NURS 6630 Foundational Neuroscience

NURS 6630 Foundational Neuroscience

1. Explain the agonist-to-antagonist spectrum of action of psychopharmacologic agents, including how partial and inverse agonist functionality may impact the efficacy of psychopharmacologic treatments.

A substance that binds to and triggers a receptor is known as an agonist. Full, partial, or inverse (Shiriaeva et al., 2022). A full agonist has high effectiveness, causing a complete reaction while occupying a small number of receptors. Comparing partial and full agonists, partial agonists are less effective. No matter the concentration, it cannot evoke the maximum response because it causes sub-maximal activation even though it occupies the whole receptor population. While binding to the same receptor binding site as an agonist, an inverse agonist exerts the opposite action.

1. Compare and contrast the actions of g couple proteins and ion-gated channels.

With between 600 to 1000 members, g couple proteins are the biggest protein family and have been connected to a variety of normal biological and pathological processes (Hu et al., 2022). They perform a broad variety of tasks, including the recognition of photons, tiny chemicals, and proteins. Ion-gated channels, on the other hand, are cellular membrane pores that permit ions to enter and exit the cell. The human genome has around 400 ion-gated channels. G-couple proteins, as opposed to ion-gated channels, are metabotropic receptors, while the latter are ionotropic.

1. 

   NURS 6630 Foundational Neuroscience

   Explain how the role of epigenetics may contribute to pharmacologic action.

The study of molecular alterations made to DNA and chromatin that result in changes in the expression of genes is known as epigenetics (Ganesan et al., 2019). Cytosine base methylation and chemical alterations to histone and nonhistone proteins, including acetylation and methylation, are examples of epigenetic modifications. The maintenance of normal phenotypic activity in cells as well as the development of diseases like cancer and neurological diseases like Alzheimer’s have all been linked to epigenetic alteration of gene activity.

1. Explain how this information may impact the way you prescribe medications to patients. Include a specific example of a situation or case with a patient in which the psychiatric mental health nurse practitioner must be aware of the medication’s action.

A psychiatric mental health nurse practitioner must grasp the pharmacology of medications to be aware of how the action of the drug will benefit the patient. For psychiatric and mental health patients, the procedure of prescribing medications is particularly important because changes brought on by neurocognitive mechanisms could change the drugs. For instance, stimulants like methylphenidate (Ritalin) and combined amphetamine salts (Adderall) have typically been found to be safe and helpful in the treatment of ADHD symptoms in teenagers and certain adults (Phoenix, 2019). However, the use of stimulants by pre-schoolers has sparked considerable debate due to the increased risk of adverse effects and worries about the medications’ impact on growth and neurodevelopment.

 References

Ganesan, A., Arimondo, P. B., Rots, M. G., Jeronimo, C., & Berdasco, M. (2019). The timeline of epigenetic drug discovery: from reality to dreams. Clinical Epigenetics, 11(1). https://doi.org/10.1186/s13148-019-0776-0

Hu, Y., Chen, M., Wang, M., & Li, X. (2022). Flow-mediated vasodilation through mechanosensitive G protein-coupled receptors in endothelial cells. Trends in Cardiovascular Medicine, 32(2), 61–70. https://doi.org/10.1016/j.tcm.2020.12.010

Phoenix, B. J. (2019). The Current Psychiatric Mental Health Registered Nurse Workforce. Journal of the American Psychiatric Nurses Association, 25(1), 38–48. https://doi.org/10.1177/1078390318810417

Shiriaeva, A., Park, D., Kim, G., Lee, Y., Hou, X., Jarhad, D. B., Kim, G., Yu, J., Hyun, Y. E., Kim, W., Gao, Z.-G., Jacobson, K. A., Han, G. W., Stevens, R. C., Jeong, L. S., Choi, S., & Cherezov, V. (2022). GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A_2A Adenosine Receptor. Journal of Medicinal Chemistry, 65(17), 11648–11657. https://doi.org/10.1021/acs.jmedchem.2c00462

Neuroscience is the scientific study of the human central nervous system to understand the brain’s dysfunction that can lead to disease, mental disorders, and physical impairment (Karmarkar & Plassmann, 2019). The complex design of a neuron is the basic understanding of communication by sending impulses to other body organs. The brain controls human behavior and the functions of body organs. The anatomy and physiology of the brain help understand the part of the brain affected by mental illness. For example, poor concentration and cognitive skills dysfunction is the forebrain pathology. Additionally, one can understand the mode of action of psychopharmacology. For example, antidepressants may function by inhibiting the serotonin or epinephrine receptors.

An Agonist-To-Antagonist Spectrum of Action and How Partial and Inverse Agonists Influence Psychopharmacologic

An antagonist binds at the receptors by blocking any event of an agonist, hence, blocking the biological response. For example, naloxone is a competitive opioid antagonist and has no effects with opioid co-administration (Gicquelais, et al, 2019). An agonist binds to a receptor causing activation of the receptor, hence, the biological response. A partial agonist activates the receptors partially with lesser effect on the brain. For example, buprenorphine is a partial agonist, and therefore, an antagonist may block its opioid function without activating its receptors. An inverse receptor binds with constitutively active receptors and inhibits receptor activity by exerting opposite pharmacological effects that suppress spontaneous receptor signaling.

Comparison between Actions of G Couple Proteins and Ion Gated Channels

G coupled proteins GPCRs are integral membrane proteins that convert extracellular responses to hormones, neurotransmitters, olfaction, and taste signals. The GPCRs work by binding to the hormones, neurotransmitters, and growth factors to initiate a cellular response. The three types of G-couple receptors are alpha, beta, and gamma, in which the ligands bind and activate (Yudin & Rohacs 2019). Ion gated channels are integral membrane proteins of excitable cells that allow a flux of ions to pass only under defined circumstances. These channels are voltage-gated sodium channel neurons and ligand-dated acetylcholine receptors of the cholinergic synapses. The ion gated channel pull and bonds to the agonist changing the protein while g coupled proteins are used by the cells to convert intracellular signals into responses.

The Role of Epigenetics In the Pharmacologic Action

Epigenetics regulate gene activity by switching off the gene activity or activating the gene activity. Epigenetics plays a role in the phenotypic activity of the cell in diseases such as cancer and neurodegenerative disorders such as Alzheimer’s disease. Epigenetics modify gene expressions after drug administration to counteract the disease states in humans. Epigenetics proves its effectiveness in treating psychiatric and neurodegenerative disorders to its ability to modify gene expressions.

The Significance of the Information to Psychiatric Mental Health Nurse Practitioner

A psychiatric mental health nurse practitioner should have basic knowledge of the concepts of foundational neuroscience. Understanding the function of agonists, inverse and partial agonists, and antagonists prevent co-administration of drugs that agonize and antagonize the same receptors. For example, in treating a patient with a depressive mood disorder, prescribing antipsychotics such as fluphenazine worsens the depressive mood because it antagonizes the dopaminergic D1 and D2 receptors depressing the release of the hypothalamic hormone.

 References

Gicquelais, R. E., Bohnert, A. S., Thomas, L., & Foxman, B. (2020). Opioid agonist and antagonist use and the gut microbiota: associations among people in addiction treatment. Scientific reports, 10(1), 1-11. https://doi.org/10.1038/s41598-020-76570-9

Karmarkar, U. R., & Plassmann, H. (2019). Consumer neuroscience: Past, present, and future. Organizational Research Methods, 22(1), 174-195.

https://doi.org/10.1177%2F1094428117730598

Yudin, Y., & Rohacs, T. (2019). The G‐protein‐biased agents PZM21 and TRV130 are partial agonists of μ‐opioid receptor‐mediated signalling to ion channels. British journal of pharmacology, 176(17), 3110-3125. https://doi.org/10.1111/bph.14702

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