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https://www.readbyqxmd.com/read/28066107/anxiolytic-activity-of-aqueous-extract-of-camellia-sinensis-in-rats
#1
Rajeshwari Shastry, Sheetal Dinkar Ullal, Shreyas Karkala, Seema Rai, Akash Gadgade
OBJECTIVES: The present study was undertaken to evaluate anxiolytic effect of Camellia sinensis (CS) and possible mechanism on acute and chronic administration in rats. MATERIALS AND METHODS: Eight groups of rats with six in each group were used. Group I served as control. Group II received diazepam (1 mg/kg). Groups III, IV, and V received CS in doses of 3.3, 16.5, and 33 mg/kg, respectively. Three pharmacologically validated experimental models - elevated plus maze (EPM), light and dark box (LDB), and open field tests (OFT) - were employed...
November 2016: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/28038309/diazepam-inhibits-electrically-evoked-and-tonic-dopamine-release-in-the-nucleus-accumbens-and-reverses-the-effect-of-amphetamine
#2
Alexander Gomez-A, Amanda Maino Fiorenza, Suelen Lucio Boschen, Adam H Sugi, Danielle Beckman, Sergio T Ferreira, Kendall H Lee, Charles D Blaha, Claudio Da Cunha
Diazepam is a benzodiazepine receptor agonist with anxiolytic and addictive properties. Although most drugs of abuse increase dopamine release in the nucleus accumbens, here we show that not only it causes the opposite effect but also prevents amphetamine action on increasing dopamine release. We used 20 min sampling in vivo microdialysis and subsecond fast-scan cyclic voltammetry recordings at carbon-fiber microelectrodes to show that diazepam caused a dose-dependent decrease in tonic and electrically-evoked dopamine release in the nucleus accumbens of urethane anesthetized adult male Swiss mice...
December 30, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28013354/gabaa-receptor-occupancy-by-subtype-selective-gabaa%C3%AE-2-3-modulators-pet-studies-in-humans
#3
Aurelija Jucaite, Zsolt Cselényi, Jaakko Lappalainen, Dennis J McCarthy, Chi-Ming Lee, Svante Nyberg, Katarina Varnäs, Per Stenkrona, Christer Halldin, Alan Cross, Lars Farde
RATIONALE: Sedation, dependence, and abuse liability limit the use of non-selective γ-aminobutyric acid (GABAA) receptor positive modulators for the treatment of anxiety. AZD7325 and AZD6280 are novel, subtype-selective GABAAα2,3 receptor positive modulators with limited sedative effects. OBJECTIVES: The current study aimed to confirm target engagement at GABAA receptors by AZD7325 and AZD6280 in humans and to determine the relationship between exposure, GABAA receptor occupancy, and tolerability...
December 24, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27986927/histological-underpinnings-of-grey-matter-changes-in-fibromyalgia-investigated-using-multimodal-brain-imaging
#4
F B Pomares, T Funck, N A Feier, S Roy, A Daigle-Martel, M Ceko, S Narayanan, D Araujo, A Thiel, N Stikov, M A Fitzcharles, P Schweinhardt
: Chronic pain patients present with cortical grey matter alterations, observed with anatomical magnetic resonance (MR) imaging. Reduced regional grey matter volumes are often interpreted to reflect neurodegeneration but studies investigating the cellular origin of grey matter changes are lacking. We used multi-modal imaging to compare 26 post-menopausal women with 25 healthy controls (age range: 50-75 years) to test whether regional grey matter volume decreases in chronic pain are associated with compromised neuronal integrity...
December 16, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27932682/preliminary-assessment-of-midazolam-fentanyl-and-fluanisone-combination-for-the-sedation-of-rhesus-macaques-macaca-mulatta
#5
Henri G M J Bertrand, Charlotte F Sandersen, Paul A Flecknell
This study was undertaken to assess the suitability of fentanyl/fluanisone ('Hypnorm', VetaPharma; 0.315 mg/mL of fentanyl citrate and 10 mg/mL of fluanisone) alone or combined with midazolam in rhesus macaques. Fifteen rhesus macaques requiring sedation for veterinary procedures received an intramuscular (IM) dose range of Hypnorm from 0.01 mL/kg to 0.3 mL/kg either alone or combined with 0.5 mg/kg of midazolam. To reverse the sedation, flumazenil in combination with either naloxone, buprenorphine or butorphanol was administered intravenously (IV) or IM...
December 8, 2016: Laboratory Animals
https://www.readbyqxmd.com/read/27924205/risperidone-in-a-child-with-untractable-emergency-delirium-a-case-report
#6
Young Hee Shin, Seung Hyeon Lee, Dae Yoon Kim
A 6-year-old boy was scheduled for thoracic magnetic resonance imaging under deep sedation with midazolam 1.8 mg and propofol 100 µg/kg/min via intravenous injection. He showed emergence delirium in the post-anesthesia care unit. The staff attempted to calm him by administering flumazenil as an antidote for midazolam, propofol for further sedation, and meperidine. However, this was not successful. A psychiatrist recommended the use of antipsychotics. Administration of risperidone led to immediate resolution of the boy's symptoms and relaxed him...
December 2016: Korean Journal of Anesthesiology
https://www.readbyqxmd.com/read/27920113/flumazenil-in-benzodiazepine-overdose
#7
Howard An, Jesse Godwin
No abstract text is available yet for this article.
December 6, 2016: CMAJ: Canadian Medical Association Journal, Journal de L'Association Medicale Canadienne
https://www.readbyqxmd.com/read/27898636/flumazenil-use-for-isolated-ataxia-in-a-child
#8
Angela Regina, David Lee, Payal Sud, Diana Crevi
No abstract text is available yet for this article.
December 2016: Pediatric Emergency Care
https://www.readbyqxmd.com/read/27886620/pet-measurement-of-gaba-shift-in-the-rat-brain-a-preclinical-application-of-bolus-plus-constant-infusion-paradigm-of-18-f-flumazenil
#9
Wook Kim, Hyun Soo Park, Byung Seok Moon, Byung Chul Lee, Sang Eun Kim
INTRODUCTION: We measured the tiagabine-induced enhancement of the GABAA receptor's affinity for benzodiazepine ligands ("GABA shift") using [(18)F]flumazenil (FMZ) PET with preclinical application of bolus plus constant infusion (B/I). Differences in quantified results of [(18)F]FMZ binding were compared to that of [(18)F]FMZ PET with single bolus injection (SB). MATERIALS AND METHODS: Sprague-Dawley rats underwent [(18)F]FMZ PET scans with B/I, which consisted of baseline and "GABA shift" sessions in a scan, or scans with SB one week apart...
February 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/27875053/pharmacological-reversal-agents-in-dental-practice-keys-to-patient-safety
#10
Mark Donaldson, Jason H Goodchild
Though uncommon, medical emergencies in the dental office are harrowing occurrences that can be the result of adverse drug reactions. Pharmacological antagonists have been developed for administration as reversal agents in emergency situations in which patients may have an untoward effect, typically caused by too much medication. Dental practitioners should be familiar with these agents to keep patients safe and help mitigate drug-induced medical emergencies. This article reviews the pharmacokinetic and pharmacodynamic principles of pharmacological antagonists; it emphasizes six specific reversal agents as they relate to the clinical practice of dentistry: naloxone, flumazenil, epinephrine, diphenhydramine, phentolamine, and atropine...
November 2016: Compendium of Continuing Education in Dentistry
https://www.readbyqxmd.com/read/27826950/effects-of-common-anesthetic-agents-on-18-f-flumazenil-binding-to-the-gabaa-receptor
#11
Mikael Palner, Corinne Beinat, Sam Banister, Francesca Zanderigo, Jun Hyung Park, Bin Shen, Trine Hjoernevik, Jae Ho Jung, Byung Chul Lee, Sang Eun Kim, Lawrence Fung, Frederick T Chin
BACKGROUND: The availability of GABAA receptor binding sites in the brain can be assessed by positron emission tomography (PET) using the radioligand, [(18)F]flumazenil. However, the brain uptake and binding of this PET radioligand are influenced by anesthetic drugs, which are typically needed in preclinical imaging studies and clinical imaging studies involving patient populations that do not tolerate relatively longer scan times. The objective of this study was to examine the effects of anesthesia on the binding of [(18)F]flumazenil to GABAA receptors in mice...
December 2016: EJNMMI Research
https://www.readbyqxmd.com/read/27803387/neurorespiratory-effects-of-buprenorphine-and-ethanol-in-combination-a-mechanistic-study-of-drug-drug-interactions-in-the-rat
#12
Camille Cohier, Lucie Chevillard, Sophie Salle, Patricia Risède, Olivier Roussel, Bruno Mégarbane
Respiratory depression and fatalities have been attributed to ethanol/buprenorphine (BUP) combination in drug addicts maintained with BUP/naloxone or BUP alone. The exact mechanisms of the ethanol/BUP interaction and the contribution to the toxicity of norbuprenorphine (NBUP), the main BUP metabolite with respiratory depressant properties are unknown. We investigated the sedative and plethsymographic effects resulting from the co-administration of intragastric ethanol (3 g/kg) and intravenous BUP (30 mg/kg) in Sprague-Dawley rats...
November 1, 2016: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/27720293/synthesis-and-pharmacological-evaluation-of-functionalized-isoindolinones-on-gaba-activated-chloride-currents-in-rat-cerebellum-granule-cells-in-culture
#13
Antonia Di Mola, Elena Gatta, Carmen Petronzi, Aroldo Cupello, Paolo De Caprariis, Mauro Robello, Antonio Massa, Rosanna Filosa
A focused N-substituted 3-(2-piperazin-1-yl-2-oxoethyl)-2-(pyridin-2-yl)iso-indolin-1-ones small library was synthesized for modulation of GABA-A receptor function and compared to Zopiclone for the ability to increase GABA-activated chloride currents. All compounds were tested for their effects on GABA-activated chloride currents in rat cerebellar granule cells by use of the whole-cell patch clamp technique. Electrophysiological studies on cultured cerebellar granule cells revealed 3-[2-(4-methylpiperazin-1-yl)-2-oxoethyl]-2-(5-nitropyridin-2-yl)iso-indolin-1-one (Id) as a partial agonist displaying 34% increase of the 10μM GABA evoked peak chloride currents, antagonized by flumazenil...
September 15, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27711224/benzodiazepine-use-during-hospitalization-automated-identification-of-potential-medication-errors-and-systematic-assessment-of-preventable-adverse-events
#14
David Franklin Niedrig, Liesa Hoppe, Sarah Mächler, Heike Russmann, Stefan Russmann
OBJECTIVE: Benzodiazepines and "Z-drug" GABA-receptor modulators (BDZ) are among the most frequently used drugs in hospitals. Adverse drug events (ADE) associated with BDZ can be the result of preventable medication errors (ME) related to dosing, drug interactions and comorbidities. The present study evaluated inpatient use of BDZ and related ME and ADE. METHODS: We conducted an observational study within a pharmacoepidemiological database derived from the clinical information system of a tertiary care hospital...
2016: PloS One
https://www.readbyqxmd.com/read/27679539/-18-f-fluorodeoxyglucose-and-18-f-flumazenil-positron-emission-tomography-in-patients-with-refractory-epilepsy
#15
REVIEW
Marina Hodolic, Raffi Topakian, Robert Pichler
BACKGROUND: Epilepsy is a neurological disorder characterized by epileptic seizures as a result of excessive neuronal activity in the brain. Approximately 65 million people worldwide suffer from epilepsy; 20-40% of them are refractory to medication therapy. Early detection of disease is crucial in the management of patients with epilepsy. Correct localization of the ictal onset zone is associated with a better surgical outcome. The modern non-invasive techniques used for structural-functional localization of the seizure focus includes electroencephalography (EEG) monitoring, magnetic resonance imaging (MRI), single photon emission tomography/computed tomography (SPECT/CT) and positron emission tomography/computed tomography (PET/CT)...
September 1, 2016: Radiology and Oncology
https://www.readbyqxmd.com/read/27672456/reversal-of-a-suspected-paradoxical-reaction-to-zopiclone-with-flumazenil
#16
Zarah Jordahn, Cheme Andersen, Anne Marie Roust Aaberg, Frank Christian Pott
We describe the care for an elderly woman who was admitted to the intensive care unit (ICU) to receive noninvasive ventilation for acute exacerbation of chronic obstructive pulmonary disease. After administration of the sleeping pill zopiclone, a nonbenzodiazepine receptor agonist (NBRA), the patient became agitated and was confused, a possible paradoxical reaction to benzodiazepines. These symptoms were immediately resolved after treatment with flumazenil, usually used to reverse the adverse effects of benzodiazepines or NBRAs and to reverse paradoxical reactions to benzodiazepines...
2016: Case Reports in Critical Care
https://www.readbyqxmd.com/read/27614005/assessing-neuronal-density-in-peri-infarct-cortex-with-pet-effects-of-cortical-topology-and-partial-volume-correction
#17
Thomas Funck, Mohammed Al-Kuwaiti, Claude Lepage, Peter Zepper, Jeffrey Minuk, Hyman M Schipper, Alan C Evans, Alexander Thiel
The peri-infarct cortex (PIC) is the site of long-term physiologic changes after ischemic stroke. Traditional methods for delineating the peri-infarct gray matter (GM) have used a volumetric Euclidean distance metric to define its extent around the infarct. This metric has limitations in the case of cortical stroke, i.e., those where ischemia leads to infarction in the cortical GM, because the vascularization of the cerebral cortex follows the complex, folded topology of the cortical surface. Instead, we used a geodesic distance metric along the cortical surface to subdivide the PIC into equidistant rings emanating from the infarct border and compared this new approach to a Euclidean distance metric definition...
January 2017: Human Brain Mapping
https://www.readbyqxmd.com/read/27573669/%C3%AE-pinene-a-major-constituent-of-pine-tree-oils-enhances-non-rapid-eye-movement-sleep-in-mice-through-gabaa-benzodiazepine-receptors
#18
Hyejin Yang, Junsung Woo, Ae Nim Pae, Min Young Um, Nam-Chul Cho, Ki Duk Park, Minseok Yoon, Jiyoung Kim, C Justin Lee, Suengmok Cho
α-Pinene is a major monoterpene of the pine tree essential oils. It has been reported that α-pinene shows anxiolytic and hypnotic effects upon inhaled administration. However, hypnotic effect by oral supplementation and the molecular mechanism of α-pinene have not been determined yet. By combining in vivo sleep behavior, ex vivo electrophysiological recording from brain slices, and in silico molecular modeling, we demonstrate that (-)-α-pinene shows sleep enhancing property through a direct binding to GABAA-benzodiazepine (BZD) receptors by acting as a partial modulator at the BZD binding site...
November 2016: Molecular Pharmacology
https://www.readbyqxmd.com/read/27568889/flumazenil-for-the-treatment-of-refractory-hypersomnolence-clinical-experience-with-153-patients
#19
Lynn Marie Trotti, Prabhjyot Saini, Catherine Koola, Vincent LaBarbera, Donald L Bliwise, David B Rye
STUDY OBJECTIVES: Patients with central disorders of hypersomnolence sometimes do not achieve satisfactory symptom control with currently available wake-promoting medications. Based on the finding that the cerebrospinal fluid from some patients with hypersomnolence demonstrates potentiation of gamma-aminobutyric acid (GABA)-A receptors in excess of that of controls, a finding that reverses with flumazenil, we initiated prescribing compounded flumazenil to carefully selected, treatment-refractory hypersomnolent patients...
October 15, 2016: Journal of Clinical Sleep Medicine: JCSM: Official Publication of the American Academy of Sleep Medicine
https://www.readbyqxmd.com/read/27563433/anticonvulsant-effects-of-lippia-citriodora-verbenaceae-leaves-ethanolic-extract-in-mice-role-of-gabaergic-system
#20
Amir Rashidian, Forogh Farhang, Habib Vahedi, Ahmad Reza Dehpour, Shahram Ejtemai Mehr, Saeed Mehrzadi, Seyed Mahdi Rezayat
BACKGROUND: Lippia citriodora Kunth is one of the Iranian traditional medicines for the treatment of convulsive disorders. The goal of this study is to investigate the anticonvulsant activity of the plant's leave ethanolic extract against electro- and chemoconvulsant-induced seizures in mice. METHODS: The anticonvulsant activity of the extract (200, 400, 800 mg/kg, per os, p.o.) was investigated in pentylenetetrazole (PTZ) and maximal electroshock (MES)-induced seizures in mice...
2016: International Journal of Preventive Medicine
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