Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents

Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents

PPharm- Wk 1 DBQ Discussion: Foundational Neuroscience

Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents

Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents from PPharm- Wk 1 DBQ Discussion: Foundational Neuroscience and get fast and reliable answer from our erudite professionals at 10% discount. Our masters prepared nursing assignment writers will also answer Compare and contrast the actions of g couple proteins and ion gated channels.Explain the role of epigenetics in pharmacologic action as well as Week 2 : Assessing and Treating Pediatric Clients With Mood Disorders: NUR 6630 Week 2: Therapy for Pediatric Clients With Mood Disorders for you!!!

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NURS 6630 Week 1: Introduction to Neuroscience

This week, as you begin to study psychopharmacology, you explore foundational neuroscience. You examine the agonist-to-antagonist spectrum of action of psychopharmacologic agents, compare the actions of g couple proteins to ion gated channels, and consider the role of epigenetics in pharmacologic action.

Note: In previous courses, the term “patient” was used to describe the person receiving medical care. In traditional medicine and nursing, this term is used to describe the person you do something to, and it often refers to a passive recipient of care and services. As you move into the realm of psychiatric mental health, a transition will occur. You will work with individuals who are active participants in their care, and these individuals are generally referred to as “clients” as opposed to “patients.” It is important to note that the term “client” is also favored in other mental health disciplines, such as psychiatry, psychology, and social work.

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The assignment should be answered in APA format using at least 3 credible sources including the course materials. The references should be no more than 5 years old and evidence-based ones are even better. Ensure that all the questions are answered in order to get full marks from the lecturer.

explain the agonist-to-antagonist spectrum of action of psychopharmacologic agents
Explain the agonist-to-antagonist spectrum of action of psychopharmacologic agents: NURS 6630 Week 1

Post a response to each of the following:

  1. Explain the agonist-to-antagonist spectrum of action of psychopharmacologic agents.
  2. Compare and contrast the actions of g couple proteins and ion gated channels.
  3. Explain the role of epigenetics in pharmacologic action.
  4. Explain how this information may impact the way you prescribe medications to clients. Include a specific example of a situation or case with a client in which the psychiatric mental health nurse practitioner must be aware of the medication’s action.

Discussion: Foundational Neuroscience

Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents: As a psychiatric mental health nurse practitioner, it is essential for you to have a strong background in foundational neuroscience. In order to diagnose and treat clients, 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.

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

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Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents Learning Resources

Note: To access this week’s required library resources, please click on the link to the Course Readings List, found in the Course Materials section of your Syllabus.

Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents Required Readings

Note: All Stahl resources can be accessed through the Walden Library using this link. This link will take you to a log-in page for the Walden Library. Once you log into the library, the Stahl website will appear.

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

Note: To access the following chapters, click on the Essential Psychopharmacology, 4th ed tab on the Stahl Online website and select the appropriate chapter. Be sure to read all sections on the left navigation bar for each chapter. Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents

  • Chapter 1, “Chemical Neurotransmission”
  • Chapter 2, “Transporters, Receptors, and Enzymes as Targets of Psychopharmacologic Drug Action”
  • Chapter 3, “Ion Channels as Targets of Psychopharmacologic Drug Action”

NURS 6630 Week 1: Introduction to Neuroscience

Modern psychopharmacology is largely the story of chemical neurotransmission. To understand the actions of drugs on the brain, to grasp the impact of diseases on the central nervous system, and to interpret the behavioral consequences of psychiatric medicines, one must be fluent in the language and principles of neurotransmission.

—Dr. Stephen M. Stahl in Stahl’s Essential Psychopharmacology

By using a combination of psychotherapy and medication therapy, psychiatric mental health nurse practitioners are positioned to provide a very unique type of care to clients with psychiatric disorders. To be successful in this role, you must have a strong theoretical foundation in pathophysiology, psychopharmacology, and neuroscience. This foundation will help you assess, diagnose, and treat clients as you relate presenting symptoms to theoretical neuronal functioning.

Required Media for Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents

Laureate Education (Producer). (2016i). Introduction to psychopharmacology [Video file]. Baltimore, MD: Author.

Note: The approximate length of this media piece is 3 minutes.

Optional Resources

Laureate Education (Producer). (2009). Pathopharmacology: Disorders of the nervous system: Exploring the human brain [Video file]. Baltimore, MD: Author.

Note: The approximate length of this media piece is 15 minutes.

Dr. 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. Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents

Laureate Education (Producer). (2012). Introduction to advanced pharmacology [Video file]. Baltimore, MD: Author.

Note: The approximate length of this media piece is 8 minutes.

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.

NB: The below work is not in academic language, so you cannot use it. Kindly ORDER NOW to get an academic-oriented paper from us.

Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents

Agonist vs Antagonist

Agonists and antagonists are known to be key players in human body and in pharmacology. Agonist and antagonist act in opposite directions. When agonist produces an action, antagonist opposes the action.

First of all when talking of muscles, agonist is that works with muscles and antagonist is that works against the muscles. Agonist works when the muscles relax and antagonist works when muscles contract. Agonists can be called as ‘prime movers’ as these very much responsible for producing specific movements.

Agonist is a substance, which combines with the cell receptor to produce some reaction that is typical for that substance. On the other hand, antagonist is a chemical, which opposes or reduces the action.

In medicines, an agonist ties to a receptor site and causes a response whereas an antagonist works against the drug and blocks the response. While agonists stimulate an action, antagonists sit idle, doing nothing.

Agonists are also chemicals or reactions, which help in binding and also altering the function of the activity of receptors. On the other hand, antagonists though help in binding receptors, they do not alter its activity.

When agonist is a compound that impersonate the action of neurotransmitter, antagonist blocks the action of neurotransmitter. Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents

Agonists combine with other chemical substances and promote some action. On the contrary, antagonists after combining with certain chemical substances only interfere with its action.

Agonist has been derived from late Latin word agnista, which means contender. Antagonist has been derived from Latin antagonista and from Greek antagonistes, which means “competitor, rival or opponent.”

Summary

  • 1. Agonist and antagonist act in opposite directions. When agonist produces an action, antagonist opposes the action.
  • 2. Agonist works when the muscles relax and antagonist works when muscles contract.
  • 3. While agonists stimulate an action, antagonists sit idle, doing nothing.
  • 4. An agonist ties to a receptor site and causes a response whereas an antagonist works against the drug and blocks the response.
  • 5. Agonists are also chemicals or reactions, which help in binding and also altering the function of the activity of receptors. On the other hand, antagonists though help in binding receptors, they do not alter its activity.
  • 6. When agonist is a compound that impersonate the action of neurotransmitter, antagonist blocks the action of neurotransmitter.
  • 7. Agonist has been derived from late Latin word agnista, which means contender. Antagonist has been derived from Latin antagonista and from Greek antagonistes, which means “competitor, rival or opponent.” Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents
Read more: Difference Between Agonist and Antagonist | Difference Between | Agonist vs Antagonist http://www.differencebetween.net/science/difference-between-agonist-and-antagonist/#ixzz5Y9bFHCE5
Discussion Week 2

On the cellar level the ligand gated ion channel an agonist can bind to a receptor and cause the same phycological response as a natural ligand.  An antagonist binds to the receptor and do not cause a phycological response but block that receptor preventing the natural ligand from going into that receptor. For example, most antipsychotic drugs act as dopamine receptor antagonist.  Blocking reuptake of dopamine (Howland, 2016).  Some antipsychotic drugs also act as inverse agonist at the serotonin receptor causing an opposite effect. An inverse agonist produces a opposite effect of the agonist.

In regard to the efficacy of a drug treatments, the NP has to provide a very good patient assessment to provide the patient with an accurate diagnosis.  The NP having knowledge, can correctly prescribe the drug (agonist, antagonist or reverse agonist) that will act on the on the targeted neurotransmitter to produce the desired effect in the patient.

Ion gated channels pull and bond to the agonist changing the protein.  G coupled proteins are proteins used by the cell to convert intracellular signals into responses (Zhao, Deng, Jiang, Oing, 2016).

Epigenetics is modifications in gene expression that is controlled by various fundamental epigenetic mechanisms leading to various physical and psychiatric diseases.  As a result, traditional treatment may often prove ineffective with these patients because these mechanisms regulate cellular and gene expression, just to name a few (Rasool, et al., 2015).

As practitioner, my patient assessment may also include an education and discussion concerning pharmacogenomics.  Particularly, if the patient comes to me after having been on various medication treatments that were unsuccessfully.   Knowledge of a medications action is important for example; treating a patient with Bipolar I that is exhibiting depression symptoms but also reported that he maxed out his credit card last week on video games. With the knowledge that an antidepressant should not be given because the action of the antidepressant would cause the patient to go into mania.

 

References

 

Berg, K., A., Clarke, W., P. (2018).  Making Sense of Pharmacology: Inverse Agonism and

Functional Selectivity, International Journal of Neuropsychopharmacology, Volume 21, Issue 10, October 2018, Pages 962–977, https://doi.org/10.1093/ijnp/pyy071

 

Howland, R. H. (2016). Pimavanserin: An inverse agonist antipsychotic drug. Journal of

Psychosocial Nursing & Mental Health Services, 54(6), 21-24. doi:http://dx.doi.org.ezp.waldenulibrary.org/10.3928/02793695-20160523-01

Rasool, M., Malik, A., Naseer, M. I., Manan, A., Ansari, S., Begum, I., Qazi, M. H., Pushparaj,

P., Abuzenadah, A. M., Al-Qahtani, M. H., Kamal, M. A., & Gan, S. (2015). The role of epigenetics in personalized medicine: challenges and opportunities. BMC medical genomics8 Suppl 1(Suppl 1), S5. https://doi.org/10.1186/1755-8794-8-S1-S5

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

STAHL’S BOOK

Ion channels as targets of psychopharmacological drug action

Many important psychopharmacological drugs target ion channels. The roles of ion channels as important regulators of synaptic neurotransmission were covered in Chapter 1. Here we discuss how targeting these molecular sites causes alterations in synaptic neurotransmission that are linked in turn to the therapeutic actions of various psychotropic drugs. Specifically, we cover ligand-gated ion channels and voltage-sensitive ion channels as targets of psychopharmacological drug action.

Ligand-gated ion channels as targets of psychopharmacological drug action

Ligand-gated ion channels, ionotropic receptors, and ion-channel-linked receptors: different terms for the same receptor/ion-channel complex

Ions normally cannot penetrate membranes because of their charge. In order to selectively control access of ions into and out of neurons, their membranes are decorated with all sorts of ion channels. The most important ion channels in psychopharmacology regulate calcium, sodium, chloride, and potassium. Many can be modified by various drugs, and this will be discussed throughout this chapter.

There are two major classes of ion channels, and each class has several names. One class of ion channels is opened by neurotransmitters and goes by the names ligand-gated ion channels, ionotropic receptors, and ion-channel-linked receptors. These channels and their associated receptors will be discussed next. The other major class of ion channel is opened by the charge or voltage across the membrane and is called either a voltage-sensitive or a voltage-gated ion channel; these will be discussed later in this chapter.

Ion channels that are opened and closed by actions of neurotransmitter ligands at receptors acting as gatekeepers are shown conceptually in Figure 3-1. When a neurotransmitter binds to a gatekeeper receptor on an ion channel, that neurotransmitter causes a conformational change in the receptor that opens the ion channel (Figure 3-1A). A neurotransmitter, drug, or hormone that binds to a receptor is sometimes called a ligand (literally, “tying”). Thus, ion channels linked to receptors that regulate their opening and closing are often called ligand-gated ion channels. Since these ion channels are also receptors, they are sometimes also called ionotropic receptors or ion-channel-linked receptors.

agonist-to-antagonist spectrum of action of psychopharmacologic agents

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Figure 3-1. Ligand-gated ion channel gatekeeper. This schematic shows a ligand-gated ion channel. In panel A, a receptor is serving as a molecular gatekeeper that acts on instruction from neurotransmission to open the channel and allow ions to travel into the cell. In panel B, the gatekeeper is keeping the channel closed so that ions cannot get into the cell. Ligand-gated ion channels are a type of receptor that forms an ion channel and are thus also called ion-channel-linked receptors or ionotropic receptors.

These terms will be used interchangeably with ligand-gated ion channels here.Numerous drugs act at many sites around such receptor/ion-channel complexes, leading to a wide variety of modifications of receptor/ion-channel actions. These modifications not only immediately alter the flow of ions through the channels, but with a delay can also change the downstream events that result from transduction of the signal that begins at these receptors. The downstream actions have been extensively discussed in Chapter 1 and include both activation and inactivation of phosphoproteins, shifting the activity of enzymes, the sensitivity of receptors, and the conductivity of ion channels. Other downstream actions include changes in gene expression and thus changes in which proteins are synthesized and which functions are amplified. Such functions can range from synaptogenesis, to receptor and enzyme synthesis, to communication with downstream neurons innervated by the neuron with the ionotropic receptor, and many more. The reader should have a good command of the function of signal transduction pathways described in Chapter 1 in order to understand how drugs acting at ligand-gated ion channels modify the signal transduction that arises from these receptors.

Drug-induced modifications in signal transduction from ionotropic (sometimes called ionotrophic) receptors can have profound actions on psychiatric symptoms. About a fifth of psychotropic drugs currently utilized in clinical practice, including many drugs for the treatment of anxiety and insomnia such as the benzodiazepines, are known to act at these receptors. Because ionotropic receptors immediately change the flow of ions, drugs that act on these receptors can have an almost immediate effect, which is why many anxiolytics and hypnotics that act at these receptors may have immediate clinical onset. This is in contrast to the actions of many drugs at G-protein-linked receptors described in Chapter 2, some of which have clinical effects – such as antidepressant actions – that may occur with a delay necessitated by awaiting initiation of changes in cellular functions activated through the signal transduction cascade. Here we will describe how various drugs stimulate or block various molecular sites around the receptor/ion-channel complex. Throughout the textbook we will show how specific drugs acting at specific ionotropic receptors have specific actions on specific psychiatric disorders.

Ligand-gated ion channels: structure and function

Are ligand-gated ion channels receptors or ion channels? The answer is “yes” – ligand-gated ion channels are a type of receptor and they also form an ion channel. That is why they are called not only a channel (ligand-gated ion channel) but also a receptor (ionotropic receptor or ion-channel-linked receptor). These terms try to capture the dual function of these ion channels/receptors.

Ligand-gated ion channels comprise several long strings of amino acids assembled as subunits around an ion channel. Decorating these subunits are also multiple binding sites for everything from neurotransmitters to ions to drugs. That is, these complex proteins have several sites where some ions travel through a channel and others also bind to the channel; where one neurotransmitter or even two cotransmitters act at separate and distinct binding sites; where numerous allosteric modulators – i.e., natural substances or drugs that bind to a site different than where the neurotransmitter binds – increase or decrease the sensitivity of channel opening.

Pentameric subtypes

Many ligand-gated ion channels are assembled from five protein subunits; that is why they are called pentameric. The subunits for pentameric subtypes of ligand-gated ion channels each have four transmembrane regions (Figure 3-2A). These membrane proteins go in and out of the membrane four times (Figure 3-2A). When five copies of these subunits are selected (Figure 3-2B), they come together in space to form a fully functional pentameric receptor with the ion channel in the middle (Figure 3-2C). The receptor sites are in various locations on each of the subunits; some binding sites are in the channel, but many are present at different locations outside the channel. This pentameric structure is typical for GABAA receptors, nicotinic cholinergic receptors, serotonin 5HT3 receptors, and glycine receptors (Table 3-1). Drugs that act directly on pentameric ligand-gated ion channels are listed in Table 3-2.

If this structure were not complicated enough, pentameric ionotropic receptors actually have many different subtypes. Subtypes of pentameric ionotropic receptors are defined based upon which forms of each

Table 3-1 Pentameric ligand-gated ion channels

agonist-to-antagonist spectrum of action of psychopharmacologic agents

of the five subunits are chosen for assembly into a fully constituted receptor. That is, there are several subtypes for each of the four transmembrane subunits, making it possible to piece toge

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