GABA, the major inhibitory neurotransmitter in the central nervous system, plays a key role in maintaining normal brain function. Therefore, any alteration in GABAergic transmission will result in the development of numerous psychiatric and neurological disorders. The aim of this master's thesis was to describe the role of the most important medications that act on different elements of GABA synapse. Given the fact that GABA exerts its effects via GABAA receptors, many clinically important drugs are thouse that achieve their specific therapeutic action by targeting GABAA receptor complex. Of particular importance are benzodiazepines, barbiturates and Z-drugs which are used for numerous indications, including anxiety, insomnia, muscle relaxation and epilepsy. Despite numerous studies conducted over the last fifty years ago, there is still a growing interest in exploring GABA system in health and disease with the aim of fully unlocking its therapeutic potential. Some of these experiments had resulted in the discovery of molecules which proved to be valuable for novel indications such as brexanolone which received its approval in 2019., becoming the first drug to be specifically approved for postpartum depression. The discovery of anxyiolytic potential of curcumol for the rhizome of Curcuma loga L. (Zingiberaceae) had resulted in an increased number of testing other natural compounds that will be as therapeutically active as benzodiazepines, the most widely udes class of GABA modulators, but without undesirable side effects, especially those associated with their long-term administration.