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In general these drugs produce stimulant and convulsant effects, and are mainly used for counteracting overdoses of sedative drugs. Examples include bicuculline, securinine and metrazol, and the benzodiazepine GABA A receptor antagonist flumazenil. Other agents which may have GABA A receptor antagonism include the antibiotic ciprofloxacin, [1 ...
A GABA reuptake inhibitor (GRI) is a type of drug which acts as a reuptake inhibitor for the neurotransmitter gamma-Aminobutyric acid (GABA) by blocking the action of the gamma-Aminobutyric acid transporters (GATs). This in turn leads to increased extracellular concentrations of GABA and therefore an increase in GABAergic neurotransmission. [1]
The effect on sodium channels could be of particular relevance for seizure protection. Although topiramate does inhibit high-voltage-activated calcium channels, its relevance to clinical activity is uncertain. Effects on specific GABA-A receptor isoforms could also contribute to the antiseizure activity of the drug.
Pregabalin, sold under the brand name Lyrica among others, is an anticonvulsant, analgesic, and anxiolytic amino acid medication used to treat epilepsy, neuropathic pain, fibromyalgia, restless legs syndrome, opioid withdrawal, and generalized anxiety disorder (GAD).
By the early 1970s, it was appreciated that there are two main classes of GABA receptors, GABA A and GABA B and also that baclofen was an agonist of GABA B receptors. Gabapentin was designed, synthesized and tested in mice by researchers at the pharmaceutical company Goedecke AG in Freiburg, Germany (a subsidiary of Parke-Davis ).
[39] [40] [41] Furosemide has been reported to reversibly antagonize GABA-evoked currents of α 6 β 2 γ 2 receptors at μM concentrations, but not α 1 β 2 γ 2 receptors. [ 39 ] [ 41 ] During development, the α 6 β 2 γ 2 receptor increases in expression in cerebellar granule neurons, corresponding to increased sensitivity to furosemide.
They have largely been replaced by drugs with fewer side effects. SSRIs (selective serotonin reuptake inhibitors), which debuted in the 1980s, work on serotonin.
Vigabatrin is an irreversible mechanism-based inhibitor of gamma-aminobutyric acid aminotransferase (GABA-AT), the enzyme responsible for the catabolism of GABA. Inhibition of GABA-AT results in increased levels of GABA in the brain. [7] [26] Vigabatrin is a racemic compound, and its [S]-enantiomer is pharmacologically active. [27], [28]
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