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https://www.readbyqxmd.com/read/28507784/geraniin-attenuates-naloxone-precipitated-morphine-withdrawal-and-morphine-induced-tolerance-in-mice
#1
Ella Anle Kasanga, Eric Boakye-Gyasi, Robert Peter Biney, James Oppong Kyekyeku, Christian Agyare, Eric Woode
BACKGROUND AND AIM: Potentially life-threatening and unpleasant side effects associated with some analgesics have fueled the drive for the search for more analgesics with better side effect profiles. Geraniin, the most dominant secondary metabolite in the aqueous extract of the aerial parts of Phyllanthus muellerianus, has been shown to possess antinociceptive properties mediated partly by opioidergic mechanisms. The purpose of this study is to determine whether geraniin exhibits tolerance and if it is able to ameliorate withdrawal signs in naloxone-precipitated morphine withdrawal...
April 2017: Journal of Intercultural Ethnopharmacology
https://www.readbyqxmd.com/read/28493329/risk-to-heroin-users-of-polydrug-use-of-pregabalin-or-gabapentin
#2
Abigail Lyndon, Suzanne Audrey, Claudia Wells, Erica S Burnell, Suzanne Ingle, Rob Hill, Matthew Hickman, Graeme Henderson
AIM: To examine the risk to heroin users of also using gabapentin or pregabalin (gabapentoids). DESIGN: Multi-disciplinary study: we (a) examined trends in drug-related deaths and gabapentoid prescription data in England and Wales to test for evidence that any increase in deaths mentioning gabapentin or pregabalin is associated with trends in gabapentoid prescribing and is concomitant with opioid use; (b) interviewed people with a history of heroin use about their polydrug use involving gabapentin and pregabalin; and (c) studied the respiratory depressant effects of pregabalin in the absence and presence of morphine in mice to determine whether concomitant exposure increased the degree of respiratory depression observed...
May 10, 2017: Addiction
https://www.readbyqxmd.com/read/28490343/roadside-opioid-testing-of-drivers-using-oral-fluid-the-case-of-a-country-with-a-zero-tolerance-law-spain
#3
Inmaculada Fierro, Mónica Colás, Juan Carlos González-Luque, F Javier Álvarez
BACKGROUND: Opioids can impair psychomotor performance, and driving under the influence of opioids is associated with an increased risk of accidents. The goals of this study were i) to determine the prevalence of opioids (heroin, morphine, codeine, methadone and tramadol) in Spanish drivers and ii) to explore the presence of opioids, more specifically whether they are used alone or in combination with other drugs. METHODS: The 2008/9 DRUID database regarding Spain was used, which provided information on 3302 drivers...
May 10, 2017: Substance Abuse Treatment, Prevention, and Policy
https://www.readbyqxmd.com/read/28489639/evaluation-of-analgesia-tolerance-and-the-mechanism-of-action-of-morphine-6-o-sulfate-across-multiple-pain-modalities-in-sprague-dawley-rats
#4
Jai Shankar K Yadlapalli, Navdeep Dogra, Anqi W Walbaum, William D Wessinger, Paul L Prather, Peter A Crooks, Maxim Dobretsov
BACKGROUND: Morphine-6-O-sulfate (M6S) is a mixed μ/δ-opioid receptor (OR) agonist and potential alternative to morphine for treatment of chronic multimodal pain. METHODS: To provide more support for this hypothesis, the antinociceptive effects of M6S and morphine were compared in tests that access a range of pain modalities, including hot plate threshold (HPT), pinprick sensitivity threshold (PST) and paw pressure threshold tests. RESULTS: Acutely, M6S was 2- to 3-fold more potent than morphine in HPT and PST tests, specifically, derived from best-fit analysis of dose-response relationships of morphine/M6S half-effective dose (ED50) ratios (lower, upper 95% confidence interval [CI]) were 2...
May 4, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28474563/opioids-and-the-blood-brain-barrier-a-dynamic-interaction-with-consequences-on-drug-disposition-in-brain
#5
Catarina Chaves, Fernando Remião, Salvatore Cisterninoa, Xavier Declèves
Opioids are widely used in pain management whose effects are due to binding to classical opioid receptors and/or Toll-like receptors (TLR) present at the central nervous system (CNS). At the blood-brain barrier (BBB), several influx and/or efflux transporters are expressed, such as the ATP-binding cassette (ABC) P-glycoprotein (P-gp, ABCB1), Breast Cancer Resistance Protein (BCRP, ABCG2) and multidrug resistance-associated proteins (MRP, ABCC) transporters, and solute carrier transporters (SLC), and are responsible for the transport of many xenobiotics from the brain into the bloodstream or vice versa...
May 3, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28462518/alvimopan-for-recovery-of-bowel-function-after-radical-cystectomy
#6
REVIEW
Shahnaz Sultan, Bernadette Coles, Philipp Dahm
BACKGROUND: Alvimopan is used in abdominal surgery to reduce postoperative ileus in patients undergoing small bowel resections with primary anastomosis. The role and efficacy of alvimopan in patients undergoing radical cystectomy with urinary diversion is not well understood. OBJECTIVES: To assess the effects of alvimopan in the context of enhanced recovery pathways compared to enhanced recovery pathways alone for perioperative bowel dysfunction in patients undergoing radical cystectomy...
May 2, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28450061/morphine-dosing-strategy-plays-a-key-role-in-the-generation-and-duration-of-the-produced-antinociceptive-tolerance
#7
Alok Kumar Paul, Nuri Gueven, Nikolas Dietis
Antinociceptive tolerance after repetitive administration of morphine severely limits its clinical use. Despite increased mechanistic understanding of morphine tolerance, little is known about the influence of dosing regimens in its development. We hypothesized that the starting dose of morphine, dosing frequency and dose increments, influence antinociception and the manifestation of antinociceptive tolerance in rats. Male rats were randomly divided into four groups with different intermittent starting-doses of daily morphine (b...
April 25, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28448398/intrathecal-morphine-versus-extended-release-epidural-morphine-for-postoperative-pain-control-in-pediatric-patients-undergoing-posterior-spinal-fusion
#8
Mindy Cohen, Jeannie Zuk, Nancy McKay, Mark Erickson, Zhaoxing Pan, Jeffrey Galinkin
BACKGROUND: Posterior spinal fusion for scoliosis is one of the most painful elective pediatric surgeries. Good postoperative pain control allows early ambulation and return of ability to tolerate oral intake. Options for analgesia in this patient population are suboptimal. We hypothesized that extended-release epidural morphine (EREM) would provide better pain control and less adverse effects compared to intrathecal (IT) morphine. METHODS: The primary outcome was total IV morphine consumption during 0-48 hours postoperatively...
June 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/28442580/ethanol-reversal-of-tolerance-to-the-antinociceptive-effects-of-oxycodone-and-hydrocodone
#9
Joanna C Jacob, Justin L Poklis, Hamid I Akbarali, Graeme Henderson, William L Dewey
This study compared the development of tolerance and its reversal by ethanol of two orally-bioavailable prescription opioids, oxycodone and hydrocodone, to that of morphine. Oxycodone (s.c) was significantly more potent in the mouse tail withdrawal assay than either morphine or hydrocodone. Oxycodone was also significantly more potent in this assay than hydrocodone when administered orally. Tolerance was seen following chronic subcutaneous administration of each of the three drugs and by the chronic administration of oral oxycodone, but not following the chronic oral administration of hydrocodone...
April 25, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28426670/mice-expressing-a-hyper-sensitive-form-of-the-cb1-cannabinoid-receptor-cb1-show-modestly-enhanced-alcohol-preference-and-consumption
#10
David J Marcus, Angela N Henderson-Redmond, Maciej Gonek, Michael L Zee, Jill C Farnsworth, Randa A Amin, Mary-Jeanette Andrews, Brian J Davis, Ken Mackie, Daniel J Morgan
We recently characterized S426A/S430A mutant mice expressing a desensitization-resistant form of the CB1 receptor. These mice display an enhanced response to endocannabinoids and ∆9-THC. In this study, S426A/S430A mutants were used as a novel model to test whether ethanol consumption, morphine dependence, and reward for these drugs are potentiated in mice with a "hyper-sensitive" form of CB1. Using an unlimited-access, two-bottle choice, voluntary drinking paradigm, S426A/S430A mutants exhibit modestly increased intake and preference for low (6%) but not higher concentrations of ethanol...
2017: PloS One
https://www.readbyqxmd.com/read/28423675/mir-219-5p-targets-camkii%C3%AE-to-attenuate-morphine-tolerance-in-rats
#11
Jian Wang, Wei Xu, Jiali Shao, Zhenghua He, Zhuofeng Ding, Jiangju Huang, Qulian Guo, Wangyuan Zou
Morphine tolerance is a clinical challenge in pain management. Emerging evidence suggests that microRNA (miRNA) plays a regulatory role in the development of morphine tolerance. miR-219-5p (miR-219) targets calmodulin-dependent protein kinase II γ (CaMKIIγ) to activate central pain sensitization via N-methyl-D-aspartate (NMDA) receptor. Therefore, we hypothesized that miR-219-5p attenuates morphine tolerance by targeting CaMKIIγ. We found that the expression of miR-219-5p was decreased significantly after chronic morphine treatment...
April 25, 2017: Oncotarget
https://www.readbyqxmd.com/read/28418861/brain-derived-neurotrophic-factor-involved-epigenetic-repression-of-ugt2b7-in-colorectal-carcinoma-a-mechanism-to-alter-morphine-glucuronidation-in-tumor
#12
Zi-Zhao Yang, Li Li, Ming-Cheng Xu, Hai-Xing Ju, Miao Hao, Jing-Kai Gu, Zai-Jie Jim Wang, Hui-Di Jiang, Lu-Shan Yu, Su Zeng
Uridine diphosphate-glucuronosyltransferase (UGT) 2B7, as one of significant drug enzymes, is responsible on the glucuronidation of abundant endobiotics or xenobiotics. We here report that it is markedly repressed in the tumor tissues of colorectal carcinoma (CRC) patients. Accordingly, morphine in CRC cells will stimulate the expression of its main metabolic enzyme, UGT2B7 during tolerance generation by activating the positive signals in histone 3, especially for trimethylated lysine 27 (H3K4Me3) and acetylated lysine 4 (H3K27Ac)...
April 25, 2017: Oncotarget
https://www.readbyqxmd.com/read/28379583/b-vitamins-potentiate-acute-morphine-antinociception-and-attenuate-the-development-of-tolerance-to-chronic-morphine-in-mice
#13
Xue-Ting Deng, Yuan Han, Wen-Tao Liu, Xue-Jun Song
Objectives. : Opiate analgesics are the most effective treatments for severe pain, but their clinical utility is often hampered by the development of analgesic tolerance. There are striking similarities between morphine actions and neuropathic pain. We have demonstrated that B vitamins can attenuate neuropathic pain after peripheral nerve injury, sensory neuron inflammation/compression, and transient spinal cord ischemia. Given this similarity, the present study investigated whether B vitamins might be able to modify the antinociceptive effect of morphine as well as morphine tolerance in mice...
March 31, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/28378462/targeting-multiple-opioid-receptors-improved-analgesics-with-reduced-side-effects
#14
REVIEW
Thomas Günther, Pooja Dasgupta, Anika Mann, Elke Miess, Andrea Kliewer, Sebastian Fritzwanker, Ralph Steinborn, Stefan Schulz
Classical opioid analgesics, including morphine, mediate all of their desired and undesired effects by specific activation of the μ-opioid receptor (μ receptor). The use of morphine for treating chronic pain, however, is limited by the development of constipation, respiratory depression, tolerance and dependence. Analgesic effects can also be mediated through other members of the opioid receptor family such as the κ-opioid receptor (κ receptor), δ-opioid receptor (δ receptor) and the nociceptin/orphanin FQ peptide receptor (NOP receptor)...
April 5, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28368571/recent-advances-in-the-realm-of-allosteric-modulators-for-opioid-receptors-for-future-therapeutics
#15
Michael Remesic, Victor J Hruby, Frank Porreca, Yeon Sun Lee
Opioids, and more specifically μ-opioid receptor (MOR) agonists such as morphine, have long been clinically used as therapeutics for severe pain states but often come with serious side effects such as addiction and tolerance. Many studies have focused on bringing about analgesia from the MOR with attenuated side effects, but its underlying mechanism is not fully understood. Recently, focus has been geared toward the design and elucidation of the orthosteric site with ligands of various biological profiles and mixed subtype opioid activities and selectivities, but targeting the allosteric site is an area of increasing interest...
April 7, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28365372/endogenous-opioid-function-and-responses-to-morphine-the-moderating-effects-of-anger-expressiveness
#16
John W Burns, Stephen Bruehl, Christopher R France, Erik Schuster, Daria Orlowska, Melissa Chont, Rajnish K Gupta, Asokumar Buvanendran
Long-term use of opioid analgesics may be ineffective or associated with significant negative side effects for some people. At present, there is no sound method of identifying optimal opioid candidates. Individuals with chronic low back pain (n = 89) and healthy control individuals (n = 102) underwent ischemic pain induction with placebo, opioid blockade (naloxone), and morphine in counterbalanced order. They completed the Spielberger Anger-Out subscale. Endogenous opioid function × Anger-out × Pain status (chronic pain, healthy control) interactions were tested for morphine responses to ischemic threshold, tolerance, and pain intensity (McGill Sensory and Affective subscales) and side effects...
March 30, 2017: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/28361126/pressure-sensitivity-and-phenotypic-changes-in-patients-with-suspected-opioid-induced-hyperalgesia-being-withdrawn-from-full-mu-agonists
#17
Ronald A Wasserman, Afton L Hassett, Steven E Harte, Jenna Goesling, Herbert L Malinoff, Daniel W Berland, Jennifer Zollars, Stephanie E Moser, Chad M Brummett
OBJECTIVES: To assess changes in phenotype and pressure sensitivity in patients with suspected opioid-induced-hyperalgesia (OIH) after transitioning to buprenorphine. METHODS: Twenty patients with suspected OIH were enrolled to transition to buprenorphine therapy. Patients completed validated self-report measures at baseline and at 1, 4, 8 weeks, and 6 months after initiation of buprenorphine along with quantitative sensory testing including measures of pressure pain threshold, pain tolerance and Pain 50 (a pain intensity rating)...
February 2017: Journal of Nature and Science
https://www.readbyqxmd.com/read/28360013/a-review-of-the-role-of-orexin-system-in-pain-modulation
#18
REVIEW
Bibi Marjan Razavi, Hossein Hosseinzadeh
The roles of orexinergic system (orexin-A, orexin-B) and their receptors (orexin receptor type-1, orexin receptor type-2) in various physiological processes such as arousal, reward seeking behavior, energy homeostasis, sensory modulation, stress processing, cognition, endocrine functions, visceral functions and pain modulation have been established. This review summarizes the studies investigating orexin antinociceptive effects and their cellular mechanisms in various types of pain including neuropathic pain, migraine and cluster headache, visceral and orofacial pains...
June 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28356897/novel-molecular-strategies-and-targets-for-opioid-drug-discovery-for-the-treatment-of-chronic-pain
#19
REVIEW
Keith M Olson, Wei Lei, Attila Keresztes, Justin LaVigne, John M Streicher
Opioid drugs like morphine and fentanyl are the gold standard for treating moderate to severe acute and chronic pain. However, opioid drug use can be limited by serious side effects, including constipation, tolerance, respiratory suppression, and addiction. For more than 100 years, we have tried to develop opioids that decrease or eliminate these liabilities, with little success. Recent advances in understanding opioid receptor signal transduction have suggested new possibilities to activate the opioid receptors to cause analgesia, while reducing or eliminating unwanted side effects...
March 2017: Yale Journal of Biology and Medicine
https://www.readbyqxmd.com/read/28352316/monocyte-chemoattractant-protein-1-contributes-to-morphine-tolerance-in-rats-with-cancer-induced-bone-pain
#20
Lei Liu, Xiu-Juan Gao, Chun-Guang Ren, Ji-Hua Hu, Xian-Wen Liu, Ping Zhang, Zong-Wang Zhang, Zhi-Jian Fu
Cancer-induced bone pain can severely compromise the life quality of patients, while tolerance limits the use of opioids in the treatment of cancer pain. Monocyte chemoattractant protein-1 (MCP-1) is known to contribute to neuropathic pain. However, the role of spinal MCP-1 in the development of morphine tolerance in patients with cancer-induced bone pain remains unclear. The aim of the present study was to investigate the role of spinal MCP-1 in morphine tolerance in bone cancer pain rats (MTBP rats). Bone cancer pain was induced by intramedullary injection of Walker 256 cells into the tibia of the rats, while morphine tolerance was induced by continuous intrathecal injection of morphine over a period of 9 days...
February 2017: Experimental and Therapeutic Medicine
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