Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Review
. 2018 May 23:14:1351-1361.
doi: 10.2147/NDT.S164307. eCollection 2018.

Valium without dependence? Individual GABAA receptor subtype contribution toward benzodiazepine addiction, tolerance, and therapeutic effects

Tianze Cheng  1 , Dominique Marie Wallace  2 , Benjamin Ponteri  1 , Mahir Tuli  3
Affiliations
Review

Valium without dependence? Individual GABAA receptor subtype contribution toward benzodiazepine addiction, tolerance, and therapeutic effects

Tianze Cheng et al. Neuropsychiatr Dis Treat. .

Abstract

Benzodiazepines are one of the most prescribed medications as first-line treatment of anxiety, insomnia, and epilepsy around the world. Over the past two decades, advances in the neuropharmacological understanding of gamma aminobutyric acid (GABA)A receptors revealed distinct contributions from each subtype and produced effects. Recent findings have highlighted the importance of α1 containing GABAA receptors in the mechanisms of addiction and tolerance in benzodiazepine treatments. This has shown promise in the development of tranquilizers with minimal side effects such as cognitive impairment, dependence, and tolerance. A valium-like drug without its side effects, as repeatedly demonstrated in animals, is achievable.

Keywords: GABAA receptor; anxiolytic; benzodiazepines; dependence; subtype; tolerance.

PubMed Disclaimer

Conflict of interest statement

Disclosure The authors report no conflicts of interest in this work.

Figures

Figure 1
Figure 1
The GABAA receptor and its approximate subtype composition (adapted from Wafford’s study). Note: Data from Wafford.9 Abbreviation: GABA, gamma aminobutyric acid.
Figure 2
Figure 2
Mechanism of benzodiazepines at VTA. Note: Data adapted from Rudolph et al and Heikkinen et al. Abbreviations: VTA, ventral tegmental area; GABA, gamma aminobutyric acid; NAcc, nucleus accumbens; mPFC, medial prefrontal cortex.
See this image and copyright information in PMC

References

    1. Olfson M, King M, Schoenbaum M. Benzodiazepine use in the United States. JAMA Psychiatry. 2015;72(2):136–142. - PubMed
    1. Dantzer R. Behavioral effects of benzodiazepines: a review. Neurosci Biobehav Rev. 1977;1(2):71–86.
    1. Shader R, Greenblatt D, Balter M. Appropriate use and regulatory control of benzodiazepines. J Clin Pharmacol. 1991;31(9):781–784. - PubMed
    1. Sternbach L. The benzodiazepine story. J Med Chem. 1979;22(1):1–7. - PubMed
    1. Olsen R, Wamsley J, Lee R, Lomax P. Benzodiazepine/barbiturate/GABA receptor-chloride ionophore complex in a genetic model for generalized epilepsy. Adv Neurol. 1986;44:365–378. - PubMed

LinkOut - more resources