Drug Information

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Brand Name
Common Name
buprenorphine XR injection
How does this medication work? What will it do for me?

Buprenorphine extended-release injection belongs to the class of medications called partial opioid agonists. It is used, together with an overall addiction treatment program that includes medical, social, and psychological support, to treat adults who are dependent on opiates (narcotics) such as oxycodone or morphine. Buprenorphine extended-release injection is used after an effective dose of buprenorphine has been established using buprenorphine sublingual tablets.

A person addicted to narcotics who suddenly stops taking the narcotic may experience severe withdrawal symptoms. Buprenorphine works by replacing the physical effects of the narcotic the person is addicted to, which can help make it easier to treat their addiction.

This medication may be available under multiple brand names and/or in several different forms. Any specific brand name of this medication may not be available in all of the forms or approved for all of the conditions discussed here. As well, some forms of this medication may not be used for all of the conditions discussed here.

Your doctor may have suggested this medication for conditions other than those listed in these drug information articles. If you have not discussed this with your doctor or are not sure why you are taking this medication, speak to your doctor. Do not stop taking this medication without consulting your doctor.

Do not give this medication to anyone else, even if they have the same symptoms as you do. It can be harmful for people to take this medication if their doctor has not prescribed it.

How should I use this medication?

The recommended starting dose of this medication is 300 mg injected subcutaneously (under the skin) in the abdominal area, once a month for two months. After two months, the dose is reduced to 100 mg injected once a month. There must be at least 26 days between doses.

This medication must not be given intravenously (into a vein). Doing so could result in serious harm and possibly death.

Buprenorphine will be injected by your health care professional. Once injected, the liquid from the syringe forms a small, solid mass that acts as a depot and slowly releases the medication over the month. This may feel like a small bump under your skin, which should get smaller over time.  Do not rub or massage the injection site. Avoid wearing tight belts or clothing waistbands that may irritate the injection site.

Many things can affect the dose of medication that a person needs, such as body weight, other medical conditions, and other medications. If your doctor has recommended a dose different from the ones listed here, do not change the way that you are taking the medication without consulting your doctor.

It is important this medication be given exactly as recommended by your doctor. If you miss an appointment to receive buprenorphine extended-release injection, contact your doctor as soon as possible to reschedule your appointment.

Store this medication in the refrigerator, protect it from light and moisture, and keep it out of the reach of children.

What form(s) does this medication come in?

Each 1 mL of clear, viscous, colourless-to-yellow-to-amber sterile solution for subcutaneous injection contains 200 mg of buprenorphine. Nonmedicinal ingredients: 50:50 Poly(DL-lactide-co-glycolide), and N-methyl-2-pyrrolidone.

Who should NOT take this medication?

Do not take this medication if you:

  • are allergic to buprenorphine or any ingredients of the medication
  • have acute alcohol addiction or are experiencing alcohol withdrawal (delirium tremens)
  • have severely reduced liver function
  • have severely reduced lung (breathing) function; acute, severe asthma; or another airway disease
  • are currently taking or have taken a MAO inhibitor (e.g., phenelzine, tranylcypromine) within the past 14 days
  • have a blockage in the digestive system or slowed movement of your digestive system 
  • are experiencing sudden severe abdominal pain that may require surgery (surgical abdomen)
  • have increased pressure inside the head or spine (increased intracranial or cerebrospinal pressure), or a head injury
  • have a seizure disorder
  • have a heart rhythm disorder called Long QT Syndrome or QT prolongation
  • have untreated low levels of potassium, magnesium, or calcium in the blood
What side effects are possible with this medication?

Many medications can cause side effects. A side effect is an unwanted response to a medication when it is taken in normal doses. Side effects can be mild or severe, temporary or permanent.

The side effects listed below are not experienced by everyone who takes this medication. If you are concerned about side effects, discuss the risks and benefits of this medication with your doctor.

The following side effects have been reported by at least 1% of people taking this medication. Many of these side effects can be managed, and some may go away on their own over time.

Contact your doctor if you experience these side effects and they are severe or bothersome. Your pharmacist may be able to advise you on managing side effects.

  • constipation
  • decreased sexual ability or interest in sexual activity
  • dizziness or lightheadedness when rising from a sitting or lying position
  • drowsiness
  • dry mouth
  • fatigue
  • headache
  • injection site discomfort (e.g., itching, pain, redness, bruising, swelling)
  • itching
  • nausea
  • poor appetite
  • stomach pain
  • sweating
  • trouble sleeping
  • vision changes
  • vomiting

Although most of the side effects listed below don't happen very often, they could lead to serious problems if you do not seek medical attention.

Check with your doctor as soon as possible if any of the following side effects occur:

  • fast, slow, or irregular heartbeat
  • fainting
  • signs of a bowel blockage (e.g., abdominal pain, severe constipation, nausea)
  • signs of liver problems (e.g., nausea, vomiting, diarrhea, loss of appetite, weight loss, yellowing of the skin or whites of the eyes, dark urine, pale stools)
  • symptoms of low blood pressure (e.g., fainting, dizziness, lightheadedness, blurred vision, nausea)

Stop taking the medication and seek immediate medical attention if any of the following occur:

  • signs of a serious allergic reaction (e.g., abdominal cramps, difficulty breathing, nausea and vomiting, or swelling of the face and throat)
  • slow, shallow, or weak breathing
  • symptoms of serotonin syndrome (e.g., confusion, fast heartbeat, hallucinations, restlessness, shaking, shivering, sudden jerking of muscles, sweating)
  • withdrawal symptoms (e.g., nausea, vomiting, diarrhea, anxiety, shivering, cold and clammy skin, body aches, loss of appetite, sweating)

Get medical help immediately if you experience any of the following symptoms of overdose or notice them in someone receiving buprenorphine treatment:

  • cold and clammy skin
  • confusion
  • difficulty walking
  • hallucinations (hearing or seeing things that aren't there)
  • poor muscle tone
  • extreme sleepiness or dizziness
  • slow or weak breathing

Some people may experience side effects other than those listed. Check with your doctor if you notice any symptom that worries you while you are taking this medication.

Are there any other precautions or warnings for this medication?

Before you begin using a medication, be sure to inform your doctor of any medical conditions or allergies you may have, any medications you are taking, whether you are pregnant or breast-feeding, and any other significant facts about your health.

Abdominal (stomach) conditions: As with other narcotic medications, buprenorphine may make the diagnosis of abdominal conditions more difficult or it may worsen these conditions. If you have abdominal problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Accidental use: When buprenorphine is used by anyone other than the person for whom it was prescribed, the effects of the medication may be fatal.

Alcohol and other medications that cause drowsiness: People taking this medication should not combine it with alcohol and avoid combining it with other medications (e.g., antidepressants, sleeping pills, anxiety medications) that cause drowsiness. Doing so can cause additional drowsiness and reduced breathing as well as other side effects, which can be dangerous and possibly fatal. It is not recommended for people with alcohol abuse problems.

Breathing: Buprenorphine can cause serious and life-threatening breathing problems. This effect on breathing may be more severe for people with breathing problems or brain damage, or those who are taking other medications that suppress breathing (e.g., codeine, morphine). If you have breathing problems, such as COPD, asthma, or respiratory depression, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Drowsiness/reduced alertness: This medication causes drowsiness or reduced alertness. Do not drive or engage in other activities requiring alertness until you know how the medication affects you. Alcohol and antianxiety medications can increase the drowsiness caused by this medication.

Head injury: Buprenorphine can cause increased pressure inside the head (intracranial pressure). If you have acute head injuries or other conditions which increase the pressure inside your head, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Heart rhythm: Buprenorphine can cause changes to the normal rhythm of the heart, including an irregular heartbeat called QT prolongation. QT prolongation is a serious life-threatening condition that can cause fainting, seizures, and sudden death.

If you are at risk for heart rhythm problems (e.g., people with a family history of abnormal heart rhythms, people with heart failure, angina, low potassium or magnesium levels, or people taking certain medications that affect heart rhythm), discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed.

Liver function: Liver disease or reduced liver function may cause this medication to build up in the body, causing side effects. If you have liver problems, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. Your doctor may want to test your liver function regularly with blood tests while you are taking this medication.

This medication may also cause injury to the liver, particularly if it is misused. If you experience symptoms of liver problems such as fatigue, feeling unwell, loss of appetite, nausea, yellowing of the skin or whites of the eyes, dark urine, pale stools, abdominal pain or swelling, and itchy skin, contact your doctor immediately.

Low blood pressure: Buprenorphine can cause low blood pressure or make low blood pressure worse. If you experience severe dizziness, especially when standing from a lying or sitting position, contact your doctor. 

Serotonin syndrome: Severe reactions are possible when buprenorphine is combined with other medications that act on serotonin, such as tricyclic antidepressants and serotonin reuptake inhibitors; medications used to treat depression. These combinations must be avoided. Symptoms of a reaction may include muscle rigidity and spasms, difficulty moving, changes in mental state including delirium and agitation. Coma and death are possible. 

If you are taking antidepressants, discuss with your doctor how this medication may affect your medical condition, how your medical condition may affect the dosing and effectiveness of this medication, and whether any special monitoring is needed. 

Short-term pain: Buprenorphine reduces the effectiveness of other opioids. Tell all health care providers involved in your care that you are taking this medication, so they can recommend effective medications.

Stopping the medication: This medication can cause withdrawal symptoms if it is stopped too quickly. Do not stop this medication without checking with your doctor first.

Pregnancy: This medication should not be used during pregnancy unless the benefits outweigh the risks. Using this medication during the last three months of pregnancy can harm the developing baby and cause the baby to experience withdrawal symptoms after birth. If you become pregnant while taking this medication, contact your doctor immediately.

Breast-feeding: Buprenorphine passes into breast milk. If you are a breast-feeding mother and are taking this medication, it may cause the baby to experience life-threatening breathing problems. Breast-feeding is not recommended for women who are taking this medication.

Children: The safety and effectiveness of using this medication have not been established for children. If this medication is taken accidentally by a child, it is a medical emergency and may be fatal.

Seniors: People over the age of 65 may be more at risk of side effects from this medication.

What other drugs could interact with this medication?

There may be an interaction between buprenorphine XR and any of the following:

  • aclidinium
  • alcohol
  • amphetamines (e.g., dextroamphetamine, lisdexamfetamine)
  • antiarrthymics (e.g., amiodarone, disopyramide, dronedarone, procainamide, quinidine, sotalol)
  • antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
  • antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
  • apalutamide
  • aprepitant
  • atropine
  • azelastine
  • "azole" antifungals (e.g., itraconazole, ketoconazole, voriconazole)
  • barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
  • belladonna
  • benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
  • benztropine
  • bosentan
  • brimonidine
  • buspirone
  • cannabis
  • chloral hydrate
  • cobicistat
  • conivaptan
  • darifenacin
  • deferasirox
  • desmopressin
  • diltiazem
  • diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
  • domperidone
  • efavirenz
  • eluxadoline
  • enzalutamide
  • etravirine
  • fesoterodine
  • flavoxate
  • general anesthetics (medications used to put people to sleep before surgery)
  • grapefruit juice
  • glycopyrrolate
  • hepatitis C antivirals (e.g., daclatasvir, dasabuvir, ombitasvir, paritaprevir)
  • HIV protease inhibitors (e.g., atazanavir, indinavir, ritonavir, saquinavir)
  • ipratropium
  • ivacaftor
  • letermovir
  • lithium
  • lumacaftor
  • ketotifen
  • macrolide antibiotics (e.g., clarithromycin, erythromycin)
  • metoclopramide
  • methadone
  • mifepristone
  • mirtazapine
  • modafinil
  • monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, rasagiline, selegiline, tranylcypromine)
  • muscle relaxants (e.g., baclofen, cyclobenzaprine, methocarbamol, orphenadrine)
  • nabilone
  • naltrexone
  • narcotic pain relievers (e.g., codeine, fentanyl, morphine, oxycodone)
  • octreotide
  • oxybutynin
  • pegvisomant
  • pramipexole
  • protein kinase inhibitors (e.g., crizotinib, dabrafenib, imatinib, nilotinib)
  • quinine
  • rifabutin
  • rifampin
  • ropinirole
  • rotigotine
  • St. John's wort
  • scopolamine
  • seizure medications (e.g., clobazam, levetiracetam, perampanel, phenobarbital, phenytoin, primidone, topiramate, valproic acid, zonisamide)
  • selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, fluoxetine, paroxetine, sertraline)
  • serotonin/norepinephrine reuptake inhibitors (SNRIs; e.g., desvenlafaxine, duloxetine, venlafaxine)
  • solifenacin
  • suvorexant
  • tapentadol
  • tiotropium
  • tocilizumab
  • tolterodine
  • tramadol
  • trazodone
  • tricyclic antidepressants (e.g., clomipramine, desipramine, imipramine)
  • tryptophan
  • umeclidinium
  • verapamil
  • zolpidem
  • zopiclone

If you are taking any of these medications, speak with your doctor or pharmacist. Depending on your specific circumstances, your doctor may want you to:

  • stop taking one of the medications,
  • change one of the medications to another,
  • change how you are taking one or both of the medications, or
  • leave everything as is.

An interaction between two medications does not always mean that you must stop taking one of them. Speak to your doctor about how any drug interactions are being managed or should be managed.

Medications other than those listed above may interact with this medication. Tell your doctor or prescriber about all prescription, over-the-counter (non-prescription), and herbal medications you are taking. Also tell them about any supplements you take. Since caffeine, alcohol, the nicotine from cigarettes, or street drugs can affect the action of many medications, you should let your prescriber know if you use them.

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