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Opioids Analgesics and Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
R. Rachana, Tanya Gupta, Saumya Yadav, Manisha Singh
Furthermore, in the presence of ultra-low-dose naltrexone, it has been shown that effect of buprenorphine for antinociception can be enhanced. Buprenorphine, an opioid agonist, has antinociceptive effect that is, blocks the pain detection stimuli by sensory neurons. To check its effect in the combination with ultra-low-dose naltrexone, 10 healthy volunteers were randomly administered with its combination as well as, naltrexone alone. The drugs were administered to either of the two arms and then subjected their hand to the ice water (cold pressor test). The results obtained, indicated a huge difference with the increase of 30.9% in cold pressor tolerance when both drugs are given at a dose ratio of 166:1 with the similar side effects (sedation, nausea, and vomiting; Hay et al., 2011).
Fibromyalgia
Published in Sahar Swidan, Matthew Bennett, Advanced Therapeutics in Pain Medicine, 2020
In a larger randomized, double-blind, placebo-controlled, crossover study, LDN was administered at a dose of 4.5 mg daily for a period of 12 weeks with 4 weeks of placebo taken either before or after the LDN treatment period depending on study arm assignment. This study also included a 2-week baseline period and a 4-week follow-up period for a total length of 22 weeks. All participants were told that they had the option to reduce their daily dosage to 3.0 mg if they experienced side effects. Each participant was given a handheld computer to record their pain, fatigue, and other symptoms on a daily basis, and they continued to record their symptoms for 4 weeks after study medication was stopped. Thirty-one women were enrolled and 28 women had sufficient data to be included in the analyses. Study patients experienced a significantly greater reduction in their pain scores while they were taking the LDN as compared with placebo (28.8% reduction versus 18.0% reduction; p = 0.016). More participants met criteria for response (defined as a significant reduction in pain plus a significant reduction in either fatigue or sleep problems) during LDN therapy compared to placebo (32% response during LDN versus 11% response during placebo; p = 0.05). They also reported improved general satisfaction with life and improved mood while taking LDN. However, there was no improvement in fatigue or sleep. All participants tolerated the LDN, with few side effects. Four individuals (three while taking LDN and one while taking placebo) requested the 3.0-mg dosage due to side effects. Side effects resulting in a dose decrease were headaches, heartburn, and irritability. These side effects were reduced by lowering the dosage to 3 mg/day. Low-dose naltrexone may be a great treatment strategy due to its high bioavailability, long history of safe use, low cost, and accessibility.134
The state-of-the-art pharmacotherapeutic options for the treatment of chronic non-cancer pain
Published in Expert Opinion on Pharmacotherapy, 2022
Ryan S. D’Souza, Brendan Langford, Rachel E. Wilson, Yeng F. Her, Justin Schappell, Jennifer S. Eller, Timothy C. Evans, Jonathan M. Hagedorn
While there may remain uncertainly in the medical community when considering use of off-label medications such as NMDA antagonists, lidocaine infusion, alpha-2-channel blockers, and cannabis, the authors emphasize that decisions should be made based on the available evidence that demonstrate clinical efficacy of these drug classes in a variety of chronic non-cancer pain conditions. In patients who fail first-line and second-line agents that carry FDA approval labels, it is entirely reasonable to consider off-label drug use particularly if Level I or II evidence is available. As an illustrative example, it is common for fibromyalgia patients to not experience significant and meaningful relief after taking FDA approved medications including pregabalin, duloxetine, or milnacipran. In this situation, it may be reasonable to offer low-dose naltrexone, which is supported by data from a randomized clinical trial and prospective observational studies.
Impact of extended release naltrexone on health-related quality of life in individuals with legal involvement and opioid use disorders
Published in Substance Abuse, 2021
Ekaterina Pivovarova, Hye Sung Min, Peter D. Friedmann
Looking at the individual QOL scores, there was significant improvement (i.e., reduction in symptoms) on item measuring experience of pain and discomfort. This finding held when we removed individuals who received any OAT during during active phase of the study. No definitive explanation for this can be offered, in speculating it is possible that this finding represents a reduction in opioid-induced hyperalgesia.41 Some research has also found that use of low-dose naltrexone has produced pain relief in inflammatory chronic conditions (e.g., fatigue syndrome,42 Chrohn’s disease,43 fibromyolagia,44 and multiple sclerosis).45 An alternative explanation is that this is a spurious finding that is statistically but not clinically meaningful.
Pilot study of tolerability and safety of opioid receptor antagonists as novel therapies for chronic pain among persons living with HIV with past year heavy drinking: a randomized controlled trial
Published in AIDS Care, 2023
Sally Bendiks, Debbie M. Cheng, Elena Blokhina, Marina Vetrova, Elena Verbitskaya, Natalia Gnatienko, Kendall Bryant, Evgeny Krupitsky, Jeffrey H. Samet, Judith I. Tsui
Opioid receptor antagonists are a candidate class of pharmacotherapy for treatment of chronic pain among PWH and heavy alcohol use. Naltrexone and nalmefene are oral competitive opioid receptor antagonists that are currently licensed to treat alcohol use disorders, but may have potential to treat pain. Low-dose naltrexone has been found effective in reducing pain for a number of conditions, including fibromyalgia and complex-regional pain syndrome (Younger et al., 2014). At low doses (4.5 mg or 1/10th of the dose used for treating alcohol use disorders) naltrexone exerts analgesic effects. Less is known about the analgesic properties of nalmefene, however, its pharmacologic similarity to naltrexone and partial kappa-opioid effects makes it a plausible pharmacotherapy candidate.