Buprenorphine and its formulations: a comprehensive review

Buprenorphine, a novel long-acting analgesic, was developed with the intention of two purposes: analgesia and opioid use disorder. Regarding its pharmacodynamics, it is a partial agonist at mu receptors, an inverse agonist at kappa receptors, and an antagonist at delta receptors. For the purpose of analgesia, three formulations of buprenorphine were developed: IV/IM injectable formulation (Buprenex (R)), transdermal patch formulation (Butrans (R)), and buccal film formulation (Belbuca (R)). Related to opioid dependence, the formulations developed were subcutaneous extended release (Sublocade (R)), subdermal implant (Probuphine (R)), and sublingual tablets (Subutex (R)). Lastly, in order to avoid misuse of buprenorphine for opioid dependence, two combination formulations paired with naloxone were developed: film formulation (Suboxone (R)) and tablet formulation (Zubsolv (R)). In this review, we present details of each formulation along with their similarities and differences between each other and clinical considerations.