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Anticonvulsants, anti-epileptics

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https://www.readbyqxmd.com/read/28088732/apelin-13-protects-rat-primary-cortical-glia-neuron-co-culture-against-pentylenetetrazole-induced-toxicity
#1
Taj Pari Kalantaripour, Saeed Esmaeili-Mahani, Vahid Sheibani, Hamid Najafipour, Majid Asadi-Shekaari M
In spite of recent advances in the treatment of epilepsy, up to 35% of people living with the condition do not respond to accessible anti-epileptic drugs (AEDs) and continue to experience regular, devastating and potentially life-threatening seizures. Neuronal death is a significant feature of epilepsy in humans and experimental models. It has been reported that apelin, an endogenous ligand for the angiotensin-1-like receptor (APJ), has anticonvulsive as well as protective effects in some neurodegenerative situations...
March 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27915186/role-of-the-purinergic-signaling-in-epilepsy
#2
REVIEW
Marek Cieślak, Andrzej Wojtczak, Michał Komoszyński
Adenine nucleotides and adenosine are signaling molecules that activate purinergic receptors P1 and P2. Activation of A1 adenosine receptors has an anticonvulsant action, whereas activation of A2A receptors might initiate seizures. Therefore, a significant limitation to the use of A1 receptor agonists as drugs in the CNS might be their peripheral side effects. The anti-epileptic activity of adenosine is related to its increased concentration outside the cell. This increase might result from the inhibition of the equilibrative nucleoside transporters (ENTs)...
February 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27887842/simple-n-n-dimethyl-phenylsulfonamides-show-potent-anticonvulsant-effect-in-two-standard-epilepsy-models
#3
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/27860117/development-of-a-core-outcome-set-for-epilepsy-in-pregnancy-e-core-a-national-multi-stakeholder-modified-delphi-consensus-study
#4
B H Al Wattar, K Tamilselvan, R Khan, A Kelso, A Sinha, A M Pirie, D McCorry, K S Khan, S Thangaratinam
OBJECTIVE: To develop a set of core outcomes for studies on pregnant women with epilepsy. DESIGN: Delphi consensus study. POPULATION: Healthcare professionals, and patient representatives with lived experience of epilepsy in the UK. METHODS: We used a modified Delphi method and a consultation meeting to achieve consensus. Potential outcomes were identified by systematic review, and were scored using a Likert scale anchored between 1 (least important) and 5 (most important)...
November 16, 2016: BJOG: An International Journal of Obstetrics and Gynaecology
https://www.readbyqxmd.com/read/27825017/a-pharmacological-overview-of-lamotrigine-for-the-treatment-of-epilepsy
#5
Venkata Ramesh Yasam, Satya Lavanya Jakki, V Senthil, M Eswaramoorthy, S Shanmuganathan, K Arjunan, M J Nanjan
Epilepsy is one of the most common neurological disorders, affecting about 2% of the population worldwide. Lamotrigine (LTG) is a second generation anti-epileptic drug (AED) with broad spectrum of activity, a favourable side-effect profile, simpler dosing than earlier drugs and efficacious in diverse epilepsy syndromes. Areas covered: The present review focuses on pharmacodynamics, pharmacokinetics, clinical efficacy, safety and tolerability of LTG and its effect on cognition, psychiatry, quality of life, women and pregnancy along with effect of enzyme inducing and enzyme inhibiting drugs over LTG and their effect on serum level fluctuations by collecting data from various studies over the years until 2016...
December 2016: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/27757273/evaluation-of-anti-epileptic-activity-of-leaf-extracts-of-punica-granatum-on-experimental-models-of-epilepsy-in-mice
#6
Gollapalle L Viswanatha, Marikunte V Venkataranganna, Nunna Bheema Lingeswara Prasad, Godavarthi Ashok
OBJECTIVES: This study was aimed to examine the anti-epileptic activity of leaf extracts of Punica granatum in experimental models of epilepsy in Swiss albino mice. MATERIALS AND METHODS: Petroleum ether leaf extract of P. granatum (PLPG), methanolic LPG (MLPG), and aqueous LPG (ALPG) extracts of P. granatum leaves was initially evaluated against 6-Hz-induced seizure model; the potent extract was further evaluated against maximal electroshock (MES) and pentylenetetrazole (PTZ)-induced convulsions...
September 2016: Journal of Intercultural Ethnopharmacology
https://www.readbyqxmd.com/read/27566615/study-of-the-anti-seizure-effects-of-low-frequency-stimulation-following-kindling-a-review-of-the-cellular-mechanism-related-to-the-anti-seizure-effects-of-low-frequency-electrical-stimulation
#7
REVIEW
Zohreh Ghotbeddin, Mahyar Janahmadi, Ali Yadollahpour
Epilepsy affects about 1-2 % of world population as a chronic neurological disease that is manifested by repeated and consecutive seizures (Grone and Baraban, Nat Neurosci 18(3):339-343, 2015). There is no definitive therapy for epilepsy and antiepileptic drugs cannot offer a permanent and definitive cure for epilepsy, and most epileptic patients become drug resistant (Sasa, J Pharmacol Sci 100(5):487-494, 2006). Surgery and removal of the epileptic focus is a substitute method for treating drug-resistant patients and epilepsy surgery of either side of the brain improves seizure control...
January 2017: Neurological Sciences
https://www.readbyqxmd.com/read/27566463/recovery-from-a-possible-cytomegalovirus-meningoencephalitis-induced-apparent-brain-stem-death-in-an-immunocompetent-man-a-case-report
#8
Theresia Monica Rahardjo, Tinni Trihartini Maskoen, Ike Sri Redjeki
BACKGROUND: Recovery from cytomegalovirus meningoencephalitis with brain stem death in an immunocompetent patient is almost impossible. We present a remarkable recovery from a possible cytomegalovirus infection in an immunocompetent man who had severe neurological syndromes, suggesting brain stem death complicated by pneumonia and pleural effusion. CASE PRESENTATION: A 19-year-old Asian man presented at our hospital's emergency department with reduced consciousness and seizures following high fever, headache, confusion, and vomitus within a week before arrival...
August 26, 2016: Journal of Medical Case Reports
https://www.readbyqxmd.com/read/27531652/the-implantation-effect-delay-in-seizure-occurrence-with-implantation-of-intracranial-electrodes
#9
M A Lane, C A Kahlenberg, Z Li, K Kulandaival, K L Secore, V M Thadani, K A Bujarski, E J Kobylarz, D W Roberts, T D Tosteson, B C Jobst
OBJECTIVE: A transient decrease in seizure frequency has been identified during therapeutic brain stimulation trials with stimulator in patients in the inactive sham group. This study was performed to examine whether the implantation of intracranial electrodes decreases seizure occurrence and explores factors that may be associated. METHODS: A retrospective review of 193 patients was performed, all evaluated with both scalp video EEG monitoring and intracranial EEG (iEEG) monitoring...
January 2017: Acta Neurologica Scandinavica
https://www.readbyqxmd.com/read/27522536/the-effect-of-leptin-ghrelin-and-neuropeptide-y-on-serum-tnf-%C3%AE-il-1%C3%AE-il-6-fgf-2-galanin-levels-and-oxidative-stress-in-an-experimental-generalized-convulsive-seizure-model
#10
Berrin Oztas, Deniz Sahin, Hale Kir, Fatma Ceyla Eraldemir, Mert Musul, Sevinç Kuskay, Nurbay Ates
The objective of this study is to examine the effects of the endogenous ligands leptin, ghrelin, and neuropeptide Y (NPY) on seizure generation, the oxidant/antioxidant balance, and cytokine levels, which are a result of immune response in a convulsive seizure model. With this goal, Wistar rats were divided into 5 groups-Group 1: Saline, Group 2: Saline+PTZ (65mg/kg), Group 3: leptin (4mg/kg)+PTZ, Group 4: ghrelin (80μg/kg)+PTZ, and Group 5: NPY (60μg/kg)+PTZ. All injections were delivered intraperitoneally, and simultaneous electroencephalography (EEG) records were obtained...
February 2017: Neuropeptides
https://www.readbyqxmd.com/read/27415827/very-long-term-outcome-of-non-surgically-treated-patients-with-temporal-lobe-epilepsy-with-hippocampal-sclerosis-a-retrospective-study
#11
Tsugiko Kurita, Kotaro Sakurai, Youji Takeda, Toru Horinouchi, Ichiro Kusumi
OBJECTIVE: Surgical intervention can result in complete seizure remission rates of up to 80% in patients with temporal lobe epilepsy with hippocampal sclerosis (TLE-HS). However, certain patients cannot be treated surgically for various reasons. We analyzed the very long-term clinical outcomes of patients with TLE-HS who could not be treated surgically. METHODS: Subjects were selected from among patients with TLE-HS who were actively followed up for >10 years and treated with medication without surgical treatment...
2016: PloS One
https://www.readbyqxmd.com/read/27267376/aberrant-epilepsy-associated-mutant-nav1-6-sodium-channel-activity-can-be-targeted-with-cannabidiol
#12
Reesha R Patel, Cindy Barbosa, Tatiana Brustovetsky, Nickolay Brustovetsky, Theodore R Cummins
Mutations in brain isoforms of voltage-gated sodium channels have been identified in patients with distinct epileptic phenotypes. Clinically, these patients often do not respond well to classic anti-epileptics and many remain refractory to treatment. Exogenous as well as endogenous cannabinoids have been shown to target voltage-gated sodium channels and cannabidiol has recently received attention for its potential efficacy in the treatment of childhood epilepsies. In this study, we further investigated the ability of cannabinoids to modulate sodium currents from wild-type and epilepsy-associated mutant voltage-gated sodium channels...
August 2016: Brain: a Journal of Neurology
https://www.readbyqxmd.com/read/27261619/neuroinformatics-analyses-reveal-gabat-and-ssadh-as-major-proteins-involved-in-anticonvulsant-activity-of-valproic-acid
#13
Sakshi Piplani, Prabhakar Kumar Verma, Ajit Kumar
The unequivocal hypotheses about anticonvulsant activity of valproic acid (VPA) have always been a basic hurdle in designing next generation neurotherapeutics, particularly the anti-epileptic drugs. The present study reports about a comprehensive in-silico investigation into qualitative and quantitative binding of VPA and corresponding natural ligands of four major enzymes involved in neurotransmissions, namely-GABA transaminase (GABAt), α-keto glutarate dehydrogenase (α-KGDH), Succinate Semialdehyde dehydrogenase (SSADH) and Glutamate Decarboxylase (GAD), respectively...
July 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27261605/saikosaponin-a-functions-as-anti-epileptic-effect-in-pentylenetetrazol-induced-rats-through-inhibiting-mtor-signaling-pathway
#14
Ming Ye, Yong-Feng Bi, Li Ding, Wei-Wei Zhu, Wei Gao
OBJECTIVE: Saikosaponin a (SSa), which is one major bioactive compound isolated from radix bupleuri, has been demonstrated to exhibit the properties of anticonvulsant and antiepileptic in few reports. This study aims to clarify the molecular mechanism by which SSa protects against pentylenetetrazol (PTZ) induced epileptic seizure. METHODS: PTZ induced rat and hippocampal neuron were established. Treated rats or hippocampal neuron with SSa, and mTOR, P70S6K, IL-1β and TNF-α were then determined...
July 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27207115/pharmacological-treatment-of-pain-in-cancer-patients-the-role-of-adjuvant-analgesics-a-systematic-review
#15
Marieke H J van den Beuken-van Everdingen, Alexander de Graeff, Joost L M Jongen, Denise Dijkstra, Irina Mostovaya, Kris C Vissers
CONTEXT: In patients with cancer, pain is one of the most feared and burdensome symptoms. Adjuvant analgesics are an important cornerstone on which treatment of pain in patients with cancer is based. OBJECTIVES: To update our guidelines for the treatment of pain in patients with cancer, we performed a systematic review on the use of adjuvant analgesics in pain in cancer. METHODS: A systematic search of the literature was performed searching for articles that studied the effect of (1) antidepressants, (2) anti-epileptics, (3) N-methyl-d-aspartate (NMDA) receptor antagonists, and (4) other adjuvant analgesics in patients with cancer pain and described their effects on pain intensity and/or side effects...
May 21, 2016: Pain Practice: the Official Journal of World Institute of Pain
https://www.readbyqxmd.com/read/26916017/polypharmacological-drugs-in-the-treatment-of-epilepsy-the-comprehensive-review-of-marketed-and-new-emerging-molecules
#16
Shikha Kumari, Chandra Bhushan Mishra, Manisha Tiwari
Epilepsy is a complex neurological disorder which has plagued the human population through the ages and continues to affect about 50 million people worldwide. A better understanding of the pathogenesis of epilepsy unmasks various molecular targets for the treatment of epilepsy. The currently used antiepileptic drugs (AEDs) predominately target voltage-gated ion channels (Na+, Ca2+ and K+), GABAA receptor, glutamate receptor, synaptic vesicle 2A (SV2A) protein and carbonic anhydrase (CA). One group of AEDs acts on a single target while another group acts via multiple targets to control seizure episodes...
2016: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/26627826/the-sensorless-pore-module-of-voltage-gated-k-channel-family-7-embodies-the-target-site-for-the-anticonvulsant-retigabine
#17
Ruhma Syeda, Jose S Santos, Mauricio Montal
KCNQ (voltage-gated K(+) channel family 7 (Kv7)) channels control cellular excitability and underlie the K(+) current sensitive to muscarinic receptor signaling (the M current) in sympathetic neurons. Here we show that the novel anti-epileptic drug retigabine (RTG) modulates channel function of pore-only modules (PMs) of the human Kv7.2 and Kv7.3 homomeric channels and of Kv7.2/3 heteromeric channels by prolonging the residence time in the open state. In addition, the Kv7 channel PMs are shown to recapitulate the single-channel permeation and pharmacological specificity characteristics of the corresponding full-length proteins in their native cellular context...
February 5, 2016: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/26364945/discovery-of-benzothiazine-derivatives-as-novel-orally-active-anti-epileptic-drug-candidates-with-broad-anticonvulsant-effect
#18
Tomoyuki Tanaka, Nana Yajima, Akihiko Tanitame, Tomoko Kiyoshi, Yoshiki Miura
In order to develop novel anti-epileptic drugs that are effective for both general and partial seizure, we conducted in vivo screening of our chemical library in the mice MES and sc-PTZ models and found the benzothiazine 1 as lead compound. Optimization of this compound led to the discovery of compound 7b, which showed potent anticonvulsant effect in the MES, scPTZ and rat amygdala kindling models. Since the chemical structure of 7b is different from that of any existing AED, it is suggested that 7b may have unique mechanism of action for relieving both partial and generalized epilepsy...
October 15, 2015: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/26216049/a-cox-5-lox-inhibitor-licofelone-revealed-anticonvulsant-properties-through-inos-diminution-in-mice
#19
Borna Payandemehr, Mahsima Khoshneviszadeh, Bardia Varastehmoradi, Ramtin Gholizadeh, Taraneh Bahremand, Hossein Attar, Arash Bahremand, Ahmad Reza Dehpour
Licofelone is a COX/5-LOX inhibitor, which recently was approved as an effective treatment for osteoarthritis. Beside its analgesic and anti-inflammatory effects, some reports show neuro-protective properties for this agent in central nervous system. Several lines of evidence declare the involvement of COX or LOX isoenzymes in epileptic disorders. To set the foundation for future research into the neurobiology of licofelone as a potential therapeutic agent, we studied the effect of licofelone in an animal model of epilepsy...
September 2015: Neurochemical Research
https://www.readbyqxmd.com/read/26168917/valerenic-acid-and-valeriana-officinalis-extracts-delay-onset-of-pentylenetetrazole-ptz-induced-seizures-in-adult-danio-rerio-zebrafish
#20
Bianca A Torres-Hernández, Lisa M Del Valle-Mojica, José G Ortíz
BACKGROUND: Anticonvulsant properties have been attributed to extracts of the herbal medicine Valeriana officinalis. Our aims were to examine the anticonvulsant properties of valerenic acid and valerian extracts and to determine whether valerian preparations interact with the activity of other anti-epileptic drugs (phenytoin or clonazepam). To achieve these goals, we validated the adult zebrafish, Danio rerio, as an animal model for studying anticonvulsant drugs. METHODS: All drug treatments were administered by immersion in water containing the drug...
July 14, 2015: BMC Complementary and Alternative Medicine
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