Buprenorphine is an opioid medication used to treat opioid use disorder (OUD), acute pain, and chronic pain. 

Buprenorphine is used for opioid addiction to reduce cravings and withdrawal symptoms without causing euphoria or dangerous side effects and helps prevent relapse. It works by being a substitute for the drug being abused, so the patient has minimal discomfort, which allows the patient to focus on their recovery. Buprenorphine for OUD is used as part of a complete treatment program that also includes counseling and behavioral therapy.

For opioid use disorder, buprenorphine is available as long-acting injections (Sublocade, Brixadi) and sublingual tablets (Subutex discontinued, generics available). 

Buprenorphine is used to treat acute pain that is severe enough to require an opioid analgesic and moderate to severe chronic pain that is not controlled by other medicines. For chronic around-the-clock pain, it is available as buprenorphine skin patches (Butrans) and buprenorphine buccal films (Belbuca), and for acute pain is available as an injection (Buprenex).

Buprenorphine-naloxone combinations are also available to be used for opioid addication and include sublingual film (Bunavail), sublingual film and sublingual tablets (Suboxone), and sublingual tablets (Zubsolv).

Buprenorphine’s mechanism of action is that is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor.

Is buprenorphine a controlled substance?

Yes, buprenorphine is a Schedule III controlled drug, which means it has a potential for abuse more than those in Schedules 4 and 5. If abused, it may lead to moderate or low physical dependence or high psychological dependence.

Warnings

MISUSE OF OPIOID MEDICINE CAN CAUSE ADDICTION, OVERDOSE, OR DEATH. Keep buprenorphine in a place where others cannot get to it.
Patient Access to Naloxone for the Emergency Treatment of Opioid Overdose. Patients should have access to naloxone to treat opioid overdose based on the patient’s risk factors for overdose, such as currently using a CNS depressant, a history of an opioid use disorder, or previous opioid overdose.  Having naloxone available is important if the patient has household members (including children) or other close contacts at risk for accidental exposure or overdose.

Taking this medicine during pregnancy may cause life-threatening withdrawal symptoms in the newborn.

Fatal side effects can occur if you use this medication with alcohol or with other drugs that cause drowsiness or slow your breathing.

Before taking this medicine

You should not use this medicine if you are allergic to buprenorphine or:

• If you have used another narcotic drug within the past 4 hours.

To make sure this medication is safe for you, tell your doctor if you have ever had:

• methadone treatment;
• breathing problems, sleep apnea;
• abnormal curvature of the spine that affects breathing;
• liver disease (especially hepatitis B or C);
• kidney disease;
• enlarged prostate, urination problems;
• a head injury or brain tumor;
• alcoholism, hallucinations, mental illness; or
• problems with your stomach, gallbladder, adrenal gland, or thyroid.

Pregnancy

If you use buprenorphine while you are pregnant, your baby could become dependent on the drug. This can cause life-threatening withdrawal symptoms in the baby after it is born. Babies born dependent on habit-forming medicine may need medical treatment for several weeks.

Infertility

Chronic use of opioids may cause reduced fertility in females and males of reproductive potential. It is not known whether these effects on fertility are reversible 

Breastfeeding

Buprenorphine can pass into breast milk and may cause drowsiness and breathing problems in a nursing baby. Ask your doctor about any risk to your baby.

How should I take buprenorphine?

Use buprenorphine exactly as it was prescribed for you. Follow the directions on your prescription label and read all medication guides. Your doctor may occasionally change your dose. Never use this medication in larger amounts, or for longer than prescribed.

Opioid Use Disorder

Buprenorphine Sublingual (for OUD)

Buprenorphine sublingual is usually taken only at the start of treatment for addiction (induction phase). Most people are later switched to long-acting buprenorphine (Sublocade injection or Brixadi injection) or another medicine that contains buprenorphine with naloxone (Bunavail, Suboxone, Zubsolv). You may receive your first doses of buprenorphine sublingual in a hospital or clinic setting until your condition improves. Use dry hands when handling the tablet. Place the tablet under your tongue and allow it to dissolve with your mouth closed. Do not chew the tablet or swallow it whole. If your doctor has prescribed more than 2 tablets per dose, place the correct number of tablets under your tongue at the same time and allow them to dissolve completely. Do not eat or drink anything until the tablet has completely dissolved in your mouth. Never crush or break a pill to inhale the powder or mix it into a liquid to inject the drug into your vein. Doing so could result in death.

Extended-release buprenorphine subcutaneous injection (for OUD)

Buprenorphine extended-release injection is given subcutaneously (just under the skin). Sublocade and Brixadi can be given in the abdomen, thigh, buttock, or the back of the upper arm. 

Sublocade should only be used when patients have received treatment with at least one dose (eg, 4 mg) of an oral transmucosal (used under the tongue or inside the cheek) buprenorphine-containing medicine. Sublocade is injected as a liquid. After the injection, Sublocade changes to a solid form called a depot. The depot may be seen or felt as a small bump under your skin at the injection site on your abdomen, thigh, buttock, or back of the upper arm, for several weeks. The depot will get smaller over time. Do not try to remove the depot, and do not rub or massage the injection site. Sublocade is part of a complete treatment plan that should include counseling.

Brixadi should only be used if you are currently receiving buprenorphine treatment or if your healthcare provider has given you a test dose of buprenorphine first to see if you are able to tolerate it. If you are new to Brixadi treatment, the upper arm should only be used after 4 doses of Brixadi in your buttock, thigh, or stomach. Brixadi is injected as a liquid; after the injection, the liquid changes to a gel form called a depot. The depot is not always felt under the skin. Do not try to remove the depot. Brixadi is part of a complete treatment plan that should include counseling.

Pain

Buprenex (buprenorphine injection) is used for pain, it is given by deep intramuscular or slow (over at least 2 minutes) intravenous injection at up to 6-hour intervals, as needed.

Butrans skin patch is used for chronic around-the-clock pain. It is applied once a week and worn continuously for 1 week. Do not change your dose. Apply Butrans exactly as prescribed by your healthcare provider. Your doctor will prescribe you the lowest effective dose for the shortest time needed. Do not take hot baths or sunbathe, use hot tubs, saunas, heating pads, electric blankets, heated waterbeds, or tanning lamps as these can cause an overdose that can lead to death.

Belbuca buccal films are used for around-the-clock treatment of moderate to severe chronic pain. Using a finger, place the yellow side of the Belbuca buccal film against the inside of your moistened cheek. Press and hold the Belbuca buccal film in place for 5 seconds and then take your finger away. Once in place, the film will dissolve completely in about 30 minutes. Do not eat or drink anything until the Belbuca film has completely dissolved in your mouth. Rinse your mouth with water after the medicine dissolves. Wait one hour after the film dissolves to brush your teeth to prevent damage to the teeth and gums. Do not chew the Belbuca film or swallow it whole. You should receive regular dental checkups while using Belbuca.

General information about using this medicine.

Never share opioid medicine with another person, especially someone with a history of drug abuse or addiction. MISUSE CAN CAUSE ADDICTION, OVERDOSE, OR DEATH. Keep the medication in a place where others cannot get to it. Selling or giving away opioid medicine is against the law.

You may need frequent blood tests to check your liver function.

If you need surgery, tell the surgeon ahead of time that you are using this medicine.

Any medical care provider who treats you should know that you are being treated for opioid addiction and that you are on buprenorphine. Make sure your family members know how to provide this information in case they need to speak for you during an emergency.

Do not stop using this medication suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to safely stop using this medicine.

Store at room temperature away from moisture and heat. Keep track of your medicine. Buprenorphine is a drug of abuse, and you should be aware if anyone is using your medicine improperly or without a prescription.

Do not keep leftover opioid medication. Just one dose can cause death in someone using this medicine accidentally or improperly. Ask your pharmacist where to locate a drug take-back disposal program. If there is no take-back program, flush the unused medicine down the toilet.

For detailed dosing information click the link below.

What happens if I miss a dose?

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line . A buprenorphine overdose can be fatal, especially in a child or other person using the medicine without a prescription.

Overdose symptoms may include extreme drowsiness or weakness, cold or clammy skin, pinpoint pupils, slow heart rate, weak pulse, very slow breathing, or coma.

What to avoid

Do not drink alcohol. Dangerous side effects or death could occur.

Avoid driving or operating machinery until you know how buprenorphine will affect you. Dizziness or drowsiness can cause falls, accidents, or severe injuries.

Buprenorphine side effects

Get emergency medical help if you have signs of an allergic reaction to buprenorphine: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Opioid medicine can slow or stop your breathing, and death may occur. A person caring for you should give naloxone and/or seek emergency medical attention if you have slow breathing with long pauses, blue colored lips, or if you are hard to wake up.

Call your doctor at once if you have:

• opioid withdrawal symptoms – shivering, goose bumps, increased sweating, feeling hot or cold, runny nose, watery eyes, diarrhea, muscle pain;
• noisy breathing, sighing, shallow breathing, breathing that stops during sleep;
• slow heartbeat or weak pulse;
• a light-headed feeling, like you might pass out;
• chest pain, trouble breathing;
• low cortisol levels – nausea, vomiting, loss of appetite, dizziness, worsening tiredness or weakness; or
• liver problems – nausea, upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

Seek medical attention right away if you have symptoms of serotonin syndrome, such as: agitation, hallucinations, fever, sweating, shivering, fast heart rate, muscle stiffness, twitching, loss of coordination, nausea, vomiting, or diarrhea.

Common buprenorphine side effects may be more likely to occur, such as:

• constipation, nausea, vomiting;
• headache;
• increased sweating;
• sleep problems (insomnia); or
• pain anywhere in your body.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects.

What other drugs will affect buprenorphine?

You may have breathing problems or withdrawal symptoms if you start or stop taking certain other medicines. Tell your doctor if you also use an antibiotic, antifungal medication, heart or blood pressure medication, seizure medication, or medicine to treat HIV or hepatitis C.

Buprenorphine can interact with many other drugs and cause dangerous side effects or death. Be sure your doctor knows if you also use:

• cold or allergy medicines, bronchodilator asthma/COPD medication, or a diuretic (“water pill”);
• medicines for motion sickness, irritable bowel syndrome, or overactive bladder;
• other narcotic medications – opioid pain medicine or prescription cough medicine;
• a sedative like Valium – diazepam, alprazolam, lorazepam, Xanax, Klonopin, Versed, and others;
• drugs that make you sleepy or slow your breathing – a sleeping pill, muscle relaxer, medicine to treat mood disorders or mental illness; or
• drugs that affect serotonin levels in your body – a stimulant, or medicine for depression, Parkinson’s disease, migraine headaches, serious infections, or nausea and vomiting.

Buprenex is an opioid medicine used to treat moderate to severe pain in adults and children at least 2 years old. An opioid is sometimes called a narcotic.

Buprenex Injection is used to relieve moderate pain that is severe enough to require an opiate pain killer and for which other medicines (e.g., non-opiate pain killers or opiate-containing combination medicines) have not been, or are not expected to be sufficient.

Buprenorphine belongs to a class of medications called opiate partial agonists. Buprenex works by changing the way the body senses pain.acute pain.

This medication guide provides information about the Buprenex brand of buprenorphine injection. Sublocade is another brand of buprenorphine injection used to treat opioid addiction.

Buprenex side effects

Get emergency medical help if you have signs of an allergic reaction to Buprenex: hives, difficult breathing, swelling of your face, lips, tongue, or throat.

Opioid medicine can slow or stop your breathing, and death may occur. A person caring for you should give naloxone and/or seek emergency medical attention if you have slow breathing with long pauses, blue colored lips, or if you are hard to wake up.

To make sure Buprenex is safe for you, tell your doctor if you have ever had:

• confusion, cold and clammy skin, slow breathing (breathing may stop);
• feeling light-headed;
• fast or uneven heart rate, shortness of breath;
• blue lips or fingernails; or
• severe constipation.

Seek medical attention right away if you have symptoms of serotonin syndrome, such as: agitation, hallucinations, fever, sweating, shivering, fast heart rate, muscle stiffness, twitching, loss of coordination, nausea, vomiting, or diarrhea.

Serious breathing problems may be more likely in older adults and people who are debilitated or have wasting syndrome or chronic breathing disorders.

Common Buprenex side effects may include:

• drowsiness, slow breathing;
• nausea, vomiting;
• dizziness, vertigo (spinning sensation);
• pinpoint pupils;
• increased sweating; or
• headache.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects.

Warnings

Buprenex may be habit-forming. Misuse can cause addiction, overdose, or death.

Using Buprenex during pregnancy may cause life-threatening withdrawal symptoms in the newborn.

Fatal side effects can occur if you use opioid medicine with alcohol, or with other drugs that cause drowsiness or slow your breathing.

Before taking this medicine

You should not use Buprenex if you are allergic to buprenorphine, or if you have:

• severe asthma or breathing problems; or
• a stomach or bowel obstruction (including paralytic ileus).

To make sure Buprenex is safe for you, tell your doctor if you have ever had:

• chronic obstructive pulmonary disease (COPD), sleep apnea, or other breathing disorder;
• a head injury, brain tumor, high pressure inside the skull, or seizures;
• problems with your bile duct, gallbladder, pancreas, thyroid, or adrenal gland;
• heart problems, an electrolyte imbalance (such as low blood levels of potassium or magnesium);
• a drug or alcohol addiction, or mental illness;
• enlarged prostate, urination problems;
• curvature of the spine that affects breathing; or
• liver or kidney disease.

Tell your doctor if you also use stimulant medicine, other opioid medicine, herbal products, or medicine for depression, mental illness, Parkinson’s disease, migraine headaches, serious infections, or prevention of nausea and vomiting. An interaction with buprenorphine could cause a serious condition called serotonin syndrome.

If you use buprenorphine during pregnancy, your baby could be born with life-threatening withdrawal symptoms, and may need medical treatment for several weeks.

Do not breastfeed. Buprenorphine in breast milk can cause life-threatening side effects in a nursing baby.

How is Buprenex given?

Buprenex is injected into a muscle or given as an infusion into a vein. A healthcare provider will give you this injection. Buprenex is usually given by injection only if you are unable to take the medicine by mouth or use another form of buprenorphine.

Buprenex is usually given at evenly spaced intervals, up to 6 hours apart. Tell your doctor if Buprenex does not relieve your pain within 1 hour after an injection.

Buprenex can cause irritation if it gets on your skin. If this occurs, remove any clothing the medicine has spilled onto, and rinse your skin with water.

Your breathing, blood pressure, oxygen levels, and other vital signs will be watched closely. You may need other medical tests.

Never share opioid medicine with another person, especially someone with a history of drug abuse or addiction. MISUSE CAN CAUSE ADDICTION, OVERDOSE, OR DEATH. Keep the medication in a place where others cannot get to it. Selling or giving away opioid medicine is against the law.

Dosing information

Usual Adult Dose of Buprenex for Pain:

Initial dose: 0.3 mg deep IM or slow IV (over at least 2 minutes); may repeat this dose once after 30 to 60 minutes if needed; then, 0.3 mg IV/IM every 6 hours as needed
-A single 0.6 mg IM dose may be given to patients who are not in a high risk category (see Warnings)
Maximum single dose: 0.3 mg (IV) or 0.6 mg (IM)

Usual Pediatric Dose of Buprenex for Pain:

2 to 12 years:
Initial dose: 2 to 6 mcg/kg IM or slow IV every 4 to 6 hours
-Some patients may not need to be remedicated for 6 to 8 hours; fixed interval or round the clock dosing should not be used until the proper inter-dose interval has been established

Over 12 years:
Initial dose: 0.3 mg deep IM or slow IV (over at least 2 minutes); may repeat this dose once after 30 to 60 minutes if needed; then, 0.3 mg IV/IM every 6 hours as needed
Maximum single dose: 0.3 mg

Comments:
-Use extra caution with IV administration, especially the first dose.
-Monitor closely for respiratory depression, especially within the first 24 to 72 hours.
-Use the lowest effective dose for the shortest duration consistent with the individual patient’s treatment goals.

Use: For the management of pain severe enough to require an opioid analgesic and for which alternate treatments are inadequate.

What happens if I miss a dose?

In a medical setting you are not likely to miss a dose.

What happens if I overdose?

In a medical setting an overdose would be treated quickly.

What should I avoid while receiving Buprenex?

Do not drink alcohol. Dangerous side effects or death could occur.

Avoid driving or hazardous activity until you know how Buprenex will affect you. Dizziness or drowsiness can cause falls, accidents, or severe injuries.

What other drugs will affect Buprenex?

You may have a fatal buprenorphine overdose if you start or stop using certain other medicines. Tell your doctor about all your medications.

Many other drugs can be dangerous when used with opioid medicine. Tell your doctor if you also use:

• medicine for allergies, asthma, blood pressure, motion sickness, irritable bowel, or overactive bladder;
• other opioid medicines;
• a benzodiazepine sedative like Valium, Klonopin, or Xanax; or
• sleep medicine, muscle relaxers, or other drugs that make you drowsy.

Bupivacaine is an anesthetic (numbing medicine) that is used as a local (in only one area) anesthetic.

Bupivacaine is given as an epidural injection into the spinal column to produce numbness during labor, surgery, or certain medical procedures.

Bupivacaine is also used as an anesthetic for dental procedures.

Bupivacaine may also be used for purposes not listed in this medication guide.

Bupivacaine side effects

Get emergency medical help if you have signs of an allergic reaction: hives, red rash, itching; sneezing, difficulty breathing; severe dizziness, vomiting; swelling of your face, lips, tongue, or throat.

Tell your caregivers at once if you have any of these serious side effects:

• feeling anxious, restless, confused, dizzy, drowsy, or like you might pass out;
• ringing in your ears, problems with speech or vision;
• metallic taste in your mouth, numbness or tingling around your mouth;
• muscle twitching, tremors, seizure (convulsions);
• weak or shallow breathing;
• fast heart rate, gasping, feeling unusually hot;
• slow heart rate, weak pulse; or
• little or no urination.

Seek medical attention right away if you develop a serious condition called methemoglobinemia. Symptoms include headache, fast heartbeats, shortness of breath, feeling tired or light-headed, or skin that looks pale, gray, or blue-colored.

Common side effects include:

• weakness, long-lasting numbness or tingling;
• feeling restless or drowsy;
• tremors;
• headache, blurred vision;
• fast or slow heartbeats;
• breathing problems;
• chills or shivering;
• back pain; or
• nausea, vomiting.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects.

Warnings

Tell your doctor if you have ever had an allergic reaction to any type of numbing medicine.

Some epidural numbing medications can have long-lasting or permanent effects on certain body processes such as sexual function, bowel or bladder control, and movement or feeling in your legs or feet. Talk with your doctor about your specific risk of nerve damage from bupivacaine.

Before taking this medicine

Tell your doctor if you have ever had an allergic reaction to any type of numbing medicine, or if you’ve ever had:

• anemia (lack of red blood cells);
• kidney or liver disease;
• a bleeding or blood clotting disorder;
• syphilis, polio, a brain or spinal cord tumor;
• numbness or tingling;
• chronic back pain, headache caused by surgery;
• low or high blood pressure;
• abnormal curvature of the spine; or
• arthritis.

It is not known whether bupivacaine will harm an unborn baby. If you are not receiving bupivacaine during childbirth, tell your doctor if you are pregnant.

It may not be safe to breastfeed while using this medicine. Ask your doctor about any risk.

How is bupivacaine given?

Bupivacaine is injected through a needle directly into or near the area to be numbed. You will receive this injection in a dental or hospital setting.

For an epidural, bupivacaine is given as an injection through a needle placed into an area of your middle or lower back near your spine.

Your breathing, blood pressure, oxygen levels, or other vital signs will be watched closely.

For a dental procedure, bupivacaine is injected directly into the mouth near the tooth or teeth your dentist will be working on.

Some epidural numbing medications can have long-lasting or permanent effects on certain body processes such as sexual function, bowel or bladder control, and movement or feeling in your legs or feet. Talk with your doctor about your specific risk of nerve damage from bupivacaine.

What happens if I miss a dose?

Since bupivacaine is given as needed before a surgery or dental procedure, you are not likely to be on a dosing schedule.

What happens if I overdose?

Since bupivacaine is given in a medical setting, you will be watched closely to make sure you do not receive too much of bupivacaine. Your caregivers will quickly treat you if you have overdose symptoms.

What should I avoid after receiving bupivacaine?

This medicine can cause numbness over a large portion of your body. After an epidural you not be able to feel or move your lower body. Take care to avoid injury while you are still numb.

After a dental procedure, avoid eating, chewing gum, or drinking a hot beverage until your mouth is no longer numb.

What other drugs will affect bupivacaine?

Tell your doctor about all other medicines you use, especially:

• an antidepressant or antipsychotic medication;
• anti-nausea medicine such as prochlorperazine (Compazine) or promethazine (Phenergan);
• blood pressure medicine–carteolol, carvedilol, labetalol, nadolol, propranolol, sotalol, timolol;
• a blood thinner such as warfarin (Coumadin, Jantoven);
• ergot medicine–dihydroergotamine, ergotamine, ergonovine, methylergonovine; or
• an MAO inhibitor–isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, tranylcypromine, and others.