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.

Each post should have at least two cited resources.

Post #1

Claire

Main question post

Agonist-to-antagonist Spectrum of Action of Psychopharmacologic Agents

An agonist is a chemical that helps bind the receptor activates with a receptor, and a biological response is produced. In comparison, an antagonist permanently blocks the action of the agonist. An agonist will always cause an activity different from an antagonist’s. Four different types of a spectrum include the inverse agonist, partial agonist, agonist, and the antagonist. The agonist opens the channel to the frequency that is allowed in the binding site and the maximum amount. Despite this, the antagonist will retain the resting state with the opening of the channel not being frequent. The inverse agonist puts the ion channel in an inactive state. The antagonist makes the ability to block an object or return the ions to a resting state possible. The agonist stimulates an action but sits idle when influenced by the antagonist (Van Baelen et al., 2022). When signal transduction is neither cold nor hot, and the ions flow, an ideal therapeutic activity of a drug is achieved as it is in equilibrium. This state varies in clinical cases depending on the balance between silent antagonism and agonism.

G couple proteins and ion gated channels.

Two families belong to the receptor proteins that help in the opening and closing of the postsynaptic ion channels. One of the receptors is called the ionotropic receptor, which is linked closely to the ion channels. Such receptors have two functional domains; one is an extracellular site, and the second one is a membrane-widening domains that forms an ion channel. Therefore, the inotropic receptors add to the channel functions, and the transmitter binds into one molecular entity called the ligand-gated ion channels (Petroff et al., 2022). These receptors are multimers and have four to five subunits of the individual subunits of proteins. The second family consists of metabotropic receptors, where the ion movements depend on either one or more metabolic phases. These receptors have no ion channels, but the activation of G proteins intermediate molecules affects the track. The G protein-coupled receptors are referred to as metabotropic receptors. The G proteins act as transducers that accord the neurotransmitter to the postsynaptic ion channels.

Epigenetics

The study of changes that affect the phenotype without causing changes in the genotype is known as epigenetics. The learning involves facts on the reversible hereditary gene expressions without modifying the DNA sequence. Today, the epigenetic mechanisms, especially the circulating miRNAs, have been used for diagnostic biomarkers. For the treatment of cancerous diseases and maintenance of the regular activity of cells, there is a need for epigenetic regulation of the activities of the gene (Bouyahya et al., 2022). Neurodegenerative disorders include schizophrenia and dementia. The rule of epigenetic mechanisms to manage infections in humans is made possible by the new classes of drugs.

Impact with prescribing

This information may impact medication as nurse practitioners must be aware of how drug actions benefit patients. It also helps in the prescription of drugs, especially for mental health patients and those with psychiatric disorders, as there might be an alteration of medications due to the changes in the neurocognitive mechanism. While working with Alzheimer’s disease patients with a mental health illness, nurse practitioners must be mindful of the medicine’s actions as the disease is chronic and symptoms appear slowly but degenerate each time. Alzheimer’s disease worsening symptoms can be controlled but cannot be treated completely. Epigenetic modifications can reverse the mechanism of neurocognitive decay. Scientists and researchers are finding ways to get a complete cure for the disease. It is possible to determine if the focus of treatment will help stop the symptoms from worsening through the knowledge of pharmacology drugs, especially while treating Alzheimer’s disease. This knowledge can also help in making efforts to reverse the disease processes.

Post #2

Melinda

Week 2 Initial Discussion Post

Agonist-to-Antagonist Spectrum

An agonist is a drug’s ability to bind to a receptor, and how they can change the receptor to produce a response, this is known as affinity and intrinsic efficacy (Berg & Clarke, 2018). Like the agonist, an antagonist has an affinity, the ability to bind to a receptor, but does not have intrinsic efficacy or the ability to elicit a response (Berg & Clarke, 2018). The intrinsic efficacy is dependent on the structure of a drug and can determine if an agonist will provide a full or partial response (Berg & Clarke, 2018). In addition to drug structure, the number of receptors needed to elicit a response can vary but still produce a maximum response (Berg & Clarke, 2018).

G-Coupled Proteins and Ion Gated Channels

The G-coupled proteins and ion-gated channels are neurotransmitter receptors (Camprodon & Roffman, 2016). The effect of the neurotransmitter receptors results in either a rapid or slow effector system (Camprodon & Roffman, 2016). A rapid effector system is the ion-gated channels, and they can quickly alter neuronal activity and membrane potential on their own (Camprodon & Roffman, 2016). The G-coupled-protein receptors require a second messenger system and result in a slow effector system (Camprodon & Roffman, 2016).

Epigenetics

The term epigenetics is used to explain how one’s environment can affect their genes (Kular & Kular, 2018). Epigenetics makes no changes to DNA, but it instructs cells to interpret signals from genes and the environment to make appropriate adjustments (Kular & Kular, 2018). Because epigenetics is a gene and behavior-based process, the use of them for treatments in psychiatry is promising (Kular & Kular, 2018).

Impact on Medication Prescribing

Prescribing medications to patients suffering from behavioral health issues is difficult as they are prescribed based on behaviors and information supplied by patients and family members. Understanding the information mentioned earlier is vital for treating an individual who suffers from an opioid use disorder. When assisting an individual through opiate detox, an agonist is prescribed, and it may be prescribed for an individual’s lifetime (Gold et al., 2020). Understanding the effect that epigenetics can have, if one’s environment and the behaviors that resulted in drug use can be changed, they may not need lifelong medication.

Week 2 Response-Sample Solution

Reply to Claire

(Epigenetics Discussion and Responses-Essays)Your post offers a concise and straightforward summary of the three subjects mentioned. You have described the various agonist and antagonist kinds and their effect on receptor activation. In addition, you discussed the function of G proteins and the two groups of receptors that regulate ion channels. You have also described epigenetics and its effects on gene expression without changing DNA sequences (Barnett- Norris et al., 2022). Although your post gives an excellent introduction to the subject matter, there is undoubtedly more to learn and explore. It is important to note that the concept of an inverse agonist only applies to receptors with some level of constitutive activity, meaning that they are active even without any ligands. Inverse agonists decrease this constitutive activity, whereas antagonists do not affect it. The distinction between inverse agonists and antagonists can be crucial in drug development, as a ligand with inverse agonist properties may have different therapeutic effects than a pure antagonist.(Epigenetics Discussion and Responses-Essays)

I also agree that mentioning the main epigenetic mechanisms, including DNA methylation, histone modifications, and non-coding RNAs such as miRNAs and lncRNAs, provided a more comprehensive overview of epigenetics (Barnett- Norris et al., 2022). It is worth noting that these mechanisms have also been linked to other psychiatric disorders, including depression, anxiety, and addiction. I would like to add that the spectrum of action can differ depending on the receptor subtype and the specific drug used. For example, a drug may act as a full agonist at one subtype of a receptor but as a partial agonist or antagonist at another subtype of the same receptor (Mattei et al., 2022). Additionally, a drug may act as an agonist at one receptor and an antagonist at another. Healthcare providers need to be aware of these nuances when prescribing medications.(Epigenetics Discussion and Responses-Essays)

References

Barnett-Norris, J., Lynch, D. L., Reggio, P. H., & Thomas, J. B. (2019). From molecular to modular pharmacology: The G protein-coupled receptor (GPCR). Journal of medicinal chemistry, 62(1), 1–46.

Mattei, A.L., Bailly, N., & Meissner, A.(2022). DNA methylation: a historical perspective. Trends in Genetics.

Reply to Melinda

(Epigenetics Discussion and Responses-Essays)The agonist-to-antagonist spectrum, G-coupled proteins, ion-gated channels, and epigenetics are all covered in your post straightforwardly and concisely. Your post accurately describes the ideas and their effect on medication prescription, particularly for opioid use disorder. I would like to add that the potency and efficacy of a drug can vary depending on the receptor subtype and the specific drug used. For example, a drug may act as a full agonist at one subtype of a receptor but as a partial agonist or antagonist at another subtype of the same receptor (Kenakin, 2019). Additionally, a drug may act as an agonist at one receptor and an antagonist at another. Healthcare providers need to be aware of these nuances when prescribing medications. Your post also accurately describes epigenetics as a process that affects gene expression without changing DNA sequences. However, it is worth noting that several epigenetic mechanisms, including DNA methylation, histone modifications, and non-coding RNAs such as miRNAs and lncRNAs, regulate gene expression. (Tsai, 2021). These mechanisms have also been linked to other psychiatric disorders, including depression, anxiety, and addiction.(Epigenetics Discussion and Responses-Essays)

References

Kenakin, T. (2019). Pharmacology in drug discovery and development: Understanding drug response (3rd ed.). Academic Press.

Tsai, C. (2021). Epigenetics in psychiatry. In M. Ritsner (Ed.), The Handbook of Neuropsychiatric Biomarkers, Endophenotypes, and Genes (pp. 1–30). Springer.