Pharmacokinetics and pharmacodynamics of buprenorphine: Relevant clinical and forensic aspects

Abstract

Background: Buprenorphine is an opioid drug synthesized from the opium alkaloid thebaine found in poppy (Papaver somniferum). Currently, buprenorphine is used for therapeutic purposes namely for the treatment of opioid dependence and substance abuse, as well as acute and chronic pain. Objectives: The aim of this work is to thoroughly review the state-of-the-art of pharmacokinetics and pharmacodynamics, as well as the diagnosis, treatment, and relevant clinical and forensic aspects of buprenorphine. Results: Buprenorphine has a low molecular weight, is lipophilic, and is water soluble, all of which contribute to its overall efficacy. Single buprenorphine's pharmacology allows for effective management of pain and opioid addiction. It is classified as a κ-receptor antagonist and a partial µ-receptor agonist, and it is extensively metabolized by CYP3A4 into norbuprenorphine, and both are then further metabolized by glucuronidation. Buprenorphine is known to be highly bound to proteins than may have deep pharmacokinetics implications, has a large volume of distribution, and is mostly excreted in the feces. Constipation, sedation, and respiratory depression, as well as the possibility of abuse and fatalities, have been reported. As a CYP2D6 and CYP3A4 inhibitor, buprenorphine has been implicated in pharmacological interactions, by increasing the levels of other drugs metabolized through those pathways. Conclusion: Buprenorphine has helped hundreds of thousands of people regain control of their lives and avoid the negative health consequences of opioid abuse and injection. Further studies are needed to completely understand the mechanism of buprenorphine as well as the pharmacogenomic characteristics that can be used to optimize therapy and determine who reacts better to this.