- 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 agents are chemicals that stimulate a reaction by binding to a target site made explicitly for that chemical. If the site or chemical is incorrect, the two cannot bind and will not elicit another reaction. An antagonist is also a chemical that binds to a specific location, but instead of producing a reaction, it blocks an agonist chemical that would then elicit a reaction. Both antagonist and agonist can create an excitatory or inhibitory response depending on the desired effect. Partial agonists induce less than the full response when they occupy the receptor. An example of a partial agonist would be buprenorphine, which binds to the opioid receptor site but only elicits a partial effect (Whelan, P. J., et al.,2012). The benefits of buprenorphine partial effects, versus. Methadone that creates a full effect does not produce the same euphoria and respiratory effect as methadone. This partial effect can help with misuse, side effects, and the eventual withdrawal of the medication. An inverse agonist will cause the exact opposite reaction as the usual chemical messenger for that site (Camprodon, J. A., et al., 2016). Beta-blockers and antihistamines are examples of inverse agonists. Beta-blockers, like carvedilol, not only block an increase in heart rate and blood pressure, they can also lower heart rate and blood pressure (Khilnani, G., et al., 2011).
- Compare and contrast the actions of g couple proteins and ion gated channels.
Ion gated channels are the primary neurotransmitter site locations on the pre and post-synaptic sites that open ion channels to elicit the next neuron to receive a signal. A Gated ion channel creates a rapid membrane potential creating fast neuron activity (Camprodon, J. A., et al., 2016). G-protein-coupled receptors (GPCRs) are a slower secondary neurotransmitter site, triggers a multi-enzyme cascade. When they receive a specific neurotransmitter, the GPCRs, located on plasma membranes, release Alpha, Beta, or Gamma subunits into the cell membrane to be converted into new chemical reactions or signals that either create or inhibit a response (Camprodon, J. A., et al., 2016).
3. Explain how the role of epigenetics may contribute to pharmacologic action.
Epigenetic differences have been shown to change a pharmacological reaction that an individual may have versus someone with a different gene expression. DNA methylation is an excellent example of how these differences can occur. The methylation of DNA is responsible for multiple processes. Gene expression, imprinting, chromatin organization, and X-chromosome inactivation are examples (Rasool, M., et al., 2018). Methylation can affect how medications work on cells by decreasing or increasing their effectiveness and metabolizing too quickly or slowly. DNA tests are available for patients to determine their responses to drugs.
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 a psychiatric mental health nurse practitioner must be aware of the medication’s action.
A good example of why a mental health nurse practitioner needs to understand the Mechanism of Action (MOA) of medications is with multiple drugs that can create steven Johnson syndrome. Steven Johnson’s syndrome is a medical emergency that can be caused by too much serotonin. Two examples are Lamictal and selective serotonin reuptake inhibitors (SSRIs). SSRIs block the ion channels that generally pull back the extra serotonin between the pre and post synapse of two neurons. By blocking the reuptake ion channel on the pre-synaptic site, there is more serotonin available for the post-synaptic neuron to receive serotonin through their ion channels. Lamictal, another medication used for an anti-seizure and commonly bipolar disease, is also believed to increase serotonin. Specifically, Lamictal has an increased chance to cause SJS with patients who have recently started taking the medication (Frey et al., 2017). The risk for SJS can also be increased using another medicine that raises serotonin levels. Knowing the mechanism of action and the results of the MOA can help nurse practitioners and their patients stay safe.
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.
Frey, N., Jossi, J., Bodmer, M., Bircher, A., Jick, S., Meier, C., & Spoendlin, J. (2017). The Epidemiology of Stevens-Johnson Syndrome and Toxic Epidermal Necrolysis in the UK. Journal of Investigative Dermatology. Retrieved 9 September 2021, from https://www.sciencedirect.com/science/article/pii/S0022202X17301768.
Khilnani, G., & Khilnani, A. K. (2011). Inverse agonism and its therapeutic significance. Indian journal of pharmacology, 43(5), 492–501. https://doi.org/10.4103/0253-7613.84947.
Rasool, M., Malik, A., Naseer, M.I. et al. The role of epigenetics in personalized medicine: challenges and opportunities. BMC Med Genomics 8, S5 (2015). https://doi.org/10.1186/1755-8794-8-S1-S5
Whelan, P. J., & Remski, K. (2012). Buprenorphine vs methadone treatment: A review of evidence in both developed and developing worlds. Journal of neurosciences in rural practice, 3(1), 45–50. https://doi.org/10.4103/0976-3147.91934
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Excellent
Point range: 90–100 |
Good
Point range: 80–89 |
Fair
Point range: 70–79 |
Poor
Point range: 0–69 |
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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. |
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.
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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.
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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.
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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.
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Writing |
Written clearly and concisely.
Contains no grammatical or spelling errors.
Adheres to current APA manual writing rules and style.
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Written concisely.
May contain one to two grammatical or spelling errors.
Adheres to current APA manual writing rules and style.
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Written somewhat concisely.
May contain more than two spelling or grammatical errors.
Contains some APA formatting errors.
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Not written clearly or concisely.
Contains more than two spelling or grammatical errors.
Does not adhere to current APA manual writing rules and style.
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Timely and full participation |
Meets requirements for timely, full, and active participation.
Posts main Discussion by due date.
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Posts main Discussion by due date.
Meets requirements for full participation.
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Posts main Discussion by due date.
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Does not meet requirements for full participation.
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Post to colleague’s main post that is reflective and justified with credible sources. |
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.
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Response has some depth and may exhibit critical thinking or application to practice setting.
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Response is on topic, may have some depth.
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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.
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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.
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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.
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Responses posted in the Discussion lack effective communication.
Response to faculty questions are missing.
No credible sources are cited.
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First Response:
Timely and full participation |
Meets requirements for timely, full, and active participation.
Posts by due date.
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Meets requirements for full participation.
Posts by due date.
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Second Response:
Post to colleague’s main post that is reflective and justified with credible sources. |
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.
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Response has some depth and may exhibit critical thinking or application to practice setting.
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Response is on topic, may have some depth.
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Response may not be on topic, lacks depth.
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Second Response:
Writing |
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.
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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.
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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.
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Responses posted in the Discussion lack effective communication.
Response to faculty questions are missing.
No credible sources are cited.
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Second Response:
Timely and full participation |
Meets requirements for timely, full, and active participation.
Posts by due date.
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Meets requirements for full participation.
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Does not meet requirements for full participation.
Does not post by due date.
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