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https://www.readbyqxmd.com/read/29342106/adrenergic-agonists-bind-to-adrenergic-receptor-like-regions-of-the-mu-opioid-receptor-enhancing-morphine-and-methionine-enkephalin-binding-a-new-approach-to-biased-opioids
#1
Robert Root-Bernstein, Miah Turke, Udaya K Tiruttani Subhramanyam, Beth Churchill, Joerg Labahn
Extensive evidence demonstrates functional interactions between the adrenergic and opioid systems in a diversity of tissues and organs. While some effects are due to receptor and second messenger cross-talk, recent research has revealed an extracellular, allosteric opioid binding site on adrenergic receptors that enhances adrenergic activity and its duration. The present research addresses whether opioid receptors may have an equivalent extracellular, allosteric adrenergic binding site that has similar enhancing effects on opioid binding...
January 17, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29342085/development-of-a-region-specific-physiologically-based-pharmacokinetic-brain-model-to-assess-hippocampus-and-frontal-cortex-pharmacokinetics
#2
Zaril Zakaria, Raj Badhan
Central nervous system drug discovery and development is hindered by the impermeable nature of the blood-brain barrier. Pharmacokinetic modeling can provide a novel approach to estimate CNS drug exposure; however, existing models do not predict temporal drug concentrations in distinct brain regions. A rat CNS physiologically based pharmacokinetic (PBPK) model was developed, incorporating brain compartments for the frontal cortex (FC), hippocampus (HC), "rest-of-brain" (ROB), and cerebrospinal fluid (CSF). Model predictions of FC and HC Cmax, tmax and AUC were within 2-fold of that reported for carbamazepine and phenytoin...
January 17, 2018: Pharmaceutics
https://www.readbyqxmd.com/read/29338151/oral-prolonged-release-oxycodone-naloxone-offers-equivalent-analgesia-to-intravenous-morphine-patient-controlled-analgesia-after-total-knee-replacement-a-randomized-controlled-trial
#3
Alberto Manassero, Andrea Fanelli, Susanna Ugues, Cristian Bailo, Stefano Dalmasso
BACKGROUND: The purpose of this study was to determine whether oral prolonged- release oxycodone-naloxone combination (OXN) could provide equivalent analgesia and a side-effect profile similar to intravenous morphine patient-controlled analgesia (IVPCA) for the control of pain in the immediate postoperative period after total knee replacement (TKR). METHODS: All patients received a sciatic nerve block with 0.3% ropivacaine 15ml, femoral nerve block with 0.5% ropivacaine 20 ml, spinal anesthesia and postoperative continuous femoral nerve infusion (ropivacaine 0...
January 16, 2018: Minerva Anestesiologica
https://www.readbyqxmd.com/read/29335074/trends-in-narcotics-and-sedative-use-during-mechanical-ventilation-of-preterm-infants-in-canadian-neonatal-intensive-care-units
#4
(no author information available yet)
OBJECTIVE: Mechanical ventilation (MV) in preterm infants (PTI) causes discomfort. Whether it causes pain is controversial. Meta analysis reviews of published work on PTI during MV have shown no clinically significant impact of opioids on pain scales, and hence not recommended for routine use in neonatal intensive care units (NICUs). Similarly regular use of sedative midazolam is also not recommended. Therefore we hypothesized a downward trend in narcotics and sedatives used in MV of PTI in NICUs...
January 2018: Zhongguo Dang Dai Er Ke za Zhi, Chinese Journal of Contemporary Pediatrics
https://www.readbyqxmd.com/read/29334500/overexpression-of-%C3%A2%C2%B5-opioid-receptors-in-peripheral-afferents-but-not-in-combination-with-enkephalin-decreases-neuropathic-pain-behavior-and-enhances-opioid-analgesia-in-mouse
#5
Amanda H Klein, Husam K Mohammad, Rabiah Ali, Brad Peper, Steven P Wilson, Srinivasa N Raja, Matthias Ringkamp, Sarah Sweitzer
BACKGROUND: The current study used recombinant herpes simplex virus type I to increase expression of µ-opiate receptors and the opioid ligand preproenkephalin in peripheral nerve fibers in a mouse model of neuropathic pain. It was predicted that viral vector delivery of a combination of genes encoding the µ-opioid receptor and preproenkephalin would attenuate neuropathic pain and enhance opioid analgesia. The behavioral effects would be paralleled by changes in response properties of primary afferent neurons...
January 15, 2018: Anesthesiology
https://www.readbyqxmd.com/read/29333821/opioid-treatment-for-mixed-pain-in-pediatric-patients-assisted-by-the-palliative-care-team-five-years-of-experience
#6
María L Yazde Puleio, Karina V Gómez, Ana Majdalani, Vilma Pigliapoco, Gisella Santos Chocler
Pain is defined as an unpleasant sensory and emotional experience associated with actual or potential tissue damage. Depending on its pathophysiological mechanism, it may be classified into nociceptive, neuropathic, and mixed pain. If pain is moderate to severe, a strong opioid should be administered and, when this is the case, morphine is the drug of choice. If morphine is ineffective or causes intolerable adverse effects, opioid rotation is recommended. Our objective was to describe the drug management for mixed pain used in patients assisted by the Palliative Care team of Hospital General de Niños Pedro de Elizalde between August 2011 and September 2015...
February 1, 2018: Archivos Argentinos de Pediatría
https://www.readbyqxmd.com/read/29331953/efficacy-tolerability-and-acceptability-of-oxycodone-for-cancer-related-pain-in-adults-an-updated-cochrane-systematic-review
#7
REVIEW
Mia Schmidt-Hansen, Michael I Bennett, Stephanie Arnold, Nathan Bromham, Jennifer S Hilgart
OBJECTIVES: To assess the efficacy, tolerability and acceptability of oxycodone for cancer pain in adults METHODS: We searched CENTRAL, MEDLINE, MEDLINE In-Process, Embase, SCI, Conference Proceedings Citation Index-Science, BIOSIS, PsycINFO and four trials registries to November 2016. RESULTS: We included 23 randomised controlled trials with 2144 patients analysed for efficacy and 2363 for safety. Meta-analyses showed no significant differences between controlled-release (CR) and immediate-release oxycodone in pain intensity or adverse events but did show significantly better pain relief after treatment with CR morphine compared with CR oxycodone...
January 13, 2018: BMJ Supportive & Palliative Care
https://www.readbyqxmd.com/read/29330245/impact-of-pharmacist-previsit-input-to-providers-on-chronic-opioid-prescribing-safety
#8
Nicholas Cox, Casey R Tak, Susan E Cochella, Eric Leishman, Karen Gunning
INTRODUCTION: Primary care providers (PCPs) account for half of opioid prescriptions, often feel chronic pain patients are challenging to manage, and there is wide variability in practice patterns. The purpose of this pilot study was to evaluate the impact of a previsit pharmacist review of high-risk patients treated with opioids for chronic pain on compliance to guideline recommendations at a family medicine residency clinic. METHODS: All adult patients with an appointment for chronic pain who were prescribed >50 morphine milligram equivalents (MMEs)/day had charts reviewed by a pharmacist before each appointment; recommendations were sent electronically to the provider before the appointment...
January 2018: Journal of the American Board of Family Medicine: JABFM
https://www.readbyqxmd.com/read/29330240/structured-management-of-chronic-nonmalignant-pain-with-opioids-in-a-rural-primary-care-office
#9
Kevin S McCann, Shawndra Barker, Raymond Cousins, Adam Franks, Clinton McDaniel, Stephen Petrany, Eric Riley
INTRODUCTION: The use of opioid medication for nonmalignant chronic pain (NMCP) increased dramatically during the last 20 years. There have been regulatory changes implemented to reduce the risk of harm to both patients and society. Much of the burden of monitoring these patients is falling on primary care physicians (PCPs), who do not have the time or resources to handle what is entailed in a best-practice approach to NMCP. METHODS: A retrospective study was conducted with all patients on opioid medication for NMCP who were enrolled onto an individual PCP's practice...
January 2018: Journal of the American Board of Family Medicine: JABFM
https://www.readbyqxmd.com/read/29330156/application-of-receptor-theory-to-the-design-and-use-of-fixed-proportion-mu-opioid-agonist-and-antagonist-mixtures-in-rhesus-monkeys
#10
Jeremy C Cornelissen, Samuel Obeng, Kenner C Rice, Yan Zhang, S Stevens Negus, Matthew Banks
Receptor theory predicts that fixed-proportion mixtures of a competitive, reversible agonist (e.g. fentanyl) and antagonist (e.g. naltrexone) at a common receptor (e.g. mu opioid receptors; MOR) will result in antagonist proportion-dependent decreases in apparent efficacy of the mixtures and downward shifts in mixture dose-effect functions. The present study tested this hypothesis by evaluating behavioral effects of fixed-proportion fentanyl/naltrexone mixtures in a warm-water tail-withdrawal procedure in rhesus monkeys (n=4)...
January 12, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29330135/apbb2-is-associated-with-amphetamine-use-and-plasma-beta-amyloids-in-patients-receiving-methadone-maintenance-treatment
#11
Chia-Chen Liu, Chiu-Ping Fang, Tung-Hsia Liu, Hsiang-Wei Kuo, Shu Chi Liu, Sheng-Chang Wang, Andrew C H Chen, Yu-Li Liu
APBB2, amyloid beta (A4) precursor protein-binding family B member 2, has been reported to be associated with opioid dependence. In this study, we reported the first time that the genetic variants in the APBB2 gene were associated with use of amphetamine in opioid dependent patients undergoing methadone maintenance treatment (MMT). 344 heroin-dependent patients undergoing MMT were recruited and assessed for use of amphetamine and opioids by urine toxicology, withdrawal severity, and side effects. DNAs were genome-widely genotyped for all patients...
January 9, 2018: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29329388/a-series-of-deaths-involving-carfentanil-in-the-uk-and-associated-post-mortem-blood-concentrations
#12
Simon P Elliott, Elena Hernandez Lopez
The potent opioid and veterinary drug, carfentanil has recently entered the illicit drug market, especially in relation to heroin and cocaine. Recent publications have reported carfentanil concentrations found in fatalities occurring in the USA. This article presents the toxicological findings in seven heroin/cocaine cases occurring in the UK within a short period of time where carfentanil was detected and measured. Carfentanil was detected along with other drugs in all cases with no alcohol detected in the post-mortem blood in any of the cases...
January 10, 2018: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29327156/effectiveness-of-celecoxib-for-pain-relief-and-antipyresis-in-second-trimester-medical-abortions-with-misoprostol-a-randomized-controlled-trial
#13
Hatern Tintara, Peangpailin Voradithi, Thanapan Choobun
PURPOSE: To evaluate the effectiveness of celecoxib for pain relief and antipyresis during second trimester abortion using sublingual misoprostol. METHODS: Fifty-six pregnant women of gestational age 14-24 weeks were randomly assigned in a double-blind randomized controlled trial to receive 400 mg of celecoxib or placebo just before sublingual administration of misoprostol 400 µg every 6 h. Pain and body temperature (BT) were assessed every 1 h until the abortion or 24 h after the first dose of misoprostol...
January 11, 2018: Archives of Gynecology and Obstetrics
https://www.readbyqxmd.com/read/29322265/the-role-of-sphingolipids-in-psychoactive-drug-use-and-addiction
#14
REVIEW
Liubov S Kalinichenko, Erich Gulbins, Johannes Kornhuber, Christian P Müller
Psychoactive drug use is a common behavior in many societies worldwide, frequently associated with drug instrumentalization. Regular use may develop into drug addiction, which is a severe psychiatric disorder with multiple pathological effects to virtually all organ systems. Treatment strategies for addiction are often insufficient with no broadly working pharmaco-treatment available. Recently, lipids, and particularly sphingolipids, have been considered as new mediators in the pathogenic pathways and as possible therapeutic targets for the treatment of addictive states...
January 10, 2018: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29322074/data-supporting-the-understanding-of-modulatory-function-of-opioid-analgesics-in-mouse-macrophage-activity
#15
Iwona Filipczak-Bryniarska, Katarzyna Nazimek, Bernadeta Nowak, Michael Kozlowski, Magdalena Wąsik, Krzysztof Bryniarski
The data presented herein expand the current understanding of the modulatory function of opioid drugs in mouse macrophage activity described in our relevant research article (Filipczak-Bryniarska et al., 2017) [1], in which we characterize the influence of morphine, buprenorphine and oxycodone on humoral and cell-mediated immune response in mice. Among other things, we have shown the effects of treatment with assayed analgesics on macrophage ability to induce antigen-specific B-cell response to sheep red blood cells as well as to generate reactive oxygen intermediates and nitric oxide...
February 2018: Data in Brief
https://www.readbyqxmd.com/read/29319627/opioid-prescription-morbidity-and-mortality-in-us-transplant-recipients
#16
Kevin C Abbott, Chyng-Wen Fwu, Paul W Eggers, Anne W Eggers, Prudence P Kline, Paul L Kimmel
BACKGROUND: CDC guidelines recommend caution in prescribing opioids for chronic pain. The characteristics of opioid prescription (OpRx) among kidney transplant (KTx) recipients has not been described in a national population. METHODS: We assessed OpRx prevalence among prevalent KTx recipients, and associated duration (chronic, defined as ≥90 days in a year) and dosing (in morphine milligram equivalents per day, MME, of <50, 50-89, and ≥90) with outcomes, death and graft loss, among incident KTx recipients using 2006-2010 US Renal Data System files, including Medicare Part D for medication ascertainment...
January 10, 2018: Transplantation
https://www.readbyqxmd.com/read/29318747/the-caudal-part-of-the-posterior-insula-of-rats-participates-in-the-maintenance-but-not-the-acquisition-of-morphine-conditioned-place-preference
#17
Yong-Mei Sun, Rong-Xiang Chen, Zhi-Fei Li, Sabine Spijker, Rong-Wei Zhai, Shang-Chuan Yang
The heterogeneous insular cortex plays an interoceptive role in drug addiction by signaling the availability of drugs of abuse. Here, we tested whether the caudal part of the multisensory posterior insula (PI) stores somatosensory-associated rewarding memories. Using Sprague Dawley rats as subjects, we first established a morphine-induced conditioned place preference (CPP) paradigm, mainly based on somatic cues. Secondly, an electrolytic lesion of the caudal portion of the PI was carried out before and after the establishment of CPP, respectively...
January 9, 2018: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/29317354/laccase-catalyzed-elimination-of-morphine-from-aqueous-systems
#18
Daniela Huber, Klaus Bleymaier, Alessandro Pellis, Robert Vielnascher, Andreas Daxbacher, Katrin J Greimel, Georg M Guebitz
Pharmaceuticals contaminate the environment for several reasons, including metabolic excretion after intake, industrial waste and improper disposal. The narcotic drug morphine is commonly utilized for chronic pain management, and the distribution of morphine in aqueous systems and in waste waters is of high concern. Here. the removal of morphine by a laccase from Myceliophthora thermophila both in its free form as well as immobilized on Accurel MP1000 beads was investigated. Complete morphine elimination was achieved within 30 min for the free and the immobilized enzyme (70% bound protein) for concentrations between 1 and 1,000 mg L-1 according to LC-TOF mass spectrometry analysis...
January 6, 2018: New Biotechnology
https://www.readbyqxmd.com/read/29316911/the-standardized-withania-somnifera-dunal-root-extract-alters-basal-and-morphine-induced-opioid-receptor-gene-expression-changes-in-neuroblastoma-cells
#19
Francesca Felicia Caputi, Elio Acquas, Sanjay Kasture, Stefania Ruiu, Sanzio Candeletti, Patrizia Romualdi
BACKGROUND: Behavioral studies demonstrated that the administration of Withania somnifera Dunal roots extract (WSE), prolongs morphine-elicited analgesia and reduces the development of tolerance to the morphine's analgesic effect; however, little is known about the underpinning molecular mechanism(s). In order to shed light on this issue in the present paper we explored whether WSE promotes alterations of μ (MOP) and nociceptin (NOP) opioid receptors gene expression in neuroblastoma SH-SY5Y cells...
January 10, 2018: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/29316592/the-addition-of-diclofenac-to-a-multimodal-pain-control-regimen-decreases-postoperative-pain-and-opioid-consumption
#20
Nicole E George, Cheryle Gurk-Turner, Jennifer I Etcheson, Chukwuweike U Gwam, Randal De Souza, Spencer S Smith, James Nace, Ronald E Delanois
INTRODUCTION: Total knee arthroplasty (TKA) is a commonly-performed orthopaedic procedure in the United States. However, inadequate postoperative pain management following TKA has been associated with a number of negative consequences, including chronic postoperative pain requiring long-term opioid use. Multimodal pain control is a recently-popularized means of maximizing analgesia and postoperative outcomes. We aimed to evaluate the outcomes of a multimodal pain regimen incorporating diclofenac, including: 1) length of stay (LOS); 2) pain intensity; and 3) opioid consumption in primary TKA patients...
December 22, 2017: Surgical Technology International
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