Ethanol interacts with two major receptors in the central nervous system (CNS) that are essential for normal CNS function: gamma-aminobutyric acid (GABA) type A receptors and N-methyl-D-aspartate (NMDA) receptors.
Ethanol predominantly targets the GABA type A receptor, where the persistent stimulation of inhibitory receptors results in downregulation of the GABA type A receptor/Cl- channel complex.[18]Brousse G, Arnaud B, Vorspan F, et al. Alteration of glutamate/GABA balance during acute alcohol withdrawal in emergency department: a prospective analysis. Alcohol Alcohol. 2012 Sep-Oct;47(5):501-8.
https://academic.oup.com/alcalc/article/47/5/501/99762
http://www.ncbi.nlm.nih.gov/pubmed/22791370?tool=bestpractice.com
[19]Roberto M, Varodayan FP. Synaptic targets: chronic alcohol actions. Neuropharmacology. 2017 Aug 1;122:85-99.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5479718
http://www.ncbi.nlm.nih.gov/pubmed/28108359?tool=bestpractice.com
[20]Littleton J. Neurochemical mechanisms underlying alcohol withdrawal. Alcohol Health Res World. 1998;22(1):13-24.
http://www.ncbi.nlm.nih.gov/pubmed/15706728?tool=bestpractice.com
[21]Lovinger DM, Roberto M. Synaptic effects induced by alcohol. Curr Top Behav Neurosci. 2013;13:31-86.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4791588
http://www.ncbi.nlm.nih.gov/pubmed/21786203?tool=bestpractice.com
The adaptive downregulation of GABA type A receptors also contributes to the development of tolerance by allowing alcohol users to maintain a level of consciousness despite the presence of a sedative ethanol concentration.[20]Littleton J. Neurochemical mechanisms underlying alcohol withdrawal. Alcohol Health Res World. 1998;22(1):13-24.
http://www.ncbi.nlm.nih.gov/pubmed/15706728?tool=bestpractice.com
[21]Lovinger DM, Roberto M. Synaptic effects induced by alcohol. Curr Top Behav Neurosci. 2013;13:31-86.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4791588
http://www.ncbi.nlm.nih.gov/pubmed/21786203?tool=bestpractice.com
Among numerous different excitatory amino acid receptor systems, the presence of a persistent blood ethanol concentration primarily affects the expression of the post-synaptic NMDA receptor-Ca+2 channel complex. In contrast to GABA type A receptor agonism, ethanol inhibits the NMDA receptor function by competitively binding to the glycine binding site on the NMDA receptor. This inhibitory effect causes a compensatory upregulation of NMDA receptors on the post-synaptic membrane.
At the pre-synaptic level, chronic alcohol use increases excitatory glutamate release while re-uptake of glutamate is inhibited.[19]Roberto M, Varodayan FP. Synaptic targets: chronic alcohol actions. Neuropharmacology. 2017 Aug 1;122:85-99.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5479718
http://www.ncbi.nlm.nih.gov/pubmed/28108359?tool=bestpractice.com
[21]Lovinger DM, Roberto M. Synaptic effects induced by alcohol. Curr Top Behav Neurosci. 2013;13:31-86.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4791588
http://www.ncbi.nlm.nih.gov/pubmed/21786203?tool=bestpractice.com
[22]Melendez RI, Hicks MP, Cagle SS, et al. Ethanol exposure decreases glutamate uptake in the nucleus accumbens. Alcohol Clin Exp Res. 2005 Mar;29(3):326-33.
http://www.ncbi.nlm.nih.gov/pubmed/15770106?tool=bestpractice.com
[23]Dahchour A, De Witte P. Effect of repeated ethanol withdrawal on glutamate microdialysate in the hippocampus. Alcohol Clin Exp Res. 1999 Oct;23(10):1698-703.
http://www.ncbi.nlm.nih.gov/pubmed/10550004?tool=bestpractice.com
There is evidence to suggest that acute alcohol use increases pre-synaptic GABA release.[19]Roberto M, Varodayan FP. Synaptic targets: chronic alcohol actions. Neuropharmacology. 2017 Aug 1;122:85-99.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5479718
http://www.ncbi.nlm.nih.gov/pubmed/28108359?tool=bestpractice.com
[21]Lovinger DM, Roberto M. Synaptic effects induced by alcohol. Curr Top Behav Neurosci. 2013;13:31-86.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4791588
http://www.ncbi.nlm.nih.gov/pubmed/21786203?tool=bestpractice.com
[24]Kelm MK, Criswell HE, Breese GR. Ethanol-enhanced GABA release: a focus on G protein-coupled receptors. Brain Res Rev. 2011 Jan 1;65(2):113-23.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005894
http://www.ncbi.nlm.nih.gov/pubmed/20837058?tool=bestpractice.com
[25]Kelm MK, Criswell HE, Breese GR. The role of protein kinase A in the ethanol-induced increase in spontaneous GABA release onto cerebellar Purkinje neurons. J Neurophysiol. 2008 Dec;100(6):3417-28.
https://www.physiology.org/doi/full/10.1152/jn.90970.2008
http://www.ncbi.nlm.nih.gov/pubmed/18945815?tool=bestpractice.com
However, the relationship between chronic alcohol use and alteration of pre-synaptic release of GABA is currently not well understood.
Adaptive mechanisms in neurotransmitter-receptor interaction maintain homeostasis between excitatory (NMDA) and inhibitory (GABA) receptor systems and mediate the development of alcohol tolerance. Abstinence from alcohol in the alcohol-dependent patient leads to a disequilibrium between NMDA and GABA type A receptor function due to decreased blood ethanol concentration from the previously maintained steady-state level. As a result, excessive glutamatergic stimulation with diminished inhibitory (GABA) activity leads to the development of clinical symptoms of alcohol withdrawal syndrome (AWS), including autonomic hyperactivity, tremors, hallucinations, and seizures.[21]Lovinger DM, Roberto M. Synaptic effects induced by alcohol. Curr Top Behav Neurosci. 2013;13:31-86.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4791588
http://www.ncbi.nlm.nih.gov/pubmed/21786203?tool=bestpractice.com
Multiple episodes of AWS increase the severity of subsequent AWS due to kindling phenomena. Kindling is a process where low chemical or electrical stimulus, which does not normally produce a behavioural response, results in behavioural effects, such as seizure, from repetitive administration.[26]Becker HC. Kindling in alcohol withdrawal. Alcohol Health Res World. 1998;22(1):25-33.
http://www.ncbi.nlm.nih.gov/pubmed/15706729?tool=bestpractice.com
[27]Ballenger JC, Post RM. Kindling as a model for alcohol withdrawal syndromes. Br J Psychiatry. 1978 Jul;133:1-14.
http://www.ncbi.nlm.nih.gov/pubmed/352467?tool=bestpractice.com
There is a growing body of evidence that kindling phenomena contribute to the exacerbation of withdrawal symptoms.[26]Becker HC. Kindling in alcohol withdrawal. Alcohol Health Res World. 1998;22(1):25-33.
http://www.ncbi.nlm.nih.gov/pubmed/15706729?tool=bestpractice.com
Clinically, a significant proportion of patients with AWS who suffer seizures have a history of multiple episodes of AWS compared with patients with AWS who do not have associated seizures.[28]Brown ME, Anton RF, Malcolm R, et al. Alcohol detoxification and withdrawal seizures: clinical support for a kindling hypothesis. Biol Psychiatry. 1988 Mar 1;23(5):507-14.
http://www.ncbi.nlm.nih.gov/pubmed/3345323?tool=bestpractice.com
[29]Booth BM, Blow FC. The kindling hypothesis: further evidence from a U.S. national study of alcoholic men. Alcohol Alcohol. 1993 Sep;28(5):593-8.
http://www.ncbi.nlm.nih.gov/pubmed/8274184?tool=bestpractice.com
[30]McCown TJ, Breese GR. Multiple withdrawals from chronic ethanol "kindles" inferior collicular seizure activity: evidence for kindling of seizures associated with alcoholism. Alcohol Clin Exp Res. 1990 Jun;14(3):394-9.
http://www.ncbi.nlm.nih.gov/pubmed/2378423?tool=bestpractice.com