Antipsychotics Flashcards by Jenna Foushee

All antipsychotics carry the risk of _____________.

QT prolongation

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What are the 2 classes of antipsychotics?

Typical/conventional (1st generation, FGA)

2. Atypical (2nd generation, SGA)

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What is EPS? What can EPS turn into?

Extra-pyramidal Symptoms from increase in ACh (Parkinsonian sx) - reversible movement disorders, such as tremor, rigidity, drooling, masked fascies, akinesia.
Can turn into tardive dyskinesia, which is irreversible.

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Explain the balance of DA and ACh.

When the body has too much DA, this decreases the amount of ACh. Anti-psychotic drugs decrease DA, thereby increasing ACh and inducing EPS.

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What is the father of the typical antipsychotics?

Chlorpromazine - it was an antihistamine that had antipsy properties

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What other binding properties do FGA have (other than D2)?

H1 blocking- Antihistamine - weight gain
Alpha-1 blocking - orthostatic hypotension
M1 blocking - Anticholinergic - anti-SLUDGE

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FGA are sometimes referred to as _______ or _______.

Neuroleptics, sedatives

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FGA drugs differ in degree of potency. Potency refer to binding capacity of __________ receptors.

Dopaminergic

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Most FGA have short/long half lives.

Long

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What is first dose phenomenon? How do you treat it?

Acute dystonic rxn

IV benztropine.

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What are the ways that you can treat EPS?

Decrease dose
Switch to a SGA
Switch to a low potency agent with high anticholinergic properties
Add an anticholinergic (Trihexyphenidyl, benztropine, diphenhydramine)

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Neuromuscular Malignant Syndrome is hallmarked by what 4 symptoms?

Hyperpyrexia (103-104)
Rigidity
Hyperactive
Increase in CPK from rhabdo

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How do you treat NMS?

D/C antipsychotic and consider dantrolene (muscle relaxer) and/or bromocriptine (DA agonist)

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What are the cons of the FGA?

EPS
Negative symptoms not treated well
Decreased adherence
Greater risk for tardive dyskinesia if on for prolonged period of time

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What are the pros of FGA?

Cheap

2. Multiple dosage forms

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Name a high potency FGA. What are 2 pros and 2 cons?

Haloperidol - Vitamin H
1. Highly potent sedative, used for agitation or sedation - calming effect without significant resp depression
2. Can clear quickly, good for elderly. (unlike benzos)
CON:
1. May lower sz threshold
2. QT prolongation

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Typical agents block the D2 receptor. Atypical agents are also called SGA. They block ____ and _____, which helps blunt ______ and treats ______ symptoms.

DA and 5HT2a
blunts EPS
treats negative

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What are the concerns raised over for SGA?

Metabolic adverse effects - weight gain, DM, dyslipidemia.

$$$$

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SGAs have more or less affinity for different receptors than FGAs.

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What are the pros of SGAs?

Improved adherance
reduced EPS in general
treats negative symptoms
starting to see different dosage forms

Quetiapine (Seroquel) treats what 3 issues at what doses?

“Quiet”

Low dose (50) - sleeping pill (hypnotic or sedation)
Medium dose (300)- depression
High dose (800) - antipsychotic

Quetiapine has a very low risk of ______ and _________, thereby making it a go-to SGA for this reason.

EPS

hyperprolactinemia (least risk)

What SGA can be used for bipolar disease?

Quetiapine

Risperidone

What are the pros and cons of Olanzapine?

Cons: 
Significant risk for metabolic effects
Pros:
Pretty good with negative symptoms
Low risk of EPS

Olanzapine is son of _________.

Clozapine, first SGA antipsychotic

________ is considered the gold standard for SGA, but it has 5 Black Box Warnings, so it is NOT first line.

Clozapine

What are the major pros/cons of Clozapine?

``` Pros: Low incidence of EPS, TD Very effective vs negative sx Cons: Risk of agranulocytosis 5 BBW ```

What do you need to monitor with Clozapine?

CBC for agranulocytosis- qweek for 1st 6mo, then every other week. max risk is 4-18 weeks after initiation of therapy

Name the 5 BBWs for Clozapine.

1. Agranulocytosis 2. Orthostatic hypotension 3. Seizures 4. Myocarditis/cardiomyopathy 5. Increased mortality in elderly with dementia related psychosis

What is the newer agent that could replace Clozapine because it has no risk of agranulocytosis?

Olanzapine (Zyprexa)

T or F. Risperidone and Paliperidone have similar characteristics. Why?

T | Paliperidone is a metabolite of Risperidone, so it carries the same risk of hyperprolactinemia

Does risperidone have a high or low risk for the following: EPS Metabolic abnormalities Hyperprolactinemia (sexual dysfunction, bone density)

Higher risk of EPS at higher doses Low risk of metabolic abnormalities *SIGNIFICANT risk for hyperprolactinemia*

Describe Lurasidone's risk for sedating/metabolic effects and EPS. Why is that way?

Low metabolic risk and Less sedating (L is for low) Greater risk for EPS ***Lack of anticholinergic properties = less sedation, more EPS

Aripiprazole has a lower/higher incidence of EPS, weight gain, prolactinemia, sedation and dyslipidemia. What else is it approved to treat?

- LOWER risk | - Augmenting SSRI/SNRIs for resistant major depressive disorder

What drug is a mood stabilizer that also has an indication for bipolar?

Lithium

T or F. Lithium has a high therapeutic index.

False - low - meaning it can become toxic easily

Lithium is a ______ with rapid absorption. What does this mean in regards to using charcoal in OD?

Metallic ion | CANNOT use charcoal

Lithium has an inverse relationship with Na. what does this mean?

Increased Na wasting will increase Li levels (and vice versa) - diuretics that waste Na will retain lithium level

What is the therapeutic level of Lithium? when do you check it?

0.4-1 mmol/L | AM trough

What are the 6 AEs of lithium? What is the heralding sign of too much lithium?

1. fine tremor*********** 2. Polys - uria, dipsia 3. Hypothyroidism (follow TSH to see if it gets high) 4. Weight gain 5. metallic taste 6. Rash

VPA is another mood stabilizer. What do you need to monitor (in general and in patients who develop lethargy, AMS, vomiting, hypothermia)

LFTs for hepatotoxicity (#1 AE) | Ammonia levels

What can you add in refractory cases of SZP or agitation?

VPA

What are the 4 Pearls?

1. ** SGAs Elderly >65 = higher risk of death from heart issues** 2. SGAs - Metabolic syndrome, esp in >65 3. Avoid in pregnancy, esp 3rd trimester 4. Aripiprazole is not a PPI.

What is the relationship between DA and prolactin?

DA hates prolactin. So some antipsychotics can cause hyperprolactinemia (decreased DA = increased prolactin)

Which SGAs carry the highest and lowest of hyperprolactinemia?

Highest - Risperidone, Paliperidone | Lowest - Quetiapine

Which SGAs have the highest and lowest risk of EPS?

``` Highest - Lurasidone (little anticholinergic properties) Higher risk at higher doses - R and P Low Risk - COQA Clozapine Olanzapine Quetiapine Aripiprazole ```

Which SGAs have the highest and lowest risk of metabolic AEs - weight gain, DM, dyslipidemia?

High risk - Clozapine, Olanzapine Mild risk - Quetiapine, R and P Low risk - Lurasidone, Aripiprazole

What are the other 2 SGA that we did not discuss?

Ziprasidone | Asenapine