Antipsychotics

Question 1

Another name for antipsychotic drugs

Answer 1

Neuroleptics

Question 2

Another name for typical antipsychotics

Answer 2

Conventional antipsychotics

Question 3

What receptors do typical antipsychotics block?

Answer 3

Dopamine type 2 (D2) receptors

Question 4

Blocking the D2 receptor decreases neurotransmission in what pathway? What is the result?

Answer 4

Mesolimbic pathway - reduces positive symptoms like hallucinations

Question 5

Are antipsychotic meds specific in terms of receptors blocked?

Answer 5

No - all receptors are blocked in multiple pathways, so lots of side FX

Question 6

What pathway is the therapeutic target of D2?

Answer 6

Mesolimbic

Question 7

Blocking the mesolimbic pathway additionally blocks what functions of the pathway? What side FX does this result in?

Answer 7

Reward and pleasure - leads to apathy, anhedonia, amotivation, social withdrawal, known as secondary negativism b/c it’s in addition to negative symptoms

Question 8

Dopamine blockade can worsen the deficit in what pathway, leading to worsening of cognitive and emotional symptoms? It may already be deficient in what disease?

Answer 8

Mesocortical pathway

Schizophrenia

Question 9

Potent D2 blockade in the nigrostriatal tract results in what short-term extrapyramidal side effects (EPS):

Answer 9

• Parkinsonian symptoms
• Dystonic symptoms
• Akathesia

Question 10

Dopamine normally suppresses what neurotransmitter activity in nigrostriatal pathway

Answer 10

Acetylcholine

Question 11

What medications are used to treat extrapyramidal side effects (EPS)

Answer 11

Anticholinergics - diphenhydramine or benztropine

Question 12

Long-term D2 blockade in nigrostriatal pathway results in what movement disorder

Answer 12

Tardive dyskinesia (TD) - involuntary tongue and facial movements

Question 13

Dopamine blockade in tuberoinfundibular tract leads to what side effects as a result of increased plasma prolactin

Answer 13

Galactorrhea, amenorrhea, infertility, bone loss

Question 14

Name the blockade that causes the following side FX:

Dry mouth, blurred vision, constipation, cognitive blunting

Answer 14

Muscarinic anticholinergic blockade

Question 15

Name the blockade that causes the following side FX:

Weight gain and drowsiness

Answer 15

Histamine blockade

Question 16

Name the blockade that causes the following side FX:

Orthostatic hypotension

Answer 16

a-1 adrenergic blockade

Question 17

What syndrome is a rxn to antipsychotics and involves:

High fever, muscle rigidity, confusion, autonomic instability, high serum creatinine phosphokinase, high liver enzymes

Answer 17

Neuroleptic Malignant Syndrome (NMS)

Question 18

Haloperidol (Haldol)

Side FX?

Answer 18

High potency typical anti-psychotic, potent D2 antagonism

-EPS, TD, NMS

Question 19

Chlorpromazine (Thorazine)

Side FX?

Answer 19

Low potency typical anti-psychotic, less potent D2 antagonism

• Anticholinergic side FX

Question 20

Mechanism differences that make an antipsychotic atypical

What side FX do these drugs decrease?

Answer 20

1) Shorter binding time at D2 receptors
2) 5HT2A antagonism

EPS and hyperprolactinemia, as well as tardive dyskinesia (b/c shorter D2 binding periods mean less striatum sensitization), decreases negative symptoms

Question 21

What receptor does serotonin bind on dopamine neurons? What action does this have?

Answer 21

5HT2A - inhibits dopamine release

Question 22

Clozapine (Clozaril)

Answer 22

Atypical antipsychotic

Reduces risk of suicide, decreases violence and aggression

Side FX: AGRANULOCYTOSIS (test question), sedation, seizures
causes few EPS, no TD, no prolactin elevation

Question 23

Olanzapine (Zyprexa)

Answer 23

Atypical antipsychotic

No EPS symptoms, very sedating,

Question 24

Risperidone (Risperdal)

Answer 24

Atypical antipsychotic at lower doses

At high doses, acts more like a typical antipsychotic, which leads to EPS and increases prolactin

Approved for pediatric use

Question 25

Paliperidone (Invega)

Answer 25

Atypical antipsychotic

Next generation of Risperidone, sustained release, more easily dosed, less EPS FX

Increases QTc interval

Question 26

Qeutiapine (Seroquel)

Answer 26

Atypical anti-psychotic

Used preferentially in Parkinson’s patients

virtually NO EPS, no prolactin elev, may have enhanced NE activity

Question 27

Ziprasidone (Geodon)

Answer 27

Atypical antipsychotic that SIGNIFICANTLY prolongs QTc interval

Low symptoms of EPS, low prolactin elev, less propensity for weight gain

Question 28

Aripiprazole (Abilify)

Answer 28

Atypical antipsychotic

Role for augmentation in depression, not as sedating, can cause agitation or akathesia, lower CM risk

Question 29

Drawbacks of atypical anti-psychotics?

Answer 29

• Increase risk factors for cardiac/metabolic disease
• Weight gain, obesity
• Diabetes
• Premature death

Question 30

Successful treatment of though disorders involves optimizing ______ function (what neurotransmitter?)

Answer 30

Dopamine

Question 31

Weight gain as a result of atypical anti-psychotics is mediated through what mechanisms

Answer 31

Histamine blockade and through actions of serotonin systems (5HT2C)

Question 32

Most risk to least risk for weight gain and CM risk amongst atypical anti-psychotics?

Answer 32

COQR/PZA
Clozaril
Olanzapine
Quetiapine
Risperidone/Paliperidone
Zipasidone
Aripiprazole