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https://www.readbyqxmd.com/read/29778948/bioisosteres-of-ethyl-8-ethynyl-6-pyridin-2-yl-4h-benzo-f-imidazo-1-5-a-1-4-diazepine-3-carboxylate-hz-166-as-novel-alpha-2-3-selective-potentiators-of-gaba-a-receptors-improved-bioavailability-enhances-anticonvulsant-efficacy
#1
J M Witkin, J L Smith, X Ping, S D Gleason, M M Poe, G Li, X Jin, J Hobbs, J M Schkeryantz, J S McDermott, A I Alatorre, J N Siemian, J W Cramer, D C Airey, K R Methuku, V V N P B Tiruveedhula, T M Jones, J Crawford, M J Krambis, J L Fisher, J M Cook, R Cerne
HZ-166 has previously been characterized as an α2,3-selective GABAA receptor modulator with anticonvulsant, anxiolytic, and anti-nociceptive properties but reduced motor effects. We discovered a series of ester bioisosteres with reduced metabolic liabilities, leading to improved efficacy as anxiolytic-like compounds in rats. In the present study, we evaluated the anticonvulsant effects KRM-II-81 across several rodent models. In some models we also evaluated key structural analogs. KRM-II-81 suppressed hyper-excitation in a network of cultured cortical neurons without affecting the basal neuronal activity...
May 3, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29774194/improper-use-of-thrombolytic-agents-in-acute-hemiparesis-following-misdiagnosis-of-acute-ischemic-stroke
#2
Min Chan Kim, Seok Won Kim
Objective: Acute hemiparesis is often an early presentation of acute ischemic stroke, though it can occur in various disorders. This study aimed to investigate the improper use of thrombolytic agents for patients with acute hemiparesis, following the misdiagnosis of acute ischemic stroke. Methods: We analyzed the clinical and radiological data of nine patients initially misdiagnosed with cerebral stroke in the emergency room from May 2013 to January 2017. All the patients were treated with tissue plasminogen activator (TPA) owing to the presence of acute hemiparesis...
April 2018: Korean Journal of Neurotrauma
https://www.readbyqxmd.com/read/29769490/comparison-of-outcome-of-eclamptic-patient-following-vaginal-delivery-versus-caeserian-delivery-by-spinal-anaesthesia
#3
M A Hossain, R K Karmoker, M S Rahman, H O Rashid, S H Khan, M A Rahman
Eclampsia is a common problem in pregnancy in Bangladesh. It is a severe form of preeclampsia which affects 5 to 7% of pregnancies is a significant cause of maternal & neonatal morbidity & mortality. Pre-eclampsia when complicated with generalized tonic-clonic convulsions and/or coma is called eclampsia. The term eclampsia is derived from a Greek word, meaning "like a flash of lightening". It may occur quite abruptly, without any warning manifestations. Eclampsia is a major cause of maternal mortality & morbidity as well as foetal loss worldwide, particularly in the third world...
April 2018: Mymensingh Medical Journal: MMJ
https://www.readbyqxmd.com/read/29765983/a-clinical-study-of-toxication-caused-by-carbamazepine-abuse-in-adolescents
#4
Wei Xu, Yu-Lin Chen, Ying Zhao, Li-Jie Wang, Jiu-Jun Li, Chun-Feng Liu
Carbamazepine is known to produce the side effect of euphoria. As such, it lends itself to being a drug of abuse, particularly in the adolescent population. This retrospective study evaluated carbamazepine abuse, treatment course, and associated morbidity in Chinese adolescents. The median dose of carbamazepine resulting in overdose was 2,000 mg (800-5,000). Patients were largely from urban-rural fringe areas (76.47%, 52.94%) with school performance within the last 1/3 range and (52.94%) unsupervised by parents...
2018: BioMed Research International
https://www.readbyqxmd.com/read/29759061/role-of-ultrasound-guided-transversus-abdominis-plane-block-as-a-component-of-multimodal-analgesic-regimen-for-lower-segment-caesarean-section-a-randomized-double-blind-clinical-study
#5
Ashok Jadon, Priyanka Jain, Swastika Chakraborty, Mayur Motaka, Sudhansu Sekhar Parida, Neelam Sinha, Amit Agrawal, Asit Kumar Pati
BACKGROUND: While opioids are the mainstay for post-operative analgesia after lower segment caesarean section, they are associated with various untoward effects. Ultrasound guided transversus abdominis plane (TAP) block has been postulated to provide effective analgesia for caesarean section. We evaluated the analgesic efficacy of this block for post caesarean analgesia in a randomised controlled trial. METHODS: One hundred thirty-nine mothers undergoing caesarean delivery were randomised to receive TAP block with either 20 ml 0...
May 14, 2018: BMC Anesthesiology
https://www.readbyqxmd.com/read/29757890/pediatric-carbon-monoxide-poisoning-in-southern-israel-a-cross-sectional-study
#6
Yariv Fruchtman, Zvi H Perry, Tom Leibson, Liat Vered Cohen, Matitiahu Lifshitz, Eugene Leibovitz
OBJECTIVES: This study aimed to describe the epidemiology and clinical burden of unintended carbon monoxide (CO) poisoning among children in the Negev region of southern Israel. METHODS: This was a cross-sectional retrospective study of CO poisoning patients admitted to Soroka University Medical Center in 2011 through 2015. RESULTS: Overall, 43 cases of CO poisoning were recorded among children younger than 18 years. Five patients died, all upon admission...
May 2, 2018: Pediatric Emergency Care
https://www.readbyqxmd.com/read/29756710/mefv-gene-mutations-and-clinical-course-in-pediatric-patients-with-henoch-sch%C3%A3-nlein-purpura
#7
Emrah Can, Zubeyde Kılınç Yaprak, Şahin Hamilçıkan, Meltem Erol, Özlem Bostan Gayret Y Özgül Yiğit
OBJECTIVE: To determine the frequency of the MEFV gene mutations in pediatric patients diagnosed with HSP and to assess the effect of the MEFV gene mutations on their prognosis. Material and Methods. Ccross-sectional study; pediatric patients between 2-11 years diagnosed with HSP were included. These cases were investigated for 6 MEFV gene mutations (M694V, M680I, A744S, R202Q, K695R, E148Q). RESULTS: Eighty cases were included in the study of which 55% were male (n= 44)...
June 1, 2018: Archivos Argentinos de Pediatría
https://www.readbyqxmd.com/read/29751085/a-predictive-index-of-biomarkers-for-ictogenesis-from-tier-i-safety-pharmacology-testing-that-may-warrant-tier-ii-eeg-studies
#8
REVIEW
David V Gauvin, Zachary J Zimmermann, Joshua Yoder, Marci Harter, David Holdsworth, Quinn Kilgus, Jonelle May, Jill Dalton, Theodore J Baird
Three significant contributions to the field of safety pharmacology were recently published detailing the use of electroencephalography (EEG) by telemetry in a critical role in the successful evaluation of a compound during drug development (1] Authier, Delatte, Kallman, Stevens & Markgraf; JPTM 2016; 81:274-285; 2] Accardi, Pugsley, Forster, Troncy, Huang & Authier; JPTM; 81: 47-59; 3] Bassett, Troncy, Pouliot, Paquette, Ascaha, & Authier; JPTM 2016; 70: 230-240) . These authors present a convincing case for monitoring neocortical biopotential waveforms (EEG, ECoG, etc) during preclinical toxicology studies as an opportunity for early identification of a central nervous system (CNS) risk during Investigational New Drug (IND) Enabling Studies...
May 8, 2018: Journal of Pharmacological and Toxicological Methods
https://www.readbyqxmd.com/read/29747021/adaptive-nocturnal-seizure-detection-using-heart-rate-and-low-complexity-novelty-detection
#9
Thomas De Cooman, Carolina Varon, Anouk Van de Vel, Katrien Jansen, Berten Ceulemans, Lieven Lagae, Sabine Van Huffel
PURPOSE: Automated seizure detection at home is mostly done using either patient-independent algorithms or manually personalized algorithms. Patient-independent algorithms, however, lead to too many false alarms, whereas the manually personalized algorithms typically require manual input from an experienced clinician for each patient, which is a costly and unscalable procedure and it can only be applied when the patient had a sufficient amount of seizures. We therefore propose a nocturnal heart rate based seizure detection algorithm that automatically adapts to the patient without requiring seizure labels...
April 26, 2018: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/29744265/convulsive-syncope-on-electroencephalogram
#10
Manabu Izumi, Taro Okabe, Masayoshi Komura, Yasushi Hayashi
No abstract text is available yet for this article.
May 2018: Journal of General and Family Medicine
https://www.readbyqxmd.com/read/29742585/cardiac-arrest-in-patients-managed-for-convulsive-status-epilepticus-characteristics-predictors-and-outcome
#11
Stephane Legriel, Edouard Bresson, Nicolas Deye, David Grimaldi, Bertrand Sauneuf, Olivier Lesieur, Jean-Baptiste Lascarrou, Laurent Argaud, Jonathan Chelly, Pascal Beuret, David Schnell, Anne-Laure Chateauneuf, Mathilde Holleville, François Perier, Virginie Lemiale, Cedric Bruel, Pierrick Cronier, Nicolas Pichon, Nicolas Mongardon, Nicolas de-Prost, Florence Dumas, Alain Cariou
OBJECTIVES: Cardiac arrest is a catastrophic event that may arise during the management of convulsive status epilepticus. We aimed to report the clinical characteristics, outcomes, and early predictors of convulsive status epilepticus-related cardiac arrest. DESIGN: Retrospective multicenter study. SETTING: Seventeen university or university affiliated participating ICUs in France and Belgium. PATIENTS: Consecutive patients admitted to the participating ICUs for management of successfully resuscitated out-of-hospital cardiac arrest complicating the initial management of convulsive status epilepticus between 2000 and 2015...
May 8, 2018: Critical Care Medicine
https://www.readbyqxmd.com/read/29739085/cerebral-venous-sinus-thrombosis-with-cerebral-hemorrhage-presenting-with-status-epilepticus-in-early-pregnancy
#12
Xuemin Feng, Teng Zhao, Jingyao Liu, Chunkui Zhou
BACKGROUND: CVST is an important cause of stroke during late pregnancy and in the puerperium, but it is seldom encountered during early pregnancy. We report a case of a 34-year-old woman presenting with convulsive status epilepticus in early pregnancy. METHODS: In this case, the cranial computed tomography detected hemorrhage. Magnetic resonance imaging revealed a bilateral hypointense signal involving the frontal lobes and a hyperintense lesion on the right temporal lobe on T1-weighted imaging, and a large bilateral hyperintense area involving the frontal lobes on T2-weighted and fluid-attenuated inversion recovery imaging...
April 1, 2018: Clinical Laboratory
https://www.readbyqxmd.com/read/29735419/characteristics-of-ictal-eeg-in-magnetic-seizure-therapy-at-various-stimulation-frequencies
#13
Felicity A Backhouse, Yoshihiro Noda, Yuliya Knyahnytska, Faranak Farzan, Jonathan Downar, Tarek K Rajji, Benoit H Mulsant, Zafiris J Daskalakis, Daniel M Blumberger
OBJECTIVES: The first objective of this study aimed to elucidate the relationship between seizure characteristics and Magnetic Seizure Therapy (MST) treatment outcome. The second objective was to determine the effect of stimulation frequency on seizure characteristics. METHODS: Using a between-subjects design, we compared the seizures of patients with unipolar depression receiving MST at three separate stimulation frequencies: 25 Hz (n = 34), 50 Hz (n = 16) and 100 Hz (n = 11)...
April 22, 2018: Clinical Neurophysiology: Official Journal of the International Federation of Clinical Neurophysiology
https://www.readbyqxmd.com/read/29729290/anticonvulsant-evaluation-of-novel-non-imidazole-histamine-h-3-r-antagonists-in-different-convulsion-models-in-rats
#14
Alaa Alachkar, Gniewomir Latacz, Agata Siwek, Annamaria Lubelska, Ewelina Honkisz, Anna Gryboś, Dorota Łażewska, Jadwiga Handzlik, Holger Stark, Katarzyna Kiec-Kononowicz, Bassem Sadek
Novel non-imidazole histamine H3 receptor (H3R) antagonists (2-8) were developed and assessed for in-vitro antagonist binding affinities at the human histamine H1-H4R. These novel H3R antagonists (2-8) were examined in-vivo for anticonvulsant effects in three different convulsion models in male adult rats. Compound 6 significantly and dose-dependently exhibited decreased duration of tonic hind limb extension (THLE) in the maximal electroshock (MES)- and fully protected animals against pentylenetetrazole (PTZ)-induced convulsion, following acute systemic administration (5, 10, and 20 mg/kg, i...
May 2, 2018: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29727818/efficacy-and-safety-of-ketogenic-diet-for-treatment-of-pediatric-convulsive-refractory-status-epilepticus
#15
Ravindra Arya, Katrina Peariso, Marina Gaínza-Lein, Jessica Harvey, Ann Bergin, J Nicholas Brenton, Brian T Burrows, Tracy Glauser, Howard P Goodkin, Yi-Chen Lai, Mohamad A Mikati, Iván Sánchez Fernández, Dmitry Tchapyjnikov, Angus A Wilfong, Korwyn Williams, Tobias Loddenkemper
PURPOSE: To describe the efficacy and safety of ketogenic diet (KD) for convulsive refractory status epilepticus (RSE). METHODS: RSE patients treated with KD at the 6/11 participating institutions of the pediatric Status Epilepticus Research Group from January-2011 to December-2016 were included. Patients receiving KD prior to the index RSE episode were excluded. RSE was defined as failure of ≥2 anti-seizure medications, including at least one non-benzodiazepine drug...
April 27, 2018: Epilepsy Research
https://www.readbyqxmd.com/read/29727742/cytokine-levels-in-febrile-seizure-patients-a-systematic-review-and-meta-analysis
#16
Aram Kwon, Byung Ok Kwak, Kyungmin Kim, Jongseok Ha, Soo-Jin Kim, Sun Hwan Bae, Jae Sung Son, Soo-Nyung Kim, Ran Lee
PURPOSE: Febrile seizures (FSs) are the most common form of childhood seizures. During infection, both pro-inflammatory and anti-inflammatory cytokines are produced. Complex interactions among immune-inflammatory process, cytokine activation, and genetic factors are involved in the pathogenesis of FSs. The association between cytokines and FSs during childhood is inconclusive due to inconsistent results reported in different studies. We performed a systematic review and meta-analysis to determine an association between cytokines and FS in children...
April 27, 2018: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/29725823/esophageal-perforation-caused-by-a-thoracic-pedicle-screw
#17
REVIEW
Stanislas Marouby, Clément Jeandel, Djamel Louahem M'Sabah, Marion Delpont, Jérôme Cottalorda
This grand round raises the risk of a rare complication that can be avoided with the knowledge of the particular anatomy of scoliosis vertebra. Transpedicular screws have been reported to enhance the operative correction in scoliosis surgery. The narrow and inconsistent shape of the thoracic pedicles makes the placement of pedicle screws technically challenging. Furthermore, in thoracic curves, the close proximity of the spinal cord and major soft tissue structures also adds a greater risk to the procedure...
May 3, 2018: European Spine Journal
https://www.readbyqxmd.com/read/29725569/nontraumatic-acetabular-fracture-sustained-during-convulsive-seizure-following-surgery-for-an-unruptured-intracranial-aneurysm-a-case-report
#18
Hirofumi Iwamoto, Kazuhiro Nakamura, Daisuke Watanabe, Kiyoyuki Yanaka, Takeshi Ainoya, Tetsuya Yamamoto
Acetabular fracture usually is related to high-energy traumatic injury or falls from heights and directly caused by seizures without trauma is extremely rare. We report a 71-years-old man who sustained a left acetabular fracture secondary to generalized seizure after clipping of an unruptured aneurysm without trauma and any risk for fracture. The patient had an aneurysm was arising from the bifurcation of the left internal carotid artery and the posterior communicating artery. After the clipping, the patient had three times tonic-clonic seizures for 1 min and resulted in an acetabular fracture...
April 2018: NMC Case Report Journal
https://www.readbyqxmd.com/read/29724056/essential-oils-and-their-constituents-targeting-the-gabaergic-system-and-sodium-channels-as-treatment-of-neurological-diseases
#19
REVIEW
Ze-Jun Wang, Thomas Heinbockel
Essential oils and the constituents in them exhibit different pharmacological activities, such as antinociceptive, anxiolytic-like, and anticonvulsant effects. They are widely applied as a complementary therapy for people with anxiety, insomnia, convulsion, pain, and cognitive deficit symptoms through inhalation, oral administration, and aromatherapy. Recent studies show that essential oils are emerging as a promising source for modulation of the GABAergic system and sodium ion channels. This review summarizes the recent findings regarding the pharmacological properties of essential oils and compounds from the oils and the mechanisms underlying their effects...
May 2, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29722902/tolerance-to-high-internalizing-delta-opioid-receptor-agonist-is-critically-mediated-by-arrestin-2
#20
Ana Vicente-Sanchez, Isaac J Dripps, Alycia F Tipton, Heba Akbari, Areeb Akbari, Emily M Jutkiewicz, Amynah A Pradhan
BACKGROUND AND PURPOSE: Delta opioid receptor (δOR) agonists are potent antihyperalgesics in chronic pain models, but tolerance develops after prolonged use. Previous evidence indicates that distinct forms of tolerance occur depending on the internalization properties of δOR agonists. Due to the importance of arrestins in receptor internalization, we investigated the role of arrestin 2 (β-arrestin 1) in mediating the development of tolerance induced by high- and low-internalizing δOR agonists...
May 3, 2018: British Journal of Pharmacology
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