Anxiolytic potential of resveratrol and rufinamide combination by modulating GABA-ergic transmission: insights from experiments, molecular docking and dynamics simulations
J Physiol Pharmacol. 2023 Oct;74(5). doi: 10.26402/jpp.2023.5.02. Epub 2023 Dec 6.ABSTRACTResveratrol is a polyphenolic phytocompound known to possess anxiolytic-like effects but its impact on central gammaaminobutyric acid (GABA) modulation has never been explored. The purpose of this study was to analyze the anxiolytic-like effects of resveratrol alone and in combination with rufinamide, an antiepileptic drug which has never been studied for its anxiolytic potential. The BALB/c mice were tested in a battery of behavior testing after administration of resveratrol (50 mg/kg) and rufinamide (50 mg/kg) alone and in combinati...
Source: J Physiol Pharmacol - December 12, 2023 Category: Drugs & Pharmacology Authors: A Parveen F Alqahtani S Javaid W Ashraf F Siddique R Rawat M F Rasool T Ahmad F Alasmari I Imran Source Type: research
Anxiolytic potential of resveratrol and rufinamide combination by modulating GABA-ergic transmission: insights from experiments, molecular docking and dynamics simulations
J Physiol Pharmacol. 2023 Oct;74(5). doi: 10.26402/jpp.2023.5.02. Epub 2023 Dec 6.ABSTRACTResveratrol is a polyphenolic phytocompound known to possess anxiolytic-like effects but its impact on central gammaaminobutyric acid (GABA) modulation has never been explored. The purpose of this study was to analyze the anxiolytic-like effects of resveratrol alone and in combination with rufinamide, an antiepileptic drug which has never been studied for its anxiolytic potential. The BALB/c mice were tested in a battery of behavior testing after administration of resveratrol (50 mg/kg) and rufinamide (50 mg/kg) alone and in combinati...
Source: Journal of Physiology and Pharmacology - December 12, 2023 Category: Drugs & Pharmacology Authors: A Parveen F Alqahtani S Javaid W Ashraf F Siddique R Rawat M F Rasool T Ahmad F Alasmari I Imran Source Type: research
Molecules, Vol. 28, Pages 7830: Simple HPLC-UV Method for Therapeutic Drug Monitoring of 12 Antiepileptic Drugs and Their Main Metabolites in Human Plasma
The objective of the present report was to develop and validate a simple, selective, and reproducible high-performance liquid chromatography method with UV detection suitable for routine therapeutic drug monitoring of the most commonly used antiepileptic drugs and some of their metabolites. Simple precipitation of plasma proteins with acetonitrile was used for sample preparation. 10,11-dihydrocarbamazepine was used as an internal standard. Chromatographic separation of the analytes was achieved by gradient elution on a Phenyl–Hexyl column at 40 °C, using methanol and potassium phosphate buffer (25...
Source: Molecules - November 28, 2023 Category: Chemistry Authors: Daniela Milosheska Robert Ro škar Tags: Article Source Type: research
Proposed Anti-Seizure Medication Combinations With Rufinamide in the Treatment of Lennox-Gastaut Syndrome: Narrative Review and Expert Opinion
First described in the mid-20th century, Lennox-Gastaut syndrome (LGS) is a severe, chronic, and complex form of epilepsy with symptoms including multiple seizure types, interictal generalized slow ( ≤2.5 Hz) spike-and-wave activity on electroencephalography (EEG), and impaired cognition [1–3]. Onset occurs typically in early childhood, most often between the ages of 3 and 5 years, and persists into adolescence and adulthood [2,4]. Many different etiologies can lead to LGS, including cerebra l anomalies, perinatal cerebral anoxia or asphyxia, tuberous sclerosis, acute encephalitis, and head injury, and may involve pre-...
Source: Seizure: European Journal of Epilepsy - May 24, 2023 Category: Neurology Authors: Raman Sankar, Michael Chez, J. Eric Pina-Garza, Tracy Dixon-Salazar, J. Robert Flamini, Ann Hyslop, Patricia McGoldrick, John J. Millichap, Trevor Resnick, Jong M. Rho, Steven Wolf Tags: Review Source Type: research
Current and emerging pharmacotherapy for the treatment of Lennox-Gastaut syndrome
Expert Opin Pharmacother. 2023 May 22. doi: 10.1080/14656566.2023.2215924. Online ahead of print.ABSTRACTINTRODUCTION: Lennox-Gastaut syndrome (LGS) is a severe childhood-onset epileptic encephalopathy, characterised by multiple seizure types, generalised slow spike-and-wave complexes on the EEG, and cognitive impairment. Seizures in LGS are typically resistant to treatment with antiseizure medications (ASMs). Tonic/atonic ("drop") seizures are of particular concern, due to their liability to cause physical injury.AREAS COVERED: We summarise evidence for current and emerging ASMs for the treatment of seizures in LGS. The r...
Source: Expert Opinion on Pharmacotherapy - May 22, 2023 Category: Drugs & Pharmacology Authors: Frank M C Besag Michael J Vasey Richard F M Chin Source Type: research
Molecules, Vol. 27, Pages 7784: Mechanochemical Approach towards Multi-Functionalized 1,2,3-Triazoles and Anti-Seizure Drug Rufinamide Analogs Using Copper Beads
Oleg N. Chupakhin
Highly regiospecific, copper-salt-free and neat conditions have been demonstrated for the 1,3-dipolar azide-alkyne cycloaddition (AAC) reactions under mechanochemical conditions. A group of structurally challenging alkynes and heterocyclic derivatives was efficiently implemented to achieve highly functionalized 1,4-disubstituted-1,2,3-triazoles in good to excellent yield by using the Cu beads without generation of unwanted byproducts. Furthermore, the high-speed ball milling (HSBM) strategy has also been extended to the synthesis of the commercially available pharmaceutical agent, Rufinamide, an ant...
Source: Molecules - November 11, 2022 Category: Chemistry Authors: Dhananjay Bhattacherjee Igor S. Kovalev Dmitry S. Kopchuk Matiur Rahman Sougata Santra Grigory V. Zyryanov Pralay Das Rituraj Purohit Vladimir L. Rusinov Oleg N. Chupakhin Tags: Article Source Type: research
Psychobehavioural and Cognitive Adverse Events of Anti-Seizure Medications for the Treatment of Developmental and Epileptic Encephalopathies
AbstractThe developmental and epileptic encephalopathies encompass a group of rare syndromes characterised by severe drug-resistant epilepsy with onset in childhood and significant neurodevelopmental comorbidities. The latter include intellectual disability, developmental delay, behavioural problems including attention-deficit hyperactivity disorder and autism spectrum disorder, psychiatric problems including anxiety and depression, speech impairment and sleep problems. Classical examples of developmental and epileptic encephalopathies include Dravet syndrome, Lennox –Gastaut syndrome and tuberous sclerosis complex. The ...
Source: CNS Drugs - October 4, 2022 Category: Neurology Source Type: research
Discovery of Triazenyl Triazoles as Na < sub > v < /sub > 1.1 Channel Blockers for Treatment of Epilepsy
Bioorg Med Chem Lett. 2022 Aug 16:128946. doi: 10.1016/j.bmcl.2022.128946. Online ahead of print.ABSTRACTThe voltage-gated sodium (Nav) channel is one of most important targets for treatment of epilepsy, and rufinamide is an approved third-generation anti-seizure drug as Nav1.1 channel blocker. Herein, by triazenylation of rufinamide, we reported the triazenyl triazoles as new Nav1.1 channel blocker for treatment of epilepsy. Through the electrophysiological activity assay, compound 6a and 6e were found to modulate the inactivation voltage of Nav 1.1 channel with shift of -10.07 mv and -11.28 mV, respectively. In the penty...
Source: Bioorganic and Medicinal Chemistry Letters - August 19, 2022 Category: Chemistry Authors: Xianjing Zhou Linwei Zeng Yi Wang Cenglin Xu Zhong Chen Sunliang Cui Source Type: research
Discovery of Triazenyl Triazoles as Na < sub > v < /sub > 1.1 Channel Blockers for Treatment of Epilepsy
Bioorg Med Chem Lett. 2022 Aug 16:128946. doi: 10.1016/j.bmcl.2022.128946. Online ahead of print.ABSTRACTThe voltage-gated sodium (Nav) channel is one of most important targets for treatment of epilepsy, and rufinamide is an approved third-generation anti-seizure drug as Nav1.1 channel blocker. Herein, by triazenylation of rufinamide, we reported the triazenyl triazoles as new Nav1.1 channel blocker for treatment of epilepsy. Through the electrophysiological activity assay, compound 6a and 6e were found to modulate the inactivation voltage of Nav 1.1 channel with shift of -10.07 mv and -11.28 mV, respectively. In the penty...
Source: Bioorganic and Medicinal Chemistry Letters - August 19, 2022 Category: Chemistry Authors: Xianjing Zhou Linwei Zeng Yi Wang Cenglin Xu Zhong Chen Sunliang Cui Source Type: research
COVID-19 and antiepileptic drugs: an approach to guide practices when nirmatrelvir/ritonavir is co-prescribed
AbstractManagement and dose adjustment are a major concern for clinicians in the absence of specific clinical outcome data for patients on antiepileptic drugs (AEDs), in the event of short-term (5 days) nirmatrelvir/ritonavir co-exposure. Therefore, in this report, we identified drugs that require dose adjustment because of drug-drug interactions (DDIs) between nirmatrelvir/ritonavir and AEDs. We hereby used four databases (Micromedex Drug Interaction,Liverpool Drug Interaction Group for COVID-19 Therapies,Medscape Drug Interaction Checker, andLexicomp Drug Interactions) andDDI-Predictor.In the light of applying theDDI-P...
Source: European Journal of Clinical Pharmacology - August 5, 2022 Category: Drugs & Pharmacology Source Type: research
Antiseizure Drugs and Movement Disorders
AbstractThe relationship between antiseizure drugs and movement disorders is complex and not adequately reviewed so far. Antiseizure drugs as a treatment for tremor and other entities such as myoclonus and restless leg syndrome is the most common scenario, although the scientific evidence supporting their use is variable. However, antiseizure drugs also represent a potential cause of iatrogenic movement disorders, with parkinsonism and tremor the most common disorders. Many other antiseizure drug-induced movement disorders are possible and not always correctly identified. This review was conducted by searching for all the ...
Source: CNS Drugs - July 21, 2022 Category: Neurology Source Type: research
Therapeutic Drug Monitoring for Rufinamide in Japanese Patients With Epilepsy: Focus on Drug Interactions, Tolerability, and Clinical Effectiveness
Conclusions:
Therapeutic drug monitoring for rufinamide is clinically useful for predicting drug interactions between rufinamide and concomitant AEDs. When a patient has tonic/atonic seizures, careful titration is required for concentrations greater than 20 mcg/mL. (Source: Therapeutic Drug Monitoring)
Source: Therapeutic Drug Monitoring - July 20, 2022 Category: Drugs & Pharmacology Tags: Original Article Source Type: research
An Investigation of the Effects of Chronic Zonisamide, Sultiam, Lacosamide, Clobazam, and Rufinamide Antiseizure Drugs on Foliculogenesis in Ovarian Tissue in Prepubertal Non-Epileptic Rats
Int J Dev Neurosci. 2022 Jun 9. doi: 10.1002/jdn.10200. Online ahead of print.ABSTRACTWe aimed to determine the morphological and histological effects of zonisamide, sultiam, lacosamide, clobazam, and rufinamide on ovarian folliculogenesis in rats. Sixty female Wistar rats were equally divided into 6 experimental groups, including control group, zonisamide, sultiam, lacosamide, clobazam, and rufinamide were administered by gavage for 90 days. According to the daily vaginal smears of the rats in the proestrus and diester phases of the estrus cycle, their ovaries were removed and placed in the fixation solution. Immunohistoc...
Source: International Journal of Developmental Neuroscience - June 9, 2022 Category: Neuroscience Authors: P ınar Özkan Kart Seren G ülşen Gürgen G ülnur Esenülkü Beril Dilber Nihal Y ıldız U ğur Yazar Hayrunnisa Ye şil Sarsmaz Ali Samet Topsakal T ülay Kamaşak Elif Acar Arslan Sevim Şahin Ali Cansu Source Type: research
