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Gamma-aminobutyric acid (GABA) is an amino acid that functions as the primary inhibitory neurotransmitter in the central nervous system (CNS). GABA is synthesized from the excitatory neurotransmitter glutamate and reduces neuronal excitability by causing neuronal hyperpolarization and decreasing neurotransmitter release. The activity of GABA is regulated by binding through 3 receptors—GABA-A, GABA-B, and GABA-C. GABAergic neurons are located in the hippocampus, thalamus, basal ganglia, hypothalamus, and brainstem. Maintaining a balance between inhibitory neuronal transmission mediated by GABA and excitatory neuronal transmission mediated by glutamate is essential for maintaining cell membrane stability and proper neurological function.[1] Disruption of the balance between glutamate and GABA has a functional role in various pathologies, including traumatic brain injury, Alzheimer disease, epilepsy, schizophrenia, and autism.[1][2] The role of GABA receptors in analgesia is also being investigated.[3][4]

GABA is a crucial inhibitory neurotransmitter in the human brain. Dysfunction in the GABA system can lead to various disease processes, resulting in an imbalance between the GABA and glutamate systems. These conditions may include psychiatric illnesses, dementia, drug dependence or addiction, and drug overdose or toxicity. Many of these conditions can be treated with medications, including GABA agonists. The healthcare team, including primary care providers, nurses, and pharmacists, must possess the necessary knowledge to prescribe and administer these medications safely. Each healthcare team member is responsible for monitoring adverse drug effects and periodically reviewing the indications for these medications to minimize risks. Additionally, healthcare providers should be able to recognize signs and symptoms of toxicity, such as severe sedation or respiratory depression, to ensure prompt diagnosis and treatment.