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NURS 6630 Discussion Foundational Neuroscience

NURS 6630 Discussion 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.

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)

  1. 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).

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

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).

  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.

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

NURS 6630 Discussion Foundational Neuroscience

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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 medicine90(1), 73–86.

RE: Week 2 Discussion

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).

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

RE: Week 2 Discussion

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

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 Psychopharmacology6(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

Name:  Discussion Rubric

  Excellent

90–100

Good

80–89

Fair

70–79

Poor

0–69

Main Posting:

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.

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%)

Meets requirements for full participation.

Posts main Discussion by due date.

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 and may have some depth.

0 (0%) – 6 (6%)

Response may not be on topic and 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 and may have some depth.

0 (0%) – 6 (6%)

Response may not be on topic and 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:  Discussion Rubric

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