Buprenorphine Pharmacodynamics and Pharmacokinetics



Buprenorphine, a derivative of the poppy alkaloid thebaine, is a semi-synthetic opioid that was initially synthesized as one of a series of compounds from oripavine [1]. Early in its development, it was recognized that buprenorphine did not behave as a typical mu opioid agonist as it could both produce mu opioid action and block mu opioid effects, hence its early characterization as an opioid agonist–antagonist [2, 3]. It is now known that buprenorphine acts as a partial opioid agonist at the mu receptor, an antagonist at the kappa opioid receptor [4], and as a partial agonist at the nociceptin/orphanin opioid-like receptor (ORL-1, FQ-NOP) [5]. As the benefits of buprenorphine in the treatment of pain and opioid dependence are attributable primarily to buprenorphine’s action at mu opioid receptors, this chapter will focus on those actions. It is unclear whether the kappa antagonist and/or nociceptin/orphanin partial agonist activity of buprenorphine produce any effects of clinical relevance, although this has been the focus of some speculation. For example, as kappa agonists are known to produce significant dysphoric effects [6, 7], studies have explored the possibility that buprenorphine, with its kappa antagonist actions, may produce euphoria as a secondary effect, thereby acting as an antidepressant to enhance mood. However, controlled studies have reported no differential benefit of buprenorphine when compared to methadone (which lacks kappa receptor blockade activity) on improvement of depressive symptoms that may occur during the course of treatment for opioid dependence [8]. With regard to the ORL-1 receptor, recent preclinical data suggest that the ORL-1 partial agonist action of buprenorphine can decrease alcohol consumption in laboratory animals [9]; however, this interesting effect has not yet been carefully explored in humans.


Opioid Dependence Opioid Withdrawal Central Nervous System Depressant Sublingual Tablet Precipitate Withdrawal 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.



The authors would like to kindly acknowledge the support of the National Institute on Drug Abuse (R01 DA016718) in preparing this chapter.


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Copyright information

© Springer Science+Business Media New York 2013

Authors and Affiliations

  1. 1.Department of Behavioral Science, Center on Drug and Alcohol ResearchUniversity of KentuckyLexingtonUSA

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