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

Authors Khanna I, Pillarisetti S

Received 29 August 2015

Accepted for publication 28 October 2015

Published 4 December 2015 Volume 2015:8 Pages 859—870

DOI https://doi.org/10.2147/JPR.S85951

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Kerui Gong

Peer reviewer comments 2

Editor who approved publication: Dr Michael Schatman


Ish K Khanna, Sivaram Pillarisetti

NeuroPn Therapeutics, Alpharetta, GA, USA

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, opioids, opioid dependence, partial agonist, hyperalgesia, neuropathic pain

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