Comparative Anticonvulsive Action of 3,5,5-trimethyloxazolidine-2,4-dione (Tridione), Dilantin and Phenobarbital

Everett, G. M.; Richards, R. K.

doi:10.1097/00000542-194507000-00047

Cited by 25 publications

(28 citation statements)

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“…4 s previously described above, clonazepam and valproic acid possess anxiolytic properties in behavioral conflict paradigms. The barbiturate phenobarbital is both an effective anticonvulsant [Everett and Richards, 1944;Costa et al, 19751 and a disinhibitory agent in conflict-induced suppression models [Geller and Seifter, 1960;Cook and Davidson, 19731. Recent evidence suggests that the effects of barbiturates may be mediated by facilitation of GABA-ergic transmission at the picrotoxinin/barbiturate site on the benzodiazepine-GABA receptor-ionophore complex [Olsen, 1981;Haefely and Polc, 1983;Rastogi and Ticku, 19861.…”

Section: Discussionmentioning

confidence: 99%

“…Recent evidence suggests that the effects of barbiturates may be mediated by facilitation of GABA-ergic transmission at the picrotoxinin/barbiturate site on the benzodiazepine-GABA receptor-ionophore complex [Olsen, 1981;Haefely and Polc, 1983;Rastogi and Ticku, 19861. And finally, trimethadione, which was approximately 80 times less potent than chlordiazepoxide in its ability to antagonize yohimbine-induced seizures, has also shown weak anticonvulsant activity in a variety of convulsant procedures [Everett and Richards, 1944;Swinyard and Castellion, 19661, as well as anxiolytic effects in the Geller and Seifter conflict and pentylenetetrazol discrimination procedures [Bennett et al, 19821. Although the mechanism of action for the anxiolytic activity of trimethadione is not known, it may produce its antianxiety effects by potentiation of GABA effects [Bennett et al, 19821. The antiepileptics that were inactive in the yohimbine-induced seizure model included diphenylhydantoin, ethosuximide, and carbamazepine.…”

Section: Discussionmentioning

confidence: 99%

“…Although the mechanism of action for the anxiolytic activity of trimethadione is not known, it may produce its antianxiety effects by potentiation of GABA effects [Bennett et al, 19821. The antiepileptics that were inactive in the yohimbine-induced seizure model included diphenylhydantoin, ethosuximide, and carbamazepine. Whereas these agents are effective to varying degrees against seizures induced by maximal electroshock, only ethosuximide and carbamazepine are effective against seizures induced by pentylenetetrazol or other chemical convulsants [Everett and Richards, 1944;Goodman et al, 1953;Swinyard and Castellion, 1966;Ferrendelli and Klunk, 1982;Woodbury, 1982;Schmutz, 19851. However, all three compounds lack anxiolytic activity in the Geller-Seifter conflict procedure (unpublished observations).…”

Section: Discussionmentioning

confidence: 99%

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Yohimbine‐induced seizures in mice: A model predictive of potential anxiolytic and GABA‐mimetic agents

Dunn¹,

Fielding²

1987

Drug Development Research

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Dunn, R.W., and S. Fielding: Yohimbine-induced seizures in mice: A model predictive of potential anxiolytic and GABA-mimetic agents. Drug Dev. Res. 10:177-188, 1987.Yohimbine potentiation of lethality in mice has been used as a model for the prediction of antidepressant agents [Quinton, 19631. However, prior to death or at sublethal doses, yohimbine induces clonic convulsions. In Swiss-Webster mice (20-28 g) individually placed in clear plastic cylinders, the CD5o (median convulsive dose) for yohimbine-induced seizures was 22.7 (18.9-27.3) mglkg sc (subcutaneously). For anticonvulsant screening, compounds were administered intraperitoneally at appropriate pretreatment times prior to the CDg5 dose of yohimbine (45 mglkg sc). The following anxiolytic and GABA-mimetic agents administered intraperitoneally dose-dependently antagonized yohimbine-induced clonic convulsions: diazepam (ED50 = 0.26 mglkg); chlordiazepoxide (2.0 mglkg); CGS 9896 (0.82 mglkg); CL 218,872 (3.7 mglkg); zopiclone (19.0 mglkg); tracazolate (61.3 mg/ kg); clonazepam (0.02 mg/kg); phenobarbital (9.0 mglkg); valproic acid (81.1 mglkg); trimethadione (163.0 mglkg); muscimol (0.82 mglkg); AOAA (16.0 mglkg); clonidine (0.22 mg/kg); and baclofen (4.0 mglkg). On the other hand, the antiepileptic agents diphenylhydantoin, ethosuximide, and carbamazepine as well as the benzodiazepine antagonists CGS 8216 and RO 15 1788 were inactive. The neuroleptics haloperidol, chlorpromazine, and thioridazine were inactive, while clozapine displayed anticonvulsant activity (ED50 = 30.7 mglkg). Other inactive compounds include phenotolamine, propranolol, atropine, alpha-methyltyrosine, PCPA, reserpine, buspirone, DMI, and imipramine. Since yohimbine has been reported to be anxiogenic in animals and man, this assay may be relevant for

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

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Yohimbine‐induced seizures in mice: A model predictive of potential anxiolytic and GABA‐mimetic agents

Dunn¹,

Fielding²

1987

Drug Development Research

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“…Everett and Richards (1944) demonstrated that both trimethadione and phenobarbital, but not phenytoin (PHT), were able to block seizures induced by the GABA A -receptor antagonist PTZ. Soon thereafter, Lennox (1945) demonstrated that trimethadione was effective at attenuating petit mal (i.e., absence epilepsy) attacks but was ineffective intreating or worsening grand mal seizures (i.e., generalized tonic-clonic seizures).…”

Section: The Mes and Ptz Testsmentioning

confidence: 99%

Plants with anticonvulsant properties: a review

Júnior¹,

Almeida²,

Lima³

et al. 2008

Rev. bras. farmacogn.

107

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RESUMO: "Uma revisão de plantas com propriedades anticonvulsivantes". Cerca de um terço dos pacientes epilépticos não conseguem ter um tratamento adequado com as drogas anticonvulsivantes atuais. Nesse sentido, as plantas medicinais surgem como uma fonte promissora de novas moléculas químicas com propriedades biológicas apreciáveis. Muitas plantas ou produtos de origem naturais têm sido propostos para o tratamento de várias patologias, tais como: epilepsia, diabetes, ansiedade, depressão, dentre outras. O presente trabalho realizou um extenso levantamento na literatura especializada de plantas medicinais com propriedades anticonvulsivantes. Um total de 355 espécies vegetais foi identifi cado, sendo 16 plantas encontradas na fl ora brasileira, com indicação para o tratamento de quadros convulsivos. Características como nome da espécie, família, partes utilizadas, país do estudo e /ou publicação, métodos e referências foram sumarizados. Além disso, os principais apectos dos modelos animais mais utilizados no estudo de plantas/substâncias com propriedades anticonvulsivantes foram revisados. Mais de 170 referências foram consultadas.Unitermos: Plantas medicinais, Produtos naturais, convulsão, atividade anticonvulsivante, modelos animais, revisão. ABSTRACT:Seizures are resistant to treatment with currently available anticonvulsant drugs in about 1 out of 3 patients with epilepsy. Thus, there is a need for new, more effective anticonvulsant drugs for intractable epilepsy. However, nature is a rich source of biological and chemical diversity and a number of plants in the world have been used in traditional medicine remedies, i.e., anticonvulsant, anxiolytic, analgesic, antidepressant. This work constitutes a literature review on medicinal plants showing anticonvulsant properties. The review refers to 16 Brazilian plants and a total 355 species, their families, geographical distribution, the utilized parts, method and references. Some aspects of research on medicinal plants and a brief review of the most common animal models to discover antiepileptic drugs are discussed. For this purpose over 170 references were consulted.

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“…Its anticonvulsant effects in animals were reported in the same year [52], and in human subjects by 1946 [53][54][55][56][57]. It was licensed for therapy in 1946 (Fig.…”

Section: Trimethadione (Tridione)mentioning

confidence: 99%

Frontmatter

2004

The Treatment of Epilepsy

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Comparative Anticonvulsive Action of 3,5,5-trimethyloxazolidine-2,4-dione (Tridione), Dilantin and Phenobarbital

Cited by 25 publications

References 0 publications

Yohimbine‐induced seizures in mice: A model predictive of potential anxiolytic and GABA‐mimetic agents

Yohimbine‐induced seizures in mice: A model predictive of potential anxiolytic and GABA‐mimetic agents

Plants with anticonvulsant properties: a review

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