Possible Interaction: Gamma-Aminobutyric Acid and Anti-Anxiety Agents

“Abstract Anxiolytics and anticonvulsants generally positively modulate the action of GABA , whereas many convulsants (including the chloride channel blocker picrotoxinin) negatively modulate the action of GABA on GABAA receptors.”

“The fast inhibitory actions of GABA are mediated by GABA type A receptors (GABA(A)Rs); they mediate both phasic and tonic inhibition in the brain and are the principle sites of action for anticonvulsant, anxiolytic , and sedative-hypnotic agents that include benzodiazepines, barbiturates, neurosteroids, and some general anesthetics.”

“Benzodiazepine (BZ) anxiolytics mediate their clinical effects by enhancing the effect of gamma-aminobutyric acid (GABA) at the GABA-A receptor.”

“These results support the hypothesis that GABA and endogenous anxiolytics mutually facilitate modulation of anxiety.”

“Benzodiazepines (BZs), which are typically used as anxiolytics , act by modulating inhibitory signaling through gamma-aminobutyric acid A (GABA)(A) receptors.”

“They act primarily through inhibiting the GABA system , their anxiolytic and sedative effects are of primary importance from the psychiatric aspect.”

“Abrupt cessation of anxiolytic treatment might therefore lead to an acute reduction in GABA function ; this change could underlie the severe symptoms associated with tranquilliser withdrawal.”

“ Anxiolytic plants may interact with either glutamic acid decarboxylase (GAD) or GABA transaminase (GABA-T) and ultimately influence brain GABA levels and neurotransmission.”

“There are a number of reports that the behavioral actions of anxiolytics can be antagonised by GABA antagonists such as bicuculline or picrotoxin but there are many contradictory findings and these drugs are difficult to use effectively in behavioral studies.”

“An anxiolytic profile (substitution for CDP and antagonism of PTZ) was associated with GABA ratios of about 2, and an anxiogenic profile with GABA ratios less than 1.”