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Agonist-to-Antagonist Spectrum

The agonist-to-antagonist spectrum of action refers to  the action  that is taken by a neurotransmitter to produces a  conformational change  (Stahl, 2013).  The spectrum starts with the  agonist action, which,  with the help of a second-messenger, can turn on  the full potential of  change (Stahl, 2013). Full agonists can be natural  transmitters used to  produce change.  An antagonist blocks the  conformational change of the  potential of the transmitter for binding  with the intended agonist  (Stahl, 2013).  The role of the antagonist is  to keep the receptors in a  baseline state in order to reverse what the  agonist has done (Stahl,  2013). This is the opposite end of the spectrum  and seeks to block  agonists.  In the middle, some partial agonists  mimic its agonist  partner to a lesser degree, and inverse agonists stop  all activity from  occurring on the receptor (Stahl, 2013).  The  conformational change is  needed for a receptor to open to the action of  drugs, particularly,  psychopharmaceutical medications in this case.

G couple proteins and Ion gated channels

G couple proteins are used at the binding site of a  neurotransmitter  to act as a conduit for enzymes (Stahl, 2013). Whereas,  ion gated  channels exist as targets to regulate chemical  neurotransmitters  (Stahl, 2013).  Ion gated channels consist of channels  and receptors  that can only be opened by the neurotransmitters.   Conversely, G couple  proteins attach to neurotransmitters and conform to  enzymes to serve  as a channel for a second messenger (Stahl, 2013).   Most psychotropic  medications aim for the ion gated channels, which open  through chemical  neurotransmission and initiate the signal transduction  cascade (Stahl,  2013).  The cascade results in faster uptake of  psychotropic  medications into the system.

The Role of Epigenetics

According to DeSocio (2016), epigenetics is the study  of how genomes  that undergo changes with certain molecular compounds and   environmental changes can leave the essential DNA unchanged.  It is a   modification of gene expression that is independent of the DNA  (DeSocio,  2016).  DNA is the code that determines much of who we are.   Changes in  that code can be seen as a result of heredity, the  environment, or  neurotransmission (Stahl, 2013).  These alterations  affect individuals  at a physical, emotional, and psychological level.   Stress and adversity  play a significant role in epigenetics by changing  the genomes, which  in turn leads to changes in a person’s DNA (Park et  al., 2019).  These  alterations influence psychological issues related  to many individuals.   It is essential to know how to combat these  changes when determining a  plan of care for clients.

Implications of Findings to Prescribing

As nurse practitioners, it is essential to have an  extensive  understanding of how the above processes affect the way we  prescribe  medications to clients.  It is also essential to take into   consideration how the environment impacts maintaining optimal health  and  healing (DeSocio, 2016).  Knowing the mechanisms of action for   medications that we are prescribing is vital to providing competent   care.  For example, a patient with a generalized anxiety disorder (GAD)   is prescribed Venlafaxine.  The PMHNP needs to understand that the   Venlafaxine works by boosting the serotonin, norepinephrine, and   dopamine neurotransmitters (Stahl, 2014).  This action blocks serotonin   reuptake, norepinephrine reuptake, and the dopamine reuptake (Stahl,   2014).  Each of these actions then increases these neurotransmissions  in  the brain providing therapeutic results. 

                                          References

DeSocio, J.E. (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

Park, C.,  Rosenblat, J.D., Brietzke, E.,  Pan, Z., Lee, Y., Cao, B.,  Zuckerman, H., Kalantarova, A., McIntyre,  R.S. (2019). Stress,  epigenetics, and depression: A systematic review. Neuroscience and Biobehavioral Reviews, 102, 139-152. https://doi.org/10.1016/j.neubiorev.2019.04.010

Stahl, S.M. (2014). The prescriber’s guide (5th ed.). New York, NY: Cambridge University Press.

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