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Buprenorphine’s Mechanism of Action (MOA)

Elena Hill, MD, MPH profile image
Medically Reviewed By Elena Hill, MD, MPH • Updated Feb 2, 2023 • 4 cited sources

Buprenorphine’s mechanism of action is that it binds to the brain’s mu-opioid receptors, reducing drug cravings, preventing withdrawal, and blocking the effects of other opioids. 

It has been shown in numerous studies to treat opioid use disorder. It is one of three FDA approved medications to treat OUD. 

What Is Buprenorphine?

Buprenorphine is a medication approved by the FDA for use in Medication for Addiction Treatment (MAT) for opioid use disorder (OUD).[1] It is a long-acting opioid partial agonist. This means it acts in a way that is similar to commonly misused full opioid agonists, like heroin or fentanyl, but with a significantly less intense effect. 

Buprenorphine is useful for a number of reasons, including its ability to suppress opioid cravings and eliminate withdrawal symptoms without producing a “high”. While it has some misuse potential, it is far lower than that associated with “full” opioids people typically misuse. [1] 

What is A Mechanism of Action (MOA)?

A substance’s mechanism of action (MOA) is the way in which it works or produces an effect on the body.[2] If we understand how a drug works in the body, we can better understand what effects it will have at different doses and what side effects it may cause. 

What Is Buprenorphine’s Mechanism of Action?

Buprenorphine works by imperfectly binding to the brain’s mu-opioid receptors. In this way, it “fills up” those opioid receptors as a substitution for other opioids, preventing the craving and withdrawal symptoms that would otherwise occur if those receptors were empty. 

At the same time, Suboxone is a “partial” opioid agonist, meaning that even though it binds to those opioid receptors, it does not “turn them on” as forcefully as a full opioid, meaning it does not cause the “high’ or euphoric effects of full opioids. In addition, this “partial” opioid effect means it does not reduce respiratory drive and cause respiratory depression anywhere near as much as a full opioid. That means the risk of overdose is essentially zero with Suboxone as compared to full opioid agonists. 

This also means that, while Suboxone is in the body, if additional opioids are taken, they do not bind to receptors, and their effects will be blunted, preventing overdose from full opioids while Suboxone is still on board in the body. 

Buprenorphine’s Effect on the Body

Buprenorphine can cause a mild euphoria and low level of respiratory depression in opioid-naïve users. However, these side effects are less common in “opioid experienced” patients whose bodies are already accustomed to opioid medications. There are a few common side effects associated with buprenorphine use, including these:

  • Constipation,nausea, and vomiting
  • Disturbance in attention
  • Dizziness
  • Drowsiness and fatigue
  • Dry mouth
  • Inability to sleep
  • Palpitations
  • Sweating
  • Tooth decay

It is sometimes difficult for people new to buprenorphine treatment to differentiate between the effects of their MAT and the general stress of opioid withdrawal, which can also cause a lot of these overlapping symptoms. 

In general, if a person taking buprenorphine or any other medication experiences a symptom (whether on the list above or not) that seems like it may be serious or is impacting their quality of life, they should talk with a doctor. Often, small adjustments can be made to their treatment to lessen the severity of unwanted symptoms. 

Also bear in mind that, just like with any new medication, many of these side effects will be temporary and will abate as your body gets used to the medication. 

Effectiveness of Buprenorphine Treatment for OUD

Buprenorphine treatment for OUD has been shown to successfully treat OUD, including risk of relapse, overdose and death. 

For example: one Swedish study found that patients treated with Suboxone are 1.82 times more likely (almost twice as likely) to stay in treatment and avoid opioid use as compared to patients that did not take Suboxone. [4] Suboxone also decreased the rate of opioid-positive drug tests by 14.2%.[4] 

Suboxone is known to be so effective for treating OUD that it was approved by the FDA for this use in 2002. Currently, it is one of three FDA approved medications to treat OUD.

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 ... Read More

  1. Buprenorphine. Substance Abuse and Mental Health Services Administration. September 2022. Accessed December 2022. 
  2. NCI Dictionary of Cancer Terms: Mechanism of Action. National Cancer Institute. Accessed December 2022.
  3. Suboxone: Rationale, Science, Misconceptions. The Ochsner Journal. 2018. Accessed December 2022.
  4. How Effective Are Medications to Treat Opioid Use Disorder? National Institute on Drug Abuse. December 2021. Accessed December 2022.
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