Antipsychotic Flashcards by Nicole Gaudreau

What are the two classes of antipsychotics?

First generation = “conventional” or “typical”

Second generation = “atypical”

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What are the pathways associated with antipsychotic efficacy?

Hyperactivity of DA neurons in the mesolimbic pathway

Deficiency of DA in the mesocortical pathway

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Which Da pathway are positive and negative sx?

Mesolimbic = positive
Mesocortical = negative

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What receptors do most antipsychotic medications target?

D2 blocker

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What receptors do antipsychotics block?

Histamine-1
Alpha-1
Muscarinic cholinergic

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What motor SE are produced from antipsychotics?

EPS

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What happens if we block the mesolimbic pathway?

Improve positive sx of schizophrenia

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What happens if we block the mesocortical pathway?

Worsening of negative sx (cognitive slowing/blunting)

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What happens if we block the nigrostriatal pathway?

EPS

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What happens if we block the tuberoinfundibular pathway?

Increase in prolactin/ hyperprolactinemia

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What does EPS include?

Dystonia
Akathisia
Pseudoparkinsonism
TD

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When is EPS more common?

FGA

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What is acute dystonia?

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

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What is the treatment of acute dystonia?

Removal of offending agent

Anticholinergics/benzo

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What is akathisia?

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

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What is the treatment of akathisia?

Removal of offending agent

Anticholinergic/propranolol

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What is pseudoparkinsonism?

Bradykinesia
Ridigity
Cogwheeling
Tremor

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What is the treatment of pseudoparkinsonism?

Removal of offending agent
Anticholinergics
Amantadine (DA)

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What is tardive dyskinesia?

Long-standing or permanent abnormal involuntary movements

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What is the treatment of TD?

Removal of offending agent

VMAT-2 inhibitors

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What is neuroleptic malignant syndrome (NMS)?

“lead pipe” rigidity
Fever
Autonomic instability
Elevated WBCs

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What is the treatment of NMS?

Removal of offending agent

Supportive care

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What drug causes QTc prolongation?

Haloperidol

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How are antipsychotics connected to mortality?

Increased mortality in elderly patients treated for dementia-related psychosis

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How long should antipsychotics be used?

Shortest duration possible

What is the MOA of second generation antipsychotics?

D2 antagonism plus "selectively modifying" effects of serotonin antagonism

What SE are reduced in second from first generation antipsychotics?

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

What are the SE of SGA?

Wt gain Diabetes Dyslipidemia

What is the most efficacious antipsychotic?

Clozapine

What are the CIs for clozapine?

H/o: Seizures Agranulocytosis

What are the warnings for clozapine?

Myocarditis Cardiomyopathy CHF

What are the SE of Clozapine

Orthostatic hypotension Sialorrhea/drooling Anticholinergic effects

What is the boxed warning for clozapine?

Agranulocytosis | Seizures

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

Must start back at 12.5mg and titrate slowly again

What is a normal ANC?

1000-1500

What ANC level warrants stopping clozapine therapy?

< 1,000

What is the biggest risk with olanzapine?

Cardiometabolic risks

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

Benzos

How do olanzapine and clozapine compare?

Pharmacologic profiles overlap

What is a SE of depot olanzapine?

Sedation-delirium syndrome requiring 3 hour post-injection monitoring

When is quetiapine preferred?

Patients with Parkinson's disease who require antipsychotic therapy

What common antipsychotic SEs are not in quetiapine?

No EPS | No prolactin elevation

How do we start quetiapine IR?

Titrate IR | Different activity at different doses

What do we monitor for quetiapine?

TSH

What is asenapine?

Related to mirtazapine chemically | Serotonin, H1, A2 and D2

How is asenapine available?

SL tab (does not work if swallowed)

What must we monitor for with asenapine?

Allergic rxn

What is a SE of risperidone?

Increased prolactin

How is risperidone related to EPS?

Administration | Dos dependent

How are risperidone/paliperidone adjusted?

renally

What special form does risperidone come in?

Long acting injectable - every 2 weeks

What is the active metabolite of risperidone?

Paliperidone

Is risperidone or paliperidone more tolerable?

Paliperidone

How is paliperidone dosed?

Once daily

How often is paliperidone long acting injection administered?

Day 1, day 8, then q4wk

Does risperidone or paliperidone need a po overlap?

Risperidone

How soon does paliperidone take for drug levels to appear?

1 day

What is the CI to ziprasidone?

QT prolongation

What are the warnings for Ziprasidone?

D/c if QT prolongation

What is the SE for ziprasidone?

Akasthesia

How is ziprasidone taken?

W/food (500 cals)

How is ziprasidone administered for acute use?

Which drug causes the most orthostatic hypotension?

Iloperidone

What happens if the pt misses 3 doses of iloperidone?

re-titrate

What is a SE of iloperidone?

QTc

What are the SE of lurasidone?

Little effect on wt gain, lipids, and BG

Which drug has the least impact on QTc?

Lurasidone

How is Lurasidone adjusted?

Renally

What enzyme is lurasidone a substrate for?

3A4

How is lurasidone taken?

With food

What is aripiprazole's MOA?

Partial dopamine 2 agonist

Is aripiprazole an activating or inactivating drug?

Activating

How do we dose adjust aripiprazole?

3A4/2D6 inducers/inhibitors

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

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

How many long acting injectables for aripiprazole are there?

2 completely different drugs

What is brexpiprazole?

Dopamine 2 receptor partial agonist

What is special about cariprazine?

Only agent with D3 preferring over D2 affinity | Dopamine 2 receptor agonist

What is the 1/2 life of cariprazine?

91 hours

When is cariprazine not used?

CrCl < 30

What is primvanserin?

Non-dopaminergic antipsychotic

What is the only FDA approved agent for PD psychosis?

Primvanserin

What cyp enzymes do many antipsychotics interact with?

1A2 (smoking) 2D6 3A4

What should be monitored with atypical antipsychotics?

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