Buprenorphine (Buccal Mucosa, Sublingual)

Buprenorphine works by numbing the central nervous system to relieve the pain, or prevent withdrawal symptoms.

Overview

Buprenorphine is a very strong, prescription only pain killer that is used to relieve severe, chronic and persistent pain. It works by numbing the central nervous system to relieve the pain experienced by the patient in various parts of the body. It is also used to treat addiction to opioids, by acting on the CNS to prevent withdrawal symptoms.

The drug is also marketed and sold under the brand names of Belbuca and Subutex in the United States.

Buprenorphine is issued in two forms, a film or a tablet, which are both administered into routes that allow the pain killer to enter the bloodstream as quick as possible, therefore achieving fast results. The film is used as a pain killer, while the tablet is used to treat opioid addiction.

When a person develops an opioid addiction (a narcotic like morphine or heroin), they form both a physical and a mental dependency on the drug. However, taking that patient off the drug straight away can cause major side effects and withdrawal symptoms. These side effects can be prevented if the patient is instead put onto buprenorphine. For treating narcotic addiction, the drug is often used in partnership with naxolene.

Buprenorphine has similar effects on the human body as other opioid drugs like codeine, morphine and heroin. It has an impact on the part of the brain that relieves cravings and addictive feelings, but without giving the patient the same high as other highly addictive opioid drugs like heroin and codeine. (ref 1)

Buprenorphine is also highly addictive, like other opioid drugs, and can lead to physical and mental dependency. It is therefore important that patients taking buprenorphine are closely and regularly monitored for signs of side effects and dependency.

Belbuca is issued as a film that is applied to the buccal area (inside the cheek), where it then dissolves into the cheek tissue and enters the blood stream directly.

Subutex is issued as a tablet that is placed under the tongue (the sublingual - or SL - route). The substance then dissolves into the blood stream through the tissues underneath the tongue. This is a quick and convenient way to get the medication into the blood.

Buprenorphine - in either its tablet form or its film form - is only available as a prescription from a registered medical care provider or doctor. It is also only prescribed under extreme circumstances and usually when other, less strong substances have been tried in the first instance. The medication is one of the strongest and fastest acting pain killers available and is highly effective at treating pain that has been caused by a variety of conditions. The medication is designed for short-term use; if a longer-term solution is required, there may be other more suitable medications.

Conditions treated

  • Addiction to opioid drugs, such as heroin, codeine and morphine (film)
  • Treatment of severe, chronic or persistent pain (tablet)

Type of medicine

  • Film (to be placed on the inside of the cheek)
  • Tablet (to be placed on the underside of the tongue)

Side effects

As with any opioid, there are various side effects that patients may experience as a result of taking buprenorphine. Most people are able to take their prescriptions of buprenorphine without any side effects, and others may be able to deal with the side effects they experience. Usually, if the benefit of the drug outweighs the discomfort of the side effects, then you should continue using the medication. However, there are some instances in which you may find the side effects to be too unpleasant to deal with. Severe side effects are rare, but you should also report any unusual or severe changes in your body or mental well-being when taking buprenorphine.

You should call 911 immediately if you experience any of the following side effects, as these can in some extreme cases lead to fatalities if they are left untreated:

  • Difficulty breathing, or severe shortness of breath
  • Swelling in any area of the face, particularly the throat, lips or tongue
  • Severe confusion
  • Clammy and cold skin
  • Dizziness
  • Severe restlessness
  • Nervousness
  • Severe weaknesses
  • Seizures
  • Slow breathing

Other side effects that you may experience, which could also be serious, include the below. You should call your doctor for advice if you notice any of these:

  • Increased or excessive sweating
  • Hives
  • Redness in the face
  • Hot flushes
  • Changes in your heartbeat, e.g. faster, slower or more irregular than normal

There are some side effects that you may experience that are considered normal or, in many cases, harmless. However, if these side effects do not go away after a short amount of time, you should contact a health care professional for advice. You may be put onto another medication. Common side effects include:

  • Nausea or vomiting
  • Lightheadedness, headache or faint feeling
  • Dizziness or drowsiness
  • Constipation

Dosage

Patients should always take the recommended dosage of buprenorphine that is prescribed to them by their doctors. You should never attempt to increase the dose based on your symptoms. If your symptoms are not improving, you should always speak to your doctor, and possibly seek alternative medication. Taking too much buprenorphine can lead to the symptoms of overdose and can be highly dangerous.

The initial dosage for opioid dependence is 8 mg, taken once per day via the sublingual route on day 1. Then this is increased to 16 mg once during day 2. The maintenance dose after this is between 4 mg and 24 mg per day. Adjustments to the dose are usually made in 2 mg increments/decrements.

The dose for chronic pain, administered via the buccal mucosa route, are 75 mcg as a single dose either once or twice per day. The maximum dose per 12 hours is not usually greater than 900 mcg.

Doses for children are usually set on body weight, and will be determined by an experienced health care professional.

Patients must stick to prescription instructions and always take their doses at the required times of day. If a dose is missed, however, do not attempt to double up on doses. This may result in the symptoms of an overdose. If you think you may have taken too much buprenorphine, you should contact your local poison control center or your doctor immediately.

Major drug interactions

There are a particularly large number of drugs that can interact with buprenorphine. When one drug reacts with another, it can lead to unknown, undesirable and sometimes very dangerous side effects for the patient. Taking one drug may lead to the ineffectiveness of another, and some drug combinations can even make the health conditions they are being used to treat worse. This is why a doctor will always ask you whether you are taking any other medications, as well as what they are. You should always keep a list of names of the medicines you are taking, and provide it to your doctor when asked.

There are 1,037 drugs that interact with buprenorphine. These drug interactions are given three levels - minor, moderate and major. Where there is a minor interaction present, the doctor will usually look for another prescription, or else will alter the dose of buprenorphine offered to you. You will also be closely monitored throughout the prescription. For drugs with moderate interactions, alternative drugs will be offered in most cases and only usually combined in extreme circumstances. Where there is a major interaction, combinations should always be avoided, as the risk of combining outweighs the benefit.

312 drugs have a major interaction with buprenorphine. These drugs are:

  • acetaminophen, butalbital
  • acetaminophen, butalbital, caffeine
  • acetaminophen, butalbital, caffeine, codeine
  • acetaminophen, caffeine, chlorpheniramine, hydrocodone, phenylephrine
  • acetaminophen, caffeine, dihydrocodeine
  • acetaminophen, chlorpheniramine, codeine
  • acetaminophen, chlorpheniramine, codeine, phenylephrine
  • acetaminophen, codeine
  • acetaminophen, codeine, guaifenesin, phenylephrine
  • acetaminophen, codeine, guaifenesin, pseudoephedrine
  • acetaminophen, dichloralphenazone, isometheptene mucate
  • acetaminophen, hydrocodone
  • acetaminophen, oxycodone
  • acetaminophen, pentazocine
  • acetaminophen, propoxyphene
  • acetaminophen, tramadol
  • acetylcarbromal
  • alprazolam
  • alvimopan
  • aminophylline, amobarbital, ephedrine
  • aminophylline, ephedrine, guaifenesin, phenobarbital
  • aminophylline, ephedrine, phenobarbital, potassium iodide
  • amitriptyline, chlordiazepoxide
  • amitriptyline, perphenazine
  • ammonium chloride, chlorpheniramine, codeine, phenylephrine
  • amobarbital
  • amobarbital, secobarbital
  • anagrelide
  • anhydrous calcium iodide, codeine
  • aripiprazole
  • arsenic trioxide
  • artemether, lumefantrine
  • aspirin, butalbital
  • aspirin, butalbital, caffeine
  • aspirin, butalbital, caffeine, codeine
  • aspirin, caffeine, dihydrocodeine
  • aspirin, caffeine, orphenadrine
  • aspirin, caffeine, propoxyphene
  • aspirin, carisoprodol
  • aspirin, carisoprodol, codeine
  • aspirin, codeine
  • aspirin, hydrocodone
  • aspirin, meprobamate
  • aspirin, methocarbamol
  • aspirin, oxycodone
  • aspirin, pentazocine
  • atropine, hyoscyamine, phenobarbital, scopolamine
  • atropine, phenobarbital
  • baclofen
  • baclofen, flurbiprofen, lidocaine topical
  • bedaquiline
  • belladonna, butabarbital
  • belladonna, caffeine, ergotamine, pentobarbital
  • belladonna, ergotamine, phenobarbital
  • belladonna, opium
  • benzoic acid, hyoscyamine, methenamine, methylene blue, phenyl salicylate
  • brexpiprazole
  • brivaracetam
  • bromodiphenhydramine, codeine
  • brompheniramine, codeine
  • brompheniramine, codeine, phenylephrine
  • brompheniramine, codeine, phenylpropanolamine
  • brompheniramine, codeine, pseudoephedrine
  • brompheniramine, dihydrocodeine, phenylephrine
  • brompheniramine, dihydrocodeine, pseudoephedrine
  • brompheniramine, hydrocodone, phenylephrine
  • brompheniramine, hydrocodone, pseudoephedrine
  • bupivacaine, fentanyl
  • bupivacaine, hydromorphone
  • bupropion
  • bupropion, naltrexone
  • buspirone
  • butabarbital
  • butabarbital, hyoscyamine, phenazopyridine
  • butalbital
  • butorphanol
  • cannabis
  • carbamazepine
  • carbinoxamine, hydrocodone, phenylephrine
  • carbinoxamine, hydrocodone, pseudoephedrine
  • cariprazine
  • carisoprodol
  • ceritinib
  • chloral hydrate
  • chlorcyclizine, codeine
  • chlorcyclizine, codeine, phenylephrine
  • chlorcyclizine, codeine, pseudoephedrine
  • chlordiazepoxide
  • chlordiazepoxide, clidinium
  • chlordiazepoxide, methscopolamine
  • chlormezanone
  • chlorphenesin
  • chlorpheniramine, codeine
  • chlorpheniramine, codeine, phenylephrine
  • chlorpheniramine, codeine, phenylephrine, phenylpropanolamine
  • chlorpheniramine, codeine, phenylephrine, potassium iodide
  • chlorpheniramine, codeine, pseudoephedrine
  • chlorpheniramine, dihydrocodeine, phenylephrine
  • chlorpheniramine, dihydrocodeine, phenylephrine, phenylpropanolamine
  • chlorpheniramine, dihydrocodeine, pseudoephedrine
  • chlorpheniramine, guaifenesin, hydrocodone, pseudoephedrine
  • chlorpheniramine, hydrocodone
  • chlorpheniramine, hydrocodone, phenylephrine
  • chlorpheniramine, hydrocodone, pseudoephedrine
  • chlorpromazine
  • chlorzoxazone
  • cisapride
  • citalopram
  • clobazam
  • clonazepam
  • clorazepate
  • clozapine
  • codeine
  • codeine, dexbrompheniramine, pseudoephedrine
  • codeine, dexchlorpheniramine, phenylephrine
  • codeine, diphenhydramine, phenylephrine
  • codeine, guaifenesin
  • codeine, guaifenesin, phenylephrine
  • codeine, guaifenesin, phenylpropanolamine
  • codeine, guaifenesin, pseudoephedrine
  • codeine, pheniramine, phenylephrine, sodium citrate
  • codeine, phenylephrine
  • codeine, phenylephrine, promethazine
  • codeine, phenylephrine, pyrilamine
  • codeine, phenylephrine, triprolidine
  • codeine, promethazine
  • codeine, pseudoephedrine
  • codeine, pseudoephedrine, pyrilamine
  • codeine, pseudoephedrine, triprolidine
  • codeine, pyrilamine
  • conjugated estrogens, meprobamate
  • crizotinib
  • cyclobenzaprine
  • dantrolene
  • dexbrompheniramine, hydrocodone, phenylephrine
  • dexchlorpheniramine, hydrocodone, phenylephrine
  • dexmedetomidine
  • dezocine
  • diazepam
  • dihydrocodeine, guaifenesin
  • dihydrocodeine, guaifenesin, phenylephrine
  • dihydrocodeine, guaifenesin, pseudoephedrine
  • dihydrocodeine, phenylephrine
  • dihydrocodeine, phenylephrine, pyrilamine
  • diphenhydramine, hydrocodone, phenylephrine
  • divalproex sodium
  • dolasetron
  • dronabinol
  • dronedarone
  • droperidol
  • droperidol, fentanyl
  • dyphylline, ephedrine, guaifenesin, phenobarbital
  • ephedrine, hydroxyzine, theophylline
  • ephedrine, phenobarbital, potassium iodide, theophylline
  • ephedrine, phenobarbital, theophylline
  • escitalopram
  • eslicarbazepine
  • estazolam
  • eszopiclone
  • ethanol
  • ethchlorvynol
  • ethosuximide
  • ethotoin
  • ezogabine
  • felbamate
  • fentanyl
  • fentanyl, ropivacaine
  • fingolimod
  • fluoxetine, olanzapine
  • fluphenazine
  • flurazepam
  • fosphenytoin
  • furazolidone
  • gatifloxacin
  • grepafloxacin
  • guaifenesin, hydrocodone
  • guaifenesin, hydrocodone, pheniramine, phenylephrine, phenylpropanolamine
  • guaifenesin, hydrocodone, pheniramine, phenylpropanolamine, pyrilamine
  • guaifenesin, hydrocodone, phenylephrine
  • guaifenesin, hydrocodone, pseudoephedrine
  • guaifenesin, hydromorphone
  • halazepam
  • halofantrine
  • haloperidol
  • heroin
  • homatropine, hydrocodone
  • hydrocodone
  • hydrocodone, ibuprofen
  • hydrocodone, pheniramine, phenylephrine, phenylpropanolamine, pyrilamine
  • hydrocodone, phenylephrine
  • hydrocodone, phenylephrine, pyrilamine
  • hydrocodone, phenylpropanolamine
  • hydrocodone, potassium guaiacolsulfonate
  • hydrocodone, potassium guaiacolsulfonate, pseudoephedrine
  • hydrocodone, pseudoephedrine
  • hydrocodone, pseudoephedrine, triprolidine
  • hydromorphone
  • hydromorphone, ropivacaine
  • hydroxyzine
  • hyoscyamine, methenamine, methylene blue, phenyl salicylate
  • hyoscyamine, methenamine, methylene blue, phenyl salicylate, sodium biphosphate
  • hyoscyamine, methenamine, methylene blue, sodium biphosphate
  • hyoscyamine, phenobarbital
  • ibuprofen, oxycodone
  • iloperidone
  • iohexol
  • iopamidol
  • isocarboxazid
  • ivabradine
  • kava
  • lamotrigine
  • levetiracetam
  • levomethadyl acetate
  • levorphanol
  • lorazepam
  • loxapine
  • lurasidone
  • meperidine
  • meperidine, promethazine
  • mephenytoin
  • mephobarbital
  • meprobamate
  • mesoridazine
  • metaxalone
  • methadone
  • methocarbamol
  • methsuximide
  • methylene blue
  • metrizamide
  • midazolam
  • mifepristone
  • molindone
  • morphine
  • morphine liposomal
  • morphine, naltrexone
  • moxifloxacin
  • nabilone
  • nalbuphine
  • naloxone, oxycodone
  • naloxone, pentazocine
  • naltrexone
  • naltrexone, oxycodone
  • nilotinib
  • olanzapine
  • opium
  • orphenadrine
  • osimertinib
  • oxazepam
  • oxcarbazepine
  • oxycodone
  • oxymorphone
  • paliperidone
  • panobinostat
  • papaverine
  • paraldehyde
  • paramethadione
  • pasireotide
  • pentazocine
  • pentobarbital
  • perampanel
  • perflutren
  • perphenazine
  • phenacemide
  • phenelzine
  • phenobarbital
  • phensuximide
  • phentermine, topiramate
  • phenytoin
  • pimavanserin
  • pimozide
  • pregabalin
  • primidone
  • procarbazine
  • prochlorperazine
  • promazine
  • propiomazine
  • propoxyphene
  • quazepam
  • ramelteon
  • risperidone
  • rufinamide
  • saquinavir
  • secobarbital
  • sodium oxybate
  • sparfloxacin
  • suvorexant
  • tasimelteon
  • temazepam
  • thioridazine
  • thiothixene
  • tiagabine
  • tizanidine
  • topiramate
  • toremifene
  • tramadol
  • tranylcypromine
  • triazolam
  • trifluoperazine
  • triflupromazine
  • trimethadione
  • valerian
  • valproic acid
  • vandetanib
  • vemurafenib
  • vigabatrin
  • zaleplon
  • ziconotide
  • ziprasidone
  • zolpidem
  • zonisamide

Warnings

You should not take buprenorphine if you are taking any other types of narcotic pain killers, sleeping tablets, mood altering drugs such as those used to treat depression, sedatives or tranquilizers.

Alcohol interactions

You should refrain from drinking alcohol while you are taking a treatment course of Buprenorphine. This is because alcohol and buprenorphine have a major interaction when taken together, causing potentially dangerous consequences. If you drink alcohol while taking this drug, you are at an increased risk of developing worsened symptoms, such as extreme nausea and vomiting, headaches and migraines, loss of consciousness, dizziness, confusion or even coma.

Operating hazourdous machinery and driving

You should not drive or operate any hazardous machinery when you start taking buprenorphine. You should instead wait to see how your body reacts to the drug before doing anything that requires acute mental concentration. Buprenorphine can affect your concentration levels, and can also impair your judgement. Speak to your doctor if you are in doubt about how this drug is impacting your ability to make judgements.

Disease Interactions

You should also tell your doctor if you suffer from any other conditions. This is because certain conditions can also interact with buprenophine. Taking this drug while suffering from any of the conditions listed below can make these conditions worse. It can also interact with any medication that you are taking to treat these conditions. You may also find that these conditions can impair the effectiveness of buprenorphine and your chronic pain or drug addiction may return. Always seek advice from your doctor if you are experiencing any of the following, or have experienced them in the past:

  • Hypothyroidism
  • Seizure Disorders
  • Urinary Retention
  • Respiratory Depression
  • Impaired Gi Motility
  • Liver Disease
  • Renal Dysfunction
  • Acute Mi
  • Adrenal Insufficiency
  • Biliary Spasm
  • Drug Dependence
  • Intracranial Pressure
  • Infectious Diarrhea
  • Prematurity

Women and pregnancy

This medication should not be used during pregnancy. Always tell your doctor if you are pregnant, or if you think you might be. Do not attempt to become pregnant while you are taking this medication as it may harm your unborn baby, leading to birth defects and abnormalities.

Children

There are limited studies into the long-term health implications of buprenorphine on children. Prescribing the medication to children should be approached with caution, and the child should be monitored regularly for signs of any serious side effects.

Storage

Keep this medication at room temperature in a closed container. This generally means temperatures of between 15 and 25 degrees centigrade. Keep it away from heat and direct light sources at all times. Do not freeze your buprenorphine prescription, and do not put it in the fridge.

Keep your prescription in the box in which it was supplied. Always keep the labels on the boxes to prevent the drug from becoming mixed up with others.

You should always keep this medication out of the reach of children. Buprenorphine can have serious consequences if consumed by children or pets so you should always take extra precautions to make sure they cannot get access to it.

Disposal

Once your medication is out of date, you should throw it away. Buprenorphine film and tablets are both suitable for flushing down the toilet and this should be done as soon as you realise you no longer intend to take the medication. You should not take medication if you realise it is past its expiry date. This is because outdated buprenorphine can cause worsened side effects, or may be less effective in treating your pain or addiction.

The safest way to dispose of your drugs if you no longer need them is by contacting your local take back scheme. These schemes were set up by the FDA to recycle unwanted medications, preventing them from getting into the wrong hands or causing harm to the environment. If you have drugs that you no longer need - including buprenorphine, you should contact the FDA to see if you can arrange a collection. This ensures that your medicine cabinet only contains the essentials, and minimizes the risk to other people and pets in your household.

Summary

Buprenorphine has been found to be a highly effective medication for treating those with opioid addictions or chronic pain. It is also often used as a safer and less severe alternative to methadone to treat drug addiction. Buprenorphine generally has less severe side effects to methadone and therefore may be suitable for a wider range of patients. If used carefully and according to the instructions given to patients by a health care professional, it can be a safe treatment with long-term health benefits.

It is important to note that there are a large number of other drugs that have a major interaction with buprenorphine. Therefore, it is especially important that the full medical history of a patient is known before prescribing the drug. Patients should be aware that the impact of taking many other medications at the same time as this one can lead to serious side effects that can be potentially dangerous. It is also important that patients are open about any other conditions they suffer from, as buprenorphine can make conditions such as renal dysfunctions and liver diseases worse.

Patients taking buprenorphine to treat drug addiction should be monitored especially closely, seen as mixing other opioids with this one can lead to severe consequences. If there are any signs of relapse onto substances like heroin or morphine, dosage may be altered or an alternative treatment like methadone may be used.

Overall, buprenorphine is an effective and potentially life-saving drug for those with life-threatening addictions and/or chronic pain, and can lead to drastic improvements in the patient's quality of life.

 

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Last Reviewed:
January 31, 2018
Last Updated:
April 02, 2018