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How Does Buprenorphine Work in the Brain?

Peter Manza, PhD profile image
Reviewed By Peter Manza, PhD • Updated Sep 18, 2023 • 6 cited sources

Buprenorphine is one of three FDA-approved medications for opioid use disorder (OUD). In March 2020 in the United States, 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.

How does Suboxone Work in the Brain?

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.[2]

Suboxone, which contains buprenorphine and naloxone, works in the brain to correct brain chemistry imbalances so you can lead a productive and happy life.

Buprenorphine’s Mechanism of Action

The buprenorphine component is a long-acting, partial opioid agonist, which binds to opioid receptors in the brain and eases cravings, reduces withdrawal symptoms and helps prevent relapse. [3] 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—this greatly increases the safety profile of the medication and decreases the risk of overdose.

How Naloxone Works

The naloxone, which is an opioid antagonist, blocks other opioids like heroin and Vicodin at the receptor site and helps to deter misuse by sending someone into precipitated withdrawal if they misuse the medication by injecting it or snorting it. [3] This means they’ll experience unpleasant opioid withdrawal symptoms immediately after misusing it, as opposed to experiencing a high. It is inactive otherwise.

On its own, naloxone is sold under the brand name, Narcan, to rapidly reverse the life-threatening effects of an opioid overdose due to its antagonistic nature. It displaces opioids at the opioid receptors in the event of an overdose, “sobering the person up” immediately and reversing respiratory depression.

IngredientDrug ClassHow it Helps
BuprenorphinePartial opioid agonistBinds to opioid receptors in the brain, alleviating withdrawal symptoms and cravings
NaloxoneOpioid antagonistBlocks opioids of abuse at the receptor site and deters Suboxone misuse

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. [3]

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

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. It does this without getting the individual high or producing feelings of pleasure. 

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.[5]

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 when taken 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.

Frequently Asked Questions About How Suboxone Works

Is Suboxone an Opioid?

Yes, Suboxone is an opioid due to the ingredient, buprenorphine, which is a partial opioid agonist. However, it is a much weaker opioid than opioids of misuse, such as heroin, fentanyl, and prescription painkillers so it won’t cause euphoria or an intense high.

What Ingredients Are in Suboxone?

Suboxone contains buprenorphine, a partial opioid agonist, and naloxone, an opioid antagonist. Together, they help to reduce withdrawal symptoms, ease cravings, prevent relapse, and deter Suboxone misuse.

How Does Suboxone Work to Treat Addiction?

Suboxone works to treat opioid use disorder by targeting the same receptors in the brain that opioids bind to. The buprenorphine element binds to the opioid receptors and displaces all other opioids like heroin, while reducing withdrawal symptoms and cravings. The naloxone element is inactive until someone attempts to misuse Suboxone by injecting it—then they will experience precipitated withdrawal symptoms.

How is Suboxone Administered?

Suboxone is prescribed as either a sublingual strip or a sublingual pill/tablet. Both are equally effective at treating opioid use disorder and which one you choose largely depends on your preferences.

How Long Does it Take for Suboxone to Work?

Typically, it takes between 20 minutes and 60 minutes for the desired effects of Suboxone to kick in, with peak effects occurring between 1.5 hours and 3 hours after taking it.

Is Suboxone Substituting One Drug for Another?

Technically, Suboxone is an opioid, and some experts will refer to Suboxone as “opioid substitution therapy,” but it’s certainly not trading one addiction for another. Addiction is a pattern of compulsive use regardless of negative consequences, whereas Suboxone therapy is a regimented treatment, used in conjunction with counseling, to help someone stop misusing opioids.

Reviewed By Peter Manza, PhD

Peter Manza, PhD received his BA in Psychology and Biology from the University of Rochester and his PhD in Integrative Neuroscience at Stony Brook University. He is currently working as a research scientist in Washington, DC. His research focuses on the role ... Read More

  1. Assessment of Filled Buprenorphine Prescriptions for Opioid Use Disorder During the Coronavirus Disease 2019 Pandemic. JAMA December 2020. Accessed January 2023.
  2. The Neurobiology of Opioid Dependence: Implications for Treatment. Addiction Science and Clinical Practice July 2002. Accessed January 2023.
  3. Buprenorphine Treatment for Opioid Use Disorder: An Overview. CNS Drugs June 2020. Accessed January 2023.
  4. Suboxone: Rationale, Science, Misconceptions. The Ochsner Journal 2018. Accessed January 2023.
  5. How Effective Are Medications to Treat Opioid Use Disorder? National Institute on Drug Abuse. December 2021. Accessed January 2023.
  6. What Is Naloxone? Substance Abuse and Mental Health Services Administration. September 2022. Accessed January 2023.

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