Nicole Washington

    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.

Neurotransmitters and some drugs that stimulate receptors are called agonists. Agonists stimulate receptors to their fullest signal transduction. Drugs that act as agonists are useful in patients who lack or are deficient in agonist neurotransmitters. In situations where the actions of a full agonist or partial agonists are undesirable, an antagonist is required to revert the receptor back to the state where no agonist exists, back to neutral. Partial agonists act as they sound, and produce a conformational change of a receptor that is halfway between the changes of a full agonist and the baseline conformation of that receptor. An antagonist can also reverse the effects of inverse agonists to the receptors baseline. An inverse agonist acts to change the conformation of a receptor to completely inactivate it and remove the baseline constitutive activity.

Compare and contrast the actions of g coupled proteins and ion gated channels.

Both G protein coupled receptors and Ion gated channels are a form of signal transduction cascades in the brain. They are both triggered by neurotransmitters, and many of the psychotropic drugs used today affect one of these two cascades. They both perform when an extracellular first messenger passes a message to an intracellular second messenger. However, G protein’s second messenger is a chemical, such as adenosine monophosphate, while the ion channel second messenger can be an ion, such as calcium. There are two classes of ion channels, Ligand gated and voltage sensitive ion channels. The ligand gated ion channels act similar to g protein receptors because they use the agonist spectrum. Voltage sensitive ion channels are opened and closed based on the voltage charge across the membrane.

Explain how the role of epigenetics may contribute to pharmacologic action.

Epigenetics determines if inherited genes are expressed or not expressed into proteins that make up the story of any one person. The mechanism of epigenetics turns genes on or off by modifying chromatin. These modifications are regulated by neurotransmitters, drugs and the environment. So drugs introduced to patients can affect a person’s epigenetics.

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.

Understanding the way medications will affect patients based on their genetic makeup, their current medications, the condition being treated, what causes the imbalance, is all important when prescribing medications. For example imipramine, a tricyclic antidepressant, inhibits the reuptake of serotonin and norepinephrine, elevating these neurotransmitters in the brain. It is important to understand if this is the cause of the patients depression before prescribing this medication because if incorrectly prescribed it could alter the patients epigenetic mechanisms in an inverse way (Boks, et al. 2012).

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Sample Answer

 

 

 

The agonist-to-antagonist spectrum of action of psychopharmacologic agents refers to the range of effects that these agents can have on neurotransmitter receptors.

An agonist is a drug that binds to a receptor and activates it, causing a biological response. A partial agonist is a drug that binds to a receptor and activates it, but to a lesser extent than a full agonist. An antagonist is a drug that binds to a receptor and blocks its activation.

Full Answer Section

 

 

The efficacy of psychopharmacologic treatments can be affected by the agonist-to-antagonist spectrum of action of the drugs used in these treatments. For example, a full agonist may be more effective than a partial agonist in treating a disorder that is caused by a deficiency of the neurotransmitter that the drug targets. However, a full agonist may also have more side effects than a partial agonist.

Inverse agonists are a type of drug that binds to a receptor and inhibits its activation. Inverse agonists can be used to treat disorders that are caused by an excess of the neurotransmitter that the drug targets. For example, inverse agonists are used to treat schizophrenia.

The agonist-to-antagonist spectrum of action is a complex topic, and the effects of different drugs on neurotransmitter receptors can vary depending on the drug, the receptor, and the individual patient.

Here are some examples of how the agonist-to-antagonist spectrum of action can affect the efficacy of psychopharmacologic treatments:

  • Bupropion: Bupropion is a partial agonist of the dopamine receptor. It is used to treat depression and attention deficit hyperactivity disorder (ADHD). Bupropion is thought to be more effective than other antidepressants in treating depression that is caused by a deficiency of dopamine. However, bupropion also has a lower risk of side effects than other antidepressants.
  • Naltrexone: Naltrexone is an antagonist of the opioid receptor. It is used to treat opioid addiction and alcoholism. Naltrexone blocks the effects of opioids, which can help to reduce cravings and prevent relapse.
  • Risperidone: Risperidone is an inverse agonist of the dopamine receptor. It is used to treat schizophrenia and other psychotic disorders. Risperidone works by reducing the activity of dopamine in the brain, which can help to improve symptoms such as hallucinations and delusions.

The agonist-to-antagonist spectrum of action is an important consideration when choosing psychopharmacologic treatments. By understanding how different drugs affect neurotransmitter receptors, doctors can select the drugs that are most likely to be effective and have the fewest side effects for each individual patient.

 

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