

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Oxycodone-Naloxone has severe interactions with the following drugs
  • Alvimopan
• Oxycodone-Naloxone has serious interactions with at least 72 other drugs.
• Oxycodone-Naloxone has moderate interactions with at least 267 other drugs.
• Oxycodone-Naloxone has minor interactions with the following drugs
  • amiodarone
  • brimonidine
  • celecoxib
  • chloroquine
  • dextroamphetamine
  • diphenhydramine
  • eucalyptus
  • haloperidol
  • imatinib
  • lidocaine
  • paroxetine
  • perphenazine
  • propafenone
  • quinacrine
  • sage
  • thioridazine
  • venlafaxine
  • ziconotide

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• 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

Effects of drug abuse

• Overdose
• Death

Short-Term Effects

• See “What Are Side Effects Associated with Using Oxycodone-Naloxone?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Oxycodone-Naloxone?”

Cautions

• 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 occurs 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, the risk is greatest during initiation of therapy or following dosage increase; monitor patients closely for respiratory depression, especially within the first 24 to 72 hours 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 leveopioids in breast milk because mothers were ultra-rapid metabolizers of opioids
• Profound sedation, respiratory depression, coma, and death may result from concomitant administration with benzodiazepines or other CNS depressants (e.g., non-benzodiazepine sedatives/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, other opioids, alcohol); because of these risks, reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate
• Use in patients with acute or severe bronchial asthma in an unmonitored setting or in absence of resuscitative equipment is contraindicated; patients with significant chronic obstructive pulmonary disease or cor pulmonale, and with substantially decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression are at increased risk of the decreased respiratory drive including apnea, even at recommended dosages
• Monoamine oxidase inhibitors (MAOIs) may potentiate the effects of opioids, opioid active metabolite, including respiratory depression, coma, and confusion; therapy should not be administered within 14 days of initiating or stopping MAOIs
• Cases of adrenal insufficiency reported with opioid use, more often following greater than one month of use; symptoms may include nausea, vomiting, anorexia, fatigue, weakness, dizziness, and low blood pressure; if adrenal insufficiency is diagnosed, treat with physiologic replacement doses of corticosteroids; wean the patient off of the opioid to allow adrenal function to recover and continue corticosteroid treatment until adrenal function recovers; other opioids may be tried as some cases reported use of a different opioid without recurrence of adrenal insufficiency
• Use caution when selecting a dosage for an elderly patient, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function and of concomitant disease or other drug therapy; because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and may be useful to monitor renal function
• Opioid pharmacokinetics may be altered in patients with renal failure; clearance may be decreased, and metabolites may accumulate much higher plasma levels in patients with renal failure as compared to patients with normal renal function; start with a lower-than-normal dosage or with longer dosing intervals and titrate slowly while monitoring for signs of respiratory depression, sedation, and hypotension
• Oxycodone exposes users to the risks of addiction, abuse, and misuse; the tablet is designed to deliver oxycodone over an extended period and contains a larger amount of oxycodone
• Do not ingest alcohol or OTC medications containing alcohol while taking opioid analgesics
• Interactions with CNS depressants: Concomitant use may cause profound sedation, respiratory depression, and death; if coadministration is required, consider a dose reduction of 1 or both drugs
• Elderly, cachectic, debilitated patients, and those with chronic pulmonary disease: Monitor closely because of the increased risk for life-threatening respiratory depression
• May cause severe hypotension, including orthostatic hypotension and syncope; this risk is increased in patients whose ability to maintain blood pressure has been compromised by reduced blood volume or coadministration with certain CNS depressants (. g, phenothiazines, general anesthetics)
• Patients with head injury or increased intracranial pressure: Monitor for sedation and respiratory depression; avoid use in patients with impaired consciousness or coma susceptible to intracranial effects of carbon dioxide retention
• Symptoms consistent with opioid withdrawal occurred in some patients in the clinical trials; monitor patients for symptoms of withdrawal during treatment
• Concomitant use of CYP3A4 inhibitors may increase opioid effects
  • CYP3A4 inducers may increase oxycodone clearance, leading to decreased oxycodone plasma concentrations, decreased efficacy, or abstinence syndrome in physically dependent patients
  • May cause spasms of the sphincter of Oddi; monitor patients with biliary tract disease, including acute pancreatitis, for worsening symptoms (also see Contraindications)
• Opioids may cause increases in the serum amylase
  • May aggravate convulsions in patients with convulsive disorders, and may induce or aggravate seizures in some clinical settings
  • May impair the mental or physical abilities needed to perform potentially hazardous activities
  • Avoid the use of mixed agonists/antagonists. e, pentazocine, nalbuphine, butorphanol) or partial agonist (buprenorphine) analgesics in patients who have received or are receiving a course of therapy with a full opioid agonist analgesic; mixed agonists/antagonists may reduce the analgesic effect and/or may precipitate withdrawal symptoms
  • Do not abruptly discontinue; gradually taper the dose to avoid withdrawal symptoms
  • Prolonged use during pregnancy can result in withdrawal symptoms in the newborn

Pregnancy and Lactation

• Prolonged use of opioid analgesics during pregnancy can cause neonatal opioid withdrawal syndrome; there is no available data on pregnant women to inform a drug-associated risk for major birth defects and miscarriage; published studies with morphine use during pregnancy have not reported a clear association with morphine and major birth defects
• Prolonged use of opioid analgesics during pregnancy for medical or nonmedical purposes can result in physical dependence in the neonate and neonatal opioid withdrawal syndrome shortly after birth; the onset, duration, and severity of neonatal opioid withdrawal syndrome vary based on the specific opioid used, duration of use, timing and amount of last maternal use, and rate of elimination of the drug by newborn; observe newborns for symptoms of neonatal opioid withdrawal syndrome and manage accordingly
• Severe fetal bradycardia was reported when administered during labor; naloxone may reverse these effects; although there are no reports of fetal bradycardia earlier in pregnancy, it is possible it may occur; the drug should be used in pregnancy only if clearly needed if the potential benefit outweighs the risk to the fetus and if appropriate measures such as fetal monitoring are taken to detect and manage the potential adverse effect on the fetus
• Labor or delivery
  • Opioids cross the placenta and may produce respiratory depression and psycho-physiologic effects in neonates; an opioid antagonist, such as naloxone, must be available for reversal of opioid-induced respiratory depression in neonates; the drug is not recommended for use in women during and immediately before  labor when the use of shorter-acting analgesics or other analgesic techniques are more appropriate; opioid analgesics can prolong labor through actions that temporarily reduce strength, duration, and frequency of uterine contractions; however, this effect is not consistent and may be offset by an increased rate of cervical dilatation, which tends to shorten labor; monitor neonates exposed to opioid analgesics during labor for signs of excess sedation and respiratory depression
• Fertility
  • Due to the effects of androgen deficiency, chronic use of opioids may cause reduced fertility in females and males of reproductive potential; it is not known whether the effects on fertility are reversible
• Lactation
  • 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 the early postpartum period
  • The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy, capsules, and any potential adverse effects on the breastfed infant from therapy or from an underlying maternal condition
  • Monitor infants exposed to drugs through breast milk for excess sedation and respiratory depression; withdrawal symptoms can occur in breastfed infants when maternal administration of an opioid analgesic is stopped, or when breastfeeding is stopped
  • Do not initiate Oxycodone-Naloxone in breastfeeding women because of the possibility of sedation or respiratory depression in an infant
  • Withdrawal signs can occur in breastfed infants when maternal administration of an opioid analgesic is stopped or when breastfeeding is stopped; naloxone may precipitate opioid withdrawal in a breast-fed infant whose mother received opioid analgesics