Feb 23, 2024 Discussion: Foundational Neuroscience NURS 6630
Discussion: Foundational Neuroscience NURS 6630
A Sample Answer For the Assignment: Discussion: Foundational Neuroscience NURS 6630
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.
The agonist spectrum can be explained best as a scale from agonist to inverse agonist; with natural neurotransmitters being an agonist or drugs that stimulate the receptors for that action. Partial agonist follows the agonist because of drugs that stimulate the same receptors on a lower gradation of the spectrum (Stahl, 2021). The next level on the spectrum is the antagonist blocking the action of the agonist (Stahl, 2021).
The final function is the inverse agonist has two behaviors: (1) block the agonist, and (2) lower the level of activity below the starting point in absence of an agonist (Stahl, 2021). The best way to explain a partial agonist is to present a medication used in the treatment of depression. Vilazodone is a serotonin reuptake inhibitor, which causes a rise in serotonin at the synaptic cleft by preventing the re-uptake of serotonin at the presynaptic axon terminal (Comprodon & Roffman, 2016).
However, Vilazodone also signals the 5HT1A presynaptic receptors and causes a decrease in the production of serotonin acting as a partial agonist (Baumgartnera et al., 2020). The outcome of partial and inverse agonists can be a marked increase or decrease in the concentration of a drug from the inhibition or excitation of the drug’s receptors (Comprodon & Roffman, 2016).
2. Compare and contrast the actions of g couple proteins and ion gated channels.
Two of the four methods of signal transduction involve neurotransmitters rather than hormones or neurotrophins (Stahl, 2021). G-coupled proteins and ion-gated channels are similar because they are stimulated by drugs that cause neurotransmitters to activate genes inside of the cell when a phosphate is added to the cAMP protein (Stahl, 2021).
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Although they have similarities, the first, G-coupled proteins, cause a slow neuronal effect as a result of its action with cAMP and protein kinase A (Comprodon & Roffman, 2016). The second, ion-gated channels, cause a rapid neuronal effect on the membrane potential as a result of calcium and a kinase called CaMK (Comprodon & Roffman, 2016).
3. Explain how the role of epigenetics may contribute to pharmacologic action.
Epigenetics describes the heritable action of DNA when gene function changes from one generation to the next because of the influence of the external milieu (Comprodon & Roffman, 2016). DNA can be affected by experiences triggering phenotype modifications rather than genotype changes medications (Quevedo et al., 2022). Stress, such as physical abuse in children, is positively correlated with the development of borderline personality disorder (Comprodon & Roffman, 2016; Quevedo et al., 2022).
Discussion Foundational Neuroscience NURS 6630
The downstream effect of neuroplasticity can result in changes at the genetic level resulting in DNA sequencing variations (Quevedo et al., 2022). Once the chromatin’s structure is modified, the encoding of proteins may alter the original behavior of synaptic uptake of drugs causing changes of pharmacological action, such as enhanced or diminished responses to medications (Quevedo et al., 2022). The increased or decreased action at the receptor site may enhance or inhibit the action of a drug and cause an unexpected outcome.
4. 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.
Epigenetic changes are crucial to understand when prescribing medications to patients who have suffered trauma (child abuse, substance misuse, malnutrition, etc.) resulting in DNA silencing or activation (Comprodon & Roffman, 2016). The stress response to physical, emotional, or sexual abuse can cause increased DNA methylation in various tissues in the body, namely blood, saliva, and brain tissue (Quevedo et al., 2022). Therefore, the PMHNP should be well versed in the biomechanics of a medication for appropriate and effective prescribing.
One example is the higher reactivity of the HPA axis to adverse childhood experiences stimulating Corticotropin Releasing Hormone (CRH), which triggers the release of adrenocorticotropin hormone from the pituitary gland (Quevedo et al., 2022). A corticotropin releasing hormone antagonist may be ineffective if one’s mental health is severely affected by a history of abuse. Therefore, the PMHNP should consider an alternative medication to a CRH antagonist.
References
Baumgartnera, K., Doeringb, M., & Schwarz, E. (2020). Vilazodone poisoning: A systematic review. Clinical Toxicology, 58(5), 360–367. https://doi.org/10.1080/15563650.2019.1691221
Links to an external site.
Camprodon, J. A., & Roffman, J. L. (2016). Psychiatric neuroscience: Incorporating pathophysiology into clinical case formulation. In T. A. Stern, M. Favo, T. E. Wilens, & J. F. Rosenbaum. (Eds.), Massachusetts General Hospital Psychopharmacology and Neurotherapeutics (pp. 1–19). Elsevier.
Quevedo, Y., Booij, L., Herrera, L., Hernández, C., & Jiménez, J. P. (2022). Potential epigenetic mechanisms in psychotherapy: A pilot study on DNA methylation and mentalization change in borderline personality disorder. Frontiers in Human Neuroscience. https://doi.org/10.3389/fnhum.2022.955005
Hello. This discussion post actually belongs to the class NURS 6630 and not NURS 4430. Kindly do not be put off by that misrepresentation.
Discussion: Foundational Neuroscience NURS 4430 SAMPLE
Agonist-to-antagonist spectrum of action of psychopharmacologic agents, including how partial and inverse agonist functionality may impact the efficacy of psychopharmacologic treatments.
An agonist action is caused by a drug that purposefully binds to the receptors. The agonist action then produces a detailed response to the targeted chemical and receptors. Alternatively, an antagonistic activity is caused by a drug that binds the receptors causing the receptors to seize from producing a reply.
This agent’s agonist to antagonist spectrum of action is that one simulates reactions while the other stops or slows down responses. Often an agonist will emulate the activities of a neurotransmitter and produce similar reactions to natural receptors of which they bid.
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Furthermore, agonists have affinity and efficacy, which means that they have target receptors they bid to and can change receptor functionality to produce the desired response (Berg & Clarke, 2018). Alternatively, antagonists have an affinity but cannot make a response. Therefore, an antagonist will reduce the receptor ability of an agonist, thus reduction of receptor response.
In cases where there is a full agonist, the essential functions of an antagonist can be blocked. This is because a full agonist produces a maximum response, whereas a partial one produces partial responses. In some cases, a full agonist can make maximum response without having to occupy the full receptors.
Compare and contrast the actions of g couple proteins and ion gated channels.
First of all, both are types of proteins integrated with cell membranes. Both types of protein are embedded in cell membranes. G coupled proteins are chains of lipophilic helical segments within the membrane, although sometimes they are short helices in the connecting loops. G coupled proteins are activated by chemical messengers, and these messages arepassed through the interaction of G+proteins.
On the other hand, Ion channels are also made from lipophilic helices, but they have various chains ingrained within them. They are built to allow ions through the channel. These channels are more restricted and gated, meaning that only some chemical messengers can lift the restriction or penetrate the gate to switch the channel on (Li, Wong & Liu, 2014). Some chemicals within the proteins are similar. For example, both may contain glutamate or acetylcholine.
Explain how the role of epigenetics may contribute to pharmacologic action.
Epigenetics are systems that have evolved to be able to switch gene activity or tune existing genetic activations. Furthermore, epigenetic regulation of such gene activities is essential in maintaining regular exercise in cells. Distorted epigenetics may lead to cell diseases such as cancer and neurodegenerative disorders like Alzheimer’s. Epigenetic systems can create implications in patients because they alter how patients respond to different drugs (McClarty, Fisher & Dong, 2018).
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.
As a nurse practitioner working in a psychiatric institution, one must know that aging-induced epigenetic alterations exist. Therefore, in a scenario where one is dealing with an elderly patient with a neurogenerative disease, one must consider how epigenetic can interfere with antipsychotic function (McClarty, Fisher & Dong,2018).
Epigenetic mechanisms and altered efficacy in agonists can increase side effects in the elderly. In such cases, the nurse can opt for an inverse agonist or partial agonist, which do not produce the same responses as a full agonist (Nutt et al., 2017). These are a new class of lingad that could work in those who find full agonists too reactive.
References
Berg, K. A., & Clarke, W. P. (2018). Making sense of pharmacology: Inverse agonism and functional selectivity. The International Journal of Neuropsychopharmacology, 21(10), 962–977. https://doi.org/10.1093/ijnp/pyy071
McClarty, B. M., Fisher, D. W., & Dong, H. (2018). Epigenetic alterations impact antipsychotic treatment in elderly patients. Current Treatment Options in Psychiatry, 5(1), 17–29. https://doi.org/10.1093/ijnp/pyy071
Li, S., Wong, A. H., & Liu, F. (2014). Ligand-gated ion channel interacting proteins and their role in neuroprotection. Frontiers in Cellular Neuroscience, 8(125), 1-5. https://doi.org/10.3389/fncel.2014.00125
Nutt, D., Stahl, S., Blier, P., Drago, F., Zohar, J., & Wilson, S. (2017). Inverse agonists – What do they mean for psychiatry?European Neuropsychopharmacology: The Journal of the European College of Neuropsychopharmacology, 27(1), 87–90. https://doi.org/10.1016/j.euroneuro.2016.11.013
Discussion: Foundational Neuroscience NURS 4430
As a psychiatric nurse practitioner, it is essential for you to have a strong background in foundational neuroscience. In order to diagnose and treat patients, you must not only understand the pathophysiology of psychiatric disorders but also how medications for these disorders impact the central nervous system. These concepts of foundational neuroscience can be challenging to understand. Therefore, this Discussion is designed to encourage you to think through these concepts, develop a rationale for your thinking, and deepen your understanding by interacting with your colleagues.
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For this Discussion, review the Learning Resources and reflect on the concepts of foundational neuroscience as they might apply to your role as the psychiatric mental health nurse practitioner in prescribing medications for patients.
By Day 3 of Week 2 of Discussion: Foundational Neuroscience NURS 4430
Post a response to each of the following:
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.Compare and contrast the actions of g couple proteins and ion gated channels.Explain how the role of epigenetics may contribute to pharmacologic action.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.Read a selection of your colleagues’ responses.
Neuroscience and Prescription
Agonists and antagonists are critical players in pharmacology and, generally, in the human body. Agonist binds to a receptor, thus altering its state and producing an appropriate response (Patinote et al.,2020). They are considered the prime movers responsible for creating a specific movement. On the other hand, the antagonists are ligands that prevent the agonist from binding to a receptor, preventing its effects (Patinote et al.,2020).
They do not by themselves contain pharmacological actions that are mediated by the receptors. Generally, this means that the agonists and antagonists act in different directions, whereby the agonists introduce an action while the antagonist opposes it. The agonist works with the muscles while the antagonists work against them. Furthermore, the agonist alters the functionality of the activities of the receptors, while the antagonists do not alter the activities of the receptors despite their binding to the receptor.
Moreover, the partial agonists cannot produce the maximal response of the tissue can regardless of whether they have the same number of receptors as full agonists. Therefore, a certain level of binding is where the partial agonist can bind the receptors without consequently producing additional effects (Patinote et al.,2020). Nevertheless, doing so may hinder the activities of other agonists, thus being seen as antagonists.
Therefore, this mixture of actions is referred to as a partial agonist. Moreover, an inverse agonist binds to a receptor and produces a response different from that of the corresponding agonist (Patinote et al.,2020). When the agonist increases the activity mediated by a receptor, the inverse agonist decreases it.
The actions of G couple proteins and the ion-gated channels share similarities and differences. They are both considered transmembrane us proteins with ligand binding sites and have an effect on the cytoplasmic (Hu et al.,2021). In addition, they both, to some extent, react to the ligand, where they change their shape.
The differences are that the G Protein receptors have a single polypeptide tied over the membrane. On the other hand, the ion channel has pores open and close when ligand binding occurs. Another difference is that the G protein-coupled receptors often interact highly with various proteins for an intracellular response (Hu et al.,2021). On the other hand, ion channels help regulate the flow of irons.
The role of epigenetics may contribute to pharmacologic action in various ways. The epigenetic regulation of the gene of activities of the gene is critical in the maintenance of normal phenotypic cell activities (Topper et al.,2020). It is also essential in developing diseases such as Alzheimer’s and cancer.
The information gained has helped me gain valuable insights and significantly impacted how one may prescribe medication to their patients. Understanding the epigenetics affected by human diseases helps define pharmacology that may be used to control the mechanism (Topper et al.,2020). As a result, it may help one make the right judgments regarding decisions related to the mediation of patients with mental health issues.
The information gained helps link neurobiology to the diagnosis of mental health to help identify the effective medication to assist in the treatment of the disease. For example, using the information on neuroscience, a professional psychiatrist can relate and make an informed diagnosis, thus prescribing the best mediation based on informed judgments.
References
Hu, Y., Chen, M., Wang, M., & Li, X. (2021). Flow-mediated vasodilation through mechanosensitive G protein-coupled receptors in endothelial cells. Trends in Cardiovascular Medicine. https://doi.org/10.1016/j.tcm.2020.12.010Links to an external site.
Patinote, C., Karroum, N. B., Moarbess, G., Cirnat, N., Kassab, I., Bonnet, P. A., & Deleuze-Masquéfa, C. (2020). Agonist and antagonist ligands of toll-like receptors 7 and 8: Ingenious tools for therapeutic purposes. European journal of medicinal chemistry, 193, 112238. https://doi.org/10.1016/j.ejmech.2020.112238Links to an external site.
Topper, M. J., Vaz, M., Marrone, K. A., Brahmer, J. R., & Baylin, S. B. (2020). The emerging role of epigenetic therapeutics in immuno-oncology. Nature Reviews Clinical Oncology, 17(2), 75-90. https://doi.org/10.1038/s41571-019-0266-5Links to an external site.
HILARIO
WK2Assgn1_Noveno_Hilario Response
Agonists are chemicals that bind to a receptor site and activate/stimulate the binding site to yield a [maximum] response or effect. While the antagonists act to oppose this effect by blocking the receptor site so that the chemicals will not bind to the receptor site and will not activate a response. Partial agonists are chemicals that have partial effects on the binding sites. Inverse agonists, as the name implies, reverse the effect of the agonists when it binds to the receptor site.
Examples
Agonists: heroin, oxycodone, methadone, hydrocodone, morphine, opium, ropinirole, pramipexole
Antagonists: naltrexone; fluoxetine is an antagonist at 5HT2C receptors; metoclopramide, prochlorperazine, promethazine
Partial agonist/antagonist: buprenorphine/naloxone; tramadol
Inverse agonist: risperidone, clozapine (partial)
The g couple proteins facilitate cellular response to many outside stimuli and activation stimulates secondary messengers to influence bodily response. These act on ion channels or enzymes in the cellular membranes. While the ion gated channels allow passive influx and/or efflux of ions as a response to receptor binding. There are three (3) ion gated channels: voltage-gated (i.e., response to changes in membrane potential), ligand/chemically-gated (i.e., opens with neurotransmitter binding), and mechanically-gated (i.e., opens with physical deformation).
Epigenetic regulation alters genetic expression without causing genotypic changes. This is an important factor on how drugs exert pharmacologic action. This is important in maintaining the normal activity of cells and treatment of many diseases including, but not limited to neurological and psychiatric conditions. There are many treatments developed for these conditions.
Every practitioner whether a medical doctor, physician assistant, or nurse practitioner should be knowledgeable of pharmacology. Each written prescription denotes full understanding of the therapeutic indications and contraindications, expected effects, side effects, adverse reactions, drug-to-drug interactions especially in patients who have complex conditions, etc. Each drug has specific pharmacological action which may be similar or completely different from other drugs.
However, care should always be on top of mind because there is drug interaction. For example, a patient who has treatment-resistant depression is being considered for tricyclic antidepressants (TCA), one of the many considerations will be to assess for presence of any cardiac arrhythmias. The TCAs inhibit presynaptic reuptake of neurotransmitters norepinephrine and serotonin which will increase concentration.
This type of antidepressant is known to cause toxicity or increased adverse effects when taken in high doses. Fatal cardiac events may occur such as wide QRS complex (in TCA toxicity), high blood pressure, and tachycardia is possible. The practitioner should consider conducting a thorough medical history, order necessary cardiac diagnostic tests, and provide patient education to assure overall safety.
References
Andreae, L. C., & Burrone, J. (2018). The role of spontaneous
neurotransmission in synapse and circuit development. Journal of
neuroscience research, 96(3), 354-359.
Cacabelos, R., & Torrellas, C. (2014). Epigenetic drug discovery for Alzheimer’s
disease. Expert Opinion on Drug Discovery, 9(9), 1059-1086.
doi:10.1517/17460441
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