Treating Chronic Pain: An Overview of Clinical Studies Centered on the Buprenorphine Option

Davis, Mellar P.; Pasternak, Gavril; Behm, Bertrand

doi:10.1007/s40265-018-0953-z

Cited by 138Pain Management and Opioid UseOpioid Use Disorder TreatmentAnesthesia and Pain Management

Treating Chronic Pain: An Overview of Clinical Studies Centered on the Buprenorphine Option

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Davis, Mellar P., Pasternak, Gavril, Behm, Bertrand·2018·Drugs

DOI 10.1007/s40265-018-0953-zPMC PMC6822392

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Abstract

The buprenorphine receptor binding profile is unique in that it binds to all three major opioid receptors (mu, kappa, delta), and also binds to the orphan-like receptor, the receptor for orphanin FQ/nociceptin, with lower affinity. Within the mu receptor group, buprenorphine analgesia in rodents is dependent on the recently discovered arylepoxamide receptor target in brain, which involves a truncated 6-transmembrane mu receptor gene protein, distinguishing itself from morphine and most other mu opioids. Although originally designed as an analgesic, buprenorphine has mainly been used for opioid maintenance therapy and only now is increasingly recognized as an effective analgesic with an improved therapeutic index relative to certain potent opioids. Albeit a second-, third-, or fourth-line analgesic, buprenorphine is a reasonable choice in certain clinical situations. Transdermal patches and buccal film formulations are now commercially available as analgesics. This review discusses buprenorphine pharmacodynamics and pharmacokinetics, use in certain populations, and provides a synopsis of systematic reviews and randomized analgesic trials. We briefly discuss postoperative management in patients receiving buprenorphine maintenance therapy, opioid equivalence to buprenorphine, rotations to buprenorphine from other opioids, and clinical relevance of buprenorphine-related QTc interval changes.

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In the US, the smallest available dose for sublingual buprenorphine is 2 mg, but buccal film is available as small as 75 ug, equivalent to 150 ug of sublingual buprenorphine, potentially facilitating some of the regimens outlined here.
“In the US, the smallest available dose for sublingual buprenorphine is 2 mg, but buccal film is available in as small as a dose of 75 ug, equivalent to 150 ug of sublingual buprenorphine, 62 potentially facilitating some of the regimens outlined here.”
From Tapering and withdrawing opioids: guidance informed by fundamental principles to minimise withdrawal symptoms (2025) · cites this paper as [62]
The Pharmacokinetics section lists a 75 μg buccal dose and gives an approximate 2:1 conversion from sublingual to buccal formulations, consistent with the stated 150 μg equivalence. But the Introduction also lists a 1.4 mg sublingual buprenorphine combination tablet, so the paper does not support the claim that 2 mg is the smallest available sublingual dose. No page numbers were provided in our copy. (LLM, conf=0.89)
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Dear DEA
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[135]Buprenorphine for chronic pain: a review of the clinical effectiveness. Ottawa (ON); Canadian Agency for Drugs and Technologies in Health; 2017. 28727399

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“In the US, the smallest available dose for sublingual buprenorphine is 2 mg, but buccal film is available in as small as a dose of 75 ug, equivalent to 150 ug of sublingual buprenorphine, 62 potentially facilitating some of the regimens out-lined here.”

Structural Determinants of Opioid and NOP Receptor Activity in Derivatives of Buprenorphine
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Authors: Davis, M. P., Pasternak, G., & Behm, B.
Affiliations: Geisinger Medical Center (US)
Memorial Sloan Kettering Cancer Center (US)
Corresponding author: Davis, Mellar P.
ORCID: Davis, Mellar P.
Pasternak, Gavril
Venue: Drugs
Publisher: Springer Science and Business Media LLC
Published: 2018-07-26
Volume: 78
Issue: 12
Pages: 1211-1228
ISSN: 0012-6667 (ISSN-L)
1179-1950
DOI: 10.1007/s40265-018-0953-z
PMC: PMC6822392
OpenAlex: W2883188098
Cited by: 138
References: 200
Citations by year: 2026: 2 · 2025: 16 · 2024: 21 · 2023: 16 · 2022: 24 · 2021: 24 · 2020: 20 · 2019: 11 · 2018: 2 · 2017: 2
FWCI: 3.48
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Licence: www.springer.com/tdm (tdm)
Locations: Drugs (publishedVersion)
PubMed (publishedVersion)
PubMed Central (acceptedVersion)
Funders: MAYDAY Fund
Memorial Sloan-Kettering Cancer Center
BioDelivery Sciences International
National Institute on Drug Abuse (R01DA007242, R01DA006241, R37DA007242, T32DA007242)
National Cancer Institute (P30CA008748)
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, chronic pain, opioid analgesia, mu-opioid receptor, nociceptin receptor, pharmacokinetics, pharmacodynamics, transdermal patch, buccal films, opioid maintenance treatment, postoperative analgesia, opioid rotation, QTc prolongation, clinical trials
MeSH terms: Systematic Reviews as Topic, Administration, Sublingual, Analgesics, Opioid, Animals, Buprenorphine, Chemistry, Pharmaceutical, Dose-Response Relationship, Drug, Drug Therapy, Combination, Drug Tolerance, Humans, Narcotic Antagonists, Receptors, Opioid, Randomized Controlled Trials as Topic, Substance-Related Disorders, Transdermal Patch, Chronic Pain, Observational Studies as Topic

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Treating Chronic Pain: An Overview of Clinical Studies Centered on the Buprenorphine Option

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