[GABA-ergic antiepileptic drugs: pharmacological action and spectrum of clinical activity of tiababine].
BACKGROUND
GABA is the major inhibitory neurotransmitter in the brain. It is synthesized by the action of glutamic decarboxylase on glutamate and preferently metabolized by the action of GABA transaminase; it experiences neuronal and glial uptake mediated by four types of highly selective transporters.


METHODS
The hypothesis that abnormalities in GABAergic function can be involved in the physiopathology of epilepsy, specially those of partial origin, is supported by data from proceeding from experimental and human epilepsies, as well as by the fact that agents that inhibit GABAergic function exert a proconvulsant action whereas gabaergic agents frequently act as anticonvulsant. On the last years, therefore, substances with gabaergic activity have been investigated as potential antiepileptic drugs.


CONCLUSIONS
Tiagabine, a nipecotic acid derivative, selectively inhibits GABA neuronal and glial uptake by blocking one of its transporters. Its antiepileptic activity has been assessed in different experimental model and it is currently used in the clinical treatment of partial epilepsies.
Pita-Calandre
E
E
Instituto de Neurociencias, Universidad de Granada, España. epita@intersalud.es
D004827:Epilepsy / Q000188:drug therapy*; D018755:GABA Agonists / Q000494:pharmacology* / Q000627:therapeutic use*; D006801:Humans; D009557:Nipecotic Acids / Q000627:therapeutic use*; D000078308:Tiagabine
D018755:GABA Agonists; D009557:Nipecotic Acids; D000078308:Tiagabine