- 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.
A molecule, such as a hormone, neurotransmitter, or drug that binds to a cell receptor site causing cell to become more active, causing a specific physiological response that can be natural or artificial (Christie, 2016). An antagonist a substance that blocks the action of another, as a drug that binds to a receptor for a hormone, neurotransmitter, or another drug blocking the action of that substance without producing any physiologic effect itself (Grandy, 2016). A partial agonist are drugs that can activate the receptors, and can decrease the response of an activated receptor by a stronger agonist (Kenakin, 2017). An inverse antagonist binds to the receptor and decreases the activity of the receptor, which reverses the effect of the binding agonist (Berg & Clarke, 2018). Discussion: Foundational Neuroscience
- Compare and contrast the actions of g couple proteins and ion gated channels.
The G-protein coupled receptors (GPCRs) are the largest and most versatile protein family. The g protein has the most abundant membrane receptors, responsible for specific functions in human. This makes them a great attraction for drug binding and interaction (Johnson & Lovinger, 2016). Ion gated channels bind to a receptor opening a channel that only allows specific ions to pass, once the channel is open the membrane may be polarized or depolarized (Bylund, 2014).
- Explain how the role of epigenetics may contribute to pharmacologic action.
Epigenetics is the study of changes in gene expression that does not involve change the DNA sequence, thus a change in phenotype, not genotype, and affects how cells read genes (Rasool et al, 2015). “Epigenetic mechanisms in health and disease has uncovered changes in DNA methylation and chromatin structure that may contribute to psychiatric disorders” (Schuebel, Gitik, Domschke, & Goldman 2016). Recent studies in epigenetics have revealed a correlations between DNA and depression; using epigenetics can help personalized a patient’s medication regimen, especially if they are not responding to traditional medicines (Rasool et al, 2015).
- 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
Understanding how a drug will affect the patient and the way the patient’s body will affect the drug is critical when prescribing medications (Laureate Education, n.d.). Knowing that labs should be obtained periodically certain medication like lithium for bipolar to monitor therapeutic ranges, kidney function and toxicity. Lithium can cause renal insufficiencies.
- Nurse practitioner must be aware of the medication’s action.
In order to safely prescribed medications and prevent adverse reactions, a Nurse Practitioner should have an understanding of drug-drug interactions and food-drug interactions (Laureate Education, n.d.). It is impossible to know all interactions, so the clinician should have resources readily available, such as a drug book or PDA (Laureate Education, n.d.). Understanding the medication’s action will require the Nurse Practitioner to have knowledge of pharmacokinetics and pharmacodynamics in particular age groups. For example, if prescribing a medication to an elderly patient that excretes through the kidneys, the clinician should understand that as a person ages, kidney functioning decreases, which depending on the drug that can cause toxicity (Ponticelli, Sala, & Glassock, 2015). The goal is to effectively treat the patient without causing harm.
References
Berg, K. & Clarke, W. (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
Bylund, D. (2014). Reference Module in Biomedical Science. Science Direct. Retrieved from https://www.sciencedirect.com/referencework/9780128012383/biomedical-sciences
Christie, M. (2016 April 28). Explainer: how do drugs work? The Conversation. Retrieved from https://theconversation.com/explainer-how-do-drugs-work-48665
Grandy, D. (2016). Neuropathology of Drug Addictions and Substance Misuse. Science Direct. Retrieved from https://www.sciencedirect.com/book/9780128002124/neuropathology-of-drug-addictions-and-substance-misuse.
Johnson, K., & Lovinger, D. (2016). Presynaptic G Protein-Coupled Receptors: Gatekeepers of Addiction? Frontier in Cellular Neuroscience. Retrieved from https://www.frontiersin.org/articles/10.3389/fncel.2016.00264/full
Kenakin, T. (2017). Pharmacology in Drug Discovery and Development Understanding Drug Response. Science Direct. Retrieved from https://www.sciencedirect.com/book/9780128037522/pharmacology-in-drug-discovery-and-development.
Laureate Education (producer). (n.d.) Introduction to advanced pharmacology [Video File]. Baltimore, MD: Author
Rasool, M., Malik, A., Naseer, M. I., Manan, A., Ansari, S., Begum, I., Qazi, M. H., Pushparaj, P., Abuzenadah, A. M., Al-Qahtani, M. H., Kamal, M. A., & Gan, S. (2015). The role of epigenetics in personalized medicine: challenges and opportunities. BMC medical genomics, 8 Suppl 1(Suppl 1), S5. https://doi.org/10.1186/1755-8794-8-S1-S5
Schuebel, K., Gitik, M., Donschke, K., & Goldman, D. (2016). Making Sense of Epigenetics. International Journal of Neuropsychopharmacology, 19(11). https://doi.org/10.1093/ijnp/pyw058