Buprenorphine

What is Buprenorphine?

Buprenorphine is a reliable medication used to treat opioid use disorder (OUD). When a person develops opioid dependence, quitting their opioid use can result in symptoms of opioid withdrawal.

While overall opiate withdrawal symptoms are not life-threatening, the cravings and discomfort often cause individuals to return to their previous substance use, which can also lead to opioid overdose.

Buprenorphine is a partial agonist that provides stabilization in early recovery stages and can be used later on as part of a recovering addict’s maintenance therapy.

Without MAT, the chances of relapse for a person who suffers from OUD are significant; studies have shown that outcomes for people with OUD are much better with MAT.

—U.S. Department of Health and Human Services (HHS)

Buprenorphine works by binding to the brain’s opiate receptors, blocking any other opiates from getting through and causing any euphoric effects. Buprenorphine can also help alleviate the uncomfortable side effects of withdrawal from opiate withdrawal, which range from a runny nose to muscle cramps.

In many instances, patient use of buprenorphine is safely self-administered through outpatient treatment programs as a take-home medication. A patient’s daily dose of buprenorphine will often appear in the form of sublingual tablets or a sublingual film.

Soboxone® is a buprenorphine formulation that includes naloxone and is particularly useful in treating opioid use disorder.

The first dose of buprenorphine is usually provided to opioid-dependent patients within 12-24 hours after they have stopped all other opioid drug use. Otherwise, the patient may experience what is known as “precipitated withdrawal,” where they will feel sudden and intense withdrawal effects soon after the ingestion of buprenorphine.

Brand Names for Buprenorphine

Buprenorphine comes in a few different forms with various brand names that have been approved for use by the FDA.

The most common brand names for buprenorphine are:

• Subutex®: Buprenorphine sublingual tablets
• Suboxone®: Buprenorphine + naloxone sublingual films
• Zubsolv®: Buprenorphine + naloxone sublingual tablets
• Bunavail®: Buprenorphine + naloxone buccal film
• Probuphine®: Buprenorphine implants
• Sublocade®: Buprenorphine extended-release injection

What Are the Side Effects of Buprenorphine?

The use of buprenorphine may cause some side effects. If you are using buprenorphine as prescribed and experience any of these side effects, particularly if those effects worsen, you should follow up with your primary care doctor or prescribing physician to review your treatment options.

Common Side Effects of Buprenorphine

According to The Substance Abuse and Mental Health Services Administration (SAMHSA), the following side effects are more common when taking buprenorphine for opioid use disorder.

These common buprenorphine side effects can include:

• Dizziness
• Drowsiness, fatigue
• Constipation, nausea, and vomiting
• Headache
• Dry mouth
• Muschel aches and champs
• Insomnia
• Excess sweating
• Tooth decay
• High temperature, including fever
• Tremors (shaky hands)
• Heart palpitations
• Blurry vision
• Difficulty concentrating

Less Common Side Effects of Buprenorphine

SAMHSA also lists these less-common side effects of taking buprenorphine when treating opioid use disorder.

Contact your primary care physician immediately if you experience any of these symptoms, as they are very serious.

These more rare, serious side effects of buprenorphine can include:

• Trouble breathing
• Overdose symptoms
• Withdrawal symptoms
• Adrenal insufficiency (low blood pressure, dizziness, skin darkening, and nausea)
• Neonatal abstinence syndrome (in newborns of breastfeeding mothers)
• Implant form of buprenorphine: Itching, pain, swelling, or nerve damage
• Injectable form of buprenorphine: Pain at the injection site

Misuse Potential of Buprenorphine

Buprenorphine acts similarly to an opioid and, therefore, still has the potential for misuse. Certain formulations of buprenorphine contain other medications, such as naltrexone, that would counteract any opioid-like effects from buprenorphine and prevent relapse in the patient.

How Buprenorphine Works – Pharmacology

Buprenorphine is categorized as a Schedule III drug, meaning it has a lower likelihood of leading to misuse or dependency in the user. Buprenorphine is considered highly successful in the treatment of opioid use disorder, as well as in the management of OUD after the patient’s initial recovery.

Pharmacodynamics

Buprenorphine works with the brain’s opioid receptors. Taking buprenorphine provides pain relief and sedation to the central nervous system. Buprenorphine should never be mixed with alcohol, as its sedative effects combined can cause serious respiratory depression.

If you are prescribed any additional medication, such as benzodiazepines, that can contribute to the sedation of your central nervous system, your doctor may prescribe you a lower dose to ensure your safety.

One positive aspect of buprenorphine is known as the “ceiling effect,” which means buprenorphine’s effects will plateau at a certain point. If an individual tries to misuse buprenorphine, at a certain point, the buprenorphine will not provide any additional effects to the user.

Mechanism of Action

Buprenorphine is a partial opioid agonist (mu receptor) and antagonist (kappa receptor). When taking buprenorphine, it not only blocks other opioids from taking effect, but buprenorphine also relieves pain and other uncomfortable withdrawal symptoms.

Absorption

Buprenorphine is taken through tablets or sheets that dissolve under the tongue, which gets it directly into the bloodstream by bypassing the stomach. If any pieces of the buprenorphine are swallowed, the stomach will break down the buprenorphine too quickly to have any effect.

Alternatively, buprenorphine is available through an intravenous shot which will also put it directly into the bloodstream.

Distribution

Once absorbed, buprenorphine passes through the circulatory system quickly. It takes 40 minutes to 3-and-a-half hours to begin working in the body. Buprenorphine will also pass through the blood-brain barrier. It can be found in the placenta and breast milk.

Metabolism and Elimination

Buprenorphine has a long half-life, which means it stays in the body for a long time. Effects of buprenorphine last between 24 to 48 hours. The liver then breaks down buprenorphine and excretes it through feces and urine.

What Should You Know Before Starting Buprenorphine?

One common misconception about most medication-assisted treatments, including buprenorphine, is that recovering addicts trade one addiction for another. While buprenorphine has some potential for misuse or dependency, it is a much milder medication than the opiates that the patient was previously addicted to.

“The medical evidence is clear: access to medication-assisted treatment, including buprenorphine that can be prescribed in office-based settings, is the gold standard for treating individuals suffering from opioid use disorder.”

—Brett P. Giroir, MD, Assistant Secretary for Health | HHS

Taking buprenorphine to help with the withdrawal process is the ideal way to get through detox and early recovery. Research shows that patients who take buprenorphine or other similar prescribed medication during treatment for opioid use disorder have a much lower relapse rate.

How Should Buprenorphine Be Used?

Buprenorphine is useful for treating opioid use disorder but is most successful when combined with behavioral therapy and rehabilitation.

Physicians may prescribe buprenorphine during a patient’s initial detox and recovery process to help ease them through withdrawals. Patients may also receive a buprenorphine prescription as part of their long-term aftercare. Some patients remain on buprenorphine indefinitely to help aid them in their opioid-free life.

Buprenorphine is NOT used in treating opioid overdose. Rather, the medication known as Naloxone (NARCAN®) can be administered in case of an opioid overdose.

Is Buprenorphine Right for Me or My Loved One?

If you’re considering medication-assisted treatment to help you with opioid use disorder, the SAMHSA program locator can help you find treatment centers near your home.