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morphine tolerance

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https://www.readbyqxmd.com/read/28626808/attenuation-of-opioid-tolerance-by-etb-receptor-agonist-irl-1620-is-independent-of-an-accompanied-decrease-in-nerve-growth-factor-in-mice
#1
Shruti Gulati, Seema Briyal, Shantel Jones, Shaifali Bhalla, Anil Gulati
AIM: ETA receptor antagonists reverse opioid tolerance but the involvement of ETB receptors is unknown. In morphine or oxycodone tolerant mice we investigated (1) the effect of ETB receptor agonist, IRL-1620, on analgesic tolerance; (2) changes in expression of the brain ETA and ETB receptors; and (3) alterations in the brain VEGF, NGF, PI3K and notch-1 expression. MAIN METHODS: Body weight, body temperature, and tail-flick latency were assessed before and after a challenge dose of morphine or oxycodone in vehicle or IRL-1620 treated mice...
June 2017: Heliyon
https://www.readbyqxmd.com/read/28603428/upregulation-of-mir-375-level-ameliorates-morphine-analgesic-tolerance-in-mouse-dorsal-root-ganglia-by-inhibiting-the-jak2-stat3-pathway
#2
Haiqin Li, Rong Tao, Jing Wang, Lingjie Xia
Several lines of evidence indicate that microRNAs (miRNAs) modulate tolerance to the analgesic effects of morphine via regulation of pain-related genes, making dysregulation of miRNA levels a clinical target for controlling opioid tolerance. However, the precise mechanisms by which miRNAs regulate opioid tolerance are unclear. In the present study, we noted that the miR-375 level was downregulated but the expression of Janus kinase 2 (JAK2) was upregulated in mouse dorsal root ganglia (DRG) following chronic morphine treatment...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28580822/effects-of-microrna-223-on-morphine-analgesic-tolerance-by-targeting-nlrp3-in-a-rat-model-of-neuropathic-pain
#3
Xiao-Juan Xie, Li-Gang Ma, Kai Xi, Dong-Mei Fan, Jian-Guo Li, Quan Zhang, Wei Zhang
Objective To investigate the effects of microRNA-223 on morphine analgesic tolerance by targeting NLRP3 in a rat model of neuropathic pain. Methods Our study selected 100 clean grade healthy Sprague-Dawley adult male rats weighing 200 to 250 g. After establishment of a rat model of chronic constriction injury, these rats were divided into 10 groups (10 rats in each group): the normal control, sham operation, chronic constriction injury, normal saline, morphine, miR-223, NLRP3, miR-223 + morphine, NLRP3 + morphine, and miR-223 + NLRP3 + morphine groups...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28576452/naldemedine-versus-placebo-for-opioid-induced-constipation-compose-1-and-compose-2-two-multicentre-phase-3-double-blind-randomised-parallel-group-trials
#4
Martin Hale, James Wild, Jyotsna Reddy, Tadaaki Yamada, Juan Camilo Arjona Ferreira
BACKGROUND: Opioid-induced constipation is a frequent side-effect of opioid treatment, and standard interventions have limited or inconsistent efficacy. This study assessed the efficacy and safety of naldemedine, a peripherally acting μ-opioid receptor antagonist, for the treatment of opioid-induced constipation in patients with chronic non-cancer pain. METHODS: We report two double-blind, randomised, placebo-controlled trials in adults with chronic non-cancer pain and opioid-induced constipation...
May 30, 2017: Lancet. Gastroenterology & Hepatology
https://www.readbyqxmd.com/read/28552056/the-orexinergic-hypocretin-system-and-nociception-an-update-to-supraspinal-mechanisms
#5
Ali Roohbakhsh, Mohaddeseh Sadat Alavi, Hassan Azhdari Zarmehri
Chronic pain is a multifaceted and complex condition that is divided into somatic, visceral, and neuropathic pain. Although opioids and nonsteroidal anti-inflammatory drugs cause analgesia and are effective in the treatment of chronic pain, their utility is hampered by side effects, abuse potential, and development of tolerance to their pain-relieving effects. So, finding alternative analgesics with good efficacy and low side effects is of great interest and the orexinergic system is a potential candidate. Orexin-A and -B are exclusively expressed in the lateral hypothalamus and are involved in the feeding, sleep/wake cycle, cardiovascular function, hormone secretion, seizure, and pain modulation...
May 28, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28551416/validation-of-a-thermal-threshold-nociceptive-model-in-bearded-dragons-pogona-vitticeps
#6
Émilie L Couture, Beatriz P Monteiro, Jessica Aymen, Eric Troncy, Paulo V Steagall
OBJECTIVES: To validate a thermal threshold (TT) nociceptive model in bearded dragons (Pogona vitticeps) and to document TT changes after administration of morphine. STUDY DESIGN: A two-part randomized, blinded, controlled, experimental study. ANIMALS: Five adult bearded dragons (242-396 g). METHODS: A TT device delivered a ramped nociceptive stimulus (0.6 °C second(-1)) to the medial thigh until a response (leg kick/escape behavior) was observed or maximum (cut-off) temperature of 62 °C was reached...
January 11, 2017: Veterinary Anaesthesia and Analgesia
https://www.readbyqxmd.com/read/28538525/trajectory-of-postoperative-wound-pain-within-the-first-2-weeks-following-posterior-spinal-fusion-surgery-in-adolescent-idiopathic-scoliosis-patients
#7
Mun Keong Kwan, Chee Kidd Chiu, Teik Seng Chan, Kok Ian Chong, Siti Mariam Mohamad, Mohd Shahnaz Hasan, Chris Yin Wei Chan
STUDY DESIGN: A prospective cohort study. OBJECTIVE: The aim of this study was to determine and evaluate the trajectory of surgical wound pain from day 1 to day 14 after posterior spinal fusion (PSF) surgery in patients with adolescent idiopathic scoliosis (AIS). SUMMARY OF BACKGROUND DATA: Information regarding how the postoperative pain improves with time offers invaluable information not only to the patients and parents but also to assist the clinician in managing postoperative pain...
June 1, 2017: Spine
https://www.readbyqxmd.com/read/28535569/reinstituting-the-bolus-new-reasoning-for-an-existing-technique
#8
Porter W McRoberts, Jason E Pope, Catalina Apostol
Improved intrathecal (IT) pump technology is increasing the accuracy of IT opioid bolus dosing and promising advances in pain therapy. Opioid bolus dosing can be used with a minimal continuous infusion or it can function as the sole therapy. Bolus-only dosing is characterized by minimal use of opioid (often less than 1 mg of IT morphine). It achieves adequate pain control while reducing tolerance and possibly opioid-induced hyperalgesia. It may prevent receptor saturation, and provide a "washing out" of the opioid receptor that prevents the observed dose escalation resulting from continuous infusions...
May 2017: Pain Physician
https://www.readbyqxmd.com/read/28533287/trv0109101-a-g-protein-biased-agonist-of-the-%C3%A2%C2%B5-opioid-receptor-does-not-promote-opioid-induced-mechanical-allodynia-following-chronic-administration
#9
Michael Koblish, Richard Carr, Edward R Siuda, David H Rominger, William Gowen-MacDonald, Conrad L Cowan, Aimee L Crombie, Jonathan D Violin, Michael W Lark
Prescription opioids are a mainstay in the treatment of acute moderate to severe pain. However, chronic use leads to a host of adverse consequences including tolerance and opioid-induced hyperalgesia (OIH), leading to more complex treatment regimens and diminished patient compliance. Patients experiencing OIH paradoxically experience exaggerated nociceptive responses instead of pain reduction after chronic opioid usage. The development of OIH and tolerance tend to occur simultaneously and, thus, present a challenge when studying the molecular mechanisms driving each phenomenon...
May 22, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28530786/morphine-for-chronic-neuropathic-pain-in-adults
#10
REVIEW
Tess E Cooper, Junqiao Chen, Philip J Wiffen, Sheena Derry, Daniel B Carr, Dominic Aldington, Peter Cole, R Andrew Moore
BACKGROUND: Neuropathic pain, which is caused by a lesion or disease affecting the somatosensory system, may be central or peripheral in origin. Neuropathic pain often includes symptoms such as burning or shooting sensations, abnormal sensitivity to normally painless stimuli, or an increased sensitivity to normally painful stimuli. Neuropathic pain is a common symptom in many diseases of the nervous system. Opioid drugs, including morphine, are commonly used to treat neuropathic pain...
May 22, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28507784/geraniin-attenuates-naloxone-precipitated-morphine-withdrawal-and-morphine-induced-tolerance-in-mice
#11
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
#12
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
#13
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
#14
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
#15
Catarina Chaves, Fernando Remião, Salvatore Cisternino, 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
#16
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
#17
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
#18
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
#19
Joanna C Jacob, Justin L Poklis, Hamid I Akbarali, Graeme Henderson, William L Dewey
This study compared the development of tolerance to two orally bioavailable prescription opioids, oxycodone and hydrocodone, to that of morphine, and the reversal of this tolerance by ethanol. 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...
July 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
#20
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
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