Recommending buprenorphine for pain management

Morphine or other opioid compounds (i.e.,oxycodone, fentanyl, etc.) produce their strong analgesic and addictive effects by acting on a G protein-coupled receptor, called the μ-opioid receptor (MOR), that is expressed in brain regions important for pain, reward and aversion (4-6). The unique binding profile of buprenorphine at MORs produces a conformation that prevents receptor phosphorylation, β-arrestin interactions and receptor downregulation (23,24). [...]buprenorphine's drug signaling signature can be characterized as Gi/o-protein signaling biased, a profile which is highly preferable and predicts fewer side effects (12). Specifically, respiratory depression, constipation, hypogonadism and abuse liability induced by buprenorphine are reduced in comparison to other MOR agonists (15,18) and clearance is independent of renal function (18), making buprenorphine a safer analgesic with a better therapeutic index and a preferred choice in case of renal failure. In summary, we believe that buprenorphine should be reconsidered by physicians and insurance companies, as a safer alternative to prototypic opiates in chronic pain management and maybe carefully considered for acute pain patients.