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1.
Farmakol Toksikol ; 43(3): 296-9, 1980.
Artigo em Russo | MEDLINE | ID: mdl-7192642

RESUMO

Among the drugs of the benzodiazepine series, clonazepam shows the highest anticonvulsant activity in experiments on mice and rats. It has the highest activity and selectivity of action according to the subcutaneous antipentylene tetrazol and antithiose-micarbazid tests. Administration of increased doses of clonazepam results in potentiation of its tranquilizing, antiaggressive and sedative effects. The tranquilizing effect exhibited by clonazepam in the conflict situation is similar to that exerted by diazepam. The sedative effect of clonazepam on Müller's labyrinth is more potent compared to diazepam. Unlike diazepam metabolites, that show high activity in experiments, the products of clonazepam biotransformation are less potent.


Assuntos
Benzodiazepinonas/farmacologia , Clonazepam/farmacologia , Diazepam/farmacologia , Agressão/efeitos dos fármacos , Animais , Anticonvulsivantes , Biotransformação/efeitos dos fármacos , Clonazepam/metabolismo , Conflito Psicológico , Diazepam/metabolismo , Antagonismo de Drogas , Humanos , Masculino , Camundongos , Relaxamento Muscular/efeitos dos fármacos
2.
Farmakol Toksikol ; 38(3): 277-81, 1975.
Artigo em Russo | MEDLINE | ID: mdl-1227900

RESUMO

Correlation between the dynamics of triftazine (stelazine, trifluoperazine) distribution in the brain, liver, and blood plasma of rats and the dynamics marking the development of cataleptic and antiagressive effects and also upset motor conditionation was studied. It was found that following oral administration of triftazine it slowly reaches the organs, the greatest part being adsorbed in the liver. On the contrary, of its intramuscular administration is characteristic a quicker accumulation in the organs and then the level of the neuroleptic in the brain and plasma is higher and in the liver - lower than with its oral introduction. A dissimilar dynamics of triftazine in the brain explains the difference of its pharmacological effects with diverse modes of administration. When given by mouth the content of the drug in the brain is insignificant and it rises but slowly, this being matched by a correspondingly slow development of the effects of triftazine. With the intramuscular route of introduction the neuroleptic's content in the brain rapidly reaches a high level, while its pharmacological effects are characterized by a quicker development than this is the case with its oral administration.


Assuntos
Trifluoperazina/metabolismo , Administração Oral , Animais , Sangue/metabolismo , Encéfalo/metabolismo , Injeções Intramusculares , Cinética , Fígado/metabolismo , Masculino , Ratos , Fatores de Tempo , Trifluoperazina/administração & dosagem , Trifluoperazina/farmacologia
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