Buprenorphine/Naloxone (Oromucosal, Sublingual)

Used to help patients reduce their dependance on narcotics, buprenorphine and naloxone is available on prescription and is a synthetic opioid.

Overview:

Buprenorphine and naloxone are medications used as a maintenance therapy to treat individuals who are addicted to or dependent on narcotics. Using this treatment allows the patient to slowly withdraw from his or her addiction while avoiding the potentially harmful withdrawal side effects normally associated with stopping opioid drug use. Buprenorphine and naloxone is delivered as a tablet or film with various dosages. Orange flavored, it is placed in the mouth usually under the tongue, where it sticks and delivers the medication through the mucosal lining in the mouth. This medication is only available by prescription.

Using buprenorphine and naloxone incorrectly can result in serious side effects, including addiction, overdose and even death. This medication should never be taken by anyone for whom it has not been prescribed, and especially should be kept out of the reach of children. Patients should understand all instructions from their doctor, and should not take more or less of this medication than is prescribed, and should follow all directions regarding daily dose frequency and amount, as well as length of the treatment, as prescribed by their doctor. By taking buprenorphine and naloxone under the supervision of a health professional, over a period of six to twelve months a patient may successfully manage their lives as well as slowly transition off the buprenorphine and naloxone to wean their nervous system off the dependency on narcotics.

Conditions Treated:

  • Opioid addiction or dependence

Type of Medicine:

  • Synthetic opioid

Side Effects:

When taking buprenorphine and naloxone, patients may experience certain unwanted side effects. Not all of these side effects will occur for every patient, but in the event they do, immediate medical attention may be required. Patients should contact their doctor right away if they experience any of these side effects: hoarseness or coughing; feeling faint, lightheaded or dizzy; feeling unusually warm or hot, or have fever, sweating or chills; have an unusual headache; have pain in their lower back or side; find it difficult or painful to urinate; or experience unusual redness or have flushing of their skin on the face or neck.

Some patients may experience swelling of the hands, feet or arms or legs; unusual weight gain or loss, or tingling in their feet or hands.

As buprenorphine and naloxone is an opioid, overdose is a possible side effect. This can be life threatening, and patients should get emergency medical help immediately if they experience any symptoms such as the following:

  • Difficulty breathing or rapid or shallow breathing
  • Confusion
  • Blurred vision
  • Drowsiness, sleepiness or an unusual tiredness or weakness
  • Pale skin or blue skin, lips, or nails.

Buprenorphine and naloxone can also cause some side effects that are not as serious in nature, and may resolve as the patient's body becomes adjusted to the medication. Some of these less severe side effects include stomach or abdominal pain, constipation, feeling weak, nausea or vomiting, difficulty sleeping, and other pain. Some of the less common side effects that fall into this category are diarrhea, back pain, and cold-like symptoms such as a runny or stuffy nose and sneezing.

There may be additional side effects which are not listed here, but which may cause discomfort or pain in some patients. For any unusual symptoms patients should contact their doctor to discuss whether this is a result of taking buprenorphine and naloxone. Patients may also call the FDA to report side effects at 1-800-FDA-1088.

Dosage:

Each patient taking buprenorphine and naloxone will have specific dosages recommended for them. It is important to follow the instructions given by the prescribing physician in order to achieve the most effective result and to avoid side effects. It is very important that a patient does not change the dose or frequency of this medication in order to avoid the effects of withdrawal and other unwanted side effects. A Medication Guide is provided with the packaging for this medication, which is important for patients to read and understand thoroughly. For any questions, patients should discuss with their doctor prior to taking buprenorphine and naloxone.

The dosages described below are averages for adult patients only, and each individual patient may have different dosages or instructions depending on their specific condition. This medication is not recommended for use in children.

For buccal (mouth) film form: A doctor may prescribe the medication as a film, which is placed in the mouth. In this form, the drug is incorporated into a small film which is placed in the mouth as directed and allowed to melt. As the medication melts, it is absorbed into the bloodstream through the mucous membrane. For adults taking the oral film form of this drug, an average dose is 8.4 milligrams (mg) of buprenorphine plus 1.4 mg of naloxone. This is taken in one dose, once per day. A doctor may provide different instructions depending on the condition.

To use this form of buprenorphine and naloxone, a patient should follow these steps:

  • First moisten the mouth, using the tongue against the inside of the cheek or by rinsing the mouth using water, near the spot where the film will be placed.
  • The film should not be torn, cut or damaged. Using a clean, dry finger, place the film on the fingertip, with any text appearing on the film to be facing upright.
  • Use the finger to put the film against the side of the cheek. Once again, if there is any text on the film, this should be on the side against the cheek. Hold the film in place against the cheek for five seconds.
  • Be sure to allow the film to stay in place until dissolved. It is important not to move, touch, chew or swallow the piece of film.
  • For patients prescribed more than a single piece of film, repeat these steps for the second film, by placing it on the cheek on the other side. Patients should not put more than two pieces of film on one side of the cheek at a time.
  • Patients should avoid eating or drinking anything until the film has dissolved completely, to ensure the medication is absorbed properly.

Sublingual (under tongue) form: Another type of buprenorphine and naloxone that comes on film is intended to be placed in the mouth under the tongue (sublingual). In this form, the drug also comes on a film, but the patient will place this film under the tongue where it will melt and become absorbed into the bloodstream. For adults taking the oral film form of this drug, an average dose is 16 mg of buprenorphine plus 4 mg of naloxone. This is also taken once per day as one dose.

To use this form of the medication, patients should follow these steps:

  • Rinse the mouth with water first, in order to moisten the mouth.
  • Using a clean finger, put the film under the tongue. Do not remove until the film has dissolved.
  • If a patient has been prescribed more than one film, he or she should put the additional film under the tongue in an opposite spot from the first.
  • Avoid moving, cutting, chewing or swallowing the film once it has been placed.

Sublingual (under tongue) tablet: A third form of buprenorphine and naloxone is a tablet that is placed under the tongue and is allowed to melt, thereby being absorbed into the bloodstream. At the beginning of treatment, the doctor will provide an initial dose on the first day, of up to 5.7 mg of buprenorphine with 1.4 mg of naloxone, which may be divided. On the second day, the patient usually takes up to 11.4 mg of buprenorphine with 2.9 mg of naloxone in one dose. For some patients who are treating a dependency on heroin, methadone or other opioid medications, a doctor may determine that the patient should only take buprenorphine. After this initial phase of treatment, the patient will begin maintenance treatment of either 11.4 (mg) of buprenorphine plus 2.9 mg of naloxone once per day, or 8 mg to 16 mg once per day, depending on the advice of the doctor.

To use this form of the medication, patients should follow these steps:

  • Patients should avoid crushing, cutting, chewing or swallowing the tablet.
  • The tablet should be placed under the tongue, and remain there under dissolved.
  • For patients prescribed two or more tablets, all tablets can be placed at once, in different spots under the tongue. Alternatively, a patient can put two tablets at a time, wait for those to dissolve, and continue with two more tablets, until the full dose has been placed and dissolved.
  • Patients should avoid eating or drinking anything until the tablets have dissolved completely, to ensure the medication is absorbed properly.

In the event that a patient misses a dose, it is important not to take two doses at one time to catch up on the missed dose. This can cause unwanted side effects. If a patient misses a dose, he or she should take it as soon as they remember. If it is getting close to the time for the next dose, however, it's better to wait until the next dose and take that one as scheduled and continue the regular schedule for the medication.

Patients should talk to their doctor before switching from one form of buprenorphine and naloxone to another, to ensure the continuity of correct dosages and treatment.

This medication has specific timing requirements for it to achieve full effectiveness. Patients will be informed by their doctor about special requirements for taking this medication in conjunction with eating food or drinking liquids.

Major Drug Interactions:

Because buprenorphine and naloxone is a synthetic opioid, it can interact with many different types of medications, both prescription and non-prescription. The list is quite extensive, which makes it very important that any patient seeking buprenorphine and naloxone treatment give a thorough and detailed medical history and list of current medications to the prescribing healthcare professional. In some cases, a patient may have to stop taking one or more medications in order to take buprenorphine and naloxone.

For one medication, Naltrexone, taking buprenorphine and naloxone in conjunction with this is not recommended. Naltrexone is a drug which works to stop the effects of opioids in the body, which would also block the effectiveness of buprenorphine and naloxone. Before taking buprenorphine and naloxone, patients taking naltrexone should seek the advice of their doctor first, as the doctor may decide to change medications or avoid buprenorphine and naloxone.

Other medications that may have interactions with buprenorphine and naloxone are listed below; taking these medications along with buprenorphine and naloxone is not recommended without the advice of a doctor. A doctor may determine that the patient can take buprenorphine and naloxone in conjunction with these medications, but may alter dosage or frequency to avoid side effects.

The list below is lengthy, but is not intended to include all possible drugs that may interact with buprenorphine and naloxone:

  • Acepromazine
  • Alfentanil
  • Almotriptan
  • Alphaprodine
  • Alprazolam
  • Alvimopan
  • Amineptine
  • Amisulpride
  • Amitriptylinoxide
  • Amobarbital
  • Amoxapine
  • Anileridine
  • Aripiprazole
  • Asenapine
  • Atazanavir
  • Baclofen
  • Benperidol
  • Bromazepam
  • Bromopride
  • Brompheniramine
  • Buprenorphine
  • Buspirone
  • Butabarbital
  • Butorphanol
  • Carbamazepine
  • Carbinoxamine
  • Cariprazine
  • Carisoprodol
  • Carphenazine
  • Chloral Hydrate
  • Chlordiazepoxide
  • Chlorpheniramine
  • Chlorpromazine
  • Chlorzoxazone
  • Citalopram
  • Clobazam
  • Clomipramine
  • Clonazepam
  • Clorazepate
  • Clozapine
  • Cocaine
  • Codeine
  • Cyclobenzaprine
  • Dantrolene
  • Desipramine
  • Desvenlafaxine
  • Dexmedetomidine
  • Dextromethorphan
  • Dezocine
  • Diacetylmorphine
  • Diazepam
  • Dibenzepin
  • Dichloralphenazone
  • Difenoxin
  • Dihydrocodeine
  • Diphenhydramine
  • Diphenoxylate
  • Dolasetron
  • Donepezil
  • Doxepin
  • Doxylamine
  • Droperidol
  • Duloxetine
  • Eletriptan
  • Enflurane
  • Escitalopram
  • Estazolam
  • Eszopiclone
  • Ethchlorvynol
  • Ethopropazine
  • Ethylmorphine
  • Fentanyl
  • Flibanserin
  • Flunitrazepam
  • Fluoxetine
  • Fluphenazine
  • Flurazepam
  • Fluspirilene
  • Fluvoxamine
  • Fospropofol
  • Frovatriptan
  • Furazolidone
  • Granisetron
  • Halazepam
  • Haloperidol
  • Halothane
  • Hexobarbital
  • Hydrocodone
  • Hydromorphone
  • Hydroxytryptophan
  • Hydroxyzine
  • Iloperidone
  • Imipramine
  • Iproniazid
  • Isocarboxazid
  • Isoflurane
  • Ketamine
  • Ketazolam
  • Ketobemidone
  • Levomilnacipran
  • Levorphanol
  • Linezolid
  • Lithium
  • Lofepramine
  • Lorazepam
  • Lorcaserin
  • Lurasidone
  • Meclizine
  • Melitracen
  • Melperone
  • Meperidine
  • Mephobarbital
  • Meprobamate
  • Meptazinol
  • Mesoridazine
  • Metaxalone
  • Methadone
  • Methdilazine
  • Methocarbamol
  • Methohexital
  • Methotrimeprazine
  • Methylene Blue
  • Methylnaltrexone
  • Midazolam
  • Milnacipran
  • Mirtazapine
  • Moclobemide
  • Molindone
  • Moricizine
  • Morphine
  • Morphine Sulfate Liposome
  • Nalbuphine
  • Nalmefene
  • Nalorphine
  • Naloxegol
  • Naloxone
  • Naratriptan
  • Nefazodone
  • Nialamide
  • Nicomorphine
  • Nitrazepam
  • Nitrous Oxide
  • Nortriptyline
  • Olanzapine
  • Ondansetron
  • Opipramol
  • Opium
  • Opium Alkaloids
  • Orphenadrine
  • Oxazepam
  • Oxycodone
  • Oxymorphone
  • Paliperidone
  • Palonosetron
  • Papaveretum
  • Paregoric
  • Paroxetine
  • Pentazocine
  • Pentobarbital
  • Perampanel
  • Perazine
  • Periciazine
  • Perphenazine
  • Phenelzine
  • Phenobarbital
  • Pimavanserin
  • Pimozide
  • Piperacetazine
  • Pipotiazine
  • Piritramide
  • Prazepam
  • Primidone
  • Procarbazine
  • Prochlorperazine
  • Promazine
  • Promethazine
  • Propofol
  • Propoxyphene
  • Protriptyline
  • Quazepam
  • Quetiapine
  • Ramelteon
  • Rasagiline
  • Remifentanil
  • Remoxipride
  • Risperidone
  • Rizatriptan
  • Safinamide
  • Samidorphan
  • Secobarbital
  • Selegiline
  • Sertindole
  • Sertraline
  • Sibutramine
  • Sodium Oxybate
  • St John's Wort
  • Sufentanil
  • Sulpiride
  • Sumatriptan
  • Suvorexant
  • Tapentadol
  • Temazepam
  • Thiethylperazine
  • Thiopental
  • Thiopropazate
  • Thioridazine
  • Thiothixene
  • Tianeptine
  • Tilidine
  • Tizanidine
  • Tolonium Chloride
  • Topiramate
  • Tramadol
  • Tranylcypromine
  • Triazolam
  • Trifluoperazine
  • Trifluperidol
  • Triflupromazine
  • Trimeprazine
  • Trimipramine
  • Tryptophan
  • Venlafaxine
  • Vilazodone
  • Vortioxetine
  • Zaleplon
  • Ziprasidone
  • Zolmitriptan
  • Zolpidem
  • Zopiclone
  • Zotepine

In addition to the drugs listed above, it is highly recommended that patients taking buprenorphine and naloxone should avoid use of alcohol, such as wine or beer, or any over the counter medications containing ethanol. Tobacco products may also interfere with taking this medication. Patients should discuss their alcohol and tobacco use with their doctor to determine the right course for them.

Warnings:

Patients who are taking buprenorphine and naloxone will need to meet with their doctor on a regular basis. Given the potential for side effects and to determine how long the patient will need to continue treatment, it is very important for the doctor to monitor progress while taking this medication to ensure that the medication is having its desired effect. In addition, the doctor will determine how long treatment will be necessary for. A doctor may also order a blood test to determine if there are any side effects.

Use of this medication without a prescription is illegal, and can be very dangerous and even deadly to anyone not prescribed this drug by a doctor. Patients should be sure to keep their medication in a secure and safe location, away from children and away from other individuals who may want to steal this drug.

This medication should only be taken as prescribed. Taking more or less of this drug, or taking it more or less frequently than instructed can result in serious or deadly side effects, including overdose. Patients having an overdose may experience severe dizziness or extreme weakness, difficulty breathing or a slow heartbeat, seizures, or clammy, damp-feeling skin. A doctor should be contacted immediately in the event of any of these symptoms.

For patients that require any kind of anesthetic for surgery, severe side effects can occur if these are combined with buprenorphine and naloxone. In advance of any type of surgery, as well as dental surgery, a patient should inform the health professional preforming the surgery that he or she is taking buprenorphine and naloxone.

There are serious side effects to taking buprenorphine and naloxone with other tranquilizer medications or when drinking alcohol. For example, patients taking either prescription or over the counter medications including: antihistamines or allergy and cold medication, sleeping pills, tranquilizers or other sedatives, any kind of prescription narcotics or pain relief medicine, seizure medication or muscle relaxers, as well as the anesthetics described above. Patients should seek the advice of their doctor about using any of these medications while taking buprenorphine and naloxone.

Some patients may find that they feel dizzier or lightheaded when they get up suddenly after sitting or lying down, including fainting in some cases. If this occurs, slowly getting to a standing position may help, and returning to a lying down position can also help relieve this feeling.

Because of this possibility of dizziness or lightheadedness, as well as the possibility of feeling sleepy or drowsy, patients should be very careful when driving, or if they use machines or perform other tasks that require being alert and attentive.

Patients should contact their doctor immediately if they experience tenderness or soreness in the area of the upper stomach, if they have pale stools or discolored or dark urine, have any unusual loss of appetite, or have stomach upset, vomiting, nausea, or yellowish skin or eyes. These symptoms may indicate that there is a possible liver problem that could be serious.

For some patients, buprenorphine and naloxone can result in a serious allergic reaction. This includes anaphylaxis which may be life-threatening. Patients should contact their doctor immediately or seek emergency medical help if they experience trouble breathing, swallowing or speaking, swelling of the face, hands or mouth while taking this medication, or any rash or itching.

Patients who have been taking buprenorphine and naloxone for more than a few weeks or more should not stop taking this medication without getting the advice of their doctor. This medication may require the patient to slowly reduce the amount of medication they take, instead of stopping suddenly. Stopping this medication suddenly can result in withdrawal symptoms, including sweating, stomach or abdominal cramps, anxiety, nausea, flu like symptoms such as a fever or runny nose, shaking or shivering, or trouble sleeping.

Taking buprenorphine and naloxone while pregnant can result in severe side effects in the fetus. Women patients who are pregnant, or who are considering becoming pregnant, should discuss with their doctor prior to taking this medication.

Patients should avoid taking any medication which they have not discussed with their doctor. This would include any other prescription medication, but also non-prescription or over-the-counter drugs, herbal supplements, vitamins, or other illicit drugs.

Patients who have other medical problems will also need to inform their doctor, and discuss whether or how taking buprenorphine and naloxone will impact their condition. Patients should especially inform their doctor if they have any of the following medical conditions:

  • Adrenal gland problem (Addison disease)
  • Current or past history of alcohol abuse
  • Severe asthma
  • History of brain tumors
  • Breathing problems
  • Chronic obstructive pulmonary disease (COPD)
  • Central nervous system (CNS) depression
  • Serious heart condition
  • Current or history of drug dependence, especially narcotics
  • Enlarged prostate
  • Gallstones or gallbladder disease
  • History of head injuries
  • Current or history of Heart disease
  • History of hepatitis B or C
  • Hypothyroidism (which is underactive thyroid)
  • Low blood volume (hypovolemia)
  • Curvature of the spine with breathing problems
  • Current or history of mental illness
  • Difficulty passing urine (may result in serious side effects)
  • Low blood pressure
  • Respiratory issues, such as very slow breathing (can cause worsening of this condition)
  • Kidney disease
  • Moderate liver disease (can increase side effects)
  • Severe liver disease (not recommended for patients who have this condition)

Storage:

This medication should be kept in a tightly closed container, and kept at room temperature at all times. Store away from moisture or humidity, heat or direct light. Avoid freeing this medication.

Buprenorphine and naloxone should always be kept out of the reach of children.

As with all medications, this medication should be disposed of when no longer needed, or after expiration. For disposal information contact a local healthcare or law enforcement professional.

Summary

Buprenorphine and naloxone are drugs used to help adult individuals who are addicted to or dependent on narcotics to withdraw from those drugs without suffering the severe symptoms. Buprenorphine and naloxone is available by prescription only, and comes in the form of tablet or film, which is placed in the mouth or under the tongue. Once placed, it dissolves, allowing the medication to be absorbed into the bloodstream. Buprenorphine and naloxone combined works to prevent the patient's central nervous system from reacting in severe ways, and permits the gradual withdrawal from the drug causing the addiction.

As an opioid, buprenorphine and naloxone can cause serious side effects, including addiction, overdose and even death. In order to avoid the worst side effects, patients should always follow their doctor's instructions, and take only the dose prescribed. Certain side effects can be uncomfortable but are not life threatening, and will resolve as the body becomes used to taking the medication.

Patients who are seeking to become free of their addiction to or dependence on narcotic drugs may find that buprenorphine and naloxone can help them reach that goal with the supervision of a doctor.

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Last Reviewed:
December 24, 2017
Last Updated:
April 02, 2018