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Discussion post reply 1
The agonist-to-antagonist spectrum of action of psychopharmacologic agents.
According to Stahl (2013), the agonist spectrum goes from full agonist to partial agonist, by way of antagonist to inverse agonist. Agonist is a natural neurotransmitter or drug that binds to receptor sites to obtain the desired effect. Some drugs can be partial agonists or stabilizers because they may function to a lesser degree than the natural chemical. Antagonists are drugs that bind to the receptor sites in the presence of an agonist to block the desired effect therefore they cannot function without an agonist. An inverse agonist also works to block the desired stimulating effect from the agonist and can also decrease activity below the baseline without the presence of an agonist.
Compare and contrast the actions of g couple proteins and ion-gated channels.
As stated by Lakna, (2022) Ion gated channels are ion channel proteins that allow the passage of ions such as chloride, calcium, potassium, and sodium upon binding with a neurotransmitter thus making it ionotropic, whereas G-coupled protein channels activate the messenger G protein to identify a great variety of ligands to open or close ion channels thus making it metabotropic. Ligand-gated ion channels couple with ion channels while G-protein coupled receptors do not.
In comparison, ligand-gated ion channels and G-protein coupled receptors are both postsynaptic receptors on the postsynaptic neurons. They liaise with ion channels to alter the cell membrane of the post-synaptic neuron through depolarization and hyperpolarization (Lakna, 2022).
Explain how the role of epigenetics may contribute to pharmacologic action.
Epigenetics is a process where genes are expressed and silenced by chromatin remodeling (Stahl 2013). This can be achieved by various chemical processes that are regulated by drugs, neurotransmitters, and environment. One such process is methylation. Methylation of histones and DNA can silence genes, while the reverse action demethylation of the same can activate the genes. When this process is affected by drugs, it controls whether genes are silenced or expressed. For example, an epigenetic change that turns off the gene that suppresses tumors can lead to uncontrolled cell multiplication (Rettner, 2013). According to Kanherkar, Bhatia-Day & Csoka (2014), it is believed that some drugs used to cure diseases may cause epigenetic changes that may be exhibited as prolonged side effects. Several screening protocols are available to identify drugs with positive and negative epigenetic effects.
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 nurse practitioner must be aware of the medication’s action.
With the knowledge of epigenetics and that it can be hereditary, I would want to obtain a thorough history of the patient including, family/genetics, medical, medication, and drug allergies before prescribing any medication. Csoka & Syzyf, (2009) states that it is believed that drug-induced tardive dyskinesia is epigenetic. In this case, if A PMHNP is treating a psychotic patient who has a history or a family history of Parkinson’s’ disease, should be cautious with the use of neuroleptic drugs as these drugs can induce the disease or worsen it.
Discussion post # 2
Berg & Clark (2018), explain that “Agonists are drugs with both affinity (they bind to the target receptor) and intrinsic efficacy (they change receptor activity to produce a response). Antagonists have affinity but zero intrinsic efficacy; therefore they bind to the target receptor but do not produce a response.” Inverse agonists decrease constitutive activity of a receptor and generate a contrary effect of an agonist. Studies suggest the importance of considering both inverse agonism and functional selectivity when drugs are applied as medicines or as research tools.
The g couple proteins and ion gated channels respond to ligand by shape transformation. Both functions in mediating ion channels to depolarize or hyperpolarize the plasma membrane of the postsynaptic neuron (Lakna, 2022). The difference between the two is basically in their activation of ion channel. Channel receptors open a gate, giving way for influx (or exit) of ions; G linked protein on the other hand, reverse their cytosol part changes configuration, binds G protein and activates it utilizing energy from GTP. Ultimately, ligand-gated ion channels and G-protein coupled receptors are two types of transmembrane proteins that make up postsynaptic ion channels. In addition, Lakna (2022) simply states that “Ligand-gated ion channels involve the direct opening of ion channels with the binding of a neurotransmitter, while G-protein coupled receptors are involved in the indirect binding of ion channels with metabolic activation of G-protein”.
Epigenetics provide knowledge of how disease originates and inherited as well as its response to therapeutic intervention. The role of epigenetics may contribute to pharmacologic actions in several ways, for instance in pain control. studies has proven that ” From prehistoric use of plants as medicines, such as aspirin-like compounds from the bark of willow trees or other salicylate-rich plants in ancient Egyptian and Greek times, man has used drugs to control our physiology” (Stefanska, & MacEwan,2015). Meanwhile, study further state that “Pharmacological intervention with SAM restores the epigenetic control of the β-secretase gene by hypermethylation and silencing followed by a decrease in formation of amyloid plaques”. Lately, Researchers are making massive improvement with the use of epigenetics not only in cancer therapy, but also in neurological disorders and autoimmune diseases.
It is known that several neurological disorders, for instance Alzheimer disease has been associated with epigenetics mutations; as mental health nurse practitioners, we should acknowledge and put this fact into consideration, while prescribing medication for better, safe, and effective outcome.