Facts About Buprenorphine
FDA approved for Opioid Use Disorder treatment in an officebased setting.
For those with tolerance to opioids as a result of OUD,
buprenorphine is often a safe choice.
Buprenorphine acts as a partial mixed opioid agonist at the μreceptor and as an antagonist at the κ-receptor. It has a higher
affinity for the μ-receptor than other opioids, and it can
precipitate withdrawal symptoms in those actively using other
opioids.
It is dosed daily, has a long half-life, and prevents withdrawal in
opioid dependent patients.
Can be in tablet, sublingual film, or injectable formulations.
Many formulations contain naloxone to prevent injection
diversion. This formulation is the preferred treatment medication.
The buprenorphine only version is often used with pregnant
women to decrease potential fetal exposure to naloxone.
There is a “ceiling effect” in which further increases above 24mg in
dosage does not increase the effects on respiratory or
cardiovascular function.
Buprenorphine should be part of a comprehensive management
program that includes psychosocial support. Treatment should
not be withheld in the absence of psychosocial support.
Overdose with buprenorphine in adults is less common, and most
likely occurs in individuals without tolerance, or who are using cooccurring substances like alcohol or benzodiazepines.