Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2015 Dec 4:8:859-70.
doi: 10.2147/JPR.S85951. eCollection 2015.

Buprenorphine - an attractive opioid with underutilized potential in treatment of chronic pain

Ish K Khanna  1 , Sivaram Pillarisetti  1
Affiliations
Review

Buprenorphine - an attractive opioid with underutilized potential in treatment of chronic pain

Ish K Khanna et al. J Pain Res. .

Abstract

Despite proven clinical utility, buprenorphine has not been used widely for the treatment of chronic pain. Questions about "ceiling effect" or bell-shaped curve observed for analgesia in preclinical studies and potential withdrawal issues on combining with marketed μ-agonists continue to hinder progress in expanding full potential of buprenorphine in the treatment of cancer and noncancer pain. Mounting evidence from clinical studies and conclusions drawn by a panel of experts strongly support superior safety and efficacy profile of buprenorphine vs marketed opioids. No ceiling on analgesic effect has been reported in clinical studies. The receptor pharmacology and pharmacokinetics profile of buprenorphine is complex but unique and contributes to its distinct safety and efficacy. The buprenorphine pharmacology also allows it to be combined with other μ-receptor opioids for additivity in efficacy. Transdermal delivery products of buprenorphine have been preferred choices for the management of pain but new delivery options are under investigation for the treatment of both opioid dependence and chronic pain.

Keywords: buprenorphine; hyperalgesia; neuropathic pain; opioid dependence; opioids; partial agonist.

PubMed Disclaimer

Figures

Figure 1
Figure 1
Structures of buprenorphine (A) and norbuprenorphine (B).
Figure 2
Figure 2
Implications of buprenorphine interactions with opioid receptors. Buprenorphine is a partial and potent agonist of μ-opioid receptor. Notes: (1) It can displace or block morphine binding to μ-receptor thus contributes to reduced opioid dependence. (2) Buprenorphine agonist activity on μ receptor is the primary contributing factor to its analgesic signaling events. (3) Buprenorphine interacts with nociceptin/ORL1 with much lower affinity and thus is unlikely to contribute to analgesic effects at therapeutic doses. It is conceivable that buprenorphine interactions with other similar receptors could contribute secondary analgesia. (4) Buprenorphine is a potent antagonist of κ-opioid receptor and this interaction could contribute to reduced tolerance and antidepressant like activity. Abbreviation: ORL1, opioid receptor-like 1.
See this image and copyright information in PMC

References

    1. Fine PG, Miaskowski C, Paice JA. Meeting the challenges in cancer pain management. J Support Oncol. 2004;2(Suppl 4):5–22. - PubMed
    1. Kress HG. Clinical update on the pharmacology, efficacy and safety of transdermal buprenorphine. Eur J Pain. 2009;13:219–230. - PubMed
    1. Breivik H, Collett B, Ventafridda V, Cohen R, Gallacher D. Survey of chronic pain in Europe: prevalence, impact on daily life, and treatment. Eur J Pain. 2006;10:287–333. - PubMed
    1. Portenoy RK, Farrar JT, Backonja MM, Cleeland CS, Yang K, Friedman M, et al. Long term use of controlled-release oxycodone for noncancer pain: results of a 3-year registry study. Clin J Pain. 2007;23:287–299. - PubMed
    1. Sites BD, Beach ML, Davis MA. Increases in the use of prescription opioid analgesics and the lack of improvement in disability metrics among users. Reg Anesth Pain Med. 2014;39(1):6–12. - PMC - PubMed