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.
Palmitoylethanolamide (PEA) is a nutraceutical endocannabinoid that was retrospectively discovered in egg yolks. Feeding poor children with known streptococcal infections prevented rheumatic fever. Subsequently, it was found to alter the course of influenza. Unfortunately, there is little known about its pharmacokinetics. Palmitoylethanolamide targets nonclassical cannabinoid receptors rather than CB1 and CB2 receptors. Palmitoylethanolamide will only indirectly activate classical cannabinoid receptors by an entourage effect. There are a significant number of prospective and randomized trials demonstrating the pain-relieving effects of PEA. There is lesser evidence of benefit in patients with nonpain symptoms related to depression, Parkinson disease, strokes, and autism. There are no reported drug–drug interactions and very few reported adverse effects from PEA. Further research is needed to define the palliative benefits to PEA.
Parenteral potent opioid availability is becoming an issue in acute pain management. Two opioids, nalbuphine and buprenorphine, are available which can be substituted for hydromorphone, fentanyl, and morphine. There are advantages and disadvantages in using these 2 opioids which are discussed, and potential dosing strategies are outlined.
Context: Patient’s rating of perceived effort (RPE) is used to assess central fatigue. Cancer-related fatigue (CRF) is believed to be of central origin. The increased RPE with a motor task, such as the Finger-Tapping Test (FTT), can easily be measured in the clinical setting. Objectives: To correlate the FTT, RPE and the Brief Fatigue Inventory (BFI) rated fatigue severity in patients with cancer. Methods: Subjective fatigue was assessed in adult patients with cancer by the BFI. Participants performed a modified FTT with the index finger of the dominant hand: 15 seconds × 2, 30 seconds × 2, and 60 seconds × 2 with 1 minute of rest between each time trial. Rating of perceived effort at the end of task was measured by the Borg 10 scale. Exclusions: Brain metastasis, history of brain radiation, Parkinson disease, Huntington Chorea, multiple sclerosis, delirium, and depression. Pearson correlation coefficients were used to describe the relationships between BFI, FTT, and Borg 10 scale. Results: Thirty patients participated. Mean age was 56.2. Sixteen were females (53.3%). The mean BFI mean was 4.1, median 4.4. Tapping rate did not correlate with fatigue severity. The RPE correlated with the mean BFI: r s 0.438, P = .0155. These correlations persisted after adjustment for age. Conclusion: An increased RPE in the absence of task failure suggests that the origin of CRF is central. The performance of an FTT with RPE helps to improve our understanding of fatigue in the clinical setting.
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