What is Buprenex?

Buprenex is a brand-name prescription medication. It's used to treat pain so severe that it requires a powerful type of pain reliever called an opioid. Before you take Buprenex, you must have already tried other pain treatments that didn't help you.

Buprenex contains the drug buprenorphine, which is a type of opioid. Buprenex belongs to a group of drugs called partial opioid agonists. Compared to other opioids, Buprenex has a lower risk of addiction or misuse.

Buprenex is approved for use in adults and children ages 2 to 12 years.

Buprenex can be given in two different ways. A healthcare provider may give you the drug as an injection into your muscle (intramuscular). Or they may give you Buprenex as an injection into your vein (intravenous, which is also called IV).

Effectiveness

Clinical studies looked at how well Buprenex eased pain compared to morphine, an opioid drug. Buprenex and morphine were similarly effective in helping ease pain.

Is Buprenex a controlled substance?

Yes, Buprenex is a controlled substance. This is a type of drug that has high risks of misuse and becoming dependent on using it.

Due to these risks, the U.S. government monitors the use of controlled substances. They put each drug into a category (group) based on its risk of being misused. These categories range from Schedule I to Schedule V. Schedule I drugs have the highest risk of misuse, and Schedule V drugs have the lowest risk. Buprenex is a Schedule III drug.

Buprenex generic

Buprenex is a brand-name medication. Buprenex is also available in generic versions.

The generics are medications that contain buprenorphine, which is the same drug that's in Buprenex. The generics are exact copies of Buprenex. But generics often cost less than the brand-name versions and are made by different companies.

If you have questions about generic versions of Buprenex, ask your doctor.

Buprenex and naloxone

Taking Buprenex may put you at risk for becoming addicted to the drug, abusing it, or misusing it.* But taking a medication called naloxone may help.

Naloxone can be used to reverse the symptoms of an overdose of Buprenex. (An overdose can occur when you've taken too much of a drug.)

Naloxone is also used with buprenorphine, the active drug in Buprenex, to help treat opioid dependence. (Opioid dependence means that you need an opioid drug to function well.) Combination products that contain naloxone and buprenorphine include:

  • Zubsolv, which is a tablet that you place under your tongue (sublingual)
  • Bunavail, which is a film that you place inside your cheek (buccal)

You keep the tablet or film in your mouth until it dissolves.

Naloxone, Zubsolv, and Bunavail can be used in or out of the hospital. But you shouldn't use the medications without your doctor's approval.

If you think you're dependent on Buprenex or have taken too much of the drug, tell your doctor right away. They can decide what treatment is best for you.

* Buprenex has a boxed warning for addiction and misuse. This is the most serious warning from the Food and Drug Administration (FDA). For more information, see "FDA warnings" at the beginning of this article.

Buprenex interactions

Buprenex can interact with several other medications. It can also interact with certain supplements as well as certain foods.

Different interactions can cause different effects. For instance, some interactions can interfere with how well a drug works. Other interactions can increase the number of side effects or make them more severe.

Buprenex and other medications

Below is a list of medications that can interact with Buprenex. This list doesn't contain all drugs that may interact with Buprenex.

Before taking Buprenex, talk with your doctor and pharmacist. Tell them about all prescription, over-the-counter, and other drugs you take. Also tell them about any vitamins, herbs, and supplements you use. Sharing this information can help you avoid potential interactions.

If you have questions about drug interactions that may affect you, ask your doctor or pharmacist.

Drugs that can increase or decrease levels of Buprenex

Taking Buprenex with medications called CYP3A4 inhibitors or CYP3A4 inducers can increase or decrease levels of Buprenex in your body.

CYP3A4 inhibitors

CYP3A4 is a protein that helps break down Buprenex so it can leave your body. This helps prevent levels of Buprenex from getting too high, which can be dangerous.

Some medications called CYP3A4 inhibitors can slow down how quickly CYP3A4 breaks down Buprenex. So CYP3A4 inhibitors may lead to high amounts of Buprenex in your body. This increases your risk for side effects, including sedation (feeling drowsy and less alert) and nausea.

Some examples of CYP3A4 inhibitors include:

  • erythromycin (Erygel, Eryped)
  • ketoconazole
  • delavirdine
  • nelfinavir (Viracept)
  • ritonavir (Norvir)

CYP3A4 inducers

Other medications called CYP3A4 inducers can increase how quickly CYP3A4 breaks down Buprenex. So CYP3A4 inducers can reduce the amount of Buprenex in your body. This can decrease how well Buprenex works in your body.

Some examples of CYP3A4 inducers include:

  • rifampin (Rimactane, Rifadin)
  • carbamazepine (Tegretol, Tegretol XR, Epitol)
  • phenytoin (Phenytek, Dilantin)
  • efavirenz (Sustiva)
  • nevirapine (Viramune)
  • etravirine (Intelence)

If you're taking a CYP3A4 inhibitor, a CYP3A4 inducer, or aren't sure, talk with your doctor. They can help you decide whether Buprenex is right for you.

Buprenex and benzodiazepines or other central nervous system depressants

Taking Buprenex with central nervous system (CNS) depressants* can lead you to have serious side effects. These include severe sedation (feeling drowsy and less alert), respiratory depression (slowed breathing), coma, or even death.

Your CNS is made up of your brain and spinal cord. Some substances called CNS depressants can slow down your CNS. So taking Buprenex with CNS depressants can make your CNS less able to send messages to your body.

Examples of CNS depressants include:

  • benzodiazepines,* a class of drugs used for seizures or anxiety, and as tranquilizers. Examples of benzodiazepines include:
    • diazepam (Valium)
    • lorazepam (Ativan)
    • clonazepam (Klonopin)
    • sedatives (sleep drugs) such as eszopiclone (Lunesta)
    • muscle relaxants such as dantrolene (Dantrium)
    • general anesthetics such as amobarbital (Amytal)
    • antipsychotics such as clozapine (Clozaril)
    • alcohol

Because Buprenex and CNS depressants may make you tired, it could be dangerous to drive or operate machinery while taking the medications. Until you're certain that Buprenex isn't making you tired, avoid such activities.

Before you take Buprenex, tell your doctor if you're using a CNS depressant. They'll try to limit your dosage of the CNS depressant and monitor you during your Buprenex treatment.

* Buprenex has a boxed warning for benzodiazepines and other CNS depressants. This is the most serious warning from the Food and Drug Administration (FDA). For more information, see "FDA warnings" at the beginning of this article.

Buprenex and serotoninergic drugs

Taking Buprenex with serotoninergic drugs can lead to very high amounts of serotonin in your body.

Serotonin is a chemical that helps your brain work properly. Medications called serotoninergic drugs increase the amount of serotonin in your body.

Buprenex can also increase how much serotonin is in your body. So taking Buprenex together with serotoninergic drugs can lead to very high amounts of serotonin. This can be dangerous and cause very serious side effects, including breathing problems and coma.

Examples of some of the most common serotoninergic drugs include:

  • selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine (Prozac)
  • serotonin and norepinephrine reuptake inhibitors (SNRIs) such as duloxetine (Cymbalta)
  • tricyclic antidepressants such as desipramine (Norpramin)
  • triptans such as almotriptan (Axert)
  • monoamine oxidase inhibitors (MAOIs) such as phenelzine (Nardil), tranylcypromine (Parnate), and linezolid (Zyvox)
  • other drugs that affect serotonin such as mirtazapine (Remeron), trazodone (Oleptro), ondansetron (Zofran), and tramadol (Ultram)

Before you take Buprenex, tell your doctor if you're taking a serotoninergic drug. They may monitor you more closely or switch you to a different medication to help treat your pain.

Buprenex and partial opioid agonists

Taking Buprenex with partial opioid agonists may reduce how well Buprenex works in your body. In severe cases, this can cause symptoms of opioid withdrawal.

Buprenex itself is a partial opioid agonist. The effects of these medications level off (stop increasing) at higher doses. So if you take Buprenex with another partial opioid agonist, you won't get the full effect of either drug.

An example of a partial agonist opioid is pentazocine (Talwin).

Before you start taking Buprenex, talk with your doctor. Tell them if you're taking a partial agonist opioid or if you're unsure. You and your doctor can discuss whether Buprenex is right for you.

Buprenex and mixed agonist/antagonist opioids

Taking Buprenex with mixed opioids may reduce how well Buprenex works in your body. In severe cases, this can cause symptoms of opioid withdrawal.

Mixed opioids might block the effects of opioids in your body. So if you take Buprenex with a mixed opioid, the effects of the two drugs might cancel each other out.

Examples of mixed opioids include butorphanol (Stadol) and nalbuphine (Nubain).

Before you start taking Buprenex, talk with your doctor. Tell them if you're taking a mixed opioid or if you're unsure. You and your doctor can discuss whether Buprenex is right for you.

Buprenex and diuretics

Diuretics are medications that tell your body to release more water. These drugs help your body get rid of excess fluid that can be harmful to you. Buprenex, on the other hand, affects a hormone that tells your body to hold on to water. Therefore, Buprenex can make diuretics less effective.

Examples of diuretics include:

  • eplerenone (Inspra)
  • furosemide (Lasix)

Before you take Buprenex, tell your doctor if you're taking a diuretic. They can help you decide whether Buprenex is right for you.

Buprenex and anticholinergics

Anticholinergic drugs can cause side effects such as severe constipation or problems urinating. Opioids like Buprenex may cause similar side effects. So taking Buprenex with an anticholinergic can increase your risk for serious side effects.

Examples of these anticholinergics include:

  • diphenhydramine (Benadryl)
  • oxybutynin (Ditropan)

Before you take Buprenex, tell your doctor if you're taking an anticholinergic. They may monitor you more closely for side effects.

Buprenex and herbs and supplements

Some herbs or supplements may change the amount of Buprenex in your body. Or they may cause similar effects to Buprenex, increasing your risk for side effects. Examples of these herbs and supplements include:

Before you use Buprenex, tell your doctor if you're taking any herbs or supplements. They can see if they're safe for you to take.

Buprenex dosage

The Buprenex dosage your doctor prescribes will depend on several factors. These include:

  • the type and severity of the pain you're having
  • your clinical history, including previous pain medication
  • your age
  • other medical conditions you may have

Typically, your doctor will start you on a low dosage. Then they'll adjust it over time to reach the amount that's right for you. Your doctor will ultimately prescribe the smallest dosage that provides the desired effect.

The following information describes dosages that are commonly used or recommended. However, be sure to take the dosage your doctor prescribes for you. Your doctor will determine the best dosage to suit your needs.

Drug forms and strengths

Buprenex comes in a vial that contains the drug in a liquid form. Buprenex only comes in one strength: 0.3 mg/mL.

Buprenex can be given in two different ways. A healthcare provider may give you the drug as an injection into your muscle (intramuscular). Or they may give you Buprenex as an injection into your vein (intravenous, which is also called IV). Your doctor will decide which type of injection is right for you based on your condition and other medications you're taking.

In people older than age 12 years, Buprenex is usually first given as a 1-mL injection. It contains 0.3 mg of Buprenex.

If your pain doesn't go away, you may receive a second dose of Buprenex. The healthcare provider will wait 30 to 60 minutes after your first dose. The amount of the injection may vary based on your pain. But the second dose shouldn't contain more than 1 mL (0.3 mg) of Buprenex.

Your doctor may want you to take more Buprenex if your pain doesn't go away. Adults with severe pain may receive up to 2 mL (0.6 mg) for each dose.

Pediatric dosage

The recommended dosage for children ages 2 to 12 years is 2 to 6 micrograms per kilogram (mcg/kg) of body weight. This means that the dosage depends on how much your child weighs.

For example, the maximum dose for a 3-year-old child who weighs 31 pounds (14 kg) would be 84 mcg (14 kg x 6 mcg). This dose would be given as one injection.

If the child's pain doesn't go away after the first dose, the healthcare provider may give additional injections of Buprenex. There should be four to six hours between doses. But sometimes the healthcare provider may wait six to eight hours between doses. This depends on how the child responds to Buprenex.

What if I miss a dose?

If you miss an appointment to have an injection of Buprenex, call your doctor to reschedule.

To help make sure that you don't miss a dose, write your treatment schedule in a calendar. You can also set reminders on your phone.

Will I need to use this drug long term?

No. Buprenex is a medication that you take only while you're at a hospital or clinic.

A healthcare provider will give you Buprenex to reduce sudden episodes of pain. Once your pain and your medical condition improve, you'll be sent home. If you have pain at home, your doctor may prescribe a different medication to help treat your pain.

Buprenex vs. methadone

You may wonder how Buprenex compares to other medications that are prescribed for similar uses. Here we look at how Buprenex and methadone are alike and different.

Uses

The Food and Drug Administration (FDA) has approved both Buprenex and methadone to treat pain. Before taking either drug, you must have already tried other pain treatments that didn't help you.

Buprenex is used to treat pain so severe that you need to take a powerful type of pain reliever called an opioid.

Methadone is used to treat moderate to severe pain. The drug can also be used to treat opioid dependence in people who cannot receive oral medication to treat their opioid dependence. (Opioid dependence means that you need an opioid drug to function.)

Buprenex contains the drug buprenorphine. Methadone contains the drug methadone. Buprenex and methadone belong to the same class of drugs called opioids. (A class of drugs is a group of medications that work in a similar way.) Both Buprenex and methadone have similar effects in the body.

Buprenex and methadone are both controlled substances. (See "Is Buprenex a controlled substance?" in the "What is Buprenex?" section above to learn more.) Both Buprenex and methadone may put you at risk for becoming addicted to them, abusing them, or misusing them.*

* Buprenex and methadone have boxed warnings for addiction and misuse. This is the most serious warning from the Food and Drug Administration (FDA). For more information, see "FDA warnings" at the beginning of this article.

Use in children

Buprenex is approved for use in children ages 2 to 12 years. The use of methadone in children younger than age 18 years isn't recommended.

Drug forms and administration

Both Buprenex and methadone come in vials that contain the drug in a liquid form. Buprenex is available in one strength: 0.3 mg/mL. Methadone is available in two strengths: 10 mg/1 mL and 200 mg/20 mL.

Buprenex can be given in two different ways. A healthcare provider may give you the drug as an injection into your muscle (intramuscular). Or they may give you Buprenex as an injection into your vein (intravenous, which is also called IV). Your doctor will decide which type of injection is right for you based on your condition and other medications you're taking.

Methadone can be given in three different ways. As with Buprenex, a healthcare professional may give you methadone as an injection into your muscle or vein. But they may also give you the drug as an injection under your skin (subcutaneous). If you have opioid dependence, you'll usually receive methadone through injections into your veins. (Dependence means you need the drug to function well.)

Side effects and risks

Buprenex and methadone have similar effects in the body. Therefore, both medications can cause very similar side effects. Below are examples of these side effects.

More common side effects

These lists contain examples of more common side effects that can occur with Buprenex, with methadone, or with both drugs (when taken individually).

  • Can occur with Buprenex:
    • vertigo (feeling a loss of balance)
    • headache
  • Can occur with methadone:
    • weight gain
  • Can occur with both Buprenex and methadone:
    • sedation (feeling drowsy and less alert)
    • dizziness
    • headache
    • nausea
    • vomiting
    • increased sweating

Serious side effects

These lists contain examples of serious side effects that can occur with Buprenex, with methadone, or with both drugs (when taken individually).

  • Can occur with Buprenex:
    • few unique serious side effects
  • Can occur with methadone:
  • Can occur with both Buprenex and methadone:
    • severe constipation
    • allergic reaction
    • serotonin syndrome (high levels of the chemical serotonin)
    • shock (your blood doesn't reach your organs)
    • life-threatening respiratory depression*
* Buprenex and methadone have boxed warnings for life-threatening respiratory depression. This is the most serious warning from the Food and Drug Administration (FDA). For more information, see "FDA warnings" at the beginning of this article.

Effectiveness

These drugs haven't been directly compared in clinical studies, but studies have found both Buprenex and methadone to be effective for treating severe pain.

Costs

Buprenex is a brand-name drug. Generic forms of Buprenex also available. Methadone is a generic drug. Generics are usually cheaper than brand-name medications.

According to estimates on GoodRx.com, Buprenex costs more than methadone. The actual price you'll pay for either drug depends on your insurance plan and your location.

Buprenex withdrawal

If you stop taking Buprenex suddenly, you may have withdrawal symptoms. These withdrawal symptoms include:

  • feeling restless
  • watery eyes
  • excess mucus in your nose
  • yawning more than often
  • excessive sweating
  • chills
  • pain in your muscles
  • pupils that are larger than usual
  • feeling irritable
  • anxiety
  • pain in your back or joints
  • weakness
  • abdominal (belly) cramps
  • insomnia (trouble sleeping)
  • nausea
  • anorexia
  • vomiting
  • diarrhea
  • increased blood pressure
  • increased breathing rate
  • increased heart rate

Call your doctor if you're having symptoms of withdrawal that are severe or that don't go away. They can recommend treatments to ease your symptoms.

Note: For more information on how to treat withdrawal symptoms, read the "Buprenex and naloxone" section above.

Withdrawal symptoms in babies

If you take Buprenex for a long time when you're pregnant, your baby may have neonatal opioid withdrawal syndrome.* This is a condition in which your baby is born with opioid withdrawal symptoms. If not treated, neonatal opioid withdrawal syndrome can be life-threatening.

Symptoms of neonatal opioid withdrawal syndrome include:

  • being fussy
  • crying much more than usual
  • muscles that twitch or seem tight
  • sweating
  • unusual sleeping patterns
  • high-pitched cry
  • tremors
  • vomiting
  • diarrhea
  • trouble feeding or not being able to gain weight
  • fever
  • seizures

If you took Buprenex while pregnant and your baby has any of these symptoms, call your doctor right away.

* Buprenex has a boxed warning for neonatal opioid withdrawal syndrome. This is the most serious warning from the Food and Drug Administration (FDA). For more information, see "FDA warnings" at the beginning of this article.

Buprenex uses

The Food and Drug Administration (FDA) approves prescription drugs such as Buprenex to treat certain conditions. Buprenex may also be used off-label for other conditions. Off-label use is when a drug that's approved to treat one condition is used to treat a different condition.

Buprenex for pain treatment

Buprenex is used to treat pain so severe that you need to take a powerful type of pain reliever called an opioid. Also, before you receive Buprenex, you must have already tried other pain treatments that didn't help you.

Buprenex can be given in two different ways. A healthcare provider may give you the drug as an injection into your muscle (intramuscular). Or they may give you Buprenex as an injection into your vein (intravenous, which is also called IV). Your doctor will decide which type of injection is right for you based on your condition and other medications you're taking. You'll receive Buprenex in a hospital or a clinic.

In clinical studies, Buprenex was effective in helping ease severe pain. Researchers looked at how well Buprenex eased pain compared to morphine, an opioid drug. Buprenex and morphine were similarly effective in helping ease pain.

Buprenex for children

Buprenex can be used to treat severe pain in children ages 2 to 12 years.

In clinical studies, 960 children ages 9 months to 18 years received Buprenex. The effectiveness of Buprenex in these children was similar to that of adults who took it.

Buprenex overdose

Using more than the recommended dosage of Buprenex can lead to serious side effects.

Overdose symptoms

Symptoms of an overdose can include:

What to do in case of overdose

If you think you've taken too much of this drug, call your doctor. You can also call the American Association of Poison Control Centers at 800-222-1222 or use their online tool. But if your symptoms are severe, call 911 or go to the nearest emergency room right away.

Your overdose may be treated with a drug called naloxone. (For more information, see "Naloxone: A Lifesaver" below and the "Buprenex and naloxone" section above.)

Naloxone: A lifesaver

Naloxone (Narcan, Evzio) is a drug that can quickly reverse overdoses from opioids, including heroin. An opioid overdose can make it hard to breathe. This can be fatal if not treated in time.

If you or someone you love is at risk for an opioid overdose, talk with your doctor or pharmacist about naloxone. Ask them to explain the signs of an overdose and show you and your loved ones how to use naloxone.

In most states, you can get naloxone at a pharmacy without a prescription. Keep the drug on hand so you can easily access it in case of an overdose.

Buprenex and pregnancy

Clinical studies of pregnant women who took Buprenex suggest that the drug doesn't cause birth defects. But using Buprenex during pregnancy can lead to problems during and after labor. Your baby may have trouble breathing while you're giving birth.

In some cases, babies can develop neonatal opioid withdrawal syndrome.* This is a condition that can occur if you take Buprenex for a long time when you're pregnant. Without treatment, neonatal opioid withdrawal syndrome can be life-threatening.

Animal studies suggest problems during pregnancy and harm to the baby if Buprenex is given to the mother. But studies in animals don't always represent what happens in humans.

If you're pregnant or plan to become pregnant, tell your doctor before you receive Buprenex. They can talk with you about the pros and cons of the medication.

* Buprenex has a boxed warning for neonatal opioid withdrawal syndrome. This is the most serious warning from the Food and Drug Administration (FDA). For more information, see "FDA warnings" at the beginning of this article.

Buprenex and birth control

Buprenex may lead to pregnancy complications. It may also harm your baby during and after birth. Talk to your doctor about your birth control needs while you're using Buprenex.

For more information, please see the "Buprenex and pregnancy" section above.

Buprenex and breastfeeding

Studies looked at pregnant women who took high doses of buprenorphine that you take under your tongue. (Buprenorphine is the active ingredient in Buprenex.) The results showed that the buprenorphine was present in breast milk. But there isn't enough information to say how this would affect a child.

In animal studies, pregnant animals who were given buprenorphine seemed to produce lower levels of breast milk. But animal studies don't always reflect what happens in humans.

If you've been taking Buprenex, it's recommended that you not breastfeed your child. Talk with your doctor about the best ways to feed your child.

Buprenex and alcohol

Taking Buprenex with alcohol* can be dangerous. It can lead to severe sedation (feeling drowsy and less alert), respiratory depression (slowed breathing), coma, or even death.

Alcohol is a type of substance called a central nervous system (CNS) depressant, which can relax your CNS. (Your CNS is made up of your brain and spinal cord.) If your CNS becomes too relaxed, your breathing may become too slow and lead to the problems mentioned above.

If you drink alcohol, talk with your doctor before taking Buprenex. They'll try to limit how much you drink and monitor you during your Buprenex treatment.

* Buprenex has a boxed warning for CNS depressants, including alcohol. This is the most serious warning from the Food and Drug Administration (FDA). For more information, see "FDA warnings" at the beginning of this article.

Buprenex side effects

Buprenex can cause mild or serious side effects. The following lists contain some of the key side effects that may occur while taking Buprenex. These lists don't include all possible side effects.

For more information on the possible side effects of Buprenex, talk with your doctor or pharmacist. They can give you tips on how to deal with any side effects that may be bothersome.

More common side effects

The more common side effects of Buprenex can include:

  • sedation (feeling drowsy and less alert)
  • nausea
  • dizziness
  • headache
  • vertigo (feeling a loss of balance)

Most of these side effects may go away within a few days or a couple of weeks. If they're more severe or don't go away, talk with your doctor or pharmacist.

Serious side effects

Serious side effects from Buprenex aren't common, but they can occur. Call your doctor right away if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you're having a medical emergency.

Serious side effects and their symptoms can include the following:

  • Serotonin syndrome (high levels of a chemical called serotonin). (For symptoms, see "Side effect details" below.)
  • Life-threatening respiratory depression.* (For symptoms, see "Side effect details" below.)
  • Severe constipation. Symptoms can include:
    • fewer than three bowel movements each week
    • hard and dry feces
    • feeling full even after a bowel movement
    • blockage in your large intestine
  • Adrenal gland problems, including low levels of cortisol. Symptoms include:
    • tiredness and fatigue (lack of energy)
    • weak muscles
    • skin that gets darker in color
    • weight loss or lack of appetite
  • Allergic reactions. (For symptoms, see "Side effect details" below.)
  • Shock (your blood doesn't reach your organs). Symptoms include:
    • fast or weak pulse, or the lack of a pulse
    • lightheadedness
    • shallow, fast breathing
    • clammy skin
    • loss of consciousness
* Buprenex has a boxed warningfor life-threatening respiratory depression. This is the most serious warning from the Food and Drug Administration (FDA). For more information, see "FDA warnings" at the beginning of this article.

Side effect details

You may wonder how often certain side effects occur with this drug, or whether certain side effects pertain to it. Here's some detail on some of the side effects this drug may or may not cause.

Allergic reaction

As with most drugs, some people can have an allergic reaction after taking Buprenex. In clinical studies, allergic reactions to Buprenex were rare, but they did occur. Most of these allergic reactions were mild.

Symptoms of a mild allergic reaction can include:

  • rash
  • hives (itchy welts on your skin)
  • itching

A more severe allergic reaction is rare but possible. Symptoms of a severe allergic reaction can include:

  • bronchospasm (wheezing or trouble breathing that gets worse)
  • swelling of the face, lips, or airways
  • anaphylactic shock (sudden drop in blood pressure and trouble breathing)

Severe allergic reactions to Buprenex can be life-threatening. Call your doctor right away if you think you are having a severe allergic reaction to Buprenex. Call 911 if your symptoms feel life-threatening or if you think you're having a medical emergency.

Constipation

If you take Buprenex, you may have constipation. Buprenex can affect the muscles in your colon, preventing waste from moving through your body. This can lead to constipation. If the constipation is severe or doesn't go away, it can lead to other problems. These problems may include blocked intestines or a serious condition called paralytic ileus.

In clinical studies, constipation occurred in less than 1% of people who took Buprenex. Other forms of buprenorphine (the active ingredient in Buprenex) caused constipation in up to 13% of people who took the drug.

If you have constipation for more than three days after taking Buprenex, tell your doctor. They can suggest treatments to help you find relief.

Weight loss

Weight loss may or may not be a side effect of Buprenex. In clinical studies, weight loss didn't occur in any people who took Buprenex. But weight loss has been reported with other forms of buprenorphine (the active ingredient in Buprenex).

If you're concerned about losing weight while taking Buprenex, talk with your doctor. They can give you nutrition advice to help make sure you're at a healthy weight.

Serotonin syndrome

If you take Buprenex, you may develop serotonin syndrome. Serotonin is a chemical that helps your brain work. Buprenex can increase the level of serotonin in your brain.

Serotonin syndrome is rare. But your risk of serotonin syndrome increases if you take Buprenex with other drugs that can increase levels of serotonin. (See "Buprenex interactions" section above to learn more.)

Symptoms of serotonin syndrome may include:

  • feeling confused
  • feeling irritable
  • anxiety
  • muscle spasms (twitches) or stiffness
  • body tremors or shaking
  • fast or abnormal heartbeat
  • nausea that doesn't go away
  • diarrhea that doesn't go away
  • hallucinations (seeing or hearing things that aren't real)
  • increased size of your pupils
  • seizures

If untreated, serotonin syndrome can lead to coma and death.

If you have symptoms of serotonin syndrome, tell your doctor. Call 911 if your symptoms feel life-threatening or if you think you are having an emergency.

Life-threatening respiratory depression

Taking Buprenex can cause a condition called respiratory depression* in which your breathing becomes slow and weak. The condition can be severe, life-threatening, or even fatal. Your doctor will monitor you during your Buprenex treatment, especially when you first take the drug or if they increase your dose.

It's not known how many people have developed respiratory depression after taking Buprenex. But respiratory depression is a known side effect of opioid drugs. According to one study, buprenorphine is less likely to cause respiratory depression than fentanyl, another opioid that's used to treat severe pain. (Buprenorphine is the active ingredient in Buprenex.)

Respiratory depression is more common in people who have breathing problems such as chronic obstructive pulmonary disease (COPD), are elderly, or are very ill.

Symptoms of respiratory depression can include:

  • feeling tired or sleepy during the day
  • shortness of breath
  • shallow or slow breathing
  • feeling confused or depressed
  • headaches that don't go away
  • seizures
  • pale or blue skin, especially in your fingers, toes, or lips

Because of these symptoms, it could be dangerous to drive or operate machinery while taking Buprenex. Until you're certain that Buprenex isn't causing these symptoms, avoid such activities.

If you have symptoms of respiratory depression, tell your doctor. Call 911 if your symptoms feel life-threatening or you think you are having an emergency.

* Buprenex has a boxed warning for life-threatening respiratory depression. This is the most serious warning from the Food and Drug Administration (FDA). For more information, see "FDA warnings" at the beginning of this article.

Side effects in children

Buprenex is approved for use in adults and children ages 2 to 12 years. The side effects in children are similar to those in adults.

Alternatives to Buprenex

Other drugs are available that can treat pain. Some may be better suited for you than others.

Examples of other drugs that may be used to treat severe pain include:

  • morphine (Arymo ER, Kadian, MorphaBond ER, MS Contin)
  • hydrocodone (Hysingla ER, Zohydro ER)
  • hydromorphone (Dilaudid, Exalgo)
  • oxycodone (Oxaydo, OxyContin, OxyFast, Roxicodone, Xtampza ER)
  • fentanyl (Duragesic)
  • meperidine (Demerol)
  • methadone (Dolophine, Methadose, Methadose Sugar-Free, Methadone Diskets)
  • tramadol (ConZip, Ultram, Ultram ER)
  • levorphanol (Levo-Dromoran)
  • oxymorphone (Opana, Opana ER, Numorphan HCl)
  • pentazocine (Talwin)
  • tapentadol (Nucynta, Nucynta ER)
  • butorphanol (Stadol)
  • nalbuphine (Nubain)

If you're interested in finding an alternative to Buprenex, talk with your doctor. They can tell you about other medications that may work well for you.

Buprenex vs. Butrans

You may wonder how Buprenex compares to other medications that are prescribed for similar uses. Here we look at how Buprenex and Butrans are alike and different.

Uses

The Food and Drug Administration (FDA) has approved both Buprenex and Butrans to treat severe pain. Both drugs are for people who have tried other pain treatments that didn't help them. However, only Butrans is for people who need to take pain medication for a long time.

Both Buprenex and Butrans contain the drug buprenorphine, so the two medications have the same effect on your body.

Buprenex and Butrans are controlled substances. (See "Is Buprenex a controlled substance?" in the "What is Buprenex?" section above to learn more.) Both Buprenex and Butrans may put you at risk for becoming addicted to them, abusing them, or misusing them.*

Buprenex is approved for use in children ages 2 to 12 years. Butrans isn't approved for use children younger than age 18 years.

* Buprenex and Butrans have boxed warnings for addiction and misuse. This is the most serious warning from the Food and Drug Administration (FDA). For more information, see "FDA warnings" at the beginning of this article.

Drug forms and administration

Buprenex comes as a vial that contains the drug in a liquid form. Buprenex only comes in one strength: 0.3 mg/mL.

Buprenex can be given in two different ways. A healthcare provider may give you the drug as an injection into your muscle (intramuscular). Or they may give you Buprenex as an injection into your vein (intravenous, which is also called IV). Your doctor will decide which type of injection is right for you based on your condition and other medications you're taking.

Butrans comes as a transdermal patch that you apply to your skin. Your body absorbs the medication through the patch. Butrans comes in five different strengths: 5 micrograms (mcg) per hour, 7.5 mcg/hour, 10 mcg/hour, 15 mcg/hour, and 20 mcg/hour.

Side effects and risks

Buprenex and Butrans both contain the drug buprenorphine. Therefore, both medications can cause very similar side effects. Below are examples of these side effects.

More common side effects

These lists contain examples of more common side effects that can occur with Buprenex, with Butrans, or with both drugs (when taken individually).

  • Can occur with Buprenex:
    • few unique common side effects
  • Can occur with Butrans:
    • redness, itchiness, or a rash where you applied the Butrans patch
    • dry mouth
  • Can occur with both Buprenex and Butrans:
    • nausea
    • vomiting
    • dizziness
    • vertigo (feeling a loss of balance)
    • headache
    • sedation (feeling drowsy and less alert)
    • increased sweating

Serious side effects

These lists contain examples of serious side effects that can occur with Buprenex, with Butrans, or with both drugs (when taken individually).

  • Can occur with Buprenex:
    • shock (your blood doesn't reach your organs)
  • Can occur with Butrans:
    • liver problems
  • Can occur with both Buprenex and Butrans:

Effectiveness

Buprenex and Butrans haven't been directly compared in clinical studies, but studies have found both Buprenex and Butrans to be effective for treating people with pain.

Costs

Buprenex and Butrans are both brand-name drugs. There are currently generic forms of both drugs. Generic versions are usually cheaper than brand-name medications.

According to estimates on GoodRx.com, Buprenex and its generic forms generally costs less than Butrans and its generic forms. The actual price you'll pay for either drug will depend on your insurance plan and your location.

Buprenex cost

As with all medications, the cost of Buprenex can vary. To find current prices for Buprenex in your area, check out GoodRx.com:

The cost you find on GoodRx.com is what you may pay without insurance. The actual price you'll pay depends on your insurance plan and your location.

Financial and insurance assistance

The cost of Buprenex may be covered by your health insurance plan. If you have questions about the cost of Buprenex or if you're unsure if it's covered by your insurance plan, call your insurance company.

How Buprenex is given

You'll receive Buprenex in a hospital or a clinic. The drug can be given in two different ways. A healthcare provider may give you Buprenex as an injection into your muscle (intramuscular). Or they may give you the drug as an injection into your vein (intravenous, which is also called IV). Your doctor will decide which type of injection is right for you based on your condition and other medications you're taking.

For an IV injection, the healthcare provider will place a needle in your vein and slowly inject Buprenex. An IV injection of Buprenex can take two minutes or longer.

Once your pain and your medical condition improve, you'll be sent home. If you have pain at home, your doctor may prescribe a different medication to help treat your pain.

How often the drug is given

If your pain doesn't go away after your first dose of Buprenex, you may be given a second injection. The healthcare provider will wait 30 to 60 minutes after your first dose. Your doctor may want you to take more Buprenex if your pain doesn't go away.

How Buprenex works

The feeling of pain is the result of information moving across your body. When your body is hurt, your brain tells those parts of your body that they're injured. As a result, you start feeling pain in those body parts.

Proteins called opioid receptors help regulate how these pain messages move between your body parts and your brain. Buprenex binds to opioid receptors in your brain and spinal cord. This action changes how your body senses pain and helps relieve your symptoms.

How long does it take to work?

When you'll start feeling pain relief depends on how you receive Buprenex. If you receive the drug as an injection into your muscle (intramuscular), it may take up to 15 minutes to feel less pain. The pain relief may last for about six hours.

If you receive Buprenex as an injection into your vein (intravenous, which is also called IV), your pain may ease even sooner. You may have pain relief in less than 15 minutes. The effect will also last for about six hours.

Common questions about Buprenex

Here are answers to some frequently asked questions about Buprenex.

Where will I be given Buprenex treatments?

You'll receive Buprenex at a hospital or a healthcare clinic. A healthcare provider may give you Buprenex as an injection into your muscle (intramuscular). Or they may give you the drug as an injection into your vein (intravenous, which is also called IV). Your doctor will decide which type of injection is right for you based on your condition and other medications you're taking.

Because Buprenex has to be given by a healthcare provider, you can't give yourself injections of the drug.

If you're concerned about after you leave the hospital or clinic, talk with your doctor. They can recommend treatments for pain relief.

Is Buprenex ever given by mouth?

No, Buprenex isn't ever given by mouth. A healthcare provider may give you Buprenex as an intramuscular injection. Or they may give you the drug as an IV injection. Your doctor will decide which type of injection is right for you based on your condition and other medications you're taking.

However, there are other medications very similar to Buprenex that are given by mouth. These include buprenorphine tablets that you take under your tongue (sublingual).

If you're not comfortable getting injections, let your doctor know. They may be able to recommend a different form of pain relief.

Can I take Buprenex if I'm being treated for anxiety?

Maybe. Certain anxiety medications can interact with Buprenex and cause serious side effects. These include severe sedation (feeling drowsy and less alert), respiratory depression (slowed breathing), coma, and even death.

Anxiety medications can include benzodiazepines and other central nervous system (CNS) depressants.*

(See the "Buprenex interactions" section above to learn more.)

If you have anxiety and want to take Buprenex, talk with your doctor. They can see whether Buprenex is right for you.

* Buprenex has a boxed warning for benzodiazepines and other CNS depressants. This is the most serious warning from the Food and Drug Administration (FDA). For more information, see "FDA warnings" at the beginning of this article.

Can I use Buprenex to treat opioid dependence?

No, you can't. Using Buprenex alone to treat opioid dependence may cause you to become addicted* to Buprenex. (With opioid dependence, you need an opioid drug to function.)

However, you might be able to use a drug called naloxone to treat opioid dependence. Naloxone is often used with buprenorphine, which is the active drug in Buprenex. Examples of combinations of naloxone and buprenorphine that are available include:

  • Zubsolv, which is a drug that you take under your tongue (sublingual)
  • Bunavail, which is a drug that you take inside your cheek (buccal)

If you're dependent on taking opioids, talk with your doctor. They can help you decide on the best treatment for you.

* Buprenex has a boxed warning for addiction and misuse. This is the most serious warning from the Food and Drug Administration (FDA). For more information, see "FDA warnings" at the beginning of this article.

Buprenex precautions

This drug comes with several precautions.

FDA warnings

This drug has several boxed warnings. A boxed warning is the most serious warning from the Food and Drug Administration (FDA). It alerts doctors and patients about drug effects that may be dangerous.

  • Addiction and misuse. Taking Buprenex may put you at risk for becoming addicted to the drug, abusing it, or misusing it. This may result in an overdose or even death. Your doctor will check your risk for drug addiction and misuse before you start taking Buprenex. They'll also monitor you during your Buprenex treatment.
  • Life-threatening respiratory depression. Taking Buprenex can cause a condition called respiratory depression in which your breathing becomes slow and weak. The condition can be severe, life-threatening, or even fatal. Your doctor will monitor you during your Buprenex treatment, especially when you first take the drug or if they increase your dose.
  • Neonatal opioid withdrawal syndrome. Taking Buprenex for a long time when you're pregnant may cause neonatal opioid withdrawal syndrome. This is a condition in which your baby is born with opioid withdrawal symptoms. Without treatment, the condition can be life-threatening.
  • Risk from using benzodiazepines and other CNS depressants. Taking Buprenex with benzodiazepines or other central nervous system (CNS) depressants, or alcohol can be dangerous. It can lead to severe sedation (feeling drowsy and less alert), respiratory depression (see above), coma, or even death. Your doctor will try to limit your dosage of these substances and monitor you during your Buprenex treatment.

Other warnings

Before taking Buprenex, talk with your doctor about your health history. Buprenex may not be right for you if you have certain medical conditions or other factors affecting your health.

Note: For more information about the potential negative effects of Buprenex, see the "Buprenex side effects" section above.

Chronic obstructive pulmonary disease (COPD)

If you have chronic obstructive pulmonary disease (COPD), taking Buprenex may make it harder to breathe.

Before you start taking Buprenex, tell your doctor if you have COPD. They'll monitor you closely to make sure that the drug isn't affecting your breathing.

Are older than age 65 years or are very ill

If you're older than age 65 years or are very ill, Buprenex may be more likely to cause serious breathing problems. (See "Life-threatening respiratory depression" in the "Side effect details" section above.)

Before you start taking Buprenex, tell your doctor if you're having trouble breathing. They can help you decide if Buprenex is right for you.

Heart conditions

Buprenex can cause serious heart problems, especially in people with certain heart conditions. These conditions include:

A family history of heart disease can also increase your risk for heart problems while taking Buprenex. Certain heart rhythm medications can increase your risk as well.

If you or anyone in your family has a history of heart disease, tell your doctor before you start taking Buprenex. Also, tell them about any heart medications that you're taking. You and your doctor can decide on the best treatment for you.

Severe low blood pressure

Rarely, Buprenex may lower your blood pressure. In some people, this can lead to fainting. If you have shock, you shouldn't take Buprenex at all. (Having shock may increase your risk for low blood pressure, and Buprenex can cause severe low blood pressure.)

If you have a history of low blood pressure or shock, tell your doctor. They can see if Buprenex is right for you or recommend another treatment.

Increased intracranial pressure

If you have increased pressure in your skull, taking Buprenex may increase that pressure even more. Increased pressure in your skull may be caused by head injuries, brain tumors, or other health problems.

If you've had increased pressure in your skull or a head injury in the past, tell your doctor. They can see if Buprenex is right for you.

Allergic reactions

If you've ever had an allergic reaction to buprenorphine, the active drug in Buprenex, you shouldn't take Buprenex. And if you don't know whether you've had an allergic reaction to buprenorphine, talk to your doctor. They can recommend the best treatment for you.

Gastrointestinal conditions

If you have a blockage in your intestines, taking Buprenex may make it worse.

Tell your doctor if you have a history of blockages in your intestines, including paralytic ileus. They can recommend the best treatment for you.

Seizures

Buprenex may increase your risk for seizures if you have a seizure disorder.

If you have a history of seizures or seizure disorders, tell your doctor. They can recommend the best treatment for you.

Pregnancy

Buprenex use during pregnancy can lead to problems during and after labor. For more information, please see the "Buprenex and pregnancy" section above.

Breastfeeding

If you've been taking Buprenex, it's recommended that you not breastfeed your child. For more information, please see the "Buprenex and breastfeeding" section above.

Professional information for Buprenex

The following information is provided for clinicians and other healthcare professionals.

Indications

Buprenex is indicated to treat patients with severe pain that requires an opioid analgesic. Its use is limited to patients who have failed or haven't tolerated previous analgesic treatments. This is due to the risks of addiction and misuse associated with opioid medications, including Buprenex.

Buprenex may be used in adults and children ages 2 to 12 years.

Mechanism of action

Buprenex has different effects on the opioid receptors. In the mu-opioid receptors, it acts by agonizing their function. In the kappa-opioid receptors, Buprenex antagonizes their function.

In vitro studies have proved that Buprenex binds to the opioid receptors with a very low dissociation rate. This dissociation rate is believed to be responsible for Buprenex's long-acting action compared to that of morphine.

Also, the dissociation rate is likely to explain why Buprenex's action can't always be reversed with the use of opioid antagonists. It also explains the low physical dependence observed in patients taking Buprenex.

Pharmacokinetics and metabolism

Most pharmacokinetic studies of Buprenex have been done in postoperative adult patients. Results have shown a mean half-life elimination of 2.2 hours following intravenous administration.

In postoperative children, the elimination of intravenous Buprenex was higher than in adults. At pediatric doses of 3μg/kg, children required a lower interdose interval than adults (four to five hours vs. six to eight hours).

Buprenex is primarily metabolized hepatically by CYP3A4. CYP3A4 metabolism results in an active metabolite, norbuprenorphine, which undergoes further metabolism via glucuronidation. Clearance of the drug is related to hepatic blood flow.

Contraindications

Buprenex is contraindicated in patients with:

Misuse and dependence

Buprenex is a Schedule III controlled substance. It can result in misuse even when administrated under medical surveillance.

Also, Buprenex can cause patient dependence on the medication. Dependence can appear in the form of tolerance or physical dependence. Physical dependence does not typically occur until after several days to weeks of continued opioid treatment.

It's recommended to avoid abrupt discontinuation of Buprenex to prevent drug dependence. Abrupt discontinuation may lead to withdrawal symptoms. In pregnant women, it can cause neonatal opioid withdrawal syndrome.

Healthcare professionals should monitor patients taking Buprenex for any symptom of withdrawal. If symptoms are observed, medical intervention should be provided to control drug dependence.

Storage

Buprenex should be stored at room temperature between 68° to 77°F (20° to 25°C).

Buprenex should be kept in its original package. All packages should be protected from the light to avoid degradation of its active and inactive ingredients.

Disclaimer: Medical News Today has made every effort to make certain that all information is factually correct, comprehensive, and up-to-date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or other healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.