buprenorphine and naloxone

Generic Name: buprenorphine and naloxone (byoo PREH nor feen and NAH lox own)
Brand Names: Suboxone

What is buprenorphine and naloxone?

Buprenorphine is an opioid medication. Buprenorphine is similar to other opioids such as morphine, codeine, and heroin however, it produces less euphoric ("high") effects and therefore may be easier to stop taking.

Naloxone blocks the effects of opioids such as morphine, codeine, and heroin. If buprenorphine and naloxone is injected, naloxone will block the effects of buprenorphine and lead to withdrawal symptoms in a person with an opioid addiction. When administered under the tongue as directed, naloxone will not affect the actions of buprenorphine.

Buprenorphine and naloxone is used to treat opiate addiction.

Buprenorphine and naloxone may also be used for purposes other than those listed in this medication guide.

What is the most important information I should know about buprenorphine and naloxone?

Buprenorphine and naloxone can cause death from overdose, especially if it is injected with a tranquilizer. Use buprenorphine and naloxone exactly as directed by your doctor.

Buprenorphine and naloxone can cause drug dependence. This means that withdrawal symptoms may occur if you stop using the medicine too quickly. Withdrawal symptoms may also occur at the start of treatment due to dependence on another drug. Buprenorphine and naloxone is not for occasional ("as needed") use. Do not stop taking buprenorphine and naloxone without first talking to your doctor. Your doctor may want to gradually reduce the dose to avoid or minimize withdrawal symptoms.

In an emergency, have family members tell emergency room staff that you are taking buprenorphine and naloxone and that you are dependent on opioids.

Use caution when driving, operating machinery, or performing other hazardous activities. Buprenorphine and naloxone may cause drowsiness, dizziness, or impaired thinking. If you experience drowsiness, dizziness, or impaired thinking, avoid these activities. Avoid alcohol while taking buprenorphine and naloxone. Alcohol may dangerously increase drowsiness and dizziness caused by the medication.

Buprenorphine and naloxone may dangerously increase the effects of other drugs that cause drowsiness, including antidepressants, alcohol, antihistamines, sedatives (used to treat insomnia), other pain relievers, anxiety medicines, and muscle relaxants. Tell your doctor about all medicines that you are taking, and do not take any other prescription or over-the-counter medicine, including herbal products, without first talking to your doctor.

What should I discuss with my healthcare provider before taking buprenorphine and naloxone?

Do not take buprenorphine and naloxone if:

• the medication was not prescribed for you; or

• you are allergic to buprenorphine, naloxone, or any components of the tablets.

Before taking buprenorphine and naloxone, tell your doctor if you have:

• lung problems or difficulty breathing;

• a head injury or brain problem;

• liver problems;
• kidney problems;

• gallbladder problems;

• adrenal gland problems, such as Addison's disease;

• low thyroid (hypothyroidism);

• enlarged prostate gland;

• problems urinating;

• a curve in the spine that affects breathing;

• severe mental problems or hallucinations (seeing or hearing thing that are not really there); or

• alcoholism.

You may not be able to take buprenorphine and naloxone, or you may require a dosage adjustment or special monitoring during treatment if you have any of the conditions listed above.

Buprenorphine and naloxone is in the FDA pregnancy category C. This means that it is not known whether buprenorphine and naloxone will be harmful to an unborn baby. Use of buprenorphine and naloxone during pregnancy may cause withdrawal symptoms in a newborn baby. Do not take buprenorphine and naloxone if you are pregnant or could become pregnant during treatment. Buprenorphine and naloxone passes into breast milk and may be harmful to a nursing baby. Do not take buprenorphine and naloxone if you are breast-feeding a baby.

How should I take buprenorphine and naloxone?

Take buprenorphine and naloxone exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.

The buprenorphine and naloxone tablets should be placed under the tongue and allowed to dissolve. This will take 2 to 10 minutes. If more than one tablet is prescribed per dose, your doctor may tell you to put all of the tablets under your tongue at the same time, or put 2 tablets under your tongue and allow them to dissolve completely, then put the next tablet or tablets under the tongue right away.

Do not chew or swallow the tablets. The medicine will not work this way and you may get withdrawal symptoms. Do not change the dose of buprenorphine and naloxone or take it more often than prescribed without first talking to your doctor. Do not inject ("shoot-up") buprenorphine and naloxone. Shooting-up is dangerous and may cause bad withdrawal symptoms.

Buprenorphine and naloxone may cause withdrawal symptoms if taken too soon after a dose of heroin, morphine, or methadone.

Buprenorphine and naloxone can cause drug dependence. This means that withdrawal symptoms may occur if you stop using the medicine too quickly. Withdrawal symptoms may also occur at the start of treatment due to dependence on another drug. Buprenorphine and naloxone is not for occasional ("as needed") use. Do not stop taking buprenorphine and naloxone without first talking to your doctor. Your doctor may want to gradually reduce the dose to avoid or minimize withdrawal symptoms.

When treatment with buprenorphine and naloxone is completed, flush any unused tablets down the toilet.

Buprenorphine and naloxone can cause constipation. Drink plenty of water (six to eight full glasses a day) to lessen this side effect. Increasing the amount of fiber in your diet can also help to alleviate constipation.

Your doctor may want to perform blood tests or other forms of monitoring during treatment with buprenorphine and naloxone.

Store buprenorphine and naloxone at room temperature away from moisture and heat. Buprenorphine and naloxone may be a target for people who abuse prescription or street drugs. Therefore, keep the tablets in a safe place to protect them from theft. Never give them to anyone else. Sell or giving away this medicine is against the law.

What happens if I miss a dose?

Take the missed dose as soon as you remember. If it is almost time for the next dose, skip the missed dose and take only the next regularly scheduled dose. Do not take a double dose of this medication.

What happens if I overdose?

Seek emergency medical attention.

Symptoms of a buprenorphine and naloxone overdose may include slow breathing, seizures, dizziness, weakness, loss of consciousness, coma, confusion, tiredness, cold and clammy skin, and small pupils.

What should I avoid while taking buprenorphine and naloxone?

In an emergency, have family members tell emergency room staff that you are taking buprenorphine and naloxone and that you are dependent on opioids.

Use caution when driving, operating machinery, or performing other hazardous activities. Buprenorphine and naloxone may cause drowsiness, dizziness, or impaired thinking. If you experience drowsiness, dizziness, or impaired thinking, avoid these activities.

Dizziness may be more likely to occur when rising from a sitting or lying position. Rise slowly to minimize dizziness and prevent a fall.

Avoid alcohol while taking buprenorphine and naloxone. Alcohol may dangerously increase drowsiness and dizziness caused by the medication.

Buprenorphine and naloxone may dangerously increase the effects of other drugs that cause drowsiness, including antidepressants, alcohol, antihistamines, sedatives (used to treat insomnia), other pain relievers, anxiety medicines, and muscle relaxants. Tell your doctor about all medicines that you are taking, and do not take any other prescription or over-the-counter medicine, including herbal products, without first talking to your doctor.

Buprenorphine and naloxone side effects

Buprenorphine and naloxone can cause drug dependence. This means that withdrawal symptoms may occur if you stop using the medicine too quickly. Withdrawal symptoms may also occur at the start of treatment due to dependence on another drug. Buprenorphine and naloxone is not for occasional ("as needed") use. Do not stop taking buprenorphine and naloxone without first talking to your doctor. Your doctor may want to gradually reduce the dose to avoid or minimize withdrawal symptoms. Seek emergency medical attention or contact your doctor immediately if you experience any of the following serious side effects:

• an allergic reaction (difficulty breathing; closing of the throat, swelling of the lips, tongue, or face; or hives);

• slow breathing;

• dizziness or confusion; or

• liver problems such as yellowing of the skin or eyes, dark colored urine, light colored stools (bowel movements), decreased appetite for several days or longer, nausea, or lower stomach pain.

Other less serious side effects may be more likely to occur. Continue to take buprenorphine and naloxone and talk to your doctor if you experience

• headache;

• pain;

• problems sleeping;

• nausea;

• sweating;

• stomach pain; or

• constipation.

Side effects other than those listed here may also occur. Talk to your doctor about any side effect that seems unusual or that is especially bothersome. You may report side effects to FDA at 1-800-FDA-1088.

See also: buprenorphine and naloxone side effects (in more detail)

Buprenorphine and naloxone Dosing Information

Usual Adult Dose for Opiate Dependence:

Sublingual tablets:
Initial dose: 8 mg on day 1.
Maintenance dose: Rapidly titrate to the recommended target dose of 16 mg/day. In clinical trials, patients received 8 mg on day 1 and 16 mg on day 2 and thereafter. Further dose adjustments may be made in 2 mg to 4 mg increments up to a level that suppresses opioid withdrawal symptoms and holds the patient in treatment. The usual daily range is 4 mg to 24 mg.

The tablets should be placed under the tongue at the same time and allowed to dissolve. If patients are taking more than 2 tablets per dose and cannot hold more than 2 under the tongue comfortably, they should use 2 tablets at a time, allowing them to dissolve completely before taking more tablets.

For patients taking heroin or short-acting opioids, the first dose should be administered at least 4 hours after the patient last used opioids or preferably when early withdrawal symptoms appear.

Withdrawal symptoms may occur during buprenorphine induction treatment of patients taking methadone or long-acting opioids, especially high opioid doses or when buprenorphine is administered shortly after the last opioid dose. The optimal time for the first dose has not been reported.

The optimal method of tapering to discontinuation has not been reported.

Sublingual film: Initial dose: Buprenorphine/naloxone sublingual film should be used in patients who have been initially inducted using buprenorphine sublingual tablets. Buprenorphine/naloxone sublingual film is administered sublingually as a single daily dose. The sublingual film should be placed under the tongue. If an additional sublingual film is necessary to achieve the prescribed dose, place the additional sublingual film sublingually on the opposite side from the first film. The sublingual film should be placed in a manner to minimize overlapping as much as possible. The sublingual film must be kept under the tongue until the film is completely dissolved. Buprenorphine/naloxone sublingual film should not be chewed, swallowed, or moved after placement.
Maintenance: Buprenorphine/naloxone sublingual film is indicated for maintenance treatment. The recommended target dosage of buprenorphine/naloxone sublingual film is 16/4 mg buprenorphine/naloxone/day as a single daily dose.

The dosage of buprenorphine/naloxone sublingual film should be progressively adjusted in increments/decrements of 2/0.5 mg or 4/1 mg buprenorphine/naloxone to a level that holds the patient in treatment and suppresses opioid withdrawal signs and symptoms.

The maintenance dose of buprenorphine/naloxone sublingual film is generally in the range of 4/1 mg buprenorphine/naloxone to 24/6 mg buprenorphine/naloxone per day depending on the individual patient. Dosages higher than this have not been demonstrated to provide any clinical advantage.

What other drugs will affect buprenorphine and naloxone?

Buprenorphine and naloxone can cause death from overdose, especially if it is injected with a tranquilizer. Use buprenorphine and naloxone exactly as directed by your doctor.

Do not take buprenorphine and naloxone without first talking to your doctor if you are taking:

• a benzodiazepine such as alprazolam (Xanax), diazepam (Valium), clonazepam (Klonopin), clorazepate (Tranxene), lorazepam (Ativan), chlordiazepoxide (Librium), oxazepam (Serax), triazolam (Halcion), temazepam (Restoril), estazolam (Prosom), quazepam (Doral), or flurazepam (Dalmane);

• erythromycin (Ery-Tab, E.E.S., E-Mycin, others) or clarithromycin (Biaxin);

• itraconazole (Sporanox) or ketoconazole (Nizoral);

• an HIV protease inhibitor such as indinavir (Crixivan), ritonavir (Norvir) or saquinavir (Fortovase, Invirase);

• rifampin (Rifadin, Rimactane), rifapentine (Priftin), or rifabutin (Mycobutin);

• phenytoin (Dilantin);

• carbamazepine (Tegretol);

• a barbiturate such as phenobarbital, mephobarbital (Mebaral), and others.

You may not be able to take buprenorphine and naloxone, or you may require a dosage adjustment or special monitoring during treatment if you are taking any of the medications listed above.

Buprenorphine and naloxone may dangerously increase the effects of other drugs that cause drowsiness, including antidepressants, alcohol, antihistamines, sedatives (used to treat insomnia), other pain relievers, anxiety medicines, and muscle relaxants. Tell your doctor about all medicines that you are taking, and do not take any other prescription or over-the-counter medicine, including herbal products, without first talking to your doctor.

Drugs other than those listed here may also interact with buprenorphine and naloxone. Talk to your doctor and pharmacist before taking any prescription or over-the-counter medicines, including herbal products.

Where can I get more information?

• Your pharmacist may have additional information about buprenorphine and naloxone written for health professionals that you may read.