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For this assignment, a response to a colleague’s post is needed from a class discussion that was assigned. Based on my colleague’s response, I am to respond with one of the followings:
- If your colleagues’ posts influenced my 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.
Below is the initial class discussion topic that is to be responded to and attached in PDF file are two (2) post that need a response based on one of the two (2) bullets above:
- 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.
For this assignment, a response to a colleague’s post is needed from a class discussion that was assigned. Based on my colleague’s response, I am to respond with one of the followings: If your colleag
[POST A Agonist-Antagonist Spectrum Agonists are drugs that activate specific receptors within the brain and cause full effect of the drug to take place and a partial agonist is a drug that acts as an agonist with a reduced degree of receptor activation (Indian Health Service, 2020). Antagonist drugs block the receptors so they are not able to bind to the agonist. Inverse agonists have the opposite actions compared to agonist but the effects of both inverse agonist and agonist can be blocked by antagonists (Nutt, et al, 2016). G-Couple Proteins and Ion Gated Channels Ion gated channels (IGCs), also known as ligand-gated ion channels, and G-protein-coupled receptors (GPCRs), also known as metabotropic receptors, are two classes of post-synaptic receptors. IGCs function to bind neurotransmitters extracellularly and to form the ion channel. GPCRS function via a second messenger system that move more slowly and are reliant on metabolic steps (Camprodon & Roffman, 2016). When a neurotransmitter binds to the GPCR it activates G-proteins leading the G-proteins to then separate from the receptor and to interact with the ion channel directly or to pair with effector proteins in order to control the ion channels via intracellular messengers (McEnery & Seigel, 2014). Epigenetics Epigenetics is the idea that gene function can be altered without changing the DNA and RNA codes; and this functional change may be inherited (Camprodon & Roffman, 2016). Epigenetics may determine how medications work on specific genes and the efficacy of that drug. For example, when a patient has an altered dopamine receptor binding may have more of an inclination for drug addiction or some degree of natural tolerance (Saad et al, 2019). Epigenetics is the logic behind why some medications work for some individuals but not for others. Effect on Prescribing Medications This information is essential to keep in mind for prescribers as it will affect the way an individual patient will respond to treatment. There is evidence to suggest that epigenetic modulations may play a part in psychiatric diseases such as schizophrenia and bipolar disorder and that analysis of epigenetic changes of psychoactive drugs can help to determine the dysfunctional genes and the pathways in the brain in order to predict potential side effects of drugs and to identify new pharmaceutical targets for the treatment of these diseases (Boyadijeva & Varadinova, 2012). An example of why this knowledge is essential is some individuals have a specific genetic variant with reduced enzyme activity that will increase their likelihood of having lithium toxicity due to a slower metabolism of lithium and a build of the drug within their systems. The reverse may occur in patients with duplications of the allele as it metabolizes the medication more quickly (Butler, 2018). Healthcare providers must be aware of these possibilities so they can adjust the dosages of lithium and make their patients aware of the potential for these adverse events. POST B Agonist to Antagonist Spectrum Psychopharmacologic drugs bind to receptor sites on neurons according to a spectrum of action from agonist to antagonist. Neurotransmitters created in the body are agonists, they bind to and activate receptors on cells. Many psychiatric medications are also agonists, so they activate receptors causing an increase in the cell’s function. An example of an agonist is an opioid, such as morphine, which mimics enkephalins and endorphins produced by the body to alleviate pain (Vallerand et al., 2017). Some psychiatric medications are antagonists, which means they bind to receptors on cells and block the action of neurotransmitters, thereby decreasing the activity of the cell. An example of an antagonist is a beta blocker such as Propranolol, which binds to beta receptors in the heart muscle and blocks the binding of adrenaline (Vallerand et al., 2017). Between the two ends of the spectrum there are psychopharmacologic agents that act as partial agonist, and some that act as inverse agonists. Partial agonists bind to receptors but only mildly increase the activity of the cell. If a partial agonist is joined by an agonist in the synaptic cleft, it becomes an antagonist, because the agonist will increase the activity of the cell to a greater degree than the partial agonist, therefore relatively is has an antagonistic action (Weir, 2020). Buprenorphine is a partial agonist, as it binds to opiate receptors, thereby decreasing pain, but in the presence of morphine, which is an agonist, buprenorphine becomes an antagonist, because it blocks pain to a lesser degree than morphine. Inverse agonists act on cells that are partially active even in the absence of an agonist neurotransmitter or medication. While antagonists’ only function is to block the ability of agonists to bind to and activate receptors, inverse agonists bind to receptors and actually decrease the activity of the cell (Rosenthal & Burchum, 2021). G-Coupled Proteins and Ion Gated Channels Both G-protein coupled receptors and ion gated channels exist on dendrites of neurons and bind with neurotransmitters or medications. In the case of psychiatric medications, the effect on the cell is determined by whether the drug is an agonist, a partial agonist, an agonist, or an antagonist, and what other neurotransmitters or drugs are in the synaptic cleft. G-protein coupled receptors are the most common type of receptor on cell surfaces in the body, but they are also slower acting, as the binding of a neurotransmitter or drug to this receptor causes a cascade of communication among protein messengers intracellularly, eventually resulting in activation of the cell to perform its function (Weir, 2020). Ion channels are made of glycoproteins and water and are bound to the phospholipid membrane of cells. Receptors on ion channels are able to bind with neurotransmitters which cause the channel to open thus allowing ions into the cell that otherwise would not have been able to cross the phospholipid barrier. The ions then cause depolarization or hyperpolarization and either activate the cell to perform it’s given function or prevent it from doing so. Ion channels allow for faster communication between cells than G-protein coupled receptors (Weir, 2020). Epigenetics and Pharmacology Behaviors and environment can affect the way an individual’s genes are expressed. As an example, G-coupled protein receptors can bind to many different chemicals, creating an effect on the cell. One way in which these chemicals may affect the cell is to affect gene expression by communicating with the cell nucleus via second messenger systems. If the chemical is a carcinogen and the patient’s DNA contains genes coding for the development of cancer, exposure to the chemical may result in these genes being expressed (CDC, 2022). In pharmacology, the binding of a drug such as a serotonin reuptake inhibitor (such as fluoxetine) to serotonin transporters can result in increased availability of serotonin for uptake by cells, and over time may repress the genetic expression of serotonin transporters, allowing for increased levels of serotonin and a decrease in depression (Baudry et al., 2019). Impact on Prescribing As a psychiatric nurse practitioner, it is important to be aware of the effects and potential side effects of the medications prescribed. We must be aware of the method of action; is the medication an agonist, partial agonist, inverse agonist, or antagonist? We need to understand the neurotransmitters the medications act on, and where else in the body these neurotransmitters are functional and how. For example, when prescribing a selective serotonin reuptake inhibitor, we must be aware that serotonin is active in the digestive tract as well as the brain, and that administration of this drug could therefore cause a side effect of diarrhea. It is also important to maintain awareness of the social determinants of health our patients are experiencing, as issues such as lifestyle factors, poverty or adverse childhood experiences can affect epigenetics and thus help us understand the disease processes our patients may be contending with.