The clinical analgesic efficacy of buprenorphine

Summary What is known and objective Based on in vitro assays and select animal models, buprenorphine is commonly called a ‘partial agonist’. An implication is that it should produce less analgesic effect in humans than so‐called ‘full agonists’ such as morphine or fentanyl. However, buprenorphine ha...

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Bibliographic Details
Published in:Journal of clinical pharmacy and therapeutics 2014-12, Vol.39 (6), p.577-583
Main Authors: Raffa, R. B., Haidery, M., Huang, H.-M., Kalladeen, K., Lockstein, D. E., Ono, H., Shope, M. J., Sowunmi, O. A., Tran, J. K., Pergolizzi Jr, J. V.
Format: Article
Language:English
Subjects:
Analgesics, Opioid - administration & dosage
Analgesics, Opioid - pharmacology
Animals
buprenorphine
Buprenorphine - administration & dosage
Buprenorphine - pharmacology
clinical data
Controlled Clinical Trials as Topic
Dose-Response Relationship, Drug
Drug Partial Agonism
efficacy
full agonist
Humans
Pain - drug therapy
Pain - physiopathology
partial agonist
Signal Transduction - drug effects
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Summary:Summary What is known and objective Based on in vitro assays and select animal models, buprenorphine is commonly called a ‘partial agonist’. An implication is that it should produce less analgesic effect in humans than so‐called ‘full agonists’ such as morphine or fentanyl. However, buprenorphine has a multimechanistic pharmacology, and thus partial agonism at a specific receptor is not particularly relevant to its overall analgesic action. We review published clinical trials that directly compared the magnitude of buprenorphine's analgesic effect to analgesics commonly considered full agonists. Comment Due to different signal transduction pathways, a drug can be a full agonist on one endpoint and a partial agonist on another. Therefore, we limited the present review to buprenorphine's analgesic effect. What is new and conclusion Twenty‐four controlled clinical trials were identified, plus a case report and dose–response curve. Based on complete or comparable pain relief, in buprenorphine had full clinical analgesic efficacy in 25 of the 26 studies. Buprenorphine is commonly called a ‘partial‐agonist’. However, it has a multimechanistic pharmacology, and thus partial agonism at a specific receptor is not particularly relevant to its overall analgesic action. In this review of published clinical trials that directly compared the magnitude of buprenorphine's analgesic effect to analgesics commonly considered full‐agonists buprenorphine had full clinical analgesic efficacy in 25 of the 26 studies.
ISSN:0269-4727
1365-2710
DOI:10.1111/jcpt.12196