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morphine tolerance

Maria Elena Giusepponi, Carlo Cifani, Maria Vittoria Micioni Di Bonaventura, Laura Mattioli, Alan Hudson, Eleonora Diamanti, Fabio Del Bello, Mario Giannella, Valerio Mammoli, Corinne Dalila Paoletti, Alessandro Piergentili, Maria Pigini, Wilma Quaglia
Tolerance and dependence associated with chronic opioid exposure result from molecular, cellular, and neural network adaptations. Such adaptations concern opioid and nonopioid systems, including α2-adrenoceptors (α2-ARs) and I1- and I2-imidazoline binding sites (IBS). Agmatine, one of the hypothesized endogenous ligands of IBS, targeting several systems including α2-ARs and IBS, proved to be able to regulate opioid-induced analgesia and to attenuate the development of tolerance and dependence. Interested in the complex pharmacological profile of agmatine and considering the nature of its targets, we evaluated two series of imidazolines, rationally designed to simultaneously interact with I1-/I2-IBS or I1-/I2-IBS/α2-ARs...
October 13, 2016: ACS Medicinal Chemistry Letters
J Voirin, I Darie, D Fischer, A Simon, I Rohmer-Heitz, F Proust
INTRODUCTION: Motor cortex stimulation is a well-known treatment modality for refractory neuropathic pain. Nevertheless, some cases of therapeutic failure have been described but alternative therapies for these cases are rarely reported. CASE REPORT: The patient presented with neuropathic pain in his right arm due to a cervical syrinx which was surgically treated by a shunt in 2003 with no clinical improvement. As alternative therapy, after an evaluation by repetitive magnetic transcranial stimulation with significant benefit, motor cortex stimulation was successfully implanted in 2004...
October 19, 2016: Neuro-Chirurgie
Pranav Prasoon, Shivani Gupta, Rahul Kumar, Mayank Gautam, Saroj Kaler, Subrata Basu Ray
OBJECTIVES: Opioids such as morphine form the cornerstone in the treatment of moderate to severe pain. However, opioids also produce serious side effects such as tolerance. Fosaprepitant is a substance P (SP) receptor antagonist, which is used for treating chemotherapy-induced nausea and vomiting. SP is an important neuropeptide mediating transmission of pain at the spinal level. Thus, it was hypothesized that combining morphine with fosaprepitant would increase the antinociceptive effect of morphine...
July 2016: Indian Journal of Pharmacology
Guang-Lun Xie, Da-Peng Guo, Zhi-Gang Li, Chang Liu, Wei Zhang
This study aimed to observe the therapeutic effects and adverse reactions of radiofrequency thermocoagulation combined with adriamycin injection in dorsal root ganglia on lung cancer rib metastasis-related refractory pain which has no response to conventional therapy.This study contained 27 patients with lung cancer rib metastasis-related moderate or severe pain which had no response to conventional therapy. Under computed tomography (CT)-guidance, radiofrequency puncture need reached the corresponding intervertebral foramens to ensure needle point near dorsal root ganglia (DRG) by sensory and motor stimulation tests, and then radiofrequency thermocoagulation was performed on each corresponding DRG followed by injection of 0...
October 2016: Medicine (Baltimore)
Taddesse Yayeh, Kyunghwa Yun, Soyong Jang, Seikwan Oh
BACKGROUND: Red ginseng and ginsenosides have shown plethoric effects against various ailments. However, little is known regarding the effect of red ginseng on morphine-induced dependence and tolerance. We therefore investigated the effect of red ginseng extract (RGE) and biotransformed ginsenosides Rh2, Rg3, and compound K on morphine-induced dependence in mice and rats. METHODS: While mice were pretreated with RGE and then morphine was injected intraperitoneally, rats were infused with ginsenosides and morphine intracranially for 7 days...
October 2016: Journal of Ginseng Research
Tyler A Johnson, Laura Milan-Lobo, Tao Che, Madeline Ferwerda, Eptisam Lambo, Nicole L McIntosh, Fei Li, Li He, Nicholas Lorig-Roach, Phillip Crews, Jennifer Lynne Whistler
Opioid therapeutics are excellent analgesics, whose utility is compromised by dependence. Morphine (1) and its clinically relevant derivatives such as OxyContin® (4), Vicodin® (5) and Dilaudid® (6) are "biased" agonists at the µ opioid receptor (OR), wherein they engage G-protein signaling but poorly engage β-arrestin and the endocytic machinery. In contrast, the endorphins, met-enkephalin (14) and β-endorphin (15), endogenous peptide agonists for ORs, are more potent analgesics then 1, show reduced liability for tolerance and dependence, and engage both G-protein and β-arrestin pathways as "balanced" agonists...
October 17, 2016: ACS Chemical Neuroscience
Ernesto Zecca, Cinzia Brunelli, Paola Bracchi, Giuseppe Biancofiore, Carlo De Sangro, Roberto Bortolussi, Luigi Montanari, Marco Maltoni, Cecilia Moro, Ugo Colonna, Gabriele Finco, Maria Teresa Roy, Vittorio Ferrari, Oscar Alabiso, Giovanni Rosti, Stein Kaasa, Augusto Caraceni
: Context Oxycodone and morphine are recommended as first-choice opioids for moderate/severe cancer pain but evidence about their relative tolerability has significant methodological limitations. OBJECTIVES: This study is mainly aimed at comparing the risk of developing adverse events (AEs) with controlled release oral morphine versus oxycodone; secondary aims were comparing their analgesic efficacy and testing heterogeneity in tolerability across different age and renal function subgroups...
October 11, 2016: Journal of Pain and Symptom Management
Darakhshan Jabeen Haleem, Shazia Nawaz
: Morphine and other opioids are amongst most effective prescription medications for the treatment of pain. Addiction and hyperalgesia associated with their long-term use, limits the clinical utility of these drugs. In view of a role of somatodendritic serotonin-1A receptors in addiction and analgesic effects of morphine, the present study concerns effects of co-use of buspirone, a partial agonist at serotonin-1A receptor, on reinforcing, hyperalgesic and motor effects of morphine in rats...
October 11, 2016: Journal of Pain: Official Journal of the American Pain Society
Sumita Chakrabarti, Andrew Chang, Nai-Jiang Liu, Alan R Gintzler
Caveolin-1 is the predominant structural protein of caveolae, a subset of (lipid) membrane rafts that compartmentalize cell signaling. Caveolin-1 binds most to G protein-coupled receptors and their signaling partners, thereby enhancing interactions among signaling cascade components and the relative activation of specific G protein-coupled pathways. This study reveals that chronic opioid exposure of μ-opioid receptor (MOR) expressing Chinese hamster ovary cells (MOR-CHO) and chronic in vivo morphine exposure of rat spinal cord augmented recruitment of multiple components of MOR-adenylyl cyclase (AC) stimulatory signaling by caveolin-1...
October 10, 2016: Journal of Neurochemistry
Xiao-Fei Wang, Elisabeth Barbier, Yi-Ting Chiu, Yi He, Jia Zhan, Guo-Hua Bi, Hai-Ying Zhang, Bo Feng, Lee-Yuan Liu-Chen, Jia Bei Wang, Zheng-Xiong Xi
: The etiology and pathophysiology underlying opioid tolerance and dependence are still unknown. Because mu opioid receptor (MOR) plays an essential role in opioid action, many vulnerability-related studies have focused on single nucleotide polymorphisms of MOR, particularly on A118G. In this study, we found that a single-point mutation at the MOR T394 phosphorylation site could be another important susceptive factor in the development of opioid tolerance and dependence in mice. T394A mutation, in which a threonine at 394 was replaced by an alanine, did not alter agonist binding to MOR and opioid analgesia, but resulted in loss of etorphine-induced MOR internalization in spinal dorsal horn neurons and opioid analgesic tolerance induced by either morphine or etorphine...
October 5, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
Daniel Ruiz-Pérez, Javier Benito, Carlota Largo, Gonzalo Polo, Susana Canfrán, Ignacio Alvarez Gómez de Segura
Unlike non-steroidal anti-inflammatory drugs (NSAIDs), metamizole has poor anti-inflammatory effects; and is suitable for models where analgesia, but not anti-inflammatory effects, is desirable. Like opioids, these drugs produce perioperative analgesia while reducing anaesthetic requirements, but it remains unclear whether they may develop tolerance or hyperalgesia, and thus decrease in analgesic efficacy. The aim was to determine whether tolerance or hyperalgesia to metamizole occurred in rats, and whether the sevoflurane minimum alveolar concentration (MAC) was affected...
September 30, 2016: Laboratory Animals
W Porter McRoberts, Catalina Apostol, Abdul Haleem
UNLABELLED: Complex regional pain syndrome (CRPS) presents a therapeutic challenge due to its many presentations and multifaceted pathophysiology. There is no approved treatment algorithm and clinical interventions are often applied empirically. In cases of CRPS where symptoms are localized to an extremity, a targeted treatment is indicated. We describe the use of intrathecal bupivacaine monotherapy, delivered through a retrograde catheter, in the treatment of CRPS affecting the lower extremity...
September 2016: Pain Physician
Lei Sima, Bifa Fan, Longtao Yan, Yuan Shui
Objective. To explore the efficacy of electroacupuncture treatment in cancer induced bone pain (CIBP) rat model with morphine tolerance and explore changes of calcitonin-gene related peptide (CGRP) expression in dorsal root ganglion (DRG). Methods. Forty SD rats were divided into five groups: sham, CIBP (B), CIBP + morphine (BM), CIBP + electroacupuncture (BE), and CIBP + morphine + electroacupuncture (BME). B, BM, BE, and BME groups were prepared CIBP model. The latter three groups then accepted morphine, electroacupuncture, and morphine combined electroacupuncture, separately, nine days consecutively (M1 to M9)...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
Sudha Arumugam, Christine Sm Lau, Ronald S Chamberlain
OBJECTIVES: Effective postoperative pain management is crucial in the care of surgical patients. Opioids, which are commonly used in managing postoperative pain, have a potential for tolerance and addiction, along with sedating side effects. Gabapentin's use as a multimodal analgesic regimen to treat neuropathic pain has been documented as having favorable side effects. This meta-analysis examined the use of preoperative gabapentin and its impact on postoperative opioid consumption. MATERIALS AND METHODS: A comprehensive literature search was conducted to identify randomized control trials that evaluated preoperative gabapentin on postoperative opioid consumption...
2016: Journal of Pain Research
Ernest A Kopecky, Alison B Fleming, Naama Levy-Cooperman, Melinda O'Connor, Edward Sellers
Oxycodone DETERx(®) (Collegium Pharmaceutical Inc, Canton, MA) is an extended-release, microsphere-in-capsule, abuse-deterrent formulation designed to retain its extended-release properties after tampering (eg, chewing/crushing). This randomized, double-blind, placebo-controlled, triple-dummy study evaluated the oral abuse potential of intact and chewed oxycodone DETERx capsules compared with crushed immediate-release oxycodone. Subjects with a history of recreational opioid use who were nondependent/nontolerant to opioids were enrolled...
September 27, 2016: Journal of Clinical Pharmacology
Mun Keong Kwan, Chee Kidd Chiu, Teik Seng Chan, Kok Ian Chong, Siti Mariam Mohamad, Mohd Shahnaz Hasan, Chris Yin Wei Chan
STUDY DESIGN: Prospective Cohort Study. OBJECTIVE: To determine and evaluate the trajectory of surgical wound pain from day 1 to day 14 after PSF surgery in AIS patients. SUMMARY OF BACKGROUND DATA: Information regarding how the post-operative pain improves with time offers invaluable information not only to the patients and parents but also to assist the clinician in managing post-operative pain. METHODS: AIS patients who were planned for elective PSF surgery from September 2015 to December 2015 were prospectively recruited into this study...
September 23, 2016: Spine
Jai Shankar K Yadlapalli, Benjamin M Ford, Amit Ketkar, Anqi Wan, Narasimha R Penthala, Robert L Eoff, Paul L Prather, Maxim Dobretsov, Peter A Crooks
: This study determined the antinociceptive effects of morphine and morphine-6-O-sulfate (M6S) in both normal and diabetic rats, and evaluated the comparative role of mu-opioid receptors (mu-ORs) and delta-opioid receptors (delta-ORs) in the antinociceptive action of these opioids. In vitro characterization of mu-OR and delta-OR-mediated signaling by M6S and morphine in stably transfected Chinese hamster ovary (CHO-K1) cells showed that M6S exhibited a 6-fold higher affinity for delta-ORs and modulated G-protein and adenylyl cyclase activity via delta-ORs more potently than morphine...
September 13, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
Zi-Zhao Yang, Li Li, Lu Wang, Ming-Cheng Xu, Sai An, Chen Jiang, Jing-Kai Gu, Zai-Jie Jim Wang, Lu-Shan Yu, Su Zeng
Regulating main brain-uptake transporter of morphine may restrict its tolerance generation, then modify its antinociception. In this study, more than 2 fold higher intracellular uptake concentrations for morphine and morphine-6-glucuronide (M6G) were observed in stable expression cells, HEK293-hOATP2B1 than HEK293-MOCK. Specifically, the Km value of morphine to OATP2B1 (57.58 ± 8.90 μM) is 1.4-time more than that of M6G (80.31 ± 21.75 μM); Cyclosporine A (CsA), an inhibitor of OATP2B1, can inhibit their intracellular accumulations with IC50 = 3...
2016: Scientific Reports
Masanori Mori, Yongli Ji, Santosh Kumar, Takamaru Ashikaga, Steven Ades
BACKGROUND: Methylnaltrexone is a peripherally acting mu-opioid receptor antagonist that has been shown to relieve severe opioid-induced constipation (OIC) in patients with advanced disease receiving palliative care. Its efficacy remains unknown in cancer patients who are not terminally ill. The primary aim of this study was to evaluate the efficacy of methylnaltrexone over 48 h in cancer patients who were not terminally ill. METHODS: In this single-dose phase II trial, cancer patients with a prognosis of ≥3 months and OIC with <3 laxations during the preceding week were eligible...
September 15, 2016: International Journal of Clinical Oncology
Xue-Ming Hu, Shou-Bin Cao, Hai-Long Zhang, Dong-Mei Lyu, Li-Ping Chen, Heng Xu, Zhi-Qiang Pan, Wen Shen
BACKGROUND: Increasing evidence suggests that microRNAs are functionally involved in the initiation and maintenance of pain hypersensitivity, including chronic morphine analgesic tolerance, through the posttranscriptional regulation of pain-related genes. We have previously demonstrated that miR-219 regulates inflammatory pain in the spinal cord by targeting calcium/calmodulin-dependent protein kinase II gamma (CaMKIIγ). However, whether miR-219 regulates CaMKIIγ expression in the dorsal root ganglia to mediate morphine tolerance remains unclear...
2016: Molecular Pain
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