- 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.
Agonist to antagonist spectrum of action on psychopharmacologic agents are unique because of intrinsic efficacy of the drug. Agonist are drugs that bind to receptors to produce a response, whereas antagonist bind to receptors while producing no response. Agonist have intrinsic efficacy giving it the ability to change a receptors activity to elicit a response. Psychopharmacologic agents are adjusted to increase or decrease the amounts of agonist and antagonist targeting various receptors to elicit a wanted response. Partial agonist produces partial response on the receptor and the inverse agonist decrease the activity of a receptor. Full, partial, and inverse agonist may differ in intrinsic efficacy allowing for pharmacologist to have a greater control over receptor functions (Berg and Clark, 2018). Naloxone is an example of an antagonist that occupies the opioid receptor and prevents the euphoric effects of opioid agonist such as heroin (Camprodon and Roffman, 2016)
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Compare and contrast the actions of g couple proteins and ion gated channels.
G proteins are metabotropic receptors that do not have ion channels as part of their structure. They contain a neurotransmitter binding site and an intracellular domain that binds to g proteins. Ion gated channels are neurotransmitters that are large in size that combine receptors and ion channel functions into a single molecule, changing the protein receptor ( Kniazeff, 2020).
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Explain how the role of epigenetics may contribute to pharmacologic action.
NURS 6630 Discussion Foundational Neuroscience
Epigenetics studies how biological mechanisms can control the expression of genes. Patients who have resistance to traditional medications can explore pharmaceutical agents through epigenetics. Though, the medications that are aimed to treat diseases through epigenetics are nonspecific, however as more research is conducted on DNA, pharmacologic action will be improved due to the increased specificity of the target medications and treatments (Prabhakar, 2017).
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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.
Information about agonist, antagonist, full, partial, and inverse agonist will impact the way I prescribe medications to patients because
based on the sort of treatment the patients’ needs will affect the class of medication, dosage, and frequency of the prescribed medications to the patient. Based on the medication that is prescribed for the patient, various side or adverse effects should be monitored to prevent harm to the patient. A psychiatric nurse practitioner is evaluating a patient who has severe depression, should properly assess the patients three week history and also thoughts of suicide. Based on this evaluation, the nurse practitioner will prescribe medications that do not have reports of increase suicidal ideations or sadness by other patients.
NURS 6630 Discussion Foundational Neuroscience 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
Camprodon, J. A., & Roffman, J. L. (2016). Psychiatric neuroscience: Incorporating pathophysiology into clinical case formulation. Massachusetts General Hospital psychopharmacology and neurotherapeutics. (pp. 1–19). Elsevier.
Kniazeff, J. (2020). Guanine Nucleotide Binding protein. Advances in Pharmacology. https://www.sciencedirect.com/topics/pharmacology-toxicology-and-pharmaceutical-science/guanine-nucleotide-binding-protein
Purves, D., et al. ( e Neuroscience. 2nd edition. Sunderland (MA): Sinauer Associates; 2001. Two Families of Postsynaptic Receptors. Available from: https://www.ncbi.nlm.nih.gov/books/NBK10855/
Prabhakar, B., Zhong, X. B., & Rasmussen, T. P. (2017). Exploiting Long Noncoding RNAs as Pharmacological Targets to Modulate Epigenetic Diseases. The Yale journal of biology and medicine, 90(1), 73–86.
RE: Week 2 Discussion
COLLAPSE
As a psychiatric and mental health 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.
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.
ResourcesBe sure to review the Learning Resources before completing this activity.
Click the weekly resources link to access the resources.
WEEKLY RESOURCES
By Day 3 of Week 2
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.Read a selection of your colleagues' responses.
Hello Temitope, your post was interesting, As you rightly mention, an antagonist is a drug designed to oppose an agonist’s actions directly. Using the lock and key analogy, an antagonist is like a key that fits nicely into the lock but does not have the right shape to turn the lock. When this key (antagonist) is inserted in the lock, the proper key (agonist) cannot go into the same lock. NURS 6630 Discussion Foundational Neuroscience
So, the agonist’s actions are blocked by the presence of the antagonist in the receptor molecule. Let’s think of morphine as an agonist for the opioid receptor. If someone is experiencing a potentially lethal morphine overdose, the opioid receptor antagonist naloxone can reverse the effects. This is because naloxone (marketed as Narcan) quickly occupies all the opioid receptors in the body and prevents morphine from binding to and activating them.
Morphine bounces in and out of the receptor in seconds. When it is not bound to the receptor, the antagonist can get in and block it. Because the receptor cannot be activated once an antagonist occupies the receptor, there is no reaction. The effects of Narcan can be dramatic. Even if the overdose victim is unconscious or near death, they can become fully conscious and alert within seconds of injection (Martínez, Ibarra & Vargas, 2019).
NURS 6630 Discussion Foundational Neuroscience 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
Martínez, A., Ibarra, I. A., & Vargas, R. (2019). A quantum chemical approach representing a new perspective concerning agonist and antagonist drugs in the context of schizophrenia and Parkinson’s disease. PLoS One, 14(12) doi:http://dx.doi.org.ezp.waldenulibrary.org/10.1371/journal.pone.0224691
A Sample Answer For the Assignment: NURS 6630 Discussion Foundational Neuroscience
Title: NURS 6630 Discussion Foundational Neuroscience
RE: Week 2 Discussion
COLLAPSE
The knowledge of the spectrum of activity of drugs allows a clinician to practice rational prescribing and use of drugs based on the pathophysiological targets. The use of drugs that modulate the agonistic and antagonistic response on the targeted receptor may be necessary for proper address of patient symptoms. A good example is the use of partial agonists such as buprenorphine in the treatment of opioid use disorder to avoid severe withdrawal symptoms such as seizures and the concomitant use of an antagonists such as naloxone to prevent side effects of opioid use such as respiratory depression and aid in ultimate abstinence from opioids and reduce risk of abuse. The combination therapy has been shown to induce modulation of dopamine homeostasis associated with reduction of drug seeking behavior, withdrawal symptoms and relapse and fostering of abstinence (Blum et al., 2018).
Epigenetic mechanisms such s histone acetylation and DNA methylation have been shown to be disturbed in pathological processes such as those observed in mood disorders and therapies targeting some of these processes such as histone deacetylase inhibitors have shown promise in management of mood disorders such as depression. The use of nutraceuticals for management of mood disorders e.g. depression such as folic acid and vitamin B12 has been shown to be linked to modulation of epigenetics due to their effect on generation of S adenosyl methionine which is the main methyl donor for several reactions including DNA methylation (Peedicayil & Kumar, 2018). NURS 6630 Discussion Foundational Neuroscience
NURS 6630 Discussion Foundational Neuroscience References
Blum, K., Gold, M., Modestino, E., Febo, M., Thanos, P. K., Baron, D., Steinberg, B., Fried, L., & Badgaiyan, R. (2018). Buprenorphine and naloxone combinations and dopamine. Current Psychopharmacology, 6(2). https://doi.org/10.2174/2211556006666170926165840
Peedicayil, J., & Kumar, A. (2018). Epigenetic drugs for mood disorders. Progress in Molecular Biology and Translational Science, 151-174. https://doi.org/10.1016/bs.pmbts.2018.01.005
Allthough I have been always amazed on how we have used medicines, especially psychotropic meds to induce agonist or antagonist effects to treat multiple psychiatric medications, what really amazes me is how we can use and benefit from epigenetics to treat and control these disoders, and may be prevent this from being passed from a parent to his/her own offsprings (Stahl, 2021). Mountain evidence suggests that epigenetic mechanisms, which induce stable and lasting changes in gene expression in response to environmental events and behavioral experiences, may play a role in the processess that contribute to the pathophysiology of psychiatric disorders (Mahgoub & Monteggia, 2013).
Epigenetics is a process that can change gene expression, without alterations of the DNA sequence and promote stable changes in the Chromatin structure (Stahl, 2021; Maghoub & Monteggia, 2013; Stern, et. al., 2016). A good application of epigenetics in psychiatric disoderders are the following examples:
- The modification of brain derived neurotrophic factor (BDNF) as a potential therapeutic target in antidepressant action as well as in mediating antidepressant response (Mahgoub & Monteggia, 2013)
- The involvement of BDNF to addiction. Acute administration of cocaine induces release of BDNF in the ventral tegmented area (reward system)
- Involvement of histone H4 deacetylases in cocaine addiction. Histone play a crucial role in regulating gene activity by inducing modifications in chromatin structure (Mahgoub & Monteggia, 2013)
- The involvement and modification of DNA methylation within GABA in schizophrenia. There was a downward regulation of several genes expressed within the GABA neurons (Chen, et. al, as cited in Mahgoub & Monteggia, 2013)
Much emphasis has been placed right now on histone modifications and DNA methylation for using pharmacologic inhibitors in treating multiple disorders. Both histone acetylation and DNA methylation can induce lasting and stable changes in gene expression, and therefore have been implicated in adaptive behaviors and neuronal changes that accompany many psychiatric disorders.
NURS 6630 Discussion Foundational Neuroscience References:
Mahgoub, M., & Monteggia, L. (2013). Epigenetics and Psychiatry. https://ncbi.nlm.nih.gov/pmc/articles/PMC3805856
Stahl, S. (2021). Stahl’s Essential Psychopharmacology: Neuroscientific Basis and Practical Approach. 5th ed. Cambridge
Stern, T., et. al (2016). Massachusetts General Hospital Psychopharmacology and Neurotherapeutics. 1st ed. Elsevier
NURS 6630 Discussion Foundational Neuroscience Grading Rubric Guidelines DQ
| Performance Category |
10 |
9 |
8 |
4 |
0 |
| Scholarliness
Demonstrates achievement of scholarly inquiry for professional and academic decisions. |
- Provides relevant evidence of scholarly inquiry clearly stating how the evidence informed or changed professional or academic decisions
- Evaluates literature resources to develop a comprehensive analysis or synthesis.
- Uses valid, relevant, and reliable outside sources to contribute to the threaded discussion
|
- Provides relevant evidence of scholarly inquiry but does not clearly state how the evidence informed or changed professional or academic decisions.
- Evaluates information from source(s) to develop a coherent analysis or synthesis.
- Uses some valid, relevant, reliable outside sources to contribute to the threaded discussion.
|
- Discusses using scholarly inquiry but does not state how scholarly inquiry informed or changed professional or academic decisions.
- Information is taken from source(s) with some interpretation/evaluation, but not enough to develop a coherent analysis or synthesis.
- Little valid, relevant, or reliable outside sources are used to contribute to the threaded discussion.
- Demonstrates little or no understanding of the topic.
|
- Discusses using scholarly inquiry but does not state how scholarly inquiry informed or changed professional or academic decisions.
- Information is taken from source(s) without any interpretation/evaluation.
- The posting uses information that is not valid, relevant, or reliable
|
- No evidence of the use of scholarly inquiry to inform or change professional or academic decisions.
- Information is not valid, relevant, or reliable
|
| Performance Category |
10 |
9 |
8 |
4 |
0 |
| Application of Course Knowledge –
Demonstrate the ability to analyze, synthesize, and/or apply principles and concepts learned in the course lesson and outside readings and relate them to real-life professional situations |
- Posts make direct reference to concepts discussed in the lesson or drawn from relevant outside sources;
- Applies concepts to personal experience in the professional setting and or relevant application to real life.
|
- Posts make direct reference to concepts discussed in the lesson or drawn from relevant outside sources.
- Applies concepts to personal experience in their professional setting and or relevant application to real life
- Interactions with classmates are relevant to the discussion topic but do not make direct reference to lesson content
|
- Posts are generally on topic but do not build knowledge by incorporating concepts and principles from the lesson.
- Does not attempt to apply lesson concepts to personal experience in their professional setting and or relevant application to real life
- Does not demonstrate a solid understanding of the principles and concepts presented in the lesson
|
- Posts do not adequately address the question posed either by the discussion prompt or the instructor’s launch post.
- Posts are superficial and do not reflect an understanding of the lesson content
- Does not attempt to apply lesson concepts to personal experience in their professional setting and or relevant application to real life
|
- Posts are not related to the topics provided by the discussion prompt or by the instructor; attempts by the instructor to redirect the student are ignored
- No discussion of lesson concepts to personal experience in the professional setting and or relevant application to real life
|
| Performance Category |
5 |
4 |
3 |
2 |
0 |
| Interactive Dialogue
Replies to each graded thread topic posted by the course instructor, by Wednesday, 11:59 p.m. MT, of each week, and posts a minimum of two times in each graded thread, on separate days.
(5 points possible per graded thread) |
- Exceeds minimum post requirements
- Replies to each graded thread topic posted by the course instructor, by Wednesday, 11:59 p.m. MT, of each week, and posts three or more times in each graded thread, over three separate days.
- Replies to a post posed by faculty and to a peer
- Summarizes what was learned from the lesson, readings, and other student posts for the week.
|
- Replies to each graded thread topic posted by the course instructor, by Wednesday, 11:59 p.m. MT, of each week, and posts a minimum of two times in each graded thread, on separate days
- Replies to a question posed by a peer
Summarizes what was learned from the lesson, readings, and other student posts for the week. |
- Meets expectations of 2 posts on 2 different days.
- The main post is not made by the Wednesday deadline
- Does not reply to a question posed by a peer or faculty
|
- Has only one post for the week
- Discussion posts contain few, if any, new ideas or applications; often are a rehashing or summary of other students’ comments
|
- Does not post to the thread
- No connections are made to the topic
|
| |
Minus 1 Point |
Minus 2 Point |
Minus 3 Point |
Minus 4 Point |
Minus 5 Point |
| Grammar, Syntax, APA
Note: if there are only a few errors in these criteria, please note this for the student in as an area for improvement. If the student does not make the needed corrections in upcoming weeks, then points should be deducted.
Points deducted for improper grammar, syntax and APA style of writing.
The source of information is the APA Manual 6th Edition |
- 2-3 errors in APA format.
- Written responses have 2-3 grammatical, spelling, and punctuation errors.
- Writing style is generally clear, focused, and facilitates communication.
|
- 4-5 errors in APA format.
- Writing responses have 4-5 grammatical, spelling and punctuation errors.
- Writing style is somewhat focused.
|
- 6-7 errors in APA format.
- Writing responses have 6-7 grammatical, spelling and punctuation errors.
- Writing style is slightly focused making discussion difficult to understand.
|
- 8-10 errors in APA format.
- Writing responses have 8-10 grammatical, spelling and punctuation errors.
- Writing style is not focused, making discussion difficult to understand.
|
- Post contains greater than 10 errors in APA format.
- Written responses have more than 10 grammatical, spelling and punctuation errors.
- Writing style does not facilitate communication.
- The student continues to make repeated mistakes in any of the above areas after written correction by the instructor
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|
0 points lost |
|
|
|
-5 points lost |
| Total Participation Requirements
per discussion thread |
The student answers the threaded discussion question or topic on one day and posts a second response on another day. |
|
|
|
The student does not meet the minimum requirement of two postings on two different days |
| Early Participation Requirement
per discussion thread |
The student must provide a substantive answer to the graded discussion question(s) or topic(s), posted by the course instructor (not a response to a peer), by Wednesday, 11:59 p.m. MT of each week. |
|
|
|
The student does not meet the requirement of a substantive response to the stated question or topic by Wednesday at 11:59 pm MT. |
