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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
Thiothixene Structure change
Thioxanthene Tricyclic Nucleus
26
Thiothixene
Navane
27
Thiothixene blocks
D2
28
Upside to Thiothixene
Reduced sedative, anticholinergic and hypoTN
29
Haloperidol structure change
Butyrophenones
30
Haloperidol
Haldol
31
Haloperidol is used as
potent antipsychotic
32
Upside to Haloperidol
Reduced sedative, anticholinergic and hypoTN
33
Downside to Haloperidol
Significant EPS and Prolactin
34
Therapeutic Actions of Classical Gen 1 Antipsychotics
``` Reduced positive symptoms (reduced hallucinations/delusions and disorganized thoughts) Sedation Reduced agitation, tension, aggression Improved motivation Require 2-6 weeks! ```
35
Acute Effect of Antipsychotics
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
36
Chronic effect of Antipsychotics
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
37
Parkinson's Disease Leads to EPS how?
Dopaine agonist blocks dopamine from binding GABA which leads to symptoms
38
Antipsychotic drugs lead to EPS how?
Antipsychotic drug block on GABA which prevents DA from bind which leads to EPS
39
D2 + Prolactin
Blockade of D@ in pituitary causes increased prolactin levels which leads to amenorrhea/galactorrhea and male infertility/gynecomastia - DA normal decrease prolactin levels
40
D2 + Emetic Center
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
ExtraPyramidal Symptoms are what?
PsedoPK: rigidity, tremor Dystonia: spasms of face/neck Akathesia: restlessness Tardive Dyskinesia: abnormal involuntary movements
42
Other Antipsychotic AE Linked to D2
``` Dyslipidemia DM Derm Hematologic Eye Sexual dysfunction ```
43
AE not linked to D2 with Antipsychotics
Sedation and HypoTN Constipation Seizures Neuroleptic Malignant Syndrome (elevated body temp, altered consciousness, rigidity - immediate attention)
44
Chlorpromazine vs Haloperidol
C: has more side effects than therapeutic effects H: Better at therapeutics
45
Overall Antipsychotic Drugs
Safe No addictive Tight and long lasting binding (EPS side effects)
46
PK of Antipsychotics
``` High plasma protein binding Long half life Hydroxylation and glucuronidation 2D6/1A2 (chlor) and 3A4/2D6/1A2 (halo) Smokers eliminate the drugs faster ```
47
Brain Occupancy for Antipsychotics
65%-80%
48
Greater than 80% leads to:
EPS side effects
49
Less than 65% leads to
No effect
50
Drugs are different?
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
Clozapine activity
``` Weaker D2 antagonism Stronger 5HT2A antagonism H1 (sedative) M1 (dry mouth/constipation) Alpha1 (hypoTN) ```
52
Clozapine is good in
2nd gen Severely ill Treatment resistant patients
53
Clozapine helps with
both negative and positive symptoms and cognition | Also, anti-suicidal
54
Upside to clozapine
Less EPS | Less Hyperprolactin
55
Downsides to clozapine
Hematotoxicity (all 2nd gen) Seizure Myocarditis Metabolic (weight gain)
56
5HT receptor agonist cause
hallucinations
57
Why might 5HT2A blockade be helpful
Serotonergic neurons function as dopaminergic brakes --> they reduce DA activity So blackade can release brake and increase DA
58
5HT2A Blockade reduces positive symptoms?
Because it can specify mesolimbic pathway and reduce DA activity here
59
5HT2A Blockade reduces negative symptoms
Blocks receptors in prefrontal cortex to increase dopamine
60
5HT2A blockade reduces EPS
Blocks receptors in stiatum increases DA which lessens EPS
61
Dopamine + Prolactin =
Inhibits
62
D2 Blocker + Prolactin =
Increases
63
Serotonin + Prolactin
Stimulates
64
Fast Off Atypical antipsychotics (metabolized quickly)
Quetiapine Clozapine Remoxipride Amisulpride
65
Medium Atypical antipsychotics
Olanzapine | Sertindole
66
Slow Traditional antipsychotics (metabolized slow)
Haloperidol Raclopride Chlorpromazine
67
Olanzapine
Zyprexa
68
Olanzapine activity
``` 5HT2A/2C Better affinity for D2 Some M1 and H1 Less Alpha 1 - treat bipolar ```
69
Upside to olanzapine
No EPS or hyperprolactin | Low incidence of agranulocytosis
70
Olanzapine AE
``` Somnolence (drowsy) Weight gain Increased appetite Dry mouth Constipation ```
71
Risperidone
Risperdal
72
Risperidone activity
High affinity for 5HT2A High affinity for D2 (10x better) No M1 Yes H1/alpha1
73
Upside to risperidone
Low EPS and weight gain
74
Risperidone AE / downsides
Raise prolactin (only atypical****) and 2D6 HypoTN, sedation, arrhythmias - Not good for patients with negative symptoms - Not good in cardiac pts
75
Quetiapine
Seroquel
76
Quetiapine
``` Little or no EPS/prolactin Short half life NE reuptake inhibitor Partial 5HTA1 agonist Weight gain ```
77
Ziprasidone
Geodon
78
Ziprasidone
Antagonist of 5HT2A and 1A agonist Low EPS and prolactin elevation No weight gain
79
Common characteristics of Atypicals
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
Main adverse effects of atypicals
``` Sedation, increased appetite/weight gain Metabolic syndrome (DM, hyperlipid) QT prolongation ```
81
Aripiprazole
Abilify
82
Aripiprazole activity
D2 partial agonist 5HT2A antagonist 5HT1A partial agonist (anxiolytic)
83
Aripiprazole upsides
Low H1, M1 | Less EPS, weigh gain, metabolic syndrome, low sedaiton
84
Aripiprazole D2 antagonists and agonist
Does allow others to bind | but it can stimulate it while bond in areas that you want to stimulate
85
SO antipsychotic effects of classical antipsychotic is a result of...
blockade of D2 receptors in mesolimbic pathway and don't want to antagonize in stiatum and pituitary
86
PK of atypicals
Lipophilic Orally well absorbed High protein High VofD
87
Iloperidone
Fanapt
88
Iloperidone info
Mixed D2/5HT2A receptor antagonist Some M1, H1 and alpha 1 Dropped
89
Asenapine
Saphris
90
Asenapine info
``` Sublingual Adults only All receptors Death in elderly Orthostatic hypoTN QT prolongation EPS Hematotoxicity ```

Neuro Quiz 2 (4 decks)

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