Subchronic treatment with antiepileptic drugs modifies pentylenetetrazol-induced seizures in mice: Its correlation with benzodiazepine receptor binding

Rocha, Luisa

doi:10.2147/ndt.s2118

Cited by 9 publications

(6 citation statements)

References 49 publications

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“…The exact mechanism of epileptogenic action of pentylenetetrazole is still unclear, but it has been reported that PTZ produces seizures by inhibiting gamma-amino butyric acid (GABA) activity 17 .Due to the enhancement of GABAergic neurotransmission it has been shown to inhibit or attenuate seizure. Whereas the inhibition of GABAergic neurotransmission or activity is known to promote or facilitate seizure 18 .…”

Section: Discussionmentioning

confidence: 99%

Anticonvulsant and Sedative Activities of Extracts of Carissa Carandas Leaves.

Shinde

Gilhotra

Chaudhari³

2018

J. Drug Delivery Ther.

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The present study was carried out to find out the preliminary phytochemical properties, anticonvulsant and sedative activities of the petroleum ether, ethyl acetate and ethanol extract of Carissa carandas leaves. The standard methods were used to screen the preliminary photochemicals present in petroleum ether, ethyl acetate and ethanol extracts of Carissa carandas leaves. The anticonvulsant efficacy of the extracts was determined using pentylenetetrazole (PTZ) in experimental animal models using diazepam as standard drug and the sedative effect was evaluated using pentobarbitone that induced sleep in mice. The efficacy of the extracts was compared against the standard drug Diazepam .The preliminary phytochemical investigation shows presence of alkaloids, glycoside, tannins, terpins . The crude extracts of ethanolic, ethyl acetate and petroleum ether at a dose 400 mg/kg has been found to significantly reduce the extensor and stupor and offer protection against convulsion induced by PTZ. The petroleum ether, ethyl acetate and ethanolic extract found to be non significant at a dose of 100 mg/kg in flexion. It is seen that the crude extracts of ethanolic, ethyl acetate and petroleum ether Of Carissa carandas leaves significantly (p < 0.05) prolonged the time of sodium pentobarbital-induced hypnosis. However, the animal study revealed that the anticonvulsant and sedative activities of Carissa carandas can be used in the treatment of epilepsy.

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Section: Discussionmentioning

confidence: 99%

Anticonvulsant and Sedative Activities of Extracts of Carissa Carandas Leaves.

Shinde

Gilhotra

Chaudhari³

2018

J. Drug Delivery Ther.

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“…[24] The possible mechanism of action of effective drugs may be enhancement of GABAergic neurotransmission such as Phenobarbital, Diazepam and tiagabine. [28] or through T-type calcium (Ca 2+ ) channels like ethosuximide. [29] In the present study, standard drug diazepam (2 mg/kg, i.p .)…”

Section: Discussionmentioning

confidence: 99%

Preliminary Screening of a Classical Ayurvedic Formulation for Anticonvulsant Activity

et al. 2016

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Background:Epilepsy is a serious and complex central nervous system disorder associated with recurrent episodes of convulsive seizures due to the imbalance between excitatory (glutamatergic) and inhibitory (GABAergic) neurotransmitters level in the brain. The available treatments are neither competent to control the seizures nor prevent progress of disease. Since ages, Herbal medicines have remained important sources of medicines in many parts of world which is evidenced through their uses in traditional systems of medicine i.e. Ayurveda, Siddha, Unani, Homeopathy and Chinese etc.Aim:A polyherbal formulation (containing Terminalia chebula Retz., Asparagus racemosus Willd., Embelia ribes Burm. F, Acorus calamus L., Tinospora cordifolia (Willd.) Miers, Convolvulus pluricaulis Choisy, Saussurea lappa C.B.Clarke, Achyranthes aspera L.) is mentioned in Ayurvedic classics Bhaiṣajya Ratnāvali. The aim of the study was to evaluate the anticonvulsant activity of the formulation in Maximum electroshock and Pentylenetetrazole induced convulsions in rats.Materials and Methods:In the present study, a polyherbal formulation was developed as directed by classical text and evaluated for the anticonvulsant activity using Maximal Electroshock Shock (MES) and Pentylenetetrazole (PTZ) induced convulsions in rats. Statistical comparison was done by one way ANOVA followed by the Tukey's multiple comparison test.Results:The obtained results showed that the PHF had a protective role on epilepsy. Treatment with PHF significantly improves antioxidant enzymes activities of superoxide dismutase (SOD) and glutathione (GSH) levels significantly as compared to controls. PHF also significantly decreased malonaldialdehyde (MDA) levels in the brain. Moreover, it also attenuated the PTZ-induced increase in the activity of GABA-T in the rat brain.Conclusion:These findings suggest that PHF might have possible efficacy in the treatment of epilepsy.

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“…Moreover, DRE needs to be carefully distinguished from other causes of therapeutic failure including tolerance development. Repeated administration of ASMs may cause pharmacodynamic or pharmacokinetic tolerance due to alterations in receptors, such as desensitization, downregulation, internalization, uncoupling from their signal transducers, or metabolic enzyme induction with consequent lower drug efficacy 114,115 . Pharmacokinetic studies support that phenytoin, carbamazepine, or phenobarbital upregulate efflux transporters in the brain and peripheral organs, affecting the bioavailability and disposition of ASMs 116 .…”

Section: Potential Mechanisms Of Drementioning

confidence: 99%

“…Repeated administration of ASMs may cause pharmacodynamic or pharmacokinetic tolerance due to alterations in receptors, such as desensitization, downregulation, internalization, uncoupling from their signal transducers, or metabolic enzyme induction with consequent lower drug efficacy. 114,115 Pharmacokinetic studies support that phenytoin, carbamazepine, or phenobarbital upregulate efflux transporters in the brain and peripheral organs, affecting the bioavailability and disposition of ASMs. 116 In this context, it is of interest that administration of ASMs can also result in epigenetic changes that negatively modify the course of the disease or may facilitate excitatory neurotransmission.…”

Section: Dre As a Multifactorial Phenomenonmentioning

confidence: 99%

Revisiting the concept of drug‐resistant epilepsy: A TASK1 report of the ILAE/AES Joint Translational Task Force

Auvin,

Galanopoulou,

Moshé

et al. 2023

Epilepsia

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Despite progress in the development of anti‐seizure medications (ASMs), one third of people with epilepsy have drug‐resistant epilepsy (DRE). The working definition of DRE, proposed by the International League Against Epilepsy (ILAE) in 2010, helped identify individuals who might benefit from presurgical evaluation early on. As the incidence of DRE remains high, the TASK1 workgroup on DRE of the ILAE/American Epilepsy Society (AES) Joint Translational Task Force discussed the heterogeneity and complexity of its presentation and mechanisms, the confounders in drawing mechanistic insights when testing treatment responses, and barriers in modeling DRE across the lifespan and translating across species. We propose that it is necessary to revisit the current definition of DRE, in order to transform the preclinical and clinical research of mechanisms and biomarkers, to identify novel, effective, precise, pharmacologic treatments, allowing for earlier recognition of drug resistance and individualized therapies.

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Subchronic treatment with antiepileptic drugs modifies pentylenetetrazol-induced seizures in mice: Its correlation with benzodiazepine receptor binding

Cited by 9 publications

References 49 publications

Anticonvulsant and Sedative Activities of Extracts of Carissa Carandas Leaves.

Anticonvulsant and Sedative Activities of Extracts of Carissa Carandas Leaves.

Preliminary Screening of a Classical Ayurvedic Formulation for Anticonvulsant Activity

Revisiting the concept of drug‐resistant epilepsy: A TASK1 report of the ILAE/AES Joint Translational Task Force

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