Benzodiazepines

Benzodiazepines and Mechanism of Action

Benzodiazepines as anxiolytic drugs reduce the symptoms of anxiety by increasing the action of the gamma-aminobutyric acid (GABA).GABA is used by the nerve cells to induce communication among them. Therefore, GABA action reduces brain activity since hyperactivity in the brain leads to anxiety or some psychiatric disorders (Picton, et al, 2018). Benzodiazepines work by promoting the binding of GABA to its receptor. The receptors are found on the postsynaptic nerve endings in the Central Nervous System with the GABA receptor complex having two alpha subunits and beta subunits. The alpha subunits are the binding sites for benzodiazepines (Griessner, et al, 2021). GABA activates the chloride ion channel that allows chloride ions to enter the neuron which hyperpolarizes and inhibits the neutron.

Buspirone is used to augment antidepressants and originates from the class of azapirone class of medications that has anxiolytic and antipsychotic medications. It works by having effects on the neurotransmitters in the brain like serotonin and dopamine (Wilson, & Tripp, 2021). Buspirone being a serotonin receptor agonist increases the action within the serotonin receptors in the brain thus alleviating the anxiety. Buspirone exerts its effects as a partial 5HT1A receptor agonist. Therefore, the addition of the drug to SSRI results in an improved serotonergic effect and improved relief on the depression symptoms. In the main treatment, the drug is used since it achieves a higher peak serum concentration with one hour with a serum half-life of 2 to 5 hours.

Serotonergic hypnotics are drugs that are used as tranquilizers or sleeping pills since they affect the central nervous system that is the brain and spinal cord resulting in a calming and relaxing effect. An example is Valium (diazepam) and it works by increasing the activity of gamma-aminobutyric acid (GABA) a neurotransmitter in the brain (Cheng, et al, 2018). The increased GABA activity in the brain leads to drowsiness and induces sleep in a person with insomnia.

References

Cheng, T., Wallace, D. M., Ponteri, B., & Tuli, M. (2018). Valium without dependence? Individual GABAA receptor subtype contribution toward benzodiazepine addiction, tolerance, and therapeutic effects. Neuropsychiatric disease and treatment, 14, 1351.

Picton, J. D., Marino, A. B., & Nealy, K. L. (2018). Benzodiazepine use and cognitive decline in the elderly. The Bulletin of the American Society of Hospital Pharmacists, 75(1), e6-e12.

Wilson, T. K., & Tripp, J. (2021). Buspirone. StatPearls [Internet].

Griessner, J., Pasieka, M., Böhm, V., Grössl, F., Kaczanowska, J., Pliota, P., … & Haubensak, W. (2021). Central amygdala circuit dynamics underlying the benzodiazepine anxiolytic effect. Molecular psychiatry, 26(2), 534-544.

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