Antipsychotics Flashcards

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1
Q

Typical antipsychotics mechanism

A

Da antagonists

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2
Q

Atypical antipsychotics mechanism

A

Da and 5HT2A antagonists

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3
Q

Four dopaminergic pathways and their function

A

Nigrostriatal –extrapyramidal motor function
Mesolimbic – reward and emotional behavior
Mesocortical - cognition
Tuberoinfundibular – inhibits the secretion of prolactin

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4
Q

Classification of the typical antipsychotics by potency

A
Low Potency (High Ach, M1, A1 blockade)
Chlorpromazine
Perphenazine (Mid level)
Fluphenazine
Haloperidol
High potency (low Ach, H1, A1 blockade)
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5
Q

Therapeutic use of the typical antipsychotics

A

Schizophrenia, schizoaffective disorder, delusional disorder, brief psychotic disorder.

Mood disorders: bipolar and mdd with psychotic features
Delirium
Violent behavior/agitation

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6
Q

Which two typical antipsychotics have a decanoate preparation?

A

Haloperidol and fluphenazine

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7
Q

Typical antipsychotic side effects

A

Extrapyramidal movements
Negative symptom increase
Prolactin levels rise (gynecomastia)

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8
Q

Which antipsychotics carry the greatest risk of EPS, TD, and neuroleptic malignant syndrome?

A

High potency (haloperidol and Fluphenazine)

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9
Q

How to treat EPS from typical antipsychotics

A

antimuscarinics (trihexylphenadyl, DA agonists)

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10
Q

Acute dystonia

A

Happens from typical antipsychotics, treat with anticholinergics

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11
Q

Akathisia, treatment

A

Subjective feeling of inner restlessness, give beta blockers, benzodiazepines, anticholinergics

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12
Q

Tardive dyskinesia, treatment

A

In 5% of patients on antipsychotics chronically. Continuous writing movements of tongue mouth fingers hands and sometimes feet. Common with high potency antipsychotics. Treat by stopping or switching the antipsychotic, increasing dose will help temporarily.

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13
Q

Neuroleptic malignant syndrome

A

Life threatening reaction from antipsychotics that can cause eps along with autonomic symptoms. Increased WBC, CPK, LFT. Happens more in young males.

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14
Q

Blockade of A1 receptors causes

A

Orthostatic hypotension, dizziness, priapism

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15
Q

Cardiac effects of antipsychotics

A

Can prolong the QT interval, cause PVCs, and sudden death

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16
Q

Atypical antipsychotic mechanism

A
Serotonin and dopamine antagonists. 
D2 antagonists with rapid dissociation
D2 partial agonists
Serotonin partial agonist at 5HT1A
Serotonin antagonist at 5HT2A
17
Q

How do 5HT2A antagonists stimulate DA release

A

They prevent serotonergic activation of Gaba interneurons that usually inhibit DA release, so there is a better balance of Dopamine released, so EPS aren’t bad

18
Q

Why are atypical antipsychotics better than typicals?

A

because they don’t any extrapyramidal side effects, thanks to the inhibition of gabaergic interneurons, so more better balance of DA.
Also, reduced risk of hyperprolactinemia
cognitive enhancement
improved adherence

19
Q

D2 antagonists with rapid dissociation

A

Hit and run, so the block isn’t too long lasting.

20
Q

Aripiprazole

A

D2 partial agonist
5HT1a partial agonist
5HT2A antagonist

really tunes control of dopamine

21
Q

Clozapine

A

More effective than all other antipsychotics, so it’s the drug of choice for treatment-resistant schizophrenics. Low D2 antagonism, but causes metabolic syndrome the most by blocking 5HT2C receptors in the hypothalamus and can cause agranulocytosis

22
Q

Risperidone

A

At therapeutic doses, occupies close to 100% of the 5HT2 receptors, but only 65% of the D2 receptors. Highest risk of the atypicals to cause extrapyramidal side effects

23
Q

Highest risk of EPS among atypical antipsychotics

A

Risperidone

24
Q

Biggest adverse effects of typicals vs atypicals

A

EPS and TD vs Weight gain, diabetes, CVD, dyslipidemia

25
Q

Metabolic syndrome

A

Visceral Obesity
Insulin Resistance
Dyslipidemia (high triglycerides, low HDL)
Hypertension

26
Q

Atypicals that cause the most weight gain

A

Clozapine and olanzapine

27
Q

Which atypical causes agranulocytosis?

A

ANC <500, clozapine – must increase gradually and check a CBC weekly

28
Q

Atypical antipsychotics that we need to know

A

Aripiprazole, Risperdone, Clozapine, Olanzapine, Quetiapine, Ziprasidone

29
Q

Atypical antipsychotics off label use

A

For dementia related psychosis (this can increase mortality in elderly)

30
Q

What type of symptoms are atypicals best for?

A

Negative symptoms

31
Q

Which drug is used to treat agitation in the medically sick?

A

Haloperidol

32
Q

First line, second line

A

First line: Atypicals (aripiprazole, quetiapine, ziprasidone, risperdone)
Second line : Clozapine and olanzapine
Thirdline: typicals