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Flashcards in Antipsychotic Drugs Deck (83):
1

FDA approved indications for anti-psychotics

Schizophrenia
Bipolar disorder
Agitation
Autism

2

Common uses for anti-psychotics

Schizophrenia and other psychotic disorders
Bipolar disorder
Major depression with psychosis
Delirium/Dementia
Substance induced psychosis
Tourette/OCD?

3

Which tract in the brain causes psychosis?

Mesolimbic tract (DA)

4

Which tract in the brain do antipsychotics work on?

Mesolimbinc tract (DA)

5

What are the 4 DA tracts in the brain?

Mesolimbic
Mesocortical
Nigrostriatal
Tuberoinfundibular

6

Dopamine binding affinity is strongly correlated with clinical anti-psychotic effects: the higher the affinity, the ____ the dose needed for anti-psychotic effects

Smaller

7

100 mg Chlorpromazine= __ mg Haloperidol

2 mg

8

Haloperidol is a ___ potency drug ( ___ binding affinity)

High

9

Chlorpromazine is a ___ potency drug ( ____ binding affinity)

Low

10

What are the limitations of the dopamine hypothesis?

- FGA tx of schizo was more effective against + symptoms
- 35% of treated patients relapse
-20-40% patients do not respond adequately

11

Other names for FGA

Neuroleptics
Major Tranquilizers
Conventional anti-psychotics
Typical anti-psychotics

12

What are the 3 Phenothiazines (FGA) and relative potencies?

Chlorpromazine- low
Thioridazine- low
Perphenazine- moderate

all end in "azine"

13

What is the 1 Thioxanthine (FGA) and relative potency?

Thiothixene - moderate

14

Describe the ideal therapeutic window for anti-psychotics (including tracts and % of D2 receptors bound)

Block >60-65% of D2 receptors in mesolimbic tract (anti-psychotic)
Block

15

What are the effects of low potency FGAs on dopamine receptors?

Antipsychotic effect and SE
-Extrapyramidal (EPS/TD)
(Due to decreased dopamine and increased Ach)
-Increased prolactin

16

What are the effects of low potency FGAs on muscarinic receptors?

= anti-cholinergic
blurred vision, urinary retention, dry mouth, constipation
"Can't see, can't pee, can't spit, can't shit"
"Self treating" for EPS

17

What are the effects of low potency FGAs on adrenergic receptors?

Orthostasis, increased fall risk

18

What are the effects of low potency FGAs on histamine receptors?

Sedation, weight gain

19

First Aid Chlorpromazine SE

Corneal deposits

20

First Aid Thioridazine SE

Retinal deposits

21

What are the 2 phenothiazines that are high potency FGA?

Fluphenazine
Trifluoperazine

"Azines"

22

What is the 1 Butyrophenone high potency FGA?

Haloperidol

23

High potency FGA Side Effects

Dopamine: extrapyramidal, increased prolactin (gynecomastia, galactorrhea, sexual dysfunction, menstrual irregularity/infertility), decreased bone density

No effects on muscarinic, adrenergic, or histamine receptors

24

What receptor(s) do high potency FGA act on?

Dopamine

25

What are some features of EPS?

Parkinsonian (resting tremor, bradykinesia, stiffness/rigidity)
Dystonia
Akathesia

26

What percentage of patients will develop EPS from taking high potency anti-psychotics?

50-90%

27

What is Tardive Dyskiensia (TD), what % of patients will develop?

involuntary movements from taking DA blockers
tardive= on meds for months - years
Classically involves lower facial and tongue movements
Does not remit, even after stopping DA antagonist
20-50%

28

Effects on which DA tract cause the extra-pyramidal side effects (EPS)?

Nigrostriatal tract

29

What is acute dystonia?

Sustained abnormal posture
Occurs within a couple weeks of someone starting the meds
Made worse by activity
Patient may report as "allergic reaction"

30

Who is at risk for EPS-dystonia?

Young males

31

What is acute akathesia?

Inner sense of restlessness and need to move?

32

Who is at risk for acute akathesia?

Women- 2x > men

33

Effect on which DA tract causes the increased prolactin?

Tuberoinfundibular tract

34

Increased prolactin causes what other symptoms?

Galactorrhea/lactation
Gynecomastia
Irregular menstruation, fertility issues
Osteopenia

35

What was the first SGA developed?

Clozapine

36

List the SGA:

Clozapine

Risperidone
Paliperidone
Ziprasidone
Lurasidone
Iloperidone

Olanzapine
Quetiapine
Asenapine

Aripiprazole

37

Describe the relative binding affinity of Clozapine for serotonin and dopamine receptors

Binding affinity for serotonin receptor is roughly 10x stronger than that for dopamine receptor

38

Describe the relative binding affinity for Onlazapine/Quietapine for serotonin and dopamine receptors

Both have relatively similar binding affinities for dopamine and serotonin receptors

39

Describe the relative binding affinity for Risperidone and ziprasidone for the serotonin and dopamine receptors

Receptor binding affinity for serotonin is higher than that for dopamine

40

What is the MOA of SGA?

Serotonin -Dopamine Dual Antagonism
-block post synaptic D2 receptors
-block pre synaptic 5-HT2 receptors (normally inhibit DA release> increased DA release)
-allows for

41

Which SGA is not going to have significant anti-histaminic side effects?

Risperidone

42

Which 2 SGAs are not going to have significant anti-muscarinic (anti-cholinergic) side effects?

Risperidone and Ziprasidone

43

Which SGA will not have anti alpha-adrenergic side effects?

TRICK! They all have some amount of anti-alpha adrenergic SE

44

List in order the likelihood that SGAs will cause EPS/TD and increased prolactin

Risperidone
Ziprasidone/Olanzapine
Quetiapine
Clozapine (none)

45

List in order the likelihood that SGAs will cause Alpha 1 related orthostasis

Clozapine
Olanzapine/Quetiapine/Risperidone
Ziprasidone

46

List in order the likelihood that SGAs will cause M1-anticholinergic SE

Clozapine
Olanzapine
Quetiapine
Risperidone/Ziprasidone (none)

47

List in order the likelihood that SGAs will cause Histamine related sedation

Clozapine/Olazapine
Quetiapine
Ziprasidone
Risperidone (none)

48

List in order the likelihood that SGAs will cause metabolic syndrome (weight gain, lipids, glucose intolerance)

Clozapine/Olanzapine
Quetiapine/Risperidone
Ziprasidone

49

Which class of SGAs are worse for weight gain- the "apines" or the "idones"

"apines"

50

What is the effect of Aripiprazole on weight?

Weight neutral

51

What is the effect of Ziprasidone on weight?

Weight neutral

52

Which SGA causes the most weight gain

Clozapine, followed closely by Olanzapine

53

SGA Partial Agonist MOA

Can have an antagonist or agonist effect depending on the level of dopamine in the env
less dopamine = agonist
more dopamine = antagonist

54

What are the indications for clozapine?

Pts non-responsive to other anti-psychotics
Treatment of negative symptoms of schizophrenia
Lowers the risk of suicide

55

What are the common SE of clozapine?

Sedating
Weight gain
Metabolic syndrome
Anti-cholinergic
Anti- alpha adrenergic

56

What are the rare/serious SE of clozapine?

Agranulocytosis
Myocarditis
Decreased seizure threshold

57

Neuroleptic Malignant Syndrome (NMS)

Seen with SGAs or FGAs, rare
Dopamine system goes haywire

58

What are the symptoms of Neuroleptic Malignant Syndrome?

Mental status change
Rigidity- increased CPK, tremor
Fever >40 C
Increased HR, inc/dec BP, inc RR

59

Treatment of NMS (neuroleptic malignant syndrome)

Stop DA blocker
Supportive therapy
FA: dantrolene, D2 agonists-bromocriptine

60

Sudden Death

Increased mortality in elderly patients with dementia psychosis
Stroke and related disorders
Increased risk with CVD
FGAs and SGAs

61

Recommendation for anti-psychotics in the elderly w/ dementia

Conservative use- low dose, minimize treatment length, alternative tx when available

62

What route of administration of the anti-psychotics provides the best bioavailability?

IM >PO

63

Anti-psychotics protein binding

90% protein bound, unbound crosses BBB

64

Which SGA has the longest half life?

Aripiprazole

65

Low potency FGA affect which receptors?

Dopamine, muscarinic, alpha-adrenergic, histamine

66

High potency FGA affect which receptors?

Dopamine 2

67

Side effects of low potency FGA correlated with receptors:

Dopamine: EPS/TD, inc prolactin
Muscarinic: treats EPS, anti-cholinergic SE
Adrenergic: dizziness, orthostasis, fall risk
Histamine: sedation, weight gain

68

Side effects of high potency FGA correlated with receptors:

Dopamine: EPS/TD

69

What is the only treatment for tardive dyskinesia?

Clozapine

70

Side effects of Clozapine (SGA) correlated with receptors:

Muscarinic: v anti-cholinergic
Adrenergic: orthostasis
Histamine: v sedating
Weight gain, serotonin syndrome

71

What is the one side effect of Lurasidone?

Akathesia

72

In Risperidone and Paliperidone, there is a dose dependent risk for ____ and ____?

EPS and increased prolactin

73

Which SGA carries an increased risk for increased qTC interval?

Ziprasidone

74

What are you options for Rx of patient with poor compliance

Long acting injectables!

75

What are the four long acting SGA injectables

Risperidal Consta
Invega Sustenna
Zyprexa
Abilift maintena

76

What form is asenapine available in?

Sublingual

77

What is the side effect of Aripiprazole?

Akathesia

78

What are the two long acting FGA injectables?

Haldol
Fluphenazine

79

Risperidone is metabolized to _______

Palliperidone

80

How is palliperidone excreted?

80% renal

81

Indications for palliperidone?

Use in pt w/ liver dises

82

Contraindication for palliperidone?

Renal clearance issues

83

Important note about absorption of Ziprasidone and Lurasidone?

take with food! 50% better absorption!