How Does Buprenorphine Work in the Brain?

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In March 2020, more than 216,000 people filled a prescription for Buprenorphine.[1] Buprenorphine is one of 3 FDA approved medications for opioid use disorder (OUD).

Buprenorphine acts on opioid receptors in the brain - the same receptors used by drugs like heroin and Vicodin. By binding to those receptors, it prevents the withdrawal symptoms from discontinuing opioid use, helping physically stabilize people so they can work on long term abstinence.

If you're struggling with OUD, Buprenorphine can be life saving. 

What Is Suboxone?

Suboxone contains Buprenorphine (the active opioid component) and Naltrexone (which is not absorbed by the body but prevents medication misuse).

Buprenorphine

Buprenorphine is a long-acting partial opioid agonist.[2] It binds to opioid receptors in the brain instead of other opioids, and suppresses withdrawal and cravings. In this way, it acts to treat OUD both acutely and on a long-term basis.

At the same time, it displays what is called a ceiling effect. Unlike other full opioids, it does not continue to turn on opioid receptors at higher and higher doses, meaning that there is a limit to how “high” a person can get off Suboxone and an upper limit to how much it can suppress the respiratory drive.

Buprenorphine allows patients to carry out their everyday activities without experiencing opioid withdrawal or cravings. In this way, it treats opioid use disorder and restores a person to physiologic normal while they focus on other aspects of their recovery.

Naltrexone

Naltrexone is an opiate antagonist, meaning it blocks drugs like heroin and Vicodin from latching to receptors and causing euphoria.[3]

In an overdose emergency, naltrexone can be a lifesaving drug. It displaces opioids on opioid receptors in the event of an overdose, “sobering them up” immediately and reversing respiratory depression.

Adding Naltrexone to Suboxone provides overdose protection. If people attempt to misuse their Suboxone (via snorting or injecting), Naltrexone will prevent overdose. This can be lifesaving, which is why Naltrexone has been added to Buprenorphine in the combination of Suboxone. 

How Does Suboxone Work in the Body?

Buprenorphine is poorly absorbed in the stomach, but much more readily absorbed sublingually (under the tongue) which is why Suboxone is sold as a dissolving strip or tablet. It absorbs directly through the oral mucosa into the bloodstream.

Once Suboxone enters the bloodstream, it binds to opioid receptors for hours to even days, blocking withdrawal symptoms and cravings for other opioids. [4]

Eventually it unbinds and its effects wear off. It is then processed by the liver into inactive metabolites, which travel to the kidney and are excreted in the urine. 

How Does Suboxone Help People With OUD?

At proper doses, Buprenorphine acts as a substitute for other opioids, binding to opioid receptors in the brain and preventing withdrawal symptoms and cravings.

Suboxone is very effective in helping people recover from OUD. In one study, 75% of people taking Suboxone had negative urine drug tests a year later compared to 0% of people taking a placebo drug.[5]  People taking 16 mg of buprenorphine or more per day are 1.82 times more likely to stay in treatment compared to those taking a placebo.[6] For this reason, it has been approved by the FDA as a first line treatment for OUD. 

Who Is a Candidate for Suboxone?

Almost anybody who meets criteria for an OUD is potentially a candidate for Suboxone. In addition, there are very few medical reasons why a person cannot take Suboxone. It is overall very safe for most patients, particularly under the supervision of a licensed Suboxone provider.

If you're struggling with an OUD and you're ready to comply with a treatment program, Suboxone could be a good choice for you. The medication is safe and effective when used under the care of a medical team.

Talk with your doctor and ask if Suboxone is right for you.

Sources

  1. Assessment of Filled Buprenorphine Prescriptions for Opioid Use Disorder During the Coronavirus Disease 2019 Pandemic. JAMA. https://jamanetwork.com/journals/jamainternalmedicine/fullarticle/2774272. December 2020. Accessed September 2022.
  2. Buprenorphine Treatment for Opioid Use Disorder: An Overview. CNS Drugs. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6585403/. June 2020. Accessed September 2022.
  3. What Is Naltrexone? UAMS. https://psychiatry.uams.edu/clinical-care/cast/what-is-naltrexone/. Accessed September 2022.
  4. Suboxone Prescribing Information. U.S. Food and Drug Administration. https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/020733s022lbl.pdf. February 2018. Accessed September 2022.
  5. Suboxone: Rationale, Science, Misconceptions. The Ochsner Journal. https://nida.nih.gov/publications/research-reports/medications-to-treat-opioid-addiction/efficacy-medications-opioid-use-disorder. 2018. Accessed September 2022. 
  6. How Effective Are Medications to Treat Opioid Use Disorder? National Institute on Drug Abuse. https://nida.nih.gov/publications/research-reports/medications-to-treat-opioid-addiction/efficacy-medications-opioid-use-disorder. December 2021. Accessed September 2022.

Medically Reviewed By Elena Hill, MD, MPH

Elena Hill, MD; MPH received her MD and Masters of Public Health degrees at Tufts Medical School and completed her family medicine residency at Boston Medical Center. She is currently an attending physician at Bronxcare Health Systems in the Bronx, NY where she works as a primary care physician as well as part time in pain management and integrated health. Her clinical interests include underserved health care, chronic pain and integrated/alternative health.

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