How Does Buprenorphine Work in the Brain?

Buprenorphine is one of three FDA-approved medications for opioid use disorder (OUD). In March 2020, more than 216,000 people filled a prescription for a buprenorphine-containing medication like Suboxone.[1]

If you’re struggling with OUD, Suboxone could change your brain chemistry. And those alterations could change your life.

Suboxone prevents opioid withdrawal symptoms and eases cravings, helping people focus on long-term abstinence.

What Is Suboxone?

Suboxone contains two ingredients: buprenorphine (the active opioid component) and naloxone (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 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 turning 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 a person’s breathing.

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

Naloxone

Naloxone is an opioid antagonist that blocks drugs like heroin and Vicodin from latching to receptors and causing euphoria.[3]

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

Adding naloxone to Suboxone provides overdose protection. If people attempt to misuse their Suboxone (via snorting or injecting), naloxone will prevent overdose.

How Does Buprenorphine Change Brain Chemistry?

Researchers say OUD doesn’t stem from a lack of willpower or a character defect. Instead, people develop substance use disorders due to longstanding exposure to chemicals that alter brain chemistry.[4]

Opioids like heroin, OxyContin, and morphine make brain cells release huge quantities of dopamine and other feel-good chemicals. In time, those cells won’t release dopamine without a push from opioids. 

Absent neurotransmitters make you feel jittery, sick, and depressed. Cravings for drugs rise, and they can seem uncontrollable. 

Buprenorphine latches to the same brain receptors, but it triggers only mild changes. You won’t feel sick, jittery, and desperate for drugs. 

Instead, you feel more like yourself. The medication corrects your brain chemistry imbalance, so you can lead a productive life. 

How Does Buprenorphine Work in the Body?

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

Once buprenorphine enters the bloodstream, it binds to opioid receptors, blocking withdrawal symptoms and cravings for other opioids.

Eventually, it unbinds and wears off. The liver then processes it 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 than those taking a placebo.[6] For this reason, the FDA has approved it as a first-line treatment for OUD.

Who Is a Candidate for Suboxone?

Almost anybody who meets the criteria for OUD is potentially a Suboxone candidate. 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 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 January 2023.
2. Buprenorphine Treatment for Opioid Use Disorder: An Overview. CNS Drugs. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6585403/. June 2020. Accessed January 2023.
3. What Is Naloxone? Substance Abuse and Mental Health Services Administration. https://www.samhsa.gov/medication-assisted-treatment/medications-counseling-related-conditions/naloxone. September 2022. Accessed January 2023.
4. The Neurobiology of Opioid Dependence: Implications for Treatment. Addiction Science and Clinical Practice. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2851054/. July 2002. Accessed January 2023.
5. Suboxone: Rationale, Science, Misconceptions. The Ochsner Journal. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5855417/. 2018. Accessed January 2023.
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 January 2023.