Antipsychotics Flashcards

1
Q

What is psychosis

A

Variety of mental disorders with delusions , auditory or visual hallucinations and disorganized thinking

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2
Q

What is schizophrenia

A

Particular kind of psychosis with clear sensorium and marked thinking disturbance

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3
Q

What are the positive symptoms of schizophrenia

A
Delusions 
hallucinations 
thoughts disorder 
abnormal disorganized behavior 
catatonia
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4
Q

Negative symptoms of psychosis

A
Social withdrawal 
flattening of emotional responses 
 anhedonia 
reluctance to perform every day tasks 
chronic and persistent and less responsive to some antipsychotic agent
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5
Q

Do we know the cause of psychosis

A

Still unclear but might be linked to genetics and environment

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6
Q

What is the serotonin hypothesis

A

Hallucination are produced by LSD and mescaline which are serotonin agonist

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7
Q

What is a key factor in mechanism of action of antipsychotic

A

Blockades of serotonin receptor 5-HT2a

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8
Q

What drugs are 5-HT2c inverse agonist

A

Clozapine
asenapine
Olanzapine

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9
Q

What happens wonder stimulation of 5HT2c

A

Inhibition of cortico and Limbic dopamin release

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10
Q

What is the dopamine hypothesis

A

Psychosis might be due to excessive Limbic dopaminergic activity

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11
Q

What happens if the drug increases dopaminergic activity

A

Aggravate schizophrenia psychosis or psychosis de novo produced

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12
Q

What type of reçeptors density is increaesed in the brain of post mortem schizophrenic

A

Dopamine receptor

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13
Q

What is the glutamate hypothesis

A

NMDA receptor do not function well so there’s reduced inhibitory influence on the neuronal function which contributes to schizophrenia

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14
Q

What are the classes of drugs part of the first generation antipsychotics

A

Phenothiazines
Thioxanthenes
Butyrophenone

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15
Q

example of phenothiazines

A
Chlorpromazine
Thioridazine 
Trifluoperazine 
Perphenazine
Fluphenazine
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16
Q

Example of thioxanthenes

A

Thiothixene

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17
Q

Examples of butyrophenone

A

Haloperidol

droperidol

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18
Q

Class of drugs in second-generation antipsychotics

A

Atypical

miscellaneous

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19
Q

Examples of atypical antipsychotics

A
Clozapine 
Asenapine
Olanzapine
Quetiapine
Sulpiride
Amisupride
Paliperidone
Risperidone
Sertindole
Ziprasidone
Zotepine
Aripiprazole
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20
Q

Example of miscellaneous antipsychotics

A

Pimozide

Molindone

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21
Q

Types of phenothiazines with sedation& weight gain effects

A

Aliphatic derivatives and piperidine derivatives

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22
Q

Most potent phenothiazines types

A

Piperazine derivatives

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23
Q

Most widely used butyrophenone

A

Haloperidol

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24
Q

ExAmple of diphenylbutylpiperidines

A

Pimozide
Clopimozide
Fluspirilene
Penfluridol

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25
The more potent with less autonomic effect l , phenothiazines or butyrophenone
butyrophenone
26
Prototype of atypical antipsychotic
Clozapine
27
Active metabolite of risperidone
Paliperidone9 hydroxyrisperidone
28
Main moa of atypical antipsychotic drugs
Alter 5HT2a receptor activity With synergy at Partial agonist of 5-HT1a
29
Name of of atypical antipsychotic that are potent for D2 and D3 receptors and antogonize 5HT7
Amisulpride | Sulpiride
30
Systemic availability of haloperidol
65%
31
Systemic availability of chlorpromazine and thioridazine
25-35%
32
Are antipsychotic drugs highly lipid soluble and protein bound
Yes
33
Dube antipsychotic drugs have large volumes of distribution
Yes
34
What is the average time for a relapse of stable patient with schizophrenia who discontinue the medication
Six months
35
How is relapse after discontinuation of clozapine
It’s very rapid and severe so should never be discontinued abruptly unless needed
36
 Metabolism of antipsychotic drugs
Oxidation or the methylation by liver cytochrome P450- cyp2d6, CYP1A2, cyp3a4
37
Would you expect antipsychotic drugs to interfere with metabolism of other drugs at typical clinical dose
No
38
What mechanism is that the basis of efficacy of phenothiazine antipsychotic drugs
D2 receptor blockade
39
Why are they adverse effects with phenothiazines antipsychotics
Block Alfa Adrenergic receptors, muscarinic receptors , h1 receptors , serotonin receptors
40
Most closely related pathway to behavior and psychosis
Mesolimbic Mesocortical pathway
41
Pathway involved in coordination of voluntary movement
Nigrostriatal pathway
42
This system neurons release dopamine which inhibits prolactin secretion from anterior pituitary
Tuberoinfundibular system
43
System involved in eating behavior
Medullary periventricular pathway
44
Pathway that regulates anticipatory motivational phase of copulatory behavior in rats
Incertohypothermic pathway
45
What are the function D1 and D5receptors
Increases cyclic AMP by G protein stimulatory activation of adenylyl cyclase
46
Action of D2, D3, D4 receptors
Decreases cyclic AMP and inhibits calcium channels
47
Effect f antipsychotics on non psychotic individuals
``` Severe EPS aka this in Sleepiness Restlessness Autonomic effects ```
48
antipsychotics that raise prolactin level
Old typiciL antipsychotics Risperidone Paliperidone
49
Cardiovascular effect of chlorpromazine and thioridazine
``` Orthostatic hypotension Tachycardia Abnormal ECG (thioridazine) ```
50
Antipsychotics with risk of arrhythmias
Sertindole Ziprasidone Quetiapine
51
Antipsychotics psychiatric indications
``` Schizophrenia Psychotic bipolar disorder Psychotic depression Treatment resistant depression Manic phase of bipolar disorder ```
52
Best treatment for catatonic schizophrenia
Benzodiazepines
53
Non psychiatric indications of antipsychotics
Antiemetics ( prochlorpromazine , benzquinamide because of dopamin receptor blockade ) ``` Pruritus for h1 receptor blockade Preoperative sedatives ( promethazine ) ``` Neuroleptanesthesia (butyrophenone
54
Atypical Antipsychotics with less weight gain
Ziprasidone
55
Only atypical antipsychotics indicated to reduce risk of suicide
Clozapine
56
When should you take clozapine
If failed to respond to substantial doses of conventional antipsychotic drugs
57
Behavioral effects of antipsychotics
Pseudodepression | Toxic confusional States
58
Neurological effect of antipsychotic
Extrapyramidal reactions Tardive dyskinesia Seizure
59
Agent with the least likelihood of causing tardive dyskinesia
Clozapine | quetiapine
60
Drugs with less potential for seizure
``` Risperidone Molindone Thioridazine Haloperidol Pimozide Trifluoperazine Fluphenazine ```
61
Metabolic effect of antipsychotics
``` Weight gain hyperglycemia hyperlipidemia diabetic ketoacidosis triglycerides HDL ratio Hyperprolactinemia  ```
62
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