Several New Diverse Anticonvulsant Agents Discovered in a Virtual Screening Campaign Aimed at Novel Antiepileptic Drugs to Treat Refractory Epilepsy
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Abstract:
A virtual screening campaign was conducted in order to discover new anticonvulsant drug candidates for the treatment of refractory epilepsy. To this purpose, a topological discriminant function to identify antiMES drugs and a sequential filtering methodology to discriminate P-glycoprotein substrates and nonsubstrates were jointly applied to ZINC 5 and DrugBank databases. The virtual filters combine an ensemble of 2D classifiers and docking simulations. In the light of the results, 10 structurally diverse compounds were acquired and tested in animal models of seizure and the rotorod test. All 10 candidates showed some level of protection against MES test.Keywords:
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Anticonvulsant effects of bilobalide, one of the constituents of Ginkgo biloba L., on the convulsions induced by 4-O-methylpyridoxine (MPN) were investigated in mice. Bilobalide reduced the duration and incidence of MPN-induced convulsions depending on its dose and the period of treatment. In addition, the anticonvulsant effect was manifested more than 24 hours after treatment and the effect lasted for 7 days after its withdrawal. In mice treated with bilobalide (30 mg/kg, p.o., once a day for 4 days), hepatic 7-methoxycoumarin O-demethylase activity was potentiated, and the disappearance of MPN in blood after MPN injection was faster than in controls. From these results, it is assumed that the anticonvulsant effect of bilobalide against convulsions induced by MPN partly involves modulation of hepatic drug-metabolizing enzyme activity, which leads to accelerated elimination of MPN.
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Levetiracetam is an antiepileptic drug with novel antiepileptic mechanism,in which binding to SV2A,a synaptic vesicle protein,may result in its anticonvulsant activity.Here we review the efficacy and safety of levetiracetam monotherapy in treating several types of epilepsy,including newly diagnosed epilepsy, partial epilepsy,generalized epilepsy,etc.
Levetiracetam
Antiepileptic drug
Generalized epilepsy
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Anticonvulsant drugs
Antiepileptic drug
Tiagabine
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A virtual screening campaign was conducted in order to discover new anticonvulsant drug candidates for the treatment of refractory epilepsy. To this purpose, a topological discriminant function to identify antiMES drugs and a sequential filtering methodology to discriminate P-glycoprotein substrates and nonsubstrates were jointly applied to ZINC 5 and DrugBank databases. The virtual filters combine an ensemble of 2D classifiers and docking simulations. In the light of the results, 10 structurally diverse compounds were acquired and tested in animal models of seizure and the rotorod test. All 10 candidates showed some level of protection against MES test.
DrugBank
Antiepileptic drug
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Summary: Noncompliance is a major factor in suboptimal control of epileptic seizures. As many as one‐third to one‐half of persons with epilepsy may be noncompliant. Noncompliance negates the usefulness of the advances made in the diagnosis and treatment of epilepsy and is perhaps the single most important factor in increasing the costs of care for people with epilepsy. Although the issue of noncompliance is very complex, realization that it is a multidimensional problem and varies from patient to patient should help individualize its evaluation and approach. Noncompliance can be described by three dimensions: behavior, extent, and intentianality. The simplest methods for determining noncompliance are measurements of the antiepileptic drug concentration and patient interview. Calculation of a coefficient of variation for serial anticonvulsant drug levels may be more descriptive, however. Education and devices to simplify dosing are the primary strategies for improving compliance.
Antiepileptic drug
Patient Compliance
Drug compliance
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The clinical management of 242 patients receiving anticonvulsant drugs in a general population of over 75,000 patients in Northern Ireland was reviewed.The prevalence of treated epilepsy was 3.99 per 1,000 population. There were differences in the classification of epilepsy recorded by the general practitioners and an independent epileptologist. In particular, partial epilepsy was under-recorded by the general practitioners. Comparisons between drug dose, type of epilepsy, frequency of fits and antiepileptic drug serum levels were difficult to make. There was, however, evidence of inadequate or inappropriate antiepileptic medication. There were also problems with compliance: 23 per cent of patients had deliberately stopped taking their medication, nearly half of them for over a month at a time.
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Repurposing
Drug repositioning
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Antiepileptic drug
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Aim. To conduct a comparative clinical analysis of the effectiveness of treatment with different generations of antiepileptic drugs in children with focal forms of epilepsy. Methods. Examined were 96 patients aged from one month to 17 years with focal forms of epilepsy treated with antiepileptic drugs of different generations (phenobarbital, topiramate or lamotrigine). Results. Positive results in the treatment (complete relief of seizures or reduction of their frequency by 50% or more) was achieved in 87% of patients receiving topiramate, in 71% lamotrigine and in 38% -phenobarbital. Conclusions. New antiepileptic drugs topiramate and lamotrigine showed a higher efficacy in the treatment of focal forms of epilepsy in children than phenobarbital.
Phenobarbital
Antiepileptic drug
Epilepsy in children
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