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Cureus 2018 Nov 23;10(11):e3625. Epub 2018 Nov 23.

Radiation Oncology, The University of Ottawa, Ottawa, CAN.

Phenytoin toxicity occurs when serum levels exceed the therapeutic level, leading to symptoms such as nystagmus, slurred speech, and decreased coordination. This toxicity is sometimes caused by drug interactions. Interactions between phenytoin and capecitabine are not commonly documented. Read More

Eur J Pharm Sci 2019 Jan 10;130:21-26. Epub 2019 Jan 10.

Department of Pharmacology & Therapeutics, Faculty of Pharmacy, Kuwait University, Kuwait.

The pharmacotherapeutic management of seizure disorders with currently available medications is not optimal due to side effects and failure of some patients to respond to all available medications. As such there is the need to develop new antiseizure drugs by looking at new chemical classes of compounds. We recently screened, in vitro, a new class of compounds, the oxazolidinones, for actions in the brain that may indicate potential for antiseizure activity. Read More

Drug Dev Res 2019 Jan 4. Epub 2019 Jan 4.

Department of Pharmacology, Faculty of Pharmacy, M. S. Ramaiah University of Applied Sciences, Bengaluru, Karnataka, India.

Hit, Lead & Candidate Discovery A variety of novel 2-(methyl/phenyl)-3-(4-(5-substituted-1,3,4-oxadiazol-2-yl)phenyl) quinazolin-4(3H)-ones have been synthesized by treating 3-(4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenyl)-2-(methyl/phenyl)-quinazolin-4(3H)-one with a variety of secondary amines. Graph theoretical analysis was used in identification of drug target that is, NMDAR (N-methyl-d-aspartate receptors). The observed reports of in silico modeling and ligand based toxicity, metabolism prediction studies were encouraging us to synthesize of title compounds and evaluate their antiepileptic effects. Read More

Medicine (Baltimore) 2018 Dec;97(51):e13689

Department of Neurology, The Second Hospital of Hebei Medical University, Shijiazhuang, Hebei, China.

Objective: In this study, we aimed to review the literature on phenytoin intoxication induced by compound phenytoin sodium, ephedrine hydrochloride and theophylline tablets (CPEHTT).

Method: A literature search was performed in the following databases: WANFANG DATA, HowNet, National Library Reference and Consultation Alliance, Full-text Database of Foreign Medical Journals, PubMed and Ovid. The search terms were "Compound Phenytoin Sodium, ephedrine Hydrochloride and Theophylline Tablets," and "poisoning," or "toxicity," in Chinese and in English. Read More

Neurol India 2018 Nov-Dec;66(6):1829-1831

Department of Neurology, King George's Medical University, Lucknow, Uttar Pradesh, India.

Ned Tijdschr Geneeskd 2018 08 16;162. Epub 2018 Aug 16.

VUmc, afd. Ziekenhuispsychiatrie, Amsterdam.

Background: Valproic acid is one of the most widely prescribed drugs for the treatment of epilepsy and bipolar disorder. As only the unbound fraction of a medicinal product is pharmacologically active, in some strong protein-bound psychotropic drugs such as valproic acid and phenytoin, a rise in this fraction can lead to severe toxicity.

Case Description: A 65-year-old male with a type 1 bipolar disorder developed a number of neurological symptoms including sluggishness, muscle weakness, difficulty in walking and disorders of micturition after his mood stabiliser was changed to valproic acid. Read More

Pak J Pharm Sci 2018 Jul;31(4(Special)):1697-1700

Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China.

The narrow therapeutic index, non-linear pharmacokinetics and unpredictable absorption require regular therapeutic monitoring of phenytoin. The influence of genetic differences, sex, age and race on the phenytoin plasma levels and its metabolites is well recognized. This study is aimed at evaluating phenytoin plasma drug concentration and its relationship with clinical response, persistent seizures and toxicity in different gender and various age groups of Chinese epileptic patients. Read More

Ther Drug Monit 2018 12;40(6):725-729

Department of Clinical Research, National Epilepsy Center, NHO, Shizuoka Institute of Epilepsy and Neurological Disorders.

Background: It is well-known that the pharmacokinetics of various drugs are influenced by inflammation. This study evaluated the relationship between C-reactive protein (CRP; an inflammation marker) and the pharmacokinetics of perampanel.

Methods: Among 111 patients who underwent measurement of both CRP and perampanel, 23 patients had a serum CRP level exceeding 1. Read More

J Investig Med High Impact Case Rep 2018 Jan-Dec;6:2324709618765862. Epub 2018 Mar 24.

Maricopa Integrated Health System, Department of Emergency Medicine, Phoenix, AZ, USA.

Tacrolimus is used in bone marrow transplant patients to prevent graft-versus-host disease. There have been few case reports of tacrolimus toxicity (>30 ng/mL) in solid organ recipients as well as in nontransplant patients. Several case reports suggest phenytoin and rifampin decrease tacrolimus levels in toxicity, but does it actually make a difference? A 60-year-old man with acute myeloblastic leukemia after allogenic stem cell transplant with fever, diarrhea, and abdominal pain was transferred to the intensive care unit for persistent hypotension and acute hypoxic respiratory failure requiring intubation. Read More

Sci Rep 2018 Jul 10;8(1):10416. Epub 2018 Jul 10.

Department of Electronics, Graduate School of Engineering, Tohoku Institute of Technology, 35-1 Yagiyama Kasumicho, Taihaku-ku, Sendai, Miyagi, 982-8577, Japan.

Functional evaluation assays using human induced pluripotent stem cell (hiPSC)-derived neurons can predict the convulsion toxicity of new drugs and the neurological effects of antiepileptic drugs. However, differences in responsiveness depending on convulsant type and antiepileptic drugs, and an evaluation index capable of comparing in vitro responses with in vivo responses are not well known. We observed the difference in synchronized burst patterns in the epileptiform activities induced by pentylentetrazole (PTZ) and 4-aminopryridine (4-AP) with different action mechanisms using multi-electrode arrays (MEAs); we also observed that 100 µM of the antiepileptic drug phenytoin suppressed epileptiform activities induced by PTZ, but increased those induced by 4-AP. Read More

Cochrane Database Syst Rev 2018 06 28;6:CD010965. Epub 2018 Jun 28.

Renal Division, Sector Metabolic and Cardiovascular Conditions, Ghent University Hospital, De Pintelaan 185, Ghent, Belgium, 9000.

Background: Chronic (present > 48 hours) non-hypovolaemic hyponatraemia occurs frequently, can be caused by various conditions, and is associated with shorter survival and longer hospital stays. Many treatments, such as fluid restriction or vasopressin receptor antagonists can be used to improve the hyponatraemia, but whether that translates into improved patient-important outcomes is less certain.

Objectives: This review aimed to 1) look at the benefits and harms of interventions for chronic non-hypovolaemic hypotonic hyponatraemia when compared with placebo, no treatment or head-to-head; and 2) determine if benefits and harms vary in absolute or relative terms dependent on the specific compound within a drug class, on the dosage used, or the underlying disorder causing the hyponatraemia. Read More

Handb Clin Neurol 2018 ;154:129-149

Research, Neurology, and Pathology Services, Veterans Affairs Medical Center and Departments of Neurology and Pathology, Albany Medical College, Albany, NY, United States. Electronic address:

This chapter summarizes the neuropathologic features of nonneoplastic disorders of the adult cerebellum. Gait ataxia and extremity dysmetria are clinical manifestations of diseases that interrupt the complex cerebellar circuitry between the neurons of the cerebellar cortex, the cerebellar nuclei (especially the dentate nuclei), and the inferior olivary nuclei. The cerebellum is a prominent target of several sporadic and hereditary neurodegenerative diseases, including multiple system atrophy, spinocerebellar ataxia, and Friedreich ataxia. Read More

Handb Clin Neurol 2018 ;155:333-352

Neurology Service, Hôpital Erasme, Brussels, Belgium.

The cerebellum is a brain region which is particularly susceptible to intoxication. Clinical presentation is heterogeneous. It is often considered that elderly patients and patients presenting pre-existing structural lesions of the posterior fossa are particularly at risk of developing a toxic-induced cerebellar syndrome (TOICS). Read More

Drug Metab Dispos 2018 08 8;46(8):1241-1250. Epub 2018 Jun 8.

Department of Pharmaceutical Sciences, School of Pharmacy, University of Connecticut, Storrs, Connecticut (S.C.P., L.C., S.Y., X.-b.Z.); Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, Pennsylvania (P.W., X.M.); and Department of Clinical Pharmacy, College of Pharmacy, University of Michigan, Ann Arbor, Michigan (J.S., H.-J.Z.)

The induction of cytochrome P450 (P450) enzymes in response to drug treatment is a significant contributing factor to drug-drug interactions, which may reduce therapeutic efficacy and/or cause toxicity. Since most studies on P450 induction are performed in adults, enzyme induction at neonatal, infant, and adolescent ages is not well understood. Previous work defined the postnatal ontogeny of drug-metabolizing P450s in human and mouse livers; however, there are limited data on the ontogeny of the induction potential of each enzyme in response to drug treatment. Read More

J Anal Methods Chem 2018 1;2018:8274131. Epub 2018 Apr 1.

Clinical Pharmacy and Epidemiology, Hospital Pharmacy, University of Basel, Spitalstrasse 26, CH-4031 Basel, Switzerland.

Phenytoin (PHT) is one of the most often used critical dose drugs, where insufficient or excessive dosing can have severe consequences such as seizures or toxicity. Thus, the monitoring and precise measuring of PHT concentrations in patients is crucial. This study develops and validates an LC-MS/MS method for the measurement of phenytoin concentrations in different body compartments (i. Read More

Epilepsia 2018 06 21;59(6):1166-1176. Epub 2018 May 21.

Department of Pharmacology, Northwestern University Feinberg School of Medicine, Chicago, IL, USA.

Objective: De novo mutations of SCN8A, encoding the voltage-gated sodium channel Na 1.6, have been associated with a severe infant onset epileptic encephalopathy. Individuals with SCN8A encephalopathy have a mean age of seizure onset of 4-5 months, with multiple seizure types that are often refractory to treatment with available drugs. Read More

J Appl Toxicol 2018 Sep 16;38(9):1215-1223. Epub 2018 May 16.

Department of Pharmacology, Laboratory of Physiology and Pharmacology of Reproduction, Universidade Federal de Goiás, Goiânia, GO, Brazil.

Children and adults with frequent and severe episodes of epilepsy that do not respond to standard treatments (such as carbamazepine, phenytoin and valproate) have long been prescribed cannabidiol (CBD) as an anticonvulsant drug. However, the safety of its chronic use in relation to reproduction has not been fully examined. This study aimed to assess the effects of chronic CBD exposure on the male reproductive system. Read More

Cureus 2018 Feb 8;10(2):e2169. Epub 2018 Feb 8.

Assistant Clinical Professor of Internal Medicine, West Virginia University School of Medicine.

Phenytoin is a medication that is used primarily in the treatment of epilepsy as well as generalized tonic-clonic seizures and status epilepticus. Phenytoin is also considered a class IB antiarrhythmic medication by shortening the duration of the action potential and increasing myocardial conduction. The neurologic adverse effects of phenytoin are well-documented and include altered mental status, ataxia, and nystagmus. Read More

Front Neurol 2018 1;9:46. Epub 2018 Mar 1.

Illinois Neurologic Institute, University of Illinois College of Medicine, Peoria, IL, United States.

Background: Previous series of bilateral vestibular loss (BVL) identified numerous etiologies, but surprisingly, a cause in a significant number of cases remains unknown. In an effort to understand possible etiology and management strategies, a global effort is currently in progress. Here, I contribute my 10-year experience with both acute and chronic BVL during the 2007-2017 decade. Read More

Yakugaku Zasshi 2018 ;138(3):277-280

Faculty of Pharmaceutical Sciences, Hiroshima International University.

　In recent years, pharmaceuticals and personal care products (PPCPs) have emerged as significant pollutants of aquatic environments and have been detected at levels in the range of ng/L to μg/L. The source of PPCPs is humans and livestock that have been administered pharmaceuticals and subsequently excreted them via urine and feces. Unlike agricultural chemicals, the environmental dynamics of PPCPs is not examined and they would undergo structural transformation by environmental factors, e. Read More

J Toxicol Sci 2018 ;43(2):75-87

Department of Drug Safety Sciences, Nagoya University Graduate School of Medicine.

Several drugs have been withdrawn from the market or restricted to avoid unexpected adverse outcomes. Drug-induced liver injury (DILI) is a serious issue for drug development. Among DILIs, idiosyncratic DILIs have been a serious problem in drug development and clinical uses. Read More

Curr Pharm Biotechnol 2017 ;18(13):1098-1105

Institute of Clinical Pharmacology, Qilu Hospital, Shandong University, Jinan, China.

Background: Phenytoin has very challenging pharmacokinetic properties. To prevent its toxicity and ensure efficacy, continuous therapeutic monitoring is required. It is hard to get a simple, accurate, rapid, easily available, economical and highly sensitive assay in one method for therapeutic monitoring of phenytoin. Read More

Basic Clin Pharmacol Toxicol 2018 Jul 13;123(1):14-20. Epub 2018 Mar 13.

Department of Neurology, The First Affiliated Hospital of Xi'an Medical University, Xi'an, China.

Overexpression of P-glycoprotein (P-gp) in the brain is an important factor leading to drug-resistant epilepsy. Clinical use of P-gp inhibitors is limited by their systemic toxicity. In this study, we tested the hypothesis that FTY720, a sphingosine 1-phosphate (S1P) analogue used for treating multiple sclerosis, modulates the up-regulation of P-gp and improves brain delivery of phenytoin (PHT) through S1P receptor 1 in the hippocampus of a pilocarpine-induced rat model of status epilepticus (SE). Read More

Neurotoxicol Teratol 2018 Mar - Apr;66:17-24. Epub 2018 Feb 3.

Laboratorio de Biomembranas (LBM), Departamento de Ciencia y Tecnología, Universidad Nacional de Quilmes, Grupo vinculado GBEyB, IMBICE, CICPBA, CCT, La Plata - CONICET, Bernal, Argentina,. Electronic address:

Epilepsy is a neurological disorder treated with antiepileptic drugs (AEDs). Since AEDs are administered in women in childbearing age, it is critical to study if drugs are capable of inducing developmental toxicity. Along the bibliography available, there is no research comparing teratogenicity and anticonvulsant effect within the same study. Read More

Drug Metab Dispos 2018 04 17;46(4):380-386. Epub 2018 Jan 17.

Department of Medicinal Chemistry (E.A.E., R.A.T.), Cardiovascular Health Research Unit, Department of Medicine (R.N.L., N.S.), Division of Cardiology (N.S.), and Computational Medicinal Core, Center for Lung Biology, Division of Pulmonary and Critical Care Medicine, Department of Medicine (S.A.G.), University of Washington, Seattle, Washington

Cytochrome P450 2J2 isoform (CYP2J2) is a drug-metabolizing enzyme that is highly expressed in adult ventricular myocytes. It is responsible for the bioactivation of arachidonic acid (AA) into epoxyeicosatrienoic acids (EETs). EETs are biologically active signaling compounds that protect against disease progression, particularly in cardiovascular diseases. Read More

J Ethnopharmacol 2018 Apr 14;215:124-131. Epub 2017 Dec 14.

Department of Pharmacology, All India Institute of Medical Sciences, New Delhi 110029, India. Electronic address:

Ethnopharmacological Relevance: Teminalia chebula (TC) has been traditionally used in the Ayurvedic system of medicine primarily for gastrointestinal disorders. Its fruit extract has also been used to treat epilepsy and other CNS disorders.

Aim Of The Study: To evaluate the effect of hydroalcoholic fruit extract of Terminalia chebula (HETC) on experimental models of seizures, seizure-induced cognitive impairment and oxidative stress in rats. Read More

Iran J Neurol 2017 Jul;16(3):125-129

Iranian Center of Neurological Research, Neuroscience Institute, Tehran University of Medical Sciences, Tehran, Iran.

To date, magnesium sulphate (MgSO) is the treatment of choice for prevention of seizure in eclampsia and preeclampsia. However, there are some limitations in the administration of MgSO due to its tocolytic effects. The aim of this study was to compare the anticonvulsant and tocolytic effects of MgSO and another drug, phenytoin, in patients with eclampsia and preeclampsia. Read More

Pediatr Neurol 2017 Dec 22;77:23-36. Epub 2017 Sep 22.

Division of Pediatric Neurology, Department of Pediatrics, Nationwide Children's Hospital, Columbus, Ohio.

Acute, symptomatic seizures or epilepsy may complicate the course of hepatic disease. Choosing the most appropriate antiepileptic drug in this setting represents a difficult challenge, as most medications are metabolized by the liver. This article focuses on the acute and chronic treatment of seizures in patients with advanced liver disease and reviews the hepatotoxic potential of specific antiepileptic drugs. Read More

Neurol Res 2018 Jan 8;40(1):26-33. Epub 2017 Oct 8.

d Laboratory of Medical Physics , National Institute of Neurology and Neurosurgery , Mexico City , Mexico.

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. Read More

Adv Exp Med Biol 2017 ;988:39-48

Medicinal Chemistry Laboratory, U.C.P.Sc., Kakatiya University, Wararagal, 506009, Telangana, India.

The new heterocyclic compounds are used to treat epilepsy. In the present work new indole derivatives i.e. Read More

Biomed Pharmacother 2017 Nov 21;95:1451-1460. Epub 2017 Sep 21.

Pharmaceutical Chemistry Research Laboratory, Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi - 221005, Uttar Pradesh, India. Electronic address:

Epilepsy is one of the dreadful neurodegenerative disorder characterized by recurrent, unprovoked seizures. Currently available antiepileptic drugs are still associated with enormous side effects resulting in search of newer, more effective and safer agents. In view of this, we have investigated anticonvulsant activity of 2-amino-6-nitrobenzothiazole derived semicarbazones (7-32) in various in-vivo animal seizure models viz. Read More

Molecules 2017 Sep 22;22(10). Epub 2017 Sep 22.

Laboratoire de biologie moléculaire, d'épidémiologie et de surveillance des bactéries et virus transmis par les aliments (Labesta), Université Ouaga I Pr Joseph KI-ZERBO, 03 P.O. 7021 Ouagadougou, Burkina Faso.

Widespread resistance of sp. populations to pyrethroid insecticides has led to the search for sustainable alternatives in the plant kingdom. Among many botanicals, there is great interest in essential oils and their constituents. Read More

Clin Transplant 2017 Nov 18;31(11). Epub 2017 Sep 18.

Department of Pharmacy, NewYork-Presbyterian Hospital, New York, NY, USA.

Objectives: To summarize the available body of evidence guiding the management of supratherapeutic concentrations of calcineurin inhibitors (CNI) using cytochrome P450 (CYP450) enzyme inducers.

Methods: A nondate restricted literature search within MEDLINE, Embase, and Scopus was performed using the terms "cyclosporine," "tacrolimus," "calcineurin inhibitor," "toxicity," "pharmacokinetics," "carbamazepine," "rifampin," "phenytoin," and "phenobarbital." Additional references were identified from a review of all included citations. Read More

Expert Opin Drug Saf 2017 Nov 29;16(11):1281-1294. Epub 2017 Aug 29.

a Department of Neurology and Psychiatry , Assiut University Hospital , Assiut , Egypt.

Introduction: Epilepsy is a chronic medical disease in one third of patients and is associated with comorbid adverse somatic conditions due to epilepsy itself or its long-term treatment with antiepileptic drugs (AEDs). Data from experimental, cross-sectional and prospective studies have evidence for the deleterious effect of some AEDs on the auditory and vestibular systems. These abnormalities may be reversible or irreversible. Read More

Environ Sci Pollut Res Int 2017 Oct 11;24(28):22361-22370. Epub 2017 Aug 11.

Department of Chemistry, Faculty of Science, University of Malaya, 50603, Kuala Lumpur, Malaysia.

This study investigated the reaction kinetics and mechanism of the degradation of 5,5-diphenylhydantoin (DPH) during conventional chlorination and UV/chlorination. DPH is one of the antiepileptic drugs, which has frequently been detected in the aquatic environment. For chlorination, the second-order rate constant for the reaction between DPH and free active chlorine (FAC) was determined at pH 5 to 8. Read More

Arch Pharm (Weinheim) 2017 Sep 31;350(9). Epub 2017 Jul 31.

Department of Pharmaceutical Chemistry, Delhi Institute of Pharmaceutical Sciences and Research (DIPSAR), New Delhi, India.

A series of new pyrimidine-triazine hybrids (4a-t) was designed and synthesized, from which potent anticonvulsant agents were identified. Most of the compounds exhibited promising anticonvulsant activity against the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) tests, along with minimal motor impairment with higher safety compared to the standard drugs, phenytoin and carbamazepine. In the series, 5-(4-(4-fluorophenyl)-6-(4-hydroxyphenyl)-2-thioxo-5,6-dihydropyrimidin-1(2H)-yl)-1,2-dihydro-1,2,4-triazin-3(6H)-one (4o) and 5-(6-(4-hydroxy-3-methoxyphenyl)-4-(4-hydroxyphenyl)-2-thioxo-5,6-dihydropyrimidin-1(2H)-yl)-1,2-dihydro-1,2,4-triazin-3(6H)-one (4s) emerged as most potent anticonvulsant agents with median doses of 22. Read More

Epilepsy Res 2017 10 13;136:5-11. Epub 2017 Jul 13.

Disciplina de Neurociência, Escola Paulista de Medicina/Universidade Federal de São Paulo, (EPM/UNIFESP), São Paulo, Brazil. Electronic address:

Objectives: Antiepileptic drugs (AEDs) exhibit adverse and beneficial effects on mitochondria, which have a strong impact on the treatment of patients with a mitochondrial disorder (MID) with epilepsy (mitochondrial epilepsy). This review aims at summarizing and discussing recent findings concerning the effect of AEDs on mitochondrial functions and the clinical consequences with regard to therapy of mitochondrial epilepsy and of MIDs in general.

Methods: Literature review. Read More

Cent Nerv Syst Agents Med Chem 2017 ;17(3):201-208

Department of Basic Science, School of Engineering and Technology, Jain University Bangalore. India.

Background: Epilepsy, one of the most frequent neurological afflictions in man characterized by excessive temporary neuronal discharges resulting in uncontrolled convulsion, requires special medical attention. Though several new anticonvulsants are introduced, some types of seizures are still not adequately treated with current therapy. Toxicity, intolerance, and lack of efficacy for certain types of seizure are some of the limitations of the current medications. Read More

Epilepsy Behav Case Rep 2017 21;8:9-11. Epub 2017 Apr 21.

Atkinson Morley Regional Neuroscience Centre, St Georges University Hospitals NHS Foundation Trust, London SW17 0QT, United Kingdom.

Sodium valproate is a commonly used antiseizure drug with broad indications for different seizuretypes and epilepsy syndromes. Well-recognised side effects include weight gain, tremor, dizziness, and unsteadiness. Non-hyperammonaemic parkinsonism, with or without cognitive impairment, is a rare adverse effect of sodium valproate. Read More

JAMA 2017 Jun;317(23):2445-2446

Department of Internal Medicine, University of Texas Southwestern Medical Center, Dallas2Parkland Health and Hospital System, Dallas, Texas.

Curr Drug Metab 2017 Oct;18(8):727-734

Department of pediatrics, BSA Medical College, New Delhi. India.

Background: Neonatal seizures are the most common clinical manifestation of Central Nervous System (CNS) dysfunction and are associated with various neurological sequelae. There are currently no evidence-based guidelines for the management of neonatal seizures and currently used drugs such as phenobarbital, and phenytoin have limited efficacy and potential toxicities. Newer second line anticonvulsant, levetiracetam, has been used in refractory neonatal seizures despite limited data and off-label use. Read More

Biomed Pharmacother 2017 Aug 24;92:240-248. Epub 2017 May 24.

Laboratorio de Sueño y Epilepsia Experimental, Dirección de Investigaciones en Neurociencias, Instituto Nacional de Psiquiatría "Ramón de la Fuente Muñiz", Calz. México-Xochimilco 101, Col. Sn Lorenzo Huipulco, 14370 México, D.F., Mexico. Electronic address:

Justicia spicigera Schltdl. is a vegetal species traditionally used to control epilepsy, but scientific evidence is required to reinforce this activity. The aim of the study was to evaluate the anticonvulsant-like activity of J. Read More

Neurol Sci 2017 Jun 11;38(6):1137-1141. Epub 2017 May 11.

Institute for Neuropathic Pain, Vespuccistraat 64-III, 1056 SN, Amsterdam, The Netherlands.

Phenytoin is an 80-year young molecule and new indications are still emerging. The neuroprotective potential of phenytoin has been evaluated for decades. Recently, a positive phase II trial supported its further development in the treatment of optic neuritis in multiple sclerosis. Read More

Neurobiol Dis 2017 Aug 29;104:41-49. Epub 2017 Apr 29.

Department of Neurology, David Geffen School of Medicine at UCLA, Los Angeles, CA, USA; Epilepsy Research Laboratory (151), Veterans Affairs Greater Los Angeles Healthcare System, Los Angeles, CA, USA; Brain Research Institute, David Geffen School of Medicine at UCLA, Los Angeles, CA, USA.

Early maladaptive internalization of synaptic GABA receptors (GABAR) and externalization of NMDA receptors (NMDAR) may explain the time-dependent loss of potency of standard anti-epileptic drugs (AED) in refractory status epilepticus (SE). We hypothesized that correcting the effects of changes in GABAR and NMDAR would terminate SE, even when treatment is delayed 40 minutes. SE was induced in adult Sprague-Dawley rats with a high dose of lithium and pilocarpine. Read More

Arch Pharm (Weinheim) 2017 Apr 20;350(3-4). Epub 2017 Mar 20.

Department of Medicinal Chemistry, Jagiellonian University Medical College, Kraków, Poland.

The focused library of new amides derived from 3,3-diphenyl-2,5-dioxo-pyrrolidin-1-yl-acetic acid (2a-t) and 3,3-diphenyl-propionic acid (3a-t) as potential anticonvulsant agents was synthesized. The final products were obtained in the amidation reaction of the given carboxylic acid (2, 3) with appropriate secondary amines in the presence of carbonyldiimidazole (CDI) as a coupling reagent. The initial anticonvulsant screening was performed in mice intraperitoneally (i. Read More

Eur J Pharm Sci 2017 May 15;102:264-274. Epub 2017 Mar 15.

CICS-UBI - Health Sciences Research Centre, University of Beira Interior, Av. Infante D. Henrique, 6200-506 Covilhã, Portugal; CNC - Center for Neuroscience and Cell Biology, University of Coimbra, 3004-517 Coimbra, Portugal. Electronic address:

Although significant advances are occurring in epilepsy research, about 30% of epileptic patients are still inadequately controlled by standard drug therapy. For this reason, it continues to be important to develop new chemical entities through which epilepsy could be effectively controlled. In this study, the anticonvulsant activity of forty-two dihydropyrimidin(thi)ones was explored and their efficacy was evaluated in rodents against the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole tests. Read More

Theranostics 2017 5;7(2):425-435. Epub 2017 Jan 5.

State Key Laboratory of Medicinal Chemical Biology and College of Pharmacy, Nankai University, Tianjin, China;; Tianjin Key Laboratory of Molecular Drug Research, Tianjin International Joint Academy of Biomedicine, Tianjin, China.

Phenytoin, an antiepileptic drug, has been widely used for wound healing. Inspired by previous studies, phenytoin silver (PnAg), a sparingly soluble silver nanocompound, was synthesized which exhibited good therapeutic efficacy in tissue repair with low toxicity (LD50 >5 g/kg). In vivo studies showed that PnAg could accelerate dermal wound healing and strong inflammation control in Sprague-Dawley rats (SD rat) and Bama minipigs. Read More

J Mol Neurosci 2017 Apr 22;61(4):553-562. Epub 2017 Feb 22.

Department of Neurology, West China Hospital, Sichuan University, 37th Guoxuexiang Road, Chengdu, Sichuan Province, 610041, China.

The mammalian target of rapamycin (mTOR) has been demonstrated to mediate multidrug resistance in various tumors by inducing P-glycoprotein (P-gp) overexpression. Here, we investigated the correlation between the mTOR pathway and P-gp expression in pharmacoresistant epilepsy. Temporal cortex specimens were obtained from patients with refractory mesial temporal lobe epilepsy (mTLE) and age-matched controls who underwent surgeries at West China Hospital of Sichuan University between June 2014 and May 2015. Read More