Week 2 Discussion NURS 6630

Discussion: Foundational Neuroscience

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.

Discussion Instructions

Post a response to each of the following:

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.

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

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

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.

5. At least 5 references

Instructions:

Respond to your colleague in one of the following ways:

· If your colleagues’ posts influenced your understanding of these concepts, be sure to share how and why. Include additional insights you gained.

· If you think your colleagues might have misunderstood these concepts, offer your alternative perspective and be sure to provide an explanation for them. Include resources to support your perspective.

**minimum of three (3) scholarly references are required for each reply cited within the body of the reply & at the end**

Reply # 1

Ozichukwu Awusah

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.

In order to be effective, drugs must be able to reach their intended cells and attach to the appropriate receptors on those cells. It will be easier to explain how partial and inverse agonist function affects the effectiveness of therapies if you understand the distinction between the agonist and antagonist spectrum of action in relation to psychopharmacologic medicines. This receptor binding alters the activity or behavior of the cell by agonizing or antagonizing the cell’s normal reaction, depending on the situation. Agonists are medications that function by activating the receptors in the body. The antagonist binds to the receptor without activating it, preventing the receptor from being triggered by additional agonists in the future. Full agonists give the greatest possible reaction since they bind to all of the accessible receptors. Partially agonists only bind to a subset of receptors, resulting in a reduced response even at larger concentrations of the agonist. Agonists constantly stimulate the receptors to produce a certain natural reaction, while the antagonist attempts to displace the agonist by blocking the agonist’s route to the receptors and preventing it from reaching the receptors. Inverse agonists have the opposite effect of their agonist counterparts. According to pharmacological definition, an inverse agonist is a substance that binds to the same receptor as an agonist but produces the pharmacological response that is the inverse of the reaction produced by the agonist.

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

Both the G coupled protein receptors (GCPR) and the ion gated channels allow our cells to communicate with extracellular contents via specific integral receptors embedded into the cell membrane. When ligands bind to the receptor on an ion gated channel, there is a conversion of a chemical signal into an electrical one. As the channel opens it allows K+, Na+, Cl+, and Ca+ to move through the cell membrane and change its electrical properties. Thus, the ion gated channels produce a faster signal than the GCPRs. G-protein coupled receptors compromise the largest family of transmembrane proteins. They convey signals across the membrane in response to the binding of a particular ligand, resulting in the initiation of a cellular signaling cascade and the generation of an intracellular reaction. While the G protein is not the actual receptor, it is a protein that is connected to the receptor and that is activated by a particular ligand that binds to the receptor in order to transmit the activity inside the cell. The activation of an intracellular signaling cascade is induced by GCPRs.

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

It has long been understood that both environmental and genetic variables influence gene expression in different ways. It is the theory of epigenetics that genes may be activated or silenced depending on the presence or absence of certain chemical changes. The nucleotide sequence of the gene is not altered as a result of these variations in gene function. Epigenetics is a study that untangles the clues that suggested gene function and sequences that can be related to illnesses, behaviors, and other health indicators (Anderson et al.,2019). This includes an understanding of the influence of the phenotype of the DNA sequence. This research has found epigenetic mechanisms that are linked to cancers, cognitive dysfunction, respiratory, cardiovascular, reproductive, autoimmune, and neurobehavioral illnesses (Anderson et al.,2019). With this knowledge, pharmacologic action related to diseases linked with epigenetics can be created to regulate epigenetic mechanisms for the management of patients.

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.

Each mental disease and its relationship to psychopharmacology should be understood by psychiatric mental health nurse practitioners (PMHNP). A patient with a bipolar illness diagnosis should be extensively assessed in terms of family history, behaviors, and patient history. In terms of parents passing down this condition, family history plays a part in bipolar disorder. According to research, clinical differences between manic and depressive episodes may allow for the discovery of biomarkers that influence mood-stabilizers on the epigenome (Legrand, et. al., 2021). Although this has been detected, no precise indicators have been discovered, and further study is required. Patient behaviors should be examined in light of neurotransmitter abnormalities associated with the condition. Neurotransmitters such as serotonin, norepinephrine, dopamine, and GABA have been linked to bipolar illness. The lack of two neurotransmitters, serotonin, and norepinephrine, has been related to depression. Shi et al. (2008) Furthermore, dopamine agonists have been demonstrated to cause manic or severe depressive episodes while alleviating manic or depressed symptoms (Shi, et. al, 2008). GABA deficiencies have been associated with bipolar depressive episodes and stress-related depression behaviors in animal studies (Shi, et. al., 2008).

References

Anderson, E. M., Penrod, R. D., Barry, S. M., Hughes, B. W., Taniguchi, M., & Cowan, C. W. (2019). It

is a complex issue: emerging connections between epigenetic regulators in drug addiction?

The European Journal of Neuroscience, 50(3), 2477–2491

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).

Stefanska, B., & MacEwan, D. J. (2015). Epigenetics and pharmacology. British Journal of

Pharmacology, 172(11), 2701–2704. https://doiorg.ezp.waldenulibrary.org/10.1111/bph.13136

Legrand, A., Iftimovici, A., Khayachi, A., & Chaumette, B. (2021). Epigenetics in bipolar disorder: a

critical review of the literature. Psychiatric genetics, 31(1), 1– 12

https://doi.org/10.1097/YPG.0000000000000267

Shi, J., Badner, J. A., Hattori, E., Potash, J. B., Willour, V. L., McMahon, F. J., Gershon, E. S., & Liu, C.

(2008). Neurotransmission and bipolar disorder: a systematic family-based association study.

American journal of medical genetics. Part B, Neuropsychiatric genetics: the official publication

Please Repond to Mackenzie Gray

Week 2 Discussion Agonist-to-Antagonist Spectrum

An agonist is a drug that binds to and activates the receptor and yields a biological response (Salahudeen & Nishtala, 2017). Agonists allow the ion channels to be fully open, which enabling the drug to bind fully to the receptor site (Stahl, 2013). Agonists have an efficacy of one; therefore, these drugs are fully capable of producing a pharmacological response when bound to a receptor (Salahudeen & Nishtala, 2017).

An antagonist is a drug that binds to receptors and obstructs the agonist from the receptor site (Salahudeen & Nishtala, 2017). Antagonists can partially block agonists and reduce the agonist’s effects; however, antagonists may also completely block agonists if the concentration is high enough (Salahudeen & Nishtala, 2017). Antagonists have an efficacy of zero; therefore, these drugs are incapable of producing a pharmacological response (Salahudeen & Nishtala, 2017). Antagonists allow ions and receptors to be in their resting states (Stahl, 2013).

Partial and inverse agonists function in ways that can interfere with psychopharmacologic treatments. A partial agonist is a drug that can bind and activate the receptor, but it is unable to produce an adequate response (Salahudeen & Nishtala, 2017). Partial agonists have an efficacy range greater than zero but less than one (Salahudeen & Nishtala, 2017). An inverse agonist is an agonist that generates the opposite pharmacological response (Salahudeen & Nishtala, 2017).

G-Protein Coupled Receptors and Ion Gated Channels

G-protein coupled receptors (GPCRs) are essential proteins because cells use them to transmit extracellular stimuli into intracellular responses (Zhao et al., 2016). For example, GPCRs respond to hormones, neurotransmitters, and senses (Zhao et al., 2016). GCPR structure has seven transmembrane helices (Zhao et al., 2016). GPCRs are numerous and are the largest transmembrane receptor group in humans (Zhao et al., 2016). GCPRs bind to G proteins, which results in further signal pathways being activated (Zhao et al., 2016). GCPRs work slowly to relay messages due to the multi-step pathway to forward information (Camprodon & Roffman, 2016).

Ligand-gated ion channels have several long amino acid strands divided into smaller subunits around an ion channel (Stahl, 2013). The amino acid strands have receptor binding sites for various items, such as neurotransmitters, ions, and drugs (Stahl, 2013). Ligand-gated ion channels are often arranged in subunits consisting of five proteins, which are further divided into four transmembrane areas (Stahl, 2013). Ions flow through the channels rapidly compared to GPCRs (Camprodon & Roffman, 2016).

Epigenetics

Epigenetics is the study of how one’s environment or behaviors may alter their gene expression without changing the genetic code (Camprodon & Roffman, 2016). Research suggests that an individual’s epigenetic changes may influence their response to drugs, and provider awareness of epigenetic changes may be essential for therapeutic response to drugs (Schuebel et al., 2016). For example, if a patient experiences alteration to chromatin, they should be treated with a drug that affects the structure of chromatic, such as valproic acid (Camprodon & Roffman, 2016).

Prescribing Considerations

When prescribing medications, PMHNPs must be cognizant of a drug’s action and how individuals may metabolize the drug. For example, fluoxetine is metabolized by the cytochrome P450 2D6 (Eli Lilly and Company, 2006). Individuals who are deficient in this cytochrome may experience slower metabolization of fluoxetine, resulting in higher concentrations of fluoxetine (Eli Lilly and Company, 2006). These individuals may need a lower dose of fluoxetine to experience therapeutic effects (Eli Lilly and Company, 2006). Patients may experience mania if fluoxetine concentrations are too high (Eli Lilly and Company, 2006).

References

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.

Eli Lilly and Company. (2006). Prozac [package insert]. Retrieved from https://www.accessdata.fda.gov/drugsatfda_docs/lab…

Salahudeen, M. S., & Nishtala, P. S. (2017). An overview of pharmacodynamic modelling, ligand-binding approach and its application in clinical practice. Saudi Pharmaceutical Journal: The Official Publication of the Saudi Pharmaceutical Society, 25(2), 165–175. https://doi.org/10.1016/j.jsps.2016.07.002

Schuebel, K., Gitik, M., Domschke, K., & Goldman, D. (2016). Making sense of epigenetics. The International Journal of Neuropsychopharmacology, 19(11), pyw058. https://doi.org/10.1093/ijnp/pyw058

Stahl, S. M. (2013). Stahl’s essential psychopharmacology: Neuroscientific basis and practical applications (4th ed.). Cambridge University Press.

Zhao, J., Deng, Y., Jiang, Z., & Qing, H. (2016). G protein-coupled receptors (GPCRs) in Alzheimer’s Disease: A focus on BACE1 related GPCRs. Frontiers in Aging Neuroscience, 8, 58. https://doi.org/10.3389/fnagi.2016.00058

ADDITIONAL INSTRUCTIONS FOR THE CLASS

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Discussion Questions (DQ)

Initial responses to the DQ should address all components of the questions asked, including a minimum of one scholarly source, and be at least 250 words. Successful responses are substantive (i.e., add something new to the discussion, engage others in the discussion, well-developed idea) and include at least one scholarly source. One or two-sentence responses, simple statements of agreement or “good post,” and responses that are off-topic will not count as substantive. Substantive responses should be at least 150 words. I encourage you to incorporate the readings from the week (as applicable) into your responses.

Weekly Participation

Your initial responses to the mandatory DQ do not count toward participation and are graded separately. In addition to the DQ responses, you must post at least one reply to peers (or me) on three separate days, for a total of three replies. Participation posts do not require a scholarly source/citation (unless you cite someone else’s work). Part of your weekly participation includes viewing the weekly announcement and attesting to watching it in the comments. These announcements are made to ensure you understand everything that is due during the week.

APA Format and Writing Quality

Familiarize yourself with the APA format and practice using it correctly. It is used for most writing assignments for your degree. Visit the Writing Center in the Student Success Center, under the Resources tab in Loud-cloud for APA paper templates, citation examples, tips, etc. Points will be deducted for poor use of APA format or absence of APA format (if required). Cite all sources of information! When in doubt, cite the source. Paraphrasing also requires a citation. I highly recommend using the APA Publication Manual, 6th edition.

Use of Direct Quotes

I discourage over-utilization of direct quotes in DQs and assignments at the Master’s level and deduct points accordingly. As Masters’ level students, it is important that you be able to critically analyze and interpret information from journal articles and other resources. Simply restating someone else’s words does not demonstrate an understanding of the content or critical analysis of the content. It is best to paraphrase content and cite your source.

LopesWrite Policy

For assignments that need to be submitted to Lopes Write, please be sure you have received your report and Similarity Index (SI) percentage BEFORE you do a “final submit” to me. Once you have received your report, please review it. This report will show you grammatical, punctuation, and spelling errors that can easily be fixed. Take the extra few minutes to review instead of getting counted off for these mistakes. Review your similarities. Did you forget to cite something? Did you not paraphrase well enough? Is your paper made up of someone else’s thoughts more than your own? Visit the Writing Center in the Student Success Center, under the Resources tab in Loud-cloud for tips on improving your paper and SI score. Week 2 Discussion NURS 6630

Late Policy

The university’s policy on late assignments is a 10% penalty PER DAY LATE. This also applies to late DQ replies. Please communicate with me if you anticipate having to submit an assignment late. I am happy to be flexible, with advance notice. We may be able to work out an extension based on extenuating circumstances. If you do not communicate with me before submitting an assignment late, the GCU late policy will be in effect. I do not accept assignments that are two or more weeks late unless we have worked out an extension. As per policy, no assignments are accepted after the last day of class. Any assignment submitted after midnight on the last day of class will not be accepted for grading.

Communication

Communication is so very important. There are multiple ways to communicate with me: Questions to Instructor Forum: This is a great place to ask course content or assignment questions. If you have a question, there is a good chance one of your peers does as well. This is a public forum for the class. Individual Forum: This is a private forum to ask me questions or send me messages. This will be checked at least once every 24 hours. Week 2 Discussion NURS 6630

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Week 2 Discussion NURS 6630