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https://www.readbyqxmd.com/read/28220535/interaction-of-approved-drugs-with-synaptic-vesicle-protein-2a
#1
Azeem Danish, Vigneshwaran Namasivayam, Anke C Schiedel, Christa E Müller
Levetiracetam (LEV) and its recently approved derivative brivaracetam are anti-epileptic drugs with a unique mechanism of action. The synaptic vesicle protein 2A (SV2A) was previously identified as their main target. In the current study, we tested a collection of 500 approved drugs for interaction with the human SV2A protein expressed in Chinese hamster ovary cells. Competition binding studies were performed using cell lysates with high SV2A expression and [(3) H]brivaracetam as a radioligand. A hit rate of 3% was obtained, defined as compounds that inhibited radioligand binding by more than 90% at a screening concentration of 20 μM...
February 21, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28212985/nonsteroidal-anti-inflammatory-drugs-in-clinical-and-experimental-epilepsy
#2
REVIEW
Beatrice Mihaela Radu, Florin Bogdan Epureanu, Mihai Radu, Paolo Francesco Fabene, Giuseppe Bertini
Current antiepileptic drugs have limited efficacy and provide little or no benefits in 30% of the patients. Given that a role for brain inflammation in epilepsy has been repeatedly reported in recent years, the potential of anti-inflammatory drugs should be explored in depth, as they may provide new therapeutical approaches in preventing or reducing epileptogenesis. Here, we review preclinical (both in vivo and in vitro) and clinical epilepsy studies in which nonsteroidal antiinflammatory drugs (NSAIDs), i...
February 9, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/28195061/overview-of-the-preclinical-pharmacological-properties-of-nigella-sativa-black-seeds-a-complementary-drug-with-historical-and-clinical-significance
#3
E Z Dajani, T G Shahwan, N E Dajani
Nigella sativa (N. sativa, black seeds; or sometimes known by many other names such as the blessed seed by the Arabs, black cumin in the Holy Bible, black caraway and Kalonji in South Asia) has been traditionally used for many years not only as a food but also as complementary drug. It is the objective of this communication to review the evidence-based pre-clinical pharmacological actions of N. sativa as a basis of its existing and potential new human clinical uses. Primary PubMed literature searches and secondary Medline searches were conducted to define N...
December 2016: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/28190698/therapeutic-effects-of-cannabinoids-in-animal-models-of-seizures-epilepsy-epileptogenesis-and-epilepsy-related-neuroprotection
#4
REVIEW
Evan C Rosenberg, Pabitra H Patra, Benjamin J Whalley
The isolation and identification of the discrete plant cannabinoids in marijuana revived interest in analyzing historical therapeutic claims made for cannabis in clinical case studies and anecdotes. In particular, sources as old as the 11th and 15th centuries claimed efficacy for crude marijuana extracts in the treatment of convulsive disorders, prompting a particularly active area of preclinical research into the therapeutic potential of plant cannabinoids in epilepsy. Since that time, a large body of literature has accumulated describing the effects of several of the >100 individual plant cannabinoids in preclinical models of seizures, epilepsy, epileptogenesis, and epilepsy-related neuroprotection...
February 9, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/28138994/megakaryocyte-expansion-and-macrophage-infiltration-in-bone-marrow-of-rats-subchronically-treated-with-mnx-n-nitroso-environmental-degradation-product-of-munitions-compound-rdx-hexahydro-1-3-5-trinitro-1-3-5-triazine
#5
Sindhura Ramasahayam, Sridhar Jaligama, Sahar M Atwa, Joshua T Salley, Marissa Thongdy, Benny L Blaylock, Sharon A Meyer
Hexahydro-1-nitroso-3,5-dinitro-1,3,5-triazine (MNX), environmental degradation product of munitions hexahydro-1,3,5-trinitro-1,3,5-triazine (RDX), causes seizures in rats with acute oral exposure like parent RDX. Our previous studies have additionally reported hematotoxicity with acute MNX exposure manifested as myelosuppression, anemia and splenic hemosiderosis. This study explored whether MNX administered subchronically continued to target bone marrow to elicit peripheral blood cytopenia. Female Sprague-Dawley rats were gavaged daily for 4 or 6 weeks with 47 mg kg(-1)  day(-1) MNX (¼ LD50 ) or vehicle (5% dimethyl sulfoxide in corn oil) and hematological and clinical chemistry parameters, spleen weights, spleen and bone marrow histopathology and immunohistochemistry with ED1 anti-CD68 macrophage marker were evaluated 24 h after the last dose...
January 31, 2017: Journal of Applied Toxicology: JAT
https://www.readbyqxmd.com/read/28131199/first-reported-cases-of-anti-nmda-receptor-encephalitis-in-vietnamese-adolescents-and-adults
#6
Mai Nguyen Thi Hoang, Phu Nguyen Hoan, Tan Le Van, Angela McBride, Nghia Ho Dang Trung, Thanh Tran Tan, Hong Nguyen Thi Thu, Dorothee Heemskerk, Jeremy Day, Angela Vincent, Chau Nguyen Van Vinh, Guy Thwaites
INTRODUCTION: Anti-NMDA receptor encephalitis is increasingly recognised as an important differential diagnosis in patients with encephalitis of unknown aetiology. We report the first case series of patients diagnosed in Vietnam. METHODS: Samples of CSF from patients with presumed encephalitis but negative microbiological investigations, who exhibited dyskinesia, autonomic instability or psychosis were tested for antibodies against the NR1 subunit of the glutamate (type-NMDA) receptor using an indirect immunofluorescence assay...
February 15, 2017: Journal of the Neurological Sciences
https://www.readbyqxmd.com/read/28087952/an-observational-study-of-trigeminal-neuralgia-patients-taking-carbamazepine-during-the-fasting-month-of-ramadan
#7
A J Ajura, S H Lau, S Nur Suffia
INTRODUCTION: Trigeminal neuralgia is an agonising orofacial pain affecting unilaterally the distribution of the trigeminal nerve and it usually occurs in the middle and older age groups. Carbamazepine which is an anti-neuralgic as well as an anti-convulsant medication is the first line drug for treatment of trigeminal neuralgia. It is commonly taken as one tablet (200 mg) three times a day. MATERIALS AND METHODS: This is an observational study carried out from April to September 2014 to determine how Muslim patients on carbamazepine treatment for trigeminal neuralgia cope with their neuralgic pain...
December 2016: Medical Journal of Malaysia
https://www.readbyqxmd.com/read/28026006/extended-eeg-and-non-convulsive-status-epilepticus-benefit-over-routine-eeg
#8
E Eskioglou, C Stähli, A O Rossetti, J Novy
OBJECTIVE: EEG monitoring is increasingly used in critically ill patients, but impact on clinical outcome remains unclear. We aimed to investigate the benefit of repeated extended EEG in the prognosis of patients with non-convulsive status epilepticus (SE). MATERIALS & METHODS: We retrospectively collected 29 consecutive patients with non-convulsive SE without coma, who underwent repeated extended EEG between 2013 and 2015. We compared these patients with an historical age-matched group of 58 patients managed between 2011 and 2013 with routine EEG only...
December 27, 2016: Acta Neurologica Scandinavica
https://www.readbyqxmd.com/read/27914529/agglutinin-isolated-from-arisema-heterophyllum-blume-induces-apoptosis-and-autophagy-in-a549-cells-through-inhibiting-pi3k-akt-pathway-and-inducing-er-stress
#9
Li-Xing Feng, Peng Sun, Tian Mi, Miao Liu, Wang Liu, Si Yao, Yi-Min Cao, Xiao-Lu Yu, Wan-Ying Wu, Bao-Hong Jiang, Min Yang, De-An Guo, Xuan Liu
Arisaema heterophyllum Blume is one of the three medicinal plants known as traditional Chinese medicine Rhizoma Arisaematis (RA). RA has been popularly used to treat patients with convulsions, inflammation, and cancer for a long time. However, the underlying mechanisms for RA effects are still unclear. The present study was designed to determine the cytotoxicity of agglutinin isolated from Arisema heterophyllum Blume (AHA) and explore the possible mechanisms in human non-small-cell lung cancer A549 cells. AHA with purity up to 95% was isolated and purified from Arisaema heterophyllum Blume using hydrophobic interaction chromatography...
November 2016: Chinese Journal of Natural Medicines
https://www.readbyqxmd.com/read/27907002/chemical-composition-an-antioxidant-cytotoxic-and-microbiological-activity-of-the-essential-oil-from-the-leaves-of-aeollanthus-suaveolens-mart-ex-spreng
#10
Rosany Lopes Martins, Ranggel Carvalho Simões, Érica de Menezes Rabelo, Ana Luzia Ferreira Farias, Alex Bruno Lobato Rodrigues, Ryan da Silva Ramos, João Batista Fernandes, Lourivaldo da Silva Santos, Sheylla Susan Moreira da Silva de Almeida
Aeollanthus suaveolens species popularly known as catinga de mulata belongs to the Lamiaceae family. In the Amazon region, it is used in folk medicine for the treatment of gastritis, convulsions of epileptic origin, stomach pain and diarrhea in the form of tea and juice. Essential oils have analgesic, anti-inflammatory, and antimicrobial activity. This study evaluated the chemical composition of the A. suaveolens essential oil, and its cytotoxic, antimicrobial and antioxidant activity on Artemia salina Leach...
2016: PloS One
https://www.readbyqxmd.com/read/27887842/simple-n-n-dimethyl-phenylsulfonamides-show-potent-anticonvulsant-effect-in-two-standard-epilepsy-models
#11
Tomoyuki Tanaka, Nana Yajima, Tomoko Kiyoshi, Yoshiki Miura, Seiji Iwama
Optimization of the previously reported benzothiazine analogue A led to the identification of compound 1, which showed anti-convulsant activity in two golden standard animal models of seizure, the MES and scPTZ models. Structure-activity relationship investigation of compound 1 revealed compounds 2, 6 and 19 as attractive anti-epileptic drug (AED) candidates with potent anticonvulsant effect in both the MES and scPTZ models. As these compounds are structurally different from existing AEDs, determination of their mechanism of actions could provide clues to understanding current therapy-resistant seizures...
January 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27882170/acute-encephalitis-with-refractory-repetitive-partial-seizures-a-case-report-and-literature-review
#12
Bin Zhang, Lin Wang
A male 46 year-old patient was admitted to the Emergency Intensive Care Unit of Qinghai Provincial People's Hospital (Xining, China) in December 2008 with complaints of a headache and fever that had lasted for three days. In addition, the patient had experienced two general convulsions accompanied with consciousness disorders for 7 h. Although the patient's clinical manifestations, laboratory tests and cerebrospinal fluid examinations were consistent with numerous features associated with acute encephalitis, the patient's clinical course was different to that of acute encephalitis, and the prognosis was poor...
November 2016: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/27875769/status-epilepticus-in-pregnant-women-with-epilepsy-after-valproate-adjustment-a-case-series
#13
Mengqian Wu, Nanya Hao, Bo Yan, Xiaosa Chi, Dong Zhou
PURPOSE: Valproate is an effective wide-spectrum anti-epileptic drug that is also known to be teratogenic. Its administration in epileptic women remains controversial. This report aims to draw more attention to valproate adjustment before and during pregnancy. METHODS: We collected medical records of pregnant women with epilepsy at West China Hospital in Chengdu, China who developed status epilepticus during pregnancy after valproate withdrawal or reduction in dose from January 2013 to July 2015...
December 2016: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/27855460/-diagnosis-and-current-therapy-of-vestibular-syndromes
#14
Michael Strupp, Thomas Brandt
Vertigo and dizziness are with an annual incidence of more than 10% and a lifetime prevalence of more than 30% among the most frequent symptoms. The keys to the diagnosis are the patient history and the bedside examination: a) for the patient history the time course, type and triggers of symptoms and accompanying symptoms, b) for the clinical examination of the vestibular system the head-impulse test (HIT), the examination for a spontaneous nystagmus, a displacement of subjective visual vertical, a positional nystagmus and the Romberg test, and c) for the differentiation between an acute peripheral and central vestibular lesion the skew deviation, central fixation nystagmus, gaze-evoked nystagmus, saccadic smooth pursuit and a normal HIT...
November 2016: Deutsche Medizinische Wochenschrift
https://www.readbyqxmd.com/read/27844311/phase-ii-study-of-medi-575-an-anti-platelet-derived-growth-factor-%C3%AE-antibody-in-patients-with-recurrent-glioblastoma
#15
Surasak Phuphanich, Jeffrey Raizer, Marc Chamberlain, Paola Canelos, Rajesh Narwal, Shengyan Hong, Robert Miday, Minal Nade, Kevin Laubscher
MEDI-575, an immunoglobulin G2κ monoclonal antibody, selectively binds to platelet-derived growth factor-α receptor (PDGFR-α) with high specificity. This multicenter, single-arm, open-label, phase II study evaluated the efficacy and safety of MEDI-575 in patients with recurrent glioblastoma. Adults with first recurrence of glioblastoma following surgery, temozolomide, and radiation received MEDI-575 25 mg/kg intravenously over 60 min every 21 days until disease progression or unacceptable toxicity. Six-month progression-free survival rate (PFS-6) was the primary end point; secondary measures included response rate, overall survival (OS), and safety/tolerability...
November 14, 2016: Journal of Neuro-oncology
https://www.readbyqxmd.com/read/27836728/altered-gene-expression-profile-in-a-mouse-model-of-scn8a-encephalopathy
#16
Ryan S Sprissler, Jacy L Wagnon, Rosie K Bunton-Stasyshyn, Miriam H Meisler, Michael F Hammer
SCN8A encephalopathy is a severe, early-onset epilepsy disorder resulting from de novo gain-of-function mutations in the voltage-gated sodium channel Nav1.6. To identify the effects of this disorder on mRNA expression, RNA-seq was performed on brain tissue from a knock-in mouse expressing the patient mutation p.Asn1768Asp (N1768D). RNA was isolated from forebrain, cerebellum, and brainstem both before and after seizure onset, and from age-matched wildtype littermates. Altered transcript profiles were observed only in forebrain and only after seizures...
February 2017: Experimental Neurology
https://www.readbyqxmd.com/read/27810155/2016-update-of-the-italian-pediatric-society-guidelines-for-management-of-fever-in-children
#17
Elena Chiappini, Elisabetta Venturini, Giulia Remaschi, Nicola Principi, Riccardo Longhi, Pier-Angelo Tovo, Paolo Becherucci, Francesca Bonsignori, Susanna Esposito, Filippo Festini, Luisa Galli, Bice Lucchesi, Alessandro Mugelli, Gian Luigi Marseglia, Maurizio de Martino
OBJECTIVE: To review new scientific evidence to update the Italian guidelines for managing fever in children as drafted by the panel of the Italian Pediatric Society. STUDY DESIGN: Relevant publications in English and Italian were identified through search of MEDLINE and the Cochrane Database of Systematic Reviews from May 2012 to November 2015. RESULTS: Previous recommendations are substantially reaffirmed. Antipyretics should be administered with the purpose to control the child's discomfort...
January 2017: Journal of Pediatrics
https://www.readbyqxmd.com/read/27783415/the-anti-convulsants-lacosamide-lamotrigine-and-rufinamide-reduce-myotonia-in-isolated-human-and-rat-skeletal-muscle
#18
Martin Skov, Frank V de Paoli, Ole B Nielsen, Thomas H Pedersen
INTRODUCTION: In myotonia congenita, loss of ClC-1 Cl(-) -channel function results in skeletal muscle hyperexcitability and myotonia. Anti-myotonic treatment has typically targeted the voltage gated sodium channel in skeletal muscle (Nav1.4). This study explored whether 3 sodium channel modulating anti-epileptics can reduce myotonia in isolated rat and human muscle. METHODS: Dissected muscles were rendered myotonic by ClC-1 channel inhibition. The ability of the drugs to suppress myotonia was then assessed from sub-clinical to maximal clinical concentrations...
October 26, 2016: Muscle & Nerve
https://www.readbyqxmd.com/read/27779658/ethanol-extract-of-baked-gardeniae-fructus-exhibits-in-vitro-and-in-vivo-anti-metastatic-and-anti-angiogenic-activities-in-malignant-cancer-cells-role-of-suppression-of-the-nf-%C3%AE%C2%BAb-and-hif-1%C3%AE-pathways
#19
Minju Im, Aeyung Kim, Jin Yeul Ma
Gardeniae Fructus (GF, Zhi Zi in China), a fruit of Gardenia jasminoides Ellis, has been used in traditional medicine to reduce inflammation and headache and to treat hepatic disorders, hypertension, and icterus. In recent studies, extract of raw or stir-baked GF was shown to have pharmacological activities for viral infection, thrombosis, hyperlipidemia, convulsion, inflammation, oxidative stress, and others. In addition, baked GF extract suppressed the proteolytic activities and altered the cellular morphology of tumor cells...
December 2016: International Journal of Oncology
https://www.readbyqxmd.com/read/27779081/calixarene-a-versatile-material-for-drug-design-and-applications
#20
Muhammad Ajaz Hussain, Muhammad Umer Ashraf, Gulzar Muhammad, Muhammad Nawaz Tahir, Syed Nasir Abbas Bukhari
The review summarizes the efforts to fabricate inclusion complexes of different therapeutic agents based on a versatile material . is a macrocyclic nano-basket which is the marvelous host with distinct hydrophobic three dimensional cavities to entrap and encapsulate biologically active guest drugs. and its derivatives are used as carriers (host-guest) for anti-cancer, anti-convulsant, anti-hypertensive, anthelmentic, anti-inflammatory, antimicrobial and anti-psychotic drugs, etc. They are the important biocompatible materials to improve solubility and chemical reactivity, and decrease cytotoxicity of poorly soluble drugs...
September 28, 2016: Current Pharmaceutical Design
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