Benefit-Risk Analysis of Buprenorphine for Pain Management

Abstract

Health care providers in the United States are facing challenges in selecting appropriate medication for patients with acute and chronic pain in the midst of the current opioid crisis and COVID-19 pandemic. When compared with conventional opioids, the partial µ-opioid receptor agonist buprenorphine has unique pharmacologic properties that may be more desirable for pain management. The formulations of buprenorphine approved by the US Food and Drug Administration for pain management include intravenous injection, transdermal patch, and buccal film. A comparison of efficacy and safety data from studies of buprenorphine and conventional opioids suggests that buprenorphine may be a better-tolerated treatment option for many patients that provides similar or superior analgesia. Our benefit-risk assessment in this narrative review suggests that health care providers should consider that buprenorphine may be an appropriate alternative for pain management over other opioids.

Triglyceride-Mimetic Prodrugs of Buprenorphine Enhance Oral Bioavailability via Promotion of Lymphatic Transport

“…Buprenorphine (BUP, Figure 1 ) is a potent µ-opioid receptor partial agonist that is widely used for pain management and opioid replacement therapy ( Johnson et al, 2005 ; Coe et al, 2019 ; Hale et al, 2021 ). Owing to high affinity for the µ-opioid receptor and slow receptor dissociation, BUP has a long duration of action, and may be used as a replacement for a number of widely used opioid analgesics, including fentanyl, oxycodone and morphine ( Mercadante et al, 2009 ; Daitch et al, 2014 ; Prommer 2015 ).…”

Current and Future Therapeutic Options in Pain Management: Multi-mechanistic Opioids Involving Both MOR and NOP Receptor Activation

“…Indeed, in moderate-to-severe post-operative pain and cancer pain, this molecule has been shown to have an analgesic efficacy comparable to that of morphine, oxycodone, and fentanyl [ 63 ]. While the pharmacological effects result from partial MOR agonism, the reduced side effects associated with buprenorphine treatment could be related to its ability to interact with DOR, KOR, and NOP receptors [ 64 ]. However, it is also interesting to point out that recent studies conducted by a rich panel of in vitro assays highlighted that the buprenorphine profile is closer to recently developed Gi-biased drugs (e.g., TRV 130 and PZM21) than morphine or fentanyl [ 65 ].…”

“…Transdermal and buccal formulations overcome the hepatic “first-pass” effect, hence increasing bioavailability and maintaining stable steady-state plasma concentrations. These two formulations have been approved for around-the-clock management of severe chronic pain requiring up to 160 mg/day of morphine milligram equivalents [ 64 , 67 ].…”

“…These formulations have been approved for the treatment of chronic pain, but their availability may vary among different countries. Transdermal buprenorphine is applied on the deltoid region or the upper chest, with sites of application to be rotated in order to avoid cutaneous reactions, for example, rash, erythema, and pruritus [ 64 , 67 ]…”

Pain Management Providers in the Era of COVID-19: Who is Taking Care of Those Who Provide Care?

“…The early literature addressed the use of telehealth to provide behavioral services to chronic pain patients, 4 along with best practices consensus statements, which were focused on interventional pain medicine. 5,6 Progressively, other issues were addressed, including the impact of the pandemic on fellowship training, 7 the safety of various medications during COVID-19, 8-10 the risks of developing chronic pain as a result of COVID-19 infection and treatment, 11 manifestations of characterological disturbances among chronic pain sufferers triggered by the pandemic, 12 dealing with disruptions of research on pain management due to the pandemic, 13 the implications of postponed joint replacement surgeries for pain management, 14 the impact of social distancing and other COVID-19-related phenomena on psychosocial aspects of chronic pain, 15,16 the impact of the redeployment of clinical staff from pain management departments due to the pandemic, 17 and the effect of the pandemic on the opioid epidemic, 18,19 among several other areas of investigation. The focus of the extant medical literature on pain patient well-being and threats to it is certainly appropriate.…”