The role of the GABAergic system on insomnia

Peeraporn Varinthra; Shameemun Naseer Mohamed Nizarul Anwar; Shu-Ching Shih; Ingrid Y Liu

doi:10.4103/tcmj.tcmj_243_23

The role of the GABAergic system on insomnia

Tzu Chi Med J. 2024 Mar 26;36(2):103-109. doi: 10.4103/tcmj.tcmj_243_23. eCollection 2024 Apr-Jun.

Authors

Peeraporn Varinthra¹, Shameemun Naseer Mohamed Nizarul Anwar², Shu-Ching Shih³, Ingrid Y Liu¹

Affiliations

¹ Institute of Medical Sciences, Tzu Chi University, Hualien, Taiwan.
² Department of Biotechnology, School of Bioengineering, College of Engineering and Technology, SRM Institute of Science and Technology, Kattankulathur, Tamil Nadu, India.
³ Department of Molecular Biology and Human Genetics, Tzu Chi University, Hualien, Taiwan.

Abstract

Sleep is an essential activity for the survival of mammals. Good sleep quality helps promote the performance of daily functions. In contrast, insufficient sleep reduces the efficiency of daily activities, causes various chronic diseases like Alzheimer's disease, and increases the risk of having accidents. The GABAergic system is the primary inhibitory neurotransmitter system in the central nervous system. It transits the gamma-aminobutyric acid (GABA) neurotransmitter via GABA_A and GABA_B receptors to counterbalance excitatory neurotransmitters, such as glutamate, noradrenaline, serotonin, acetylcholine, orexin, and dopamine, which release and increase arousal activities during sleep. Several studies emphasized that dysfunction of the GABAergic system is related to insomnia, the most prevalent sleep-related disorder. The GABAergic system comprises the GABA neurotransmitter, GABA receptors, GABA synthesis, and degradation. Many studies have demonstrated that GABA levels correlate with sleep quality, suggesting that modulating the GABAergic system may be a promising therapeutic approach for insomnia. In this article, we highlight the significance of sleep, the classification and pathology of insomnia, and the impact of the GABAergic system changes on sleep. In addition, we also review the medications that target the GABAergic systems for insomnia, including benzodiazepines (BZDs), non-BZDs, barbiturates, GABA supplements, and Chinese herbal medicines.

Keywords: Benzodiazepines; Chinese herbal medicine; Gamma-aminobutyric acid; Insomnia; Sleep.

Publication types

Review