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Pharmacology > L15: Anti-Psychotics I > Flashcards

L15: Anti-Psychotics I Flashcards

1
Q

Chloropromazine and Haloperidol belong to which class of anti-psychotics….
A. First generation
B. Second generation

A

A. First generation

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2
Q

True or False: Aripiprazole, Clozapine, Olazapine, and Risperidone belong to the second generation anti-psychotics

A

True

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3
Q

True or False: Psychosis is not unique to schizophrenia and is not present in all patients with schizo at all times

A

True

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4
Q

Which two hallucinogens are serotonin (5-HT) agonists that led to search for endogenous hallucinogens in patients with schizophrenia?

A

LSD and Mescaline

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5
Q

The identification of many 5-HT receptor subtypes led to identification of ___ and ____, which are the basis for hallucinatory effects of these agents

A

2A and 3C

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6
Q

True or False: Serotonin receptors modulate release of DA, NE, Glutamate, GABA, and Ach, among other NT, in the cortex, limbic, and striatum

A

True

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7
Q

Stimulation of which receptors leads to DEPOLARIZATION of GLUTAMATE neurons, as well as STABILIZATION of NMDA receptor on post-synaptic neurons, which also occurs with ingestion of hallucinogens?
A. 5-HT 1A
B. 5-HT 2A

A

B. 5-HT 2A

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8
Q

Which of the following are the main class of second generation anti-psychotic drugs?

A

Inverse agonists of the 5-HT2A

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9
Q

True or False: Many anti-psychotics strongly block post-synaptic D1 receptors in the CNS

A

False - strongly block post-synaptic D2 receptors in CNS

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10
Q

Drugs that increase dopaminergic activity either (1) ______ or (2) produce _____

A

(1) aggravate schizo psychosis

(2) produce psychosis de novo in some patients

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11
Q

True or False: Dopamine-receptor density has been found postmortem to be DECREASED in brains of schizophrenics who have been treated with anti-psychotics

A

False - Dopamine-receptor density has been found postmortem to be INCREASED in the brains of schizophrenics who have been treated with anti-psychotics

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12
Q

Imaging studies have shown measures consistent with increase ___ dopamine synthesis and release

A

striatal

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13
Q

True or False: The dopamine hypothesis for schizophrenia remains considered adequate to explain all aspects of schizophrenia

A

False - it is NOT! (especially the cognitive impairment)

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14
Q

True or False: Several of the atypical anti-psychotic drugs have much less effect on D2 receptors and, yet, are effective in treating schizophrenia

A

True

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15
Q

What are the four dopamine pathways involved in schizophrenia?

A
  1. Mesolimbic
  2. Mesocortical
  3. Nigrostriatal
  4. Tuberohypophyseal
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16
Q

Anti-psychotics that act on the tuberohypophyseal pathway commonly have ___ side effects, which commonly leads to increase breast tissue in men

A

hyperprolactinemia

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17
Q

Extrapyramidal (EPS) and tardive dyskinesia (TD) side effects are most closely associated which which dopamine pathway?

A

Nigral Striatal

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17
Q

Extrapyramidal (EPS) and tardive dyskinesia (TD) side effects are most closely associated which which dopamine pathway?
A. Mesolimbic
B. Mesocortical
C. Nigrostriatal
D. Tuberohypophyseal

A

C. Nigrostriatal

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18
Q

True or False: The mesolimbic dopamine pathway is associated with DA HYPERACTIVITY and positive symptoms

By contrast, the mesocortical pathway is associated with DA HYPOACTIVITY and negative symptoms

A

True

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19
Q

True or False: First generation psychotics primary affect nigrostriatal receptors

A

True

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20
Q

The ___ generation anti-psychotic agents block __ receptors and their binding affinity is very strongly correlated with clinical anti-psychotic and extrapyramidal potency
A. First gen; D1
B. Second gen; D2
C. First gen; D2

A

C. first-generation; D2

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21
Q

True or False: Therapeutic potency does NOT correlate with affinity for anti-psychotics binding to D1-R

A

True

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22
Q

Which of the following extrapyramidal symptom typically has an onset 5-30 days after starting a new anti-psychotic drug?
A. Pseudo-Parkinsonism
B. Acute Dystonia
C. Akathisia
D. Tardive Dyskinesia

A

A. Pseudo-Parkinsonism

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23
Q

Which dopamine pathway is most closely associated with parkinson’s like symptoms?

A

Nigrostriatal Pathway

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24
Q

Which of the following extrapyramidal symptom typically has an onset 5-60 days after starting a new anti-psychotic drug?
A. Pseudo-Parkinsonism
B. Acute Dystonia
C. Akathisia
D. Tardive Dyskinesia

A

C. Akathisia

  • Similar to restless leg syndrome
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25
Q

Which of the following extrapyramidal symptom typically has an onset 1-5 days after starting a new anti-psychotic drug?
A. Pseudo-Parkinsonism
B. Acute Dystonia
C. Akathisia
D. Tardive Dyskinesia

A

B. Acute Dystonia

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26
Q

True or False: Tardive Dyskinesia is an extrapyramidal symptom that can occur months to years after starting an anti-psychotic

A

True

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27
Q

Neuroleptic-induced EPS are thought to be caused by blockade of which dopamine tract?

A

Nigrostriatal dopamine tract

  • Results in relative increase in cholinergic activity
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28
Q

What is one of the reason 1st generation anti-psychotics fell out of favor?

A

Can cause pseudo-parkinsonism

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29
Q

Which patient population is at the greatest risk of developing acute dystonia while taking anti-psychotics?

Which patient population is at greatest risk of develop parkinsonism and TD while taking anti-psychotics?

A

Dystonia - Young, naiive patients

TD/Parkinsonism - elderly

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30
Q

Under which conditions can neuroleptic malignant syndrome develop?

A

After stopping anti-psychotic – weeks to months

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31
Q

True or False: A patient who develops neuroleptic malignant syndrome was likely taking a second generation

A

False - first generation

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32
Q

A patient who has developed silent syndrome was likely taking which drug?
A. Sertraline
B. Lithium
C. Risperidone
D. Haloperidol

A

B. Lithium

33
Q

Why can Neuroleptic Malignant Syndrome be fatal?

A

Extreme rigidity, fever, unstable BP

34
Q

True or False: Parkinsonism (Bradykinesia) is associated with low DA and elevated levels of Ach and GABA

By contrast, choreiform movements (Dyskinesia) is associated with low Ach and GABA, as well as elevated levels of DA

35
Q

In emergency situations, ____ blocks muscarinic receptors, as well as H1. Therefore, it is used as an antidote for drug-induced parkinsonism in emergency rooms

A

Diphenhydramine

36
Q

____ and ___ are non-competitive inhibitors of the NMDA receptor that exacerbate both cognitive impairment and psychosis in patients with schizophrenia

A

PCP and MK-801

37
Q

True or False: Selective 5-HT2A antagonists are much LESS potent than D2 antagonists in blocking the effects of PCP and related-drug MK-801

A

False - selective 5-HT2A antagonists are much MORE potent than D2 antagonists in blocking the effects of PCP (and the related-drug, MK-801)

38
Q

What is the effect of hypofunction of NMDA receptors, located on GABAergic interneurons?

A
  1. Diminished inhibitory influences on neuronal function, contribute to schizophrenia
39
Q

Diminished GABAergic activity can induce disinhibition of downstream glutamatergic activity, which can lead to _____ of cortical neurons via ____ receptors

A

hyperstimulation ; non-NMDA

40
Q

True or False: Hallucinations, Delusions, and Disorganized thoughts are positive symptoms while Flattened affect, anhedoia, and Asociality are negative symptoms

41
Q

Since drugs for Parkinson’s Disease can cause de novo psychosis, dopamine can affect ___ symptoms
A. Negative symptoms
B. Positive symptoms

A

B. Positive symptoms

42
Q

True or False: Serotonin can affect positive, negative, and cognitive symptoms. By contrast, glutamate affects cognitive and negative symptoms

43
Q

True or False: Although dopamine can cause de novo psychosis, schizophrenia involves a number of neurotransmitters (Serotonin, Glutamate, GABA, and Ach)

44
Q

Chloropromazine and Thioridazine are the ___ potent first generation anti-psychotics/phenothiazines
A. most
B. least

Trifluoperazine, Periphenazine, and Fluphenazine are __ potent first generation anti-psychotics; also associated with EPS’s
A. most
B. least

Are all of these drugs thioxanthene derivatives? phenothiazine derivatives?

A

least; most

phenothiazine derivatives

45
Q

Which of the following is the most commonly used 1st generation drug and results in high levels of EPS’s?
A. Chloropromazine
B. Trifluroperazine
C. Haloperidol
C. Thiothixene

A

C. Haloperidol

46
Q

True or False: Chloropromazine is a thioxanthene derivative

A

False - it is a phenothiazine derivative

47
Q

True or False: Chloropromazine blocks 5-HT2A receptors better than D2 receptors

A

False - Chloropromazine blocks D2 receptors better than 5-HT2A

48
Q

Which three receptors are blocked by Chloropromazine?

A

Alpha, muscarinic, and H1

49
Q

Decreased seizure threshold, QT prolongation, and CNS depression are most closely associated with which first generation anti-psychotic?
A. Thiorodazine
B. Fluphenazine
C. Chloropromazine

A

C. Chloropromazine

50
Q

What are the two psychiatric applications that can be treated with chloropromazine?

A
  1. Schizophrenia
    (alleviate positive symptoms)
  2. Bipolar disorder
    (manic)
51
Q

True or False: Chloropromazine can be used for non-psychiatric applications, such as: pre-op sedation, pruritis, and anti-emesis

52
Q

True or False: Chloropromazine can result in akathisia, dystonia, parkinson symptoms, TD, and hyperprolactinemia

53
Q

True or False: Although Chloropromazine is a phenothiazine derivative while Thiothixene is a thioxanthene derivative, they have a lot in common

54
Q

____ is a butyrophenone derivative that works by blocking D2 receptors more than 5-HT2A receptors

A

Haloperidol

55
Q

True or False: While haloperidol has some blockade of alpha receptor, it has MINIMAL blockade of M-receptors and is associated with less sedation than phenothiazines

56
Q

What are the four clinical applications of Haloperidol?

A
  1. Schizo (positive sx)
  2. Bipolar (manic)
  3. Huntington’s Chorea
  4. Tourette’s
57
Q

What are the four clinical applications of Haloperidol?

A
  1. Schizo (positive sx)
  2. Bipolar (manic)
  3. Huntington’s Chorea
  4. Tourette’s
58
Q

Which first generation anti-psychotic, which is a butyrophone derivative, is associated with extrapyramidal dysfunction, as well as hyperprolactinemia?
A. Thiothixene
B. Haloperidol
C. Chloropromaxine
D. Fluphenazine

A

B. Haloperidol

59
Q

True or False: Blockade of D2 receptors > than 5-HT2A in 1st gene

Blockade of 5-HT2A>D2 receptors in 2nd gen

60
Q

Which generation of anti-psychotics often acts as partial agonist at 5-HT1A-R, which produces synergistic effects with 5-HT1A receptor antagonism?

A

Second generation

61
Q

True or False: First generation anti-psychotics have equivalent potency for D2 and D3 receptors, but they are also 5-HT7 antagonists

A

False - second generation anti-psychotics do this…

62
Q

____ is a 5-HT2A inverse agonists used to treat Parkinson’s Dementia. However, it is associated with increased mortality.
A. Risperidone
B. Cloapzine
C. Olanzapine
D. Ariprazole
E. Pimavanserin

A

E. Pimavanserin

63
Q

Which two second generation anti-psychotics can be used to treat autism spectrum disorder?

A

Risperidone and Aripiprazole

64
Q

Which two second generation anti-psychotics can be used to treat agitation present in Alzheimer’s and Parkinson’s patients?

A

Risperidone and Clozapine - low doses

65
Q

True or False: Aripiprazole can be used to treat major depression, ASD, and Tourette Syndrome

66
Q

What is the main condition that is treated by Ariprazole and Clozapine?

A

Schizophrenia – improves (+) and (-) symptoms

67
Q

Valproate or Lithium are adjuncts for treatment of…
A. Schizo
B. Bipolar
C. Alzheimer’s

A

B. Bipolar

68
Q

There can be metabolic changes with use of cloazipine and olanzapine, which can lead to ____, _____, or ____

A

diabetes; high cholesterol; weight gain

69
Q

First gen anti-psychotics are most likely to bind to D2-R, meaning they have ____ as a side effect

A

Extra-pyramidal symptoms

70
Q

Why are second generation anti-psychotics less likely to cause extra-pyramidal symptom?

A

Act as partial agonists
- also will not block D2 quite as strongly

71
Q

True or False: First generation anti-psychotic drugs are associated with 5-HT2A binding

A

False - second generation anti-psychotics

72
Q

True or False: Second generation drugs typically provide psychosis treatment without the EPS

73
Q

Which of the following 1st gen anti-psychotics have greatest M1 binding?
A. Haloperidol
B. Chloropromazine
C. Thioridazine

A

B. Chloropromazine

74
Q

Which two 2nd generation anti-psychotics have greatest M1 binding?

A

Clozapine and Olazapine

75
Q

Hypotension is associated with use of …

A

Risperidone and Pimavanserin
(2nd gen)

Chloropromazine (1st gen)

76
Q

Which three anti-psychotics act on H1 receptor?

A

Chloropromazine (1st gen)

Olanzapine and Clozapine (2nd gen)

  • sedation and weight gain
77
Q

Which is a partial D2 agonist (and, thus, also an antagonist)
A. Haloperidol
B. Aripiprazole
C. Dopamine

A

B. Aripiprazole

78
Q

In the absence of dopamine, agonist affects are apparent (green(

79
Q

____, an antagonist without agonist activity, completely antagonists D2 receptor activation (red line)
A. Haloperidol
B. Aripiprazole
C. Dopamine

A

A. Haloperidol

80
Q

____ and ____ have similar potency

A

Dopamine and Aripriazole

81
Q

Dry mouth, constipation, urinary retention, blurred vision, increased HR and decreased sweating is associated with activation of which receptor?

A

Muscarinic M1 Receptor

Pharmacology (53 decks)

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