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Synonyms: Buprenex® | Buvidal® | CAM2038 | Sixmo® (buprenorphine hydrochloride) | Subutex® | Temgesic®
buprenorphine is an approved drug (FDA (1981), EMA (2006))
Compound class: Natural product or derivative
Comment: Buprenorphine is a more potent and longer lasting analgesic than morphine.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: buprenorphine
|No information available.|
|Summary of Clinical Use|
|Used to treat severe pain and to ameliorate opioid dependence.
Probuphine®, the first buprenorphine implant for the maintenance treatment of opioid dependence was US FDA approved in May 2016. The earliest EMA authorisation was for a fixed dose combination of buprenorphine and naloxone for the treatment of opioid dependence. Approval for buprenorphine use as a monotherapy for this indication was granted in 2018.
|Mechanism Of Action and Pharmacodynamic Effects|
|Buprenorphine appears to act as a partial agonist at μ- and κ-opioid receptors and as an antagonist at δ-opioid receptors.|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)