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

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.

Advances in Achieving Opioid Analgesia Without Side Effects

“…Similarly, good quality, randomized studies in neuropathic pain patients are needed. In randomized trials of postoperative or osteoarthritis pain, buprenorphine was concluded to produce fewer respiratory complications, but equivalent analgesia to other opioids ( Davis et al, 2018 ), although the reason for the lack of ceiling analgesic effects in contrast to respiratory depression is unclear, and other studies reported high rate of drop-out due to nausea/vomiting ( Fishman and Kim, 2018 ). Together, as buprenorphine is successfully used for opioid maintenance therapy, the evidence for its analgesic superiority over other opioids in clinical setting appears moderate and more good quality comparative studies are needed ( Davis et al, 2018 ).…”

A Practical Approach for the Management of the Mixed Opioid Agonist-Antagonist Buprenorphine During Acute Pain and Surgery

“…The bioavailability of oral buprenorphine is less than 15%, resulting in the need for other routes of administration. 28 Table 1 provides an overview of the formulations, available strengths, frequency of administration, bioavailability, and extrapolated equivalent dose information. 29 High-dose buprenorphine therapy can be defined as any dose that equals or exceeds an equivalent dose of 24 mg of daily sublingual buprenorphine, whereas low-dose therapy can be defined by any equivalent daily dose less than or equal to 8 mg sublingually.…”

Best Practices in the Management of Nonmedical Opioid Use in Patients with Cancer-Related Pain

“…Buprenorphine and methadone are indicated for opioid use disorders and are also effective analgesics, suggesting they may have an important role in patients with cancer‐related pain and NMOU. Canadian guidelines for the management of patients with chronic non–cancer‐related pain and substance use disorder recommend opioid agonist treatment with buprenorphine‐naloxone as the preferred treatment; however, methadone is also acceptable.…”