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Cited by 47Pain Management and Opioid UseOpioid Use Disorder TreatmentAnesthesia and Pain Management

Buprenorphine—Clinically useful but often misunderstood

Butler, Stephen·2013·Scandinavian Journal of Pain
DOI 10.1016/j.sjpain.2013.05.004
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Abstract

Background: There are a number of false myths about buprenorphine based on unconfirmed animal data, even from isolated animal organs, and early clinical research. These myths came into textbooks on pharmacology and pain about 30 years ago and have been difficult to eradicate. Animal models of pain and pain relief are notoriously unreliable as predictors of human clinical effects. The fact is that in clinical practice there is NO bell-shaped dose-response curve, there is NO plateau on the dose-response curve, and there is NO antagonist effect from buprenorphine on other mu -opioid agonists. Methods: This narrative, topical review of relevant research publications evaluates new knowledge on the pharmacodynamics and pharmacokinetics of buprenorphine of importance in clinical practice. Results: Buprenorphine is a potent opioid analgesic acting on all four opioid receptors: it is an agonist on the mu -, the delta , and the ORL-1 receptors. It is an antagonist at the kappa -receptor. Buprenorphine has a number of active metabolites with different effects on the four opioid receptors; all except the norbup-3-glu are analgesic. Buprenorphine itself is not a respiratory depressant or sedative, but some of its active metabolites are. Buprenorphine and its active metabolites are not excreted by the kidney. Therefore buprenorphine may be used in patients with advanced renal failure. Buprenorphine has a slow onset and a long offset. These properties are advantageous, except sometimes when treating severe acute pain. Its agonist effect on the ORL-1 receptor reduces reward-effects and slows the development of tolerance to the analgesic effects. Buprenorphine inhibits voltage-gated sodium-channels and enhances and prolongs peripheral nerve blocks. Its ORL-1 -effect at the spinal cord may do the same. Buprenorphine is well suited for treatment of chronic pain, especially chronic neuropathic pain and cancer pain. The beneficial effects as a co-medication during treatment of the opioid-abuse disease are due to its slow onset (less “kick-effect”). Its prolonged offset-time reduces the likelihood of acute withdrawal problems and reduces the “craving” of opioids. Adverse effects: Buprenorphine, being a mu -agonist, may induce or maintain opioid addiction. Illegally obtained high-dose transmucosal buprenorphine, intended for treatment of addiction, is dissolved and injected by opioid abusers. This is an increasing problem in some countries. Conclusions: Buprenorphine’s unusual pharmacodynamics and pharmacokinetics make it an ideal opioid for treatment of most chronic pain conditions where opioid therapy is indicated. Implications: Buprenorphine is a well studied and often misunderstood analgesic opioid drug. The evidence base predicts that it will be an increasingly important alternative for treatment of chronic pain conditions caused by cancer and non-cancer diseases. It will continue to be an attractive alternative to methadone for opioid abuse rehabilitation.

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  • Buprenorphine acts as a partial agonist at mu opioid receptors and an antagonist at kappa opioid receptors.

    “Buprenorphine, a mu opioid receptor partial agonist (274-276) and a kappa opioid receptor antagonist (277)”

    From A brain-centric model of suicidal behavior (2020) · cites this paper as [277]

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Authors
Butler, S.
Affiliations
Uppsala University Hospital (SE)
Corresponding author
Butler, Stephen
ORCID
Butler, Stephen
Venue
Scandinavian Journal of Pain
Publisher
Walter de Gruyter GmbH
Published
2013-07-01
Volume
4
Issue
3
Pages
148-152
ISSN
  • 1877-8860 (ISSN-L)
  • 1877-8879
DOI
10.1016/j.sjpain.2013.05.004
OpenAlex
W2083935847
Cited by
47
References
40
Citations by year
2026: 1 · 2025: 4 · 2024: 1 · 2023: 1 · 2022: 3 · 2021: 5 · 2020: 8 · 2019: 5 · 2018: 5 · 2017: 6 · 2016: 4 · 2015: 2 · 2014: 1 · 2013: 1
FWCI
3.41
Type
journal article
Language
en
Open access
closed
Licence
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations
  • Scandinavian Journal of Pain (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Health Sciences › Medicine › Anesthesiology and Pain Medicine › Pain Management and Opioid Use
  • Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Opioid Use Disorder Treatment
  • Health Sciences › Medicine › Surgery › Anesthesia and Pain Management
Keywords
buprenorphine, opioid analgesics, pharmacodynamics, pharmacokinetics, mu-opioid receptor, kappa opioid receptor, delta opioid receptor, ORL1 receptor, norbuprenorphine, dose-response curves, opioid tolerance, opioid use disorder, chronic neuropathic pain, cancer pain, opioid withdrawal, opioid antagonism, renal failure

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