Assignment:
Post a discussion of BOTH the pharmacokinetics and pharmacodynamics related to anxiolytic medications used to treat generalized anxiety disorder. In your discussion, utilizing the discussion highlights, compare and contrast different treatment options that can be used.
Comparing and Contrasting Pharmacologic Options for the Treatment of Generalized Anxiety Disorder
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Comparing and Contrasting Pharmacologic Options for the Treatment of Generalized Anxiety Disorder
Anxiety is one of the most common mental disorders. The effects of anxiety disorder can be detrimental if not properly addressed. Several medications are available for the treatment of generalized anxiety disorder (GAD). Escitalopram is a selective serotonin reuptake inhibitor used in the treatment of GAD (Strawn et al., 2020). The medication causes an increase in serotonin levels in neuronal synapses by preventing the re-uptake of serotonin (5-HT) into the presynaptic terminals of serotonergic neurons. It is administered orally and absorption completes after 4-5 hours (Strawn et al., 2020). It exhibits relatively low protein binding at approximately 55-56%. It is metabolized to a propionic acid metabolite. It is eliminated in the urine.
Diazepam is another treatment option. it is a long-acting benzodiazepine used to treat anxiety disorder. It exerts anxiolytic, sedative, muscle- relaxant, anticonvulsant and amnestic effects. all these effects result from the facilitation of the action of gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter in the central nervous system (Dhaliwal et al., 2020). It is taken orally and absorbed from the gastrointestinal tract. Its peak plasma concentration is 1 – 1.5 hours. Diazepam is N-demethylated by CYP3A4 and 2C19 to the active metabolite N-desmethyldiazepam, and is hydroxylated by CYP3A4 to the active metabolite temazepam. It is excreted mainly in the urine.
The third treatment option is Alprazolam, a triazolobenzodiazepine, used to treat anxiety disorder. It binds γ-aminobutyric acid (GABA) type-A receptors (GABAARs) to enhance their inhibitory effect on neurotransmission, specifically in the brain. It is administered orally and rapidly absorbed in the gastrointestinal tract (Dangkoob et al., 2015). Alprazolam is metabolized to less effective metabolites by various CYPs including CYP3A4, CYP3A5, CYP3A7, and CYP2C9. Alprazolam is mainly eliminated in the urine.
Reference
Dhaliwal, J. S., Rosani, A., & Saadabadi, A. (2020). Diazepam. StatPearls [Internet]. https://www.ncbi.nlm.nih.gov/books/NBK537022/
Dangkoob, F., Housaindokht, M. R., Asoodeh, A., Rajabi, O., Zaeri, Z. R., & Doghaei, A. V. (2015). Spectroscopic and molecular modeling study on the separate and simultaneous bindings of alprazolam and fluoxetine hydrochloride to human serum albumin (HSA): With the aim of the drug interactions probing. Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy, 137, 1106-1119. https://doi.org/10.1016/j.saa.2014.08.149
Strawn, J. R., Mills, J. A., Schroeder, H., Mossman, S. A., Varney, S. T., Ramsey, L. B., … & DelBello, M. P. (2020). Escitalopram in adolescents with generalized anxiety disorder: a double-blind, randomized, placebo-controlled study. The Journal of Clinical Psychiatry, 81(5), 0-0. https://www.psychiatrist.com/jcp/depression/escitalopram-in-adolescents-with-gad/