Table 3.

Summary of buprenorphine pharmacology

FEATURERESULT
Very tight binding to opioid receptorsDisplaces other opioids from opioid receptors
Triggers withdrawal in patients physically dependent on opioids
Blocks the analgesic action of other opioids
Slow dissociation from opioid receptorsLong duration of action
Relieves withdrawal and cravings for 24 h or longer
No bioaccumulationAllows quick titration to effective dose
Partial agonist with ceiling effectVery low risk of overdose
Might be less effective than higher doses of methadone
SL and IV absorption; poor oral absorptionCan be abused intravenously
Combined with naloxoneWhen injected, naloxone will trigger withdrawal in patients physically dependent on opioids; this serves as a deterrent to IV use
  • IV—intravenous, SL—sublingual.