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Agonist-to-Antagonist Spectrum of The action of Psychopharmacologic Agents

Agonist-to-Antagonist Spectrum of The action of Psychopharmacologic Agents

Agonist-to-Antagonist Spectrum of The action of Psychopharmacologic Agents

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As mental health nurse practitioners, we need to understand the. basic knowledge of neuroscience to adequately treat and take care of our patients with mental health disorders. Agonist-to-Antagonist Spectrum of The action of Psychopharmacologic Agents


The Agonist-to-Antagonist Spectrum of The action of Psychopharmacologic Agents

An agonist is a pharmacologic agent that binds to a receptor and generates a biological response while an antagonist binds to a receptor and inhibits a response. Agonists have intrinsic efficacy which is the ability to increase the activity of a receptor, antagonists have the ability to decrease the activity of a receptor (Berg & Clarke, 2018). The agonist to antagonist spectrum of therapeutic agents includes agonist, partial agonist, antagonist, and inverse agonist (Berg & Clarke, 2018). Most typical and atypical antipsychotics act as inverse agonists when bound to the 5-HT2A and 5-HT2C receptors. An inverse agonist binds to receptors and produces an opposite effect to that of the full agonist (Sullivan et al. 2015).

G-protein Coupled Receptors and Ion Gated Channels

G-protein coupled receptor and ligand-gated ion channels are both proteins involved in membrane transport and intracellular communication (Duncan et al., 2020). Both G-protein coupled receptors and the ligand-gated ion channel transmembrane receptors control the opening and closing of ion channels allowing for extracellular ions to flow intracellularly.

The opening or closing of postsynaptic ion channels is accomplished in different ways by two families of receptor proteins. First is the ionotropic receptors linked directly to ion channels. These receptors contain an extracellular site that binds neurotransmitters and a membrane-spanning domain that forms an ion channel. The second is the G-protein coupled receptors do not have ion channels as part of their structure; instead, they affect channels by the activation of intermediate molecules called G-proteins (Purves et al., 2001).

Epigenetics in Pharmacology

Epigenetics refers to the regulation of gene expression through alterations in DNA or associated factors. These factors control the diverse manifestations of diseases. Understanding the epigenetic modification may lead to new therapies for diseases (Feinberg, 2018). The understanding of the actual function of the entire genome has made pharmacology to be modified further in tackling diseases not in the conventional ‘drug‐receptor’ sense, but in a more ‘global‐response’ sense. Epigenetic regulatory mechanisms may span more than one gene or family of proteins that regulate large groups of genes. Pharmacological agents targeting epigenetic changes have formed the bases of drug treatment of specific disease entities (Stefanska & MacEwan, 2015). Agonist-to-Antagonist Spectrum of The action of Psychopharmacologic Agents

Impact of Foundational Neuroscience on the Prescription of Medication.

According to Seo et al., (2018), Olanzapine as an antipsychotic modifies epigenetic changes in the BDNF gene. Serotonin, histamine, and dopamine as neurotransmitters utilize the ligand-gated ion channels mechanism to allow for ionic influx into the inner cell membrane. This action triggers signaling processes. The knowledge of the effect of agitation and schizophrenia on the central nervous system coupled with the mechanism of action, side effects, or toxicity of the antipsychotic (Olanzapine) will enable the nurse practitioner to prescribe the appropriate medication for patients.

A patient presented with severe agitation, visual and auditory hallucinations, and delusions. Equipped with the knowledge of the mechanism of action of Olanzapine, the Nurse practitioner gathered information about the patient’s past medical history that could affect the metabolism, efficacy, and toxicity of the medication. For example, Olanzapine is metabolized in the liver and excreted by the kidney. The Nurse Practitioner rules out any liver and kidney disease.

In conclusion, understanding the basics of neuroscience, epigenetic changes, and cell communication is important to mental health providers.


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

Duncan, A. L., Song, W., & Sansom, M. S. (2020). Lipid-dependent regulation of ion channels and G protein-coupled receptors: Insights from structures and simulations. Annual Review of Pharmacology and Toxicology, 60(1), 31-50. https://doi.org/10.1146/annurev-pharmtox-010919-023411

Feinberg, A. (2018). The key role of epigenetics in human disease prevention and mitigation. N Engl J Med. DOI: 10.1056/NEJMra1402513. https://www.nejm.org/doi/full/10.1056/nejmra1402513

Purves D, Augustine GJ, & Fitzpatrick D. (2001). Two Families of Postsynaptic Receptors. Neuroscience. 2nd edition. Sunderland (MA): Sinauer Associates; 2001. https://www.ncbi.nlm.nih.gov/books/NBK10855/

Seo, M. K., Kim, Y. H., McIntyre, R. S., Mansur, R. B., Lee, Y., Carmona, N. E., Choi, A. J., Kim, G., Lee, J. G., & Park, S. W. (2018). Effects of antipsychotic drugs on the epigenetic modification of brain-derived neurotrophic factor gene expression in the hippocampi of chronic restraint stress rats. Neural Plasticity, 2018, 1-10. https://doi.org/10.1155/2018/2682037

Stefanska, B., & MacEwan, D. J. (2015). Epigenetics and pharmacology. British Journal of Pharmacology, 172(11), 2701–2704. https://doi.org.ezp.waldenulibrary.org/10.1111/bph.13136

Sullivan, L., Clarke, W., & Berg, K. (2015). Atypical antipsychotics and inverse agonism at 5-HT<sub>2</sub> receptors. Current Pharmaceutical Design,


Kara Thomas-Jenkins

32 yo pregnant


My scenario is that of a 32-year-old pregnant lesbian (TJ) who is here to see me for her annual physical exam. Her chief complaint or issue coming in is that of vaginal discharge. I am her primary care provider and will not be doing an extensive obstetrician exam but will relay on previous notes that said she has had an uncomplicated pregnancy so far. She and her partner used sperm from a sperm bank to conceive. This discussion will look at how to get a comprehensive health assessment while remaining culturally sensitive.

Cultural and Lifestyle Awareness

Although the sexual orientation of a person should not influence how a health assessment is done, research suggests that there are many medical disparities of that of the lesbian, gay, bisexual, and transgender (LGBT) communities (Bidell, 2017). One way that LGQT communities feel discriminated against is that of lack of training of medical professionals to deal with the unique challenges the LGQT has (Bidell, 2017). This specific lack of training can cause clinical judgment and personal bias to leak into medical decisions (TIAN & HEN, 2019). This can cause the perfect storm of devaluing the patient’s insight into their health and dismissing symptoms due to this bias (TIAN & HEN, 2019).

Targeted Questions and explanation of Why Chosen

With the thought that personal ideas and judgment can leak into decision-making for my patient, it is important to fall back on basic questions I would ask any of my patients who presented with the same chief complaint.

  1. What does the vaginal discharge, look like, and is there a smell? This question is asked to try and narrow down what type of gynecological issue is present. Is this leaking of the fluid or rupture of membranes? Is she having bleeding that needs to be emergently looked at? Is a sample of this discharge needed? These are all questions I would be able to narrow down once I understood what type of discharge it was.
  2. How long have you had this discharge? Again, this will help facilitate where to go from there, if it is something I can treat or if she needs to be seen by an OBGYN
  3. Have you had discharge like this before? This could possibly help narrow down the diagnosis.
  4. How has your mental health been? This question is good for any pregnant woman and can spark conversation about what else might be going on in her life.
  5. Are there any other issues you are having or that concern you? This is a good open-ended question to allow a conversation to flow and for my patient to open up and inform of anything else that might be on their mind. Agonist-to-Antagonist Spectrum of The action of Psychopharmacologic Agents

Strategies for Being Culturally Sensitive

Being sensitive and understanding to different cultures and lifestyles is imperative in the medical community. It might be impossible to fully understand each culture’s unique and diverse traits but it is the job of medical professionals to be aware of their own bias (Bidell, 2017). That being said one of the most important strategies a medical professional can do to keep these bias low and increase their own cultural competence is to continue to learn (Ndiwane et al.,2017). It is imperative that we do not get complacent but strive for more learning (Ndiwane et al., 2017). One of the best ways to learn is to use a simulation on how you might treat a patient and then learn of their culture (Ndiwane et al., 2017). Once this is done you retry the simulation and see how you might treat the patient differently or ask/frame a question differently (Ndiwane et al., 2017). This allows real-time information on bias without using patients as the test subjects. This allows failure and growth without hurting or misdiagnosing a real patient (Ndiwane et al., 2017).


Bidell, M. P. (2017). The Lesbian, Gay, Bisexual, and Transgender Development of Clinical Skills Scale (LGBT-DOCSS): Establishing a New Interdisciplinary Self-Assessment for Health Providers. Journal of Homosexuality, 64(10), 1432–1460. https://doi-org.ezp.waldenulibrary.org/10.1080/009…

Ndiwane, A. N., Baker, N. C., Makosky, A., Reidy, P., & Guarino, A. J. (2017). Use of Simulation to Integrate Cultural Humility Into Advanced Health Assessment for Nurse Practitioner Students. Journal of Nursing Education, 56(9), 567–571. https://doi-org.ezp.waldenulibrary.org/10.3928/014…

Shu-Hui TIAN, & Man-Hua SHEN. (2019). The Implementation of the Right to Equality in the Care of a Vulnerable Medical Population: Pregnant and Postpartum Lesbians. Journal of Nursing, 66(5), 71–78.