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Anticonvulsant

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https://www.readbyqxmd.com/read/29045762/synthesis-determination-of-the-lipophilicity-anticonvulsant-activity-and-preliminary-safety-of-new-derivatives-of-n-4-arylpiperazin-1-yl-alkyl-pyrrolidine-2-5-dione
#1
Sabina Rybka, Jolanta Obniska, Paweł Żmudzki, Paulina Koczurkiewicz, Katarzyna Wójcik-Pszczoła, Elżbieta Pękala, Adrian Bryła, Anna Rapacz
A new series of derivatives of 1,3-substituted pyrrolidine-2,5-dione as potential anticonvulsant agents are described in this paper. Initial pharmacological screening for these compounds was performed using acute models of seizures (MES and scPTZ tests) in mice after intraperitoneal administration. A quantitative pharmacological research revealed that the most promising compound were N-[{4-(3-trifluoromethylphenyl)-piperazin-1-yl}-propyl]-3-benzhydryl-pyrrolidine-2,5-dione monohydrochloride (11) with ED50=75...
October 18, 2017: ChemMedChem
https://www.readbyqxmd.com/read/29044858/pharmacological-and-chemical-features-of-nepeta-l-genus-its-importance-as-a-therapeutic-agent
#2
REVIEW
Ipek Süntar, Seyed Mohammad Nabavi, Davide Barreca, Nicolas Fischer, Thomas Efferth
Medicinal plants have always had great value for the human population due to their valuable constituents and potential bioactivities. The objective of this review is to present an updated overview of an important medicinal plant genus Nepeta L., from the family Lamiaceae, revealing its traditional utilization, biological activity, phytoconstituents, and mechanisms of action. For this purpose, a literature survey was carried out by using SciFinder, ScienceDirect, Scopus, PubMed, and Web of Science followed by a revision of the bibliographies of the related articles...
October 18, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/29037915/linalool-rich-essential-oils-from-the-amazon-display-antidepressant-type-effect-in-rodents
#3
Éverton Renan Q Dos Santos, Cristiane Socorro F Maia, Enéas A Fontes Junior, Ademar S Melo, Bruno G Pinheiro, José Guilherme S Maia
ETHNOPHARMACOLOGICAL RELEVANCE: The essential oils of the leaves of Aniba rosaeodora (pau-rosa), Aniba parviflora (macacaporanga) and Aeollanthus suaveolens (catinga-de-mulata), rich in linalool, are used in the traditional medicine of the Brazilian Amazon for its effects on the central nervous system, such as sedative, anticonvulsant and antidepressant, among other therapeutic properties. AIM OF THE STUDY: To analyze the chemical composition of these oils and to evaluate their neurobehavioral effects in rodents, based on different and established behavioral tests...
October 13, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/29035798/sexual-function-and-related-factors-in-iranian-woman-with-epilepsy
#4
Zahra Atarodi-Kashani, Nourossadat Kariman, Abbas Ebadi, Hamid Alavi Majd, Nahid Beladi-Moghadam
PURPOSE: Epileptic women are faced with many sexual challenges in their life due to medical and non-medical factors. The present study was conducted to assess sexual function in epileptic women and its related factors. METHOD: The present cross-sectional study was conducted on 196 epileptic married women of reproductive age who were members of the Iranian Epilepsy Association and were selected continuously over six months through convenience sampling. The data collection tools included the Female Sexual Function Index (FSFI) and questions about the causes of sexual dysfunction...
October 5, 2017: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/29034137/valproic-induced-hyperammonemic-encephalopathy-in-a-known-case-of-epilepsy
#5
Syed F Imam, Omair Ul Haq Lodhi, Rizwan Zafar, Saneeya Nasim, Waseem T Malik
Valproic acid, a broad-spectrum anticonvulsant drug, commonly causes elevated ammonia levels, which is usually asymptomatic in most cases. On rare occasions, potentially fatal hyperammonemia-induced encephalopathy can occur. We present a case of a 24-year-old female who presented to the emergency department with status epilepticus that was being managed with valproic acid. Further workup was done because of prolonged postictal state, which revealed increased ammonia levels; she was eventually diagnosed with valproic-induced hyperammonemic encephalopathy...
August 10, 2017: Curēus
https://www.readbyqxmd.com/read/29032429/dna-damage-and-oxidative-stress-induced-by-seizures-are-decreased-by-anticonvulsant-and-neuroprotective-effects-of-lobeline-a-candidate-to-treat-alcoholism
#6
Liana Dantas da Costa E Silva, Patrícia Pereira, Gabriela Gregory Regner, Fernanda Brião Menezes Boaretto, Cleonice Hoffmann, Pricila Pflüger, Lucas Lima da Silva, Luiza Reinhardt Steffens, Ana Moira Morás, Dinara Jaqueline Moura, Jaqueline Nascimento Picada
The alkaloid lobeline (Lob) has been studied due to its potential use in treatment of drug abuse. This study evaluates the possible anticonvulsant and neuroprotective activities of Lob to obtain new information on its properties that could confirm it as a candidate in the treatment of alcohol addiction. The anticonvulsant effect of Lob was evaluated using a pilocarpine-induced seizure model. In addition, possible neuroprotective effects were investigated measuring DNA damage using the comet assay, assessing free radical levels by dichlorofluorescein diacetate (DCF) oxidation, and measuring the antioxidant potential using the α, α-diphenyl-β-picrylhydrazyl (DPPH) scavenging assay, besides measuring superoxide dismutase (SOD) and catalase (CAT) enzyme activities in brain tissues...
October 14, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/29030992/inadequate-safety-reporting-in-pre-eclampsia-trials-a-systematic-evaluation
#7
James M N Duffy, Martin Hirsch, Louise Pealing, Marian Showell, Khalid S Khan, Sue Ziebland, Richard J McManus
BACKGROUND: Randomised trials and their syntheses in meta-analyses offer a unique opportunity to assess the frequency and severity of adverse reactions. OBJECTIVE: To assess safety reporting in pre-eclampsia trials. SEARCH STRATEGY: Systematic search using bibliographic databases, including Cochrane Central Register of Controlled Trials, Embase, and MEDLINE, from inception to August 2017. SELECTION CRITERIA: Randomised trials evaluating anticonvulsant or antihypertensive medication for pre-eclampsia...
October 14, 2017: BJOG: An International Journal of Obstetrics and Gynaecology
https://www.readbyqxmd.com/read/29027610/risk-factors-for-and-incidence-of-seizures-in-metastatic-castration-resistant-prostate-cancer-a-real-world-retrospective-cohort-study
#8
Charles Dharmani, Machaon Bonafede, Andrew Krivoshik
BACKGROUND AND OBJECTIVE: This real-world study assessed the prevalence, risk factors for, and incidence of seizures in patients with metastatic castration-resistant prostate cancer (mCRPC). METHODS: Patients with mCRPC were selected from MarketScan Commercial and Medicare Supplemental Databases between 1 January 2009 and 31 July 2012. Prevalence of seizure risk factors were described separately and in combination with other risk factors. Seizure incidence was calculated overall and for each risk factor group...
October 13, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/29026579/amlodipine-induced-gingival-enlargement
#9
Abhilash Koratala, Indirakshi Jamalpur, Harikrishna Reddy Mogili
The three most common classes of medications implicated in drug-induced gum enlargement are anticonvulsives, calcineurin inhibitors, and calcium channel blockers. Treatment primarily consists of withdrawing the offending agent whenever possible, in addition to maintaining good oral hygiene. Gingivectomy or flap surgery may be needed in resistant cases.
October 2017: Clinical Case Reports
https://www.readbyqxmd.com/read/29026345/tolerated-drugs-in-subjects-with-severe-cutaneous-adverse-reactions-scars-induced-by-anticonvulsants-and-review-of-the-literature
#10
REVIEW
Fabrizio De Luca, Laura Michelina Losappio, Corrado Mirone, Jan Walter Schroeder, Antonella Citterio, Maria Gloria Aversano, Joseph Scibilia, Elide Anna Pastorello
BACKGROUND: Anticonvulsant hypersensitivity syndrome represents a rare but potentially fatal kind of adverse drug reaction. This clinical picture often hampers the flexibility with which alternative anticonvulsants or even other classes of drugs are prescribed in these patients, negatively affecting the efficacy of treatment and the course of the disease. The aim of this study was to analyse a group of six patients with severe cutaneous drug reactions induced by anticonvulsants and to report which alternative antiepileptic drugs and which drugs of other classes were tolerated...
2017: Clinical and Molecular Allergy: CMA
https://www.readbyqxmd.com/read/29019915/revolutionizing-therapeutic-drug-monitoring-with-the-use-of-interstitial-fluid-and-microneedles-technology
#11
REVIEW
Tony K L Kiang, Sahan A Ranamukhaarachchi, Mary H H Ensom
While therapeutic drug monitoring (TDM) that uses blood as the biological matrix is the traditional gold standard, this practice may be impossible, impractical, or unethical for some patient populations (e.g., elderly, pediatric, anemic) and those with fragile veins. In the context of finding an alternative biological matrix for TDM, this manuscript will provide a qualitative review on: (1) the principles of TDM; (2) alternative matrices for TDM; (3) current evidence supporting the use of interstitial fluid (ISF) for TDM in clinical models; (4) the use of microneedle technologies, which is potentially minimally invasive and pain-free, for the collection of ISF; and (5) future directions...
October 11, 2017: Pharmaceutics
https://www.readbyqxmd.com/read/29019022/distribution-of-lacosamide-in-the-rat-brain-assessed-by-in-vitro-slice-technique
#12
Zsolt Gáll, Szende Vancea
Lacosamide is a newer anticonvulsant and is the only one that enhances the slow inactivation of voltage gated sodium channels. It is also claimed to have disease-modifying potential, but its pharmacokinetic properties have been much less discussed in the literature. In rats, lacosamide shows restricted distribution to tissues, and the brain-to-plasma partition coefficient (Kp) is only 0.553. In this study, the brain disposition of lacosamide was evaluated in rat brains, and its neuropharmacokinetic parameters (i...
October 10, 2017: Archives of Pharmacal Research
https://www.readbyqxmd.com/read/29018404/socioeconomic-outcome-and-quality-of-life-in-adults-after-status-epilepticus-a-multicenter-longitudinal-matched-case-control-analysis-from-germany
#13
Lena-Marie Kortland, Susanne Knake, Felix von Podewils, Felix Rosenow, Adam Strzelczyk
BACKGROUND: There is a lack of data concerning socioeconomic outcome and quality of life (QoL) in patients after status epilepticus (SE) in Germany. PATIENTS AND METHODS: Adult patients treated between 2011 and 2015 due to SE at the university hospitals in Frankfurt, Greifswald, and Marburg were asked to fill out a questionnaire regarding long-term outcome of at least 3 months after discharge. The SE cohort consisted of 25.9% patients with an acute symptomatic, 42% with a remote symptomatic and previous epilepsy, 22...
2017: Frontiers in Neurology
https://www.readbyqxmd.com/read/29018345/involvement-of-ppar%C3%AE-in-the-anticonvulsant-activity-of-ep-80317-a-ghrelin-receptor-antagonist
#14
Chiara Lucchi, Anna M Costa, Carmela Giordano, Giulia Curia, Marika Piat, Giuseppina Leo, Jonathan Vinet, Luc Brunel, Jean-Alain Fehrentz, Jean Martinez, Antonio Torsello, Giuseppe Biagini
Ghrelin, des-acyl ghrelin and other related peptides possess anticonvulsant activities. Although ghrelin and cognate peptides were shown to physiologically regulate only the ghrelin receptor, some of them were pharmacologically proved to activate the peroxisome proliferator-activated receptor gamma (PPARγ) through stimulation of the scavenger receptor CD36 in macrophages. In our study, we challenged the hypothesis that PPARγ could be involved in the anticonvulsant effects of EP-80317, a ghrelin receptor antagonist...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29018010/unusual-complications-from-amitriptyline-intoxication
#15
Takeshi Nishimura, Hayato Maruguchi, Atsunori Nakao, Shinichi Nakayama
Althoughtricyclic antidepressants(TCAs) are frequently prescribed to patients with depression, these drugs can also be misused. A 21-year-old comatose patient was referred to our hospital presenting with ventricular tachycardia. Despite initial treatment including intravascular lipid emulsion, ventricular fibrillation occurred soon after arrival. Venoarterial extracorporeal membrane oxygenation and therapeutic hypothermia were administered. Refractory arrhythmia disappeared on the next day. A high concentration of amitriptyline was identified in his blood samples on arrival...
October 10, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/29017388/pathophysiological-bases-of-comorbidity-tbi-and-ptsd
#16
Gary B Kaplan, Kimberly A Leite-Morris, Lei Wang, Kendra K Rumbika, Stephen C Heinrichs, Xiang Zeng, Liquan Wu, Danielle T Arena, Yang D Teng
The high rates of TBI and PTSD diagnoses encountered in recent years by the U.S. Veterans Affairs Healthcare System have increased public awareness and research investigation into these conditions. In this review, we analyze the neural mechanisms underlying the TBI/PTSD comorbidity. TBI and PTSD present with common neuropsychiatric symptoms including anxiety, irritability, insomnia, personality changes and memory problems and this overlap complicates diagnostic differentiation. Interestingly, both TBI and PTSD can be produced by overlapping pathophysiological changes that disrupt neural connections termed the "connectome"...
October 10, 2017: Journal of Neurotrauma
https://www.readbyqxmd.com/read/28991361/withdrawn-anticonvulsants-for-fibromyalgia
#17
REVIEW
Nurcan Üçeyler, Claudia Sommer, Brian Walitt, Winfried Häuser
BACKGROUND: Fibromyalgia (FM) is a clinically well-defined chronic condition of unknown aetiology characterised by chronic widespread pain that often co-exists with sleep problems and fatigue. People often report high disability levels and poor health-related quality of life (HRQoL). Drug therapy focuses on reducing key symptoms and disability, and improving HRQoL. Anticonvulsants (antiepileptic drugs) are drugs frequently used for the treatment of chronic pain syndromes. OBJECTIVES: To assess the benefits and harms of anticonvulsants for treating FM symptoms...
October 9, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28991263/structural-basis-for-gabaa-receptor-potentiation-by-neurosteroids
#18
Paul S Miller, Suzanne Scott, Simonas Masiulis, Luigi De Colibus, Els Pardon, Jan Steyaert, A Radu Aricescu
Type A γ-aminobutyric acid receptors (GABAARs) are the principal mediators of inhibitory neurotransmission in the human brain. Endogenous neurosteroids interact with GABAARs to regulate acute and chronic anxiety and are potent sedative, analgesic, anticonvulsant and anesthetic agents. Their mode of binding and mechanism of receptor potentiation, however, remain unknown. Here we report crystal structures of a chimeric GABAAR construct in apo and pregnanolone-bound states. The neurosteroid-binding site is mechanically coupled to the helices lining the ion channel pore and modulates the desensitization-gate conformation...
October 9, 2017: Nature Structural & Molecular Biology
https://www.readbyqxmd.com/read/28988516/quinine-and-carbenoxolone-enhance-the-anticonvulsant-activity-of-some-classical-antiepileptic-drugs
#19
Javier Franco-Pérez, Joaquín Manjarrez-Marmolejo, Cesar Rodríguez-Balderas, Nelly Castro, Paola Ballesteros-Zebadua
Objective Quinine (QUIN) and carbenoxolone (CNX) elicit anticonvulsant effects typically characterized by the reduction of the epileptiform activity as well as changes in behavioral parameters related to seizures. Therefore, the aim of this study was to analyze the effects of these molecules on the anticonvulsant activity of some classical antiepileptic drugs. Methods Male Wistar rats were used. Valproate (VPA), phenytoin (PHT), or carbamazepine (CBZ) was administered at sub-therapeutic doses for intraperitoneal via...
October 8, 2017: Neurological Research
https://www.readbyqxmd.com/read/28987270/involvement-of-nitrergic-system-in-anticonvulsant-effect-of-zolpidem-in-lithium-pilocarpine-induced-status-epilepticus-evaluation-of-inos-and-cox-2-genes-expression
#20
Seyyed Majid Eslami, Maryam Ghasemi, Taraneh Bahremand, Majid Momeny, Mahdi Gholami, Mohammad Sharifzadeh, Ahmad Reza Dehpour
This study aims to investigate the role of zolpidem in lithium-pilocarpine induced status epilepticus (SE) and probable mechanisms involved in seizure threshold alteration. In the present study, lithium chloride (127mg/kg) was administered 20h prior to pilocarpine (60mg/kg) to induce SE in adult male Wistar rats. Different doses of zolpidem (0.1, 1, 2, 5, 10mg/kg) were injected 30min before pilocarpine administration. Furthermore, to find out whether nitric oxide (NO) plays a role in the observed effect, L-arginine and L-NAME were injected 15min before zolpidem...
October 4, 2017: European Journal of Pharmacology
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