Why Does Buprenorphine Contain Naloxone?

Buprenorphine is combined with naloxone in the opioid use disorder (OUD) medication called Suboxone. Buprenorphine is a partial opioid agonist that relieves opioid withdrawal symptoms and cravings. Naloxone, an opioid antagonist, is added to buprenorphine to deter misuse of this medication. Naloxone acts as a misuse-deterrent because it will trigger precipitated withdrawal symptoms if someone injects or snorts Suboxone.

What Does Naloxone Do in Suboxone?

What Is Buprenorphine & How Is It Used?

Buprenorphine is a partial opioid agonist that is used as a 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 euphoric high that full opioid agonists like fentanyl, heroin and oxycodone do. However, it provides enough opioid activity that it prevents opioid cravings and eliminates withdrawal symptoms. In this way, it serves as a treatment for OUD.

That said, some people may attempt to misuse buprenorphine because of its opioid effects. That’s where naloxone comes in.

Why Is Naloxone Combined With Buprenorphine?

‍Naloxone is combined with buprenorphine in Suboxone as an additional misuse-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 Suboxone is taken sublingually as directed, naloxone is not absorbed and the patient only experiences the therapeutic effects of the buprenorphine. 

However, naloxone becomes active if Suboxone is injected or snorted. If a patient tries to misuse 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. [2]

Misusing Naloxone/Buprenorphine Results in Precipitated Withdrawal

If someone snorts or injects Suboxone, they will go into immediate precipitated withdrawal, which includes distressing symptoms, such as: [8]

• Sweating
• Muscle and bone pain
• Insomnia
• Runny nose and teary eyes
• Agitation and anxiety
• Diarrhea, nausea and stomach cramps

Knowing that misusing Suboxone won’t result in euphoria and will cause precipitated withdrawal can prevent misuse of the medication and also prevent a Suboxone overdose. 

Naloxone vs. Suboxone

Naloxone is an opioid antagonist that, on its own, is a medication that can rapidly reverse the life-threatening effects of an opioid overdose. 

When it’s combined with buprenorphine, it’s an “inactive” ingredient and only becomes active if the medication is misused. It prevents people from misusing their OUD medication and helps maintain recovery. 

Suboxone, on the other hand, is the brand name for the combination medication consisting of buprenorphine and naloxone. Suboxone is prescribed to treat opioid use disorder, whereas naloxone, on its own, is not.

Are Buprenorphine and Naloxone Safe?

Yes, 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 is absorbed by 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 and 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.