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Pharm - Psychiatry > Antipsychotics - SGA's > Flashcards

Antipsychotics - SGA's Flashcards

(58 cards)

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1
Q

Name the SGA’s

A

Clozapine

Risperidone
Ziprasidone
Iloperidone
Paliperidone
Lurasidone

Olanzapine
Asenzapine
Quetiapine

Aripiprazole

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2
Q

Which SGA is the first “atypical” antipsychotic and what was special about it?

A

Clozapine

It didn’t given EPS/Tardive Dyskinesia

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3
Q

What’s unique about Aripiprazole?

A

Partial Agonist MOA

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4
Q

Describe receptor binding for clozapine.

A

Receptor binding of 5HT2 is 10x stronger than DA blocking

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5
Q

Describe receptor binding for olanzapine and quetiapine

A

Similar binding affinities for 5HT2 and D2

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6
Q

Describe receptor binding for risperidone and ziprasidone

A

There’s greater 5HT2C antagonism

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7
Q

What is the 5HT-DA antagonism hypothesis?

A

Blocking presynaptic 5-HT2A gives inc DA release in basal ganglia (nigrostriatal system)

The DA competes with the antipsychotic medication for D2 receptors

Simultaneous antagonism of DA and 5-HT2 results in a net dec of the degree to which D2 receptors are blocked in the striatum - leads to dec EPS/tardive dyskinesia

*most clearly noticed at low doses

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8
Q

What is the hit and run hypothesis?

A

Minority view
DA blockade is “loose” and doesn’t last long enough to give DA side effects (but lasts long enough to give antipsychotic effect)

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9
Q

What 2 medications does the Hit and Run hypothesis apply to?

A

Clozapine and Quetiapine

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10
Q

Which SGA doesn’t have significant anti-histaminic effects?

A

Risperidone

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11
Q

Which SGAs don’t have anti-muscarinic/anti-cholinergic side effects?

A

Risperidone and Ziprasidone

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12
Q

Which SGA doesn’t really have Metabolic syndrome side effects?

A

Ziprasidone

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13
Q

Which SGAs don’t really have EPS and hyperprolactinemia?

A

Quetiapine and Clozapine

*Thus it supports the hit and run hypothesis

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14
Q

What symptoms are seen in metabolic syndrome?

A

Weight gain, hyperglycemia, diabetes mellitus, dyslipidemia

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15
Q

With metabolic syndrome, there is an increased rate of what disease?

A

Cardiovascular Disease

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16
Q

What are the top 2 SGAs that give weight gain?

A

Clozapine and Olanzapine

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17
Q

What SGA’s don’t really have weight gain as an issue?

A

Ziprasidone, Aripiprazole, Lurasidone, Asenapine

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18
Q

Which SGA is a partial agonist?

A

Aripiprazole

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19
Q

What is the Rheostat analogy?

A

Says that the receptor is neither completely on or off - the drug is changeable depending on amount of receptor stimulation

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20
Q

According to the rheostat analogy, in a low neuroreceptor stimulation environment, what happens

A

With the partial agonist there’s little AGONIST

activity (the cell isn’t completely OFF)

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21
Q

According to the rheostat analogy, in a high neuroreceptor stimulation environment, what happens

A

With the partial agonist there’s little ANTAGONIST activity (the cell isn’t completely ON)

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22
Q

What does Aripiprazole do in low DA environments?

A

Binds to D2 receptors with high affinity and acts as agonist

Keeps

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23
Q

What does Aripiprazole do in high DA environments?

A

Binds/blocks D2 recetors and acts as antagonist

Keeps >65% but

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24
Q

What is the first DA-5HT system stabilizer?

25
When is Clozapine used?
3rd line treatment used after failure of at least 2 other antipsychotics
26
Which medication is high risk and high reward? What does this mean?
Clozapine
27
How is Clozapine high reward?
High reward - More effective than any other medications in treatment resistant patients as well as reducing suicide risk, also helps with negative symptoms (may even with treating tardive dyskinesia )
28
How is Clozapine high risk?
High risk - serious side effects associated with it
29
What are common side effects of Clozapine?
Sedation Weight gain Metabolic syndrome Anti-chilinergic
30
What are rare/serious side effects of Clozapine?
AGRANULOCYTOSIS - bone marrow stops producing wbcs Myocarditis Dec seizure threshold (aka inc seizure risk)
31
Asenapine has an increased risk of?
EPS
32
QTc elongation is seen with which meds?
Thioridazine (FGA) > Ziprasdisone (SGA) > others
33
Top 2 for sedation are?
Clozapine and Olanzapine
34
NMS (Neuroleptic Malignant Sydrome) is a rare side effect of what drugs?
FGAs SGAs MEtoclopramide Prochlorperazine
35
What happens with NMS (Neuroleptic Malignant Sydrome)?
``` DA system goes haywire Mental status changes/confusion Rigidity (tremor and inc CPK) Fever > 40 degrees Celsius Dysautonomia (inc HR, BP change, inc RR, hypoxia) ```
36
Is inc CPK diagnostic for NMS?
Not by itself | It helps gauage how severe the NMS is
37
How long does it take for NMS to resolve?
7-10 days
38
How do you treat NMS?
Stop the medication! | Supportive therapy
39
What is a black box warning for SGAs and FGAs?
Risk of inc mortality (sudden death) in elderly who have dementia with psychosis Typically from CV or stroke
40
How do you alter SGA/FGA use in elderly?
Low dose (risk inc with higher doses) Minimize treathment length Use something else if possible
41
What population may be at an inc risk of sudden death with FGAs/SGAs?
Elderly | ex: nursing homes
42
Describe PK (bioavailability) of FGAs/SGAs
IM > PO | PO gives incomplete absorption and first pass effect
43
Peak plasma level for FGAs/SGAs in IM vs PO
``` IM = 30 min PO = 1-4 hrs ```
44
Protein binding of FGAs/SGAs?
90% protein bound Unbound passes thru BBB *is very lipid soluble
45
FGAs/SGAs are stored where?
In body fat
46
Half life of FGAs/SGAs? Steady state?
Half life of 20 hours | Steady state 4-7 days
47
What's the exception to half lives for SGAs and what is it's half life?
Aripiprazole | Has a long half life of about 3 days
48
Clozapine is used for?
Refractory schizo
49
EPS side effects and inc prolactin is dose dependent for?
Risperidone and Paliperidone
50
Inc qTc interval is a concern with?
Ziprasidone
51
Akathisia is a concern with?
Lurasidone (and Aripiprazole)
52
Which drug is only available as a sublingual form?
Asenapine
53
Long acting injectable form is seen with?
Aripiprazole Risperidone/Paliperidone Haldol (FGA) Flufenazine (FGA)
54
Risperidone is metabolized to?
Palliperidone
55
Palliperidone is used for?
Liver disease b/c 80% renal excretion
56
Ziprasidone and Lurasidone are taken with ___?
Food b/c 50% better absorption
57
If less than 80% nigrostriatal D2 receptors are blocked, then?
Reduced/No EPS
58
If less than 80% tuberoinfundibular D2 receptors are blocked, then?
Decreased/No hyperprolactinemia

Pharm - Psychiatry (6 decks)

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