How Does Buprenorphine Work? Pharmacists Answer 6 FAQs

Opioid use disorder (OUD) is a serious medical condition that affects over 2.5 million people in the U.S. Medication for opioid use disorder (MOUD) is the gold standard for treating OUD. This approach involves taking 1 of 3 FDA-approved medications for OUD. It can also involve behavioral therapies and counseling. 

Buprenorphine is one of the medications that’s FDA approved to treat OUD. It can help reduce opioid cravings, ease withdrawal symptoms, and save lives by lowering the risk of death from opioid overdose.

Buprenorphine and buprenorphine-containing products, like Suboxone (buprenorphine / naloxone), work in unique ways. If you or a loved one has OUD, understanding how buprenorphine works, along with the research on its safety and efficacy, can help you decide if the medication is a good option for you.

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Below, we cover the answers to six frequently asked questions about buprenorphine.

1. How does buprenorphine work?

Buprenorphine is considered an opioid (scientifically known as an opioid agonist). So it has some similarities to typical opioids like oxycodone (Roxicodone, Oxycontin), hydrocodone / acetaminophen, and tramadol (Qdolo, Conzip). Like these opioids, buprenorphine attaches to opioid receptors (binding sites). This is how opioids relieve pain. But it also causes the following opioid side effects:

• Drowsiness

• Nausea

• Constipation

• Slowed breathing, which can lead to an overdose

But buprenorphine is different from typical opioids because it’s only a partial opioid agonist. This makes it less likely to cause the side effects discussed above, including overdose.

Buprenorphine works by performing unique actions at four receptors:

• Activates the mu (μ) opioid receptor: Buprenorphine attaches more strongly to this receptor than typical opioids. But it doesn’t fully activate the receptor the way other opioids do. So it doesn’t cause a “high,” and there’s a lower risk of opioid side effects, including a lower risk for slowed breathing and misuse. Binding to the mu opioid receptor relieves withdrawal symptoms and cravings for opioids in people with OUD. It also relieves pain in people with chronic pain.

• Blocks the delta (δ) opioid receptor: This helps minimize opioid side effects like constipation and slowed breathing.

• Blocks the kappa (κ) opioid receptor: This helps minimize typical opioid side effects. It may also help improve depression symptoms and decrease the risk of suicidal thoughts and behaviors.

• Activates the opioid receptor-like 1 (ORL1) receptor: This may contribute to pain relief. It may also mean there’s a lower risk for misuse with buprenorphine than with typical opioids.

While the long-term effects of buprenorphine on the brain aren’t fully known, some research shows that taking buprenorphine improves brain function over time for people with OUD. This is important because OUD has been shown to change brain structure and function.

2. What are buprenorphine and buprenorphine / naloxone used for?

Some buprenorphine products are approved to treat OUD. Others are approved to treat chronic pain.

OUD

Along with counseling and other mindfulness practices, buprenorphine products can be an effective part of an OUD treatment plan. Even when used alone, buprenorphine can be lifesaving. For example, a study of over 17,500 people found that people taking buprenorphine had a lower risk of opioid overdose death than those not taking medication for OUD.

The FDA-approved buprenorphine products for OUD are:

• Buprenorphine sublingual (dissolved under the tongue) tablets 

• Buprenorphine extended-release injection (Sublocade, Brixadi)

• Buprenorphine / naloxone sublingual film (Suboxone)

• Buprenorphine / naloxone sublingual tablets (Zubsolv)

Chronic pain

Though some buprenorphine products are approved for chronic pain, it’s not a first-choice medication for pain. Opioids, including buprenorphine, are only meant to be used for moderate-to-severe pain that isn’t relieved by non-opioid medications. If buprenorphine is prescribed for pain, it’s usually in one of two situations:

1. If you have a pain condition and a history of OUD: Even if non-opioid medications don’t work for your pain, you’ll want to avoid taking opioids for pain relief if you have a history of OUD. Since buprenorphine is a partial opioid agonist, it has a different effect on the body than full opioids and may be a safe option.

2. If you’re prescribed opioids for chronic pain but you don’t have adequate pain control: Some experts believe that long-term opioid use can cause opioid-induced hyperalgesia. This is when people become more sensitive to pain after taking opioids for a while. Buprenorphine may decrease your sensitivity to pain, providing more pain relief than a full opioid.

The forms of buprenorphine that are FDA approved to treat chronic pain are:

• A buccal film (Belbuca) that’s placed between the gum and cheeks

• A transdermal (skin) patch (Butrans)

3. Why is buprenorphine combined with naloxone in some medications?

Some buprenorphine products approved to treat OUD also contain naloxone. Naloxone is an opioid antagonist medication, meaning it blocks the effects of opioids. In fact, you may have heard of injectable or nasal naloxone products — like Narcan or Zimhi — that are used to reverse an opioid overdose.

Historically, the naloxone component in Suboxone and Zubsolv was thought to keep people from misusing the medications. The idea is that naloxone can block the effects of buprenorphine if it's misused (injected). However, some evidence suggests this isn’t true.

Regardless of which buprenorphine product you use, taking it exactly as prescribed is the best way to prevent misuse. And know that when taken by mouth, naloxone isn’t absorbed well and has little effect.

4. Is buprenorphine a controlled substance?

Yes, all buprenorphine products are controlled substances. Controlled substances have a higher risk for dependence and misuse compared to non-controlled substances. So there are restrictions on how they’re prescribed and refilled.

Taking buprenorphine can lead to dependence and misuse. This increases your risk of serious side effects like overdose and death. However, when used under the guidance of a trained healthcare professional, buprenorphine can be an effective part of an OUD or chronic pain treatment plan.

5. Is buprenorphine safe? And what should you avoid while taking it?

When prescribed by a trained healthcare professional, buprenorphine is considered safe. But following best practices for how to take buprenorphine is important. These actions can significantly decrease your risk of misuse and overdose with buprenorphine:

• Only take buprenorphine exactly as prescribed. Don’t take extra doses of buprenorphine without consulting your prescriber. If you have OUD and you’re having opioid cravings, talk to your prescriber about whether you need a dosage increase. And if you’re taking buprenorphine for chronic pain but not experiencing pain relief, let your prescriber know. But don’t make any changes to your dosage without talking to your prescriber first. Increasing your dosage on your own can lead to overdose.

• Avoid taking buprenorphine with other medications that can slow your breathing. Certain medications — including opioids, benzodiazepines, and non-benzodiazepine sedative hypnotics (“Z-drugs”) — can slow your breathing and increase your risk of overdose when combined with buprenorphine. In most cases, it’s best to avoid these medications while taking buprenorphine.

• Avoid drinking alcohol while taking buprenorphine. Alcohol can slow down your brain and your breathing. Taking it with buprenorphine can increase your risk of overdose.

6. What are some alternatives to buprenorphine?

There is no one-size-fits-all treatment plan for OUD or chronic pain. The best plan for you depends on several personal factors. Your healthcare professional can help you determine what your options are if you’re interested in alternatives to buprenorphine.

OUD medication alternatives

Buprenorphine-containing products are one of three FDA-approved medications for treating OUD. The other two medications are:

• Methadone (Methadose): This is a full opioid agonist. It works similarly to typical opioids, but its effects last a long time and it works more slowly. It can only be prescribed through licensed opioid treatment programs (OTPs), so you’ll need to go to a clinic everyday when you first start taking it. It’s also more likely to cause opioid side effects like constipation and nausea. But it may work better than buprenorphine for some people.

• Naltrexone: Naltrexone is also a full opioid antagonist. It comes in oral and injectable (Vivitrol) forms. The oral form isn’t recommended for OUD, but the injection (given in the muscle) may be an option. In general, naltrexone isn’t as effective as buprenorphine or methadone for treating OUD.

Chronic pain treatment alternatives

As mentioned previously, opioids, including buprenorphine, aren’t first-choice options for treating chronic pain. So it’s possible that your healthcare professional will want you to try several other treatment options before trying buprenorphine. There are many options for treating chronic pain, including lifestyle changes, medications, and medical procedures. 

Read this GoodRx Health article to learn more about chronic pain treatment options.

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Written by:

Amy B. Gragnolati, PharmD, BCPS

Amy Gragnolati, PharmD, BCPS, is a pharmacy editor for GoodRx. Amy currently holds her pharmacist license in Georgia and California.

Reviewed by:

Karen Hovav, MD, FAAP

Karen Hovav, MD, FAAP, has more than 15 years of experience as an attending pediatrician in a variety of clinical settings. She has worked in a large academic center in an urban city, a small community hospital, a private practice, and an urgent care clinic.

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If you or someone you know struggles with substance use, help is available. Call SAMHSA’s National Helpline at 1-800-662-4357 to learn about resources in your area.