Buprenorphine

By Naomi Carr

Last updated: 19 March 2024 & medically reviewed by Dr. David Miles

What is buprenorphine?

Buprenorphine is a synthetic opioid medication used to treat pain and opioid use disorder. It was approved by the US Food & Drug Administration for these uses in 2002 and is a Schedule III controlled substance. While buprenorphine is a type of opioid, it is much less potent than other opioids. ^[1]

Buprenorphine for opioid use disorder treatment

Buprenorphine is commonly used for opioid use disorder (OUD) treatment. It is an opioid agonist and can be used as a replacement therapy, as a substitute for the opioid of abuse. By replacing the abused substance with an opioid of lower potency, the individual can be at less risk of harmful effects, withdrawal symptoms, and cravings while receiving additional treatment. ^[1][2]

Buprenorphine treatment can be commenced 12-24 hours after the last use of an opioid. It should not be taken before this time as it can, depending on multiple factors, cause the onset of acute withdrawal symptoms if an opioid is still in the body. ^[2]

When cravings, withdrawal symptoms, and side effects have reduced, the individual can begin a gradual taper off buprenorphine. As it is long-lasting, the dose can be reduced from once per day to once every other day in certain circumstances. This can then be reduced to a complete cessation or can continue long-term as a maintenance therapy to help prevent relapse. ^[3]

Buprenorphine is often utilized alongside additional interventions to treat OUD, such as psychotherapies and holistic approaches, as this is often the most effective treatment plan. ^[4]

How does buprenorphine work?

Buprenorphine is a partial agonist of the mu-opioid receptor and an antagonist of the kappa-opioid receptor. It acts on the central nervous system and can produce an analgesic effect that is 20-50 times more potent than morphine when compared milligram to milligram. ^[1][5]

However, after reaching a certain dose, increases in the dosage of buprenorphine will not increase the effects of the substance, known as the ceiling effect. This effect means that buprenorphine is a much safer substance than other opioids in terms of overdose risk. ^[1][5]

As a partial opioid agonist, buprenorphine can bind to the receptor, displacing other opioids and preventing their effects. The action of buprenorphine helps those with an OUD manage their cravings during detox while producing little euphoric effect and causing a low risk of respiratory depression. ^[3]

Buprenorphine is less likely to lead to dependence, misuse, and side effects compared to other opioids, and is a long-acting medication so it can be taken less frequently. ^[2]

Buprenorphine and naloxone

Naloxone is an opioid antagonist, which blocks the effects of opioids. It is often used as a life-saving medication in the event of an opioid overdose, as it can reverse harmful effects. If naloxone is taken while an opioid is in the system, it can cause the sudden onset of withdrawal symptoms. ^[6]

Buprenorphine medication is often combined with naloxone as this can help reduce abuse and diversion potential. Buprenorphine alone can cause some euphoric effects and may be abused, particularly by those who have developed opioid dependence. Buprenorphine and naloxone combination medications do not cause euphoric effects, preventing abuse. ^[1][7]

Methods of administration for buprenorphine

Buprenorphine is available in various methods of administration and as a lone or combination medication. Some of the available versions of buprenorphine, along with their most well-known brand names, include: ^[2]

• Buprenorphine sublingual tablets (Subutex)

• Buprenorphine transdermal patch (butrans)

• Buprenorphine and naloxone sublingual films (Suboxone)

• Buprenorphine and naloxone sublingual tablets (Zubsolv)

• Buprenorphine and naloxone buccal film (Belbuca)

• Buprenorphine extended-release injection (Sublocade)

• Buprenorphine implants (Probuphine)(discontinued)

Tablets should be swallowed whole, without crushing or breaking. 

Sublingual tablets and films should be placed under the tongue and left there to dissolve. 

Buccal films should be placed on the tongue until dissolved. 

Sublocade is injected into the abdomen and can only be administered by a healthcare professional.

Side effects of buprenorphine

Do all rehab treatments for OUD use buprenorphine?

Buprenorphine is a safe and effective treatment for OUD so it is commonly used for this purpose. Most rehab centers will offer this treatment, although it may not be effective or appropriate for some people. In these cases, other treatments may be used, such as: ^[4]

• Methadone

• Naltrexone

• Withdrawal symptom management, such as clonidine or lofexidine

Alongside medications, rehab centers will often offer therapeutic interventions, including behavioral therapies such as cognitive behavioral therapy (CBT), group therapies, and psychosocial interventions. ^[4]

Is buprenorphine treatment covered under health insurance?

If buprenorphine is considered necessary for treatment, it may be covered by health insurance. However, health insurance plans tend to differ in their coverage, so it is recommended to contact the provider directly to be clear about what treatments are covered, which healthcare providers are in-network, and if there are any out-of-pocket costs involved.

Safety precautions for buprenorphine

Buprenorphine may not be a suitable treatment for certain people and may need to be used with caution in some circumstances. Additionally, certain safety precautions should be considered when using buprenorphine treatment.

Drug interactions

Some substances and medications can interact with buprenorphine which can cause a change in the effectiveness of the medication or an increased risk of side effects. This includes antihistamines, benzodiazepines, anticonvulsants, antidepressants, HIV medications, diuretics, glaucoma medications, Parkinson’s disease medications, analgesics, migraine medications, and sedatives. ^[1][7]

Central nervous system (CNS) depressants, such as opioids, benzodiazepines, and alcohol, should not be used with buprenorphine as the CNS depressant effects are likely to be increased. This can lead to severe or even fatal effects such as oversedation, respiratory depression, and coma. ^[1]

Physical health

People with a history of liver or kidney disease, head injury, or stomach, thyroid, or gallbladder issues may not be able to safely take buprenorphine or should use the medication with caution and increased monitoring. ^[7]

People with respiratory conditions, such as COPD or asthma, should use buprenorphine with caution as it can worsen breathing difficulties. ^[1]

Mental health

People with a history of mental illness, including psychosis, may require increased monitoring when using buprenorphine, as it can worsen symptoms. ^[7]

Pregnancy

Buprenorphine can cause neonatal opioid withdrawal syndrome (NOWS) when used during pregnancy. However, untreated OUD can also cause a risk of severe harm to the fetus, so it is recommended to consult with a doctor about the benefits and risks before treatment. ^[2]

Opioid naïve people

Buprenorphine can cause severe or fatal effects in individuals who have not used an opioid before. ^[7]

Treatment commencement

Buprenorphine should not be commenced while an opioid is still in the system, as this can cause the sudden onset of withdrawal symptoms. It is recommended to commence treatment after 12-24 hours of abstinence. ^[2]

Dependence and withdrawal

Buprenorphine can cause dependence, which may lead to withdrawal symptoms when treatment is stopped. As such, a gradual taper is recommended when stopping treatment. ^[7]

Storage

Buprenorphine should be stored safely, away from the reach of children, pets, or others, as it can be fatal when taken by those for whom it is not prescribed. ^[2]

Driving safety

Buprenorphine can cause drowsiness and impaired functioning, so it is recommended not to drive or operate heavy machinery while using the medication. ^[1]