NURS 6630 Week 2 Agonist to Antagonist Spectrum

NURS 6630 Week 2 Agonist to Antagonist Spectrum Response

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Mackenzie Gray

Agonist-to-Antagonist Spectrum

An agonist is a drug that binds to and activates the receptor and yields a biological response (Salahudeen & Nishtala, 2017). Agonists allow the ion channels to be fully open, which enabling the drug to bind fully to the receptor site (Stahl, 2013). Agonists have an efficacy of one; therefore, these drugs are fully capable of producing a pharmacological response when bound to a receptor (Salahudeen & Nishtala, 2017).

An antagonist is a drug that binds to receptors and obstructs the agonist from the receptor site (Salahudeen & Nishtala, 2017). Antagonists can partially block agonists and reduce the agonist’s effects; however, antagonists may also completely block agonists if the concentration is high enough (Salahudeen & Nishtala, 2017). Antagonists have an efficacy of zero; therefore, these drugs are incapable of producing a pharmacological response (Salahudeen & Nishtala, 2017). Antagonists allow ions and receptors to be in their resting states (Stahl, 2013).

Partial and inverse agonists function in ways that can interfere with psychopharmacologic treatments. A partial agonist is a drug that can bind and activate the receptor, but it is unable to produce an adequate response (Salahudeen & Nishtala, 2017). Partial agonists have an efficacy range greater than zero but less than one (Salahudeen & Nishtala, 2017). An inverse agonist is an agonist that generates the opposite pharmacological response (Salahudeen & Nishtala, 2017).

G-Protein Coupled Receptors and Ion Gated Channels

G-protein coupled receptors (GPCRs) are essential proteins because cells use them to transmit extracellular stimuli into intracellular responses (Zhao et al., 2016). For example, GPCRs respond to hormones, neurotransmitters, and senses (Zhao et al., 2016). GCPR structure has seven transmembrane helices (Zhao et al., 2016). GPCRs are numerous and are the largest transmembrane receptor group in humans (Zhao et al., 2016). GCPRs bind to G proteins, which results in further signal pathways being activated (Zhao et al., 2016). GCPRs work slowly to relay messages due to the multi-step pathway to forward information (Camprodon & Roffman, 2016).

Ligand-gated ion channels have several long amino acid strands divided into smaller subunits around an ion channel (Stahl, 2013). The amino acid strands have receptor binding sites for various items, such as neurotransmitters, ions, and drugs (Stahl, 2013). Ligand-gated ion channels are often arranged in subunits consisting of five proteins, which are further divided into four transmembrane areas (Stahl, 2013). Ions flow through the channels rapidly compared to GPCRs (Camprodon & Roffman, 2016).

Epigenetics

Epigenetics is the study of how one’s environment or behaviors may alter their gene expression without changing the genetic code (Camprodon & Roffman, 2016). Research suggests that an individual’s epigenetic changes may influence their response to drugs, and provider awareness of epigenetic changes may be essential for therapeutic response to drugs (Schuebel et al., 2016). For example, if a patient experiences alteration to chromatin, they should be treated with a drug that affects the structure of chromatic, such as valproic acid (Camprodon & Roffman, 2016).

Prescribing Considerations

When prescribing medications, PMHNPs must be cognizant of a drug’s action and how individuals may metabolize the drug. For example, fluoxetine is metabolized by the cytochrome P450 2D6 (Eli Lilly and Company, 2006). Individuals who are deficient in this cytochrome may experience slower metabolization of fluoxetine, resulting in higher concentrations of fluoxetine (Eli Lilly and Company, 2006). These individuals may need a lower dose of fluoxetine to experience therapeutic effects (Eli Lilly and Company, 2006). Patients may experience mania if fluoxetine concentrations are too high (Eli Lilly and Company, 2006).

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 (pp. 1–19). Elsevier.

Eli Lilly and Company. (2006). Prozac [package insert]. Retrieved from /orders/www.accessdata.fda.gov/drugsatfda_docs/lab…

Salahudeen, M. S., & Nishtala, P. S. (2017). An overview of pharmacodynamic modelling, ligand-binding approach and its application in clinical practice. Saudi Pharmaceutical Journal: The Official Publication of the Saudi Pharmaceutical Society, 25(2), 165–175. /orders/doi.org/10.1016/j.jsps.2016.07.002

Schuebel, K., Gitik, M., Domschke, K., & Goldman, D. (2016). Making sense of epigenetics. The International Journal of Neuropsychopharmacology, 19(11), pyw058. /orders/doi.org/10.1093/ijnp/pyw058

Stahl, S. M. (2013). Stahl’s essential psychopharmacology: Neuroscientific basis and practical applications (4th ed.). Cambridge University Press.

Zhao, J., Deng, Y., Jiang, Z., & Qing, H. (2016). G protein-coupled receptors (GPCRs) in Alzheimer’s Disease: A focus on BACE1 related GPCRs. Frontiers in Aging Neuroscience, 8, 58. /orders/doi.org/10.3389/fnagi.2016.00058

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Discussion Questions (DQ)

Initial responses to the DQ should address all components of the questions asked, including a minimum of one scholarly source, and be at least 250 words. Successful responses are substantive (i.e., add something new to the discussion, engage others in the discussion, well-developed idea) and include at least one scholarly source. One or two-sentence responses, simple statements of agreement or “good post,” and responses that are off-topic will not count as substantive. Substantive responses should be at least 150 words. I encourage you to incorporate the readings from the week (as applicable) into your responses.

Weekly Participation

Your initial responses to the mandatory DQ do not count toward participation and are graded separately. In addition to the DQ responses, you must post at least one reply to peers (or me) on three separate days, for a total of three replies. Participation posts do not require a scholarly source/citation (unless you cite someone else’s work). Part of your weekly participation includes viewing the weekly announcement and attesting to watching it in the comments. These announcements are made to ensure you understand everything that is due during the week.

APA Format and Writing Quality

Familiarize yourself with the APA format and practice using it correctly. It is used for most writing assignments for your degree. Visit the Writing Center in the Student Success Center, under the Resources tab in Loud-cloud for APA paper templates, citation examples, tips, etc. Points will be deducted for poor use of APA format or absence of APA format (if required). Cite all sources of information! When in doubt, cite the source. Paraphrasing also requires a citation. I highly recommend using the APA Publication Manual, 6th edition.

Use of Direct Quotes

I discourage over-utilization of direct quotes in DQs and assignments at the Master’s level and deduct points accordingly. As Masters’ level students, it is important that you be able to critically analyze and interpret information from journal articles and other resources. Simply restating someone else’s words does not demonstrate an understanding of the content or critical analysis of the content. It is best to paraphrase content and cite your source.

LopesWrite Policy

For assignments that need to be submitted to Lopes Write, please be sure you have received your report and Similarity Index (SI) percentage BEFORE you do a “final submit” to me. Once you have received your report, please review it. This report will show you grammatical, punctuation, and spelling errors that can easily be fixed. Take the extra few minutes to review instead of getting counted off for these mistakes. Review your similarities. Did you forget to cite something? Did you not paraphrase well enough? Is your paper made up of someone else’s thoughts more than your own? Visit the Writing Center in the Student Success Center, under the Resources tab in Loud-cloud for tips on improving your paper and SI score.

Late Policy

The university’s policy on late assignments is a 10% penalty PER DAY LATE. This also applies to late DQ replies. Please communicate with me if you anticipate having to submit an assignment late. I am happy to be flexible, with advance notice. We may be able to work out an extension based on extenuating circumstances. If you do not communicate with me before submitting an assignment late, the GCU late policy will be in effect. I do not accept assignments that are two or more weeks late unless we have worked out an extension. As per policy, no assignments are accepted after the last day of class. Any assignment submitted after midnight on the last day of class will not be accepted for grading.

Communication

Communication is so very important. There are multiple ways to communicate with me: Questions to Instructor Forum: This is a great place to ask course content or assignment questions. If you have a question, there is a good chance one of your peers does as well. This is a public forum for the class. Individual Forum: This is a private forum to ask me questions or send me messages. This will be checked at least once every 24 hours.

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NURS 6630 Week 2 Agonist to Antagonist Spectrum