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Posted: June 14th, 2023
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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.
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Agonist-to-Antagonist Spectrum of Action of Psychopharmacologic Agents:
Psychopharmacologic agents are drugs that alter brain function, mood, and behavior. They work by interacting with specific receptors in the brain, either mimicking or blocking the action of endogenous neurotransmitters. The agonist-to-antagonist spectrum refers to the range of actions that psychopharmacologic agents can have on these receptors.
An agonist is a drug that binds to a receptor and activates it, producing a response similar to that of the endogenous neurotransmitter. For example, morphine is an agonist of the mu opioid receptor and produces analgesia and euphoria.
An antagonist is a drug that binds to a receptor and blocks its activation by endogenous neurotransmitters. For example, naloxone is an antagonist of the mu opioid receptor and is used to reverse opioid overdose.
Partial agonists are drugs that bind to a receptor and produce a partial response, intermediate between that of an agonist and an antagonist. For example, buprenorphine is a partial agonist of the mu opioid receptor and is used to treat opioid addiction.
Inverse agonists are drugs that bind to a receptor and produce the opposite effect of an agonist, reducing receptor activity below baseline. For example, beta-blockers are inverse agonists of the beta-adrenergic receptor and are used to treat hypertension.
The efficacy of psychopharmacologic treatments can be impacted by the functionality of partial and inverse agonists. Partial agonists can have a ceiling effect, meaning that as the dose increases, the response plateaus and does not continue to increase. Inverse agonists can have a paradoxical effect, meaning that in some cases, they can worsen symptoms instead of improving them.
Sources:
Stahl, S. M. (2017). Stahl’s essential psychopharmacology: neuroscientific basis and practical applications. Cambridge University Press.
Nutt, D. J., & Cowen, P. J. (2020). Psychopharmacology of depression. Handbook of Clinical Neurology, 175, 221-238.
G Protein-Coupled Receptors vs. Ion-Gated Channels:
G protein-coupled receptors (GPCRs) and ion-gated channels are two types of membrane receptors that play important roles in the action of psychopharmacologic agents.
GPCRs are a large family of receptors that are involved in a wide range of physiological processes, including neurotransmission. They are so named because they activate intracellular signaling pathways by interacting with G proteins. When an agonist binds to a GPCR, it induces a conformational change that activates a G protein, leading to downstream signaling events. Many psychopharmacologic agents, such as antipsychotics and antidepressants, target GPCRs.
Ion-gated channels, also known as ligand-gated ion channels, are receptors that allow ions to flow across the cell membrane in response to a neurotransmitter binding to the receptor. They are important for fast synaptic transmission in the brain. When an agonist binds to an ion-gated channel, it causes a conformational change that opens the channel and allows ions to flow. Examples of psychopharmacologic agents that target ion-gated channels include benzodiazepines and barbiturates, which enhance the action of the inhibitory neurotransmitter GABA by binding to its receptor.
While both GPCRs and ion-gated channels are involved in neurotransmission, they differ in their mechanism of action and the speed of their response. GPCRs activate intracellular signaling pathways, which can take seconds to minutes to produce a response. Ion-gated channels allow ions to flow across the cell membrane, producing a rapid response within milliseconds.
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