Lecture 79: Antipsychotics Flashcards Preview

Brain and Behavior > Lecture 79: Antipsychotics > Flashcards

Flashcards in Lecture 79: Antipsychotics Deck (38):
1

Typical antipsychotics are pure..

Dopamine antagonists

2

Atypical antipsychotics are both...

Dopamine antagonists and 5HT2A antagonists

3

Antipsychotics are also called

Neuroleptics

4

All DA receptors are...

G-protein coupled

5

Neuroleptics act on...which is coupled to? This causes

D2; Gi; less DA neurotransmission

6

Low potency antipyschotic

Clorpromazine

7

Mid potency antipyschotic

Perphenazine

8

High potency antipyschotics (2)

Fluphenazine, haloperidol

9

Anitpsychotic "potency" is based on...Why is this important?

D2 Blockade; higher potent = less dirty

10

Describe "dirty" SEs of antipsychotics via receptors

ACh, H1, alpha1 blockade

11

Therapeutic use of antipsychotics (5)

Primary and secondary psychotic disorder, mood disorders (bipolar and MDD w/ psychotic features), severe agitation, delirium, Tourette's

12

What drugs are available once-a-month dosing?

F

13

DA-related effects of antipsychotics and pathway

1. Parkinsonian-like (nigrostriatal); 2. Relief of psychosis (mesolimbic); 3. Increased negative symptoms (mesocortical); 4. Elevated prolactin --> breast enlargement/lactation (tuberoinfundibular pathway)

14

Neurological adverse effects (3). Which drugs convey highest risk?

1. Extrapyramindal symptoms (EPS; Parkinsonism, acute dystonia, akathisia); 2. Tardive dyskineasia; 3. Neuroleptic malignant syndrome; high potency drugs

15

How many patients get neuroleptic-induced Parkisonism (%)? When do they occur? What is treatment? Why?

15%; within several months; anticholinergics --> typically balance b/t DA and ACh, if you block DA, you should block ACh to re-achieve balance

16

Describe acute dystonic reaction: symptoms, when it occurs, treatment

Spastic contractions in face and body; occurs quickly (within days); anticholinergic

17

Describe akathisia: symptoms

Subjective feeling of inner restlessness w/ objective increased motor activity

18

Describe tardive dyskinesia: symptoms, onset (%), treatment

Writhing movements of mostly face; 5%/year (long-term use); not reversible --> stopping/switching antipsychotic

19

Describe neuroleptic malignant syndrome: symptoms, onset time, mortality (%)

Autonomic symptoms (fever, sweating), motor & behavior symptoms (rigidity, dystonia, agitation, confusion); can occur ANY TIME; 20-30% if untreated

20

Other antipsychotic SEs by 3 receptors and 1 other important SE

M1, H1, alpha1 receptor blockade; cardiac (QT prolongation)

21

Atypical antipsychotics

Clozapine, risperidone, olazapine, ziprasidone, quetiapine, aripiprazole

22

What makes an antipsychotic atypical (2)

1. D2 AND 5HT2A antagonists; 2. Rapid dissociation from D2 receptor

23

Why does 5HT2A antagonism work? How does it work in real patients?

Turns off GABA interneuron --> more DA release (tempering DA blockade); complicated net actions on DA activity, varies per patient

24

Theoretical benefits of atypicals and which are true/not true (4)

Reduced EPS (true), reduced hyperprolactinemia (true), cognitive enhancement (not true), improved adherence (not true)

25

How to choose an antipsychotic? Example.

Look at receptor binding profile (i.e. olazapine blocks H1 more than risperidone, so it is more sedating, good for agitated people)

26

Therapeutic use of antipsychotics (3)

1. Psychotic disorders; 2. Mood disorders w/ psychotic features; 3. Treatment resistant MDD; 4. Aggression/irritability in children with autism (Risperidone)

27

T/F: Atypicals are associated with off-label uses

True! Multiple

28

How is Aripiprazole different?

"Third generation" --> partial agonist at DA D2 receptor and 5-HT1A; antagonist at 5-HT2A

29

What is the most effective AND drug of choice for treatment resistant schizophrenia? What's interesting about this drug and why is it not always first line?

Clozapine; low potency as D2-receptor antagonist; potentially irreversible risk of agranulocytosis

30

Risperidone has similar SEs to...why?

Typicals because it is a strong blocker of D2

31

Adverse effect of atypical antipsychotics

Metabolic syndrome: visceral obesity, low insulin resistance, high triglycerides, hypertension low HDL-cholesterol

32

Mortality with atypical antipsychotics

2-3x increased mortality from all causes

33

What are the "worst" atypicals for metabolic syndrome. Best?

Clozapine and olanzapine; aripiprazole

34

Other adverse effects of antipsychotics

Cardiac, sedation, EPS (risperidone), seizures...

35

Rare serious SEs of clozapine

Agranulocytosis and myocarditis

36

What is a common off label use of antipsychotics? Good data? Why is this concerning?

Treat behavioral disturbances in ELDERLY; NO; can cause over sedation/falls (orthostatic hypotension), increases ALL CAUSES of mortality

37

The only two antispychotics shown to increase cognition/social life. But these are...Why?

Clozapine and olanzapine; 2nd line; more likely to induce metabolic syndrome (and scary SEs)

38

Why do we use atypical antipsychotics first line?

You CAN treat metabolic syndrome but NOT tardive dyskinesia

Decks in Brain and Behavior Class (56):