Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

PCTH 325 > Antipsychotics > Flashcards

Antipsychotics Flashcards

1
Q

Describe the 4 dopamine pathways and their relation to schizophrenia

A
  1. Mesolimbic: memory and emotions - hyperfunctional in schizophrenia, (+) symptoms. High dopamine activity
  2. Mesocortical: cognition and motivation - hypofunctional in schizophrenia, (-) symptoms. Low dopamime activity
  3. Nigrostriatal: motor movement, normal dopamine activity in schizophrenia
  4. Tuberoinfundibular: prolactin secretion, normal dopamine activity in schizophrenia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is the dopamine hypothesis of schizophrenia?

A

-Drugs that increase dopamine -> psychotic symptoms
-Antipsychotics antagonize D2 receptors -> diminish symptoms
-Does not explain dopamine deficiency in pre-frontal cortex (mesocortical pathway) in schizophrenia

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What do First Generation Antipsychotics (FGA) do?

A

Antagonize D2, H1, alpha-1, and M1 receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are examples of FGAs (10)?

A
  1. Chlorpromazine
  2. Flupenthixol
  3. Fluphenazine
  4. Haloperidol
  5. Loxapine
  6. Perphenazine
  7. Pimozide
  8. Thiothixene
  9. Trifluoperazine
  10. Zuclopenthixol
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

How do FGAs antagonizing D2 affect the 4 dopamine pathways?

A
  1. Mesolimbic: 65-75% antagonism -> treates psychosis
  2. Mesocortical: cause secondary negative symptoms
  3. Nigrostriatal: >80% antagonism -> EPS
  4. Tuberoinfundibular: Significant antagonism -> prolactin secretion
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What are side effects of FGAs antagonizing other non-D2 receptors?

A

H1: Sedation, increased appetite, weight gain
alpha-1: orthostatic hypotension, dizziness, drowsiness
M1: Dry mouth, urinary retention, blurred vision, constipation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Example and side effects of FGAs with low potency for D2 receptors

A

Example: Chlorpromazine
Side effects: H1, alpha-1, M1 receptor antagonism related
(sedation, weight gain, hypotension, urinary retention)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Example and side effects of FGAs with high potency for D2 receptors

A

Example: Haloperidol
Side effects: D2 receptor antagonism related (EPS, increased prolactin release)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What do Second Generation Antipsychotics (SGAs) do?

A

Antagonize D2, H1 alpha-1, M1 and 5HT2A receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What are examples of SGAs (8)

A
  1. Clozapine
  2. Asenapine
  3. Lurasidone
  4. Olanzapine
  5. Paliperidone
  6. Quetiapine
  7. Risperidone
  8. Ziprasidone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

MOA of 5HT2A antagonism

A

-Serotonin inhibits dopamine release
-5HT2A receptor antagonism -> release of dopamine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

How do SGAs antagonizing 5HT2A receptors affect the mesocortical and nigrostriatal pathways?

A
  1. Mesocortical: improve negative symptoms (from hypoactive -> release more D2)
  2. Nigrostriatal: reduce EPS liability
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What do Third Generation Antipsychotics (TGAs) do?

A

D2, D3, 5HT1A receptor partial agonist
H1, alpha-1, M1, 5HT2A receptor antagonist
*some have high intrinsic activity - qualify as D2 agonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What are examples of TGAs (3)?

A
  1. Aripiprazole
  2. Brexpiprazole
  3. Cariprazine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Taking all the different antipsychotics into account, rank them in order of treating:
-positive symptoms of schizophrenia
-negative symptoms of schizophrenia

A

Positive symptoms: TGA=SGA=FGA, with the exception of clozapine for treatment-resistant patients
Negative symptoms:
TGA>SGA>FGA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Antipsychotics therapeutic effect + side effect of D2

A

Therapeutic (antagonist or partial agonist): treat psychosis
Side effects (antagonist): EPS, (-) symptoms, increased prolactin

17
Q

Antipsychotics therapeutic effect + side effect of D3

A

Therapeutic (antagonist or partial agonist): treat psychosis, improve (-) symptoms, antidepressant action, reduce drug-seeking/cravings, improve cognition
Side effects (agonist): craving

18
Q

Antipsychotics therapeutic effect of 5-HT1A

A

Therapeutic (partial agonist): antidepressant and anxiolytic action, reduced EPS

19
Q

Antipsychotics therapeutic effect + side effect of 5-HT2A

A

Therapeutic (Antagonist): reduce EPS, improve (-) symptoms
Side effects (agonist): agitation, anxiety, EPS, sexual dysfunction, insomnia, cognitive dulling, akathisia

20
Q

Antipsychotics side effect of alpha-1

A

Side effect (antagonist): orthostatic hypotension, sedation, dizziness, reflex tachycardia, sexual dysfunction

21
Q

Antipsychotics therapeutic effect + side effect of H1

A

Therapeutic (Antagonist): Anxiolytic
Side effect (Antagonist): sedation, increased appetite, weight gain

22
Q

Antipsychotics therapeutic effect + side effect of M1

A

Therapeutic effect (Antagonist): Reduce EPS
Side effect (Antagonist): blurred vision, dry mouth, constipation, urinary retention, impaired memory, sinus tachycardia, QRS changes, confusion, worsening condition, delirium

23
Q

What is the biggest clinical difference between SGAs and TGAs?

A

SGAs are D2 antagonist (w/ exception of clozapine and quetiapine - low D2 receptor affinity)
TGAs are partial D2 agonist

24
Q

How do SGAs and TGAs clinically differ in managing prolactin?

A

SGAs = D2 antagonist -> increase prolactin
TGAs = D2 partial agonists -> reduce prolactin

25
Q

What are side effects of increased prolactin levels?

A

increase risk of breast cancer (women)

26
Q

How do SGAs and TGAs clinically differ in managing dysphoria (life dissatisfaction)?

A

SGAs = D2 antagonist -> cause dysphoria
TGAs = D2 partial agonist -> don’t cause dysphoria

27
Q

How do SGAs and TGAs clinically differ in dopamine supersensitivty psychosis?

A

SGAs = D2 antagonist -> upregulate D2 receptors -> dopamine supersensitivity -> psychosis
TGas = D2 partial agonist -> don’t upregulate D2 receptors

28
Q

What are the treatment guidelines of schizophrenia?

A
  1. Start/optimize trial of SGA or TGA
  2. Wait 6-8 weeks to evaluate treatment response
29
Q

What if there is no response of the antipsychotic after initial 6-8 weeks of treatment?

A

-Gradual switch to new trial or different SGA/TGA
-Long acting injectable (LAI) antipsychotics

30
Q

Why are Long-Acting Injectables (LAI) antipsychotics used?

A

-low risk of rehospitalization and treatment failure
-effective

31
Q

What if there is no response even with different trials of SGAs or TGAs and LAIs?

A

Switch to clozapine

32
Q

What is clozapine used to specifically treat?

A

-Treatment resistant schizophrenia (caused by dopamine supersensitivity)
-Clozapine downregulates D2 -> no psychosis

33
Q

What if there is no response with clozapine?

A

Clozapine augmentation

PCTH 325 (19 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions