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📖PHARM: Psych, RA & Gout > 2-18 Anti-Psychotics > Flashcards

2-18 Anti-Psychotics Flashcards

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1
Q

A: Mesolimbic DA system

B: Which symptoms is this system associated with?



A

A: DA neurons from VTA -> subcortical structures of the brain (NA)
B: Psychotic symptoms

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2
Q

A: Nigrostriatal DA system

B: Which symptoms is this system associated with?

A

A: DA neurons from [Substantia nigra: compacta] -> striatum

B: Extrapyramidal Side Effects (EPS)

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3
Q

A: Mesocortical DA system

B: Which symptoms is this system associated with?

A

A: DA from VTA -> frontal cortex

B: Negative symptoms (and part of positive symptoms)

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4
Q

A: Tuberoinfundibular DA system

B: Which symptoms is this system associated with?

A

A: DA neurons projecting from the hypothalamus to the [ant. Pituitary]

B: Hyperprolactinemia and associated adverse effects

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5
Q

Other names for FGAs (First Generational Antipsychotics) (4)

A
  1. Major tranquilizers,
  2. Neuroleptics,
  3. [conventional antipsychotics],
  4. [Typical antipsychotics]
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6
Q

List the types of FGAs (3)

A
  1. Phenothiazines
  2. Thioxanthines
  3. Butyrophenones
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7
Q

Examples of Phenothiazine FGAs (5)

A

-azine

  1. Chlorpromazine
  2. Thioridazine
  3. Perphenazine
  4. Trifluoperazine
  5. Fluphenazine
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8
Q

Examples of Thioxanthine FGAs

A

Thiothixene

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9
Q

Examples of Butyrophenone FGAs

A

Haloperidol

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10
Q

List the Low Potency FGAs (2)

A

“Cheating Thieves are Low”

  1. Chlorpromazine
  2. Thioridazine
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11
Q

List the Middle Potency FGAs (2)

A
  1. Perphenazine
  2. Thiothixene
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12
Q

A: List the HIGH Potency FGAs (3)

B: Which of these has the highest affinity for D2 receptors?

A

“Try to Fly High”

A:

  1. Trifluperazine
  2. Fluphenazine
  3. Haloperidol = Binding affinity for D2 receptor is 10x greater than any other receptor
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13
Q

Which FGAs can be administered as Long acting injectables (2)

A
  1. Haloperidol
  2. Fluphenazine
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14
Q

Anti-Psychotic Indications (8)

A

OMASTABA!

  1. [Autism in children/adolescents]
  2. Bipolar DO (Acute mania/Maintenance/Depression)
  3. Agitation 2° to Schizophrenia vs. bipolar
  4. Schizophrenia (acute & maintenance)
  5. [Med-induced Psychosis] (Delirium/Dementia/Substance induced Psychosis)
  6. Tourette’s
  7. OCD
  8. Anxiety disorder
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15
Q

[Low Potency FGA] Side Effects (4)

A
  1. [ExtraPyramidalSx] / Tardive Dyskinesia
  2. Hyperprolactinemia
  3. [Muscarinic vs. A1 adrenergic] Effects
  4. Histamine Effects
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16
Q

[HIGH Potency FGA] Side Effects (2)

A
  1. [ExtraPyramidalSx] / Tardive Dyskinesia
  2. Hyperprolactinemia
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17
Q

A: Why is IM route for Anti-Psychotics a more effective route than PO? (2)

B: Describe Anti-Psychotic Protein binding

C: Describe Anti-Psychotic Solubility

A
  1. Poor GI absorption
  2. [Hepatic first-pass effect]

B: 90% Protein bound (the 10% unbound crosses BBB)

C: VERY LIPID SOLUBLE –> STORED IN FAT and slowly removed

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18
Q

Anti-Psychotics Half-Life

A

20 hours (at steady state, half life = 4-7 days)

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19
Q

MOA for FGA Therapeutic Effect

A

occurs [when >65% of [Mesolimbic DA2 receptors] are BLOCKED]

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20
Q

MOA for FGA [ESP Side Effects]

A

occurs [when >80% of [Nigrostriatal DA2 receptors] are BLOCKED]

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21
Q

MOA for FGA [Hyperprolactinemia Side Effects]

A

occurs [when >80% of [Tuberoinfundibular DA2 receptors] are BLOCKED]

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22
Q

A: List components of [Drug induced Parkinsonism] (4)

B: What are the other 2 components of EPS?

A

EPS = DAD

  1. [Drug induced Parkinsonism]
  2. Dystonia
  3. Akathisia

A: [Drug induced Parkinsonism]= PARK = [Pill rolling tremor] / [Areflexia posturally –> Falls] / [Rigidity Cogwheel] / [Kinesia (bradykinesia)]

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23
Q

A: List components of Dystonia (3)

B: What are the other 2 components of EPS? (2)

A

EPS = DAD

  1. [Drug induced Parkinsonism]
  2. Dystonia
  3. Akathisia

A: Dystonia:

  • Sustained muscle spasm–>Abnormal twisted posture
  • Exacerbated with activity
  • Demographic: Young males
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24
Q

A: List components of Akathisia (2)

B: What are the other 2 components of EPS? (2)

A

EPS = DAD

  1. [Drug induced Parkinsonism]
  2. Dystonia
  3. Akathisia

A: Akathisia: Sense of restlessness (typically legs) with need to move. Mistaken for agitation

-Demographic: Women

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25
Q

A: What is Tardive Dyskinesia

B: What area of the body is most commonly affected?

A

A: Abnormal involuntary mvmnt that typically does not remit even after drug cessation.

B: Facio-Masticatory-Oro-lingual

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26
Q

Effects of Hyperprolactinemia (4)

A
  • Galactorrhea/lactation
  • Gynecomastia
  • DEC GnRH –> [DEC LH & FSH] –> [Irregular menstruation & infertility]
  • Osteopenia
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27
Q

Effects of Antipsychotics blocking [Muscarinic System] (Effect of Anticholinergic action) (5)

A

can’t see, can’t spit, can’t pee, can’t shit, can’t think

[Blurred vision / Dry Mouth / Urinary Retention / Constipation / Confusion]

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28
Q

Effects of Antipsychotics blocking [A1 Adrenergic System]

A

Orthostatic hypOtension –> Fall Risk!

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29
Q

Effects of Antipsychotics binding to [Histamine Receptors] (2)

A

Sedation vs. Wt.Gain

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30
Q

Describe Neuroleptic Malignant Syndrome

A

RARE SE of Any Dopamine Blocker (Antipsychotics vs. GI meds) that –> FEVER

  • [Fever > 40C]
  • Encephalopathy (Confusion)
  • Vitals unstable (INC HR / RR / BP from autonomic dysfunction)
  • Enzymes INC (CPK)
  • Rigitidy INC (Tremor)
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31
Q

Risk Factors for Sudden Death when taking Antipsychotics (4)

A
  1. Dementia –> Death from Stroke when taking Antipsychotics
  2. Higher doses
  3. Prior CV Dz
  4. Black Box Warning
32
Q

List the Atypical [SGAs - Second Generational Antipsychotics] (10)

A

It’s atypical for old pale clozets to quietly risper from AA to Z

  • Olanzapine
  • Paliperidone (Metabolite of Risperidone​)
  • Clozapine
  • Quetiapine
  • Risperidone
  • Aripiprazole & Asenapine
  • ZiL - Ziprasidone / iLoperidone / Lurasidone
33
Q

Which SGA works as a partial agonist

A

Aripiprazole

34
Q

A: Which SGA is a [High Risk / High Reward] Drug? What is its indication?

B: What are the common Side effects of this SGA (3)

C: Dangerous Side Effects (3)

D: Explain the Reward component of this SGA

A

A: Clozapine = [3rd Line Schizophrenia tx]

B: [Sedation / Anticholinergic / metabolic syndrome]

C:

  • Agranulocytosis (1-2% of pts)
  • Myocarditis
  • INC Seizures

D: Treats negative sx (tardive dyskinesia / suicide / treatment resistant schizophrenia)

35
Q

Which SGAs can be administered as Long acting injectables (4)

B: Which of these are excreted via RENAL

A

“OPRAH”

  1. Risperidone
  2. Paliperidone (Metabolite of Risperidone)
  3. Olanzapine
  4. Aripiprazole

B: Paliperidone = SHOULD NOT BE USED IN RENAL FAILURE PTS

Haloperidone = FGA is also long acting injectable

36
Q

Which SGAs should be taken with food for better absorption? (3)

A

“PLZ take with food!”

  1. Ziprasidone
  2. Lurasidone
  3. Paliperidone
37
Q

Which SGA is sublingual

A

ASenapine

38
Q

A: MOA for Aripiprazole (2)

B: Explain its binding affinity with [low vs. High Dopamine] environments

A
  • Partial agonist tht sits on receptor & blocks the receptor from other stimulation but also partially turns it on
  • Changes the receptor conformation slightly (G protein organization changes)

B:

  • In low DA receptor stimulation environment, binds DA2 receptor with HIGH AFFINITY & has partial agonist effect
  • In high DA stimulation environment, exerts antagonist action
39
Q

A: Side Effect for [Aripiprazole AND Lurasidone]

B: Half life for Aripiprazole

A

“Arielle & Lura are restless studiers!”

A: Akathisia (restlessness)

B: 3 Days (longest out of the SGAs)

40
Q

A: MOA for [SGA: Serotonin Dopamine Dual Antagnoism]

B: Why does this enhance Cortical Function

C: What Radiographic Tool supports this Hypothesis

A

A: 5HT2A blockade in [Mesolimbic/ Nigrostriatal / Tuberoinfundibular] tract (blocking yellow piece) —> DA release (blue bullets) from BG: This DA competes with antipsychotic mediation (black sphere) for DA2 receptors –> DEC EPS

B: Mesocortical: 5HT2A blockade may normalize cortical function (possibly by enhancing DA release and ACh release in frontal cortex, thereby reducing negative symptoms/ cognitive deficit

C: PET Scan

41
Q

MOA for [SGA: Hit & Run Concept]

A

Lower potency DA2 blockade by atypical antipsychotics –> loose receptor blockade with shorter-lasting effect. Effect is present long enough to have antipsychotic therapeutic effect

42
Q

Which two drugs delineate evidence of the [SGA: Hit & Run Concept]

A

[Clozapine & Quetiapine] have the lowest incidence of EPS or Tardive Dyskinesia

43
Q

Relative effects on nigrostriatal system by SGAs (5)

A

Risperidone > [Ziprasidone = Olanzapine] > Quetiapine > Clozapine

44
Q

Relative effects on tuberoinfundibular system by SGAs (5)

A

Risperidone > [Ziprasidone = Olanzapine] > Quetiapine > Clozapine

45
Q

Relative effects on [A1 adrenergic system] by SGAs (5)

A

Clozapine > [Olanzapine = Quetiapine = Risperidone] > Ziprasidone

46
Q

A: Relative effects on [M1 muscarinic system] by SGAs (4)

B: Which SGAs do NOT have an affect on this system (5)

A

A: Clozapine > Olanzapine > Quetiapine > Iloperidone

B: NOT: Risperidone, Aripiprazole, Asenapine, Ziprasidone, Lurasidone

47
Q

Relative effects on H1 system by SGAs (4)

A

Clozapine > Quetiapine > Olanzapine = Ziprasidone

48
Q

Relative effects on metabolic syndrome by SGAs (5)

A

[Clozapine = Olanzapine] > [Quetiapine = Risperidone] > Ziprasidone

49
Q

Which antipsychotics cause QT elongation (2)

A

“QT elongated by TZ”

Thioridazine > Ziprasidone

50
Q

From Greatest to least, list SGAs that cause sedation (4)

A

Clozapine > Olanzapine > Quetiapine > [Risperidone/Paliperidone]

51
Q

3 SGAs that cause the greatest weight gain

A

“i Cause Obesity”

iLoperidone / Clozapine / Olanzapine

Clozapine & Olanzapine cause [Metabolic Syndrome] as well

52
Q

Side Effects of [SGA: Asenapine]

A

High H1 and a1 binding –> [sedation & orthostasis]

53
Q

Which SGA causes the most D2 mediated SEs

A

Risperidone

54
Q

Which SGA causes the least D2 mediated SEs

A

Clozapine

55
Q

Which SGA causes the least [A1 adrenergic] mediated SEs

A

Ziprasidone

56
Q

Which SGA causes the MOST [A1 adrenergic] mediated SEs

A

Clozapine

57
Q

Which SGAs cause the least M1 mediated SEs (2)

A

Risperidone and Ziprasidone

58
Q

Which SGAs cause the MOST M1 mediated SEs (2)

A

Clozapine

59
Q

Which SGA causes the least H1 mediated SEs

A

Risperidone

60
Q

Which SGA causes the MOST H1 mediated SEs

A

Clozapine

61
Q

Which SGA causes the least metabolic syndrome SEs (3)

A

Ziprasidone, Molazodone, Ariprazole

62
Q

Which SGA causes the MOST metabolic syndrome SEs (2)

A

Clozapine and Olanzapine

63
Q

A: High binding SEs of Risperidone (2)

B: Which receptor causes this

A

A:

  1. INC Prolactin
  2. EPS

B: [A1 adrenergic]

64
Q

low binding SEs of Risperidone

A

NONE

65
Q

A: High binding SEs of Clozapine (2)

B: Which receptors are blocked (3)

A

A:

  1. Wt Gain
  2. Metabolic Syndrome

B: [A1 adrenergic] / M1 / H1

66
Q

Which antipsychotic DOES NOT cause EPS

A

Clozapine

67
Q

A: High binding SEs of Olanzapine (2)

B: Which Receptors are blocked (2)

A

A:

  1. Wt. Gain
  2. Metabolic Syndrome

B: [A1 adrenergic] / H1

68
Q

low binding SEs of Olanzapine

A

EPS

69
Q

Which receptors does Quetiapine block at High concentrations? (2)

A

[A1 Adrenergic] & H1

70
Q

low binding SEs of Quetiapine

A

EPS (has very low incidence of EPS or Tardive Dyskinesia 2º to HIt & Run Concept)

71
Q

Which receptors does Asenapine block at High concentrations? (2)

A

[A1 Adrenergic] & H1

72
Q

low binding SEs of Asenapine

A

[Metabolic Syndrome from M1 Blockade]

73
Q

A: HIGH binding SEs of iLoperidone

B: Moderate binding SEs of iLoperidone (2)

A

A: None

B: [A1 Adrenergic blockade] & [Wt. Gain]

74
Q

low binding SEs of iLoperidone (3)

A
  1. EPS
  2. H1 blockade
  3. Metabolic Syndrome
75
Q

What’s the ideal therapeutic window when blocking dopamine receptors? (in terms of % of receptors blocked)

A

60-80% blockage of D2 receptors

> 60% (needed to therapeutically affect mesolimbic tract)

<80% (above which you cause adverse effects)

📖PHARM: Psych, RA & Gout (6 decks)

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