Oxycodone and naloxone

In the U.S.

• Targiniq ER

In Canada

• Targin

Available Dosage Forms:

• Tablet, Extended Release

Pharmacologic Class: Naloxone

Chemical Class: Oxycodone

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 oxycodone and naloxone, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to oxycodone and naloxone 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 in order to avoid potentially serious side effects.

Pregnancy

Breast Feeding

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.

Interactions with Medicines

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 oxycodone and naloxone, 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 oxycodone and naloxone 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.

• Amifampridine
• Nalmefene
• Naltrexone
• Safinamide

Using oxycodone and naloxone 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
• Acepromazine
• Alfentanil
• Almotriptan
• Alprazolam
• Alvimopan
• Amineptine
• Amiodarone
• Amisulpride
• Amitriptyline
• Amitriptylinoxide
• Amobarbital
• Amoxapine
• Amphetamine
• Amprenavir
• Anileridine
• Aprepitant
• Aripiprazole
• Asenapine
• Atazanavir
• Baclofen
• Benperidol
• Benzphetamine
• Boceprevir
• Bromazepam
• Bromopride
• Brompheniramine
• Buprenorphine
• Buspirone
• Butabarbital
• Butorphanol
• Carbamazepine
• Carbinoxamine
• Carisoprodol
• Carphenazine
• Ceritinib
• Chloral Hydrate
• Chlordiazepoxide
• Chlorpheniramine
• Chlorpromazine
• Chlorzoxazone
• Citalopram
• Clarithromycin
• Clobazam
• Clomipramine
• Clonazepam
• Clorazepate
• Clozapine
• Cobicistat
• Cocaine
• Codeine
• Conivaptan
• Cyclobenzaprine
• Darunavir
• Desipramine
• Desmopressin
• Desvenlafaxine
• Dexmedetomidine
• Dextroamphetamine
• Dextromethorphan
• Dezocine
• Diazepam
• Dibenzepin
• Dichloralphenazone
• Difenoxin
• Dihydrocodeine
• Diphenhydramine
• Diphenoxylate
• Dolasetron
• Donepezil
• Doxepin
• Doxylamine
• Droperidol
• Duloxetine
• Eletriptan
• Enflurane
• Enzalutamide
• Erythromycin
• Escitalopram
• Estazolam
• Eszopiclone
• Ethchlorvynol
• Ethopropazine
• Ethylmorphine
• Fentanyl
• Flibanserin
• Fluoxetine
• Fluphenazine
• Flurazepam
• Fluspirilene
• Fluvoxamine
• Fosaprepitant
• Fosphenytoin
• Fospropofol
• Frovatriptan
• Furazolidone
• Granisetron
• Halazepam
• Haloperidol
• Halothane
• Hexobarbital
• Hydrocodone
• Hydromorphone
• Hydroxytryptophan
• Hydroxyzine
• Idelalisib
• Imipramine
• Indinavir
• Iproniazid
• Isocarboxazid
• Isoflurane
• Itraconazole
• Ketamine
• Ketazolam
• Ketobemidone
• Ketoconazole
• Levomilnacipran
• Levorphanol
• Linezolid
• Lisdexamfetamine
• Lithium
• Lofepramine
• Lopinavir
• Lorazepam
• Lorcaserin
• Loxapine
• Lumacaftor
• Meclizine
• Melitracen
• Melperone
• Meperidine
• Mephobarbital
• Meprobamate
• Meptazinol
• Mesoridazine
• Metaxalone
• Methadone
• Methamphetamine
• Methdilazine
• Methocarbamol
• Methohexital
• Methotrimeprazine
• Methylene Blue
• Methylnaltrexone
• Midazolam
• Milnacipran
• Mirtazapine
• Mitotane
• Moclobemide
• Molindone
• Moricizine
• Morphine
• Morphine Sulfate Liposome
• Nalbuphine
• Naldemedine
• Nalorphine
• Naloxegol
• Naloxone
• Naratriptan
• Nefazodone
• Nelfinavir
• Nialamide
• Nicomorphine
• Nitrazepam
• Nitrous Oxide
• Nortriptyline
• Olanzapine
• Ondansetron
• Opipramol
• Opium
• Opium Alkaloids
• Orphenadrine
• Oxazepam
• Oxycodone
• Oxymorphone
• Palonosetron
• Papaveretum
• Paregoric
• Paroxetine
• Pentazocine
• Pentobarbital
• Perampanel
• Perazine
• Periciazine
• Perphenazine
• Phenelzine
• Phenobarbital
• Phenytoin
• Pimozide
• Piperacetazine
• Pipotiazine
• Piritramide
• Posaconazole
• Prazepam
• Primidone
• Procarbazine
• Prochlorperazine
• Promazine
• Promethazine
• Propofol
• Protriptyline
• Quazepam
• Quetiapine
• Ramelteon
• Rasagiline
• Remifentanil
• Remoxipride
• Ribociclib
• Ritonavir
• Rizatriptan
• Samidorphan
• Saquinavir
• Secobarbital
• Selegiline
• Sertindole
• Sertraline
• Sibutramine
• Sodium Oxybate
• Sufentanil
• Sulpiride
• Sumatriptan
• Suvorexant
• Tapentadol
• Telaprevir
• Telithromycin
• Temazepam
• Thiethylperazine
• Thiopental
• Thiopropazate
• Thioridazine
• Tianeptine
• Tilidine
• Tizanidine
• Tolonium Chloride
• Topiramate
• Tramadol
• Tranylcypromine
• Trazodone
• Triazolam
• Trifluoperazine
• Trifluperidol
• Triflupromazine
• Trimeprazine
• Trimipramine
• Tryptophan
• Venlafaxine
• Vilazodone
• Vortioxetine
• Zaleplon
• Ziprasidone
• Zolmitriptan
• Zolpidem
• Zopiclone
• Zotepine

Using oxycodone and naloxone 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
• Miconazole
• Rifampin
• St John's Wort
• Voriconazole
• Yohimbine

Interactions with Food/Tobacco/Alcohol

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 oxycodone and naloxone 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 oxycodone and naloxone, or give you special instructions about the use of food, alcohol, or tobacco.

• Ethanol

Other Medical Problems

The presence of other medical problems may affect the use of oxycodone and naloxone. 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, severe or
• Liver disease, moderate to severe or
• Paralytic ileus (intestine stops working and may be blocked) or
• Respiratory depression (very slow breathing) or
• Stomach or bowel blockage—Should not be used in patients with these conditions.

• Hypotension (low blood pressure) or
• Pancreatitis (inflammation or 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.

It is very important that your doctor check your progress while you are taking oxycodone and naloxone. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to take it.

oxycodone and naloxone may cause a serious type of allergic reaction called anaphylaxis. Anaphylaxis 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 oxycodone and naloxone.

Do not use more of oxycodone and naloxone 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.

oxycodone and naloxone 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 oxycodone and naloxone.

oxycodone and naloxone 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.

oxycodone and naloxone may make you dizzy, drowsy, or lightheaded. Make sure you know how you react to oxycodone and naloxone before you drive, use machines, or do anything else that could be dangerous if you are dizzy or not alert.

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 oxycodone and naloxone 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 oxycodone and naloxone while you are pregnant may cause serious unwanted effects in your newborn baby. Tell your doctor right away if you think you are pregnant or if you plan to become pregnant while using oxycodone and naloxone.

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 oxycodone and naloxone may cause infertility (unable to have children). Talk with your doctor before using oxycodone and naloxone 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.

Applies to naloxone / oxycodone: oral tablet extended release

Cardiovascular

Common (1% to 10%): Hypertension, hypotension
Uncommon (0.1% to 1%): Angina pectoris, (especially in patients with history of coronary artery disease), palpitations, peripheral edema, chest pain
Rare (less than 0.1%): Syncope
Frequency not reported: Flushing, bradycardia, ST depression, supraventricular tachycardia[Ref]

Dermatologic

Common (1% to 10%): Pruritus, rash, cold sweat
Postmarketing reports: Hyperhidrosis, exfoliative dermatitis, dry skin, urticaria[Ref]

Endocrine

Common (1% to 10%): Hot flush[Ref]

Gastrointestinal

Common (1% to 10%): Diarrhea, abdominal pain, dry mouth, flatulence, vomiting, nausea, anorexia, increased appetite, gastroenteritis, dyspepsia, constipation
Frequency not reported: Thirst, eructation, colic, dysphagia, stomatitis, taste perversion, dental caries, ileus, flatulence[Ref]

Genitourinary

Frequency not reported: Urinary tract infection, micturition urgency, ureteric spasm, erectile dysfunction, urinary retention, amenorrhea[Ref]

Hepatic

Frequency not reported: Biliary colic, increased liver enzymes, biliary spasm, cholestasis[Ref]

Hypersensitivity

Rare (less than 0.1%): Allergic reactions, anaphylactic reactions[Ref]

Immunologic

Common (1% to 10%): Influenza
Rare (less than 0.1%): Herpes simplex
Frequency not reported: Lymphadenopathy[Ref]

Metabolic

Common (1% to 10%): Loss of appetite
Rare (less than 0.1%): Dehydration, increased appetite
Frequency not reported: Increased serum triglycerides, hyponatremia[Ref]

Musculoskeletal

Common (1% to 10%): Back pain, fall, arthralgia, myalgia
Frequency not reported: Myalgia, neck pain, striated and nonstriated muscle spasms, muscle twitching, muscle rigidity, osteoarthritis, abnormal gait, hypertonia, involuntary muscle contractions, abnormal coordination[Ref]

Nervous system

Common (1% to 10%): Headache, fatigue, dizziness, drug withdrawal syndrome, sedation, tremor, sinus headache, somnolence
Uncommon (0.1% to 1%): Disturbance in attention, paraesthesia, speech disorder, malaise
Rare (less than 0.1%): Convulsions (particularly in persons with epileptic disorder or predisposition to convulsions)
Frequency not reported: Syncope
Postmarketing reports: Raised intracranial pressure, sciatica, tremor, vertigo, drowsiness, paraesthesia, somnolence, speech disorder, amnesia, hypertonia, migraine, feeling hot and cold, chills, tinnitus[Ref]

Ocular

Common (1% to 10%): Lacrimation increased
Uncommon (0.1% to 1%): Visual disturbances, miosis[Ref]

Oncologic

Common (1% to 10%): Malignant neoplasm progression

Psychiatric

Common (1% to 10%): Drug abuse, anxiety, restlessness
Uncommon (0.1% to 1%): Abnormal thinking, confusion, depression, hallucination, altered mood, personality change, euphoric mood, decreased activity, psychomotor hyperactivity, agitation, nervousness, insomnia, perception disturbances (e.g., hallucination, derealization), reduced libido, mood changes, disorientation, dysphoria, nightmares[Ref]

Respiratory

Common (1% to 10%): Dyspnea, rhinorrhea, yawning
Uncommon (0.1% to 1%): Respiratory depression, bronchial spasm, spasms of nonstriated muscles, suppression of the cough reflex
Frequency not reported: Bronchitis, nasopharyngitis, pharyngitis, voice alteration, sinusitis, lower respiratory tract infection, hiccup[Ref]

Some side effects of naloxone / oxycodone may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

Mild to severe renal impairment: Reduce initial dose by one-half followed by careful dose titration

AU: Use is contraindicated. UK, US: Use should be avoided. Excreted into human milk: Unknown (naloxone); Yes (oxycodone) Comments: This drug can harm a nursing infant.

No information is available on the excretion of naloxone into breastmilk. Because it is not orally bioavailable, it is unlikely to affect the breastfed infant. Maternal use of opioid narcotics during breastfeeding can cause infant drowsiness, central nervous system depression, and even death. Infant sedation is common with maternal use of this drug. Newborn infants are particularly sensitive to the effects of even small dosages of narcotic analgesics. It is best to provide pain control with a nonnarcotic analgesic if possible and limit maternal intake of this drug to a few days. A maximum dosage of 30 mg daily is suggested. The infant should be monitored closely for drowsiness, adequate weight gain, and developmental milestones, especially in younger, exclusively breastfed infants.