Buprenorphine (Injection Route) Description and Brand Names

Description and Brand Names

Drug information provided by: Merative, Micromedex®

US Brand Name

Buprenex

Descriptions

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. Brixadi™ and Sublocade® injection is available only under a restricted distribution program called Brixadi™ REMS (Risk Evaluation and Mitigation Strategy) Program and Sublocade® REMS Program.

This product is available in the following dosage forms:

Solution

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 Brixadi™ and 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 this medicine 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.

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 receiving 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.

Bepridil
Cisapride
Dronedarone
Fluconazole
Ketoconazole
Levoketoconazole
Mesoridazine
Nalmefene
Naltrexone
Pimozide
Piperaquine
Posaconazole
Safinamide
Samidorphan
Saquinavir
Sparfloxacin
Terfenadine

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.

Acecainide
Acepromazine
Aclidinium
Adagrasib
Alfentanil
Alfuzosin
Almotriptan
Alprazolam
Amantadine
Amiloride
Amineptine
Amiodarone
Amisulpride
Amitriptyline
Amitriptylinoxide
Amobarbital
Amoxapine
Amphetamine
Amprenavir
Anagrelide
Anileridine
Apalutamide
Apomorphine
Aprepitant
Aripiprazole
Aripiprazole Lauroxil
Armodafinil
Arsenic Trioxide
Asenapine
Astemizole
Atazanavir
Atropine
Azithromycin
Baclofen
Bedaquiline
Belladonna
Bemetizide
Bendroflumethiazide
Benperidol
Bentazepam
Benzhydrocodone
Benzphetamine
Benzthiazide
Benztropine
Biperiden
Boceprevir
Bosentan
Bromazepam
Bromopride
Brompheniramine
Bumetanide
Bupropion
Buserelin
Buspirone
Butabarbital
Butorphanol
Calcium Oxybate
Cannabidiol
Cannabis
Canrenoate
Canrenone
Carbamazepine
Carbinoxamine
Cariprazine
Carisoprodol
Carphenazine
Cenobamate
Ceritinib
Cetirizine
Chloral Hydrate
Chlordiazepoxide
Chloroquine
Chlorothiazide
Chlorpheniramine
Chlorpromazine
Chlorthalidone
Chlorzoxazone
Cimetidine
Ciprofloxacin
Citalopram
Clarithromycin
Clemastine
Clidinium
Clobazam
Clofazimine
Clomipramine
Clonazepam
Clopamide
Clopidogrel
Clorazepate
Clothiapine
Cloxazolam
Clozapine
Cobicistat
Cocaine
Codeine
Conivaptan
Crizotinib
Cyclobenzaprine
Cyclopenthiazide
Cyclopentolate
Cyclosporine
Cyclothiazide
Cyproheptadine
Dabrafenib
Dantrolene
Daridorexant
Darifenacin
Darunavir
Dasatinib
Degarelix
Delamanid
Delavirdine
Delorazepam
Desipramine
Deslorelin
Desmopressin
Desvenlafaxine
Deutetrabenazine
Dexamethasone
Dexmedetomidine
Dextroamphetamine
Dextromethorphan
Dezocine
Diacetylmorphine
Diazepam
Diazoxide
Dibenzepin
Dichloralphenazone
Dicyclomine
Difenoxin
Diltiazem
Dimenhydrinate
Diphenhydramine
Diphenoxylate
Dipyrone
Disopyramide
Dofetilide
Dolasetron
Domperidone
Donepezil
Doxepin
Doxylamine
Droperidol
Duloxetine
Duvelisib
Ebastine
Efavirenz
Elagolix
Eletriptan
Encorafenib
Enflurane
Entrectinib
Enzalutamide
Eplerenone
Eribulin
Erythromycin
Escitalopram
Esketamine
Eslicarbazepine Acetate
Estazolam
Eszopiclone
Ethacrynic Acid
Ethchlorvynol
Ethopropazine
Ethylmorphine
Etozolin
Etrasimod
Etravirine
Famotidine
Felbamate
Fenfluramine
Fentanyl
Fesoterodine
Fexinidazole
Fingolimod
Flavoxate
Flecainide
Flibanserin
Flunitrazepam
Fluoxetine
Fluphenazine
Flurazepam
Fluspirilene
Fluvoxamine
Formoterol
Fosamprenavir
Fosaprepitant
Foscarnet
Fosnetupitant
Fosphenytoin
Fospropofol
Fostemsavir
Frovatriptan
Furosemide
Gabapentin
Gabapentin Enacarbil
Galantamine
Gatifloxacin
Gemifloxacin
Gepirone
Glasdegib
Glycopyrrolate
Glycopyrronium Tosylate
Gonadorelin
Goserelin
Granisetron
Halazepam
Halofantrine
Haloperidol
Halothane
Hexobarbital
Histrelin
Homatropine
Hydrochlorothiazide
Hydrocodone
Hydroflumethiazide
Hydromorphone
Hydroquinidine
Hydroxyamphetamine
Hydroxychloroquine
Hydroxytryptophan
Hydroxyzine
Hyoscyamine
Ibutilide
Idelalisib
Iloperidone
Imatinib
Imipramine
Indapamide
Indinavir
Inotuzumab Ozogamicin
Ipratropium
Isocarboxazid
Isoflurane
Itraconazole
Ivabradine
Ivacaftor
Ivosidenib
Josamycin
Ketamine
Ketazolam
Ketobemidone
Lacosamide
Lapatinib
Larotrectinib
Lasmiditan
Lefamulin
Lemborexant
Lenacapavir
Lenvatinib
Lesinurad
Letermovir
Leuprolide
Levocetirizine
Levofloxacin
Levomilnacipran
Levorphanol
Linezolid
Lisdexamfetamine
Lithium
Lofepramine
Lofexidine
Lomitapide
Lonafarnib
Lopinavir
Loprazolam
Lorazepam
Lorcaserin
Lorlatinib
Lormetazepam
Loxapine
Lumacaftor
Lumefantrine
Lurasidone
Macimorelin
Magnesium Oxybate
Meclizine
Medazepam
Mefloquine
Melitracen
Melperone
Mepenzolate
Meperidine
Mephobarbital
Meprobamate
Meptazinol
Metaclazepam
Metaxalone
Methadone
Methamphetamine
Methdilazine
Methocarbamol
Methohexital
Methotrimeprazine
Methyclothiazide
Methylene Blue
Metoclopramide
Metolazone
Metronidazole
Mibefradil
Midazolam
Mifepristone
Milnacipran
Mirtazapine
Mitotane
Mizolastine
Mobocertinib
Modafinil
Molindone
Moricizine
Morphine
Moxifloxacin
Nafarelin
Nafcillin
Nalbuphine
Naratriptan
Nefazodone
Nelfinavir
Netupitant
Nevirapine
Nicomorphine
Nilotinib
Nitrazepam
Nitrous Oxide
Nordazepam
Norfloxacin
Nortriptyline
Octreotide
Ofloxacin
Olanzapine
Oliceridine
Ondansetron
Opipramol
Opium
Opium Alkaloids
Orphenadrine
Osilodrostat
Osimertinib
Oxaliplatin
Oxazepam
Oxcarbazepine
Oxitropium Bromide
Oxybutynin
Oxycodone
Oxymorphone
Ozanimod
Pacritinib
Palbociclib
Paliperidone
Palonosetron
Panobinostat
Papaveretum
Papaverine
Paregoric
Paroxetine
Pasireotide
Pazopanib
Pentamidine
Pentazocine
Pentobarbital
Perampanel
Perazine
Periciazine
Perphenazine
Phenelzine
Phenobarbital
Phenytoin
Pimavanserin
Pinazepam
Pipamperone
Pipenzolate Bromide
Piperacetazine
Pipotiazine
Pirenzepine
Piretanide
Piritramide
Pitolisant
Polythiazide
Ponesimod
Potassium Oxybate
Prazepam
Prednisone
Pregabalin
Primidone
Probucol
Procainamide
Procarbazine
Prochlorperazine
Procyclidine
Promazine
Promethazine
Propafenone
Propantheline
Propiverine
Propofol
Protriptyline
Quazepam
Quetiapine
Quinethazone
Quinidine
Quinine
Quizartinib
Ramelteon
Ranitidine
Ranolazine
Rasagiline
Relugolix
Remifentanil
Remimazolam
Remoxipride
Ribociclib
Rifabutin
Rifampin
Rifapentine
Risperidone
Ritonavir
Rizatriptan
Ropeginterferon Alfa-2b-njft
Schisandra sphenanthera
Scopolamine
Secobarbital
Selegiline
Selpercatinib
Sertindole
Sertraline
Sevoflurane
Sibutramine
Siponimod
Sodium Oxybate
Sodium Phosphate
Sodium Phosphate, Dibasic
Sodium Phosphate, Monobasic
Solifenacin
Sorafenib
Sotalol
Spironolactone
St John's Wort
Stramonium
Sufentanil
Sulpiride
Sultopride
Sumatriptan
Sunitinib
Suvorexant
Tacrolimus
Tamoxifen
Tapentadol
Telaprevir
Telavancin
Telithromycin
Telotristat Ethyl
Temazepam
Terodiline
Tetrabenazine
Tetrazepam
Thiethylperazine
Thiopental
Thiopropazate
Thioridazine
Thiothixene
Tianeptine
Tilidine
Tiotropium
Tizanidine
Tolonium Chloride
Tolterodine
Topiramate
Toremifene
Torsemide
Tramadol
Tranylcypromine
Trazodone
Treosulfan
Triamterene
Triazolam
Trichlormethiazide
Triclabendazole
Trifluoperazine
Trifluperidol
Triflupromazine
Trihexyphenidyl
Trimeprazine
Trimipramine
Triptorelin
Troleandomycin
Tropicamide
Trospium
Tryptophan
Tucatinib
Umeclidinium
Vandetanib
Vardenafil
Vemurafenib
Venlafaxine
Verapamil
Vilanterol
Vilazodone
Vinflunine
Voclosporin
Voriconazole
Vorinostat
Vortioxetine
Voxelotor
Xipamide
Zaleplon
Ziprasidone
Zolmitriptan
Zolpidem
Zopiclone
Zotepine
Zuclopenthixol
Zuranolone

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

Proper Use

A nurse or other trained health professional will give you or your child this medicine. This medicine 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 Brixadi™ and Sublocade® REMS program, and become familiar with the Brixadi™ and 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 this medicine 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

It is very important that your doctor check the progress of you or your child while receiving 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 or your child should continue to take it.

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

This medicine 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.

Symptoms of an overdose include: drowsiness, extreme dizziness or weakness, irregular, fast or slow, or shallow breathing, pale or blue lips, fingernails, or skin, pinpoint pupils, relaxed and calm, slow heartbeat or breathing, seizures, sleepiness, trouble breathing, or cold, clammy skin. Tell your doctor right away if you notice these symptoms. Your doctor may also give naloxone to treat an overdose.

This medicine may cause sleep-related breathing problems (eg, sleep apnea, sleep-related hypoxemia). Your doctor may decrease your dose if you have sleep apnea (stop breathing for short periods during sleep) while using this medicine.

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

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

If you or your child has been receiving this medicine 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, stomach cramps, fever, runny nose, anxiety, or restlessness).

This medicine may increase your risk for serious injection site reactions. Check with your doctor right away if you have bleeding, blistering, burning, coldness, discoloration of 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.

Using this medicine 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.

Call your doctor right away if you have worsening of pain, increased sensitivity to pain, or new pain after taking this medicine. These may be symptoms of opioid-induced hyperalgesia and allodynia.

Check with your doctor right away if you have darkening of the skin, diarrhea, dizziness, fainting, loss of appetite, mental depression, nausea, skin rash, unusual tiredness or weakness, or vomiting. These may be symptoms of adrenal gland problems.

Dizziness, lightheadedness, or fainting may occur, especially when you get up suddenly from a lying or sitting position. Getting up slowly may help. Also, lying down for a while may relieve dizziness or lightheadedness. If this problem continues or gets worse, check with your doctor right away.

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.

This medicine may cause serious allergic reactions, including anaphylaxis, which can be life-threatening and require 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 or your child are receiving this medicine.

Check with your doctor right away if you have dark urine, general tiredness and weakness, light-colored stools, nausea and vomiting, upper right stomach pain, and yellow eyes and skin. These may be symptoms of liver problems.

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.

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.

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, discomfort, or tightness
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
unusual behavior

Incidence not known

Agitation
anxiety
chills
cold sweats
coma
cool, pale skin
cough
darkening of the skin
deep or fast breathing with dizziness
diarrhea
dizziness
dry mouth
fainting
fever
increased hunger
increased sensitivity to pain
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
nightmares
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
worsening of pain

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

Symptoms of overdose

Blurred vision
confusion
difficult or trouble breathing
dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position
irregular, fast or slow, or shallow breathing
pale or blue lips, fingernails, or skin
pinpoint pupils
relaxed and calm
sleepiness or unusual drowsiness
sweating
unusual tiredness or weakness

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
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.

Portions of this document last updated: April 01, 2024

Original article: https://www.mayoclinic.org/drugs-supplements/buprenorphine-injection-route/description/drg-20073977

Buprenorphine (Injection Route)

Description and Brand Names

US Brand Name

Descriptions

Before Using

Allergies

Pediatric

Geriatric

Breastfeeding

Drug Interactions

Other Interactions

Other Medical Problems

Proper Use

Precautions

Side Effects

More common

Rare

Incidence not known

Symptoms of overdose

Less common

Rare

Incidence not known

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