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Antipsychotic Flashcards

1
Q

What are the two classes of antipsychotics?

A

First generation = “conventional” or “typical”

Second generation = “atypical”

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2
Q

What are the pathways associated with antipsychotic efficacy?

A

Hyperactivity of DA neurons in the mesolimbic pathway

Deficiency of DA in the mesocortical pathway

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3
Q

Which Da pathway are positive and negative sx?

A 
Mesolimbic = positive
Mesocortical = negative
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4
Q

What receptors do most antipsychotic medications target?

A

D2 blocker

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5
Q

What receptors do antipsychotics block?

A

Histamine-1
Alpha-1
Muscarinic cholinergic

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6
Q

What motor SE are produced from antipsychotics?

A

TD

EPS

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7
Q

What happens if we block the mesolimbic pathway?

A

Improve positive sx of schizophrenia

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8
Q

What happens if we block the mesocortical pathway?

A

Worsening of negative sx (cognitive slowing/blunting)

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9
Q

What happens if we block the nigrostriatal pathway?

A

EPS

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10
Q

What happens if we block the tuberoinfundibular pathway?

A

Increase in prolactin/ hyperprolactinemia

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11
Q

What does EPS include?

A

Dystonia
Akathisia
Pseudoparkinsonism
TD

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12
Q

When is EPS more common?

A

FGA

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13
Q

What is acute dystonia?

A

Muscular rigidity and cramping often involving the neck, tongue, and face

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14
Q

What is the treatment of acute dystonia?

A

Removal of offending agent

Anticholinergics/benzo

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15
Q

What is akathisia?

A

Subjective feeling of intense restlessness (shaking/twitching/fidgeting)

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16
Q

What is the treatment of akathisia?

A

Removal of offending agent

Anticholinergic/propranolol

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17
Q

What is pseudoparkinsonism?

A

Bradykinesia
Ridigity
Cogwheeling
Tremor

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18
Q

What is the treatment of pseudoparkinsonism?

A

Removal of offending agent
Anticholinergics
Amantadine (DA)

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19
Q

What is tardive dyskinesia?

A

Long-standing or permanent abnormal involuntary movements

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20
Q

What is the treatment of TD?

A

Removal of offending agent

VMAT-2 inhibitors

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21
Q

What is neuroleptic malignant syndrome (NMS)?

A

“lead pipe” rigidity
Fever
Autonomic instability
Elevated WBCs

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22
Q

What is the treatment of NMS?

A

Removal of offending agent

Supportive care

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23
Q

What drug causes QTc prolongation?

A

Haloperidol

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24
Q

How are antipsychotics connected to mortality?

A

Increased mortality in elderly patients treated for dementia-related psychosis

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25
Q

How long should antipsychotics be used?

A

Shortest duration possible

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26
Q

What is the MOA of second generation antipsychotics?

A

D2 antagonism plus “selectively modifying” effects of serotonin antagonism

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27
Q

What SE are reduced in second from first generation antipsychotics?

A

Reduced risk of causing EPS and TD
Do not raise prolactin levels
Improve negative symptoms more than conventional antipsychotics

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28
Q

What are the SE of SGA?

A

Wt gain
Diabetes
Dyslipidemia

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29
Q

What is the most efficacious antipsychotic?

A

Clozapine

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30
Q

What are the CIs for clozapine?

A

H/o:
Seizures
Agranulocytosis

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31
Q

What are the warnings for clozapine?

A

Myocarditis
Cardiomyopathy
CHF

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32
Q

What are the SE of Clozapine

A

Orthostatic hypotension
Sialorrhea/drooling
Anticholinergic effects

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33
Q

What is the boxed warning for clozapine?

A

Agranulocytosis

Seizures

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34
Q

What do we do if clozapine is interrupted for 2+ days?

A

Must start back at 12.5mg and titrate slowly again

35
Q

What is a normal ANC?

36
Q

What ANC level warrants stopping clozapine therapy?

37
Q

What is the biggest risk with olanzapine?

A

Cardiometabolic risks

38
Q

If olanzapine is given IM, what other medications should not be administered IM within an hour of each other?

39
Q

How do olanzapine and clozapine compare?

A

Pharmacologic profiles overlap

40
Q

What is a SE of depot olanzapine?

A

Sedation-delirium syndrome requiring 3 hour post-injection monitoring

41
Q

When is quetiapine preferred?

A

Patients with Parkinson’s disease who require antipsychotic therapy

42
Q

What common antipsychotic SEs are not in quetiapine?

A

No EPS

No prolactin elevation

43
Q

How do we start quetiapine IR?

A

Titrate IR

Different activity at different doses

44
Q

What do we monitor for quetiapine?

45
Q

What is asenapine?

A

Related to mirtazapine chemically

Serotonin, H1, A2 and D2

46
Q

How is asenapine available?

A

SL tab (does not work if swallowed)

47
Q

What must we monitor for with asenapine?

A

Allergic rxn

48
Q

What is a SE of risperidone?

A

Increased prolactin

49
Q

How is risperidone related to EPS?

A

Administration

Dos dependent

50
Q

How are risperidone/paliperidone adjusted?

51
Q

What special form does risperidone come in?

A

Long acting injectable - every 2 weeks

52
Q

What is the active metabolite of risperidone?

A

Paliperidone

53
Q

Is risperidone or paliperidone more tolerable?

A

Paliperidone

54
Q

How is paliperidone dosed?

A

Once daily

55
Q

How often is paliperidone long acting injection administered?

A

Day 1, day 8, then q4wk

56
Q

Does risperidone or paliperidone need a po overlap?

A

Risperidone

57
Q

How soon does paliperidone take for drug levels to appear?

58
Q

What is the CI to ziprasidone?

A

QT prolongation

59
Q

What are the warnings for Ziprasidone?

A

D/c if QT prolongation

60
Q

What is the SE for ziprasidone?

A

Akasthesia

61
Q

How is ziprasidone taken?

A

W/food (500 cals)

62
Q

How is ziprasidone administered for acute use?

63
Q

Which drug causes the most orthostatic hypotension?

A

Iloperidone

64
Q

What happens if the pt misses 3 doses of iloperidone?

A

re-titrate

65
Q

What is a SE of iloperidone?

66
Q

What are the SE of lurasidone?

A

Little effect on wt gain, lipids, and BG

67
Q

Which drug has the least impact on QTc?

A

Lurasidone

68
Q

How is Lurasidone adjusted?

69
Q

What enzyme is lurasidone a substrate for?

70
Q

How is lurasidone taken?

71
Q

What is aripiprazole’s MOA?

A

Partial dopamine 2 agonist

72
Q

Is aripiprazole an activating or inactivating drug?

A

Activating

73
Q

How do we dose adjust aripiprazole?

A

3A4/2D6 inducers/inhibitors

74
Q

What SE do we not need to worry about with aripiprazole?

A

Relatively nonsedating
Reduced EPS
Little impact on BG, lipids, wt

75
Q

How many long acting injectables for aripiprazole are there?

A

2 completely different drugs

76
Q

What is brexpiprazole?

A

Dopamine 2 receptor partial agonist

77
Q

What is special about cariprazine?

A

Only agent with D3 preferring over D2 affinity

Dopamine 2 receptor agonist

78
Q

What is the 1/2 life of cariprazine?

79
Q

When is cariprazine not used?

80
Q

What is primvanserin?

A

Non-dopaminergic antipsychotic

81
Q

What is the only FDA approved agent for PD psychosis?

A

Primvanserin

82
Q

What cyp enzymes do many antipsychotics interact with?

A

1A2 (smoking)
2D6
3A4

83
Q

What should be monitored with atypical antipsychotics?

A 
Hx
Vitals
Waist circumference
FBG
A1c
Lipid profile
QTc
Prolactin
Electrolytes
Renal function
Liver function
CBC

Psych (9 decks)

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