An Overview of Buprenorphine

Jeffrey A. Gudin, MD

Director of Pain Management and Palliative Care
Englewood Hospital and Medical Center
Englewood, NJ

Buprenorphine is a partial μ-opioid receptor agonist that is used in the treatment of chronic pain and opioid addiction. Owing to a “ceiling effect,” increasing the buprenorphine dosage will eventually result in a plateau of opioid-related effects. This phenomenon makes buprenorphine useful for patients with addiction disorders, who are more likely to overdose. In fact, the US Food and Drug Administration has approved sublingual formulations of buprenorphine (with and without the opioid antagonist naloxone) for the treatment of opioid dependence. Moreover, the analgesic effects of buprenorphine have led to the development of a 7-day transdermal patch, which has been associated with sustained improvements in pain relief, functionality, and quality of life for patients with chronic pain. Clinicians should be aware, however, that the affinity of buprenorphine for opioid receptors is high enough to displace other opioids, potentially causing patients to go into withdrawal. Thus, to safely transition patients from other opioids, individuals must be in active withdrawal prior to beginning buprenorphine treatment. Here, Dr. Gudin discusses the history of buprenorphine and potential applications for pain or addiction management.

References

1.    Kahan M, Srivastava A, Ordean A, Cirone S. Buprenorphine: new treatment of opioid addiction in primary care. Can Fam Physician. 2011;57:281-289.
2.    Vadivelu N, Anwar M. Buprenorphine in postoperative pain management. Anesthesiol Clin. 2010;28:601-609.
3.    Orman JS, Keating GM. Buprenorphine/naloxone: a review of its use in the treatment of opioid dependence. Drugs. 2009;69:577-607.
4.    Gordon A, Rashiq S, Moulin DE, et al. Buprenorphine transdermal system for opioid therapy in patients with chronic low back pain. Pain Res Manag. 2010;15:169-178.

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