What is Buprenorphine (BUPE)?

From the Guidelines

Buprenorphine (BUPE) is a partial opioid agonist with a high binding affinity for the μ-opioid receptor, making it a beneficial treatment for opioid use disorder and chronic pain management. This medication works by activating opioid receptors to a lesser degree than full agonists, reducing cravings and withdrawal symptoms in individuals dependent on opioids while producing limited euphoria and respiratory depression 1. The high affinity of buprenorphine for opioid receptors also blocks the effects of other full opioid agonists, providing a safer alternative for patients in recovery from opioid addiction.

Key Characteristics of Buprenorphine

• High binding affinity for the μ-opioid receptor, which diminishes the ability of other more potent full agonist opioids to dislodge it from the receptor 1
• Available in various formulations, including sublingual tablets, sublingual films, 6-month implants, and transdermal patches, each approved for specific indications such as opioid use disorder or chronic pain management
• Can be prescribed off-label for pain management, but the transdermal patch is specifically approved for chronic pain and cannot be prescribed off-label for opioid use disorder

Clinical Considerations

• During acute episodes of pain, buprenorphine may pose challenges in achieving analgesia compared to other opioids like methadone, but its dose can be increased to provide additional analgesia 1
• The ceiling effect of buprenorphine on respiratory depression has been verified, but its ceiling effect on analgesia is less clear, suggesting potential benefits at higher doses for pain management 1
• For patients on buprenorphine for opioid use disorder who experience chronic pain, switching to a transdermal buprenorphine patch may provide better analgesia and safety compared to full opioid agonists 1

Treatment Approaches

• Buprenorphine can be used in conjunction with other treatments for chronic pain, including nonpharmacologic therapies and nonopioid pharmacotherapies, with the option to add high-potency opioids like fentanyl or hydromorphone if necessary 1
• The choice of buprenorphine formulation and dosage should be tailored to the individual patient's needs, considering factors such as the severity of opioid use disorder, the presence of chronic pain, and the patient's medical history and current medications.

From the FDA Drug Label

Buprenorphine (bue” pre nor’ feen) Sublingual Tablets CIII Rx Only Buprenorphine Sublingual Tablets contain an opioid that can cause physical dependence. What is Buprenorphine Sublingual Tablets Buprenorphine Sublingual Tablets are a prescription medicine used to begin treatment in adults who are addicted to (dependent on) opioid drugs (either prescription or illegal drugs), as part of a complete treatment program that also includes counseling and behavioral therapy.

Buprenorphine (BUPE) is a prescription medicine, specifically an opioid, used to treat adults addicted to opioid drugs as part of a complete treatment program including counseling and behavioral therapy 2.

From the Research

Definition and Properties of Buprenorphine

• Buprenorphine is a partial mu-opioid receptor agonist, which is used for the treatment of opioid addiction and chronic pain 3.
• It has a superior safety profile compared to methadone, a full mu-opioid receptor agonist, and is formulated for sublingual administration 3.
• Buprenorphine can be initiated and maintained through primary care, has a low risk for overdose, but needs to be started only when moderate withdrawals have begun 4.

Uses of Buprenorphine

• Buprenorphine is used as a medication-assisted treatment (MAT) for opioid use disorder, and it has been shown to reduce relapse and harm reduction 4, 3.
• It is also used for the treatment of chronic pain, especially in the elderly, as it may be associated with less cognitive impairment, falls, sexual dysfunction, and sarcopenia compared to schedule II opioids 5.
• Buprenorphine may be useful in patients with comorbid substance use disorder or non-medical opioid use, as there is less risk of misuse and euphoria, and it may improve mood 5.

Administration and Efficacy

• Buprenorphine can be administered sublingually, and a subdermal implant with a 6-month duration of action is being considered for approval by the U.S. Food and Drug Administration 3.
• A monthly buprenorphine depot injection, known as BUP-XR, has been shown to be effective in reducing opioid use and improving treatment outcomes, with a safety profile consistent with other buprenorphine products 6.
• The efficacy of buprenorphine in treating opioid use disorder has been demonstrated in several studies, with significant reductions in illicit opioid use and improvements in treatment retention 4, 3, 6.

Initiating Buprenorphine Treatment

• There is no single recommended approach for buprenorphine initiation, and different methods, such as standard, low-dose, bridging-strategy, and naloxone-facilitated initiation techniques, may be used 7.
• Buprenorphine initiation should be guided by the patient's individual needs and medical history, and providers should be aware of the complex pharmacologic properties and varying government regulations surrounding its use 7.