Antipsychotics

Question 1

hallucinations, delusions, disorganized speech, agitation, behavioral dyscontrol caused by change in what neurotransmitter and receptor?

Answer 1

increased dopamine binding to post synaptic D2-receptors (positive symptoms)

Question 2

apathy, avolition, alogia + cognitive deficits caused by change in what neurotransmitter and receptor?

Answer 2

decreased dopamine binding to D1-receptors (negative symptoms)

Question 3

D1 or D2 sx easier to tx?

Answer 3

D2 (positive) - all antipsychotic drugs target D2

Question 4

class of antipsychotic:
Haloperidol
Chlorpromazine
Fluphenazine

Answer 4

typical agents - “azine”

Question 5

class of antipsychotic:
Aripiprazole
Brexpiprazole

Clozapine
Olanzapine
Quetiapine

Paliperidone
Risperidone
Ziprasidone

Answer 5

atypical agents - “piprazole” and “apine” and “idones”

Question 6

Main difference between typical and atypical antipsychotics

Answer 6

Reduction in movement‐disorder SE’s (EPS) with atypical drug development - esp high potency fluphenazine and haloperidol

Question 7

Four receptors that atypicals can block

Answer 7

D1, D2, D4, 5H-T

Question 8

***2 Atypical agents also a partial agonist at presynaptic (D2 /D3 & 5HT1A)

Answer 8

apripirazole and brexpiprazole

Question 9

1 Atypical agent’s metabolite that also potently blocks NERT

Answer 9

(norquetiapine) quetiapine

Question 10

Typical Antipsychotic agent that is low potency - drug name and this means?

Answer 10

Chlorprimazine

-More sedation, hypotension and seizure‐threshold reduction - less mvmt disorders.

Question 11

AE of high potency typical antipsychotics - and name of two drugs

Answer 11

fluphenazine, haloperidol

-EPS movement disorder if >80% D2 receptor occupancy

Question 12

Three receptors, other than Dopamine Receptors, that may be blocked by antipsychotics and side effects.

Answer 12

o Muscarinic (anti-cholinergic) = dry mouth, constipation, urinary retention, blurred vision, sedation
o Histaminic (H1 primarily) = sedation
o Alpha‐adrenergic (α1 & α2) = orthostatic hypotension and impotency

Question 13

**Three possible (anti-cholinergic) drugs to treat acute Dystonia/Akathisia/Dyskinesia/Parkinsonism‐like symptoms (EPS) caused by Typical Class

Answer 13

Anticholinergic agents
• Diphenhydramine (Benadryl)
• Benztropine (Cogentin)
• Trihexyphenidyl

Question 14

Severe side effect of clozapine. So monitor what?

Answer 14

agranulocytosis

-monitor WBC

Question 15

Define Neuroleptic Malignant Syndrome

Answer 15

Rare but potentially‐fatal, severe Parkinson’s‐like movement disorder
• Autonomic instability, Stupor, Hyperpyrexia, Muscle rigidity, Altered mental status
• More common with injectable, high‐potency Typical agents but possible with all agents

Question 16

Four classic Atypical Class side effects. So monitor what?

Answer 16

• Seizure threshold reduction
• Stroke
• Metabolic syndrome - wt gain, hyperglycemia, hyperlipidemia
• QT prolongation/ECG changes

Monitor: Baseline serum glucose, lipids, weight, blood pressure, and when possible, waist circumference and personal and family histories of metabolic and CV disease.

Question 17

A dementia patient taking Olanzapine, Paliperidone, Risperidone - major risk increase?

Answer 17

stroke

Question 18

**EPS:
worst
best

Answer 18

worst: haloperidol
best: atypical class

Question 19

**Weight gain:
worst
best

Answer 19

worst - clozapine, olanzapine "pines"
best - All of the typical class and the "piprazoles"

Question 20

**Stoke risk:
worst
best

Answer 20

worst - olanzapine, paliperidone, risperidone

best - any other, esp typicals

Question 21

**ECG changes
worst
best

Answer 21

worst - chlorpromazine (typical), fluphenazine (typical), ziprasidone (atypical)
best - “apine”, “piprazole”

Question 22

four drugs that affect 5HT1 receptors

Answer 22

atypicals - ariprazole, brexpiperazole, clozapine, ziprasidone

Question 23

Used for?
• Haloperidol decanoate
• Fluphenazine decanoate

Ri Ol Ar Pa
• Risperidone
• Olanzapine pamoate
• Aripiprazole
• Paliperidone palmitate

Answer 23

Non‐adherence can be managed with long‐acting injectable agents (LAIAs) (every 1‐4 weeks, depending on agent, dose & patient factors)

Question 24

Psychotic with anti‐suicidal‐thoughts/behaviors

Major adverse effect.

Answer 24

clozapine

SE: agranulocytosis - monitor WBC

Question 25

In comparing typical antipsychotics, what is associated with skeletal muscle rigidity, tremor at rest, uncontrollable restlesness, and spastic torticollis?

Answer 25

haloperidol (this is EPS)

Question 26

Woman has schizophrenia. Current tx is a typical agent, experiencing amenorrhea and galactorrhea. What antipsychotic agent would decrease severity?

Answer 26

atypical class

Question 27

**Prolactin (amenorrhea and glactorrhea dt D effects)
worst
best

Answer 27

worst - typical class
best - atypical class

Question 28

blurred vision, dry mouth, mydriasis - what receptor are these SE of?

Answer 28

muscarininc

Question 29

**drug induced orthostatic hypotension

Answer 29

chlorpromazine or clozapine (*many SE - WBC, seizures)

least-fluphenazine, haloperidol, paliperidone, ziprasidone

Question 30

first line drug with least weight gain

Answer 30

ziprasidone, paliperidone, aripiprazole, brexipiprazole

Question 31

Sedation.
typical class: least and most
atypical: most

Answer 31

typical: Least-fluphenazine, haloperidol.

• *typical: Most-chlorpromazine
  atypical: Most-olanzapine, quetiapine**

Question 32

Muscarinic

Answer 32

Most - clozapine, olanzapine.

Least - paliperidone

Question 33

**seizures
most
least

Answer 33

most - clozapine, olanzapine, typicals

least - the reast of the atypicals are 0/+

Question 34

severe muscle rigidity (typically the initial symptom)
fever (often greater than 40oC)
autonomic changes (fluctuating blood pressure, pulse rate, tachypnea)
altered consciousness (stupor that can progress to coma)

Answer 34

Neuroleptic Malignant Syndrome