Understanding Buprenorphine: A Key Opioid Medication
Buprenorphine is a partial opioid agonist used extensively in medication-assisted treatment (MAT) for Opioid Use Disorder (OUD) and for managing severe pain [1.2.1]. First approved in the U.S. in 1981, it is classified as a Schedule III controlled substance [1.2.1]. As a partial agonist, it binds to and activates the same mu-opioid receptors in the brain as full opioids like heroin or fentanyl, but its effects are weaker [1.5.1, 1.3.2]. This action helps to diminish withdrawal symptoms and cravings without producing the same intense euphoria, which lowers its potential for misuse [1.5.1].
One of buprenorphine's most significant safety features is its "ceiling effect" [1.3.2]. This means that at higher doses, its effects on respiratory depression plateau, reducing the risk of overdose compared to full opioid agonists [1.3.2, 1.3.3]. Due to its high affinity for opioid receptors, buprenorphine can also block other opioids from binding, meaning if a person relapses, they are less likely to experience a euphoric high [1.3.3].
Buprenorphine-Only Medications
Several medications contain only buprenorphine and are prescribed for both OUD and chronic pain management. They come in multiple formulations tailored to different patient needs [1.2.7].
- Sublocade (extended-release injection): A once-monthly subcutaneous injection used for OUD in patients who have already started treatment with a sublingual buprenorphine product [1.2.1].
- Brixadi (extended-release injection): Another subcutaneous injection for OUD, which can be administered either weekly or monthly [1.2.1, 1.2.2].
- Butrans (transdermal patch): A patch applied to the skin every seven days to manage severe, chronic pain that requires around-the-clock treatment [1.2.1, 1.2.7].
- Belbuca (buccal film): A film that is applied to the inside of the cheek every 12 hours for chronic pain management [1.2.1, 1.2.7].
- Buprenex (injection): An injectable form used in medical settings for moderate to severe pain, which can be administered intravenously or intramuscularly [1.2.1, 1.2.7].
- Subutex (sublingual tablets): This was one of the original buprenorphine products for OUD but has been largely discontinued [1.2.1]. Generic sublingual buprenorphine tablets are still available [1.2.2].
Buprenorphine and Naloxone Combination Medications
To deter misuse, particularly via injection, buprenorphine is often combined with naloxone, an opioid antagonist [1.7.2, 1.7.5]. Naloxone has poor absorption when taken sublingually (under the tongue) or buccally (inside the cheek) as prescribed [1.3.2, 1.7.7]. However, if the combination product is dissolved and injected, the naloxone becomes active and can rapidly induce unpleasant withdrawal symptoms in someone dependent on opioids [1.7.2, 1.7.6]. This mechanism discourages parenteral abuse [1.7.7].
These combination products are a cornerstone of OUD treatment [1.2.2]:
- Suboxone (sublingual film or tablet): A widely used medication that dissolves under the tongue or in the cheek [1.2.2, 1.6.4]. It is available in multiple strengths.
- Zubsolv (sublingual tablet): These tablets have a different formulation than Suboxone and are noted for higher bioavailability, meaning a lower dose can achieve a similar effect [1.6.1, 1.6.3]. It also features a menthol flavor [1.6.1].
- Generic Buprenorphine and Naloxone: Tablets and films are also available in generic forms [1.2.2].
Comparison of Common Buprenorphine Medications
| Medication | Active Ingredients | Formulation | Administration Frequency | Primary Use |
|---|---|---|---|---|
| Suboxone | Buprenorphine, Naloxone | Sublingual Film/Tablet | Daily [1.6.2] | Opioid Use Disorder [1.2.2] |
| Zubsolv | Buprenorphine, Naloxone | Sublingual Tablet | Daily [1.6.1] | Opioid Use Disorder [1.2.2] |
| Sublocade | Buprenorphine | Subcutaneous Injection | Monthly [1.2.1, 1.6.2] | Opioid Use Disorder [1.2.1] |
| Butrans | Buprenorphine | Transdermal Patch | Every 7 days [1.2.1] | Severe Chronic Pain [1.2.1] |
| Belbuca | Buprenorphine | Buccal Film | Every 12 hours [1.2.1] | Severe Chronic Pain [1.2.1] |
Common and Serious Side Effects
Like all medications, those containing buprenorphine have potential side effects. It's important to discuss these with a healthcare provider.
Common side effects include [1.5.1, 1.5.2]:
- Headache
- Nausea and vomiting
- Constipation
- Drowsiness and fatigue
- Sweating
- Mouth numbness or irritation (with oral forms)
- Insomnia
The FDA has also warned about the risk of dental problems, including cavities and tooth decay, with buprenorphine medicines dissolved in the mouth [1.5.2, 1.5.3]. To mitigate this risk, patients should take a large sip of water after the medication has dissolved, swish it gently, and swallow. It is also recommended to wait at least one hour before brushing teeth [1.5.2, 1.5.3].
Serious side effects can include [1.5.1, 1.5.5]:
- Respiratory distress, especially when mixed with other depressants like alcohol or benzodiazepines
- Adrenal insufficiency
- Liver problems
- Dependence and withdrawal
- Risk of overdose
Conclusion
Buprenorphine is a versatile and vital medication available in numerous formulations and brand names, each designed to meet specific needs for treating Opioid Use Disorder or managing severe pain. From daily oral films like Suboxone to long-acting injections like Sublocade, these medications provide effective, evidence-based options that reduce cravings and withdrawal symptoms, supporting individuals on their path to recovery [1.3.4, 1.5.1]. The addition of naloxone in many products serves as an important deterrent against misuse [1.7.2]. A healthcare provider can determine the most appropriate medication and dosage for an individual's specific circumstances.
For more information, you can visit the Substance Abuse and Mental Health Services Administration (SAMHSA). [1.5.1]
