Psychopharmacology Scavenger Hunt Concept Map

“scavenger” the literature as you research the agonist spectrum and key neurotransmitters and pathways targeted in psychopharmacology. You will have the opportunity to apply your knowledge as you create a Concept Map exploring each of the agonist spectrum listed below. Support your answers with evidence-based, peer-reviewed scholarly literature. APA style format title page, citations, and references will apply.

To prepare for this Assignment:
• Review the Learning Resources assigned this week.
• Review the Concept Map resources.
• Explore the listed agonist spectrum and consider the action and receptor of each:
o Agonist
o Partial agonist
o Antagonist
o Inverse agonist

• Describe the different characteristics of the four agonists and how each mediates distinct biological activities. Include proposed mechanisms and the receptor it is targeting.
• Identify how the P450 enzyme system plays a role in the body’s absorption, distribution, and clearance of medication.
• Scavenge the literature after describing each agonist on the spectrum for research that is based on the medications in the table below.
• Apply the medications to the appropriate agonist on the agonist spectrum in your Concept Map.
Medications
Oxycodone
Brexpiprazole
Haloperidol
Naloxone
Aripiprazole
Amphetamine
Risperidone
Pimavanserin

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Sample Answer

 

 

 

 

Understanding the Agonist Spectrum

Before diving into the medications, we need to clarify the agonist spectrum:

  • Agonist:
    • A substance that binds to a receptor and activates it, producing a biological response.  
    • It mimics the action of an endogenous ligand (e.g., neurotransmitter).  
    • Mechanism: Binds to the receptor’s active site, inducing a conformational change that initiates a signaling cascade.  
    • Example: A full agonist produces the maximum possible response.  
  • Partial Agonist:
    • A substance that binds to a receptor and activates it, but produces a submaximal response.  
    • It has affinity for the receptor but lower efficacy than a full agonist.  
    • Mechanism: Binds to the receptor, but the conformational change it induces is less effective at initiating signaling.  
    • It can act as an antagonist in the presence of a full agonist   

Full Answer Section

 

 

 

 

  • Antagonist:
    • A substance that binds to a receptor and blocks the action of an agonist.
    • It has affinity for the receptor but no efficacy.
    • Mechanism: Binds to the receptor, preventing the agonist from binding and activating it.
  • Inverse Agonist:
    • A substance that binds to a receptor and produces the opposite effect of an agonist.
    • It binds to the same receptor as an agonist but stabilizes a different conformation, leading to an opposite biological response.
    • This indicates that the receptor possesses a baseline of activity, that an inverse agonist acts to reduce.  

P450 Enzyme System

  • The cytochrome P450 (CYP450) enzyme system is a family of enzymes primarily located in the liver.  
  • It plays a crucial role in the metabolism of many drugs.
    • Absorption: some P450 enzymes can modify drugs before they are absorbed into the body.
    • Distribution: by modifiying the drugs chemical makeup, P450 enzymes effect the amount of drug that makes it to target tissues.
    • Clearance: It metabolizes drugs into inactive metabolites, facilitating their elimination from the body.
  • Genetic variations in CYP450 enzymes can affect drug metabolism, leading to variations in drug response.  
  • Drug interactions can occur when multiple drugs compete for the same CYP450 enzyme, potentially affecting their concentrations.  

Concept Map and Medication Placement

Now, let’s place the medications on the agonist spectrum:

  • Agonist:
    • Oxycodone: A full opioid agonist that binds to opioid receptors (primarily mu-opioid receptors) in the central nervous system, producing analgesia.  
    • Amphetamine: Acts as a potent agonist at certain receptors, increasing the amount of dopamine and norepinephrine in the synapses.  
  • Partial Agonist:
    • Brexpiprazole: Acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors, while also acting as an antagonist at serotonin 5-HT2A receptors.  
    • Aripiprazole: Similar to Brexpiprazole, it acts as a partial agonist at dopamine D2 and serotonin 5-HT1A receptors and an antagonist at serotonin 5-HT2A receptors.
  • Antagonist:
    • Naloxone: An opioid antagonist that binds to opioid receptors and blocks the effects of opioid agonists.  
    • Haloperidol: A typical antipsychotic that primarily acts as a dopamine D2 receptor antagonist.  
    • Risperidone: An atypical antipsychotic that acts as an antagonist at dopamine D2 and serotonin 5-HT2A receptors.  
  • Inverse Agonist:
    • Pimavanserin: An inverse agonist at the serotonin 5-HT2A receptor. This action is thought to be responsible for its antipsychotic effects.  

Key Neurotransmitters and Pathways

  • Dopamine: Involved in reward, motivation, movement, and cognition.
  • Serotonin: Involved in mood, sleep, appetite, and cognition.  
  • Opioid Receptors: Involved in pain modulation, reward, and euphoria.  

Creating the Concept Map

Your concept map should visually represent the following:

  1. The four categories of the agonist spectrum (agonist, partial agonist, antagonist, inverse agonist).
  2. For each category:
    • A description of its mechanism of action.
    • The receptor(s) it targets.
    • The medications that fall within that category.
    • The primary neurotransmitter impacted.
  3. Include a section explaining the role of the P450 enzyme system.
  4. Supporting scholarly sources for each medication action.

Important Notes:

  • Always refer to reputable sources such as PubMed, PsycINFO, and reputable pharmacology textbooks for the most accurate and up-to-date information.
  • Pay close attention to the specific receptors targeted by each medication, as this is crucial for understanding its mechanism of action.

By meticulously following these steps and “scavenging” the relevant literature, you will develop a comprehensive and informative concept map.

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