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Buprenorphine (Injection)

bue-pre-NOR-feen

Injection route(Solution)

Use of buprenorphine hydrochloride increases the risk of opioid addiction, abuse, or misuse, which may cause overdose or death. Assess the risk prior to therapy and monitor for signs of addiction, abuse, or misuse during therapy. Serious, life-threatening, or fatal respiratory depression may occur, particularly at treatment initiation and with dose increases. Monitor for signs of respiratory depression during treatment. Prolonged use during pregnancy may result in neonatal opioid withdrawal syndrome, which may be life-threatening if unnoticed and untreated. If prolonged use is required in a pregnant woman, advise the patient of the risk to the fetus. Concomitant use of benzodiazepines and opioids may result in profound sedation, respiratory depression, coma, and death. Reserve concomitant prescribing for patients with inadequate alternative treatment options. Limit dosages and durations to the minimum required, and follow patients for signs and symptoms of respiratory depression and sedation .

Medically reviewed: March 25, 2018

Commonly used brand name(s)

In the U.S.

  • Buprenex

Available Dosage Forms:

  • Solution

Therapeutic Class: Analgesic

Pharmacologic Class: Opioid Agonist/Antagonist

Chemical Class: Opioid

Uses For buprenorphine

Buprenorphine injection is used to relieve moderate to severe pain. It is also used in patients who have received treatment with an oral form of buprenorphine that is placed under the tongue or inside the cheek for 7 days, followed by an adjustment in the dose for at least 7 days.

Buprenorphine belongs to the group of medicines called narcotic analgesics (pain medicines). It acts on the central nervous system (CNS) to relieve pain.

When a narcotic medicine 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.

Buprenorphine injection and Buprenex® are available only with your doctor's prescription. Sublocade™ injection is available only under a restricted distribution program called Sublocade™ REMS (Risk Evaluation and Mitigation Strategy) Program.

Before Using buprenorphine

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 buprenorphine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to buprenorphine 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 Sublocade™ injection in the pediatric population. Safety and efficacy have not been established.

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of buprenorphine injection and Buprenex® in children 2 to 12 years of age. However, safety and efficacy have not been established in children younger than 2 years of age.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of buprenorphine injection in the elderly. However, elderly patients may be more sensitive to the effects of buprenorphine than younger adults, and are more likely to have age-related kidney, liver, heart, or lung problems, which may require caution and an adjustment in the dose for patients receiving buprenorphine injection.

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 receiving buprenorphine, 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 buprenorphine 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
  • Amisulpride
  • Bepridil
  • Cisapride
  • Dronedarone
  • Fluconazole
  • Ketoconazole
  • Mesoridazine
  • Nalmefene
  • Naltrexone
  • Pimozide
  • Piperaquine
  • Posaconazole
  • Safinamide
  • Saquinavir
  • Sparfloxacin
  • Terfenadine

Using buprenorphine 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.

  • Acecainide
  • Acepromazine
  • Alfentanil
  • Alfuzosin
  • Almotriptan
  • Alprazolam
  • Amineptine
  • Amiodarone
  • Amitriptyline
  • Amitriptylinoxide
  • Amobarbital
  • Amoxapine
  • Amphetamine
  • Anagrelide
  • Apomorphine
  • Aripiprazole
  • Aripiprazole Lauroxil
  • Arsenic Trioxide
  • Asenapine
  • Astemizole
  • Atazanavir
  • Azithromycin
  • Baclofen
  • Bedaquiline
  • Benperidol
  • Benzphetamine
  • Bromazepam
  • Bromopride
  • Brompheniramine
  • Buserelin
  • Buspirone
  • Butabarbital
  • Butorphanol
  • Carbamazepine
  • Carbinoxamine
  • Cariprazine
  • Carisoprodol
  • Carphenazine
  • Chloral Hydrate
  • Chlordiazepoxide
  • Chloroquine
  • Chlorpheniramine
  • Chlorpromazine
  • Chlorzoxazone
  • Ciprofloxacin
  • Citalopram
  • Clarithromycin
  • Clobazam
  • Clomipramine
  • Clonazepam
  • Clorazepate
  • Clozapine
  • Cocaine
  • Codeine
  • Crizotinib
  • Cyclobenzaprine
  • Dabrafenib
  • Dantrolene
  • Dasatinib
  • Degarelix
  • Delamanid
  • Desipramine
  • Deslorelin
  • Desmopressin
  • Desvenlafaxine
  • Deutetrabenazine
  • Dexmedetomidine
  • Dextroamphetamine
  • Dextromethorphan
  • Dezocine
  • Diazepam
  • Dibenzepin
  • Dichloralphenazone
  • Difenoxin
  • Diphenhydramine
  • Diphenoxylate
  • Disopyramide
  • Dofetilide
  • Dolasetron
  • Domperidone
  • Donepezil
  • Doxepin
  • Doxylamine
  • Droperidol
  • Duloxetine
  • Ebastine
  • Efavirenz
  • Eletriptan
  • Enflurane
  • Eribulin
  • Erythromycin
  • Escitalopram
  • Estazolam
  • Eszopiclone
  • Ethchlorvynol
  • Ethopropazine
  • Ethylmorphine
  • Famotidine
  • Felbamate
  • Fentanyl
  • Fingolimod
  • Flecainide
  • Flibanserin
  • Fluoxetine
  • Fluphenazine
  • Flurazepam
  • Fluspirilene
  • Fluvoxamine
  • Formoterol
  • Foscarnet
  • Fosphenytoin
  • Fospropofol
  • Frovatriptan
  • Furazolidone
  • Galantamine
  • Gatifloxacin
  • Gemifloxacin
  • Gonadorelin
  • Goserelin
  • Granisetron
  • Halazepam
  • Halofantrine
  • Haloperidol
  • Halothane
  • Hexobarbital
  • Histrelin
  • Hydrocodone
  • Hydromorphone
  • Hydroquinidine
  • Hydroxychloroquine
  • Hydroxytryptophan
  • Hydroxyzine
  • Ibutilide
  • Iloperidone
  • Imipramine
  • Inotuzumab Ozogamicin
  • Iproniazid
  • Isocarboxazid
  • Isoflurane
  • Itraconazole
  • Ivabradine
  • Ketamine
  • Ketazolam
  • Ketobemidone
  • Lapatinib
  • Leuprolide
  • Levofloxacin
  • Levomilnacipran
  • Levorphanol
  • Linezolid
  • Lisdexamfetamine
  • Lithium
  • Lofepramine
  • Lorazepam
  • Lorcaserin
  • Loxapine
  • Lumefantrine
  • Lurasidone
  • Macimorelin
  • Meclizine
  • Mefloquine
  • Melitracen
  • Melperone
  • Meperidine
  • Mephobarbital
  • Meprobamate
  • Meptazinol
  • Metaxalone
  • Methadone
  • Methamphetamine
  • Methdilazine
  • Methocarbamol
  • Methohexital
  • Methotrimeprazine
  • Methylene Blue
  • Metoclopramide
  • Metronidazole
  • Midazolam
  • Mifepristone
  • Milnacipran
  • Mirtazapine
  • Mizolastine
  • Moclobemide
  • Molindone
  • Moricizine
  • Morphine
  • Moxifloxacin
  • Nafarelin
  • Nalbuphine
  • Naratriptan
  • Nefazodone
  • Nelfinavir
  • Nialamide
  • Nicomorphine
  • Nilotinib
  • Nitrazepam
  • Nitrous Oxide
  • Norfloxacin
  • Nortriptyline
  • Octreotide
  • Ofloxacin
  • Olanzapine
  • Ondansetron
  • Opipramol
  • Opium
  • Opium Alkaloids
  • Orphenadrine
  • Oxazepam
  • Oxycodone
  • Oxymorphone
  • Paliperidone
  • Palonosetron
  • Panobinostat
  • Papaveretum
  • Paregoric
  • Paroxetine
  • Pasireotide
  • Pazopanib
  • Pentamidine
  • Pentazocine
  • Pentobarbital
  • Perampanel
  • Perazine
  • Periciazine
  • Perphenazine
  • Phenelzine
  • Phenobarbital
  • Pimavanserin
  • Pipamperone
  • Piperacetazine
  • Pipotiazine
  • Piritramide
  • Pitolisant
  • Prazepam
  • Primidone
  • Probucol
  • Procainamide
  • Procarbazine
  • Prochlorperazine
  • Promazine
  • Promethazine
  • Propafenone
  • Propofol
  • Protriptyline
  • Quazepam
  • Quetiapine
  • Quinidine
  • Quinine
  • Ramelteon
  • Ranolazine
  • Rasagiline
  • Remifentanil
  • Remoxipride
  • Ribociclib
  • Risperidone
  • Ritonavir
  • Rizatriptan
  • Secobarbital
  • Selegiline
  • Sertindole
  • Sertraline
  • Sevoflurane
  • Sibutramine
  • Sodium Oxybate
  • Sodium Phosphate
  • Sodium Phosphate, Dibasic
  • Sodium Phosphate, Monobasic
  • Solifenacin
  • Sorafenib
  • Sotalol
  • St John's Wort
  • Sufentanil
  • Sulpiride
  • Sultopride
  • Sumatriptan
  • Sunitinib
  • Suvorexant
  • Tacrolimus
  • Tamoxifen
  • Tapentadol
  • Telaprevir
  • Telavancin
  • Telithromycin
  • Temazepam
  • Tetrabenazine
  • Thiethylperazine
  • Thiopental
  • Thiopropazate
  • Thioridazine
  • Thiothixene
  • Tianeptine
  • Tilidine
  • Tizanidine
  • Tolonium Chloride
  • Tolterodine
  • Topiramate
  • Toremifene
  • Tramadol
  • Tranylcypromine
  • Trazodone
  • Triazolam
  • Trifluoperazine
  • Trifluperidol
  • Triflupromazine
  • Trimeprazine
  • Trimipramine
  • Triptorelin
  • Tryptophan
  • Vandetanib
  • Vardenafil
  • Vemurafenib
  • Venlafaxine
  • Vilanterol
  • Vilazodone
  • Vinflunine
  • Voriconazole
  • Vorinostat
  • Vortioxetine
  • Zaleplon
  • Ziprasidone
  • Zolpidem
  • Zopiclone
  • Zotepine
  • Zuclopenthixol

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 buprenorphine 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 buprenorphine, 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 buprenorphine. Make sure you tell your doctor if you have any other medical problems, especially:

  • Addison's disease (adrenal gland problem) or
  • Alcohol abuse, or history of or
  • Brain tumor or
  • CNS depression, history of or
  • Congestive heart failure or
  • Drug dependence, especially narcotic abuse or dependence, history of or
  • Enlarged prostate (BPH, prostatic hypertrophy) or
  • Head injuries or
  • Heart disease, unstable or
  • Heart rhythm problems (eg, atrial fibrillation, slow heartbeat, long QT syndrome) or
  • Hypokalemia (low potassium in the blood) or
  • Hypomagnesemia (low magnesium in the blood) or
  • Hypothyroidism (an underactive thyroid) or
  • Kyphoscoliosis (curvature of spine that can cause breathing problems) or
  • Lung or breathing problems (eg, chronic obstructive pulmonary disease [COPD], cor pulmonale, hypercapnia, hypoxia) or
  • Mental illness, history of or
  • Problems with passing urine—Use with caution. May increase risk for more serious side effects.
  • Gallbladder problems or
  • Hypertension (high blood pressure) or
  • Pancreatitis (inflammation of the pancreas) or
  • Seizures, history of—Use with caution. May make these conditions worse.
  • Kidney disease or
  • Liver disease—Use with caution. The effects may be increased because of slower removal of the medicine from the body.
  • Lung or breathing problems, severe or
  • Stomach or bowel blockage (eg, paralytic ileus)—Should not be used in patients with these conditions.

Proper Use of buprenorphine

A nurse or other trained health professional will give you or your child buprenorphine. buprenorphine is given as a shot under your skin, into a muscle, or into a vein.

It is very important that you understand the requirements of the Sublocade™ REMS program, and become familiar with the Sublocade™ medication guide. Read and follow these instructions carefully. Ask your doctor if you have any questions. Ask your pharmacist for the medication guide if you do not have one.

Your doctor will give you a few doses of buprenorphine until your condition improves, and then switch you or your child to an oral medicine that works the same way. If you have any concerns about this, talk to your doctor.

Precautions While Using buprenorphine

It is very important that your doctor check the progress of you or your child while receiving buprenorphine. This will allow your doctor to see if the medicine is working properly and to decide if you or your child should continue to take it.

Do not use buprenorphine if you are using or have used an MAO inhibitor (eg, Eldepryl®, Marplan®, Nardil®, or Parnate®) within the past 14 days.

buprenorphine may be habit-forming. If you or your child feels that the medicine is not working as well, do not use more than your prescribed dose. Call your doctor for instructions.

Using narcotics for a long time can cause severe constipation. To prevent this, your doctor may direct you or your child 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.

buprenorphine 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 the other medicines listed above while you or your child is receiving buprenorphine.

buprenorphine may make you dizzy, drowsy, confused, or disoriented. Do not drive do anything else that could be dangerous until you know how buprenorphine affects you.

If you or your child has been receiving buprenorphine regularly for several days, do not suddenly stop receiving it without first checking with your doctor. You or your child may be directed to slowly reduce the amount you are using before stopping treatment completely to lessen the chance of withdrawal side effects (eg, abdominal or stomach cramps, fever, runny nose, anxiety, or restlessness).

Using buprenorphine while you are pregnant may cause neonatal withdrawal syndrome in your newborn babies. Tell your doctor right away if your baby has an abnormal sleep pattern, diarrhea, a high-pitched cry, irritability, shakiness or tremors, weight loss, vomiting, or fails to gain weight.

Contact your doctor right away if you have any changes to your heart rhythm. You might feel dizzy or faint, or you might have a fast, pounding, or uneven heartbeat. Make sure your doctor knows if you or anyone in your family has ever had a heart rhythm problem such as QT prolongation.

buprenorphine may cause serious allergic reactions, including anaphylaxis. This can be life-threatening and requires immediate medical attention. Call your doctor right away if you have a rash, itching, trouble breathing, trouble swallowing, or any swelling of your hands, face, or mouth while you are receiving buprenorphine.

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 buprenorphine may cause infertility (unable to have children). Talk with your doctor before using buprenorphine if you plan to have children.

Make sure any doctor or dentist who treats you knows that you have been using Sublocade™ injection within the last 6 months.

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.

buprenorphine 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 or nurse immediately if any of the following side effects occur:

More common
  • Drowsiness
  • relaxed and calm feeling
  • sleepiness
Rare
  • Bleeding, blistering, burning, coldness, discoloration of the skin, feeling of pressure, hives, infection, inflammation, itching, lumps, numbness, pain, rash, redness, scarring, soreness, stinging, swelling, tenderness, tingling, ulceration, or warmth at the injection site
  • bluish color of the fingernails, lips, skin, palms, or nail beds
  • blurred vision
  • burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings
  • chest pain or discomfort
  • confusion
  • difficult or labored breathing
  • feeling, seeing, or hearing things that are not there
  • feeling that others are watching you or controlling your behavior
  • feeling that others can hear your thoughts
  • headache
  • severe mood or mental changes
  • slurred speech
  • tightness of the chest
  • unusual behavior
Incidence not known
  • Agitation
  • anxiety
  • cough
  • darkening of the skin
  • deep or fast breathing with dizziness
  • diarrhea
  • dizziness
  • dry mouth
  • fainting
  • fever
  • irregular heartbeats
  • irritability
  • large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs
  • loss of appetite
  • loss of muscle coordination
  • nausea
  • nervousness
  • noisy breathing
  • overactive reflexes
  • poor coordination
  • restlessness
  • seizures
  • shaking
  • shivering
  • skin rash
  • sweating
  • talking or acting with excitement which you cannot control
  • trouble sleeping
  • twitching
  • unusual tiredness or weakness
  • vomiting

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
  • Constricted, pinpoint, or small pupils (black part of the eye)
  • dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
  • extremely shallow or slow breathing
  • sweating
Rare
  • Burning, dry, or itching eyes
  • chills
  • continuing ringing or buzzing or other unexplained noise in the ears
  • decrease in the frequency of urination
  • decrease in urine volume
  • depression
  • difficulty in passing urine (dribbling)
  • discharge, excessive tearing
  • dreaming
  • dry mouth
  • false or unusual sense of well-being
  • fast, pounding, or irregular heartbeat or pulse
  • feeling of warmth
  • hearing loss
  • itching of the skin
  • painful urination
  • pounding in the ears
  • redness of the face, neck, arms, and occasionally, upper chest
  • redness, pain, or swelling of the eye, eyelid, or inner lining of the eyelid
Incidence not known
  • Belching
  • bloated
  • bluish lips or skin
  • change in vision
  • excess air or gas in the stomach or intestines
  • feeling of fullness
  • feeling of unreality
  • general feeling of discomfort or illness
  • heartburn
  • hives or welts
  • impaired vision
  • indigestion
  • not breathing
  • paleness of the skin
  • passing gas
  • redness of the skin
  • sense of detachment from self or body
  • stomach discomfort, upset, or pain

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.

See also: Side effects (in more detail)

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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