What is the use of Buprenorphine (partial opioid agonist)?

From the Guidelines

Buprenorphine is a highly effective treatment for opioid use disorder and chronic pain management, with a favorable safety profile due to its ceiling effect on respiratory depression 1.

Key Points

• Buprenorphine is a partial opioid agonist with a high binding affinity for the μ-opioid receptor, making it beneficial for treating opioid use disorder and chronic pain 1.
• The medication is available in several formulations, including sublingual tablets/films, monthly injectable forms, and implants, with the transdermal patch being approved for chronic pain management 1.
• Treatment typically begins with an induction dose of 2-4mg sublingually, titrated up to a maintenance dose of 8-24mg daily, with the goal of reducing cravings and withdrawal symptoms while minimizing the risk of overdose 1.
• Buprenorphine has been shown to be effective in preventing relapse among patients with opioid use disorder, with some studies suggesting that combining it with behavioral therapies can improve treatment outcomes 1.
• The medication is generally well-tolerated, with common side effects including headache, nausea, constipation, insomnia, and sweating, although higher doses may be associated with more pronounced side effects 1.

Clinical Considerations

• Clinicians should consider switching patients from buprenorphine/naloxone to buprenorphine transdermal alone for chronic pain management, as the transdermal patch may provide better analgesia and fewer adverse events 1.
• When treating acute episodes of pain, clinicians may need to consider adding high-potency opioids such as fentanyl or hydromorphone to buprenorphine, as the medication may not provide adequate analgesia on its own 1.
• Patients should be aware of the potential for buprenorphine to precipitate withdrawal if taken too soon after other opioids, highlighting the importance of proper induction timing 1.

Recommendations

• Buprenorphine should be considered a first-line treatment for opioid use disorder due to its favorable safety profile and effectiveness in reducing illicit opioid use and overdose risk 1.
• Clinicians should work to ensure sufficient treatment capacity for opioid use disorder at the practice level, including identifying community resources and providing medication-assisted treatment with buprenorphine or methadone in combination with behavioral therapies 1.

From the FDA Drug Label

The FDA drug label does not answer the question.

From the Research

Buprenorphine Treatment

• Buprenorphine is a highly effective treatment for opioid use disorder, with a treatment retention rate of more than 50% at 1 year and substantially less risk of respiratory depression compared with methadone 2.
• The optimal dose of buprenorphine in opioid use disorder treatment is not well established, but doses under 8 mg are insufficient to produce opioid receptor blockade, and doses higher than 16 mg may not confer added blockade benefit 3.
• Buprenorphine treatment should be individualized based on a continuous clinical benefit-risk assessment, and further research is needed to better understand the relationship between dose and efficacy over time in patients with opioid use disorder 3.

Efficacy and Safety

• Buprenorphine has been shown to be effective for the treatment of opioid use disorder, with a lower risk of diversion and improved adherence compared with other treatments 4.
• Buprenorphine is a maintenance treatment for a chronic disease and should be continued for as long as it is beneficial, with relapse rates after discontinuation lower in patients who complete 1 year of treatment 2.
• Counseling or behavior therapy is not necessary for success and should be offered based on each patient's needs and preferences, with regular urine drug testing helping to identify patients who may benefit from more intense treatment or other options 2.

Treatment Guidelines

• Physicians should screen adult patients with a validated tool and offer buprenorphine to those with moderate or severe opioid use disorder, with doses titrated quickly to fully suppress cravings and withdrawal symptoms, typically 16 to 32 mg/day 2.
• Treatment choices in opioid use disorder pharmacotherapy should be based on the needs of the individual and characteristics of medications, with access to opioid agonist therapy prioritized in the treatment of opioid use disorder 5.
• Special groups, such as pregnant women, prisoners, and patients with mental health problems, have specific needs that must be addressed with expert input 5.