What is Buprenorphine?
Buprenorphine is a synthetic opioid derived from thebaine that acts as a partial opioid agonist. Unlike full opioid agonists such as morphine or heroin, buprenorphine produces a "ceiling effect"—its opioid effects, such as euphoria and respiratory depression, level off at moderate doses. This unique pharmacological property makes it a safer option for treating opioid use disorder (OUD) by reducing cravings and withdrawal symptoms while also lowering the risk of misuse and overdose. In lower doses, buprenorphine is also effective for managing moderate to severe chronic pain.
Buprenorphine Products for Opioid Use Disorder (OUD)
For the treatment of OUD, buprenorphine is most commonly combined with naloxone in order to deter misuse. Naloxone is an opioid antagonist that has poor bioavailability when taken sublingually but can precipitate withdrawal symptoms if the medication is injected, thus discouraging that route of administration. Several different product types are available for OUD treatment.
Sublingual Tablets and Films
Sublingual formulations are designed to be placed under the tongue, where they dissolve and are absorbed into the bloodstream. This route avoids first-pass metabolism in the liver, increasing the medication's bioavailability.
- Suboxone (buprenorphine and naloxone) film and tablet: A combination product widely used for maintenance treatment of OUD.
- Zubsolv (buprenorphine and naloxone) sublingual tablet: Another combination product with a unique formulation designed for faster dissolving.
- Buprenorphine (generic Subutex) sublingual tablet: This monoproduct contains buprenorphine without naloxone and is sometimes prescribed for specific situations, such as during pregnancy, though the brand-name Subutex was discontinued.
- Bunavail (buprenorphine and naloxone) buccal film: A film applied to the inside of the cheek that has a high bioavailability.
Extended-Release Injections and Implants
Long-acting formulations offer an alternative to daily dosing, potentially improving medication adherence and reducing the risk of diversion.
- Sublocade (buprenorphine) extended-release injection: A monthly subcutaneous injection administered by a healthcare professional.
- Brixadi (buprenorphine) extended-release injection: Available as both a weekly and monthly subcutaneous injection, also administered in a clinical setting.
- Probuphine (buprenorphine) subdermal implant: A set of four rods surgically implanted under the skin of the upper arm, providing a constant dose for up to six months. It is used for patients who are clinically stable on low-to-moderate doses of a transmucosal buprenorphine product.
Buprenorphine Products for Pain Management
Lower-dose buprenorphine products are used to manage moderate to severe chronic pain that requires continuous opioid treatment. The dosage for pain is much lower than for OUD, and these formulations do not typically include naloxone.
- Butrans (buprenorphine) transdermal patch: This weekly patch provides continuous, around-the-clock opioid analgesia for patients with chronic pain.
- Belbuca (buprenorphine) buccal film: A dissolving film placed inside the cheek for chronic pain management, with doses taken every 12 hours.
- Buprenex (buprenorphine) injection: An injectable formulation typically reserved for short-term, acute pain management in hospital settings.
Comparison of Key Buprenorphine Medications
| Feature | Suboxone (Sublingual Film) | Butrans (Transdermal Patch) | Sublocade (Extended-Release Injection) |
|---|---|---|---|
| Primary Use | Opioid Use Disorder (OUD) | Chronic Pain Management | Opioid Use Disorder (OUD) |
| Formulation | Film dissolved under the tongue | Patch applied to the skin | Subcutaneous injection |
| Frequency | Once daily | Once every 7 days | Once monthly |
| Buprenorphine/Naloxone | Yes, contains both | No, buprenorphine only | No, buprenorphine only |
| Administration | Self-administered at home | Self-administered at home | Administered by a healthcare provider |
| Primary Advantage | Prevents withdrawal and deters misuse | Continuous, stable pain relief | Improves adherence, reduces diversion risk |
| Key Disadvantage | Risk of misuse if crushed/injected | Not for acute pain; potential skin reactions | Requires clinic visits; no immediate dose flexibility |
The Role of Naloxone in OUD Medications
The inclusion of naloxone in medications like Suboxone and Zubsolv serves a specific purpose: to deter illicit injection. When taken as prescribed, the buprenorphine is absorbed effectively, while the naloxone is poorly absorbed, having little to no effect. However, if an individual attempts to inject the dissolved medication, the naloxone becomes active and blocks the opioid receptors, triggering immediate opioid withdrawal symptoms. This built-in safeguard significantly reduces the street value and abuse potential of the medication.
New Regulations and Increased Access
Regulatory changes have aimed to expand access to buprenorphine treatment for OUD. The federal requirement for a special training waiver (X-waiver) for practitioners to prescribe buprenorphine was eliminated in 2023, allowing more clinicians to offer this life-saving treatment in their offices. This move is intended to address the ongoing opioid epidemic by making Medication-Assisted Treatment (MAT) more accessible and reducing the barriers to care for those with OUD. This does not mean buprenorphine is available over-the-counter; it is still a controlled substance requiring a prescription and medical supervision.
Conclusion
In summary, the term what drugs contain buprenorphine refers to a diverse range of prescription medications, each tailored for a specific medical purpose. Whether used to treat OUD through sublingual films and long-acting injections or to manage chronic pain via transdermal patches, buprenorphine's partial opioid agonist properties provide a valuable therapeutic tool. The development of various formulations and regulatory changes have made buprenorphine-based treatment more accessible and safer for patients. It is crucial to remember that these medications should always be used as part of a comprehensive treatment plan, under the guidance of a healthcare professional, to maximize their effectiveness and safety. For more information on opioid addiction and treatment options, consult the Substance Abuse and Mental Health Services Administration (SAMHSA) guidelines.
The Role of Naloxone in OUD Medications
The inclusion of naloxone in medications like Suboxone and Zubsolv serves a specific purpose: to deter illicit injection. When taken as prescribed, the buprenorphine is absorbed effectively, while the naloxone is poorly absorbed, having little to no effect. However, if an individual attempts to inject the dissolved medication, the naloxone becomes active and blocks the opioid receptors, triggering immediate opioid withdrawal symptoms. This built-in safeguard significantly reduces the street value and abuse potential of the medication.
Conclusion
In summary, the term what drugs contain buprenorphine refers to a diverse range of prescription medications, each tailored for a specific medical purpose. Whether used to treat OUD through sublingual films and long-acting injections or to manage chronic pain via transdermal patches, buprenorphine's partial opioid agonist properties provide a valuable therapeutic tool. The development of various formulations and regulatory changes have made buprenorphine-based treatment more accessible and safer for patients. It is crucial to remember that these medications should always be used as part of a comprehensive treatment plan, under the guidance of a healthcare professional, to maximize their effectiveness and safety. For more information on opioid addiction and treatment options, consult the Substance Abuse and Mental Health Services Administration (SAMHSA) guidelines.
Comparison of Key Buprenorphine Medications
| Feature | Suboxone (Sublingual Film) | Butrans (Transdermal Patch) | Sublocade (Extended-Release Injection) |
|---|---|---|---|
| Primary Use | Opioid Use Disorder (OUD) | Chronic Pain Management | Opioid Use Disorder (OUD) |
| Formulation | Film dissolved under the tongue | Patch applied to the skin | Subcutaneous injection |
| Frequency | Once daily | Once every 7 days | Once monthly |
| Buprenorphine/Naloxone | Yes, contains both | No, buprenorphine only | No, buprenorphine only |
| Administration | Self-administered at home | Self-administered at home | Administered by a healthcare provider |
| Primary Advantage | Prevents withdrawal and deters misuse | Continuous, stable pain relief | Improves adherence, reduces diversion risk |
| Key Disadvantage | Risk of misuse if crushed/injected | Not for acute pain; potential skin reactions | Requires clinic visits; no immediate dose flexibility |
The Role of Naloxone in OUD Medications
The inclusion of naloxone in medications like Suboxone and Zubsolv serves a specific purpose: to deter illicit injection. When taken as prescribed, the buprenorphine is absorbed effectively, while the naloxone is poorly absorbed, having little to no effect. However, if an individual attempts to inject the dissolved medication, the naloxone becomes active and blocks the opioid receptors, triggering immediate opioid withdrawal symptoms. This built-in safeguard significantly reduces the street value and abuse potential of the medication.
Conclusion
In summary, the term what drugs contain buprenorphine refers to a diverse range of prescription medications, each tailored for a specific medical purpose. Whether used to treat OUD through sublingual films and long-acting injections or to manage chronic pain via transdermal patches, buprenorphine's partial opioid agonist properties provide a valuable therapeutic tool. The development of various formulations and regulatory changes have made buprenorphine-based treatment more accessible and safer for patients. It is crucial to remember that these medications should always be used as part of a comprehensive treatment plan, under the guidance of a healthcare professional, to maximize their effectiveness and safety. For more information on opioid addiction and treatment options, consult the Substance Abuse and Mental Health Services Administration (SAMHSA) guidelines.
New Regulations and Increased Access
Regulatory changes have aimed to expand access to buprenorphine treatment for OUD. The federal requirement for a special training waiver (X-waiver) for practitioners to prescribe buprenorphine was eliminated in 2023, allowing more clinicians to offer this life-saving treatment in their offices. This move is intended to address the ongoing opioid epidemic by making Medication-Assisted Treatment (MAT) more accessible and reducing the barriers to care for those with OUD. This does not mean buprenorphine is available over-the-counter; it is still a controlled substance requiring a prescription and medical supervision.
Conclusion
In summary, the question of what drugs contain buprenorphine leads to a diverse list of prescription medications designed for specific purposes, primarily OUD treatment and chronic pain management. Its unique partial agonist properties allow it to alleviate withdrawal symptoms and pain with a lower risk of misuse and overdose compared to full opioid agonists. The wide range of formulations—from films and tablets to long-acting injections and implants—ensures that treatment can be tailored to individual patient needs and circumstances. The inclusion of naloxone in OUD combination products adds an important safety feature against injection misuse. It is crucial for patients and healthcare providers to understand the distinctions between these products to choose the most appropriate and effective treatment plan.
