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

Study of the metabolic stability profiles of perampanel, rufinamide and stiripentol and prediction of drug interactions using HepaRG cells as an in vitro human model
Toxicol In Vitro. 2022 May 18:105389. doi: 10.1016/j.tiv.2022.105389. Online ahead of print.ABSTRACTNew-generation antiepileptic drugs as perampanel, rufinamide and stiripentol emerged as alternatives in chronic epilepsy polytherapy. Hence, their metabolic stability and potential involvement in relevant drug-drug interactions (DDI) are of great clinical interest, being HepaRG cells herein used as an in vitro human model. To characterize their metabolic stability profiles, HepaRG cells were incubated with perampanel (1 μM), rufinamide (100 μM) or stiripentol (5 μM) for 12-h. HepaRG cells, pretreated with known CYP450 iso...
Source: Toxicology in Vitro - May 21, 2022 Category: Toxicology Authors: Sara Meirinho M árcio Rodrigues Ana Fortuna Am ílcar Falcão Gilberto Alves Source Type: research

Study of the metabolic stability profiles of perampanel, rufinamide and stiripentol and prediction of drug interactions using HepaRG cells as an in vitro human model
Toxicol In Vitro. 2022 May 18:105389. doi: 10.1016/j.tiv.2022.105389. Online ahead of print.ABSTRACTNew-generation antiepileptic drugs as perampanel, rufinamide and stiripentol emerged as alternatives in chronic epilepsy polytherapy. Hence, their metabolic stability and potential involvement in relevant drug-drug interactions (DDI) are of great clinical interest, being HepaRG cells herein used as an in vitro human model. To characterize their metabolic stability profiles, HepaRG cells were incubated with perampanel (1 μM), rufinamide (100 μM) or stiripentol (5 μM) for 12-h. HepaRG cells, pretreated with known CYP450 iso...
Source: Toxicology in Vitro - May 21, 2022 Category: Toxicology Authors: Sara Meirinho M árcio Rodrigues Ana Fortuna Am ílcar Falcão Gilberto Alves Source Type: research

Impact of Antiseizure Medications on Appetite and Weight in Children
AbstractThere are numerous potential factors that may affect growth in children with epilepsy, and these must be evaluated in any child with appetite and weight concerns. Antiseizure medications (ASMs) have potential adverse effects, and many may affect appetite, thus impacting normal growth and weight gain. The aim of this review is to focus on the impact of both epilepsy and ASMs on appetite and weight in children. We systematically reviewed studies using Medline assessing the impact of ASMs on appetite and weight in children. Eligible studies included randomized controlled trials and open-label studies (open-label exten...
Source: Pediatric Drugs - May 21, 2022 Category: Pediatrics Source Type: research

Impact of Antiseizure Medications on Appetite and Weight in Children
Paediatr Drugs. 2022 May 21. doi: 10.1007/s40272-022-00505-2. Online ahead of print.ABSTRACTThere are numerous potential factors that may affect growth in children with epilepsy, and these must be evaluated in any child with appetite and weight concerns. Antiseizure medications (ASMs) have potential adverse effects, and many may affect appetite, thus impacting normal growth and weight gain. The aim of this review is to focus on the impact of both epilepsy and ASMs on appetite and weight in children. We systematically reviewed studies using Medline assessing the impact of ASMs on appetite and weight in children. Eligible st...
Source: Paediatric Drugs - May 20, 2022 Category: Pediatrics Authors: Ersida Buraniqi Hicham Dabaja Elaine C Wirrell Source Type: research

Impact of Antiseizure Medications on Appetite and Weight in Children
Paediatr Drugs. 2022 May 21. doi: 10.1007/s40272-022-00505-2. Online ahead of print.ABSTRACTThere are numerous potential factors that may affect growth in children with epilepsy, and these must be evaluated in any child with appetite and weight concerns. Antiseizure medications (ASMs) have potential adverse effects, and many may affect appetite, thus impacting normal growth and weight gain. The aim of this review is to focus on the impact of both epilepsy and ASMs on appetite and weight in children. We systematically reviewed studies using Medline assessing the impact of ASMs on appetite and weight in children. Eligible st...
Source: Paediatric Drugs - May 20, 2022 Category: Pediatrics Authors: Ersida Buraniqi Hicham Dabaja Elaine C Wirrell Source Type: research

Impact of Antiseizure Medications on Appetite and Weight in Children
Paediatr Drugs. 2022 May 21. doi: 10.1007/s40272-022-00505-2. Online ahead of print.ABSTRACTThere are numerous potential factors that may affect growth in children with epilepsy, and these must be evaluated in any child with appetite and weight concerns. Antiseizure medications (ASMs) have potential adverse effects, and many may affect appetite, thus impacting normal growth and weight gain. The aim of this review is to focus on the impact of both epilepsy and ASMs on appetite and weight in children. We systematically reviewed studies using Medline assessing the impact of ASMs on appetite and weight in children. Eligible st...
Source: Paediatric Drugs - May 20, 2022 Category: Pediatrics Authors: Ersida Buraniqi Hicham Dabaja Elaine C Wirrell Source Type: research