Buprenorphine-naloxone (bup/nal in 4:1 ratio; Suboxone®, Reckitt Benckiser Pharmaceuticals Incorporation, Richmond, VA) is approved by the Food and Drug Administration for outpatient office-based addiction treatment. In the past few years, bup/nal has been increasingly prescribed off-label for chronic pain management. The current data suggests that bup/nal may provide pain relief in chronic pain patients with opioid dependence or addiction. However, the unique pharmacological profile of bup/nal confers it to be a weak analgesic that is unlikely to provide adequate pain relief for patients without opioid dependence or addiction. Possible mechanisms of pain relief by bup/nal therapy in opioid-dependent chronic pain patients may include reversal of opioid-induced hyperalgesia as well as improvement in opioid tolerance and addiction. Additional studies are needed to assess the implication of bup/nal therapy in clinical anesthesia and perioperative pain management.

C hronic pain can be devastating and has enormous impact on quality of life, health care costs, and work productivity. Although many opioid medications have been developed, with their increased use has come an increase in opioid abuse. This has been associated with a steady increase in the nonmedical use of opioids and number of deaths from unintentional opioid overdoses. Buprenorphine-naloxone (bup/nal) is a semisynthetic opioid developed as an analgesic but is also effective in opioidreplacement therapy. It has been prescribed off-label for treatment of chronic pain, despite lack of consensus on its effectiveness. Assessment of its effectiveness should involve 3 patient groups: those who have opioid addiction but no chronic pain, those who have chronic pain on high-dose opioids, and those who are dependent on or addicted to opioids with coexisting chronic pain. This review article examines the effectiveness of bup/nal in these groups, compares the effectiveness of bup/nal with that of methadone in pain management, discusses implications of bup/nal therapy in clinical anesthesia and perioperative pain therapy, and examines possible mechanisms of bup/nal therapy in patient management.PubMed and Google Scholar were searched for articles on the effectiveness of bup/nal for pain management; all clinical trials relating bup/nal to pain management were conducted from 2002 onward. This review is considered a topical review because the literature pool on the topic is still small and not suitable for a traditional systematic review with a rating on the published articles.Buprenorphine, a semisynthetic opioid, is a derivative of thebaine. It has a high binding affinity for the μ-opioid receptor, effectively competing with other opioids that bind to the same receptor; it functions as a partial μ-opioid receptor agonist and mimics the effect of an opioid but to a lesser extent, thus preventing opioid withdrawal symptoms. It has a slow rate of dissociation from the μ-opioid receptor, which produces a prolonged duration of action compared with other opioids. It is also a full κ-opioid receptor antagonist, has a large volume of distribution, and is highly protein bound (96%). It reaches its peak plasma concentration 90 minutes after administration. Naloxone is a short-acting broad opioid receptor antagonist that binds to opioid receptors with high affinity, becoming a competitive antagonist of opioid receptors. At low doses, it reverses opioid adverse effects without notably reversing analgesia. At high does, it blocks opioid analgesia causing opioid withdrawal. It is~45% protein bound, mostly to albumin.Buprenorphine-naloxone is a sublingual combination tablet in a fixed 4:1 ratio. When given sublingually, the bioavailability of buprenorphine at 40% is higher than the 10% of naloxone, so the buprenorphine will exert the predominate effect. If given intravenously, the duration of buprenorphine is 966 minutes compared with 105 minutes for naloxone. Adverse effects of bup/ nal, mostly through drug-drug interactions, are nausea, ...