[ANSWERED 2023] Explain the agonist-to-antagonist spectrum of action of psychopharmacologic agents, including

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Explain the agonist-to-antagonist spectrum of action of psychopharmacologic agents, including how partial and inverse agonist functionality

For this Discussion, review the Learning Resources and reflect on the concepts of foundational neuroscience as they might apply to your role as the psychiatric mental health nurse practitioner in prescribing medications for patients.

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.
Compare and contrast the actions of g couple proteins and ion gated channels.
Explain how the role of epigenetics may contribute to pharmacologic action.
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.

******* REQUIRED READINGS/RESOURCES

-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.

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Expert Answer

Neurotransmitters and Receptor Theory

Agonist-To-Antagonist Spectrum of Action of Psychopharmacologic Agents

An agonist is a chemical that fixes a receptor and activates it to yield a biological response. However, an antagonist is a group of institutions, characters, or concepts representing or stands in opposition and must be contended by the protagonist (Wager et al., 2017). In other words, the antagonist is an individual or group of persons opposing a protagonist.

The agonist and antagonist’s difference is that agonist causes an action while antagonist opposes an action of the former. Inverse agonist produces a biological response opposite from that of agonist. In pharmacology, partial agonists are medications that fit themselves on a given receptor and activate them. Their efficacy is partial compared to full agonists (Camprodon & Roffman, 2016).

Partial agonists can be used to activate the receptors so that they can respond to medications. Inverse agonists can be used to induce a pharmacological response of the agonist.

Actions of G-Couple Proteins and Ion Gated Channels

G couple proteins receptors, also known as &TM receptors or serpentine receptors, are part of evolutionarily-related proteins, the largest and diverse class of membrane receptors found in the eukaryotes (Meng, Kang & Zhou, 2018). The g couple proteins function as an inbox for messages in peptides, light energy, sugars, lipids, and proteins.

On the other hand, ion gated channels are a group of proteins known as transmembrane ion-channel, which open to permit ions, such as sodium, calcium, potassium, or chloride, to pass through the cell membrane in response to the action of a ligand. The key difference between the two elements is that G protein-coupled receptors have a wide variety of functions, including transmitting signals from many stimuli outside the cell into the cell.

However, ion gated channels are pores in the cell membrane that allow the passage of in and out of the cell. The similarity is that these two elements are fundamental in pharmacology in that they determine how humans respond to certain medications.

Impact of Epigenetics Role in Pharmacologic Action

Epigenetics is the study of how environment and behavior can cause transitions that impact the functions of one’s genes. Unlike genetics, epigenetics changes cannot alter the DNA sequence and are reversible but can change how the body sees the DNA sequence. The role of epigenetics may have a huge contribution to pharmacologic action, especially pharmacokinetics or drug metabolism.

The changes in the expression of enzymes involved in drug metabolism can impact the pharmacokinetic process. For instance, Mestre-Fos et al. (2018) report that minRNAs can help medication behavior by changing the drug’s distribution of metabolism.

Impact of the Information in Drug Prescription

Epigenetic alterations are fundamental in both disease and normal state of a patient. The alterations include phosphorylation, acetylation, methylation, and ubiquitylation of the histone chromatin and the DNA (Mestre-Fos et al., 2018). Few patients respond to standard therapies because of various gene alterations in their cells.

Therefore, when prescribing medications, a caregiver should evaluate the patient’s epigenetics. In mental health, epigenetics can determine the side effects of medications and identify new pharmaceutical targets for treatment (Camprodon & Roffman, 2016). For instance, a drug such as aripiprazole can have an epigenetic effect on a patient’s gene. Hence, when prescribing it, psychiatric mental health should be aware of its action.

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.

Meng, X. Y., Kang, S. G., & Zhou, R. (2018). Molecular mechanism of phosphoinositides’ specificity for the inwardly rectifying potassium channel Kir2. 2. Chemical science, 9(44), 8352-8362. DOI: 10.1039/C8SC01284A

Mestre-Fos, S., Penev, P. I., Suttapitugsakul, S., Ito, C., Petrov, A. S., Wartell, R. M., … & Williams, L. D. (2018). Dynamic G-quadruplexes on the surface of the human ribosome. bioRxiv, 435594. doi: 10.1016/j.jmb.2019.03.010

Wager, T. T., Chappie, T., Horton, D., Chandrasekaran, R. Y., Samas, B., Dunn-Sims, E. R., … & Schmidt, C. J. (2017). Dopamine D3/D2 receptor antagonist PF-4363467 attenuates opioid drug-seeking behavior without concomitant D2 side effects. ACS chemical neuroscience, 8(1), 165-177. https://doi.org/10.1021/acschemneuro.6b00297

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Alternative Answer

Agonist-Antagonist Spectrum of Action of Psychopharmacologic Agents

Foundational neuroscience is one of the crucial backgrounds that mental health practitioners should have. Knowledge in this field allows to increase the understanding of the pathophysiology of mental conditions as well as how the medications affect the central nervous system (Saleh et al., 2016).

An agonist is a chemical or biomolecule which interacts with a cell receptor to produce relevant reaction while an antagonist is substance which reduces or opposes the action of an agonist (Saleh et al., 2016). A drug that has the agonist characteristics often ties to the site of reception and causes the required response. On the other hand, antagonists bind with the receptors and limit such action by reducing the number of sites available for the agonist to bind.

Comparison of Actions of G Couple Proteins and Ion-gated Channels

Due to their charge in them, it is impossible for ions to naturally penetrate membranes. The selective control of ions out of and into neurons is made possible with the decoration of membranes with ion channels (Zamponi, Han, & Waxman, 2016). Binding of a neurotransmitter to a receptor results in the conformational changes that bring about opening of the ion channels.

Ligand gated ion channels are those that are linked to the receptors to allow this opening and closing of the channels (Zamponi, Han, & Waxman, 2016). When patients take up drugs, these drugs often bind with the receptor and ion channel complexes t all the necessary modifications of the ion channels to take place. In a similar way, G-protein receptors activate intracellular signaling pathways to allow for the modulation of the ion channel activities (Zamponi, Han, & Waxman, 2016). G Couple Proteins are known to be the most versatile and largest protein families in the genome of all mammals.

A major difference between the ion-gated channels and the G Couple proteins is the fact that the ion channels work by inducing rapid modifications in the membrane potentials so as to bring about the necessary action potentials, while the G Couple Proteins activate hosts of the diverse signaling cascades so as to produce the necessary action (Stahl, 2013).

The G Couple proteins have the potential to regulate other cellular functions that help in the release of the hormones (Stahl, 2013). On the other hand, ion-gated channels, after generating the required action potentials initiate the process of exocytosis and eventually the release of hormones (Stahl, 2013).

Role of Epigenetics in Pharmacologic Action

Epigenetics is a system of gene regulation in which the expression of genes in an organism is successfully repressed without having to alter its genetic code. This alters the gene expression while the genome sequence remains intact (Younus & Reddy, 2017). In pharmacology, epigenetics can be used to alter the body of patients to make them compatible with rare but effective drugs in the treatment of their conditions (Younus & Reddy, 2017).

How this Information may Impact my Prescriptions to Clients

Among the primary ways in which this information may impact my prescriptions to clients is that I will have higher levels of confidence when dictating various instructions to the patients I have. Specifically, for the patients who have neurology defects, I will be sure to give them relevant background knowledge about the drugs, which may increase their levels of compliance. Also, in case of a condition in which epigenetics could increase the chances of compatibility of the client with various drugs, I will be sure to recommend them to the necessary procedures of epigenetics so as to improve the outcomes of the care process.

References

Saleh, N., Saladino, G., Gervasio, F. L., Haensele, E., Banting, L., Whitley, D. C., … & Clark, T. (2016). A three‐site mechanism for agonist/antagonist selective binding to vasopressin receptors. Angewandte Chemie, 128(28), 8140-8144.

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

Younus, I., & Reddy, D. S. (2017). Epigenetic interventions for epileptogenesis: a new frontier for curing epilepsy. Pharmacology & therapeutics, 177, 108-122.

Zamponi, G. W., Han, C., & Waxman, S. G. (2016). Voltage-Gated Ion Channels as Molecular Targets for Pain. In Translational Neuroscience (pp. 415-436). Springer, Boston, MA.

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Agonist and antagonist drugs example

Agonist drugs and antagonist drugs are two types of drugs that interact with specific receptors in the body to produce a certain effect. An agonist drug activates a receptor and produces a biological response, while an antagonist drug blocks a receptor and prevents it from being activated. Here are some examples of agonist and antagonist drugs: Agonist drugs:

Morphine - a painkiller that works by activating opioid receptors in the brain and spinal cord.
Epinephrine - a hormone and neurotransmitter that activates adrenergic receptors to increase heart rate and blood pressure.
Nicotine - a chemical found in tobacco products that activates nicotinic acetylcholine receptors in the brain, producing feelings of pleasure and alertness.
Albuterol - a bronchodilator drug that activates beta-2 adrenergic receptors in the lungs, helping to open up airways and ease breathing.
Insulin - a hormone that activates insulin receptors in cells, promoting the uptake of glucose from the bloodstream to be used for energy.

Antagonist drugs:

Naloxone - an opioid antagonist drug that blocks the effects of opioids by binding to opioid receptors and preventing their activation.
Propranolol - a beta-blocker drug that blocks beta-adrenergic receptors, reducing heart rate and blood pressure.
Flumazenil - a benzodiazepine antagonist drug that blocks the effects of benzodiazepines by binding to their receptors in the brain.
Cimetidine - a histamine H2 receptor antagonist drug that reduces stomach acid production by blocking H2 receptors in the stomach lining.
Naltrexone - an opioid and alcohol antagonist drug that blocks the effects of opioids and alcohol by binding to their respective receptors in the brain.

These are just a few examples of agonist and antagonist drugs, and there are many more examples of each type of drug.

Inverse agonist example

An inverse agonist is a type of drug that binds to the same receptor as an agonist but produces the opposite effect by reducing the basal activity of the receptor. Here is an example of an inverse agonist:

Diphenhydramine (also known as Benadryl) - Diphenhydramine is an antihistamine drug that is used to treat allergies, hay fever, and other conditions caused by histamine release. Diphenhydramine is also a potent inverse agonist at the H1 histamine receptor, which reduces the basal activity of the receptor, leading to sedation and reduced wakefulness.

Another example of an inverse agonist is Rimonabant, which was developed as an anti-obesity drug but has been withdrawn from the market due to side effects. Inverse agonists have an opposite effect to agonists, which activate the receptor and increase its activity. This makes inverse agonists potentially useful for treating diseases caused by overactive receptors or excess receptor signaling.

Inverse agonist vs antagonist

An inverse agonist and an antagonist are both types of drugs that interact with receptors in the body, but they have different effects on receptor activity. An antagonist is a drug that binds to a receptor and blocks its activation by preventing other molecules, such as agonists or natural ligands, from binding to the receptor. Antagonists do not have any intrinsic activity on the receptor and simply block the activity of other molecules that would normally activate the receptor. An inverse agonist, on the other hand, is a drug that binds to the same receptor as an agonist but produces the opposite effect by reducing the basal activity of the receptor. Inverse agonists have an opposite effect to agonists, which activate the receptor and increase its activity. So, the key difference between an inverse agonist and an antagonist is that an inverse agonist reduces the basal activity of a receptor, whereas an antagonist simply blocks the activity of other molecules that would normally activate the receptor. Additionally, an inverse agonist can have an opposite effect to a natural ligand that binds to the receptor, while an antagonist simply prevents the natural ligand from binding. In terms of therapeutic applications, antagonists are typically used to block the effects of certain hormones or neurotransmitters, while inverse agonists are used to reduce the activity of overactive receptors.

Partial agonist

A partial agonist is a type of drug that binds to a receptor and produces a weaker effect than a full agonist, even when it is fully bound to the receptor. Partial agonists have an intermediate level of intrinsic activity compared to full agonists, which produce the maximum effect that can be achieved by a receptor. Partial agonists can produce different effects depending on the level of receptor activation, and their effects can vary depending on the level of endogenous agonist present. In some cases, partial agonists can behave like full agonists when endogenous agonist levels are low, but produce weaker effects when endogenous agonist levels are high. Here are a few examples of partial agonists:

Buprenorphine - Buprenorphine is a partial agonist at the mu-opioid receptor and is used to treat opioid addiction. Buprenorphine produces less euphoria and respiratory depression than full agonists like heroin or morphine.
Aripiprazole - Aripiprazole is a partial agonist at the dopamine D2 receptor and is used to treat schizophrenia and bipolar disorder. Aripiprazole produces weaker dopamine receptor activation than full agonists like cocaine or amphetamine.
Buspirone - Buspirone is a partial agonist at the serotonin 5-HT1A receptor and is used to treat anxiety. Buspirone produces less sedation and fewer side effects than full agonists like benzodiazepines.

Partial agonists can be useful in treating conditions where full agonists can produce unwanted side effects or have a high potential for abuse. By producing weaker effects than full agonists, partial agonists can provide therapeutic benefits with fewer risks.

Agonist and antagonist neurotransmitters

Agonist and antagonist drugs can act on different types of neurotransmitters in the brain to produce different effects. Here are some examples of agonist and antagonist neurotransmitters: Agonist neurotransmitters:

Dopamine - Dopamine is a neurotransmitter that is involved in reward and motivation, as well as movement and coordination. Drugs that increase dopamine activity, such as amphetamines or cocaine, act as dopamine agonists and can produce feelings of euphoria and increased energy.
Serotonin - Serotonin is a neurotransmitter that is involved in regulating mood, appetite, and sleep. Drugs that increase serotonin activity, such as selective serotonin reuptake inhibitors (SSRIs), act as serotonin agonists and are used to treat depression, anxiety, and other mood disorders.

Antagonist neurotransmitters:

GABA - GABA is a neurotransmitter that is involved in regulating anxiety and sleep. Drugs that block GABA receptors, such as benzodiazepines, act as GABA antagonists and can produce feelings of relaxation and sedation.
Acetylcholine - Acetylcholine is a neurotransmitter that is involved in muscle movement, attention, and memory. Drugs that block acetylcholine receptors, such as anticholinergic drugs, act as acetylcholine antagonists and can produce side effects like dry mouth, blurred vision, and cognitive impairment.
Norepinephrine - Norepinephrine is a neurotransmitter that is involved in the "fight or flight" response, as well as attention and arousal. Drugs that block norepinephrine receptors, such as beta blockers, act as norepinephrine antagonists and can be used to treat high blood pressure, anxiety, and other conditions.