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Opioid tolerance

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https://www.readbyqxmd.com/read/29769132/toots-tastes-and-tester-shots-user-accounts-of-drug-sampling-methods-for-gauging-heroin-potency
#1
Sarah G Mars, Jeff Ondocsin, Daniel Ciccarone
BACKGROUND: Internationally, overdose is the primary cause of death among people injecting drugs. However, since 2001, heroin-related overdose deaths in the United States (US) have risen sixfold, paralleled by a rise in the death rate attributed to synthetic opioids, particularly the fentanyls. This paper considers the adaptations some US heroin injectors are making to protect themselves from these risks. METHODS: Between 2015 and 2016, a team of ethnographers collected data through semi-structured interviews and observation captured in field notes and video recording of heroin preparation/consumption...
May 16, 2018: Harm Reduction Journal
https://www.readbyqxmd.com/read/29768254/neuroprotection-against-hypoxic-ischemic-injury-%C3%AE-opioid-receptors-and-bdnf-trkb-pathway
#2
Shiying Sheng, Jingzhong Huang, Yi Ren, Feng Zhi, Xuansong Tian, Guoqiang Wen, Guanghong Ding, Terry C Xia, Fei Hua, Ying Xia
The delta-opioid receptor (DOR) is one of three classic opioid receptors in the opioid system. It was traditionally thought to be primarily involved in modulating the transmission of messages along pain signaling pathway. Although there were scattered studies on its other neural functions, inconsistent results and contradicting conclusions were found in past literatures, especially in terms of DOR's role in a hypoxic/ischemic brain. Taking inspiration from the finding that the turtle brain exhibits a higher DOR density and greater tolerance to hypoxic/ischemic insult than the mammalian brain, we clarified DOR's specific role in the brain against hypoxic/ischemic injury and reconciled previous controversies in this aspect...
May 11, 2018: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29764265/use-of-methadone-to-reverse-opioid-escalation-in-a-patient-with-surgical-pain
#3
Muhammad Jaffar, Gwin Cunningham, Michael Chandler, Thomas Webb
Acute pain is a prevalent issue for patients recovering from surgical procedures. Methadone has been recognized as a unique option for treatment of surgical pain due to its multiple mechanisms of analgesia and its potential to decrease tolerance to other opioids. Studies of methadone use in postoperative settings are sparse in part due to safety concerns, such as complex pharmacokinetics, risk of respiratory depression, and association with arrhythmias. In this case study of a 70-year-old male with postsurgical abdominal pain, methadone utilization over a period of 9 days resulted in patient-reported analgesia and aided in de-escalating overall opioid use...
May 15, 2018: Journal of Pain & Palliative Care Pharmacotherapy
https://www.readbyqxmd.com/read/29762332/extended-release-liposomal-bupivacaine-injection-exparel-for-early-postoperative-pain-control-following-palatoplasty
#4
Kristopher M Day, Narayanan M Nair, Larry A Sargent
INTRODUCTION: Liposomal bupivacaine (LB) is a long-acting local anesthetic reported to decrease postoperative pain in adults. The authors demonstrate the safe use of LB in pediatric patients with improved pain control following palatoplasty. MATERIALS AND METHODS: Retrospective patient series of all single-surgeon palatoplasty patients treated at a tertiary craniofacial center from August 2014 to December 2015 were included. All patients received 1.3% LB intraoperatively as greater palatal nerve and surgical field blocks in 2-flap V-Y pushback palatoplasty...
May 14, 2018: Journal of Craniofacial Surgery
https://www.readbyqxmd.com/read/29761672/emergency-department-administration-of-oxycodone-by-nurses-treating-musculoskeletal-pain-an-observational-prospective
#5
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
#6
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
#7
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
#8
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/29739537/opioid-free-anesthesia-opioid-side-effects-tolerance-and-hyperalgesia
#9
REVIEW
Patricia Lavand'homme, Arnaud Steyaert
Opioids are the most potent drugs used to control severe pain. However, neuroadaptation prevents opioids' ability to provide long-term analgesia and produces opposite effects, i.e., enhancement of existent pain and facilitation of chronic pain development. Neuroadaptation to opioids use results in the development of two interrelated phenomena: tolerance and "opioid-induced hyperalgesia" (OIH). Tolerance, a pharmacologic concept, and OIH, a clinical syndrome, have been mostly observed under experimental conditions in animals and in human volunteers...
December 2017: Best Practice & Research. Clinical Anaesthesiology
https://www.readbyqxmd.com/read/29738425/a-pilot-open-label-8-week-study-evaluating-desvenlafaxine-for-treatment-of-major-depression-in-methadone-maintained-individuals-with-opioid-use-disorder
#10
Cynthia El Hage, Maykel F Ghabrash, Simon Dubreucq, Suzanne Brissette, François Lespérance, Paul Lespérance, Clairélaine Ouellet-Plamondon, Julie Bruneau, Didier Jutras-Aswad
Depression is one of the most prevalent psychiatric disorders among opioid-dependent individuals. Clinical trials testing selective serotonin reuptake inhibitors among depressed patients on methadone maintenance therapy (MMT) failed to show efficacy, whereas those on tricyclic antidepressants produced mixed results with potential for cardiotoxicity. Desvenlafaxine (DESV) is a SNRI with minimal cardiotoxicity and drug interactions. This study sought to assess feasibility and tolerability of using DESV in depressed patients on MMT...
May 7, 2018: International Clinical Psychopharmacology
https://www.readbyqxmd.com/read/29737176/synthesis-and-structural-elucidation-of-a-pyranomorphinan-opioid-and-in-vitro-studies
#11
Mohd Imran Ansari, Jason R Healy, Kellie Hom, Jeffrey R Deschamps, Rae R Matsumoto, Andrew Coop
During optimization of the synthesis of the mixed μ opioid agonist/δ opioid antagonist 5-(hydroxymethyl)oxymorphone (UMB425) for scale-up, it was unexpectedly discovered that the 4,5-epoxy bridge underwent rearrangement on treatment with boron tribromide (BBr3 ) to yield a novel opioid with a little-studied pyranomorphinan skeleton. This finding opens the pyranomorphinans for further investigations of their pharmacological profiles and represents a novel drug class with the dual profile (μ vs δ) predicted to yield lower tolerance and dependence...
May 8, 2018: Organic Letters
https://www.readbyqxmd.com/read/29729777/methadone-maximizing-safety-and-efficacy-for-pain-control-in-patients-with-cancer
#12
REVIEW
Mary Lynn McPherson, Ryan C Costantino, Alexandra L McPherson
Methadone is a valuable opioid in the management of patients who have cancer with pain. Methadone is a mu-, kappa-, and delta-opioid agonist, and an N-methyl-D-aspartate receptor antagonist. These mechanisms of action make methadone an attractive option for complex pain syndromes. It is critically important that providers consider a patient's risk status before beginning methadone. Careful consideration must be given to dosing methadone in both opioid-naïve and opioid-tolerant patients, with vigilant monitoring for therapeutic effectiveness and potential toxicity until the patient achieves steady state...
June 2018: Hematology/oncology Clinics of North America
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
#13
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/29727163/aminoguanidine-hydrazone-derivatives-as-non-peptide-npff1-receptor-antagonists-reverse-opioid-induced-hyperalgesia
#14
Hassan Hammoud, Khadija Elhabazi, Raphaëlle Quillet, Isabelle Bertin, Valérie Utard, Emilie Laboureyras, Jean-Jacques Bourguignon, Frederic Bihel, Guy Simonnet, Frederic Simonin, Martine Schmitt
Neuropeptide FF receptors (NPFF1R and NPFF2R) and their endogenous ligand Neuropeptide FF have been shown previously to display anti-opioid properties and to play a critical role in the adverse effects associated with chronic administrations of opiates including the development of opioid-induced hyperalgesia and analgesic tolerance. In this work, we sought to identify novel NPFF receptors ligands by focusing our interest on a series of heterocycles as rigidified non-peptide NPFF receptor ligands, starting from already described aminoguanidine hydrazones (AGH's)...
May 4, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29726847/opioid-induced-hyperalgesia-in-the-nonsurgical-setting-a-systematic-review
#15
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/29722902/tolerance-to-high-internalizing-delta-opioid-receptor-agonist-is-critically-mediated-by-arrestin-2
#16
Ana Vicente-Sanchez, Isaac J Dripps, Alycia F Tipton, Heba Akbari, Areeb Akbari, Emily M Jutkiewicz, Amynah A Pradhan
BACKGROUND AND PURPOSE: Delta opioid receptor (δOR) agonists are potent antihyperalgesics in chronic pain models, but tolerance develops after prolonged use. Previous evidence indicates that distinct forms of tolerance occur depending on the internalization properties of δOR agonists. Due to the importance of arrestins in receptor internalization, we investigated the role of arrestin 2 (β-arrestin 1) in mediating the development of tolerance induced by high- and low-internalizing δOR agonists...
May 3, 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29715354/effect-of-atropine-with-propofol-vs-atropine-with-atracurium-and-sufentanil-on-oxygen-desaturation-in-neonates-requiring-nonemergency-intubation-a-randomized-clinical-trial
#17
Xavier Durrmeyer, Sophie Breinig, Olivier Claris, Pierre Tourneux, Cénéric Alexandre, Elie Saliba, Alain Beuchée, Camille Jung, Corinne Levy, Laetitia Marchand-Martin, Marie-Odile Marcoux, Agnes Dechartres, Claude Danan
Importance: Propofol or a combination of a synthetic opioid and muscle relaxant are both recommended for premedication before neonatal intubation but have yet to be compared. Objective: To compare prolonged desaturation during neonatal nasotracheal intubation after premedication with atropine-propofol vs atropine-atracurium-sufentanil treatment. Design, Setting, and Participants: Multicenter, double-blind, randomized clinical trial (2012-2016) in 6 NICUs in France that included 173 neonates requiring nonemergency intubation...
May 1, 2018: JAMA: the Journal of the American Medical Association
https://www.readbyqxmd.com/read/29713452/challenges-of-the-pharmacological-management-of-benzodiazepine-withdrawal-dependence-and-discontinuation
#18
REVIEW
Dimy Fluyau, Neelambika Revadigar, Brittany E Manobianco
Background: Benzodiazepines (BZDs) are among the most prescribed sedative hypnotics and among the most misused and abused medications by patients, in parallel with opioids. It is estimated that more than 100 million Benzodiazepine (BZD) prescriptions were written in the United States in 2009. While medically useful, BZDs are potentially dangerous. The co-occurring abuse of opioids and BZD, as well as increases in BZD abuse, tolerance, dependence, and short- and long-term side effects, have prompted a worldwide discussion about the challenging aspects of medically managing the discontinuation of BZDs...
May 2018: Therapeutic Advances in Psychopharmacology
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
#19
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
#20
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
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