Oxycodone And Naloxone (Oral Route) Before Using

Description and Brand Names

Drug information provided by: Merative, Micromedex®

US Brand Name

Targiniq ER

Canadian Brand Name

Targin

Descriptions

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

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:

Allergies

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.

Pediatric

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.

Geriatric

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.

Breastfeeding

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.

Drug Interactions

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.

Levoketoconazole
Nalmefene
Naltrexone
Safinamide
Samidorphan

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.

Abiraterone Acetate
Acepromazine
Aclidinium
Adagrasib
Alfentanil
Almotriptan
Alosetron
Alprazolam
Alvimopan
Amantadine
Amifampridine
Amineptine
Amiodarone
Amitriptyline
Amitriptylinoxide
Amobarbital
Amoxapine
Amphetamine
Amprenavir
Anileridine
Apalutamide
Aprepitant
Aripiprazole
Aripiprazole Lauroxil
Armodafinil
Asciminib
Asenapine
Atazanavir
Atropine
Avacopan
Baclofen
Belladonna
Benperidol
Bentazepam
Benzhydrocodone
Benzphetamine
Benztropine
Berotralstat
Biperiden
Boceprevir
Bosentan
Bromazepam
Bromopride
Brompheniramine
Buprenorphine
Bupropion
Buspirone
Butabarbital
Butorphanol
Calcium Oxybate
Cannabidiol
Cannabis
Carbamazepine
Carbinoxamine
Carisoprodol
Carphenazine
Celecoxib
Cenobamate
Ceritinib
Cetirizine
Chloral Hydrate
Chlordiazepoxide
Chlorpheniramine
Chlorpromazine
Chlorzoxazone
Cimetidine
Cinacalcet
Ciprofloxacin
Citalopram
Clarithromycin
Clemastine
Clidinium
Clobazam
Clomipramine
Clonazepam
Clopidogrel
Clorazepate
Cloxazolam
Clozapine
Cobicistat
Cocaine
Codeine
Conivaptan
Crizotinib
Cyclobenzaprine
Cyclopentolate
Cyclosporine
Cyproheptadine
Dabrafenib
Dantrolene
Daridorexant
Darifenacin
Darunavir
Delavirdine
Delorazepam
Desipramine
Desmopressin
Desvenlafaxine
Dexamethasone
Dexmedetomidine
Dextroamphetamine
Dextromethorphan
Dezocine
Diacetylmorphine
Diazepam
Dibenzepin
Dichloralphenazone
Dicyclomine
Difenoxin
Dihydrocodeine
Diltiazem
Dimenhydrinate
Diphenhydramine
Diphenoxylate
Dolasetron
Donepezil
Doxepin
Doxylamine
Dronedarone
Droperidol
Duloxetine
Efavirenz
Elagolix
Eletriptan
Enasidenib
Enflurane
Enzalutamide
Erythromycin
Escitalopram
Esketamine
Eslicarbazepine Acetate
Estazolam
Eszopiclone
Ethchlorvynol
Ethopropazine
Ethylmorphine
Etravirine
Fedratinib
Fenfluramine
Fentanyl
Fesoterodine
Fexinidazole
Flavoxate
Flibanserin
Fluconazole
Flunitrazepam
Fluoxetine
Fluphenazine
Flurazepam
Fluspirilene
Fluvoxamine
Fosamprenavir
Fosaprepitant
Fosnetupitant
Fosphenytoin
Fospropofol
Frovatriptan
Furazolidone
Gabapentin
Gabapentin Enacarbil
Gepirone
Glycopyrrolate
Glycopyrronium Tosylate
Granisetron
Halazepam
Haloperidol
Halothane
Hexobarbital
Homatropine
Hydrocodone
Hydromorphone
Hydroxyamphetamine
Hydroxytryptophan
Hydroxyzine
Hyoscyamine
Idelalisib
Imatinib
Imipramine
Indinavir
Ipratropium
Iproniazid
Isocarboxazid
Isoflurane
Itraconazole
Ivacaftor
Ketamine
Ketazolam
Ketobemidone
Ketoconazole
Lacosamide
Lanreotide
Larotrectinib
Lasmiditan
Lefamulin
Lemborexant
Lenacapavir
Letermovir
Levocetirizine
Levomilnacipran
Levorphanol
Linezolid
Lisdexamfetamine
Lithium
Lofepramine
Lofexidine
Lomitapide
Lopinavir
Loprazolam
Lorazepam
Lorcaserin
Lorlatinib
Lormetazepam
Loxapine
Lumacaftor
Magnesium Oxybate
Mavacamten
Meclizine
Medazepam
Melitracen
Melperone
Mepenzolate
Meperidine
Mephobarbital
Meprobamate
Meptazinol
Mesoridazine
Metaclazepam
Metaxalone
Methadone
Methamphetamine
Methdilazine
Methocarbamol
Methohexital
Methotrimeprazine
Methylene Blue
Methylnaltrexone
Metoclopramide
Mibefradil
Midazolam
Mifepristone
Milnacipran
Mirabegron
Mirtazapine
Mitotane
Mobocertinib
Moclobemide
Modafinil
Molindone
Moricizine
Morphine
Morphine Sulfate Liposome
Nafcillin
Nalbuphine
Naldemedine
Nalorphine
Naloxegol
Naloxone
Naratriptan
Nefazodone
Nelfinavir
Netupitant
Nevirapine
Nialamide
Nicomorphine
Nilotinib
Nirogacestat
Nitrazepam
Nitrous Oxide
Nordazepam
Nortriptyline
Octreotide
Olanzapine
Oliceridine
Omaveloxolone
Ondansetron
Opipramol
Opium
Opium Alkaloids
Orphenadrine
Oxazepam
Oxcarbazepine
Oxitropium Bromide
Oxybutynin
Oxycodone
Oxymorphone
Ozanimod
Palbociclib
Palonosetron
Papaveretum
Paregoric
Paroxetine
Pentazocine
Pentobarbital
Perampanel
Perazine
Periciazine
Perphenazine
Phenelzine
Phenobarbital
Phenytoin
Pimozide
Pinazepam
Pipenzolate Bromide
Piperacetazine
Pipotiazine
Pirenzepine
Piritramide
Pirtobrutinib
Posaconazole
Potassium Oxybate
Prazepam
Prednisone
Pregabalin
Primidone
Procarbazine
Prochlorperazine
Procyclidine
Promazine
Promethazine
Propantheline
Propiverine
Propofol
Protriptyline
Quazepam
Quetiapine
Quinidine
Quinine
Ramelteon
Ranitidine
Ranolazine
Rasagiline
Remifentanil
Remimazolam
Remoxipride
Repotrectinib
Ribociclib
Rifabutin
Rifampin
Rifapentine
Ritlecitinib
Ritonavir
Rizatriptan
Rolapitant
Ropeginterferon Alfa-2b-njft
Saquinavir
Scopolamine
Secobarbital
Selegiline
Selpercatinib
Sertindole
Sertraline
Sibutramine
Sodium Oxybate
Solifenacin
Sotorasib
Stramonium
Sufentanil
Sulpiride
Sumatriptan
Suvorexant
Tapentadol
Taurursodiol
Telaprevir
Telithromycin
Temazepam
Terbinafine
Terodiline
Tetrazepam
Thiethylperazine
Thiopental
Thiopropazate
Thioridazine
Thiothixene
Tianeptine
Tilidine
Tiotropium
Tizanidine
Tocilizumab
Tolonium Chloride
Tolterodine
Topiramate
Tramadol
Tranylcypromine
Trazodone
Triazolam
Trifluoperazine
Trifluperidol
Triflupromazine
Trihexyphenidyl
Trimeprazine
Trimipramine
Trofinetide
Tropicamide
Trospium
Tryptophan
Tucatinib
Umeclidinium
Venlafaxine
Verapamil
Vilazodone
Vonoprazan
Voriconazole
Vortioxetine
Voxelotor
Zaleplon
Ziprasidone
Zolmitriptan
Zolpidem
Zopiclone
Zotepine
Zuranolone

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.

Clonidine
St John's Wort
Yohimbine

Other Interactions

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.

Ethanol
Grapefruit Juice

Proper Use

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.

Dosing

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.

Missed Dose

If you miss a dose of this medicine, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

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.

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.

Drop off any unused narcotic medicine at a drug take-back location right away. If you do not have a drug take-back location near you, flush any unused narcotic medicine down the toilet. Check your local drug store and clinics for take-back locations. You can also check the DEA web site for locations. Here is the link to the FDA safe disposal of medicines website: www.fda.gov/drugs/resourcesforyou/consumers/buyingusingmedicinesafely/ensuringsafeuseofmedicine/safedisposalofmedicines/ucm186187.htm

Precautions

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

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:

Incidence not known

Agitation
blurred vision
confusion
cough
darkening of the skin
diarrhea
difficult or troubled breathing
difficulty swallowing
dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
fast heartbeat
fever
hives, itching, skin rash
irregular, fast or slow, or shallow breathing
loss of appetite
mental depression
nausea
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
restlessness
seizures
shivering
sweating
talking or acting with excitement you cannot control
tightness in the chest
trembling or shaking
twitching
unusual tiredness or weakness
vomiting

Get emergency help immediately if any of the following symptoms of overdose occur:

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

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:

Less common

Back pain
difficulty having a bowel movement
difficulty with moving
fear or nervousness
feeling of warmth
headache
muscle pain or stiffness
pain in the joints
redness of the face, neck, arms, and occasionally, upper chest
stomach pain
sudden sweating
trouble sleeping

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.

Portions of this document last updated: April 01, 2024

Original article: https://www.mayoclinic.org/es-es/drugs-supplements/oxycodone-and-naloxone-oral-route/before-using/drg-20112977

Oxycodone And Naloxone (Oral Route)