Assignment: Psychopharmacological Approach To Treat Psychopathology/NURS 6630

Assignment: Psychopharmacological Approach To Treat Psychopathology/NURS 6630

Assignment: Psychopharmacological Approach To Treat Psychopathology/NURS 6630

Psychopharmacological Approach to Treat Psychopathology

In pharmacodynamics, the main considerations are medication effects and mechanisms in the body. Therefore, for any medication to interact with the body, these drugs must get to their target cell to bind with a receptor. According to Rollema and Hurst (2018), receptors refer to specialized proteins within cells that bind to a ligand, a signal molecule, where they can easily alter their activity or shape. Such changes are crucial since they lead to cell behaviors and activity changes. Hence, depending on the drug’s effect on the receptor, these drugs usually exist in two categories, the antagonist and the agonists.

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As the discussion post explains, agonists refer to drugs or medications that usually mimic signal ligand actions in terms where it binds and activates the receptor. For the antagonist, it refers to the medications that can easily bind to receptors with no activation. Still, in return, they decrease the receptor’s ability to be activated by an agonist. Within the classification, there are still medications under the partial agonists, which tend to resemble an agonist, but the difference is that its receptor activation is minimized. Hence, the maximal response associated with an agonist can be determined by receptors’ intrinsic activity or receptors’ numbers linked with the agonist, which mainly depends on provided agonist amount (Coleman et al., 2019).

In elaborating on the reactions between an agonist, antagonist, and partial agonist, these reactions happen mostly in individuals who use opioids. For instance, a drug like methadone is an agonist; it binds to receptors and becomes addictive. On the other hand, Naloxone presents itself as an antagonist, while an example of a partial agonist is the Buprenorphine. Therefore, if a patient has had a methadone overdose the clinician can opt for an antagonist like Naloxone to reverse binding and block any chance of methadone binding with the receptors (Mégarbane et al., 2020).

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References

Coleman, R. A., Woodrooffe, A. J., Clark, K. L., Toris, C. B., Fan, S., Wang, J. W., & Woodward, D. F. (2019). The affinity, intrinsic activity and selectivity of a structurally novel EP2 receptor agonist at human prostanoid receptors. British journal of pharmacology, 176(5), 687-698. https://doi.org/10.1111/bph.14525

Mégarbane, B., Chevillard, L., & Vodovar, D. (2020). Naloxone should remain the appropriate antidote to treat opioid overdose. Critical Care, 24(1), 1-3. https://doi.org/10.1186/s13054-020-2835-5

Rollema, H., & Hurst, R. S. (2018). The contribution of agonist and antagonist activities of α4β2* nAChR ligands to smoking cessation efficacy: a quantitative analysis of literature data. Psychopharmacology, 235(9), 2479-2505. https://doi.org/10.1007/s00213-018-4921-9

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The agonist/antagonist spectrum represents how drugs can act on specific receptors. In psychophamacotherapy, G-protein-linked receptors are often targeted by medications using this spectrum (Stahl et al., 2021). On one side, you have an agonist. It is meant to fully activate a specific receptor (Stahl et al., 2021). Without an agonist, you still have the potential for particular receptors to be acted on naturally, but more weakly; this is called constitutive activity (Stahl et al., 2021). Agonists, as stated previously, can fully activate a receptor. They can do this both directly, by binding to a neurotransmitter site, or indirectly, by blocking both inactivation processes and eliminating neurotransmitters (Stahl et al., 2021). In sort of the middle of the spectrum are antagonists. Antagonists may erroneously be categorized as the opposite of an agonist. But, antagonists are simply silent security that lay in wait to block the specific neurotransmitter agonist they’ve been set for (Stahl et al., 2021).

Between agonist and antagonist, you have a partial agonist. An antagonist also blocks partial agonists. They act more strongly than no agonist but less than a full one. They can be used when less action is needed or if stabilization is the goal (Stahl et al., 2021). Lastly, we have inverse agonist, which is actually on the opposite end of the spectrum from agonist. There is more than just something blocking the receptor to specific agonists with an inverse agonist. An inverse agonist can decrease signal transduction and completely stop an agonist from working on a receptor to the point of causing an opposite reaction (Stahl et al., 2021).

Both ion-gated channels and G-couple proteins use receptors to collect ligands from extracellular space (though there are rare exceptions where the receptors are in the intracellular area). Specific ligands fit perfectly into their bio channel receptor, changing their shape (Weir, n.d.) How they do this, though, is entirely different. Ion channels are closed until a specific ligand attaches to an allosteric site; from there, it can control the opening of the channel (Weir, 2010). The permeability of the plasma membrane is changed, and ions are free to move through. They can cause either hyperpolarization or depolarization (Weir, 2010).

On the other hand, G-couple proteins have seven transmembrane alpha helixes that bind to GTP and GDP. A specific ligand binds to the receptor and causes a conformational change. The GPCR exchanges GDP for GTP, which causes the alpha subunit to separate from beta and gamma, and then they can both interact with target proteins (Weir, 2010.) The alpha unit can activate selected protein and relay signals until the process is stopped by the hydrolysis of GTP, forming GDP and ending the loop (Weir, 2010)

Epigenetics studies molecularly mediated interaction between genomes and the environment (DeSocio, 2016). The mechanism of epigenetics works by altering chromatin, which can then control the expression of a gene (Stahl et al., 2021). The critical distinction between epigenetics and genetics is that epigenetic changes are reversible (Camprodon & Roffman, 2016). Epigenetic studies supply evidence that supports the combination approach of medication, therapy, and education in psychiatry (DeSocio, 2016). This means that epigenetics can help to guide pharmaceutical strategies.

All of this information is valuable to a Nurse Practioner. Being conscious of how the drug class works on the receptor and what pathway we are targeting can be vital to care. Epigenetics also proves crucial as it helps establish a multifaceted approach as ideal in psychiatric care. There are many instances in which this knowledge could be beneficial. One particular example that comes to mind would be in the case of schizophrenia. Dopamine is thought to be the primary neurotransmitter involved (Camprodon & Roffman, 2016). Antipsychotics are typically antagonists that target dopamine receptors, but some are different, like ariprpazole, a partial agonist. So if we find that a typical antipsychotic isn’t working well to control symptoms or causes unwanted side effects, we might try something like aripiprazole that will work a little differently and perhaps help regulate dopamine more evenly.

References

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. Elsevier.

DeSocio, J. (2016) Epigenetics: An emerging framework for advanced practice psychiatric nursing. Perspectives in Psychiatric Care, 52(3), 201-207. https://doi.org/10.1111/ppc.12118

Stahl, S. M., Grady, M. M., & Muntner, N. (2021). Stahl’s essential psychopharmacology neuroscientific basis and practical applications. Cambridge University Press.

Weir, C. J. (2010). Ion channels, receptors, agonists, and antagonists. Anaesthesia & Intensive Care Medicine, 11(9), 377–383. https://doi.org/10.1016/j.mpaic.2010.06.002

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