Discussion Of Pharmacokinetics And Pharmacodynamics

Discussion Of Pharmacokinetics And Pharmacodynamics

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Generalized Anxiety Disorder (GAD) has been a common problem globally, and only a few receive treatment. An individual is diagnosed with GAD through the existence of three or more signs and symptoms like restlessness, irritability, and impaired concentration. Also, GAD patients find it hard to control their anxiety and worrying levels and should not be under six months (Carl et al., 2020)Discussion Of Pharmacokinetics And Pharmacodynamics. Such factors help distinguish GAD from worry since, in most cases, worry happens within a short period and is caused by a specific stressor. Furthermore, an important factor is that women have higher chances of developing GAD than men. The paper will compare and contrast GAD’s treatment options, pharmacological and pharmacokinetic, that are more viable in the United States. Hence, the paper will evaluate Benzodiazepines and Pregabalin’s pharmacodynamics and pharmacokinetics factors.

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Comparison and Contrast of Anxiolytics Pharmacodynamics and Pharmacokinetics

Benzodiazepines

Benzodiazepines contains sedative, anticonvulsant, anxiolytic and myorelaxant properties. Such properties then require clinicians always to ensure that the patients understand the treatment duration and how to discontinue the medication (Baldwin, 2022) gradually. That is because of the risks associated with these medications.

Pharmacokinetics

Benzodiazepine drugs contain homogenous pharmacological properties and individualized chemical structures. These drugs’ use and characteristics mainly rely on their metabolism and pharmacokinetics (LaGrotta & Thomas, 2020)Discussion Of Pharmacokinetics And Pharmacodynamics. These drugs’ properties contain weak acids with high lipophilicity and variable constant dissociation, allowing rapid membrane passage. Most benzodiazepines, apart from midazolam, dipotassium-clorazepate, and chlordiazepoxide, have insolubility properties, thus needing organic solutions like clonazepam and Diazepam.

 Pharmacodynamics

Benzodiazepines act as the main modulator of gamma-aminobutyric acid (GABA) –A receptor that refers to a ligand-gated chloride-selective ion channel. GABA is one of the main prevalent central nervous system’s (CNS) neurotransmitters that contains high concentration within the limbic and cortex system. GABA contains an inhibitory effect on the neurons, which lowers the neurons’ excitability (LaGrotta & Thomas, 2020). Also, GABA affects the brain through sedative effects. Since GABA has three receptors, A, B, and C, the receptor that interacts with Benzodiazepines are the A-receptor. The receptor is complex and contains five glycoprotein subunits that contain various isoforms. These subunits are divided into 2-2-1 though there is only one benzodiazepine binding site, which causes the GABA-A receptor to have a different conformation that allows GABA to bind. On the other hand, benzodiazepines also bind to the formed pockets, leading the GABA-A receptor to change its conformation (LaGrotta & Thomas, 2020)Discussion Of Pharmacokinetics And Pharmacodynamics. That leads to conformational change within the GABA-A receptor’s chloride channel that causes cell hyperpolarization and leads to its inhibitory effect in CNS.

Pregabalin

Pregabalin falls under the anticonvulsant medication that helps treat fibromyalgia and neuropathic pain (Kloiber & Konstantinou, 2021). Also, it is a partial-onset seizure when used alongside other anticonvulsants.

Pharmacokinetics

Unlike the insoluble case of benzodiazepines, pregabalin is easily absorbed on an empty stomach, meaning it is soluble. As a result, its bioavailability is approximately 90 percent, and it is also dose-independent, unlike benzodiazepines (Chen et al., 2019). After the drug administration, the equilibrium state is achieved within twenty-four to forty-eight hours. However, the patient uses the medication as they take their meal, and the pregabalin’s absorption rate decreases though it has no associated clinical risks. Like benzodiazepines, pregabalin also passes through the blood-brain barrier and is within milk, but it has no affinity for plasma proteins.

Pharmacodynamics

Despite having a similar structure to GABA, pregabalin does not bind with GABA receptors like in the case of Benzodiazepines. Within the central nervous system, pregabalin binds the alpha2-delta, which is a presynaptic subunit of the voltage-gated calcium channel (Chen et al., 2019)Discussion Of Pharmacokinetics And Pharmacodynamics. However, pregabalin does not affect serotonin, dopamine, sodium channels, or opiate receptors like Benzodiazepines.

Conclusion

The discussion has addressed the pharmacokinetics and pharmacodynamics of Benzodiazepines and pregabalin, a form of anxiolytics. The main similarity is that they both pass through the blood-brain barrier and are present in milk. However, the main difference is that pregabalin does not bind with GABA receptor-like Benzodiazepines. In addition, pregabalin is also soluble, thus easily absorbing in the body, while benzodiazepines are insoluble Discussion Of Pharmacokinetics And Pharmacodynamics.

References

Carl, E., Witcraft, S. M., Kauffman, B. Y., Gillespie, E. M., Becker, E. S., Cuijpers, P., … & Powers, M. B. (2020). Psychological and pharmacological treatments for generalized anxiety disorder (GAD): a meta-analysis of randomized controlled trials. Cognitive Behaviour Therapy, 49(1), 1-21. https://doi.org/10.1080/16506073.2018.1560358

Baldwin, D. S. (2022). Clinical management of withdrawal from benzodiazepine anxiolytic and hypnotic medications. Addiction, 117(5), 1472-1482. https://doi.org/10.1111/add.15695

Chen, X., van Gerven, J., Cohen, A., & Jacobs, G. (2019). Human pharmacology of positive GABA-A subtype-selective receptor modulators for the treatment of anxiety. Acta Pharmacologica Sinica, 40(5), 571-582. https://doi.org/10.1038/s41401-018-0185-5

LaGrotta, C., & Thomas, A. (2020). Benzodiazepines and Other Sedatives, Hypnotics, and Anxiolytics. In Absolute Addiction Psychiatry Review (pp. 139-151). Springer, Cham. DOI: 10.1007/978-3-030-33404-8_9

Kloiber, S., & Konstantinou, G. (2021). Tranquilizers/Anxiolytics: Definition, Indications, Contraindications, and Treatment. In NeuroPsychopharmacotherapy (pp. 1-15). Cham: Springer International Publishing. Doi:10.1007/978-3-319-56015-1_59-1Discussion Of Pharmacokinetics And Pharmacodynamics

Week 8 Discussion: Comparing and Contrasting Pharmacologic Options for the Treatment of Generalized Anxiety Disorder
Psychological disorders, such as depression, bipolar, and anxiety disorders can present several complications for patients of all ages. These disorders affect patients physically and emotionally, potentially impacting judgment, school and/or job performance, and relationships with family and friends. Since these disorders have many drastic effects on patients’ lives, it is important for advanced practice nurses to effectively manage patient care. With patient factors and medical history in mind, it is the advanced practice nurse’s responsibility to ensure the safe and effective diagnosis, treatment, and education of patients with psychological disorders.

Generalized Anxiety Disorder is a psychological condition that affects 6.1 million Americans, or 3.1% of the US Population. Despite several treatment options, only 43.2% of those suffering from GAD receive treatment. This week you will review several different classes of medication used in the treatment of Generalized Anxiety Disorder. You will examine potential impacts of pharmacotherapeutics used in the treatment of GAD. Please focus your assignment on FDA approved indications when referring to different medication classes used in the treatment of GAD. Discussion Of Pharmacokinetics And Pharmacodynamics

To Prepare
• Review the Resources for this module and consider the principles of pharmacokinetics and pharmacodynamics.
• Reflect on your experiences, observations, and/or clinical practices from the last 5 years and think about how pharmacokinetic and pharmacodynamic factors altered his or her anticipated response to a drug.
• Consider factors that might have influenced the patient’s pharmacokinetic and pharmacodynamic processes, such as genetics (including pharmacogenetics), gender, ethnicity, age, behavior, and/or possible pathophysiological changes due to disease.
• Think about a personalized plan of care based on these influencing factors and patient history with GAD.

Post a discussion of pharmacokinetics and pharmacodynamics related to anxiolytic medications used to treat GAD. In your discussion, utilizing the discussion highlights, compare and contrast different treatment options that can be used (in United States)Discussion Of Pharmacokinetics And Pharmacodynamics

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Reading and links
Rosenthal, L. D., & Burchum, J. R. (2021). Lehne’s pharmacotherapeutics for advanced practice nurses and physician assistants (2nd ed.) St. Louis, MO: Elsevier.
• Chapter 26, “Antipsychotic Agents and Their Use in Schizophrenia” (pp. 203–213)
• Chapter 27, “Antidepressants” (pp. 214–226)
• Chapter 28, “Drugs for Bipolar Disorder” (pp. 228–233)
• Chapter 29, “Sedative-Hypnotic Drugs” (pp. 234–242)
• Chapter 30, “Management of Anxiety Disorders” (pp. 243–247)
• Chapter 31, “Central Nervous System Stimulants and Attention-Deficit/Hyperactivity Disorder” (pp. 248–254)Discussion Of Pharmacokinetics And Pharmacodynamics