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https://www.readbyqxmd.com/read/29761672/emergency-department-administration-of-oxycodone-by-nurses-treating-musculoskeletal-pain-an-observational-prospective
#1
Mansour Khoury, Sigalit Caspi, Ruth Stalnikowics, Elad Peless, Ela Raiizman, Shaden Salameh
BACKGROUND: Acute musculoskeletal pain is one of the most commonly reported symptoms among patients visiting the emergency department (ED). Treatment with over-the-counter pain medications, given by nurses, results in improved pain management and reduces the waiting time to drug administration without significant side effects. Opioid analgesics are extensively used for acute pain in the ED. Compared to morphine, oxycodone has a much more specific pharmacological activity, higher analgesic potential, and more tolerable side effects...
May 2018: Israel Medical Association Journal: IMAJ
https://www.readbyqxmd.com/read/29757600/dark-classics-in-chemical-neuroscience-morphine
#2
Andrea L Devereaux, Susan L Mercer, Christopher W Cunningham
As the major psychoactive agent in opium and direct precursor for heroin, morphine is a historically critical molecule in chemical neuroscience. A structurally complex phenanthrene alkaloid produced by Papaver somniferum, morphine has fascinated chemists seeking to disentangle pharmacologically beneficial analgesic effects from addiction, tolerance, and dependence liabilities. In this review, we will detail the history of morphine, from the first extraction and isolation by Sertürner in 1804 to the illicit use of morphine and proliferation of opioid use and abuse disorders currently ravaging the United States...
May 14, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29752818/fluoxetine-uses-in-nociceptive-pain-management-a-promising-adjuvant-to-opioid-analgesics
#3
Mostafa M Hamdy, Mohamed M Elbadr, Ahmed Barakat
Fluoxetine, a commonly prescribed antidepressant, use in nociceptive pain management represent one of the unsettled issues of fluoxetine therapeutics. By reviewing the literature about fluoxetine's possible roles in this setting; those could be solitary antinociceptive effect, enhancement of acute morphine analgesia, blocking morphine tolerance development, and blocking dependence development and associated abstinence syndrome. In this study, we examined those four alleged roles of fluoxetine. Moreover, since effective alleviation of morphine tolerance, dependence, and abstinence syndrome represents one of the most challenging medical needs, we biochemically analyzed fluoxetine effect on these phenomena...
May 12, 2018: Fundamental & Clinical Pharmacology
https://www.readbyqxmd.com/read/29751227/ampa-receptor-positive-allosteric-modulators-attenuate-morphine-tolerance-and-dependence
#4
Xiaoyu Hu, Xuebi Tian, Xiao Guo, Ying He, Haijun Chen, Jia Zhou, Zaijie Jim Wang
Development of opioid tolerance and dependence hinders the use of opioids for the treatment of chronic pain. In searching for the mechanism and potential intervention for opioid tolerance and dependence, we studied the action of two positive allosteric modulators of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor (AMPAR PAMs). In mice treated with morphine (100 mg/kg, s.c.), acute morphine tolerance and dependence developed in 4-6 h. Treatment with aniracetam, a well-established AMPAR PAM, was able to completely prevent and reverse the development of acute antinociceptive tolerance to morphine...
April 25, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29729431/effects-of-cannabinoid-type-2-receptor-agonist-am1241-on-morphine-induced-antinociception-acute-and-chronic-tolerance-and-dependence-in-mice
#5
Mingyue Zhang, Linlin Dong, Huichao Zou, Junnan Li, Quanyi Li, Guonian Wang, Hulun Li
Morphine is a potent opioid analgesic used to alleviate moderate or severe pain but the development of drug tolerance and dependence limits its use in pain management. Previous studies showed that cannabinoid type 2 (CB2 ) receptor ligands may modulate opioid effects. However, there is no report of the effect of CB2 receptor agonist on acute morphine tolerance and physical dependence. We therefore investigated the effect of a CB2 receptor agonist (AM1241) on morphine-induced morphine tolerance and physical dependence in mice...
May 2, 2018: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/29726847/opioid-induced-hyperalgesia-in-the-nonsurgical-setting-a-systematic-review
#6
David Z Yang, Billy Sin, Joshua Beckhusen, Dawei Xia, Rebecca Khaimova, Ilia Iliev
BACKGROUND: Opioid-induced hyperalgesia (OIH) is a phenomenon that causes an increased pain sensitization and perception of pain to noxious stimuli secondary to opioid exposure. While this clinical effect has been described in the surgical setting, it is unclear if OIH occurs in the nonsurgical setting. STUDY QUESTION: To review the available literature which evaluated OIH in nonsurgical settings. DATA SOURCES: A comprehensive literature search was performed using PubMed (January 1946-July 2017) using a variety of keywords for OIH...
January 31, 2018: American Journal of Therapeutics
https://www.readbyqxmd.com/read/29713080/complex-formation-between-the-vasopressin-1b-receptor-%C3%AE-arrestin-2-and-the-%C3%AE-opioid-receptor-underlies-morphine-tolerance
#7
Taka-Aki Koshimizu, Kenji Honda, Sachi Nagaoka-Uozumi, Atsuhiko Ichimura, Ikuo Kimura, Michio Nakaya, Nobuya Sakai, Katsushi Shibata, Kentarou Ushijima, Akio Fujimura, Akira Hirasawa, Hitoshi Kurose, Gozoh Tsujimoto, Akito Tanoue, Yukio Takano
Chronic morphine exposure upregulates adenylate cyclase signaling and reduces analgesic efficacy, a condition known as opioid tolerance. Nonopioid neurotransmitters can enhance morphine tolerance, but the mechanism for this is poorly understood. We show that morphine tolerance was delayed in mice lacking vasopressin 1b receptors (V1bRs) or after administration of V1bR antagonist into the rostral ventromedial medulla, where transcripts for V1bRs and μ-opioid receptors are co-localized. Vasopressin increased morphine-binding affinity in cells expressing both V1bR and μ-opioid receptors...
April 30, 2018: Nature Neuroscience
https://www.readbyqxmd.com/read/29710079/neurobiology-of-opioid-use-disorder-and-comorbid-traumatic-brain-injury
#8
Thomas R Kosten, David P Graham, David A Nielsen
Importance: Treating patients with opioid use disorder (OUD) and traumatic brain injury illustrates 6 neurobiological principles about the actions of 2 contrasting opioid analgesics, morphine and fentanyl, as well as pharmacotherapies for OUD, methadone, naltrexone, and buprenorphine. Observations: This literature review focused on a patient with traumatic brain injury who developed OUD from chronic morphine analgesia. His treatment is described in a neurobiological framework of 6 opioid action principles...
April 25, 2018: JAMA Psychiatry
https://www.readbyqxmd.com/read/29709623/kisspeptin-modulates-pain-sensitivity-of-cflp-mice
#9
Krisztina Csabafi, Zsolt Bagosi, Éva Dobó, Júlia Szakács, Gyula Telegdy, Gyula Szabó
Kisspeptin, a hypothalamic neuropeptide, is a member of the RF-amide family, which have been known to modify pain sensitivity in rodents. The aim of the present study was to investigate the effect of kisspeptin-13 (KP-13), an endogenous derivative of kisspeptin, on nociception in adult male and female CFLP mice and the possible interaction of KP-13 with morphine on nociception. Mice were injected with different doses of KP-13, 30, 60 and 120 min after of which the nociceptive sensitivity were assessed via the tail-flick test...
April 27, 2018: Peptides
https://www.readbyqxmd.com/read/29708942/a-bifunctional-biased-mu-opioid-agonist-neuropeptide-ff-receptor-antagonist-as-analgesic-with-improved-acute-and-chronic-side-effects
#10
Armand Drieu la Rochelle, Karel Guillemyn, Maria Dumitrascuta, Charlotte Martin, Valérie Utard, Raphaëlle Quillet, Séverine Schneider, François Daubeuf, Tom Willemse, Pieter Mampuys, Bert U W Maes, Nelly Frossard, Frédéric Bihel, Mariana Spetea, Frédéric Simonin, Steven Ballet
Opioid analgesics, such as morphine, oxycodone and fentanyl, are the cornerstones for treating moderate to severe pain. However, upon chronic administration, their efficiency is limited by prominent side effects such as analgesic tolerance and dependence liability. Neuropeptide FF (NPFF) and its receptors (NPFF1R and NPFF2R) are recognized as an important pronociceptive system involved in opioid-induced hyperalgesia and analgesic tolerance. Herein, we report the design of multitarget peptidomimetic compounds that show high affinity binding to the mu opioid receptor (MOPr) and NPFFRs...
April 26, 2018: Pain
https://www.readbyqxmd.com/read/29699732/vertebral-fragility-fractures-vff-who-when-and-how-to-operate
#11
Opinder Sahota, Terence Ong, Khalid Salem
Vertebral Fragility Fractures (VFF) are common and lead to pain, long term disability and increased mortality. Most patients will have mild to moderate pain symptoms and can be managed conservatively. However, patients with severe pain who have minimal or no pain relief with potent analgesia, or who only achieve adequate pain relief with high doses of morphine based analgesia which results in significant adverse events, should be considered for vertebral augmentation. Ideally, for vertebral augmentation, patients should present within four months of the fracture (onset of acute pain) and have at least 3 weeks of failure of conservative treatment although early intervention may be more appropriate for hospitalised patients, who tend to be older, more frail and likely to be less tolerant to the adverse effects of conservative treatment...
April 22, 2018: Injury
https://www.readbyqxmd.com/read/29676689/intravenous-acetaminophen-for-postoperative-supratentorial-craniotomy-pain-a-prospective-randomized-double-blinded-placebo-controlled-trial
#12
Walavan Sivakumar, Michael Jensen, Julie Martinez, Michael Tanana, Nancy Duncan, Robert Hoesch, Jay K Riva-Cambrin, Craig Kilburg, Safdar Ansari, Paul A House
OBJECTIVE Acute pain control after cranial surgery is challenging. Prior research has shown that patients experience inadequate pain control post-craniotomy. The use of oral medications is sometimes delayed because of postoperative nausea, and the use of narcotics can impair the evaluation of brain function and thus are used judiciously. Few nonnarcotic intravenous (IV) analgesics exist. The authors present the results of the first prospective study evaluating the use of IV acetaminophen in patients after elective craniotomy...
April 20, 2018: Journal of Neurosurgery
https://www.readbyqxmd.com/read/29662325/sonic-hedgehog-signaling-in-spinal-cord-contributes-to-morphine-induced-hyperalgesia-and-tolerance-through-upregulating-brain-derived-neurotrophic-factor-expression
#13
Su Liu, Jun-Li Yao, Xin-Xin Wan, Zhi-Jing Song, Shuai Miao, Ye Zhao, Xiu-Li Wang, Yue-Peng Liu
Purpose: Preventing opioid-induced hyperalgesia and tolerance continues to be a major clinical challenge, and the underlying mechanisms of hyperalgesia and tolerance remain elusive. Here, we investigated the role of sonic hedgehog (Shh) signaling in opioid-induced hyperalgesia and tolerance. Methods: Shh signaling expression, behavioral changes, and neurochemical alterations induced by morphine were analyzed in male adult CD-1 mice with repeated administration of morphine...
2018: Journal of Pain Research
https://www.readbyqxmd.com/read/29649035/pharmacological-characterization-of-levorphanol-a-g-protein-biased-opioid-analgesic
#14
Valerie Le Rouzic, Ankita Narayan, Amanda Hunkle, Gina F Marrone, Zhigang Lu, Susruta Majumdar, Jin Xu, Ying-Xian Pan, Gavril W Pasternak
BACKGROUND: Levorphanol is a potent analgesic that has been used for decades. Most commonly used for acute and cancer pain, it also is effective against neuropathic pain. The recent appreciation of the importance of functional bias and the uncovering of multiple µ opioid receptor splice variants may help explain the variability of patient responses to different opioid drugs. METHODS: Here, we evaluate levorphanol in a variety of traditional in vitro receptor binding and functional assays...
April 11, 2018: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29626506/hippocampal-glial-cells-modulate-morphine-induced-behavioral-responses
#15
Fatemehsadat Seyedaghamiri, Soomaayeh Heysieattalab, Narges Hosseinmardi, Mahyar Janahmadi, Azadeh Elahi-Mahani, Farhad Salari, Mehdi Golpayegani, Habibeh Khoshbouei
Drugs of abuse cause persistent alterations in synaptic plasticity that is thought to underlie addictive-like behaviors. Although, the perisynaptic glial cells are implicated in metabolic maintenance and support of the nervous systems, accumulating evidence suggests that glial cells exert a modulatory action on synaptic functions and participate in synaptic plasticity. However, it is well-documented that glial cells are associated with the acquisition of rewarding effects of abused drugs. The role of hippocampal glial cells in addictive-like behaviors remains poorly understood...
April 4, 2018: Physiology & Behavior
https://www.readbyqxmd.com/read/29615865/the-regulatory-mechanisms-and-therapeutic-potential-of-micrornas-from-chronic-pain-to-morphine-tolerance
#16
REVIEW
Zhao Dai, Haichen Chu, Jiahai Ma, Ying Yan, Xueying Zhang, Yongxin Liang
Chronic pain, including cancer-related pain, is a pain condition often caused by inflammation or dysfunctional nerves. Chronic pain treatment poses a significant health care challenge, where opioids especially morphine are widely used and patients often develop tolerance over time with aggravated pain. microRNA (miRNA) is known to play important roles in regulating gene expressions in the nervous system to affect neuronal network plasticity related to algogenesis and the developing of morphine tolerance. In this article, we reviewed studies conducted in rodent animal models investigating the mechanisms of miRNAs regulation in chronic pain with different phenotypes and morphine tolerance...
2018: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/29609700/use-of-topical-morphine-to-relieve-painful-pressure-ulcers
#17
Sandra L Discala, Danny Basri, Christine M Vartan, Michael A Silverman
INTRODUCTION: Topical morphine is a potential treatment option for painful pressure ulcers in hospice and palliative care patients who favor avoidance of systemic opioid therapy. CASE: A 65-year-old male African-American veteran with a painful stage 3 sacral pressure injury was hesitant to take systemic opioids to control his pain, as he wished to stay alert for family and friends. Topical morphine was initiated, and within 24 hours the patient reported a significant reduction in pain on the numeric rating scale...
April 1, 2018: Consultant Pharmacist: the Journal of the American Society of Consultant Pharmacists
https://www.readbyqxmd.com/read/29589831/cellular-tolerance-at-the-%C3%A2%C2%B5-opioid-receptor-is-phosphorylation-dependent
#18
Seksiri Arttamangkul, Daniel A Heinz, James R Bunzow, Xianqiang Song, John T Williams
Phosphorylation of the μ-opioid receptor (MOR) is known as a key step in desensitization and internalization but the role in the development of long-term tolerance at the cellular level is not known. Viral expression of wild type (exWT) and mutant MORs, where all phosphorylation sites on the C-terminus (Total Phosphorylation Deficient (TPD)) were mutated to alanine, were examined in locus coeruleus neurons in a MOR knockout rat. Both receptors activated potassium conductance similar to endogenous receptors in wild type animals...
March 28, 2018: ELife
https://www.readbyqxmd.com/read/29587571/-express-clinical-opioids-differentially-induce-co-internalization-of-%C3%AE-and-%C3%AE-opioid-receptors
#19
Fenghua Bao, Chang-Lin Li, Xu-Qiao Chen, Ying-Jin Lu, Lan Bao, Xu Zhang
Opioid receptors play an important role in mediating the spinal analgesia. The μ-opioid receptor (MOR) is the major target of opioid drugs widely used in clinics. However, the regulatory mechanisms of analgesic effect and tolerance for clinical MOR-targeting opioids remain to be fully investigated. Previous studies showed the interaction of δ-opioid receptor (DOR) with MOR to form the MOR/DOR heteromers that could be processed in the degradation pathway after DOR agonist treatment. Here we showed that clinical MOR-targeting opioids, morphine, fentanyl and methadone, but not tramadol, caused MOR co-internalization with DORs in both transfected human embryonic kidney 293 cells and primary sensory neurons...
January 1, 2018: Molecular Pain
https://www.readbyqxmd.com/read/29582414/the-novel-%C3%AE-opioid-receptor-agonist-pzm21-depresses-respiration-and-induces-tolerance-to-antinociception
#20
Rob Hill, Alex Disney, Alex Conibear, Katy Sutcliffe, William Dewey, Stephen Husbands, Chris Bailey, Eamonn Kelly, Graeme Henderson
BACKGROUND AND PURPOSE: PZM21 is a novel μ-opioid receptor (MOPr) ligand that has been reported to induce minimal arrestin recruitment and be devoid of the respiratory depressant effects characteristic of classical μ-opioid ligands such as morphine. We have re-examined the signalling profile of PZM21 and its ability to depress respiration. EXPERIMENTAL APPROACH: G protein (Gi ) activation and arrestin-3 translocation were measured in vitro in MOPr expressing HEK 293 cells using BRET assays...
March 26, 2018: British Journal of Pharmacology
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