Approach to treatment

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  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.  Provide specific examples to agonists, antagonists, partial agonists and inverse agonists that we use in Psychotherapy
  2. Compare and contrast the actions of g couple proteins and ion gated channels.
  3. Explain how the role of epigenetics may contribute to pharmacologic action.
  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.

Read a selection of your colleagues’ responses.

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.

2

Herbert

Question 1

Based on the effects of a medication on the receptors, these medications may primarily be divided into antagonists and agonists. An agonist represents a medication that imitates signal ligand action through the activation of a receptor by binding. Conversely, antagonist medication binds to a receptor without activation. However, antagonists alleviate the receptor’s ability for activation by other agonists (Zamolodchikova et al., 2021). The agonist spectrum is classified into partial agonist, agonist, inverse agonist and antagonist. The agonist is responsible for channel opening for maximal frequency and amount for the binding site. In contrast, the antagonist, centrally sited at the spectrum, maintains a resting state while allowing channel opening. On the other hand, an inverse agonist keeps the ion channel inactive and closed. Lastly, antagonists can block materials in the agonist spectrum, which allows ions to return to a resting state. For an enhanced therapeutic action, ion flow and other signal transductions are needed with the right balance. This ideal state differs from one clinical case to the other depending on silent antagonism and agonism balance.

Question 2: g couple proteins vs. ion gated channels

Ligand-gated ion channels and G-protein coupled receptors represent two transmembrane protein types forming postsynaptic ion channels. G-couple proteins are, therefore, metabotropic receptors, while ion-gated channels are ionotropic receptors (Li et al., 2014). Gated ion channels involve the direct opening of ion channels through neurotransmitter binding, while g couple of proteins is involved in indirect ion channels binding with G-protein metabolic activation. In addition, ion-gated channels are coupled with ion channels, while G-proteins fail to couple with ion channels. Furthermore, gated ion channels represent a transmembrane ion-channel protein that opens to allow ion passage such as sodium, potassium and calcium into the membrane in response to a chemical messenger binding. On the other hand, G-coupled proteins are proteins in the cell membrane that bind extracellular substances and transmit signals to intracellular molecules named the G-protein from substances.

Question 3: Role of Epigenetics in the pharmacologic action

Epigenetics studies changes that affect the phenotype without leading to genotype changes. According to Lundstorm (2015), epigenetics may be defined as studying heritable but reversible gene expression changes without primary DNA sequence modifications. Each epigenetic gene regulation is essential for maintaining normal phenotypic cell activity and treatment for diseases such as neurodegenerative disorders and cancer.

Question 4: information and medicine prescription

Drug pharmacology knowledge is vital for mental health nurses as it may be key to understanding drug effects on patient health outcomes. For example, a mental health nurse should have adequate knowledge of drugs when dealing with Alzheimer’s patients. This disease cannot be completely treated, but its symptoms are controllable. Currently, researchers are focused on determining a cure for Alzheimer’s disease by reversing the mechanism causing neurocognitive decline (John Hopkins Medicine, 2022). Therefore, pharmacology knowledge of drugs will ensure a nurse determines whether to issue drugs to alleviate symptoms or reverse mechanisms causing the neurocognitive decline for Alzheimer patients.  

 

 

References

John Hopkins Medicine, (2022). Early-onset Alzheimer’s disease. 
Hopkinsmedicine.org. Retrieved from 

https://www.hopkinsmedicine.org/health/conditions-and-diseases/alzheimers-disease/earlyonset-alzheimer-disease Links to an external site.
.

Li, S., Wong, A. H., & Liu, F. (2014). Ligand-gated ion channel interacting proteins and their role in neuroprotection. 
Frontiers in cellular neuroscience
8, 125. 

https://doi.org/10.3389/fncel.2014.00125 Links to an external site.
.

Lundstrom K. (2015). What is the potential of epigenetics in drug development? 
Future medicinal chemistry
7(3), 239–242. 

https://doi.org/10.4155/fmc.15.2 Links to an external site.
.

Zamolodchikova, T. S., Tolpygo, S. M., & Kotov, A. V. (2021). From Agonist to Antagonist: Modulation of the Physiological Action of Angiotensins by Protein Conjugation-Hemodynamics and Behavior. 
Frontiers in pharmacology
12, 772217. 

https://doi.org/10.3389/fphar.2021.772217 Links to an external site.
.

FELICIA

ntroduction: Ligands are Ions or molecules that can bind to a receptor to produce a reaction or no reactions. Some examples of ligands are agonists, antagonists, partial agonists, and inverse agonists. A receptor is a molecule outside a cell that ligands can bind to and responds with an effect; it is quiet when not activated.

An agonist is an ion that binds with a receptor and produces a maximum effect on the receptor, changing the receptor’s shape, e.g., Morphine. A partial agonist binds with the receptor but cannot exert the full impact on the receptor; hence it is named a partial agonist; it can change the receptor’s shape slightly but not entirely like an agonist, e.g., Buprenorphine.

An antagonist ion binds to the receptor but exerts no effect; the receptor maintains its shape, e.g., Naloxone. An inverse agonist binds to the receptor and produces negative effects, e.g., Flumazenil.

Agonist-antagonist spectrum, if an agonist like Morphine binds to the receptor, it produces euphoria, sedating effect, and a reduction of pain. However, if an antagonist like Naloxone is taken, it will sit at the mu-opioid receptor and block the impact of the Morphine. When a Partial agonist tablet like Buprenorphine is taken, it will bring out reactions like respiratory depression even at a low dose, the response is weaker than an agonist like Morphine or heroin, so it is a safe medication with fewer addiction properties. When an inverse agonist like Flumazenil binds to the receptor, it prevents any usual activities, producing conflicting effects to the agonist, and blocking the receptor, so a patient who overdosed on an opioid will be given Flumazenil and that will reverse the impact of the opioid (Berg & Clarke, 2018).

Comparison between g protein and ion-gated channels: They are both postsynaptic ion channels that change and alter postsynaptic neurons. They are both signaling molecule membranes, and Neurotransmitters bind to both. In ion gated channel, a ligand will bind with the receptor, and the gate will open and allows ions like sodium, potassium, etc., to pass through to balance the negative and positive environment within the membrane; this is done by converting chemical signals to electrical reaction. The g protein-coupled receptor has a few steps to go through before opening the channel; when chemical neurotransmitter bind to the receptor instead of opening, it will turn on some g-protein which will join the extracellular materials and pass alerts to the intracellular g-protein. (Stahl, 2021).

 Role of epigenetics to pharmacologic action: Epigenetics studies how cells change gene activity while the DNA sequence remains intact; when there is a mutation in the DNA, diseases can ensue like cystic fibrosis, because epigenetics can target so many cells, so medications are now being manufactured to have broad effects, on the different epigenetic effects. (Stefanska & MacEwan 2015).

Importance of
 knowing the effect of epigenetics on pharmacologic action will assist the provider in knowing which medication to start the patient on in a timely fashion to prevent any adverse reaction; it will also help the Psychiatric Mental health nurse practitioner to understand how to dose the patient for maximum therapeutic effect, for example, knowing the action of Narcan, which is an opioid antagonist, when a patient is experiencing an opioid overdose, it is imperative to quickly administer Narcan to prevent death.

 

References

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 Links to an external site.

Stahl, S. M. (2021). 
Stahl’s Essential Psychopharmacology: Neuroscientific Basis and Practical (5th ed.) Cambridge University Press; 

https://doi.org/10.1017/9781108975292 Links to an external site.

Stefanska, B., & MacEwan, D. J. (2015). Epigenetics and pharmacology. 
British Journal of Pharmacology, 
172(11), 2701–2704, 

https://doi.org/10.1111/bph.13136 Links to an external site.

 

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