NURS 6630 Discussion: Foundational Neuroscience

Discussion: Foundational Neuroscience

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The outstanding role that Psychiatric mental health nurse practitioners play in the management of psychiatric disorders cannot be underestimated. Undeniably, their knowledge regarding the pathophysiology of multifarious mental disorders need to be top notch. However, in addition to the pathophysiological knowhow, PMNHPs need to understand the various mechanisms of action of relevant medications and the manner in which they influence the central nervous system to stabilize the neurochemicals responsible for the existence of these conditions. Thus, PMNHPs require to have knowledge concerning the impact of psychopharmacological medications from their agnostic-to-antagonist spectrum of action. In addition, knowing about the roles of g-coupled proteins and ion gated channels in the entire process of managing mental health conditions becomes an important tool for these nurses. Further, other factors such as epigenetics also influence the pharmacologic action of drugs. As such, a collation of the above information may be fundamental in the prescription of medications to clients; hence, their analysis becomes important.

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Agonist-To-Antagonist Spectrum of Action of Psychopharmacologic Agents

            The prescription of psychopharmacological agents occurs based on the mechanisms of action of each molecule. Fundamentally, pharmacological actions of antipsychotics such as agonism and antagonism principally influences neurotransmitters or receptors. According to scholarship on the matter, agonists are referred to as the kinds of drugs or receptor ligands that bind to certain receptors in order to produce the desired therapeutic effect (Lee & Barron, 2017). Specifically, agonists bind to receptors and modulate the activation of the receptors in order to produce the requisite action. The modulation occurs when the agonists alter the conformation of the receptor in order to optimally open the ion channel as well as induce the maximum frequency of the receptors for binding purposes. As a consequence, a maximum downstream signal transduction that has the capacity to be mediated by a receptor occurs.

The above spectrum then moves to antagonists, which are utilized to stabilize the receptor to the resting phase. In other words, the antagonists are used to return ta receptor to its state when the agonists were not available. However, the resting state occasioned by the antagonists still has certain levels of ion flowing through the channel since the ion channel is not fully closed. Therefore, the agonist-to-antagonist spectrum of pharmacological agents entails agonists that open a receptor channel to maximal frequency and amount via antagonists that retain the resting state of a receptor, and lastly to inverse agonists that close and inactivate the receptor ion channel (Stahl, 2013). In between the antagonists and agonists are partial agonists that partially influences the receptor ion channels in comparison to the two. Further, antagonists have the potential to block everything within the agonist spectrum thus ensuring that the ion channel returns to its resting state. Thus, psychopharmacological agents assume this spectrum when addressing certain mental health conditions………….…………………….

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NUR 6630 Week 1 Discussion: Foundational Neuroscience

In one’s role as a psychiatric mental health nurse practitioner, it becomes critically important that they possess knowledge in foundational neuroscience. The knowledge is particularly significant when it comes to the diagnosis and treatment of clients as it will

enable one to comprehend the pathophysiology of the various conditions in addition to the impact of psychotropic medications on the central nervous system. However, the theories involved in foundational neuroscience can become very difficult to understand. For this reason, the present Discussion: Foundational Neuroscience is formulated to encourage one to ruminate about the concepts, establish a rationale for their thinking as well as deepen their understanding by interaction with their colleagues.

Learning Objectives

Students will:

• Compare the actions of g couple proteins to ion gated channels
• Analyze the agonist-to-antagonist spectrum of action of psychopharmacologic agents
• Analyze the impact of foundational neuroscience on the prescription of medications
• Analyze the role of epigenetics in pharmacologic action

Learning Resources

Note: To access this week’s required library resources, please click on the link to the Course Readings List, found in the Course Materials section of your Syllabus.

Required Readings

Note: All Stahl resources can be accessed through the Walden Library using this link. This link will take you to a log-in page for the Walden Library. Once you log into the library, the Stahl website will appear.

Stahl, S. M. (2013). Stahl’s essential psychopharmacology: Neuroscientific basis and practical applications (4th ed.). New York, NY: Cambridge University Press *Preface, pp. ix–x

• Note: To access the following chapters, click on the Essential Psychopharmacology, 4th ed tab on the Stahl Online website and select the appropriate chapter. Be sure to read all sections on the left navigation bar for each chapter.
• Chapter 1, “Chemical Neurotransmission”
• Chapter 2, “Transporters, Receptors, and Enzymes as Targets of Psychopharmacologic Drug Action”
• Chapter 3, “Ion Channels as Targets of Psychopharmacologic Drug Action”
• Document: Midterm Exam Study Guide (PDF)
• Document: Final Exam Study Guide (PDF)
• Required Media

Laureate Education (Producer). (2016i). Introduction to psychopharmacology [Video file]. Baltimore, MD: Author.

Note: The approximate length of this media piece is 3 minutes.

Accessible player

Discussion: Foundational Neuroscience

The traditional receptor theory classified the pharmacological agents as agonists and antagonists. An agonist is a chemical substance that binds to the receptor to stabilize the receptor inactive conformation to produce a biological response. The agonist causes the action, whereas the antagonist blocks the effect of an agonist. The drugs that fix and stimulates the receptor are known as an agonist, and the drugs that fix but not stimulate the receptors are known as the agonist. The agonists have two main properties, which are affinity and efficacy. Affinity is the tendency of the medicine to bind with the target cells or receptor, and efficacy is the capability of the agonist to generate biological influence by affecting neurotransmitter function and influencing or activating the target receptor sites (Beaulieu and Gainetdinov, 2011). The same receptor type can be related to a different kind of drug-producing the same response despite being different in affinity and functionality. The antagonist has the affinity but not efficacy; hence they occupy the receptor and stops or reduce the agonists from producing the response. The intrinsic efficacy of the agonists is variable and is characterized as full or partial agonists. The partial agonists are the psychotropic drugs that influence the receptors to a smaller degree than the natural neurotransmitters (Stahl, 2013). For example, aripiprazole is partial agonist dopamine and is effective in treating Schizophrenia by acting as an antipsychotic. A partial agonist can produce either agonist or antagonist effects. When a partial agonist is utilized with the full agonist, a partial agonist produces an antagonist effect by competing with the full agonist (Berg & Clarke, 2018). For example, methadone is full opioid agonist while buprenorphine is a partial agonist in the absence of the methadone reducing craving and withdrawal. Buprenorphine has a strong affinity for opioid receptors as it acts as a partial antagonist and competes against morphine methadone to reduce its affinity. When Buprenorphine (partial agonist) and naloxone are given together, naloxone has inverse agonist effects that prevent abuse (Lutfy & Cowan, 2004).

Comparisons and contrast of the actions of g couple protein and ion gated channels

Ion channel receptors are an essential component of the nervous system that signals and directly converts a chemical neurotransmitter message to an electrical current. Protein-protein interactions with other ion channels regulate ionotropic receptors, G-protein coupled receptors, and intracellular proteins (Li, Wong & Lu, 2014). G-couple proteins have receptors that are structured with seven transmembrane regions. They span the membrane seven times, containing binding sites for neurotransmitters that enable targeting specific psychotropic drugs (Stahl, 2013). G-protein is responsible for maintaining the electrochemical gradient across the cell. Ion channels open and close in direct response to the binding of a chemical messenger like a neurotransmitter. Both ion-gated channels and G-couple protein are protein receptors embedded in the cell membranes that bind to a signaling molecule (Stahl, 2013). Membrane changes can cause an electrical current, resulting in a pulse of neurotransmitter and electrical signal or change of voltage across the targeted cell membrane, which will allow for rapid transmission of the signal synapse.

Role of epigenetics in the pharmacologic action

Epigenetics is the mechanism of gene control that can promote or suppress the expression of the genes without altering the genetic coding of an organism. In epigenetics, an explanation of the composition of all the cells in the body is similar to gene pairs, but differentiation in the elements of deleted or expressed genes is described. Neurotransmission, genes, drugs, or environment determines the type of genes which are expressed or inhibited and influence the memory, stress response, brain learning, mental disorders, and improvement of disorders through drugs or psychotherapy (Stahl, 2013). Epigenetics does not directly affect people’s psychiatric or mental health but affects the way medication works on the patient (Stefanski, & MacEwan, 2015).

Explanation of the impact on the prescription of medications to clients

As a health care provider, it is essential to know the drug actions and interactions and the importance of the concepts before prescribing the medication to clients. For example, for the treatment of benzodiazepine overdose, flumazenil is utilized. Flumazenil is a benzodiazepine antagonist. Transduction reduction occurs when an agonist is present, and the antagonist is given as channels get closed instead of maximal flow (Nutt, Stahl, Blier, Drago & Zohar, 2017). Therefore, it is essential to know the mechanism to prevent complications & to improve the clinical effect when utilizing multiple medications. In addition, patients who have developed a dependence on benzodiazepines may experience withdrawal symptoms such as seizures when administrated flumazenil (Nutt, Stahl, Blier, Drago & Zohar, 2017).

References

Beaulieu, J. M., and Gainetdinov, R. R. (2011). The physiology, signaling, and pharmacology of dopamine receptors. Pharmacology. Rev. 63, 182–217. Retrieved from doi: 10.1124/pr.110.002642.

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

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. https://doi.org/10.3389/fncel.2014.00125

Lutfy, K., & Cowan, A. (2004). Buprenorphine: a unique drug with complex pharmacology. Current Neuropharmacology, 2(4), 395–402. https://doi.org/10.2174/1570159043359477

Nutt, D.S., Stahl, A.P, Blier, D., Drago, N.S., & Zohar. Key Concept in Psychopharmacology. Psychiatry 6(7), 263-267. Retrieved from https://doi.org/10.1016/j.mppsy.2007.05.002.

Stahl, S. M. (2013). Stahl’s essential psychopharmacology: Neuroscientific basis and practical applications (4th ed.). New York, NY: Cambridge University Press *Preface, pp. ix–x

Stefanski, B., & MacEwan, D. J. (2015, June). Epigenetics and pharmacology. British Journal of Pharmacology, 172(11), 2701-2704.

SAMPLE 3

Discussion Post Week 1

When a drug binds to a receptor there are one of two paths it can take; these drugs either mimic the action of the regulatory molecules or they block the action of these regulatory molecules. An agonist is defined as a drug that mimics the body’s regulatory molecules. Partial agonists are drugs that can bind to the receptor but are not capable of producing the full effect of an agonist. These partial agonists produce responses that are moderately intrinsic.  Any drug that has been classified as an antagonist will block the receptors so that they are unable to bind to the agonist (Rosenthal & Burchum, 2021).

One example of how a partial agonist may affect the overall efficacy of psychopharmacologic treatment would be the treatment of pain with the medication pentazocine, this medication alone could potentially offer some relief to the patient by binding to the receptors. If pentazocine is administered and the patient has already received the medication meperidine which is a full agonist, the pentazocine may alter the efficacy of the pentazocine by blocking some of the receptors; this partial agonist will not only be working as if it is an agonist but also appear to be working as an antagonist (Rosenthal & Burchum, 2021).

Two classes of postsynaptic receptors are G-protein coupled receptors and ion gated channels. Neurotransmitter receptors that are ligand-gated ion channels typically cause more rapid postsynaptic responses, G protein-coupled receptors mediate slower postsynaptic responses (Lodish et al, 2000).

As a provider, it is especially important to understand which medications our patients are prescribed and what each of these medications mechanism of action is if we unknowingly provide the patient with two medications that bind to the same receptors, we may in fact reduce the risk of properly treating our patient and causing the patient a great deal of pain or discomfort.

Epigenetics is the concept that genes may be altered without the alteration of the gene code and gene function maybe inherited (Stern et. al, 2016). Using epigenetics in pharmacology is beneficial as it allows us to create medications that can target many different receptor types and in turn provide more of a “global response” type of care (Stefanska & MacEwan, 2015). This type of epigenetic regulatory mechanism could potentially regulate large groups of genes, and this large group of genes maybe the underlying cause of a particular disease. By using epigenetics and a more global type of response we can treat diseases more effectively while if we were to target one single protein we may not be as successful in treating our patients.

References:

Rosenthal, L. D., & Burchum, J. R. (2021). Lehne’s pharmacotherapeutics for advanced

 

practice nurses and physician assistants (2^nd ed.) St. Louis, MO: Elsevier.

 

Lodish, H., Berk, A., & Zibursky, S. L. (2000). Molecular cell biology 4th edition. W H Freeman

& Co.

Stern T.A, Favo, M., Wilens, T.E., & Rosenbaum, J. F. (2016). Massachusetts General Hospital Psychopharmacology and neurotherapeutics (pp. 1-19). Elsevier.

Stefanska, B., & MacEwan, D. J. (2015). Epigenetics and pharmacology. British journal of pharmacology, 172(11), 2701–2704. https://doi.org/10.1111/bph.13136

Optional Resources

Laureate Education (Producer). (2009). Pathopharmacology: Disorders of the nervous system: Exploring the human brain [Video file]. Baltimore, MD: Author.

Note: The approximate length of this media piece is 15 minutes.

Dr. Myslinski reviews the structure and function of the human brain. Using human brains, he examines and illustrates the development of the brain and areas impacted by disorders associated with the brain.

Accessible player

Laureate Education (Producer). (2012). Introduction to advanced pharmacology [Video file]. Baltimore, MD: Author.

Note: The approximate length of this media piece is 8 minutes.

In this media presentation, Dr. Terry Buttaro, associate professor of practice at Simmons School of Nursing and Health Sciences, discusses the importance of pharmacology for the advanced practice nurse.

Accessible player

To prepare for this Discussion:

Review this week’s Learning Resources.

Reflect on concepts of foundational neuroscience.

Rubric Detail

Select Grid View or List View to change the rubric’s layout.

Name: NURS_6630_Week2_Discussion_Rubric

Response to the Discussion question is reflective with critical analysis and synthesis representative of knowledge gained from the course readings for the module and current credible sources.
40 (40%) – 44 (44%)
Thoroughly responds to the Discussion question(s).

Is reflective with critical analysis and synthesis representative of knowledge gained from the course readings for the module and current credible sources.

No less than 75% of post has exceptional depth and breadth.

Supported by at least three current credible sources.
35 (35%) – 39 (39%)
Responds to most of the Discussion question(s).

Is somewhat reflective with critical analysis and synthesis representative of knowledge gained from the course readings for the module.

50% of the post has exceptional depth and breadth.

Supported by at least three credible references.
31 (31%) – 34 (34%)
Responds to some of the Discussion question(s).

One to two criteria are not addressed or are superficially addressed.

Is somewhat lacking reflection and critical analysis and synthesis.

Somewhat represents knowledge gained from the course readings for the module.

Post is cited with fewer than two credible references.
0 (0%) – 30 (30%)
Does not respond to the Discussion question(s).

Lacks depth or superficially addresses criteria.

Lacks reflection and critical analysis and synthesis.

Does not represent knowledge gained from the course readings for the module.

Contains only one or no credible references.
Main Posting:

Writing
6 (6%) – 6 (6%)
Written clearly and concisely.

Contains no grammatical or spelling errors.

Adheres to current APA manual writing rules and style.
5 (5%) – 5 (5%)
Written concisely.

May contain one to two grammatical or spelling errors.

Adheres to current APA manual writing rules and style.
4 (4%) – 4 (4%)
Written somewhat concisely.

May contain more than two spelling or grammatical errors.

Contains some APA formatting errors.
0 (0%) – 3 (3%)
Not written clearly or concisely.

Contains more than two spelling or grammatical errors.

Does not adhere to current APA manual writing rules and style.
Main Posting:

Timely and full participation
9 (9%) – 10 (10%)
Meets requirements for timely, full, and active participation.

Posts main Discussion by due date.
8 (8%) – 8 (8%)
Posts main Discussion by due date.

Meets requirements for full participation.
7 (7%) – 7 (7%)
Posts main Discussion by due date.
0 (0%) – 6 (6%)
Does not meet requirements for full participation.

Does not post main Discussion by due date.
First Response:

Post to colleague’s main post that is reflective and justified with credible sources.
9 (9%) – 9 (9%)
Response exhibits critical thinking and application to practice settings.

Responds to questions posed by faculty.

The use of scholarly sources to support ideas demonstrates synthesis and understanding of learning objectives.
8 (8%) – 8 (8%)
Response has some depth and may exhibit critical thinking or application to practice setting.
7 (7%) – 7 (7%)
Response is on topic, may have some depth.
0 (0%) – 6 (6%)
Response may not be on topic, lacks depth.
First Response:
Writing
6 (6%) – 6 (6%)
Communication is professional and respectful to colleagues.

Response to faculty questions are fully answered, if posed.

Provides clear, concise opinions and ideas that are supported by two or more credible sources.

Response is effectively written in Standard, Edited English.
5 (5%) – 5 (5%)
Communication is mostly professional and respectful to colleagues.

Response to faculty questions are mostly answered, if posed.

Provides opinions and ideas that are supported by few credible sources.

Response is written in Standard, Edited English.
4 (4%) – 4 (4%)
Response posed in the Discussion may lack effective professional communication.

Response to faculty questions are somewhat answered, if posed.

Few or no credible sources are cited.
0 (0%) – 3 (3%)
Responses posted in the Discussion lack effective communication.

Response to faculty questions are missing.

No credible sources are cited.
First Response:
Timely and full participation
5 (5%) – 5 (5%)
Meets requirements for timely, full, and active participation.

Posts by due date.
4 (4%) – 4 (4%)
Meets requirements for full participation.

Posts by due date.
3 (3%) – 3 (3%)
Posts by due date.
0 (0%) – 2 (2%)
Does not meet requirements for full participation.

Does not post by due date.
Second Response:
Post to colleague’s main post that is reflective and justified with credible sources.
9 (9%) – 9 (9%)
Response exhibits critical thinking and application to practice settings.

Responds to questions posed by faculty.

The use of scholarly sources to support ideas demonstrates synthesis and understanding of learning objectives.
8 (8%) – 8 (8%)
Response has some depth and may exhibit critical thinking or application to practice setting.
7 (7%) – 7 (7%)
Response is on topic, may have some depth.
0 (0%) – 6 (6%)
Response may not be on topic, lacks depth.
Second Response:
Writing
6 (6%) – 6 (6%)
Communication is professional and respectful to colleagues.

Response to faculty questions are fully answered, if posed.

Provides clear, concise opinions and ideas that are supported by two or more credible sources.

Response is effectively written in Standard, Edited English.
5 (5%) – 5 (5%)
Communication is mostly professional and respectful to colleagues.

Response to faculty questions are mostly answered, if posed.

Provides opinions and ideas that are supported by few credible sources.

Response is written in Standard, Edited English.
4 (4%) – 4 (4%)
Response posed in the Discussion may lack effective professional communication.

Response to faculty questions are somewhat answered, if posed.

Few or no credible sources are cited.
0 (0%) – 3 (3%)
Responses posted in the Discussion lack effective communication.

Response to faculty questions are missing.

No credible sources are cited.
Second Response:
Timely and full participation
5 (5%) – 5 (5%)
Meets requirements for timely, full, and active participation.

Posts by due date.
4 (4%) – 4 (4%)
Meets requirements for full participation.

Posts by due date.
3 (3%) – 3 (3%)
Posts by due date.
0 (0%) – 2 (2%)
Does not meet requirements for full participation.

Does not post by due date.
Total Points: 100
Name: NURS_6630_Week2_Discussion_Rubric

Stahl, S. M. (2013). Stahl’s essential psychopharmacology: Neuroscientific basis and practical applications (4th ed.). New York, NY: Cambridge University Press *Preface, pp. ix–x