Buprenorphine
Subutex · Suboxone
Partial Opioid AgonistSchedule IIIGeneric availableTDM data
Buprenorphine sublingual tablets contain buprenorphine, a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor.
Compare Buprenorphine →FDA-Approved Indications
- Opioid use disorder — sublingual; preferred for induction (adults)
Common Off-Label Uses
- Chronic pain
- Treatment-resistant depression (investigational)
- Neonatal abstinence syndrome prevention
What Sets This Drug Apart
- Partial mu-opioid agonist (and kappa antagonist) — ceiling effect on respiratory depression makes it safer than full agonists (methadone) in overdose
- FDA-approved for opioid use disorder maintenance; available sublingual (Subutex/Suboxone), buccal, implant (Probuphine), and monthly injection (Sublocade)
- Naloxone combination formulation (Suboxone) deters IV misuse — naloxone is inactive sublingual but precipitates withdrawal if injected
- Can be prescribed in office-based settings (DEA X-waiver requirement eliminated 2023) — unlike methadone which requires OTP clinic dispensing
- Long half-life (31-35h) provides stable opioid receptor occupancy; missed doses are less destabilizing than with methadone
- CYP3A4 substrate — strong inhibitors (azole antifungals) can increase levels; strong inducers can precipitate withdrawal