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Antipsychotic Drugs✔️ Flashcards

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1
Q

What type of receptors are dopamine (DA) receptors?

A

G-protein coupled receptors.

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2
Q

What are the D1-like dopamine receptors and their signaling pathway?

A

D1 and D5

they activate adenylyl cyclase (AC), increase cAMP, and activate PKA.

(AC activation → ↑ cAMP → PKA)

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3
Q

What are the D2-like dopamine receptors and their signaling pathway?

A

D2S (short), D2L (long), D3 & D4;

they inhibit adenylyl cyclase, leading to no cAMP and no PKA activation.

(AC inhibition = ❌ No cAMP and PKA)

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4
Q

What determines the difference in dopamine (DA) affinity between D1-like and D2-like receptors?

A

• Extracellular dopamine concentration

• Type of release (burst firing favors D1, tonic activity favors D2)

• Timescale of engagement

• Receptor abundance in complex circuits

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5
Q

Which dopamine receptor type is favored by BURST firing?

A

D1 receptors

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6
Q

Which dopamine receptor type is favored by TONIC firing?

A

D2 receptors

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7
Q

Why can drugs targeting 5HT receptors have multiple effects?

A

Because 5HT receptor subtypes are widely distributed and control various functions such as sleep, memory, anxiety, appetite, vomiting, and more.

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8
Q

True or False:

Antipsychotic drugs cure schizophrenia.

A

False

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9
Q

What is the effect of antipsychotic drugs on hallucinations and delusions?

A

They reduce the intensity of hallucinations and delusions.

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10
Q

What are the two generations of antipsychotic drugs?

A

First generation (typical) and second generation (atypical).

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11
Q

Which dopamine pathways are associated with the antipsychotic effects of these drugs?

A

Mesolimbic and mesocortical dopamine pathways.

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12
Q

Effects on which dopamine pathway are responsible for motor side effects of antipsychotic drugs?

A

The nigrostriatal dopamine pathway

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13
Q

What are the three criteria used to classify antipsychotic drugs into 1st and 2nd generation?

A

• Receptor profile
• Incidence of extrapyramidal side effects
• Efficacy against negative symptoms

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14
Q

True or false

All antipsychotics block D2 receptors in the brain and periphery.

A

True

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15
Q

True or false

All antipsychotics increase dopamine transmission.

A

False

Reduce

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16
Q

What additional receptors do 2nd generation antipsychotics block?

A

5-HT (serotonin) receptors

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17
Q

Why do antipsychotics take several weeks to work?

A

Due to secondary effects like increased D2 receptor numbers in limbic structures, which may be more important than direct D2 blockade

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18
Q

How do 1st generation antipsychotics bind to D2 receptors?

A

They bind more tightly than dopamine itself and dissociate slowly.

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19
Q

List 4 effects of the loose and fast binding of 2nd generation antipsychotics to D2 receptors.

A

• Allows normal DA transmission
• Keeps prolactin levels normal
• Spares cognition
• Causes fewer extrapyramidal side effects (EPS)

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20
Q

True or False:

Second-generation (atypical) antipsychotics bind loosely to D2 receptors and dissociate faster than dopamine.

A

True

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21
Q

What is the primary mechanism of 1st generation typical antipsychotics?

A

D₂ receptor blockade.

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22
Q

What other receptors may 1st generation antipsychotics block besides D₂?

A

H₁, M₁, and α₁ receptors (among others).

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23
Q

What is the primary serotonin receptor targeted by 2nd generation antipsychotics?

A

5-HT₂A

they block this receptor more strongly than they block D₂ receptors.

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24
Q

Do 2nd generation antipsychotics block D₂ receptors?

A

Yes, but loosely, with a fast dissociation constant.

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25
Which second-generation antipsychotics are also 5-HT₁A agonists?
• Clozapine • Quetiapine • Ziprasidone
26
What does 5-HT₁A agonists do in the prefrontal cortex?
Increases dopamine release and reduces glutamate release.
27
Which drug shows partial D₂ agonism among second-generation antipsychotics?
Aripiprazole.
28
What other receptors can some 2nd generation antipsychotics block?
H₁, M₁, and α₁ receptors.
29
True or False: Both first- and second-generation antipsychotics may block H₁, M₁, and α₁ receptors.
True
30
What is chlorpromazine, and what was discovered about it in 1951?
It is a phenothiazine that was serendipitously discovered to be effective against the POSITIVE symptoms of schizophrenia. (First generation)
31
Are phenothiazines like chlorpromazine effective against NEGATIVE and cognitive symptoms of schizophrenia?
No, they are less effective against negative and cognitive symptoms.
32
True or False: A common issue with phenothiazine use is that they have many adverse effects.
True
33
What drug in the butyrophenone class was introduced in 1958, and what are its characteristics?
Haloperidol it has better side effect profile than phenothiazines but is still ineffective in treating negative and cognitive symptoms.
34
What are examples of first-generation (typical) antipsychotic drugs?
• Chlorpromazine • Haloperidol • Fluphenazine • Thioridazine
35
What is the mechanism of action of first-generation (typical) antipsychotics, and which other receptors can they block?
They produce antipsychotic effects by competitively blocking D2 receptors. They can also block H1, M1, and α1 receptors (among others).
36
True or False: First-generation antipsychotics are associated with extrapyramidal symptoms (EPS), which are movement-related side effects.
True
37
Which first-generation antipsychotic has a higher EPS risk: haloperidol or chlorpromazine?
Haloperidol, because it binds tightly to D2 receptors. Whereas chlorpromazine binds weakly = less likely for EPS
38
Why do haloperidol and fluphenazine have a higher risk of EPS when compared to Thioridazine?
They preferentially block D2 receptors, causing a DA/ACh imbalance.
39
Which antipsychotic causes fewer EPS due to strong anticholinergic activity?
Thioridazine
40
At what D₂ receptor occupancy level do extrapyramidal symptoms (EPS) typically begin to appear?
EPS typically begin when D₂ receptor occupancy exceeds 78%.
41
Which second-generation antipsychotic introduced in 1990 revolutionized the treatment of schizophrenia?
Clozapine
42
What symptoms of schizophrenia are second-generation antipsychotics effective against?
Both positive and negative symptoms.
43
How do second-generation antipsychotics compare to first-generation (like phenothiazines & butyrophenones) in terms of EPS?
They cause fewer extrapyramidal symptoms (EPS).
44
What is Meltzer’s hypothesis regarding the 5HT₂A/D₂ ratio?
5HT₂A antagonism may increase dopamine transmission in the nigrostriatal pathway, reducing EPS, and may improve negative and cognitive symptoms by increasing dopamine release in the prefrontal cortex.
45
True or false A high 5HT₂A to D₂ blocking ratio always means fewer side effects like EPS.
False. Some first-generation drugs also block 5HT₂A, but still cause EPS. So the ratio alone isn’t a reliable indicator.
46
True or False: Second-generation antipsychotics are effective against depression symptoms in patients with schizophrenia.
True
47
Can second-generation antipsychotics be used for mood and anxiety disorders not linked to schizophrenia?
Yes, they can be used as monotherapy or as adjuncts to antidepressants and mood stabilizers.
48
Which second-generation antipsychotics are used as monotherapy for bipolar manic depression and generalized anxiety disorder?
• Aripiprazole • Olanzapine • Risperidone
49
How are second-generation antipsychotics used in unipolar depression?
As adjunct/combination therapy with SSRIs and SNRIs.
50
Which drugs are effective as adjuncts in treatment-resistant depression?
• Aripiprazole • Risperidone
51
What type of side effects are commonly associated with second-generation antipsychotics?
• Metabolic side effects ( i.e diabetes, hypercholesterolemia, etc) • Weight gain.
52
What is the mechanism of action of clozapine, risperidone, and olanzapine?
They block 5HT2A and D2 receptors, with a higher affinity for 5HT2A blockade. (2nd generation)
53
What is clozapine’s mechanism of action?
High affinity for 5HT2, D1, D4, muscarinic, and α-adrenergic receptors, with weak D2 blockade
54
Why is clozapine reserved for refractory patients?
Due to serious side effects like • bone marrow suppression • seizures • cardiovascular issues.
55
What is a life-threatening risk of clozapine requiring frequent lab monitoring?
Severe agranulocytosis, which requires frequent monitoring of white blood cell (WBC) count.
56
What is the mechanism of action of aripiprazole?
• Partial agonist at D2 and 5HT1 receptors • Antagonist at 5HT2 receptors
57
Is it clear whether blocking H1, M1, and α1 receptors causes the clinical effects of second-generation antipsychotics?
No, it is unclear; however, blocking these receptors is associated with some of the side effects.
58
What produces the antipsychotic effects of antipsychotics?
Blocking D2 receptors in the mesolimbic pathways. (All antipsychotics)
59
What gives antipsychotics their antiemetic effect?
Blocking D2 receptors in the chemoreceptor trigger zone (CTZ) of the medulla. (most antipsychotics except aripiprazole).
60
What are the anticholinergic effects of certain antipsychotics? and what benefit do they provide? Provide examples
• Blurred vision • Confusion • Inhibition of smooth muscle in the gastrointestinal and urinary tracts Benefit: helps reduce the risk of extrapyramidal symptoms (EPS) Examples: Chlorpromazine, olanzapine, clozapine
61
What are the extrapyramidal symptoms (EPS) associated with antipsychotic use, and what causes them?
Acute reversible dystonias & Parkinson-like symptoms: • Involuntary movements, tremor, rigidity • Likely due to D2 receptor blockade in the nigrostriatal pathway Tardive dyskinesia: • Involuntary movements of the face and limbs • Appears after months or years of treatment • Often irreversible, but a long holiday from antipsychotics may help in some cases • May be due to increase in (presynaptic?) dopamine receptors in the corpus striatum
62
Which antipsychotics are associated with a lower risk of acute dystonias and tardive dyskinesia, and why?
Lower risk with 2nd generation atypical antipsychotics Very low risk with: • Clozapine (2nd gen) • Aripiprazole (2nd gen) • Thioridazine (1st gen) Possible reasons: • Strong antimuscarinic activity • Greater selectivity for mesolimbic dopamine pathways over nigrostriatal pathways
63
What antipsychotic side effects result from muscarinic receptor block?
• Dry mouth • Urinary retention • Blurred vision (Cholinergic effects)
64
What causes orthostatic hypotension and lightheadedness with antipsychotics?
Block of α-adrenergic receptors
65
What causes sedation in antipsychotic use?
Potent H1 histamine receptor blockade
66
What is poikilothermia and how is it related to antipsychotics?
• It’s the body’s inability to regulate core temperature • Rare but potentially fatal side effect
67
Why do antipsychotics cause increased prolactin and gynecomastia?
Due to D2 receptor blockade in the pituitary
68
What is neuroleptic malignant syndrome? What to do if developed?
• A potentially fatal reaction to antipsychotics • Requires drug discontinuation and supportive therapy
69
What are the metabolic side effects of antipsychotics (especially 2nd gen)?
• Weight gain • Worsening of pre-existing diabetes • Hyperlipidemia • Hypercholesterolemia
70
What reproductive side effects may occur with antipsychotics?
• Amenorrhea • Infertility
71
What cardiac side effect is associated with antipsychotic drugs, especially thioridazine?
QT prolongation
72
What is a neurological risk associated with all antipsychotics?
All antipsychotics may lower the seizure threshold.
73
Why should antipsychotics be used cautiously in elderly patients with psychosis or dementia-related behavioral issues?
Because they may increase mortality in these populations.
74
What must be monitored when antipsychotics are used in mood disorders?
Worsening mood, suicidal ideation, and suicidal behaviors.
75
What type of drug is Mirtazapine and in what condition is it used?
Atypical antidepressant Schizophrenia
76
What is the mechanism of action (MOA) of Mirtazapine?
• Enhances 5HT & NA release & thus neurotransmission by antagonising presynaptic α2-adrenoceptors (autoreceptors → NA release & heteroreceptors → 5HT release) • Antagonist at 5HT2A & 5HT2C • Blockade of 5HT2C → antidepressant effects as well • 5HT3 blockade → antiemetic • Sedation due to potent antihistaminic activity at H1 (Summary in picture)
77
What are the side effects of Mirtazapine?
Increased appetite, weight gain (frequent) and very sedating (used as sleep aid in depressed patients/other patients with difficulty sleeping)
78
What are the clinical uses of Mirtazapine?
Used in major depressive disorder, anxiety disorders, emesis, insomnia & as add on to antipsychotics in schizophrenia (−ve symptoms)

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