Overview
Pros:
- partial mu, ceiling effect for resp depression
- no renal dose adjustment
- lower misuse potential (especially suboxone)
Cons:
- Can precipitate withdrawal d/t high receptor affinity
- CYP3A4 substrate
Adverse Effects
Common:
- Somnolence, nausea, constipation, xerostomia
Serious: - Respiratory depression (when given with other CNS depressants), QTc prolongation at high doses
Uses
Opioid Use Disorder
Cancer Pain
Useful in patients with consistent pain and those who may be more susceptible to full-agonist side effects (constipation, confusion, respiratory depression, etc)
MOA
Partial Mu-Opioid Agonist
Mu Opioid Receptor Affinity
- Greater mu-opioid receptor affinity than most opioids (e.g., oxycodone and heroin)
- high-dose buprenorphine (>8-12 mg daily) will block the ability to use most opioids for breakthrough pain.
- At lower buprenorphine doses, there may be synergistic analgesia between buprenorphine and other opioids
- buprenorphine, hydromorphone, and fentanyl have relatively similar affinities
- breakthrough pain can be treated with high doses of hydromorphone or fentanyl.