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Opioid tolerance

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https://www.readbyqxmd.com/read/27926949/efficacy-and-tolerability-of-co-administering-full-%C3%A2%C2%B5-opioid-receptor-agonists-with-buprenorphine-and-mixed-opioid-agonists
#1
X Ruan, J Luo, A Kaye
No abstract text is available yet for this article.
December 7, 2016: Drug Research
https://www.readbyqxmd.com/read/27923161/antinociceptive-tolerance-to-nsaids-in-the-rat-formalin-test-is-mediated-by-the-opioid-mechanism
#2
Nana Tsiklauri, Ivliane Nozadze, Gulnaz Gurtskaia, Merab G Tsagareli
BACKGROUND: In the past decade it has been shown that tolerance develops to the antinociceptive effect of repeated systemic administration of commonly used non-steroidal anti-inflammatory drugs (NSAIDs) in acute pain models using rats. This is similar to the tolerance observed with opioid-induced analgesia. In the present study, we investigated the development of tolerance to the analgesic effects of NSAIDs diclofenac, ketorolac and xefocam in a chronic inflammatory pain model, the formalin test...
October 6, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27922029/safety-of-eluxadoline-in-patients-with-irritable-bowel-syndrome-with-diarrhea
#3
Brooks D Cash, Brian E Lacy, Philip S Schoenfeld, Leonard S Dove, Paul S Covington
OBJECTIVES: Eluxadoline is a mixed μ-opioid receptor (OR) and κ-OR agonist and δ-OR antagonist, approved for the treatment of irritable bowel syndrome with diarrhea (IBS-D). This analysis evaluated the safety and tolerability of eluxadoline 75 and 100 mg twice daily (BID) in one Phase 2 (IBS-2001) and two Phase 3 (IBS-3001 and IBS-3002) studies. METHODS: Adults with IBS-D (Rome III criteria) were randomized to placebo or eluxadoline (75 or 100 mg) BID for 12 (IBS-2001), 26 (IBS-3002), or 52 (IBS-3001) weeks...
December 6, 2016: American Journal of Gastroenterology
https://www.readbyqxmd.com/read/27921252/opioid-induced-bowel-dysfunction-in-patients-undergoing-spine-surgery-comparison-of-oxycodone-and-oxycodone-naloxone-treatment
#4
Merja Kokki, Moona Kuronen, Toivo Naaranlahti, Timo Nyyssönen, Ira Pikkarainen, Sakari Savolainen, Hannu Kokki
INTRODUCTION: Opioids are needed for postoperative pain in spine surgery patients, but opioid-induced constipation is a harmful adverse event. The aim of this clinical trial was to compare the use of a controlled-release oxycodone-naloxone combination product with oxycodone controlled-release tablets in these patients. The main outcome measure was the prevalence of constipation at 7 days postoperatively assessed with a Bowel Function Index questionnaire. A follow-up assessment at 21 days after surgery was also included...
December 5, 2016: Advances in Therapy
https://www.readbyqxmd.com/read/27918873/loperamide-the-poor-man-s-methadone-brief-review
#5
Cornel N Stanciu, Samantha A Gnanasegaram
Loperamide is widely available as an inexpensive, over-the-counter remedy commonly used for management of diarrhea. Although an opioid, at therapeutic doses it acts primarily on the gastrointestinal tissues; however, larger than recommended amounts facilitate central nervous system (CNS) penetration. Such high doses of loperamide have recently gained popularity among users of opioids to manage withdrawal symptomatology and, less frequently, to achieve psychoactive effects. Chronic loperamide use can result in development of tolerance and, upon abrupt cessation of use, withdrawal...
December 5, 2016: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/27905916/study-protocol-a-dose-escalating-phase-2-study-of-oral-lisdexamfetamine-in-adults-with-methamphetamine-dependence
#6
Nadine Ezard, Adrian Dunlop, Brendan Clifford, Raimondo Bruno, Andrew Carr, Alexandra Bissaker, Nicholas Lintzeris
BACKGROUND: The treatment of methamphetamine dependence is a continuing global health problem. Agonist type pharmacotherapies have been used successfully to treat opioid and nicotine dependence and are being studied for the treatment of methamphetamine dependence. One potential candidate is lisdexamfetamine, a pro-drug for dexamphetamine, which has a longer lasting therapeutic action with a lowered abuse potential. The purpose of this study is to determine the safety of lisdexamfetamine in this population at doses higher than those currently approved for attention deficit hyperactivity disorder or binge eating disorder...
December 1, 2016: BMC Psychiatry
https://www.readbyqxmd.com/read/27900781/the-present-and-future-of-opioid-analgesics-in-small-animal-practice
#7
REVIEW
B T Simon, P V Steagall
Opioids are the cornerstone for the treatment of acute pain in small animal patients. This is primarily because of their remarkable safety profile, high efficacy, and benefit of reversibility. There have been some significant advances in our knowledge on opioid pharmacology and clinical usage in companion animal medicine. This review discusses the progression of opioid use in small animal practice providing current misconceptions and controversies in light of routes of administration. Potential targets for research and drug development and novel therapies are discussed in addition to the concepts of glial cell modulators, individual variability, and opioid tolerance and hyperalgesia...
November 30, 2016: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27900763/parecoxib-propacetamol-and-their-combination-for-analgesia-after-total-hip-arthroplasty-a-randomized-non-inferiority-trial
#8
F Camu, A Borgeat, R J Heylen, E J Viel, M E Boye, R Y Cheung
BACKGROUND: This study assessed non-inferiority of parecoxib vs. combination parecoxib+propacetamol and compared the opioid-sparing effects of parecoxib, propacetamol, and parecoxib+propacetamol vs. placebo after total hip arthroplasty. METHODS: In this randomized, placebo-controlled, parallel-group, non-inferiority study, patients received one of four IV treatments after surgery: parecoxib 40 mg bid (n = 72); propacetamol 2 g qid (n = 71); parecoxib 40 mg bid plus propacetamol 2 g qid (n = 72); or placebo (n = 38) with supplemental IV patient-controlled analgesia (morphine)...
January 2017: Acta Anaesthesiologica Scandinavica
https://www.readbyqxmd.com/read/27899254/thalidomide-attenuates-the-development-and-expression-of-antinociceptive-tolerance-to-%C3%AE-opioid-agonist-morphine-through-l-arginine-inos-and-nitric-oxide-pathway
#9
Muhammad Imran Khan, Sattar Ostadhadi, Faiza Mumtaz, Majid Momeny, Farima Moghaddaskho, Mahsa Hassanipour, Shahram Ejtemaei-Mehr, Ahmad Reza Dehpour
Morphine is a μ-opioid analgesic drug which is used in the treatment and management of chronic pain. However, due to development of antinociceptive tolerance its clinical use is limited. Thalidomide is an old glutamic acid derivative which recently reemerged because of its potential to counteract a number of disorders including neurodegenerative disorders. The potential underlying mechanisms and effects of thalidomide on morphine-induced antinociceptive tolerance is still elusive. Hence, the present study was designed to explore the effect of thalidomide on the development and expression of morphine antinociceptive tolerance targeting l-arginine-nitric oxide (NO) pathway in mice and T98G human glioblastoma cell line...
November 26, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27884758/magnesium-enhances-opioid-induced-analgesia-what-we-have-learnt-in-the-past-decades
#10
REVIEW
Magdalena Bujalska-Zadrożny, Jan Tatarkiewicz, Kamila Kulik, Małgorzata Filip, Marek Naruszewicz
Opioids are increasingly used in alleviating pain, including cancer-related pain and postoperative pain. Unfortunately, the development of tolerance, the resistance of neuropathic pain on opioid analgesia or other undesirable effects may limit their utility. In order to reduce opioid doses, and thereby to avoid the risk of side effects and sudden deaths due to overdosing, attempts have been made to introduce co-analgesics. Due to an increasing amount of data concerning a potential enhance of opioid analgesia by the physiological antagonist of N-methyl-d-aspartate receptors, magnesium ions (Mg(2+)), a concomitant use of such a combination seems to be interesting from a clinical point of view...
November 21, 2016: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27882782/lidocaine-5-medicated-plaster-for-localized-neuropathic-pain-in-thoracic-surgical-patients
#11
Ulderico Freo, Carlo Ori, Francesco Ambrosio
Context Neuropathic pain is a common and distressing symptom in surgical thoracic patients. When it consistently presents with measurable sensory changes in a circumscribed area, neuropathic pain can be diagnosed as a localized neuropathic pain (LNP). Objective The purpose of this study was to report the efficacy of lidocaine 5% medicated plaster (Lido5%P) in the treatment of LNP in surgical thoracic patients. Methods We retrospectively reviewed the records of sixteen, cancer and noncancer, thoracic patients treated with Lido5%P for LNP...
November 24, 2016: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/27878732/endomorphins-and-%C3%AE-endorphin-do-not-affect-heart-tolerance-to-the-pathogenic-effect-of-reperfusion
#12
A V Mukhomedzyanov, L N Maslov, S Yu Tsibulnikov, J M Pei
Selective agonists of μ1- and μ2-opioid receptors endomorphin-2 and endomorphin-1 injected intravenously in a dose of 4500 nmol/kg in 5 min before coronary blood flow resumption had no effect on cardiac reperfusion damage. Consequently, μ1- and μ2-opioid receptors are not involved in the regulation of heart tolerance to reperfusion injury. Nonselective opioid receptor agonist β-endorphin (100 nmol/kg) also did not affect heart tolerance to the pathogenic effect of reperfusion.
November 23, 2016: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/27875800/evaluation-of-tspo-pet-imaging-a-marker-of-glial-activation-to-study-the-neuroimmune-footprints-of-morphine-exposure-and-withdrawal
#13
Sylvain Auvity, Sébastien Goutal, Benoît Thézé, Catarina Chaves, Benoît Hosten, Bertrand Kuhnast, Wadad Saba, Raphaël Boisgard, Irène Buvat, Salvatore Cisternino, Nicolas Tournier
INTRODUCTION: A growing area of research suggests that neuroimmunity may impact the pharmacology of opioids. Microglia is a key component of the brain immunity. Preclinical and clinical studies have demonstrated that microglial modulators may improve morphine-induced analgesia and prevent the development of tolerance and dependence. Positron emission tomography (PET) using translocator protein 18kDa (TSPO) radioligand is a clinically validated strategy for the non-invasive detection of microglial activation...
November 8, 2016: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/27873179/oxycodone-deterx-%C3%A2-a-novel-abuse-deterrent-extended-release-analgesic-option-for-the-treatment-of-patients-with-chronic-pain
#14
REVIEW
Jeff Gudin
BACKGROUND: Extended-release (ER) opioid analgesics are commonly used to provide safe and effective pain relief to treat pain severe enough to require around-the-clock, long-term dosing. These ER opioid formulations usually contain more drug per dosage unit than immediate-release (IR) agents, and therefore bring with them challenges related to both opioid abuse and misuse, often through manipulation of the dosage form. Oxycodone DETERx(®) (Xtampza(®) ER, Collegium Pharmaceutical, Inc...
December 2016: Pain and Therapy
https://www.readbyqxmd.com/read/27872689/role-of-nitric-oxide-on-dopamine-release-and-morphine-dependency
#15
REVIEW
Amir Arash Motahari, Hedayat Sahraei, Gholam Hossein Meftahi
The catastrophic effects of opioids use on public health and the economy are documented clearly in numerous studies. Repeated morphine administration can lead to either a decrease (tolerance) or an increase (sensitization) in its behavioral and rewarding effects. Morphine-induced sensitization is a major problem and plays an important role in abuse of the opioid drugs. Studies reported that morphine may exert its effects by the release of nitric oxide (NO). NO is a potent neuromodulator, which is produced by nitric oxide synthase (NOS)...
October 2016: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/27870477/ascending-single-dose-double-blind-placebo-controlled-safety-study-of-noribogaine-in-opioid-dependent-patients
#16
Paul Glue, Gavin Cape, Donna Tunnicliff, Michelle Lockhart, Fred Lam, Noelyn Hung, C Tak Hung, Sarah Harland, Jane Devane, R S Crockett, John Howes, Borje Darpo, Meijian Zhou, Holger Weis, Lawrence Friedhoff
Ibogaine is a psychoactive substance that may reduce opioid withdrawal symptoms. This was the first clinical trial of noribogaine, ibogaine's active metabolite, in patients established on methadone opioid substitution therapy (OST). In this randomized, double-blind, placebo-controlled single ascending-dose study, we evaluated the safety, tolerability, and pharmacokinetics of noribogaine in 27 patients seeking to discontinue methadone OST who had been switched to morphine during the previous week. Noribogaine doses were 60, 120, or 180 mg (n = 6/dose level) or matching placebo (n = 3/dose level)...
November 2016: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/27867308/effect-of-n-methyl-d-aspartate-receptor-antagonist-dextromethorphan-on-opioid-analgesia-in-pediatric-intensive-care-unit
#17
Mohammed Naeem, Hala Al Alem, Ali Al Shehri, Majed Al-Jeraisy
Objective. Pain control is an essential goal in the management of critical children. Narcotics are the mainstay for pain control. Patients frequently need escalating doses of narcotics. In such cases an adjunctive therapy may be beneficial. Dextromethorphan (DM) is NMDA receptor antagonist and may prevent tolerance to narcotics; however, its definitive role is still unclear. We sought whether dextromethorphan addition could decrease the requirements of fentanyl to control pain in critical children. Design. Double-blind, randomized control trial (RCT)...
2016: Pain Research & Management: the Journal of the Canadian Pain Society
https://www.readbyqxmd.com/read/27865771/cholinergic-activation-affects-the-acute-and-chronic-antinociceptive-effects-of-morphine
#18
Kinga Gawel, Ewa Gibula-Bruzda, Marcin Dziedzic, Malgorzata Jenda-Wojtanowska, Marta Marszalek-Grabska, Jerzy Silberring, Jolanta H Kotlinska
Current studies indicate that the cholinergic and opioid systems interact to modulate pain. In the present work, we investigated the influence of the cholinesterase inhibitors, donepezil (0.5; 1 or 3mg/kg, i.p.) and rivastigmine (0.03; 0.5 or 1mg/kg, i.p.), on the acute antinociceptive effects of morphine (5mg/kg, i.p.) in the hot plate test in mice. Herein, both inhibitors were found to enhance and prolong the analgesic effects of morphine without affecting latencies themselves. In an extension of this work, we determined which cholinergic receptors subtype mediates the enhancement of analgesic effects of morphine, following inhibition of cholinesterases...
November 16, 2016: Physiology & Behavior
https://www.readbyqxmd.com/read/27860208/randomized-double-blind-trial-of-oral-methylnaltrexone-for-the-treatment-of-opioid-induced-constipation-in-patients-with-chronic-noncancer-pain
#19
Richard Rauck, Neal E Slatkin, Nancy Stambler, Joseph R Harper, Robert J Israel
BACKGROUND: Subcutaneous methylnaltrexone, a peripherally acting μ-opioid receptor antagonist, improves opioid-induced constipation (OIC) in patients with chronic noncancer pain. An oral methylnaltrexone formulation has been developed. METHODS: In this phase 3, double-blind trial, adults with chronic noncancer pain receiving opioid doses of ≥50 mg/d oral morphine equivalents with OIC were randomly assigned to oral methylnaltrexone (150 mg, 300 mg, or 450 mg) or placebo once daily (QD) for 4 weeks followed by as-needed dosing for 8 weeks...
November 17, 2016: Pain Practice: the Official Journal of World Institute of Pain
https://www.readbyqxmd.com/read/27853984/fentanyl-pectin-nasal-spray-for-painful-mucositis-in-head-and-neck-cancers-during-intensity-modulated-radiation-therapy-with-or-without-chemotherapy
#20
R Mazzola, F Ricchetti, A Fiorentino, N Giaj-Levra, S Fersino, U Tebano, S Albanese, S Gori, F Alongi
PURPOSE: The aim of the current analysis was to evaluate the effectiveness and tolerability of rapid onset opioid in a cohort of head and neck cancer (HNC) patients affected by painful mucositis influencing swallowing function during RT ± ChT with definitive or adjuvant intent. METHODS: A retrospective analysis was conduct on HNC patients during RT ± ChT that received fentanyl pectin na sal spray (FPNS) for incidental BTP due to painful mucositis 13 min before the main meals...
November 16, 2016: Clinical & Translational Oncology
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