Buprenorphine

Buprenorphine treats moderate to severe pain. It is also used to treat patients who are addicted to opioids. May cause constipation. Do not drink alcohol with this medication.

Buprenorphine Overview

Reviewed: June 12, 2012
Updated: 

Buprenorphine is a prescription medication used to treat moderate to severe pain and chronic, around-the-clock pain that will last a long period of time. Buprenorphine is also used to treat patients who are dependent on opioids (addiction to opioid drugs including heroin and narcotic painkillers).

Buprenorphine belongs to a group of drugs called opioid partial agonist-antagonists, which help to relieve pain by binding to certain opioid receptors in the body. It treats dependence because it produces similar effects to opioids.

This medication comes in skin patch form and is usually applied for a week at a time.

This medication also comes in tablet form to be dissolved under the tongue (sublingual) once daily.

This medication comes as a film that is applied to the buccal mucosa (the inside lining of the cheek) once or twice a day. 

This medication comes as an implantable rod that is placed under the skin of the upper arm by a healthcare professional. 

This medication is additionally available in an injectable form to be given directly into a vein (IV), muscle (IM), or under the skin (subcutaneously) by a healthcare professional.

Some of the common side effects of buprenorphine include constipation, nausea, and headache. Buprenorphine can cause dizziness and drowsiness. Do not drive or operate machinery until you know how buprenorphine will affect you. Do not drink alcohol while taking this medication.

 

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Buprenorphine Cautionary Labels

precautionsprecautionsprecautionsprecautionsprecautions

Uses of Buprenorphine

Buprenorphine is a prescription medicine used to treat moderate to severe chronic pain. Buprenorphine is also used to treat patients who are dependent on opioids (addiction to opioid drugs including heroin and narcotic painkillers). The buprenorphine patch is used when a continuous, around-the-clock opioid analgesic is needed for an extended period of time.

The subcutaneous form of buprenorphine is used to treat adults with moderate-to-severe addiction (dependence) to opioid drugs (prescription or illegal) who:

  • have received treatment with an oral transmucosal (used under the tongue or inside the cheek) buprenorphine‐containing medicine for 7 days and 
  • are taking a dose that controls withdrawal symptoms for at least seven days

Subcutaneous buprenorphine is part of a complete treatment plan that should include counseling.

It is not known if subcutaneous buprenorphine is safe or effective in children.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Buprenorphine Brand Names

Buprenorphine may be found in some form under the following brand names:

Buprenorphine Drug Class

Buprenorphine is part of the drug class:

Side Effects of Buprenorphine

Buprenorphine may cause serious side effects. See "Drug Precautions"

The most common side effects of buprenorphine include:

  • nausea
  • headache
  • dizziness
  • constipation
  • drowsiness
  • vomiting
  • dry mouth
  • depression
  • back pain
  • toothache and throat pain
  • itching, redness, or rash (patch and implant form)
  • itching or pain at the injection site (injectable form)

Constipation (incomplete or hard bowel movements) is a very common side effect of all opioid medicines. Talk to your doctor about the use of laxatives (medicines to treat constipation) and stool softeners to prevent or treat constipation while using buprenorphine.

Talk to your doctor about any side effect that bothers you or do not go away.

These are not all the possible side effects of buprenorphine. For a complete list, ask your doctor or pharmacist.

Buprenorphine Interactions

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Some medicines may cause serious or life-threatening medical problems when taken with buprenorphine. Sometimes, the doses of certain medicines and buprenorphine need to be changed if used together.

Especially tell your doctor if you take:

  • other pain medicines
  • antidepressant medicines
  • sleeping pills
  • antihistamines
  • anti-anxiety medicines
  • muscle relaxants
  • anti-nausea medicines
  • sedative or tranquilizer medicines (medicines that make you sleepy)
  • a medicine for abnormal heartbeats
  • medications that block a protein in the body (CYP3A4) such as some macrolide antibiotics (clarithromycin, telithromycin), some HIV protease inhibitors (indinavir, nelfinavir, ritonavir, saquinavir), some HCV protease inhibitors (boceprevir, telaprevir), some azole antifungals (ketoconazole, itraconazole, posaconazole, voriconazole), delavirdine (Rescriptor), and nefazodone
  • medications that increase the activity of the enzyme CYP3A4 such as carbamazepine (Tegretol, Equetro, Carbatrol), phenobarbital, phenytoin (Dilantin), rifampin (Rifadin), and St John's wort
  • diuretics such as acetazolamide (Diamox), amiloride (Midamor), bumetanide (Bumex), chlorothiazide (Diuril), chlorthalidone (Thalitone), ethacrynic acid (Edecrin), furosemide (Lasix), hydrochlorothiazide (Microzide, HCTZ), metolazone (Zaroxolyn), torsemide (Demadex), andtriamterene (Dyrenium, Dyazide, Maxzide)
  • anticholinergics such as glycopyrrolate (Cuvposa, Robinul), trospium (Sanctura), oxybutynin (Anturol, Gelnique, Oxytrol, Ditropan), solifenacin (Vesicare), dicyclomine (Bentyl), propantheline (Pro-Banthine), and atropine (Atropen, Sal-Tropine)

You should not take buprenorphine if you already take a monoamine oxidase inhibitor medicine (MAOI) or within 14 days after you stop taking an MAOI medicine.

Ask your doctor if you are not sure if your medicine is one listed above.

Know the medicines you take. Keep a list of your medicines to show your doctor and pharmacist. Your doctor will tell you if it is safe to take other medicines while you are using buprenorphine.

Buprenorphine Precautions

Serious side effects include:

  • Serious breathing problems that can be life-threatening. This can happen because of an overdose or if the dose you are using is too high for you. Call your doctor or get emergency medical help right away if you:
    • have trouble breathing or have changes in breathing
    • have extreme drowsiness with slowed breathing
    • have slow shallow breathing (little chest movement with breathing)
    • feel faint, very dizzy, confused, or have any other unusual symptoms
    • have a slow heartbeat
    • have severe sleepiness
    • have cold, clammy skin
  • Allergic reactions. Rash, itching, and hives are the most common symptoms of an allergic reaction. Call your doctor if you have these symptoms. Get medical help right away if you have any of these symptoms of an allergic reaction while taking buprenorphine:
    • swelling of your lips or tongue
    • breathing problems
    • wheezing
    • chest pain
  • Buprenorphine can cause a drop in your blood pressure. Low blood pressure can make you feel dizzy if you get up too fast from sitting or lying down. Low blood pressure is also more likely to happen if you take other medicines that can also lower your blood pressure. Severe low blood pressure can happen if you lose blood or take certain other medicines.
  • Liver problems. Tell your healthcare provider about any signs or symptoms of liver damage, including loss of appetite, weight loss, nausea, vomiting, feeling tired, stomach pain, dark urine, light-colored stools, fever, rash, and yellowing of the skin or the whites of the eyes. Your doctor may do tests before you start and while you take buprenorphine.
  • Buprenorphine can increase your chances of having a seizure if you have a history of seizures. Tell your doctor if you have a seizure or convulsion while taking buprenorphine.
  • Buprenorphine can cause physical dependence. Do not stop using buprenorphine or any other opioid without talking to your doctor. You could become sick with uncomfortable withdrawal symptoms because your body has become used to these medicines. Physical dependence is not the same as drug addiction.
  • There is a chance of abuse or addiction with buprenorphine. The chance is higher if you are or have been addicted to or abused other medicines, street drugs or alcohol in the past. You may have a greater risk of developing abuse or addiction again while using buprenorphine.
  • Call your doctor right away or get emergency medical help if you:
  • Tell your healthcare provider if you have any symptoms of adrenal insufficiency, including nausea, vomiting, anorexia, fatigue, weakness, and dizziness.
  • Symptoms of opioid withdrawal may include shaking, excessive sweating, feeling hot or cold more than normal, runny nose, watery eyes, goose bumps, diarrhea, vomiting, and muscle aches
  • You should not drive, operate heavy machinery, or do other dangerous activities, until you know how you react to this medicine. Buprenorphine can make you sleepy and cause you to feel dizzy or lightheaded. This may affect your ability to think and react. Ask your doctor when it is okay to do these activities.
  • You should not drink alcohol or use prescription or non-prescription medicines that have alcohol in them while using buprenorphine. Alcohol can increase your chances of having serious side effects including death.

Topical:

Severe skin reactions. Buprenorphine [patch] can cause skin reactions at the site where the patch is applied.

  • Do not place direct heat on buprenorphine patch. Exposure of buprenorphine patch to direct heat may cause too much of the medicine to pass into your body. This can lead to overdose and death. Keep the buprenorphine patch away from:
    • heating pads
    • electric blankets
    • heaters
    • tanning lamps
    • saunas
    • hot tubs
    • heated waterbeds
    • hot baths
    • sunbathing
  • Place the buprenorphine patch only on clean skin. Do not use on broken, irritated and cracked skin.
  • Do not use buprenorphine patch if the seal on the protective pouch is broken or if the patch is cut, damaged or changed. Do not cut the patch.
  • Buprenorphine is not for occasional or “as needed” use

Oral:

  • Buprenorphine sublingual tablets are not for occasional or “as needed” use

Do not use buprenorphine if you:

  • have trouble breathing, severe asthma or severe lung problems
  • have a bowel blockage called paralytic ileus.
  • are allergic to any of the ingredients in buprenorphine.​​​​​​​

Buprenorphine Food Interactions

Medicines can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of buprenorphine, grapefruit and grapefruit juice may interact with buprenorphine and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

Inform MD

Before taking buprenorphine, tell your doctor about all of your medical conditions including if you have:

  • breathing or lung problems
  • history of a heart problem called Long QT syndrome (or if a family member has this condition)
  • head injury or brain problems
  • low blood pressure
  • liver problems
  • kidney problems
  • hepatitis B or hepatitis C
  • had convulsions or seizures
  • severe scoliosis
  • thyroid problems
  • prostate problems or trouble urinating
  • Addison’s disease
  • alcoholism, or a family history of this problem
  • depression or hallucinations (seeing or hearing things that are not there)
  • drug abuse or addiction problem, or a past problem, or a family history of this problem
  • have any other medical conditions

Tell your doctor if you are pregnant or breastfeeding.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements.

Buprenorphine and Pregnancy

Tell your doctor if you are pregnant or plan to become pregnant.

In animal studies, pregnant animals were given this medication and had some babies born with problems. There are limited well-controlled studies that have been done in humans.

There is a risk of neonatal opioid withdrawal syndrome (NOWS). NOWS is a treatable outcome of the long-term use of opioids during pregnancy. NOWS may be life‐threatening if not recognized and treated in the infant. Healthcare professionals must observe newborns for signs of NOWS and treat the newborn accordingly. 

This risk should be balanced against the risk of untreated opioid addiction. 

Buprenorphine and Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed.

Buprenorphine passes into your breast milk. You and your doctor should decide if you will take buprenorphine or breastfeed. You should not do both. Talk to your doctor about the best way to feed your baby if you take buprenorphine.

Buprenorphine Usage

Oral:

  • Always take buprenorphine sublingual (under the tongue) tablets exactly as your doctor tells you. Your doctor may change your dose after seeing how it affects you. Do not change your dose unless your doctor tells you to change it.
  • Do not take buprenorphine sublingual tablets more often than prescribed by your doctor. Ask your doctor for instructions on the right way to take buprenorphine sublingual tablets.
  • Follow the same instructions every time you take a dose of buprenorphine sublingual tablets.
  • Put the tablets under your tongue. Let them dissolve completely.
  • While buprenorphine sublingual tablets are dissolving, do not chew or swallow the tablet because the medicine will not work as well.
  • Talking while the tablet is dissolving can affect how well the medicine in buprenorphine sublingual tablets is absorbed.
  • If you miss a dose of buprenorphine sublingual tablets, take your medicine when you remember. If it is almost time for your next dose, skip the missed dose and take the next dose at your regular time. Do not take 2 doses at the same time unless your doctor tells you to. If you are not sure about your dosing, call your doctor.
  • Do not stop taking buprenorphine sublingual tablets suddenly. You could become sick and have withdrawal symptoms because your body has become used to the medicine. Physical dependence is not the same as drug addiction. Your doctor can tell you more about the differences between physical dependence and drug addiction. To have fewer withdrawal symptoms, ask your doctor how to stop using buprenorphine sublingual tablets the right way.

Topical:

  • Before applying the buprenorphine patch:
    • Do not use soap, alcohol, lotions, oils, or other products to remove any leftover medicine gel from a patch because this may cause more buprenorphine to pass through the skin.
    • Each patch is sealed in its own protective pouch. Do not remove a patch from the pouch until you are ready to use it.
    • Do not use a patch if the seal on the protective pouch is broken or if the patch is cut, damaged or changed in any way.
    • Buprenorphine patches are available in different strengths and patch sizes. Make sure you have the right strength patch that has been prescribed for you
  • Where to apply buprenorphine patches:
    • Buprenorphine patches should be applied to the upper outer arm, upper chest, upper back, or the side of the chest. These 4 sites (located on both sides of the body) provide 8 possible application sites. You should change the skin site where you apply a a patch each week, making sure that at least 3 weeks (21 days) pass before you re-use the same skin site.
    • Apply the patch to a hairless or nearly hairless skin site. If needed, you can clip the hair at the skin site. Do not shave the area. The skin site should not be irritated. Use only water to clean the application site. You should not use soaps, alcohol, oils, lotions, or abrasive devices. Allow the skin to dry before you apply the patch.
    • The skin site should be free of cuts and irritation (rashes, swelling, redness, or other skin problems).
  • When to apply the patch:
    • When you apply a new patch, write down the date and time that the patch is applied. Use this to remember when the patch should be removed.
    • Change the patch at the same time of day, one week (exactly 7 days) after you apply it.
    • After removing and disposing of the patch, write down the time it was removed and how it was disposed.
  • How to apply the patch:
    • If you are wearing a patch, remember to remove it before applying a new one.
    • Each patch is sealed in its own protective pouch.
    • Use scissors to cut open the pouch along the dotted line and remove the patch. Do not remove the patch from the pouch until you are ready to use it. Do not use patches that have been cut or damaged in any way.
    • Hold the patch with the protective liner facing you.
    • Gently bend the patch along the faint line and slowly peel the larger portion of the liner, which covers the sticky surface of the patch.
    • Do not touch the sticky side of the patch with your fingers.
    • Using the smaller portion of the protective liner as a handle, apply the sticky side of the patch to one of the 8 body locations described above
    • While still holding the sticky side down, gently fold back the smaller portion of the patch. Grasp an edge of the remaining protective liner and slowly peel it off.
    • Press the entire patch firmly into place with the palm (See Figure 7) of your hand over the patch, for about 15 seconds. Do not rub the patch.
    • Make sure that the patch firmly sticks to the skin.
    • Go over the edges with your fingers to assure good contact around the patch.
    • Always wash your hands after applying or handling a patch.
    • After the patch is applied, write down the date and time that the patch is applied. Use this to remember when the patch should be removed.
  • If the patch falls off right away after applying, throw it away and put a new one on at a different skin site.
  • If a patch falls off, do not touch the sticky side of the patch with your fingers. A new patch should be applied to a different site. Patches that fall off should not be re-applied. They must be thrown away correctly.
  • If the edges of the patch start to loosen:
    • Apply first aid tape only to the edges of the patch.
    • If problems with the patch not sticking continue, cover the patch with special see-through adhesive dressings (for example Bioclusive or Tegaderm).
      • Remove the backing from the transparent adhesive dressing and place it carefully and completely over the patch, smoothing it over the patch and your skin.
  • Never cover a patch with any other bandage or tape. It should only be covered with a special see-through adhesive dressing. Talk to your doctor or pharmacist about the kinds of dressing that should be used.
  • If your patch falls off later, but before 1 week (7 days) of use, throw it away properly and apply a new patch at a different skin site. Be sure to let your doctor know that this has happened. Do not replace the new patch until 1 week (7 days) after you put it on (or as directed by your doctor).
  • Disposing a buprenorphine patch:
    • Patches must be disposed of by flushing them down the toilet or using the Patch-Disposal Unit.
    • To flush your patch down the toilet:
      • Remove your patch, fold the sticky sides of a used patch together and flush it down the toilet right away.
    • When disposing of unused patches you no longer need, remove the leftover patches from their protective pouch and remove the protective liner. Fold the patches in half with the sticky sides together, and flush the patches down the toilet.
    • Do not flush the pouch or the protective liner down the toilet. These items can be thrown away in the trash.
    • If you prefer not to flush the used patch down the toilet, you must use the Patch-Disposal Unit provided to you to discard the patch.
    • Never put used patches in the trash without first sealing them in the Patch-Disposal Unit.
    • To dispose of patches in household trash using the Patch-Disposal Unit:
      • Remove your patch and follow the directions printed on the Patch-Disposal Unit (See Figure 9) or see complete instructions below. Use one Patch-Disposal Unit for each patch.
      1. Peel back the disposal unit liner to show the sticky surface.
      2. Place the sticky side of the used or unused patch to the indicated area on the disposal unit.
      3. Close the disposal unit by folding the sticky sides together, Press firmly and smoothly over the entire disposal unit so that the patch is sealed within.
      4. The closed disposal unit, with the patch sealed inside may be thrown away in the trash.
      • Do not put unused patches in household trash without first sealing them in the Patch-Disposal Unit.
      • Always remove the leftover patches from their protective pouch and remove the protective liner. The pouch and liner can be disposed of separately in the trash and should not be sealed in the Patch-Disposal Unit.

Implantable Rod (Probuphine):

This medication is available as an implant that is surgically inserted under the skin on the inside of the upper arm. It consists of four one-inch rods. Once inserted, it will provide a constant low dose of buprenorphine. If after six months treatment is still warranted, it may be inserted in the opposite arm for an additional six months.

Subcutaneous injectable (Sublocade):

This medication is available as an injectable form that is given once a month just under the skin (subcutaneously) by a healthcare professional.

Injectable:

  • This medication is additionally available in an injectable form to be given directly into a vein (IV) or muscle (IM) by a healthcare professional.

Buprenorphine Dosage

The buprenorphine dose your doctor recommends will be based on the following:

  • other medical conditions you have
  • other medications you are taking
  • how you respond to this medication
  • your weight
  • your age

Oral:

The recommended dose range with buprenorphine sublingual tablets is 4 mg to 24 mg per day.

Topical:
  • If you have not been taking other opioids, the standard starting dosage is one buprenorphine patch 5 mcg/hour patch applied once a week. If your pain is not adequately controlled after three days, your healthcare provider may increase your dosage. The increase will be based on the amount of short-acting pain medication you needed, or how much "breakthrough" pain you experienced, in the two to three days after starting this medication.
  • The maximum buprenorphine patch dose is one 20-mcg/hour patch applied once a week. Higher doses increase the risk for dangerous changes in the heart rhythm (QTc interval prolongation).

Injectable:

  • The usual dosage of buprenorphine injectable into a muscle (IM) or into a vein (IV) will vary according to age, the severity of the condition, and other factors.
  • The usual dose of buprenorphine injectable to be given under the skin (subcutaneous) is 300 mg once a month for 2 months. After 2 months, the recommended maintenance dose is 100 mg once monthly. 

Buprenorphine Overdose

If you take too much buprenorphine call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If buprenorphine is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if an overdose is suspected, seek emergency medical attention.

Other Requirements

  • Store buprenorphine at room temperature, between 59°F to 86°F (15°C to 30°C).
  • Keep the buprenorphine patch in its unopened protective pouch until you are ready to use it.
  • Keep buprenorphine in a safe place out of the reach of children.
  • Buprenorphine is a controlled substance (CIII) because it contains buprenorphine that can be a target for people who abuse prescription medicines or street drugs. Prevent theft, misuse and abuse. Keep buprenorphine in a safe place to protect from being stolen. Never give buprenorphine to anyone else, even if they have the same symptoms you have. It may harm them or even cause death. Selling or giving away this medicine is against the law.

Buprenorphine FDA Warning

WARNING: IMPORTANCE OF PROPER PATIENT SELECTION, POTENTIAL FOR ABUSE, AND LIMITATIONS OF USE

Proper Patient Selection:

Buprenorphine is a transdermal formulation of buprenorphine indicated for the management of moderate to severe chronic pain in patients requiring a continuous, around-the-clock opioid analgesic for an extended period of time. 

Potential for Abuse:

Buprenorphine is a mu opioid partial agonist and a Schedule III controlled substance. Buprenorphine can be abused in a manner similar to other opioid agonists, legal or illicit. Consider the abuse potential when prescribing or dispensing buprenorphine in situations where the physician or pharmacist is concerned about an increased risk of misuse, abuse, or diversion. 

Persons at increased risk for opioid abuse include those with a personal or family history of substance abuse (including drug or alcohol abuse or addiction) or mental illness (e.g., major depression). Assess patients for their clinical risks for opioid abuse or addiction prior to being prescribed opioids. Routinely monitor all patients receiving opioids for signs of misuse, abuse, and addiction. 

Limitations of Use:

Do not exceed a dose of one 20 mcg/hour buprenorphine system due to the risk of QTc interval prolongation. 

Avoid exposing the buprenorphine application site and surrounding area to direct external heat sources. Temperature-dependent increases in buprenorphine release from the system may result in overdose and death.