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https://www.readbyqxmd.com/read/28087496/digital-pills-to-measure-opioid-ingestion-patterns-in-emergency-department-patients-with-acute-fracture-pain-a-pilot-study
#1
Peter R Chai, Stephanie Carreiro, Brendan J Innes, Rochelle K Rosen, Conall O'Cleirigh, Kenneth H Mayer, Edward W Boyer
BACKGROUND: Nonadherence to prescribed regimens for opioid analgesic agents contributes to increasing opioid abuse and overdose death. Opioids are frequently prescribed on an as-needed basis, placing the responsibility to determine opioid dose and frequency with the patient. There is wide variability in physician prescribing patterns because of the lack of data describing how patients actually use as-needed opioid analgesics. Digital pill systems have a radiofrequency emitter that directly measures medication ingestion events, and they provide an opportunity to discover the dose, timing, and duration of opioid therapy...
January 13, 2017: Journal of Medical Internet Research
https://www.readbyqxmd.com/read/28078167/a-novel-strategy-for-attenuating-opioid-withdrawal-in-neonates
#2
Giovanni C Santoro, Samarth Shukla, Krishna Patel, Jakub Kaczmarzyk, Stergiani Agorastos, Sandra Scherrer, Yoon Young Choi, Christina Veith, Joseph Carrion, Rebecca Silverman, Danielle Mullin, Mohamed Ahmed, Wynne K Schiffer, Jonathan D Brodie, Stephen L Dewey
The rate of Neonatal Abstinence Syndrome (NAS) has drastically increased over the past decade. The average hospital expense per NAS patient has tripled, while the number of babies born to opioid-dependent mothers has increased to 5 in 1000 births. Current treatment options are limited to opioid replacement and tapering. Consequently, we examined the efficacy of prenatal, low-dose and short-term vigabatrin (γ-vinyl GABA, GVG) exposure for attenuating these symptoms as well as the metabolic changes observed in the brains of these animals upon reaching adolescence...
August 2016: Journal of Addiction Research & Therapy
https://www.readbyqxmd.com/read/28077540/leukemia-inhibitory-factor-lif-potentiates-antinociception-activity-and-inhibits-tolerance-induction-of-opioids
#3
H J Tu, K H Kang, S Y Ho, H C Liou, H H Liou, C P Lin, W M Fu
BACKGROUND: The efficacy of opioids typically decreases after long-term use owing to the development of tolerance. Glial activation and the upregulation of proinflammatory cytokines are related to the induction of tolerance. We investigated the effect of leukemia inhibitory factor (LIF) on morphine analgesia and tolerance. METHODS: LIF concentrations in rat spinal cords were measured by polymerase chain reaction (PCR) and enzyme-linked immunosorbent assay (ELISA) after morphine administration...
October 2016: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/28073248/interplay-of-g-protein-coupled-receptors-with-the-membrane-insights-from-supra-atomic-coarse-grain-molecular-dynamics-simulations
#4
Xavier Periole
G protein-coupled receptors (GPCRs) are central to many fundamental cellular signaling pathways. They transduce signals from the outside to the inside of cells in physiological processes ranging from vision to immune response. It is extremely challenging to look at them individually using conventional experimental techniques. Recently, a pseudo atomistic molecular model has emerged as a valuable tool to access information on GPCRs, more specifically on their interactions with their environment in their native cell membrane and the consequences on their supramolecular organization...
January 11, 2017: Chemical Reviews
https://www.readbyqxmd.com/read/28072811/evaluation-of-the-ototoxicity-potential-of-once-daily-single-entity-hydrocodone-in-patients-with-chronic-pain-results-of-two-phase-3-clinical-studies
#5
Kathleen Campbell, J Walter Kutz, Angela Shoup, Warren Wen, Shau Yu Lynch, Ellie He, Steven R Ripa
BACKGROUND: Use/misuse of the opioid combination hydrocodone-acetaminophen has been associated with permanent hearing loss. Although reports have been rare, this potential effect can have significant detrimental effect on patients' overall quality of life. To date, the ototoxic effect of hydrocodone alone has not been systematically investigated. OBJECTIVE: In this report, we aimed to evaluate the potential ototoxicity of a novel, single-entity, once-daily, extended-release hydrocodone tablet (Hysingla® ER; HYD)...
January 2017: Pain Physician
https://www.readbyqxmd.com/read/28071341/identification-of-novel-hits-as-highly-prospective-dual-agonists-for-mu-and-kappa-opioid-receptors-an-integrated-in-silico-approach
#6
Indrani Bera, Mrinal Vishwas Marathe, Pavan V Payghan, Nanda Ghoshal
Opioid agonists are used clinically for the treatment of acute and chronic pain, however, their clinical use is limited due to the presence of undesired side effects. Dual agonists, simultaneously targeting mu and kappa opioid receptors, show fewer side effects than that of selective agonists. In the present work, 2D- and 3D- Quantitative Structure Activity Relationship studies were performed on a series of aminomorphinan derivatives as dual agonists, using a wide range of descriptors. The aim of the study was to identify the structural requirements for the activity of these compounds towards mu and kappa opioid receptors and using the models, with best external predictability, for predicting the activities of new hits obtained from shape based virtual screening of drug like compounds from ZINC database...
January 10, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28069442/novel-signaling-of-dynorphin-at-%C3%AE%C2%BA-opioid-receptor-bradykinin-b2-receptor-heterodimers
#7
Bingyuan Ji, Haiqing Liu, Rumin Zhang, Yunlu Jiang, Chunmei Wang, Sheng Li, Jing Chen, Bo Bai
The κ-opioid receptor (KOR) and bradykinin B2 receptor (B2R) are involved in a variety of important physiological processes and share many similar characteristics in terms of their distribution and functions in the nervous system. We first demonstrated the endogenous expression of KOR and B2R in human SH-SY5Y cells and their co-localization on the membrane of human embryonic kidney 293 (HEK293) cells. Bioluminescence and fluorescence resonance energy transfer and the proximity ligation assay were exploited to demonstrate the formation of functional KOR and B2R heteromers in transfected cells...
January 7, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28065792/the-analgesic-effects-of-oxytocin-in-the-peripheral-and-central-nervous-system
#8
Qing Xin, Bo Bai, Wenyan Liu
Pain is a ubiquitously unpleasant feeling among humans as well as many animal species often caused by actual and potential tissue damage. However, it is absolutely crucial for our survival in many ways. Acute pain can signal the presence of danger or life-threatenting events, which help escape noxious stimuli. By contrast, when pain becomes chronic or persistent, it becomes an encumbrance and exerts deleterious effects to the body and mind, often co-occured with anxiety and depression. Additionaly, chronic pain is more or less an economic burden for the patients because it requires immediate medical treatments and seriously hinders pepople in their work...
January 5, 2017: Neurochemistry International
https://www.readbyqxmd.com/read/28063773/the-implementation-of-a-naloxone-rescue-program-in-university-students
#9
Shannon G Panther, Brenda S Bray, John R White
OBJECTIVE: Responding to the nationwide opioid overdose epidemic, Washington State University initiated a naloxone safety net project intending to increase awareness of opioid overdose, increase the availability of naloxone, and examine university students' perceptions regarding the usefulness of a novel, large-group audience-training model. SETTING: A Washington State University campus. PRACTICE DESCRIPTION: In September 2014, university students were recruited to attended a large-group audience training event which included opioid overdose prevention, recognition, and first response...
January 4, 2017: Journal of the American Pharmacists Association: JAPhA
https://www.readbyqxmd.com/read/28063353/rationally-designed-benzopyran-fused-isoxazolidines-and-derived-%C3%AE-2-3-3-amino-alcohols-as-potent-analgesics-synthesis-biological-evaluation-and-molecular-docking-analysis
#10
Gagandeep Singh, Gurjit Singh, Rajbir Bhatti, Vivek Gupta, Ajay Mahajan, Palwinder Singh, Mohan Paul Singh Ishar
Based on structure activity analysis of morphine related opiates, we have synthesized some novel benzopyran fused isoxazolidines (2a-e) and derived conformationally constrained β(2,3,3)-amino alcohols (3a-e), which were evaluated in vivo for their anti-nociceptive activity through acetic acid induced writhing test (peripheral) and formalin induced algesia (central). Results showed that, compound 2a possesses significant opioid agonist activity. Further, molecular docking analysis reveals that compound 2a binds to δ-opioid receptor (DOR) with comparatively better D-score than to μ (MOR) and κ (KOR) receptors...
December 28, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28062251/opioid-suppression-of-conditioned-anticipatory-brain-responses-to-breathlessness
#11
Anja Hayen, Vishvarani Wanigasekera, Olivia K Faull, Stewart F Campbell, Payashi S Garry, Simon J M Raby, Josephine Robertson, Ruth Webster, Richard G Wise, Mari Herigstad, Kyle T S Pattinson
Opioid painkillers are a promising treatment for chronic breathlessness, but are associated with potentially fatal side effects. In the treatment of breathlessness, their mechanisms of action are unclear. A better understanding might help to identify safer alternatives. Learned associations between previously neutral stimuli (e.g. stairs) and repeated breathlessness induce an anticipatory threat response that may worsen breathlessness, contributing to the downward spiral of decline seen in clinical populations...
January 3, 2017: NeuroImage
https://www.readbyqxmd.com/read/28054242/anti-nociceptive-and-anti-inflammatory-actions-of-sulforaphane-in-chronic-constriction-injury-induced-neuropathic-pain-mice
#12
Cheng Wang, Congpin Wang
Neuropathic pain is still considered as incurable disease as current therapies are not ideal in terms of efficacy and tolerability. It is imperative to search for novel drugs to obtain better treatments. Sulforaphane (SFN), a derivative of glucoraphanin present in cruciferous vegetables, exhibits therapeutic effects on inflammation-related diseases. Since inflammation plays an important role in regulating chronic pain, in the present study, we investigated anti-nociceptive effects of SFN and its underlying mechanisms in a neuropathic pain mouse model, sciatic nerve chronic constriction injury (CCI)...
January 4, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28043894/propionic-acid-metabolism-asd-and-vitamin-b12-is-there-a-role-for-environmental-nitrous-oxide
#13
Keith Fluegge
Foley et al. (2014) published their findings in this journal on the role of prenatal exposure to propionic acid (PPA) and behavioral outcomes in treated rat pups. The authors show that PPA treated pups displayed subtle differences in behavior including nest seeking, novel object recognition, and locomotor activity. Others have previously proposed that PPA infusion in rat could represent a valid animal model of ASD since many of the diagnostic criteria for the disorder spectrum manifest under such conditions...
December 30, 2016: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/28042019/endomorphin-2-analogs-with-c-terminal-esterification-produce-potent-systemic-antinociception-with-reduced-tolerance-and-gastrointestinal-side-effects
#14
Chang-Lin Wang, Ting-Ting Qiu, Dai-Jun Yang, Bi-Yu Yuan, Feng-Tong Han, Li Li, Ning Gu
C-terminal esterification of opioid peptides may change their opioid activities due to the modified physicochemical properties. In the present study, the pharmacological activities of C-terminal esterified endomorphin-2 (EM-2) analogs 1-3 were characterized by in vitro metabolic stability and octanol/buffer distribution assays. Also, the antinociceptive profiles in the radiant heat paw withdrawal test and related side effects of these analogs were determined. Our results showed that all three analogs significantly increased the metabolic stability and lipophilicity...
December 29, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/28035708/solid-phase-microextraction-of-methadone-in-urine-samples-by-electrochemically-co-deposited-sol-gel-cu-nanocomposite-fiber
#15
Sirwan Mohammadiazar, Fatemeh Hasanli, Mehdi Maham, Somayeh Payami Samarin
Electrochemically co-deposited sol-gel/Cu nanocomposites has been introduced as a novel, simple and single step technique for preparation of solid phase microextraction coating to extract methadone (MDN) (a synthetic opioid) in urine samples. The porous surface structure of the sol-gel/Cu nanocomposite coating was revealed by scanning electron microscopy (SEM). Direct immersion-solid phase microextraction (DI-SPME) followed by HPLC-UV determination was employed. The factors influencing the SPME procedure such as the salt content, desorption solvent type, pH and equilibration time were optimized...
December 30, 2016: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/28035035/analysis-of-u-47700-a-novel-synthetic-opioid-in-human-urine-by-lc-ms-ms-and-lc-qtof
#16
Steven W Fleming, Justin C Cooley, Leonard Johnson, C Clinton Frazee, Kristina Domanski, Kurt Kleinschmidt, Uttam Garg
The illicit drug market has rapidly evolved from synthetic cannabinoids to cathinone derivatives and now a new emerging threat of synthetic opioids. These compounds were mostly developed by pharmaceutical companies during drug discovery. The new psychoactive substances are not routinely covered in drug screening and may go undetected. Recently fentanyl analogous, AH-7921, MT-45 and now U-47700 have been encountered in clinical and forensic casework. U-47700 is gaining popularity on drug user forms as a legal alternative to heroin...
December 29, 2016: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28033462/the-pharmacological-heterogeneity-of-nepenthone-analogs-in-conferring-highly-selective-and-potent-%C3%AE-opioid-agonistic-activities
#17
Wei Li, Jian-Dong Long, Yuan-Yuan Qian, Yu Long, Xue-Jun Xu, Yu-Jun Wang, Qing Shen, Zuo-Neng Wang, Xi-Cheng Yang, Li Xiao, Hong-Peng Sun, Yulong Xu, Yiyi Chen, Qiong Xie, Yonghui Wang, Liming Shao, Jing-Gen Liu, Zhuibai Qiu, Wei Fu
To develop novel analgesics with no or less side effects than that of traditional opioids is highly demanded to treat opioid receptors mediated pain and addiction issues. Recently, Κ-opioid receptor (KOR) is established as an attractive target, although its selective agonists could bear heterogeneous pharmacological activities. In this study, we designed and synthesized two new series of nepenthone derivatives by inserting a spacer (carbonyl) between 6α,14α-endo-ethenyl-thebaine and the 7α-phenyl substitution of the skeleton, and by substituting the 17-N-methyl group with a cyclopropylmethyl group...
December 29, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28031725/skin-matters-the-role-of-keratinocytes-in-nociception-a-rational-argument-for-the-development-of-topical-analgesics
#18
REVIEW
Jan M Keppel Hesselink, David J Kopsky, Arun K Bhaskar
Treatment of neuropathic pain using topical formulations is still in its infancy. Only few topical analgesic formulations have become available for clinical use, and among these, analgesic creams are still rare. This is unfortunate because analgesic creams offer a number of advantages over patches, such as convenience, ease of adapting the frequency of application, and dose, and "rubbing cream where it hurts" involves the patient much more in the therapeutic process compared to patches and other localized treatment modalities...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/28029366/computational-aided-design-of-magnetic-ultra-thin-dummy-molecularly-imprinted-polymer-for-selective-extraction-and-determination-of-morphine-from-urine-by-high-performance-liquid-chromatography
#19
Shuangling Xi, Kai Zhang, Deli Xiao, Hua He
In this work, a novel magnetic ultra-thin dummy molecularly imprinted polymer (MMIP) for morphine (MO) was prepared. In order to obtain highly selective recognition cavities, the MMIP has been designed using semi-flexible docking to screen the optimal monomer and its ratio to morphine from six representative monomers. Furthermore, the dummy template was creatively screened by semi-flexible docking method from opioid drugs. The system of dihydrocodeine (DI) as dummy template, methacrylamide (MAC) as founctional monomer, ethyleneglycol dimethacrylate (EGDMA) as crosslinker was chosen for MO imprinting...
October 1, 2016: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28028255/-a-new-treatment-strategy-novel-cell-free-and-concentrated-ascites-reinfusion-system-km-cart-for-massive-malignant-ascites
#20
Keisuke Matsusaki
Massive ascites associated with cancerous peritonitis can result in severe respiratory discomfort and abdominal fullness. Additionally, it can significantly impair the activities of daily living of a patient, and relaxation is difficult to achieve, even with opioids. Frequent ascites drainage can cause rapid worsening of the patient's general condition, and a large amount of ascites can lead to discontinuation of anti-cancer treatment. Cell-free and concentrated ascites reinfusion therapy(CART)for refractory ascites was first covered by the insurance system in 1981...
December 2016: Gan to Kagaku Ryoho. Cancer & Chemotherapy
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