Expanding Horizons of Buprenorphine: A Comprehensive Narrative Review of Its Pharmacological Properties and Clinical Applications in Chronic Pain

Stein C. Opioid receptors. Annu Rev Med. 2016;67:433–51.

CAS  PubMed  Google Scholar 

Corder G, Castro DC, Bruchas MR, Scherrer G. Endogenous and exogenous opioids in pain. Annu Rev Neurosci. 2018;41:453–73.

CAS  PubMed  PubMed Central  Google Scholar 

Alorfi NM. Pharmacological methods of pain management: narrative review of medication used. IJGM. 2023;16:3247–56.

CAS  Google Scholar 

Ballantyne JC. Opioid therapy in chronic pain. Phys Med Rehabil Clin N Am. 2015;26:201–18.

PubMed  Google Scholar 

Warner EA. Opioids for the treatment of chronic noncancer pain. Am J Med. 2012;125:1155–61.

CAS  PubMed  Google Scholar 

Plante GE, VanItallie TB. Opioids for cancer pain: the challenge of optimizing treatment. Metab Clin Exp. 2010;59:S47-52.

CAS  PubMed  Google Scholar 

Paice JA, Portenoy R, Lacchetti C, Campbell T, Cheville A, Citron M, et al. Management of chronic pain in survivors of adult cancers: American Society of Clinical Oncology clinical practice guideline. J Clin Oncol [Internet]. 2016. https://doi.org/10.1200/JCO.2016.68.5206.

PubMed  Google Scholar 

Gudin J, Fudin J. A narrative pharmacological review of buprenorphine: a unique opioid for the treatment of chronic pain. Pain Ther. 2020;9:41–54.

PubMed  PubMed Central  Google Scholar 

Sizar O, Genova R, Gupta M. Opioid-Induced Constipation. StatPearls [Internet]. Treasure Island (FL): StatPearls Publishing. 2024. http://www.ncbi.nlm.nih.gov/books/NBK493184/. Accessed 19 Oct 2024.

Mercadante S, Arcuri E, Santoni A. Opioid-induced tolerance and hyperalgesia. CNS Drugs. 2019;33:943–55.

CAS  PubMed  Google Scholar 

Jalali MS, Botticelli M, Hwang RC, Koh HK, McHugh RK. The opioid crisis: a contextual, social-ecological framework. Health Res Policy Syst. 2020;18:87.

PubMed  PubMed Central  Google Scholar 

Webster L, Gudin J, Raffa RB, Kuchera J, Rauck R, Fudin J, et al. Understanding buprenorphine for use in chronic pain: expert opinion. Pain Med. 2020;21:714–23.

PubMed  PubMed Central  Google Scholar 

Davis MP, Pasternak G, Behm B. Treating chronic pain: an overview of clinical studies centered on the buprenorphine option. Drugs. 2018;78:1211–28.

PubMed  PubMed Central  Google Scholar 

Khanna IK, Pillarisetti S. Buprenorphine—an attractive opioid with underutilized potential in treatment of chronic pain. JPR. 2015;8:859–70.

CAS  Google Scholar 

Li L, Chen J, Li Y-Q. The downregulation of opioid receptors and neuropathic pain. Int J Mol Sci. 2023;24:5981.

CAS  PubMed  PubMed Central  Google Scholar 

Fields H. State-dependent opioid control of pain. Nat Rev Neurosci. 2004;5:565–75.

CAS  PubMed  Google Scholar 

Lambert D. Drugs and receptors. Contin Educ Anaesth Crit Care Pain. 2004;4:181–4.

Google Scholar 

Leffler A, Frank G, Kistner K, Niedermirtl F, Koppert W, Reeh PW, et al. Local anesthetic-like inhibition of voltage-gated Na+channels by the partial μ-opioid receptor agonist buprenorphine. Anesthesiology. 2012;116:1335.

CAS  PubMed  Google Scholar 

Schmid CL, Kennedy NM, Ross NC, Lovell KM, Yue Z, Morgenweck J, et al. Bias factor and therapeutic window correlate to predict safer opioid analgesics. Cell. 2017;171:1165-1175.e13.

CAS  PubMed  PubMed Central  Google Scholar 

Pergolizzi JV Jr, Raffa RB. Safety and efficacy of the unique opioid buprenorphine for the treatment of chronic pain. J Pain Res. 2019;12:3299–317.

CAS  PubMed  Google Scholar 

Pedersen MF, Wróbel TM, Märcher-Rørsted E, Pedersen DS, Møller TC, Gabriele F, et al. Biased agonism of clinically approved μ-opioid receptor agonists and TRV130 is not controlled by binding and signaling kinetics. Neuropharmacology. 2020;166: 107718.

CAS  PubMed  Google Scholar 

Rankovic Z, Brust TF, Bohn LM. Biased agonism: an emerging paradigm in GPCR drug discovery. Bioorg Med Chem Lett. 2016;26:241–50.

CAS  PubMed  Google Scholar 

Kelly E, Conibear A, Henderson G. Biased agonism: lessons from studies of opioid receptor agonists. Annu Rev Pharmacol Toxicol. 2023;63:491–515.

CAS  PubMed  Google Scholar 

Kuo A, Magiera J, Rethwan N, Andersson Å, Leen Lam A, Wyse B, et al. In vitro profiling of opioid ligands using the cAMP formation inhibition assay and the β-arrestin2 recruitment assay: no two ligands have the same profile. Eur J Pharmacol. 2020;872: 172947.

CAS  PubMed  Google Scholar 

Bidlack JM, Knapp BI, Deaver DR, Plotnikava M, Arnelle D, Wonsey AM, et al. In vitro pharmacological characterization of buprenorphine, samidorphan, and combinations being developed as an adjunctive treatment of major depressive disorder. J Pharmacol Exp Ther. 2018;367:267–81.

CAS  PubMed  Google Scholar 

Papa A, Salzano AM, Di Dato MT, Desiderio V, Buonavolontà P, Mango P, et al. Long-term efficacy and reduced side-effects of buprenorphine in patients with moderate and severe chronic pain. Front Pharmacol [Internet]. 2024. https://doi.org/10.3389/fphar.2024.1454601/full.

PubMed  Google Scholar 

Gringauz M, Rabinowitz R, Stav A, Korczyn AD. Tolerance to the analgesic effect of buprenorphine, butorphanol, nalbuphine, and cyclorphan, and cross-tolerance to morphine. J Anesth. 2001;15:204–9.

CAS  PubMed  Google Scholar 

Baldo BA. Toxicities of opioid analgesics: respiratory depression, histamine release, hemodynamic changes, hypersensitivity, serotonin toxicity. Arch Toxicol. 2021;95:2627–42.

CAS  PubMed  Google Scholar 

Infantino R, Mattia C, Locarini P, Pastore AL, Maione S, Luongo L. Buprenorphine: far beyond the “ceiling.” Biomolecules. 2021;11:816.

CAS  PubMed  PubMed Central  Google Scholar 

DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, et al. A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine. J Pharmacol Exp Ther. 2013;344:708–17.

CAS  PubMed  Google Scholar 

Kliewer A, Schmiedel F, Sianati S, Bailey A, Bateman JT, Levitt ES, et al. Phosphorylation-deficient G-protein-biased μ-opioid receptors improve analgesia and diminish tolerance but worsen opioid side effects. Nat Commun. 2019;10:367.

CAS  PubMed  PubMed Central  Google Scholar 

Bachmutsky I, Wei XP, Durand A, Yackle K. ß-arrestin 2 germline knockout does not attenuate opioid respiratory depression. Elife. 2021;10:e62552.

CAS  PubMed  PubMed Central  Google Scholar 

Montandon G, Ren J, Victoria NC, Liu H, Wickman K, Greer JJ, et al. G-protein-gated inwardly rectifying potassium channels modulate respiratory depression by opioids. Anesthesiology. 2016;124:641–50.

CAS  PubMed  Google Scholar 

Dahan A, Yassen A, Romberg R, Sarton E, Teppema L, Olofsen E, et al. Buprenorphine induces ceiling in respiratory depression but not in analgesia. BJA Br J Anaesth. 2006;96:627–32.

CAS  PubMed  Google Scholar 

Dahan A, Yassen A, Bijl H, Romberg R, Sarton E, Teppema L, et al. Comparison of the respiratory effects of intravenous buprenorphine and fentanyl in humans and rats. Br J Anaesth. 2005;94:825–34.

CAS  PubMed  Google Scholar 

Moss LM, Algera MH, Dobbins R, Gray F, Strafford S, Heath A, et al. Effect of sustained high buprenorphine plasma concentrations on fentanyl-induced respiratory depression: a placebo-controlled crossover study in healthy volunteers and opioid-tolerant patients. PLoS One. 2022;17: e0256752.

CAS  PubMed  PubMed Central  Google Scholar 

Pergolizzi J, Böger RH, Budd K, Dahan A, Erdine S, Hans G, et al. Opioids and the management of chronic severe pain in the elderly: consensus statement of an international expert panel with focus on the six clinically most often used world health organization step III opioids (buprenorphine, fentanyl, hydromorphone, methadone, morphine, oxycodone). Pain Pract. 2008;8:287–313.

PubMed  Google Scholar 

Huestis MA, Cone EJ, Pirnay SO, Umbricht A, Preston KL. Intravenous buprenorphine and norbuprenorphine pharmacokinetics in humans. Drug Alcohol Depend. 2013;131:258–62.

CAS  PubMed  Google Scholar 

Bai SA, Xiang Q, Finn A. Evaluation of the pharmacokinetics of single- and multiple-dose buprenorphine buccal film in healthy volunteers. Clin Ther. 2016;38:358–69.

CAS  PubMe

Comments (0)

No login
gif