Why Does Buprenorphine Contain Naloxone?

October 12, 2022

Table of Contents

Buprenorphine is combined with naloxone in the medication called Suboxone.

Naloxone is a deterrent to abuse as it will trigger withdrawal symptoms if the medication is abused. This helps to prevent the misuse of Suboxone. Learn how it works here.

What Is Buprenorphine & How Is It Used?

Buprenorphine is a partial opioid agonist that is used as medication for addiction treatment (MAT) for opioid use disorder (OUD).[1] It is administered as a tablet, sublingual or buccal film, implant, or injection.

As a partial opioid agonist, buprenorphine does not produce the same “high” that full opioid agonists like fentanyl, heroin and oxycodone do. However, it provides enough opioid activity that it prevents cravings and eliminates withdrawal symptoms from full opioids. In this way, it serves as a treatment for OUD. 

Why Is Naloxone Combined With Buprenorphine?

Naloxone is added to buprenorphine in Suboxone as an additional abuse-deterrent.

When Suboxone is dissolved under the tongue, the naloxone component is not readily absorbed because it has a low bioavailability and sublingual absorption rate compared to buprenorphine.[2] Therefore, when taken sublingually as directed, naloxone is not absorbed and the patient only experiences the effects of the buprenorphine. 

However, naloxone becomes active if Suboxone is injected intravenously. If a patient tries to inject Suboxone, the naloxone will be absorbed along with the buprenorphine, binding preferentially to the body’s opioid receptors and preventing the patient from getting “high” off Suboxone. 

This prevents misuse of the medication and also prevents an overdose. The addition of naloxone to buprenorphine therefore prevents misuse of the medication.

Is This Combination Safe?

Combination medications with both buprenorphine and naloxone are safe and effective for treating opioid use disorder (OUD). Naloxone does not absorb at the same rate as buprenorphine, with less than 10% bioavailability through sublingual absorption. Therefore, if taken appropriately, the only medication that enters the body is Buprenorphine. Moreover, Naloxone is a very safe medication and has very few side effects. Rates of allergy to this medication are exceedingly low. 

Combination medications also contain more buprenorphine than naloxone, generally at a ratio of 4 to 1.[3] These are examples of medications containing buprenorphine and naloxone for the treatment of OUD:[4]

  • Suboxone: 2 mg buprenorphine/0.5 mg naloxone; 4 mg buprenorphine/1 mg naloxone; 8 mg buprenorphine/2 mg naloxone; 12 mg buprenorphine/3 mg naloxone
  • Zubsolv: 0.7 mg buprenorphine/0.18 mg naloxone; 1.4 mg buprenorphine/0.6 mg naloxone; 2.9 mg buprenorphine/0.71 mg naloxone; 5.7 mg buprenorphine/1.4 mg naloxone; 8.6 mg buprenorphine/2.1 mg naloxone; 11.4 mg buprenorphine/2.9 mg naloxone
  • Bunavail: 2.1 mg buprenorphine/0.3 mg naloxone; 4.2 mg buprenorphine/0.7 mg naloxone; 6.3 mg buprenorphine/1 mg naloxone
  • Cassipa: 16 mg buprenorphine/4 mg naloxone

Effectiveness of Buprenorphine & Naloxone in OUD Treatment 

Suboxone is remarkably effective in treating OUD. In one study of people recovering from heroin use disorder, nearly 90% of people using Suboxone were still abstinent after 8 months. [5] In another study, 82% of people who used both methadone and Suboxone preferred Suboxone.[6] Since this medication can be taken at home (rather than in a doctor's office or another clinical setting), it's much more convenient, which could keep people engaged in treatment longer.[7]

If you are recovering from an opioid use disorder and think Suboxone might be helpful, talk to your doctor or reach out to us here at Bicycle health for more information.

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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Citations

  1. Buprenorphine. Substance Abuse and Mental Health Services Administration. https://www.samhsa.gov/medication-assisted-treatment/medications-counseling-related-conditions/buprenorphine. May 2021. Accessed January 2022. 
  2. Reconsidering the Usefulness of Adding Naloxone to Buprenorphine. Frontiers in Psychology. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7517938/. September 2020. Accessed January 2022.
  3. Suboxone: Rationale, Science, Misconceptions. The Ochsner Journal. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5855417/. Spring 2018. Accessed January 2022.
  4. Buprenorphine/Naloxone (Suboxone). National Alliance on Mental Illness. https://www.nami.org/About-Mental-Illness/Treatments/Mental-Health-Medications/Types-of-Medication/Buprenorphine/Buprenorphine-Naloxone-(Suboxone). Accessed January 2022.
  5. Medically Assisted Recovery From Opiate Dependence Within the Context of the UK Drug Strategy (Buprenorphine-Naloxone) Patients Compared. Journal of Substance Abuse Treatment. https://www.sciencedirect.com/science/article/abs/pii/S0740547212000803. January 2013. Accessed August 2022. 
  6. Suboxone Efficacy in Treating Drug Addiction: Comparison with Methadone and Monitoring of Patients in Therapy at SERT of Masala. IRIS UniPA. https://iris.unipa.it/handle/10447/244120. 2017. Accessed August 2022. 
  7. The Efficacy of Suboxone as Part of Treatment for Opioid Use Disorder. Lynchburg Journal of Medical Science. https://digitalshowcase.lynchburg.edu/dmscjournal/vol2/iss2/23/. 2020. Accessed August 2022.
  8. Long-Term Suboxone Treatment and Its Benefit on Long-Term Remission for Opiate Dependence. Journal of Psychiatry. https://citeseerx.ist.psu.edu/viewdoc/download?doi=10.1.1.682.3650&rep=rep1&type=pdf. 2014. Accessed August 2022.

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