PSYCHOPHARMACOLOGY SCAVENGER HUNT CONCEPT MAP ANSWERS

PSYCHOPHARMACOLOGY SCAVENGER HUNT CONCEPT MAP ANSWERS

PSYCHOPHARMACOLOGY SCAVENGER HUNT CONCEPT MAP ANSWERS

Agonists

Definition:
Fully activates a receptor, producing a maximal biological response.

Pharmacological Agents:
Oxycodone, Amphetamine

Mode of Action:

Oxycodone:
Binds to µ-opioid receptors (MOR), inhibiting pain signaling.

Amphetamine: Reverses dopamine transporter (DAT), increasing dopamine release.

Role of Cytochrome Enzymes:

Oxycodone: Metabolized by CYP3A4, CYP2D6, affecting drug clearance.

Amphetamine: Primarily metabolized by CYP2D6, affecting duration of action.

Therapeutic Uses

Oxycodone: Pain management.

Amphetamine: ADHD, narcolepsy treatment.

Expected Side Effects:

Oxycodone: Respiratory depression, addiction, constipation.

Amphetamine: Insomnia, hypertension, tachycardia (Rosenthal & Burchum, 2021).

 

Partial Agonist

Definition:
Binds to a receptor but only partially activates it, leading to a submaximal response.

Pharmacological Agents:
Brexpiprazole, Aripiprazole

Mode of Action:

Brexpiprazole & Aripiprazole: Partial D2 dopamine receptor agonists, balancing dopamine activity; also act on 5-HT1A (serotonin) receptors.

Role of Cytochrome Enzymes:

Metabolized primarily by CYP3A4 & CYP2D6, affecting plasma levels and drug efficacy (Siwek et al., 2023)..

Therapeutic Uses

Schizophrenia, bipolar disorder, adjunct in major depressive disorder (MDD).

Expected Side Effects:

Weight gain, akathisia, sedation, gastrointestinal issues (Siwek et al., 2023).

 

Antagonist

Definition:
Blocks receptor activation without stimulating a biological response.

Pharmacological Agents:
Haloperidol, Risperidone

Mode of Action:

Haloperidol: Blocks dopamine D2 receptors, reducing dopaminergic activity.

Risperidone: Blocks dopamine D2 and serotonin 5-HT2A receptors, reducing psychotic symptoms.

Role of Cytochrome Enzymes:

Haloperidol: Metabolized by CYP3A4 & CYP2D6, influencing drug clearance.

Risperidone: Primarily metabolized by CYP2D6, with some CYP3A4 involvement.

Therapeutic Uses

Haloperidol: Schizophrenia, Tourette’s syndrome, acute psychosis.

Risperidone: Schizophrenia, bipolar disorder, autism-related irritability.

Expected Side Effects:

Extrapyramidal symptoms (EPS), sedation, weight gain, metabolic changes (Rosenthal & Burchum, 2021).

 

Inverse Agonist

Definition:
Binds to a receptor and induces an opposite effect by reducing baseline receptor activity.

Pharmacological Agents: Naloxone, Pimavanserin

Mode of Action:

Naloxone: Inverse agonist at µ-opioid receptors (MOR), reversing opioid effects.

Pimavanserin: Inverse agonist at serotonin 5-HT2A receptors, modulating psychotic symptoms in Parkinson’s disease (Rosenthal & Burchum, 2021).

Role of Cytochrome Enzymes:

Naloxone: Metabolized by CYP3A4 & CYP2D6, with rapid hepatic clearance.

Pimavanserin: Metabolized by CYP3A4, affecting bioavailability.

Therapeutic Uses:

Naloxone: Opioid overdose reversal.

Pimavanserin: Parkinson’s disease psychosis.

Expected Side Effects:

Naloxone: Withdrawal symptoms (nausea, sweating, agitation).

Pimavanserin: QT prolongation, confusion, peripheral edema (Rosenthal & Burchum, 2021)

 

PSYCHOPHARMACOLOGY SCAVENGER HUNT CONCEPT MAP ANSWERS

Agonist (Oxycodone, Amphetamine)

Agonists fully activate their target receptors to the maximal biological effect. The µ-opioid receptor agonist oxycodone is a drug for the treatment of moderate-to-severe pain, but its use may result in respiratory depression and dependence (Rosenthal & Burchum, 2021). Oxycodone is metabolized in part by the CYP3A4 and CYP2D6 enzymes, which can affect its plasma concentration and analgesic efficacy (Barrett et al., 2023). Amphetamine, a dopamine transporter (DAT) agonist, increases synaptic dopamine levels and, as a result, has a positive effect on focus in ADHD patients. The rest is mainly by CYP2D6, hence duration and individual response. Hypertension, tachycardia, and insomnia are adverse effects.

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Partial Agonist (Brexpiprazole, Aripiprazole)

Partial agonists affect a submaximal receptor response by helping to balance neurotransmitter activity. Brexpiprazole and aripiprazole partially stimulate dopamine D2 and serotonin 5HT1A receptors, leading to a decrease in psychotic symptoms with decreased side effects involving dopamine blockade (Siwek et al., 2023). The bioavailability and drug interactions of both drugs are, in part, affected by their metabolism by CYP3A4 and CYP2D6 (Rosenthal & Burchum, 2021). They are effective in schizophrenia and major depressive disorder (MDD) while having fewer extrapyramidal symptoms, according to studies. They can cause akathisia, weight gain, and sedation; however. Part of their activity regulates dopamine flux fluctuations, thereby making treatment more tolerable.

 

Antagonist (Haloperidol, Risperidone)

They prevent neurotransmitters from having effects by blocking receptor activation. The dopamine D2 antagonist, haloperidol, is widely used in schizophrenia and acute psychosis but is associated with a high risk of extrapyramidal symptoms (EPS) (Sampogna et al., 2023). D2 and serotonin 5-HT2A antagonist Risperidone, with a lower risk of EPS, is used to treat schizophrenia and bipolar disorder and has the potential for weight gain and metabolic disturbances (Rosenthal & Burchum, 2021). Drug clearance and interaction profile with both drugs are dependent on CYP2D6 metabolism. They have antagonistic properties which can effectively reduce hallucinations, delusions and agitation.

Inverse Agonist (Naloxone, Pimavanserin)

Unlike other agonists, inverse agonists can decrease baseline receptor activity. µ-opioid receptor inverse agonist naloxone rapidly reverses opioid overdose by displacing opioids from their receptors (Pagan et al., 2024). CYP3A4 and CYP2D6 metabolize it, inducing rapid hepatic clearance and requiring frequent dosing (Rosenthal & Burchum, 2021). The serotonin 5-HT2A inverse agonist pimavanserin reduces Parkinson’s disease psychosis without worsening motor symptoms. It is metabolized through CYP3A4 and has a long half-life but carries a risk of QT prolongation, peripheral edema, and confusion.

References

Barrett, J. E., Shekarabi, A., & Inan, S. (2023).
Oxycodone: A current perspective on its pharmacology, abuse and pharmacotherapeutic developments
. PHARMREV-000506.
https://doi.org/10.1124/pharmrev.121.000506

Pagan, F. L., Schulz, P. E., Torres-Yaghi, Y., & Pontone, G. M. (2024). On the
optimal diagnosis
and the evolving role of pimavanserin in parkinson’s disease psychosis.
CNS Drugs
,
38
(5), 333–347.
https://doi.org/10.1007/s40263-024-01084-1

Rosenthal, L. D., & Burchum, J. R. (2021).
Lehne’s pharmacotherapeutics for advanced practice nurses and physician assistants
(2nd ed.). Elsevier.

Sampogna, G., Di Vincenzo, M., Giuliani, L., Menculini, G., Mancuso, E., Arsenio, E., Cipolla, S., Rocca, B. D., Martiadis, V., Signorelli, M. S., & Fiorillo, A. (2023). A systematic review on the effectiveness of antipsychotic drugs on the quality of life of patients with schizophrenia.
Brain Sciences
,
13
(11), 1577–1577.
https://doi.org/10.3390/brainsci13111577

Siwek, M., Wojtasik-Bakalarz, K., Krupa, A. J., & Chrobak, A. A. (2023). Brexpiprazole pharmacologic properties and use in schizophrenia and mood disorders.
Brain Sciences
,
13
(3), 397–397.
https://doi.org/10.3390/brainsci13030397 
 PSYCHOPHARMACOLOGY SCAVENGER HUNT CONCEPT MAP ANSWERS