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Neuro Quiz 2 > Antipsychotics > Flashcards

Antipsychotics Flashcards

1
Q

NT most frequently implicated in schizophrenia?

A

Dopamine

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2
Q

All effective anti-psychotic drugs are:

A

antagonists at the D2 dopamine receptors

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3
Q

Paranoid delusions occurs when

A

increased level synaptic DA (caused by psychostimulants)

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4
Q

Antipsychotics block

A

D2 receptors upon exposure but effects aren’t seen for several days

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5
Q

Positive Symptoms

A

Reflect an increase in the presence of abnormal behaviors

  • Hallucinations
  • Delusions
  • Thought disorder
  • Movement disorder
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6
Q

Negative Symptoms

A

Refer to an absence of normal behaviors found in healthy individuals

  • Loss of interest
  • Appearing to lack emotion
  • Reduced ability to plan or carry out activities
  • Neglect personal hydiene
  • Social withdrawal
  • Loss of motivation
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7
Q

Cognitive Symptoms

A

Problems with thought process

  • Making sense of information
  • Difficulty paying attention
  • Memory
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8
Q

Mesolimbic Dopaminergic Pathways

A

Significant improvement in positive symptoms due to D2 receptor blockade

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9
Q

Mesocortical Dopaminergic Pathway

A

Little or no improvement in negative and cognitive symptoms

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10
Q

Striatal Dopaminergic Pathway

A

EPS and Tardive Dyskinesia Side effects

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11
Q

Tuberoinfundibular Dopaminergic Pathways

A

Increased release of prolactin

side effect of D2 antagonists

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12
Q

1st Generation Antipsychotics Hit & structure

A

D2, H1, M1 and alpha 1

Phenothiazine Tricyclic Nucleus

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13
Q

Histamine H1 Receptor Blocker Causes

A

Wight gain

Drowsiness

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14
Q

Acetylcholine M1 Receptor Blocker Causes

A

Constipation
Blurred vision
Dry mouth
Drowsiness

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15
Q

Alpha 1 Adrenergic Receptor Blocker causes

A

Dizziness
Drowsiness
Decreased blood pressure

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16
Q

Chlorpromazine

A

Thorazine

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17
Q

Chlorpromazine is

A

Prototype
Low D2 antagonists
H1, M1, alpha 1, and D2

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18
Q

Thioridazine

A

Mellaril

First drug used in treatment of schizo

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19
Q

Thioridazine blocks what

A

Low D2 potency
Good anti-dopaminergic activity (so high EPS and high prolactin)
High anti-cholinergic

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20
Q

Down side to thioridazone?

A

PROLONGATION OF QT INTERVAL

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21
Q

Fluphenazine

A

Prolixin

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22
Q

Fluphenazine blocks what

A

High D2 blockage

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23
Q

Upside fluphenazine

A

Reduced sedation, anticholinergic, and hypoTN

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24
Q

Downside to Fluphenazine

A

Still significant EPS and prolactin

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25
Q

Thiothixene Structure change

A

Thioxanthene Tricyclic Nucleus

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26
Q

Thiothixene

A

Navane

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27
Q

Thiothixene blocks

A

D2

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28
Q

Upside to Thiothixene

A

Reduced sedative, anticholinergic and hypoTN

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29
Q

Haloperidol structure change

A

Butyrophenones

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30
Q

Haloperidol

A

Haldol

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31
Q

Haloperidol is used as

A

potent antipsychotic

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32
Q

Upside to Haloperidol

A

Reduced sedative, anticholinergic and hypoTN

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33
Q

Downside to Haloperidol

A

Significant EPS and Prolactin

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34
Q

Therapeutic Actions of Classical Gen 1 Antipsychotics

A 
Reduced positive symptoms (reduced hallucinations/delusions and disorganized thoughts)
Sedation
Reduced agitation, tension, aggression
Improved motivation
Require 2-6 weeks!
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35
Q

Acute Effect of Antipsychotics

A

Block D2 receptors which causes negative inhibitory feedback on presynaptic release to be compromise
Other DA receptors are stimulation
So overall reduction in DA NT is blunted

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36
Q

Chronic effect of Antipsychotics

A

D2 receptors are blocked and there is limited negative feedback
DA storage and release overwhelmed or depolarization blockade comprises activity
DA NTransmission is decreased even futher

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37
Q

Parkinson’s Disease Leads to EPS how?

A

Dopaine agonist blocks dopamine from binding GABA which leads to symptoms

38
Q

Antipsychotic drugs lead to EPS how?

A

Antipsychotic drug block on GABA which prevents DA from bind which leads to EPS

39
Q

D2 + Prolactin

A

Blockade of D@ in pituitary causes increased prolactin levels which leads to amenorrhea/galactorrhea and male infertility/gynecomastia
- DA normal decrease prolactin levels

40
Q

D2 + Emetic Center

A

Blockade of D2 in emetic leads to center not being stimulated and anti-emetic effect (can’t throw up)
- DA normally excites this center

41
Q

ExtraPyramidal Symptoms are what?

A

PsedoPK: rigidity, tremor
Dystonia: spasms of face/neck
Akathesia: restlessness
Tardive Dyskinesia: abnormal involuntary movements

42
Q

Other Antipsychotic AE Linked to D2

A 
Dyslipidemia
DM
Derm
Hematologic
Eye
Sexual dysfunction
43
Q

AE not linked to D2 with Antipsychotics

A

Sedation and HypoTN
Constipation
Seizures
Neuroleptic Malignant Syndrome (elevated body temp, altered consciousness, rigidity - immediate attention)

44
Q

Chlorpromazine vs Haloperidol

A

C: has more side effects than therapeutic effects
H: Better at therapeutics

45
Q

Overall Antipsychotic Drugs

A

Safe
No addictive
Tight and long lasting binding (EPS side effects)

46
Q

PK of Antipsychotics

A 
High plasma protein binding
Long half life
Hydroxylation and glucuronidation
2D6/1A2 (chlor) and 3A4/2D6/1A2 (halo)
Smokers eliminate the drugs faster
47
Q

Brain Occupancy for Antipsychotics

A

65%-80%

48
Q

Greater than 80% leads to:

A

EPS side effects

49
Q

Less than 65% leads to

A

No effect

50
Q

Drugs are different?

A

Haloperidol as 85% occupancy and is one of the best

Cloazpine needs big doses to get to therapeutic effects and will rarely have EPS

51
Q

Clozapine activity

A 
Weaker D2 antagonism 
Stronger 5HT2A antagonism
H1 (sedative)
M1 (dry mouth/constipation)
Alpha1 (hypoTN)
52
Q

Clozapine is good in

A

2nd gen
Severely ill
Treatment resistant patients

53
Q

Clozapine helps with

A

both negative and positive symptoms and cognition

Also, anti-suicidal

54
Q

Upside to clozapine

A

Less EPS

Less Hyperprolactin

55
Q

Downsides to clozapine

A

Hematotoxicity (all 2nd gen)
Seizure
Myocarditis
Metabolic (weight gain)

56
Q

5HT receptor agonist cause

A

hallucinations

57
Q

Why might 5HT2A blockade be helpful

A

Serotonergic neurons function as dopaminergic brakes –> they reduce DA activity
So blackade can release brake and increase DA

58
Q

5HT2A Blockade reduces positive symptoms?

A

Because it can specify mesolimbic pathway and reduce DA activity here

59
Q

5HT2A Blockade reduces negative symptoms

A

Blocks receptors in prefrontal cortex to increase dopamine

60
Q

5HT2A blockade reduces EPS

A

Blocks receptors in stiatum increases DA which lessens EPS

61
Q

Dopamine + Prolactin =

A

Inhibits

62
Q

D2 Blocker + Prolactin =

A

Increases

63
Q

Serotonin + Prolactin

A

Stimulates

64
Q

Fast Off Atypical antipsychotics (metabolized quickly)

A

Quetiapine
Clozapine
Remoxipride
Amisulpride

65
Q

Medium Atypical antipsychotics

A

Olanzapine

Sertindole

66
Q

Slow Traditional antipsychotics (metabolized slow)

A

Haloperidol
Raclopride
Chlorpromazine

67
Q

Olanzapine

A

Zyprexa

68
Q

Olanzapine activity

A 
5HT2A/2C
Better affinity for D2
Some M1 and H1
Less Alpha 1
- treat bipolar
69
Q

Upside to olanzapine

A

No EPS or hyperprolactin

Low incidence of agranulocytosis

70
Q

Olanzapine AE

A 
Somnolence (drowsy)
Weight gain
Increased appetite
Dry mouth
Constipation
71
Q

Risperidone

A

Risperdal

72
Q

Risperidone activity

A

High affinity for 5HT2A
High affinity for D2 (10x better)
No M1
Yes H1/alpha1

73
Q

Upside to risperidone

A

Low EPS and weight gain

74
Q

Risperidone AE / downsides

A

Raise prolactin (only atypical**) and 2D6
HypoTN, sedation, arrhythmias
- Not good for patients with negative symptoms
- Not good in cardiac pts

75
Q

Quetiapine

A

Seroquel

76
Q

Quetiapine

A 
Little or no EPS/prolactin
Short half life
NE reuptake inhibitor
Partial 5HTA1 agonist
Weight gain
77
Q

Ziprasidone

A

Geodon

78
Q

Ziprasidone

A

Antagonist of 5HT2A and 1A agonist
Low EPS and prolactin elevation
No weight gain

79
Q

Common characteristics of Atypicals

A

High affinity for 5HT2A receptor (no PD, no prolactin increase - except risp, co anti-emetic effect)
Helps with regulation of DA, ACh and glutamate
Cognitive improvement compared to 1st gen
Little effect for negative symptoms

80
Q

Main adverse effects of atypicals

A 
Sedation, increased appetite/weight gain
Metabolic syndrome (DM, hyperlipid)
QT prolongation
81
Q

Aripiprazole

A

Abilify

82
Q

Aripiprazole activity

A

D2 partial agonist
5HT2A antagonist
5HT1A partial agonist (anxiolytic)

83
Q

Aripiprazole upsides

A

Low H1, M1

Less EPS, weigh gain, metabolic syndrome, low sedaiton

84
Q

Aripiprazole D2 antagonists and agonist

A

Does allow others to bind

but it can stimulate it while bond in areas that you want to stimulate

85
Q

SO antipsychotic effects of classical antipsychotic is a result of…

A

blockade of D2 receptors in mesolimbic pathway and don’t want to antagonize in stiatum and pituitary

86
Q

PK of atypicals

A

Lipophilic
Orally well absorbed
High protein
High VofD

87
Q

Iloperidone

A

Fanapt

88
Q

Iloperidone info

A

Mixed D2/5HT2A receptor antagonist
Some M1, H1 and alpha 1
Dropped

89
Q

Asenapine

A

Saphris

90
Q

Asenapine info

A 
Sublingual
Adults only
All receptors
Death in elderly
Orthostatic hypoTN
QT prolongation
EPS
Hematotoxicity

Neuro Quiz 2 (4 decks)

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