Oxycodone and naloxone (Oral route)
ox-i-KOE-done hye-droe-KLOR-ide, nal-OX-one hye-droe-KLOR-ide
- Targiniq ER
Warnings:Oral route(Tablet, Extended Release)
Addiction, Abuse, and MisuseOxycodone and naloxone ER exposes patients and other users to the risks of opioid addiction, abuse, and misuse, which can lead to overdose and death. Assess each patient’s risk prior to prescribing oxycodone and naloxone ER and monitor all patients regularly for the development of these behaviors and conditions.Opioid Analgesic Risk Evaluation and Mitigation Strategy (REMS)To ensure that the benefits of opioid analgesics outweigh the risks of addiction, abuse, and misuse, the Food and Drug Administration (FDA) has required a REMS for these products. Under the requirements of the REMS, drug companies with approved opioid analgesic products must make REMS-compliant education programs available to healthcare providers. Healthcare providers are strongly encouraged to: complete a REMS-compliant education program, counsel patients and/or their caregivers, with every prescription, on safe use, serious risks, storage, and disposal of these products, emphasize to patients and their caregivers the importance of reading the Medication Guide every time it is provided by their pharmacist, and consider other tools to improve patient, household, and community safety.Life-Threatening Respiratory DepressionSerious, life-threatening, or fatal respiratory depression may occur with use of oxycodone and naloxone ER. Monitor for respiratory depression, especially during initiation of oxycodone and naloxone ER or following a dose increase. Instruct patients to swallow oxycodone and naloxone ER tablets whole; crushing, chewing, or dissolving oxycodone and naloxone ER tablets can cause rapid release and absorption of a potentially fatal dose of oxycodone.Accidental IngestionAccidental ingestion of even one dose of oxycodone and naloxone ER, especially by children, can result in a fatal overdose of oxycodone.Neonatal Opioid Withdrawal SyndromeProlonged use of oxycodone and naloxone ER during pregnancy can result in neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated, and requires management according to protocols developed by neonatology experts. If opioid use is required for a prolonged period in a pregnant woman, advise the patient of the risk of neonatal opioid withdrawal syndrome and ensure that appropriate treatment will be available.Cytochrome P450 3A4 InteractionThe concomitant use of oxycodone and naloxone ER with all cytochrome P450 3A4 inhibitors may result in an increase in oxycodone plasma concentrations, which could increase or prolong adverse drug effects and may cause potentially fatal respiratory depression. In addition, discontinuation of a concomitantly used cytochrome P450 3A4 inducer may result in an increase in oxycodone plasma concentration. Monitor patients receiving oxycodone and naloxone ER and any CYP3A4 inhibitor or inducer.Risks From Concomitant Use With Benzodiazepines or Other CNS DepressantsConcomitant use of opioids with benzodiazepines or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing of oxycodone and naloxone extended-release and benzodiazepines or other CNS depressants for use in patients for whom alternative treatment options are inadequate. Limit dosages and durations to the minimum required. Follow patients for signs and symptoms of respiratory depression and sedation .
Uses of This Medicine:
Oxycodone and naloxone combination is used to treat pain severe enough to require daily, around-the-clock, long-term opioid treatment and when other pain medicines did not work well enough or cannot be tolerated.
Oxycodone belongs to the group of medicines called narcotic analgesics (pain medicines). It acts on the central nervous system (CNS) to relieve pain. Naloxone is used to treat an opioid emergency such as an overdose or a possible overdose of a narcotic medicine.
Oxycodone and naloxone combination should not be used if you need pain medicine for just a short time, such as when recovering from surgery. Do not use this medicine to relieve mild pain, or in situations when non-narcotic medication is effective. This medicine should not be used to treat pain that you only have once in a while or "as needed".
When oxycodone is used for a long time, it may become habit-forming, causing mental or physical dependence. However, people who have continuing pain should not let the fear of dependence keep them from using narcotics to relieve their pain. Mental dependence (addiction) is not likely to occur when narcotics are used for this purpose. Physical dependence may lead to withdrawal side effects if treatment is stopped suddenly. However, severe withdrawal side effects can usually be prevented by gradually reducing the dose over a period of time before treatment is stopped completely.
This medicine is available only under a restricted distribution program called the Opioid Analgesic REMS (Risk Evaluation and Mitigation Strategy) program.
Before Using This Medicine:
In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:
Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.
Appropriate studies have not been performed on the relationship of age to the effects of oxycodone and naloxone combination in the pediatric population. Safety and efficacy have not been established.
Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of oxycodone and naloxone combination in the elderly. However, elderly patients are more likely to have age-related lung, liver, or kidney problems, which may require caution and an adjustment in the dose for patients receiving oxycodone and naloxone combination.
There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.
Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.
Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- Chloral Hydrate
- Eslicarbazepine Acetate
- Methylene Blue
- Morphine Sulfate Liposome
- Nitrous Oxide
- Opium Alkaloids
- Sodium Oxybate
- Tolonium Chloride
Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.
- St John's Wort
Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.
Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.
- Grapefruit Juice
Other medical problems—
The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:
- Adrenal problems or
- Alcohol abuse, or history of or
- Brain tumor, history of or
- Breathing problems (eg, hypoxia) or
- Chronic obstructive pulmonary disease (COPD) or
- Cor pulmonale (serious heart condition) or
- Depression or
- Drug dependence, especially with narcotics, or history of or
- Gallbladder disease or gallstones or
- Head injuries, history of or
- Weakened physical condition—Use with caution. May increase risk for more serious side effects.
- Asthma, acute or severe or
- Liver disease, moderate to severe or
- Respiratory depression (very slow breathing) or
- Stomach or bowel blockage (eg, paralytic ileus), known or suspected—Should not be used in patients with these conditions.
- Hypotension (low blood pressure) or
- Pancreatitis (swelling of the pancreas) or
- Seizures, history of—Use with caution. May make these conditions worse.
- Kidney disease or
- Liver disease, mild—Use with caution. The effects may be increased because of slower removal of the medicine from the body.
Proper Use of This Medicine:
Take this medicine only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. This is especially important for elderly patients, who may be more sensitive to the effects of pain medicines. If too much of this medicine is taken for a long time, it may become habit-forming (causing mental or physical dependence).
It is very important that you understand the rules of the Opioid Analgesic REMS program to prevent addiction, abuse, and misuse of oxycodone. This medicine should also come with a Medication Guide. Read and follow these instructions carefully. Read it again each time you refill your prescription in case there is new information. Ask your doctor if you have any questions.
Swallow the extended-release tablet whole. Do not break, crush, cut, chew, or dissolve it.
The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
- For oral dosage form (extended-release tablets):
- For moderate to severe pain:
- Patients who are not taking narcotic medicines:
- Adults—At first, 10 milligrams (mg) of oxycodone and 5 mg of naloxone every 12 hours. Your doctor may adjust your dose as needed.
- Children—Use and dose must be determined by your doctor.
- Patients who are taking regular oxycodone:
- Adults—The tablet is given every 12 hours. The total amount of milligrams (mg) per day is half of the total amount of regular oxycodone that is taken per day. The total amount per day will be given as 2 divided doses during the day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 80 mg of oxycodone and 40 mg of naloxone per day.
- Children—Use and dose must be determined by your doctor.
- Patients switching from other narcotic medicines:
- Adults—The tablet is given every 12 hours. The total amount of milligrams (mg) per day will be determined by your doctor and depends on which narcotic you were using. The total amount per day will be given as 2 divided doses during the day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 80 mg of oxycodone and 40 mg of naloxone per day.
- Children—Use and dose must be determined by your doctor.
- Patients who are not taking narcotic medicines:
- For moderate to severe pain:
If you miss a dose of this medicine, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Oxycodone can cause serious unwanted effects if taken by adults who are not used to strong narcotic pain medicines, children, or pets. Make sure you store the medicine in a safe and secure place to prevent others from getting it.
You should flush unused tablets down the toilet.
Precautions While Using This Medicine:
It is very important that your doctor check your progress while you are using this medicine, especially within the first 24 to 72 hours of treatment. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to take it. Blood tests may be needed to check for unwanted effects.
Do not use this medicine if you have used an MAO inhibitor (MAOI) (eg, isocarboxazid [Marplan®], linezolid [Zyvox®], phenelzine [Nardil®], selegiline [Eldepryl®], tranylcypromine [Parnate®]) within the past 14 days.
This medicine may cause a serious type of allergic reaction called anaphylaxis, which can be life-threatening and requires immediate medical attention. Call your doctor right away if you have a rash, itching, hoarseness, trouble breathing, trouble swallowing, or any swelling of your hands, face, or mouth while you are using this medicine.
Do not use more of this medicine or take it more often than your doctor tells you to. This can be life-threatening. Symptoms of an overdose include: extreme dizziness or weakness, slow heartbeat or breathing, seizures, trouble breathing, and cold, clammy skin. Call your doctor right away if you notice these symptoms.
This medicine will add to the effects of alcohol and other CNS depressants (medicines that can make you drowsy or less alert). Some examples of CNS depressants are antihistamines or medicine for allergies or colds, sedatives, tranquilizers, or sleeping medicine, other prescription pain medicine or narcotics, medicine for seizures or barbiturates, muscle relaxants, or anesthetics, including some dental anesthetics. Check with your doctor before taking any of these medicines while you are using this medicine.
This medicine may be habit-forming. If you feel that the medicine is not working as well, do not use more than your prescribed dose. Call your doctor for instructions.
Dizziness, lightheadedness, or fainting may occur when you get up suddenly from a lying or sitting position. Getting up slowly may help lessen this problem. Also, lying down for a while may relieve the dizziness or lightheadedness.
This medicine may make you dizzy, drowsy, or lightheaded. Do not drive or do anything else that could be dangerous until you know how this medicine affects you.
Using narcotics for a long time can cause severe constipation. To prevent this, your doctor may direct you to take laxatives, drink a lot of fluids, or increase the amount of fiber in your diet. Be sure to follow the directions carefully, because continuing constipation can lead to more serious problems.
If you have been using this medicine regularly for several weeks or longer, do not change your dose or suddenly stop using it without checking with your doctor. Your doctor may want you to gradually reduce the amount you are using before stopping it completely. This may help prevent worsening of your condition and reduce the possibility of withdrawal symptoms, such as abdominal or stomach cramps, anxiety, fever, nausea, runny nose, sweating, tremors, or trouble sleeping.
Using this medicine while you are pregnant may cause serious unwanted effects, including neonatal opioid withdrawal syndrome in your newborn baby. Tell your doctor right away if you think you are pregnant or if you plan to become pregnant while using this medicine.
For nursing mothers taking Belbuca®:
- Talk to your doctor if you have any questions about taking oxycodone and naloxone combination or about how this medicine may affect your baby.
- Call your doctor if you become extremely tired and have difficulty caring for your baby.
- Your baby should generally nurse every 2 to 3 hours and should not sleep for more than 4 hours at a time.
- Check with your doctor or hospital emergency room immediately if your baby shows signs of increased sleepiness (more than usual), difficulty breastfeeding, difficulty breathing, or limpness. These may be symptoms of an overdose and need immediate medical attention.
Check with your doctor right away if you have anxiety, restlessness, a fast heartbeat, fever, sweating, muscle spasms, twitching, nausea, vomiting, diarrhea, or see or hear things that are not there. These may be symptoms of a serious condition called serotonin syndrome. Your risk may be higher if you also take certain other medicines that affect serotonin levels in your body.
Using too much of this medicine may cause infertility (unable to have children). Talk with your doctor before using this medicine if you plan to have children.
Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.
Side Effects of This Medicine:
- Incidence not known
- blurred vision
- darkening of the skin
- difficult or troubled breathing
- difficulty swallowing
- dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
- fast heartbeat
- hives, itching, skin rash
- irregular, fast or slow, or shallow breathing
- loss of appetite
- mental depression
- overactive reflexes
- pale or blue lips, fingernails, or skin
- poor coordination
- puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue
- talking or acting with excitement you cannot control
- tightness in the chest
- trembling or shaking
- unusual tiredness or weakness
- Symptoms of overdose
- Bigger, dilated, or enlarged pupils (black part of the eye)
- change in consciousness
- chest pain or discomfort
- cold, clammy skin
- coughing that sometimes produces a pink frothy sputum
- decreased awareness or responsiveness
- difficult, fast, noisy breathing
- increased sensitivity of the eyes to light
- increased sweating
- loss of consciousness
- severe sleepiness
- sleepiness or unusual drowsiness
- slow or irregular heartbeat
- swelling in the legs and ankles
- Less common
- Back pain
- difficulty having a bowel movement
- difficulty with moving
- fear or nervousness
- feeling of warmth
- muscle pain or stiffness
- pain in the joints
- redness of the face, neck, arms, and occasionally, upper chest
- stomach pain
- sudden sweating
- trouble sleeping
Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.
Check with your doctor immediately if any of the following side effects occur:
Get emergency help immediately if any of the following symptoms of overdose occur:
Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:
Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.
Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.
Last Updated: 9/5/2019