Feb 23, 2024 Discussion: Foundational Neuroscience.
Discussion: Foundational Neuroscience.
Discussion: Foundational Neuroscience.
The agonist-to-antagonist spectrum of action of psychopharmacologic agents
Agonists are chemical substances that, when attached or bound to their respective receptors, would lead to activation, manifesting as a biological response. More, when an agonist binds, there is an opening of the ion channels, and the maximum opening would make it possible for more binding. On the other hand, an antagonist would block the effects brought about by the agonist, but an inverse agonist would produce an opposite effect of what the agonist would cause (Cornelissen, 2019).
An antagonist found at the middle of the spectrum would often prevent the opening of the channels, making it infrequent. Therefore, the mechanism of action of the inverse agonist involves the inactivation of the receptors, and there are times when it completely closes it. There are times when the antagonist binds to the ion channels and then takes it back to the resting state. There is a need to strike a balance between signal transduction and ion flow to confer a good therapeutic effect of drugs.
The Ion Gated Channels vs. the G-Couple Proteins
The ion channels are made by the extracellular sites, which bind the neurotransmitters and the other ones that pass through membranes, forming an ion channel (Pereira, Borges-Pereira, & Garcia, 2021). Therefore, the ionotropic receptors act as single entities for the entry of molecules, and these are called ligand-gated ion channels.
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On the other hand, the G-proteins are also called metabotropic receptors and channels whose effects are received via the activation of intermediate molecules (Nájera et al., 2019). The metabotropic receptors are monomeric, having both the intracellular and the extracellular components, while the ion channels are considered multimeric. Once the metabotropic receptors are bound to the G-proteins, they would dissociate and interact with ion channels. Usually, the G-proteins function as transducers which then couple to neurotransmitters through binding postsynaptic ion channels.
How the role of epigenetics may contribute to pharmacologic action.
The epigenetics depict the changes which then influence phenotypes, although this would not cause changes in the genotype. Epigenetics thus looks at the reversible, heritable changes occurring in the process of gene expression, although not modifying the primary sequence of the genes within the DNA (Rastgoo, Abdi, Hou, & Chang, 2017). Epigenetic mechanisms have found wide use in mRNA, being exploited as diagnostic markers. In addition, epigenetic regulation is essential in maintaining the phenotypic activity of cells and the management of diseases such as cancer and neurodegenerative conditions.
How Information may impact medication Prescription
The PMHNP needs to ensure they are aware of the mechanism of action of drugs useful to the patients. Psychiatric medications would lead to changes in patient’s cognitive abilities, and therefore, there is a need for a lot of care when administering them. Diseases like Alzheimer’s disease are particularly of interest because they are very common today, especially among the elderly. There is ongoing research to determine the cure for neurodegenerative disorders by the use of epigenetics. Pharmacology would therefore be essential for nurses, and this would make them able to decide whether to treat the patient’s symptoms or address the overall presentation of the condition.
References
Cornelissen, J. (2019). Pharmacological assessment of adjuncts to enhance mu-opioid receptor
agonist antinociception in male rhesus monkeys: Does one+ one= three?.
Nájera, N., Martínez Vega, R. P., Martínez, A. P., Vilchis, P. O., & Ceballos, G. (2019).
G-proteins coupled receptors. Cardiovascular and Metabolic Science, 30(2), 50-59.
Pereira, P. H., Borges-Pereira, L., & Garcia, C. R. (2021). Evidences of G Coupled-Protein
Receptor (GPCR) Signaling in the human Malaria Parasite Plasmodium falciparum for Sensing its Microenvironment and the Role of Purinergic Signaling in Malaria Parasites. Current Topics in Medicinal Chemistry, 21(3), 171-180.
Rastgoo, N., Abdi, J., Hou, J., & Chang, H. (2017). Role of epigenetics-microRNA axis in drug
resistance of multiple myeloma. Journal of hematology & oncology, 10(1), 1-10.
Week 2: Neurotransmitters and Receptor Theory
Receptors and neurotransmitters are like a lock-and-key system. Just as it takes the right key to open a specific lock, it takes the right neurotransmitter to bind to a specific receptor. Not surprisingly, as it concerns psychopharmacology, the pharmacotherapeutics that are prescribed must trigger the release of certain neurotransmitters that bind to the correct receptors in order to elicit a favorable response for the patient. The mechanism of this binding and the response that follows reflects receptor theory and lies at the foundation of pharmacology.
This week, you will continue your examination of neuroanatomy and neuroscience as you engage with you colleagues in a Discussion. You will also explore the potential impacts of foundational neuroscience on the prescription of pharmacotherapeutics.
Learning Objectives
Students will:
Analyze the agonist-to-antagonist spectrum of action of psychopharmacologic agents
Compare the actions of g couple proteins to ion gated channels
Analyze the role of epigenetics in pharmacologic action
Analyze the impact of foundational neuroscience on the prescription of medications
Learning Resources
Required Readings (click to expand/reduce)
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.
Required Media (click to expand/reduce)
The University of British Columbia. (n. d.). Neuroanatomy videos. http://neuroanatomy.ca/videos.htmlNote: Please review all of the media under the neuroanatomy series.
Optional Resources (click to expand/reduce)
Pathopharmacology: Disorders of the Nervous System: Exploring the Human BrainDr. Norbert 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. (15m)
Introduction to Advanced Pharmacology
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. (6m)
Discussion: Foundational Neuroscience
As a psychiatric 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.
Photo Credit: Getty Images/Cultura RF
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.
By Day 3 of Week 2
Post a response to each of the following:
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.
Compare and contrast the actions of g couple proteins and ion gated channels.
Explain how the role of epigenetics may contribute to pharmacologic action.
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.
By Day 6 of Week 2
Respond to at least two of your colleagues on two different days in one of the following ways:
If your colleagues’ posts influenced your understanding of these concepts, be sure to share how and why. Include additional insights you gained.
If you think your colleagues might have misunderstood these concepts, offer your alternative perspective and be sure to provide an explanation for them. Include resources to support your perspective.
Note: For this Discussion, you are required to complete your initial post before you will be able to view and respond to your colleagues’ postings. Begin by clicking on the “Post to Discussion Question” link and then select “Create Thread” to complete your initial post. Remember, once you click on Submit, you cannot delete or edit your own posts, and you cannot post anonymously. Please check your post carefully before clicking on Submit!
Submission and Grading Information
Grading Criteria
To access your rubric:Week 2 Discussion Rubric
Post by Day 3 of Week 2 and Respond by Day 6 of Week 2
To Participate in this Discussion:Week 2 Discussion
What’s Coming Up in Week 3?
Photo Credit: [BrianAJackson]/[iStock / Getty Images Plus]/Getty Images
Next week, you will explore medication adherence and strategies to help overcome non-adherence to pharmacotherapeutics. You will also complete a Quiz that addresses the content covered throughout this module.
Next Week
To go to the next week:Week 3
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Discussion: Foundational Neuroscience
As a psychiatric mental health nurse practitioner, it is essential for you to have a strongbackground in foundational neuroscience. In order to diagnose and treat clients, you must notonly understand the pathophysiology of psychiatric disorders, but also how medications for thesedisorders impact the central nervous system. These concepts of foundational neuroscience can bechallenging to understand. Therefore, this Discussion is designed to encourage you to thinkthrough these concepts, develop a rationale for your thinking, and deepen your understanding byinteracting with your colleagues.
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NURS 6630 – Psychopharmacologic Approaches to Treatment of Psychopathology EssayAssignmentRequired ReadingsNote: All Stahl resources can be accessed through the Walden Library using this link. This linkwill take you to a log-in page for the Walden Library. Once you log into the library, the Stahlwebsite will appear.Stahl, S. M. (2013). Stahl’s essential psychopharmacology: Neuroscientific basis and practicalapplications (4th ed.). New York, NY: Cambridge University Press *Preface, pp. ix–xNote: To access the following chapters, click on the Essential Psychopharmacology, 4th ed tabon the Stahl Online website and select the appropriate chapter. Be sure to read all sections on theleft navigation bar for each chapter.
Chapter 1, “Chemical Neurotransmission”
Chapter 2, “Transporters, Receptors, and Enzymes as Targets of Psychopharmacologic DrugAction”Chapter 3, “Ion Channels as Targets of Psychopharmacologic Drug Action”Document: Midterm Exam Study Guide (PDF)Document: Final Exam Study Guide (PDF)Required MediaLaureate Education (Producer). (2016i). Introduction to psychopharmacology [Video file].Baltimore, MD: Author.NURS 6630 – Psychopharmacologic Approaches to Treatment of Psychopathology EssayAssignmentNote: The approximate length of this media piece is 3 minutes.
Accessible player
Optional ResourcesLaureate Education (Producer). (2009). Pathopharmacology: Disorders of the nervous system:Exploring the human brain [Video file]. Baltimore, MD: Author.NURS 6630 –Psychopharmacologic Approaches to Treatment of Psychopathology Essay AssignmentNote: The approximate length of this media piece is 15 minutes.Dr. Myslinski reviews the structure and function of the human brain. Using human brains, heexamines and illustrates the development of the brain and areas impacted by disorders associatedwith the brain.
Accessible player
Laureate Education (Producer). (2012). Introduction to advanced pharmacology [Video file].Baltimore, MD: Author.NURS 6630 – Psychopharmacologic Approaches to Treatment ofPsychopathology Essay AssignmentNote: The approximate length of this media piece is 8 minutes.In this media presentation, Dr. Terry Buttaro, associate professor of practice at Simmons Schoolof Nursing and Health Sciences, discusses the importance of pharmacology for the advancedpractice nurse.Accessible playerTo prepare for this Discussion:Review this week’s Learning Resources.Reflect on concepts of foundational neuroscience.
An agonist-to-antagonist spectrum of action of psycho pharmacologic agents, -is explained as when a chemical binds or connect to a receptor, the receptor activates, and a biological response is produced. When agonists activate receptors, like hormones, neurotransmitters, and other endogenous regulators that activate the receptors to which they bind (Golier, J. A., & Yehuda, R. (2018). Antagonists have no effects on the receptor function, but it can block effectiveness and prevent receptor activation by endogenous molecules and drugs(Golier, J. A., & Yehuda, R. (2018).The antagonist can be a drug with an affinity to bind to a receptor but does not have any intrinsic activity.
The process is considered an example of a full agonist (Golier, J. A., & Yehuda, R. (2018). A partial agonist means that the molecules do not elicit a full response therefore does not obtain the maximum response from system even when they bind to the same number of receptors as an agonist (Golier, J. A., & Yehuda, R. (2018). When there is an agonist and a partial agonist working at the same time the partial agonist becomes an antagonist because they are both fighting for space on the same receptors (Frånberg, O et al).. An antagonist refers to molecules that block agonist mediated responses. Inverse agonists are molecules that want to attach to the same receptors as agonists, but they produce an opposite response than the agonist on the target cell (Golier, J. A., & Yehuda, R. (2018).
Compare and contrast the actions of g couple proteins and ion gated channels.
G protein-coupled receptors (GPCRs) are a large family of cell surface receptors on the plasma membrane that transmit signals inside the cell through a type of protein called a G protein (Sunamita de Carvalho et al 2018). G protein-coupled receptors serve many purposes in the body, and the disorder of GPCR signaling can cause disease. G proteins bind with nucleotide guanosinetriphosphate (GTP) (Sunamita de Carvalho et al 2018). G protein divides into two portions (one called the α subunit, the other consisting of the β and γ subunits), which are released from the GPCR (Sunamita de Carvalho et al 2018). The subunits can interact with other proteins, triggering other signaling pathways that lead to different responses.
When communication is allow to occur from one cell to the next cell through a lipid membrane, charged molecules need assistance in the form of ion channels (Sunamita de Carvalho et al 2018). Ion channels control cellular excitability by using membrane-bound glycol proteins that contain pores filled with water (ion channels) which allows for the charged molecules to move from an extracellular to intracellular (Sunamita de Carvalho et al 2018). Charged molecules can go into the cell while allowing for uncharged molecules to move out of the cell in an organized, efficient manner.
This movement of ions is important in the role of cell excitation, muscle contraction and intracellular signaling (Weir, 2020). G-protein-coupled receptors (GPCRs) are the largest category of receptors allowing for the bodies physiological function (Sunamita de Carvalho et al 2018). Most medications are made to target GPCRs due to their large distribution throughout the body. They are necessary membrane proteins used by cells to convert extracellular signals into intracellular responses by using hormones (Sunamita de Carvalho et al 2018).
Explain how the role of epigenetics may contribute to pharmacologic action.
Epigenetics is when the expression of a gene can be controlled, promoting or repressing the expression of the gene without changing the code or genome’s sequence (Kumsta, R. 2019).Epigenetics is gene function is changed by an adaptation in the code. The role of epigenetics may contribute to pharmacologic action by changing a DNA molecule, resulting in amended gene expression. When a DNA molecule is amended, then pharmacologic action is then modified. Gene articulation can be modified because of the variation of the DNA molecule chromatin. Long-term effects of cognition and behavior can be a result of the alteration of development brought on by abuse or mistreatment in childhood (Kumsta, R. 2019). Heritability is an effect of gene expression changes in the long-term
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.
As a provider, when prescribing medication, it is necessary to treat each patient as individual patient with his or her own familiar history. The assessment should include genetic questing that will be use for the implementation of diagnosing implementation for treatment. Will also access for allergy since most antipsychotics’ medication are commonly cause allergy reaction. Closely monitor medications prescribed for the treatment of psychosis and behavioral and psychological symptoms of dementia in elderly patients for any adverse reaction (Kumsta, R. 2019) Monitoring should always continue; it should not only be at the beginning of the therapy because patient can develop tolerance to medication and eventually medication or doses that use to work might not work. Doses should be monitor and adjusted appropriately. Also, since aging can affect drug metabolism and clearance, additional pharmacokinetic and pharmacodynamic changes require additional attention (Kumsta, R. 2019).
References:
Sunamita de Carvalho Lima, Lucas de Carvalho Porta, Álvaro da Costa Lima, Joana D’Arc Campeiro, Ywlliane Meurer, Nathália Bernardes Teixeira, Thiago Duarte, Eduardo Brandt Oliveira, Gisele Picolo, Rosely Oliveira Godinho, Regina Helena Silva, & Mirian Akemi Furuie Hayashi. (2018). Pharmacological characterization of crotamine effects on mice hind limb paralysis employing both ex vivo and in vivo assays: Insights into the involvement of voltage-gated ion channels in the crotamine action on skeletal muscles. PLoS Neglected Tropical Diseases, 12(8), e0006700. https://doi.org/10.1371/journal.pntd.0006700
Frånberg, O., Wiker, C., Marcus, M., Konradsson, Å., Jardemark, K., Schilström, B., Shahid, M., Wong, E., & Svensson, T. (2008). Asenapine, a novel psychopharmacologic agent: preclinical evidence for clinical effects in schizophrenia. Psychopharmacology, 196(3), 417–429. https://doi.org/10.1007/s00213-007-0973-y
Kumsta, R. (2019). The role of epigenetics for understanding mental health difficulties and its implications for psychotherapy research. Psychology and Psychotherapy: Theory, Research and Practice, 92(2), 190–207. https://doi.org/10.1111/papt.12227
Golier, J. A., & Yehuda, R. (2018). Mifepristone as a Psychopharmacologic Agent: Consideration of Efficacy, Plasma Levels, and Mechanism of Action. Biological Psychiatry, 84(1), 5–
Hello Anitha, I enjoyed reading your post, and I agree with you with the fact that epigenetics affects the pharmacokinetics and pharmacodynamics of a drug, and the variability is often linked to alterations or mutations in the drug metabolizing enzymes and drug transporters encoded by several hundred genes. The term epigenetics describes genetic information that is ‘beyond’ or ‘above’ that information coded solely by our genetic code. Disease can be generated by a single base mutation [for example the deletion in cystic fibrosis patients of the phenylalanine (F) at position 508 of the cystic fibrosis transmembrane conductance regulator (CFTR)]. However, epigenetics may create disease in humans that have pristine un-mutated DNA (Stefanska & MacEwan, 2015).
In addition, with recent improvements in understanding of the actual function of the entire genome, pharmacology has to modify itself further to think of tackling diseases not in the conventional ‘drug-receptor’ sense, but in a more ‘global-response’ sense. Drugs may not be designed to be as exact to a particular ligand or specific to a particular gene or protein subtype, they may indeed have to be able to be more broad-acting over a range of epigenetic large-scale events. (Stefanska & MacEwan, 2015).
References
Stefanska, B., & MacEwan, D. J. (2015). Epigenetics and pharmacology. British Journal of Pharmacology, 172(11), 2701–2704. https://doi.org/10.1111/bph.13136
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