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https://www.readbyqxmd.com/read/28521199/safety-profile-of-injectable-hydromorphone-and-diacetylmorphine-for-long-term-severe-opioid-use-disorder
#1
Eugenia Oviedo-Joekes, Suzanne Brissette, Scott MacDonald, Daphne Guh, Kirsten Marchand, Salima Jutha, Scott Harrison, Amin Janmohamed, Derek Z Zhang, Aslam H Anis, Michael Krausz, David C Marsh, Martin T Schechter
AIMS: To review the safety profile of injectable hydromorphone and diacetylmorphine and explore if adverse events (AEs) or serious adverse events (SAEs) were associated with dose and patterns of attendance. METHODS: This was a non-inferiority randomized double-blind controlled trial (Vancouver, Canada) testing hydromorphone (n=100) and diacetylmorphine (n=102) for the treatment of severe opioid use disorder. Medications were delivered under the supervision of trained Registered Nurses up to three times daily...
May 10, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28515426/tolerability-of-opioid-analgesia-for-chronic-pain-a-network-meta-analysis
#2
Zengdong Meng, Jing Yu, Michael Acuff, Chong Luo, Sanrong Wang, Lehua Yu, Rongzhong Huang
Aim of this study was to study the tolerability of opioid analgesia by performing a network meta-analysis (NMA) of randomized-controlled trials (RCTs) which investigated effectiveness of opioids for the management of chronic pain. Research articles reporting outcomes of RCT/s comparing 2 or more opioid analgesics for the management of chronic pain were obtained by database search. Bayesian NMAs were performed to combine direct comparisons between treatments with that of indirect simulated evidence. Study endpoints were: incidence of adverse events, incidence of constipation, trial withdrawal rate, and patient satisfaction with treatment...
May 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28514235/ondansetron-does-not-reduce-withdrawal-in-patients-with-physical-dependence-on-chronic-opioid-therapy
#3
Larry F Chu, John Sun, Anna Clemenson, Matthew J Erlendson, Tom Rico, Erika Cornell, Hannah Obasi, Zahra N Sayyid, Ellen M Encisco, Jeff Yu, Jamison G Gamble, Ian Carroll, J David Clark
OBJECTIVES: Individuals taking opioids for an extended period of time may become physically dependent, and will therefore experience opioid withdrawal should they stop taking the medication. Previous work in animal and human models has shown that the serotonin (5-HT3) receptor may be implicated in opioid withdrawal. In this study, we investigated if ondansetron, a 5-HT3-receptor antagonist, could reduce the symptoms of opioid withdrawal after chronic opioid exposure in humans. METHODS: In this double-blinded, randomized, crossover study, 33 chronic back pain patients (N = 33) were titrated onto sustained-release oral morphine for 30 days...
May 16, 2017: Journal of Addiction Medicine
https://www.readbyqxmd.com/read/28512665/involvement-of-%C3%A2%C2%B5-opioid-receptors-and-%C3%AE%C2%BA-opioid-receptors-in-itch-related-scratching-behaviour-of-imiquimod-induced-psoriasis-like-dermatitis-in-mice
#4
Nobuaki Takahashi, Mitsutoshi Tominaga, Ryohei Kosaka, Yayoi Kamata, Yoshie Umehara, Hironori Matsuda, Azumi Sakaguchi, Hideoki Ogawa, Kenji Takamori
The pathogenesis of psoriatic itch is poorly understood. The aim of this study was to investigate the involvement of opioid receptors in scratching behaviour of imiquimod-induced psoriasis-like dermatitis model mice. Topical application of 5% imiquimod cream to the rostral back skin of mice induced antihistamine-resistant scratching behaviour. The expression of µ-opioid receptor (MOR) protein increased in the epidermis, dorsal root ganglia (DRG) and spinal cord of imiquimod-treated mice. In contrast, the expression of κ-opioid receptor (KOR) protein decreased in the DRG and spinal cord of imiquimod-treated mice, and was undetectable in the epidermis of both groups...
May 17, 2017: Acta Dermato-venereologica
https://www.readbyqxmd.com/read/28512601/anti-nociceptive-and-anti-inflammatory-potentials-of-vernoniaamygdalina-leaf-extract-via-reductions-of-leucocyte-migration-and-lipid-peroxidation
#5
Samuel Adetunji Onasanwo, Oyetola Tolulope Oyebanjo, Abayomi Mayowa Ajayi, Mujeedat Adebukola Olubori
BACKGROUND: Vernonia amygdalina is well known as a medicinal plant in folk medicine as antidiabetic, anthelmintic, antimalarial, laxative/purgative, and expectorant among others. AIM: This study was conducted to investigate the antinociceptive and anti-inflammatory effects of V. amygdalina. MATERIALS AND METHODS: Methanol extract of V. amygdalina leaf (MEVA) was evaluated for antinociceptive effect and possible mechanisms of action in the presence of naloxone (1 mg/kg), atropine (2 mg/kg), and prazosin (1 mg/kg) using acetic acid writhing test in mice...
April 2017: Journal of Intercultural Ethnopharmacology
https://www.readbyqxmd.com/read/28509855/the-hypnotic-anxiolytic-and-antinociceptive-profile-of-a-novel-%C3%A2%C2%B5-opioid-agonist
#6
Guilherme Carneiro Montes, Bianca Nascimento Monteiro da Silva, Bismarck Rezende, Roberto Takashi Sudo, Vitor Francisco Ferreira, Fernando de Carvalho da Silva, Angelo da Cunha Pinto, Bárbara Vasconcellos da Silva, Gisele Zapata-Sudo
5'-4-Alkyl/aryl-1H-1,2,3-triazole derivatives PILAB 1-12 were synthesized and a pharmacological screening of these derivatives was performed to identify a possible effect on the Central Nervous System (CNS) and to explore the associated mechanisms of action. The mice received a peritoneal injection (100 µmol/kg) of each of the 12 PILAB derivatives 10 min prior to the injection of pentobarbital and the mean hypnosis times were recorded. The mean hypnosis time increased for the mice treated with PILAB 8, which was prevented when mice were administered CTOP, a µ-opioid antagonist...
May 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28508104/quercetin-inhibits-gout-arthritis-in-mice-induction-of-an-opioid-dependent-regulation-of-inflammasome
#7
Kenji W Ruiz-Miyazawa, Larissa Staurengo-Ferrari, Sandra S Mizokami, Talita P Domiciano, Fabiana T M C Vicentini, Doumit Camilios-Neto, Wander R Pavanelli, Phileno Pinge-Filho, Flávio A Amaral, Mauro M Teixeira, Rubia Casagrande, Waldiceu A Verri
We investigated the anti-inflammatory and analgesic effects of quercetin in monosodium urate crystals (MSU)-induced gout arthritis, and the sensitivity of quercetin effects to naloxone, an opioid receptor antagonist. Mice were treated with quercetin, and mechanical hyperalgesia was assessed at 1-24 h after MSU injection. In vivo, leukocyte recruitment, cytokine levels, oxidative stress, NFκB activation, and gp91(phox) and inflammasome components (NLRP3, ASC, Pro-caspase-1, and Pro-IL-1β) mRNA expression by qPCR were determined in the knee joints at 24 h after MSU injection...
May 15, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28507784/geraniin-attenuates-naloxone-precipitated-morphine-withdrawal-and-morphine-induced-tolerance-in-mice
#8
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/28506507/syndrome-surveillance-of-fentanyl-laced-heroin-outbreaks-utilization-of-ems-medical-examiner-and-poison-center-databases
#9
P Quincy Moore, Joseph Weber, Steven Cina, Steven Aks
OBJECTIVE: Describe surveillance data from three existing surveillance systems during an unexpected fentanyl outbreak in a large metropolitan area. METHODS: We performed a retrospective analysis of three data sets: Chicago Fire Department EMS, Cook County Medical Examiner, and Illinois Poison Center. Each included data from January 1, 2015 through December 31, 2015. EMS data included all EMS responses in Chicago, Illinois, for suspected opioid overdose in which naloxone was administered and EMS personnel documented other criteria indicative of opioid overdose...
May 8, 2017: American Journal of Emergency Medicine
https://www.readbyqxmd.com/read/28504483/comparison-of-a-new-intranasal-naloxone-formulation-to-intramuscular-naloxone-results-from-hypothesis-generating-small-clinical-studies
#10
Brandon T Gufford, Garrett R Ainslie, John R White, Matthew E Layton, Jeannie M Padowski, Gary M Pollack, Mary F Paine
Easy-to-use naloxone formulations are needed to help address the opioid overdose epidemic. The pharmacokinetics of intravenous, intramuscular, and a new intranasal naloxone formulation (2 mg) were compared in six healthy volunteers. Relative to intramuscular naloxone, geometric mean [90% CI] absolute bioavailability of intranasal naloxone was modestly lower (55 [43-70] versus 41 [27-62] %), whereas average (± SE) mean absorption time was substantially shorter (74 ± 8.8 versus 6.7 ± 4.9 min). The opioid-attenuating effects of intranasal naloxone were compared to intramuscular naloxone (2 mg) after administration of oral alfentanil (4 mg) to a separate group of six healthy volunteers pre-treated with 240 ml of water or grapefruit juice...
May 15, 2017: Clinical and Translational Science
https://www.readbyqxmd.com/read/28502631/a-brain-targeted-ampakine-compound-protects-against-opioid-induced-respiratory-depression
#11
Wei Dai, Dian Xiao, Xiang Gao, Xin-Bo Zhou, Tong-Yu Fang, Zheng Yong, Rui-Bin Su
The use of opioid drugs for pain relief can induce life-threatening respiratory depression. Although naloxone effectively counteracts opioid-induced respiratory depression, it diminishes the efficacy of analgesia. Our studies indicate that ampakines, in particular, a brain-targeted compound XD-8-17C, are able to reverse respiratory depression without affecting analgesia at relatively low doses. Mice and rats were subcutaneously or intravenously injected with the opioid agonist TH-030418 to induce moderate or severe respiratory depression...
May 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28502630/new-opioid-receptor-antagonist-naltrexone-14-o-sulfate-synthesis-and-pharmacology
#12
Ferenc Zádor, Kornél Király, András Váradi, Mihály Balogh, Ágnes Fehér, Dóra Kocsis, Anna I Erdei, Erzsébet Lackó, Zoltán S Zádori, Sándor Hosztafi, Béla Noszál, Pál Riba, Sándor Benyhe, Susanna Fürst, Mahmoud Al-Khrasani
Opioid antagonists, naloxone and naltrexone have long been used in clinical practice and research. In addition to their low selectivity, they easily pass through the blood-brain barrier. Quaternization of the amine group in these molecules, (e.g. methylnaltrexone) results in negligible CNS penetration. In addition, zwitterionic compounds have been reported to have limited CNS access. The current study, for the first time gives report on the synthesis and the in vitro [competition binding, G-protein activation, isolated mouse vas deferens (MVD) and mouse colon assay] pharmacology of the zwitterionic compound, naltrexone-14-O-sulfate...
May 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28498506/a-novel-pregabalin-functionalized-salicylaldehyde-derivative-afforded-prospective-pain-inflammation-and-pyrexia-alleviating-propensities
#13
Nisar Ahmad, Fazal Subhan, Nazar Ul Islam, Muhammad Shahid, Faiz Ur Rahman, Khwaja Fawad
A novel pregabalin derivative named as pregsal ((S,E)-3-(((2-hydroxybenzylidene)amino)methyl)-5-methylhexanoic acid) was synthesized by a simple imination reaction between pregabalin and salicylaldehyde and was evaluated in the in vivo testing paradigms. The compound was characterized by UV, IR, (1) H, (13) C NMR, HR ESI-MS, and elemental analysis. It was screened (30, 50, 75, and 100 mg/kg) for antinociceptive, anti-inflammatory, and antipyretic activities in relation to pregabalin. The synthesized compound significantly attenuated the tonic acetic acid-induced nociceptive pain (30 mg/kg (P < 0...
May 12, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28496466/validated-spectrophtometric-method-for-simultaneous-determination-of-buprenorphine-and-naloxone-in-pharmaceutical-dosage-forms
#14
Effat Souri, Farzaneh Sadat Ahmadi, Maliheh Barazandeh Tehrani, Majid Mohammad Hosseini, Sedigheh Fadaye Vatan
Buprenorphine is a partial mu agonist and kappa antagonist which is used for the treatment of pain and opioid addiction. A mixture of buprenorphine hydrochloride and naloxone hydrochloride has been approved for the treatment of opioid dependence. In this study a third order derivative spectrophotometric method based on zero-crossing technique has been used for the simultaneous determination of buprenorphine hydrochloride and naloxone hydrochloride in tablets. The measurements were carried out at wavelengths of 257...
2017: Iranian Journal of Pharmaceutical Research: IJPR
https://www.readbyqxmd.com/read/28493563/nalmefene-prevents-alcohol-induced-neuroinflammation-and-alcohol-drinking-preference-in-adolescent-female-mice-role-of-tlr4
#15
Jorge Montesinos, Anabel Gil, Consuelo Guerri
BACKGROUND: We previously showed that, by activating innate immune receptors toll-like 4 (TLR4), adolescent intermittent ethanol exposure causes neuroinflammation, myelin damage and behavioral dysfunctions. Recent findings reveal that clinically-used opioid antagonists naltrexone (NT) and naloxone (NX) inhibit opioid-induced TLR4 signaling, and that NT, NX and nalmefene (NF), the 6-methylene derivative of NX, are able to reduce alcohol drinking escalation. METHODS: NF (0...
May 11, 2017: Alcoholism, Clinical and Experimental Research
https://www.readbyqxmd.com/read/28486076/medical-providers-knowledge-and-concerns-about-opioid-overdose-education-and-take-home-naloxone-rescue-kits-within-veterans-affairs-health-care-medical-treatment-settings
#16
Rachel P Winograd, Corey S Davis, Maria Niculete, Elizabeth Oliva, Richard P Martielli
BACKGROUND: Overdose from opioids is a serious public health and clinical concern. Veterans are at increased risk for opioid overdose compared with the civilian population, suggesting the need for enhanced efforts to address overdose prevention in Department of Veterans Affairs (VA) health care settings, such as primary care clinics. METHODS: Prescribing providers (N = 45) completed surveys on baseline knowledge and concerns about the VA Overdose Education and Naloxone Distribution (OEND) initiative prior to attending an OEND educational training...
April 2017: Substance Abuse
https://www.readbyqxmd.com/read/28484390/spatiotemporal-mapping-techniques-show-clozapine-impairs-neurogenic-and-myogenic-patterns-of-activity-in-the-colon-of-the-rabbit-in-a-dose-dependent-manner
#17
Susanna Every-Palmer, Roger G Lentle, Gordon Reynolds, Corrin Hulls, Paul Chambers, Helen Dunn, Pete M Ellis
Background: Clozapine, an antipsychotic used in treatment-resistant schizophrenia, has adverse gastrointestinal effects with significant associated morbidity and mortality. However, its effects on defined patterns of colonic contractile activity have not been assessed. Method: We used novel radial and longitudinal spatiotemporal mapping techniques, combined with and monitoring of ambient lumen pressure, in ex vivo preparations of triply and of singly haustrated portions of rabbit colon. We identified the contractile patterns of mass peristalses, fast phasic, and ripple contractions and directly qualified the effects of clozapine, at concentrations of 10 μmol/L, 20 μmol/L, and 30 μmol/L, and of norclozapine, the main metabolite of clozapine, on contractile patterns...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28481656/multiple-naloxone-administrations-among-emergency-medical-service-providers-is-increasing
#18
Mark Faul, Peter Lurie, Jeremiah M Kinsman, Michael W Dailey, Charmaine Crabaugh, Scott M Sasser
BACKGROUND: Opioid overdoses are at epidemic levels in the United States. Emergency Medical Service (EMS) providers may administer naloxone to restore patient breathing and prevent respiratory arrest. There was a need for contemporary data to examine the number of naloxone administrations in an EMS encounter. METHODS: Using data from the National Emergency Medical Services Information System, we examined data from 2012-5 to determine trends in patients receiving multiple naloxone administrations (MNAs)...
May 8, 2017: Prehospital Emergency Care
https://www.readbyqxmd.com/read/28478713/continuous-infusion-ketorolac-for-postoperative-analgesia-following-unilateral-total-knee-arthroplasty
#19
Amy J Schwinghammer, Alex N Isaacs, Rodney W Benner, Heather Freeman, Jacob A O'Sullivan, Sarah A Nisly
BACKGROUND: Previous clinical trials have demonstrated benefit with the addition of continuous infusion (CI) ketorolac to a multimodal pain regimen in surgical patients. Data following major orthopedic surgery are minimal and conflicting. OBJECTIVES: To evaluate CI ketorolac use following unilateral total knee arthroplasty (TKA) through assessment of patient-reported pain scores, opioid consumption, and safety outcomes. METHODS: This was a retrospective, open-label cohort study that included patients undergoing unilateral TKA at a single-center teaching hospital...
June 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28475079/treatment-of-opioid-overdose-a-brief-review-of-naloxone-pharmacology-and-delivery
#20
Thomas M Hendley, Elliot V Hersh, Paul A Moore, Berry Stahl, Mana Saraghi
No abstract text is available yet for this article.
May 2017: General Dentistry
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