Drug intelligence / Profile preview

buprenorphine

Development stage
Approved
Lead developer
Indivior
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Sublingual, Transdermal, Buccal, Subcutaneous, Intramuscular
01

Overview

Buprenorphine is a synthetic opioid medication used primarily for the treatment of opioid use disorder (OUD), as well as for acute and chronic pain. It acts as a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. This unique mechanism allows it to reduce cravings and withdrawal symptoms in patients with OUD while producing less euphoria and respiratory depression compared to full opioid agonists. Buprenorphine has a high affinity but low intrinsic activity at the mu-opioid receptor, leading to a "ceiling effect" that increases safety in overdose situations. Developed in the late 1960s as a synthetic analog of thebaine, buprenorphine is available under various brand names and formulations including sublingual tablets/films, transdermal patches, buccal films, subcutaneous injections, and intramuscular injections[1][3][8].

Brand names
SublocadeBrixadiSubutexButransBelbucaBuprenex
Other names
buprenorphine hemiadipate hydrochloride
02

Targets

MOR (Mu opioid receptor)KOR (Kappa opioid receptor)DOR (Opioid Receptor Delta 1)

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