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

Abstract

Buprenorphine has gained significant attention for its unique pharmacological properties, making it a valuable tool in chronic pain management. Unlike traditional opioids, buprenorphine's partial and biased agonist actions at the μ-opioid receptor provide potent analgesia while minimizing risks such as respiratory depression, tolerance, and dependence. Its favorable pharmacokinetic profile provides the potential for expanding its clinical use in different patient populations. A literature search was conducted in PubMed, Web of Science, and Google Scholar to identify peer-reviewed studies on recent developments in the pharmacological features and new clinical applications of buprenorphine, including original research, reviews, and consensus statements. This comprehensive review explores the expanding clinical applications of buprenorphine, emphasizing its role in managing chronic pain in elderly patients, individuals with cardiac conditions, and those with renal impairments. Emerging evidence highlights its utility in addressing chronic pain in younger adults and its potential in mitigating side effects associated with aromatase inhibitor therapy in patients with breast cancer. Additionally, buprenorphine's lower endocrine side-effect profile and antidepressant properties open new therapeutic avenues for pain-associated depression. With its unique pharmacodynamics, transdermal formulations for sustained drug release, and reduced adverse effects, buprenorphine represents a promising option for tailored, multimodal pain management strategies, especially in populations with complex medical needs. Further studies are warranted to confirm its broad therapeutic potential.

Keywords: Buprenorphine; Buprenorphine transdermal formulation; Chronic pain management.

Fig. 1

Opioid mechanism of action involves both pre-synaptically and post-synaptically effects. Adapted from Ref. [2]. Ca²⁺ calcium ion, cAMP cyclic adenosine monophosphate, K⁺ potassium ion

Fig. 2

Summary of the beneficial clinical effects of buprenorphine. CNS central nervous system