From the Guidelines
Buprenorphine is a partial opioid agonist, not a full narcotic agonist-antagonist, as it activates the mu-opioid receptors with less intensity than full agonists like morphine or heroin.
Key Characteristics of Buprenorphine
- It has a 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.
- This property is beneficial in the treatment of opioid use disorder and chronic pain, providing analgesia over a long period of time 1.
- Buprenorphine is available in various formulations, including sublingual tablets, sublingual films, 6-month implants for opioid use disorders, and transdermal patches for chronic pain 1.
Clinical Use and Considerations
- For patients on buprenorphine for opioid use disorder who experience chronic pain, switching from buprenorphine/naloxone to buprenorphine transdermal alone may be considered to potentially provide better analgesia 1.
- When pain is acute, high-potency opioids like fentanyl or hydromorphone can be given in addition to buprenorphine, as it does not occupy all opioid receptors 1.
- The perioperative management of buprenorphine involves continuing it, with consideration of tapering higher doses to 12 mg daily preoperatively, although evidence is not conclusive 1.
Safety and Efficacy
- Buprenorphine has a ceiling effect on respiratory depression, making it safer than full opioid agonists in overdose situations 1.
- It has been shown to provide comparable pain relief with fewer adverse events compared to full opioid agonists like transdermal fentanyl and morphine 1.
From the FDA Drug Label
12.1 Mechanism of Action Buprenorphine Sublingual Tablets contain buprenorphine, a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor.
Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor, which can be characterized as an opioid agonist-antagonist. Key points:
- Partial agonist at the mu-opioid receptor
- Antagonist at the kappa-opioid receptor 2
From the Research
Buprenorphine Classification
- Buprenorphine is classified as a partial mu-opioid receptor agonist and a kappa-opioid receptor antagonist 3, 4, 5, 6, 7
- It has a unique pharmacological profile, with high affinity for mu-opioid receptors and low efficacy, resulting in a partial effect upon binding 4, 5, 7
- Buprenorphine's actions at opioid receptors have not been completely characterized, but it is generally regarded as a mu-opioid receptor partial agonist and a kappa-opioid receptor antagonist 7
Narcotic Agonist-Antagonist Properties
- Buprenorphine was initially classified as a "mixed agonist-antagonist analgesic" or a narcotic antagonist analgesic 5
- It has been shown to have a ceiling effect for respiratory depression, but not for analgesia, in humans 5
- Buprenorphine's partial agonist activity at mu-opioid receptors and its long half-life make it an excellent alternative to methadone for either maintenance therapy or detoxification of the opioid addict 7
Clinical Applications
- Buprenorphine is used in the treatment of opioid addiction, including maintenance therapy and detoxification 3, 6, 7
- It is also used as an analgesic agent, with a potentially favorable safety profile compared to full mu-opioid receptor agonists 4
- Buprenorphine's unique pharmacological properties make it a useful agent in office-based opioid treatment for addiction 6