Behavioral pharmacology of buprenorphine, with a focus on preclinical models of reward and addiction

The general conclusion is that despite the high affinity of buprenorphine for the µ receptor it appears to be a remarkably safe drug, with a benign overall side effect profile and low addictive and dependence-inducing potential.

Abstract

Since buprenorphine is a potent opioid drug, the issue of addiction and dependence in this context is an important one. Although there are still some gaps in the behavioral pharmacological characterization of buprenorphine, the general conclusion that can be drawn from the reviewed literature is that despite the high affinity of buprenorphine for the mu receptor it appears to be a remarkably safe drug, with a benign overall side effect profile and low addictive and dependence-inducing potential. This favorable side effect profile appears to be due, to a large extent, to the partial agonistic properties of the drug, in combination with its particular receptor kinetics (i.e. very slow dissociation from the mu receptor after binding).