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https://www.readbyqxmd.com/read/28645915/cebranopadol-blocks-the-escalation-of-cocaine-intake-and-conditioned-reinstatement-of-cocaine-seeking-in-rats
#1
Giordano de Guglielmo, Alessandra Matzeu, Jenni Kononoff, Julia Mattioni, Remi Martin-Fardon, Olivier George
Cebranopadol is a novel agonist of nociceptin/orphanin FQ peptide (NOP) and opioid receptors with analgesic properties that is being evaluated in clinical Phase 2 and Phase 3 trials for the treatment of chronic and acute pain. Recent evidence indicates that the combination of opioid and NOP receptor agonism may be a new treatment strategy for cocaine addiction. We sought to extend these findings by examining the effects of cebranopadol on cocaine self-administration (0.5 mg/kg/infusion) and cocaine conditioned reinstatement in rats with extended access to cocaine...
June 23, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28645137/-to-take-or-not-to-take-the-association-between-perceived-addiction-risk-expected-analgesic-response-and-likelihood-of-trying-novel-pain-relievers-in-self-identified-chronic-pain-patients
#2
D Andrew Tompkins, Andrew S Huhn, Patrick S Johnson, Michael T Smith, Eric C Strain, Robert R Edwards, Matthew W Johnson
BACKGROUND AND AIMS: Probability discounting refers to the effect of outcome uncertainty on decision making. Using probability discounting, we examined the degree to which self-identified chronic pain patients (CPP) were likely to try a novel analgesic medication given increasing addiction risk. We postulated that propensity for opioid misuse, trait impulsivity, and previous opioid experience would be positively associated with likelihood of risky medication use. DESIGN: This cross-sectional online study determined state/trait associations with addiction-related medication decisions in CPP...
June 23, 2017: Addiction
https://www.readbyqxmd.com/read/28644196/cebranopadol-a-novel-first-in-class-analgesic-drug-candidate-first-experience-in-patients-with-chronic-low-back-pain-in-a-randomized-clinical-trial
#3
Annette Christoph, Marie-Henriette Eerdekens, Maurits Kok, Gisela Volkers, Rainer Freynhagen
Chronic low back pain (LBP) is a common condition, usually with involvement of nociceptive and neuropathic pain components, high economic burden and impact on quality of life. Cebranopadol is a potent, first-in-class drug candidate with a novel mechanistic approach, combining nociceptin/orphanin FQ peptide and opioid peptide receptor agonism. We conducted the first Phase II, randomized, doubleblind, placebo- and active-controlled trial, evaluating the analgesic efficacy, safety, and tolerability of cebranopadol in patients with moderate to severe chronic LBP with and without neuropathic pain component...
June 21, 2017: Pain
https://www.readbyqxmd.com/read/28642282/kappa-opioid-receptors-mediate-heterosynaptic-suppression-of-hippocampal-inputs-in-the-rat-ventral-striatum
#4
Julie Brooks, Patricio O'Donnell
Kappa opioid receptors (KOR) are highly enriched within the ventral striatum (VS) and are thought to modulate striatal neurotransmission. This includes presynaptic inhibition of local glutamatergic release from excitatory inputs to the VS. However, it is not known which inputs drive this modulation and what impact they have on the local circuit dynamics within the VS. Individual medium spiny neurons (MSNs) within the VS serve as a site of convergence for glutamatergic inputs arising from the prefrontal cortex (PFC) and limbic regions, such as the hippocampus (HP)...
June 22, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28633314/qualitative-identification-of-fentanyl-analogs-and-other-opioids-in-postmortem-cases-by-uhplc-ion-trap-msn
#5
Elisa N Shoff, M Elizabeth Zaney, Joseph H Kahl, George W Hime, Diane M Boland
Since 2013, the Miami-Dade County Medical Examiner Department has experienced an increase in the number of opioid-related deaths. The majority of cases coincided with the introduction of fentanyl into the local heroin supply. From 2014 to 2015, Miami-Dade County experienced a near 600% increase in fentanyl-related deaths, followed by an additional 200% increase in 2016. In 2015, two novel fentanyl analogs were identified in medical examiner cases: beta-hydroxythiofentanyl and acetyl fentanyl. In 2016, four additional fentanyl analogs emerged: para-fluoroisobutyryl fentanyl, butyryl fentanyl, furanyl fentanyl and carfentanil, as well as the synthetic opioid U-47700...
June 13, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28632997/epidemiology-of-obesity-and-pharmacologic-treatment-options
#6
Vignesh Shettar, Sarang Patel, Srividya Kidambi
Prevalence of obesity and its related morbidity have increased to alarming levels in adults and children in the United States and globally. Weight loss results in improvement of much of the obesity-related morbidity. Lifestyle changes such as dietary modifications, increased physical activity, and behavioral therapy form the crux of weight management. However, many individuals need additional assistance (pharmacologic or surgical) to initiate or sustain weight loss. Pharmacologic therapy consists of a number of agents that work by decreasing appetite, gastric emptying, or nutrient absorption or by increasing satiety...
June 1, 2017: Nutrition in Clinical Practice
https://www.readbyqxmd.com/read/28631421/impact-of-synthetic-cannabinoids-on-the-duration-of-opioid-related-withdrawal-and-craving-among-patients-of-addiction-clinics-in-kazakhstan-a-prospective-case-control-study
#7
Mariya Prilutskaya, Francesco Saverio Bersani, Ornella Corazza, Sergey Molchanov
OBJECTIVE: The aim of the study was to prospectively assess whether regular use of synthetic cannabinoids (SCs) affects the duration of opioid-related withdrawal and craving symptoms in patients undergoing drug detoxification treatments. METHODS: Patients (n = 193) with opioid use disorder, among which 47 patients are regularly using SCs, underwent integrated drug detoxification therapies. The Clinical Opiate Withdrawal Scale and a specific visual analogue scale were used to assess opioid withdrawal and craving symptoms over time...
June 20, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28627589/effect-of-the-spinal-apelin%C3%A2-apj-system-on-the-pathogenesis-of-chronic-constriction-injury%C3%A2-induced-neuropathic-pain-in-rats
#8
Qingming Xiong, Wanyou He, Hanbing Wang, Jun Zhou, Yajun Zhang, Jian He, Chengxiang Yang, Bin Zhang
Apelin is hypothesized to serve a dual function in pain processing. Spinal administration of apelin induces hyperalgesia, while opioid receptors are implicated in the antinociceptive effects of apelin in acute nociceptive models. However, whether the apelin‑apelin receptor (APJ) system is involved in neuropathic pain remains to be elucidated. The present study aimed to evaluate the impact and mechanism of the spinal apelin‑APJ system in neuropathic pain. Chronic constriction injury (CCI) of the sciatic nerve produced sustained spinal apelin and APJ upregulation, which was associated with mechanical allodynia and heat hyperalgesia development in the hind‑paw plantar surface...
June 9, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28625446/a-novel-treatment-for-chronic-opioid-use-after-surgery
#9
Paul F White, Ofelia Loani Elvir-Lazo, Hector Hernandez
In a recent article from the Center for Disease Control, the authors addressed the current opioid epidemic in America and emphasized the importance of utilizing non-opioid analgesic alternatives to opioid medication for treating chronic pain. In cases where non-opioid analgesic drugs alone have failed to produce adequate pain relief, these authors suggested that non-pharmacologic therapies should also be considered. This Case Series describes a pilot study designed to evaluate a novel non-pharmacologic approach to treating long-standing (>1year) opioid dependency...
August 2017: Journal of Clinical Anesthesia
https://www.readbyqxmd.com/read/28623508/clinical-pharmacokinetic-characteristics-of-cebranopadol-a-novel-first-in-class-analgesic
#10
Elke Kleideiter, Chiara Piana, Shaonan Wang, Robert Nemeth, Michael Gautrois
BACKGROUND AND OBJECTIVES: Cebranopadol is a novel first-in-class analgesic acting as a nociceptin/orphanin FQ peptide and opioid peptide receptor agonist with central analgesic activity. It is currently in clinical development for the treatment of chronic pain conditions. This trial focuses on the clinical pharmacokinetic (PK) properties of cebranopadol after oral single- and multiple-dose administration. METHODS: The basic PK properties of cebranopadol were assessed by means of noncompartmental methods in six phase I clinical trials in healthy subjects and patients...
June 16, 2017: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/28618002/novel-psychoactive-substance-use-among-treatment-seeking-opiate-users-the-role-of-life-events-and-psychiatric-symptoms
#11
Máté Kapitány-Fövény, Judit Farkas, Patrícia Andrea Pataki, Anna Kiss, Janka Horváth, Róbert Urbán, Zsolt Demetrovics
OBJECTIVE: Over the past 5 years, a shift to the use of novel psychoactive substances (NPS) has been observed among opioid users. The aim of this study was to assess the potential reasons for NPS use among treatment-seeking patients receiving opiate substitution therapy. METHOD: A structured questionnaire was filled out by a sample of 198 opiate dependent patients of Hungary's National Institute of Psychiatry and Addiction. This questionnaire assessed demographics, treatment characteristics, lifetime substance use, potential reasons for NPS use, negative life events (Life Events Scale), and psychiatric symptoms (Brief Symptom Inventory)...
June 15, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28608586/metabolism-of-novel-opioid-agonists-u-47700-and-u-49900-using-human-liver-microsomes-with-confirmation-in-authentic-urine-specimens-from-drug-users
#12
Alex J Krotulski, Amanda L A Mohr, Donna M Papsun, Barry K Logan
Recently, the number of adverse events, including death, involving novel opioids has continued to increase, providing additional and sustained challenges for forensic and medical communities. Identification of emerging novel opioids can be challenging, compounded by detection windows and unknown metabolic profiles. In this study, human liver microsomes were used for the generation of in vitro metabolic profiles of U-47700 and U-49900. Generated metabolites were analyzed via a SCIEX TripleTOF® 5600+ quadrupole time-of-flight mass spectrometer and resulting data files were processing using MetabolitePilot™...
June 13, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28607342/continuous-regional-anesthesia-a-review-of-perioperative-outcome-benefits
#13
Dario Bugada, Daniela Ghisi, Edward R Mariano
Routine use of regional anesthesia for patients having surgery is supported by general safety and proven effectiveness as a targeted modality in the prevention and treatment of acute pain. Recently, perioperative physicians have become much more interested in improving long-term outcomes after surgery rather than focusing on the well-established short-term benefits of regional anesthesia. This interest has raised important questions regarding the potential influence of regional anesthesia on morbidity and mortality, persistent pain and cancer prognosis...
June 12, 2017: Minerva Anestesiologica
https://www.readbyqxmd.com/read/28605020/report-of-increasing-overdose-deaths-that-include-acetyl-fentanyl-in-multiple-counties-of-the-southwestern-region-of-the-commonwealth-of-pennsylvania-in-2015-2016
#14
Jessica B Dwyer, Jennifer Janssen, Todd M Luckasevic, Karl E Williams
Acetyl fentanyl is a Schedule I controlled synthetic opioid that is becoming an increasingly detected "designer drug." Routine drug screening procedures in local forensic toxicology laboratories identified a total of 41 overdose deaths associated with acetyl fentanyl within multiple counties of the southwestern region of the state of Pennsylvania. The range, median, mean, and standard deviation of blood acetyl fentanyl concentrations for these 41 cases were 0.13-2100 ng/mL, 11 ng/mL, 169.3 ng/mL, and 405...
June 12, 2017: Journal of Forensic Sciences
https://www.readbyqxmd.com/read/28603962/novel-opioid-analgesics-and-side-effects
#15
Giovanna Del Vecchio, Viola Spahn, Christoph Stein
Conventional opioids mediate analgesia as well as severe adverse effects via G-protein coupled opioid receptors (OR) in both inflamed (peripheral injured tissue) and healthy (brain, intestinal wall) environments. To exclude side effects, OR activation can be selectively achieved in damaged tissue by lowering the pKa of an opioid ligand to the acidic pH of inflammation. As a result, protonation of the ligand and consequent OR binding and activation of G-proteins is pH- and injury-specific. A novel compound (NFEPP) demonstrates the feasibility of this approach and displays blockade of pain transmission only at the peripheral site of injury, but with lack of central and gastrointestinal adverse effects...
June 12, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28602640/design-and-synthesis-of-novel-%C3%AE-opioid-receptor-agonists-with-an-azatricyclodecane-skeleton-for-improving-blood-brain-barrier-penetration
#16
Yoshikazu Watanabe, Kohei Hayashida, Daisuke Saito, Toshihiro Takahashi, Junichi Sakai, Eriko Nakata, Takashi Kanda, Takashi Iwai, Shigeto Hirayama, Hideaki Fujii, Tomio Yamakawa, Hiroshi Nagase
We designed and synthesized novel δ opioid receptor (DOR) agonists 3a-i with an azatricyclodecane skeleton, which was a novel structural class of DOR agonists. Among them, 3b exhibited high values of binding affinity and potent agonistic activity for the DOR that were approximately equivalent to those of 2 which bore an oxazatricyclodecane skeleton. In vitro assays using the blood-brain barrier (BBB) permeability test kit supported the idea that 3b achieved an excellent BBB permeability by converting an oxygen atom of 2 to a carbon atom (methylene group) in the core skeleton...
May 26, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28602044/the-dynamic-interaction-between-pain-and-opioid-misuse
#17
REVIEW
Adrianne R Wilson-Poe, Jose A Moron
In 2014, drug overdose surpassed automobile accidents as the number one cause of accidental death for the first time in US history. The overdose epidemic is largely driven by opioids, and genuine prescription opioid analgesics play the biggest role in this phenomenon. Despite advancements in abuse deterrent formulations, prescription drug monitoring programs, and clinical assessments for the detection of abuse potential, drug overdoses continue to escalate. The CDC has recently issued new guidelines for opioid prescription, yet even these recommendations have their shortcomings...
June 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28601204/battlefield-analgesia-in-tactical-combat-casualty-care
#18
REVIEW
Ian S Wedmore, Frank K Butler
At the start of the Afghanistan conflict, battlefield analgesia for US military casualties was achieved primarily through the use of intramuscular (IM) morphine. This is a suboptimal choice, since IM morphine is slow-acting, leading to delays in effective pain relief and the risk of overdose and death when dosing is repeated in order to hasten the onset of analgesia. Advances in battlefield analgesia, pioneered initially by Tactical Combat Casualty Care (TCCC), and the Army's 75th Ranger Regiment, have now been incorporated into the Triple-Option Analgesia approach...
June 2017: Wilderness & Environmental Medicine
https://www.readbyqxmd.com/read/28593835/pharmacokinetics-of-a-novel-transdermal-fentanyl-solution-in-rhesus-macaques-macaca-mulatta
#19
Gregory W Salyards, Marie-Josee Lemoy, Heather K Knych, Ashley E Hill, Kari L Christe
Rhesus macaques (Macaca mulatta) are the most commonly used NHP biomedical model and experience both research andclinical procedures requiring analgesia. Opioids are a mainstay of analgesic therapy. A novel, transdermal fentanyl solution(TFS) has been developed as a long-acting, single-administration topical opioid and was reported to provide at least 4 d ofeffective plasma concentrations in beagles (Canis familiaris). To evaluate the pharmacokinetic profile of TFS in healthy adultrhesus macaques, we used a 2-period, 2-treatment crossover study of a single topical administration of 1...
June 7, 2017: Journal of the American Association for Laboratory Animal Science: JAALAS
https://www.readbyqxmd.com/read/28590391/misuse-of-novel-synthetic-opioids-a-deadly-new-trend
#20
Matthew P Prekupec, Peter A Mansky, Michael H Baumann
: Novel synthetic opioids (NSOs) include various analogs of fentanyl and newly emerging non-fentanyl compounds. Together with illicitly manufactured fentanyl (IMF), these drugs have caused a recent spike in overdose deaths, whereas deaths from prescription opioids have stabilized. NSOs are used as stand-alone products, as adulterants in heroin, or as constituents of counterfeit prescription medications. During 2015 alone, there were 9580 deaths from synthetic opioids other than methadone. Most of these fatalities were associated with IMF rather than diverted pharmaceutical fentanyl...
June 5, 2017: Journal of Addiction Medicine
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