NURS 6630 Explain The Agonist-to-Antagonist Spectrum of Action of Psychopharmacologic Agents

NURS 6630 Discussion: Concepts of Foundational Neuroscience

NURS 6630 Explain The Agonist-to-Antagonist Spectrum of Action of Psychopharmacologic Agents

Explain the agonist-to-antagonist spectrum of action of psychopharmacologic agents

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.

The agonist and antagonist are understood to be the main players in the human body and pharmacology and are considered as two basic drug groups, working in opposite directions where the agonist generates an action, while the antagonist opposes the action. In this case, the agonist may occur naturally or as a drug, that binds to the activated receptor, while the antagonist binds to receptors, leading to no activation, inhibiting the agonist from binding (Clark, 2018). Consequently, the agonist produces changes in the G-protein sites, activating and signaling another messenger to the highest possible extent in a cascade effect, which also works with the ligand-gated ion channels (Berg & Clarke, 2018). The antagonist in return inhibits the agonist action and stabilizes the site of the receptor in a rest state. The agonist spectrum is categorized into four types including agonist, partial agonist, antagonist, and inverse agonist. Thus, the agonist opens the channel to a full amount and regularity permitted by the site of binding, while the antagonist lying in the center of the spectrum retains the state of rest with the sporadic opening of the channel. The inverse agonist puts the ion channel in a closed and inactive state, where the antagonist holds the capability of blocking everything in the agonist spectrum, returning the ions to their state of resting in every instance. In psychopharmacologic treatments, the antagonist plays a significant role in controlling the transmission of neurons because it is the full activation of the signal transduction cascade, which may lead to undesirable impacts. Conferring to Ma, Raivio, Sabria, and Ortiz (2015), an atypical antipsychotic drug aripiprazole binds with a great affinity to the G-protein coupled receptors, which includes the Dopamine D2 receptors, though its effectiveness as a partial agonist is still contentious.

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In the second part of NURS 6630 Explain The Agonist-to-Antagonist Spectrum of Action of Psychopharmacologic Agents, Compare and contrast the actions of g couple proteins and ion gated channels.

Both the G coupling proteins and the ion gated channels’ structural patterns and the linked pathways follow the same patterns between the receptors (Clark, 2018). However, the ion gated channels bind a ligand and open a channel via the membrane, permitting special ions to go through while the G couple

NURS 6630 Explain The Agonist-to-Antagonist Spectrum of Action of Psychopharmacologic Agents

protein binds the ligand, activating the protein-membrane known as G-protein, which then interacts with either the ion channel or an enzyme inside the membrane (Zhao et al., 2016). In addition, the ion gated channels response occurs within milliseconds while the response of the G couple protein occurs within seconds because of the mechanism of coupling, which adds additional complexity to stimulate a response (Stahl, 2013). This means that the G couple proteins have a slower response to signals compared to the ion gated channels.

In the third part of NURS 6630 Explain The Agonist-to-Antagonist Spectrum of Action of Psychopharmacologic Agents, Explain how the role of epigenetics may contribute to pharmacologic action.

Epigenetics is defined as the study of how our behaviors and surroundings lead to modifications affecting how our genes work (CDC, 2020). In this case, the genes are transcribed from the DNA to the RNA proteins, where the epigenetic mechanisms activate and deactivate the genes by changing the structure of the chromatin in the nucleus cells (Mason, 2018). Thus, through epigenetics, the control of the activities of the genes is significant in maintaining the cell’s normal phenotypic activities. This has been proven by extensive researches, especially in the development of ailments like cancer and neurodegenerative illnesses like Alzheimer’s (Stefanska & McEwan, 2015). However, new drug classes have been and are still developed to control the mechanism of epigenetics to respond to illnesses. For instance, Dogan et al., (2018), carried out research on integrated genetic and epigenetic prediction of coronary artery disease in a Framington heart study. The aim was to incorporate genetic and epigenetic facts to establish a classifier that will predict symptomatic CAD as a step towards showing the capability of using an incorporated method for risk models in the future as a substitute to current algorithms.

In the fourth part of NURS 6630 Explain The Agonist-to-Antagonist Spectrum of Action of Psychopharmacologic Agents, 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.

When the Psychiatric mental health nurse practitioner is prescribing medication he/she needs to understand the mechanism of action to ensure the patient is prevented or minimized from severe side effects or fatal events (Stahl, 2013). This is because the neural transmitters interact at all its subtypes of the receptor, whereas a lot of drugs tend to be more selective compared to the neurotransmitter itself for specific subtypes of the receptors (Clarks, 2018). This defines and explains the pharmacological receptor subtype, where they interact specifically. For example, when prescribing psychotropic medications the nurse needs to be more careful since a lot of drugs have been linked to prolongation of the QT interval. For instance, the use of amitriptyline is to treat depression and pain in the nerves, where the TCA prevents the channels of potassium (Stahl, 2013). As a result, this leads to hyperkalemia, which is normally linked to torsades de pointes a ventricular tachycardia, which may cause sudden cardiac death.

References

Berg, K., A., Clarke, W., P. (2018). Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity, International Journal of Neuropsychopharmacology, Vol. 21, (10): 962–977. https://doi.org/10.1093/ijnp/pyy071

Clarks, C. (2018). Basic principles of pharmacology. Tulane University School of Medicine. Retrieved 2021 March, 03 from http://tmedweb.tulane.edu/pharmwiki/doku.php/basic_principles_of_pharm?do=

CDC. (2020 August, 03). What is Epigenetics? Retrieved from: https://www.cdc.gov/genomics/disease/epigenetics.htm

Dogan, M. V., Grumbach, I. M., Michaelson, J. J., & Philibert, R. A. (2018). Integrated genetic and epigenetic prediction of coronary heart disease in the Framingham Heart Study. Plos ONE, 13 (1), 1-18. doi:10.1371/journal.pone.0190549

Ma, G. F., Raivio, N., Sabria, J., & Ortiz, J. (February 19, 2015). Agonist and Antagonist Effects of Aripiprazole on D2-Like Receptors Controlling Rat Brain Dopamine Synthesis Depend on the Dopaminergic Tone. International Journal of Neuropsychopharmacology, Vol.18: 4.

Mason, L. E. (2018). Epigenetics and Drug Discovery. Retrieved 2021 February, 03 from: Technology Networks: https://www.technologynetworks.com/drug-discovery/articles/epigenetics-and-drug-discovery-306821

Stefanska, B., & McEwan, D. J. (2015). Epigenetics and pharmacology. British journal of pharmacology, Vol. 172 (11): 2701-4. doi: 10.1111/bph.13136

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

Zhao, J., Deng, Y., Jiang, Z., Oing, H. (2016). G Protein-Coupled Receptors (GPCRs) in Alzheimer’s Disease; A Focus om BACE1 Related GPCRs. Frontier in Aging Neuroscience. https://doi.org/10.3389/fnagi.2016.00058

Foundational Neuroscience

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.

An inverse agonist binds to the receptor and prevents the occurrence of the normal activity and exerts the occurrence of an opposite pharmacological action. An agonist binds to a receptor resulting in the activation of the receptor and signal transduction leading to a biological response. On the other hand, an antagonist binds to a receptor and blocks it from binding in any agonist, resulting in no biological response. A partial agonist binds and results in the activation of a receptor but only with partial efficacy that is relative to the endogenous and full agonist (Berg & Clarke, 2018).

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

Both the g-protein and ion gated channels are triggered by the neurotransmitters. They are, however, distinct in the sense the g-couple proteins are involved in the transmission of signals to different transductions within a cell, whereas the ion gated channels trigger the movement of certain types of ions through receptors by selectively opening and closing. They are similar in some way- both allow both the transmission of signals and ions internally. The G-couple originates from the plasma (Stahl, 2018).

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

Epigenetics comprise heritable genetic modifications that alter gene function and expression without changes in DNA sequence. Epigenetics explains the capability of gene expression regulation without modifying the genetic sequence. Epigenetic mechanisms occur due to alterations in either the molecules or characteristics that, in turn, affect the gene expression without changing sequences of DNA, DNA methylation, histone modification, and non-coding RNAs(Waghmare et al., 2020).

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.

It is clear that a lot remains to be discovered in terms of the effect of epigenetics in neuroscience. New evidence implicates the dysregulation of epigenetic mechanisms in neurodegenerative disorders and diseases. This necessitates openness in terms of thinking about the effects of epigenetics when administering medications (Waghmare et al., 2020).

References

Berg, K. A., & Clarke, W. P. (2018). Making Sense of Pharmacology: Inverse Agonism and Functional Selectivity. International Journal of Neuropsychopharmacology, 21(10), 962. https://doi.org/10.1093/IJNP/PYY071

Stahl, S. M. (2018). Stahl’s Essential Psychopharmacology: Neuroscientific basis and practical applications (4th ed.). New York, NY: Cambridge University Press

Waghmare, S. S., Bhusnure, O. G., Mali, M. R., & Mule, S. T. (2020). Epigenetics: Pharmacology and Modification Mechanisms Involved in Cardiac, Hepatic and Renal Disease. Journal of Drug Delivery and Therapeutics, 10(4), 260–266. https://doi.org/10.22270/JDDT.V10I4.4148

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.Medications work by various mechanisms, which are still being studied and understood today. There is thought to be a spectrum of action related to how psychopharmacologic agents produce the effects we see in patients when medications are used to treat various symptoms. The spectrum ranges from agonist, inverse agonist, and antagonist, describing the function by which medications influence receptor activity (Berg & Clarke, 2018). The term agonist represents medications that bind to a receptor and can modify receptor action, ranging to partial or full efficacies (Berg & Clarke, 2018). Inverse agonists, on the contrary, reduce the activity of a receptor, while antagonists bind to receptors to inhibit the receptor from producing a response (Berg & Clarke, 2018). Research is still advancing to understand these functions drugs cause on receptors. It helps us better understand how medication produces effects and aid in the understanding needed to make new medications with specific desired results.

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

Both G-protein–coupled receptors (GPCRs) and ion gated channels are cell membrane receptors that regulate the function of cells in our body to produce specific effects valuable in targeting pharmacology at a cellular level (Dolphin et al., 2020). GPCRs are activated by molecules that bind to the cell, causing activation of signals transduction pathways to cause a cascade of cellular activity, causing the seen effects (Wang et al., 2020). Ion-gated channels, in contrast, open and allow the passage of specific ions into the cell via the channel pathway when specific binding sites are activated (Dolphin et al., 2020).

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

Epigenetics is the study of how an individual’s behaviors can influence a person’s genes and environmental stimuli, altering the way the gene expression occurs or when genes are active or inactive due to gene expression changes (CDC, 2020). Since these alterations can be affected by environment and behaviors, epigenetic changes can be reversed when changes to lifestyle such as diet modification, monitoring the substances ingested, and exercise occurs. In contrast, some are affected by permanent changes like age or disease and may not be reversible (CDC, 2020). Pharmacologic action can better be understood by appreciating how a gene’s current function would be altered by medication or medications to treat various conditions that may be more or less effective with some gene expression (Lockwood & Youssef, 2017).

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.

While the specific details of the complex interworking of cells may be intimidating and challenging to comprehend, the nurse practitioner must have a basic understanding of these processes to prescribe medications appropriately. It is crucial to have the knowledge to assess the patients for desired outcomes from medication administration. Likewise, making prescribing choices with knowledge of the way the medicines will cause binding actions in the cells, how the agonist-to-antagonist spectrum will affect the efficacy of the medications, and how the role of epigenetics will affect the pharmacologic activity of prescribed medications. For example, if a psychiatric nurse practitioner thought it would be beneficial to prescribe the antidepressant bupropion, it would be essential to understand a few things. Bupropion acts by inhibiting the neurotransmitters dopamine and norepinephrine reuptake transporters and acts as an antagonist on ion channel receptors (Pandhare et al., 2017). Understanding the drug action helps the practitioner make informed prescribing choices and helps better understand effects in the body that may occur because of the administration. Also, contradictions with prescribing the medication may exist when given with certain conditions or coupled with other medicines. When inadequate treatment results occur, we have some possible explanations to explain the outcome. For instance, a study related to epigenetics reported that low DNA methylation, a gene expression change, present in some study participants was related to decreased response to bupropion treatment (Webb et al., 2020). Understanding these gene expression changes affect treatment outcomes helps explain why one patient may respond well and others not to certain medication regimes.

Berg, K. A., & Clarke, W. P. (2018). Making sense of pharmacology: Inverse agonism and functional selectivity. International Journal of Neuropsychopharmacology, 21(10), 962–977. https://doi.org/10.1093/ijnp/pyy071

Centers for Disease Control and Prevention. (2020). What is epigenetics? Centers for Disease Control and Prevention. https://www.cdc.gov/genomics/disease/epigenetics.htm.

Dolphin, A. C., Insel, P. A., Blaschke, T. F., & Meyer, U. A. (2020). Introduction to the theme “ion channels and neuropharmacology: From the past to the future.” Annual Review of Pharmacology and Toxicology, 60(1), 1–6. https://doi.org/10.1146/annurev-pharmtox-082719-110050

Lockwood, L., & Youssef, N. (2017). Systematic review of epigenetic effects of pharmacological agents for bipolar disorders. Brain Sciences, 7(12), 154. https://doi.org/10.3390/brainsci7110154

Pandhare, A., Pappu, A. S., Wilms, H., Blanton, M. P., & Jansen, M. (2017). The antidepressant bupropion is a negative allosteric modulator of serotonin type 3A receptors. Neuropharmacology, 113, 89–99. https://doi.org/10.1016/j.neuropharm.2016.09.021

Wang, Y., Yutuc, E., & Griffiths, W. J. (2020). Neuro‐oxysterols and neuro‐sterols as ligands to nuclear receptors, gpcrs, ligand‐gated ion channels and other protein receptors. British Journal of Pharmacology, 178(16), 3176–3193. https://doi.org/10.1111/bph.15191

Webb, L. M., Phillips, K. E., Ho, M. C., Veldic, M., & Blacker, C. J. (2020). The relationship between DNA methylation and antidepressant medications: A systematic review. International Journal of Molecular Sciences, 21(3). https://doi.org/10.3390/ijms21030826

NURS_6630_Week2_Discussion_Rubric

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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. 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.
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