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Lec. 4: Antipsychotic Drugs Flashcards

1
Q

First generation antipsychotics are considered typical/atypical and second generation antipsychotics are considered typical/atypical.

A
  1. Typical

2. Atypical

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2
Q

What are the five categories of typical antipsychotic drugs?

A
  1. Phenothiazenes
  2. Thioxanthenes
  3. Dibenzoxazapines
  4. Butyrophenones and Diphenylbutylpiperidines
  5. Dihydroindolone
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3
Q

Give five examples of atypical antipsychotic drugs.

A
  1. Clozapine
  2. Risperidone
  3. Olanzapine
  4. Quetiapine
  5. Aripiprazole
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4
Q

Give three examples of active symptoms and passive symptoms associated with schizophrenia.

A 
Active:
1. Delusions
2. Hallucinations
3. Disorganized thoughts and speech
Passive:
1. Flat affect (no emotions)
2. Social withdrawal
3. Impaired process planning/memory/personal hygiene
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5
Q

What are the three components of schizophrenia?

A
  1. Positive symptoms
  2. Negative symptoms
  3. Impaired cognition
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6
Q

What is the main hypothesis for cause of schizophrenia?

A

Excessive dopamine

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7
Q

Enhanced transmission of what neurotransmitter exacerbates symptoms of schizophrenia?

A

Dopamine

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8
Q

Clinical potency of first generation anti-psychotics (typical) is generally correlated with degree of ? receptor antagonism.

A

Dopamine

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9
Q

What is the most common drug to treat schizophrenia?

A

1st generation antipsychotics

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10
Q

T or F. 1st generation antipsychotics improve both positive and negative symptoms of schizophrenia.

A

False. They improve positive symptoms only.

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11
Q

Which antipsychotic drug will alleviate both positive and negative symptoms of schizophrenia?

A

2nd generation antipsychotics (atypical)

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12
Q

What drug has been approved for treatment for Tourette’s syndrome?

A

Pimozide

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13
Q

What are the three main groups of Phenothiazine?

A
  1. Aliphatic chain at R1
  2. Piperidine ring at R1
  3. Piperazine ring at R1
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14
Q

Give an example of a phenothiazine with a piperazine ring at R1 and list three characteristics of it.

A

Fluphenazine

  1. HIGH potency
  2. Strong EPS
  3. Least sedating of the three groups
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15
Q

Give an example of a phenothiazine with a piperidine ring at R1 and list three characteristics of it.

A

Thioridazine

  1. LOW potency
  2. Higher sedating potential
  3. Hypotensive
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16
Q

Give two examples of a phenothiazine with a aliphatic chain at R1 and give examples of each.

A
  1. Chlorpromazine: low potency, high sedating potential

2. Trifluoperazine: high potency

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17
Q

Give two examples of a thioxanthene and characteristics of each.

A
  1. Thiothixene: high potency, EPS

2. Chlorprothixene: high potency, high EPS

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18
Q

Give an example of buterophenone and list some characteristics of it.

A

Haloperidol: high potency, less sedating, strong EPS

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19
Q

What is an example of a dihydroindolone?

A

Molindone

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20
Q

What is an example of a Dibenzoxapine?

A

Laxapine

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21
Q

Pimozide is an example of what first generation antipsychotic drug?

A

Diphenylbutylpiperidine

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22
Q

How are most neuroleptic drugs absorbed?

A

Erratically in the GI tract

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23
Q

T or F. Neuroleptic drugs are highly lipophilic and highly protein bound.

A

True

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24
Q

T or F. 1st generation antipsychotics also block muscarinic, adrenergic, histaminergic, and sertoninergic receptors.

25
Do FGA's or SGA's cause serious EPS?
1st generation antipsychotics
26
What is the important trend seen with FGA and SGA?
Low potency = High sedation | High potency = Strong EPS
27
Most neuroleptic drugs are metabolized by what enzymes in the liver and brain?
Cytochrome P-450s
28
What are the four major dopamine related pathways that are associated with adverse effects of typical neuroleptics?
1. Mesolimbic pathway 2. Mesocortical pathway 3. Nigrostriatal pathway 4. Tuberoinfundibular pathway
29
Negative symptoms are associated with what pathway?
Meso-cortical pathway
30
Positive symptoms are associated with what pathway?
Meso-limbic pathway
31
What are two positive symptoms?
1. Delusions | 2. Hallucinations
32
What are three negative symptoms?
1. Withdrawal 2. Lack of motivation 3. Lack of pleasure
33
Which pathway is associated with coordination of body movements?
Nigrostriatal pathway
34
Which pathway inhibits the release of prolactin?
Tuberoinfundibular pathway
35
What is Tardive Dyskinesia and how is it treated?
It is an anti-dopaminergic side effect that causes repetitive, involuntary movements. Treat it by upping the dose of neuroleptic and switch to an atypical neuroleptic drug, like clozapine.
36
Name five symptoms associated with anti-dopaminergic side effects.
1. Acute dystonia 2. Akathisia 3. Pseudoparkinsonism 4. Tardive dyskinesia 5. Hyper-prolactinemia
37
Name five general adverse effects of typical neurlopetics.
1. Anti-dopaminergic side effects 2. Anticholinergic/antimuscarininc side effects 3. Antiadrenergic side effects 4. Antihistaminergic side effects 5. Photosensitivity
38
What is acute dystonia and what is it associate with?
It is involuntary muscle contraction and it is associated with anti-dopaminergic side effects.
39
What is akathisia?
Inner restlessness and constant urge to move; restless leg syndrome.
40
What is pseudoparkinsonism?
Bradykinesia, tremor, rigidity, postural instability
41
What is hyper-prolactinemia?
Increased prolactin secretion
42
Neuoleptic Malignant Syndrom is associated with adverse effects of what drugs?
Antipsychotic drugs
43
The acronym F.E.V.E.R is associated with what syndrome?
Neuroleptic Malignant Syndrome
44
What does the acronym F.E.V.E.R stand for?
``` F: Fever E: Encephalopathy V: Vital signs E: Enzymes R: Rigidity of muscles ```
45
Name two drugs that can be used to treat Neuroleptic Malignant syndrome and give their effect.
1. Dentrolene: muscle relaxant | 2. Bromocriptine: increase dopamine neurotransmission
46
T or F. Patients treated with antipychotic drugs may elicit severe forms of neurotoxicity.
True. Neuroleptic Malignant Syndrome
47
What are four properties of 2nd generation antipsychotic drugs?
1. Block 5-HT > D2 receptors 2. At low doses, produce fewer EPS and less sedation 3. Effective against positive AND negative symptoms of schizophrenia 4. Has varying blocking activities
48
What are the two main side effects when taking the SGA clozapine?
1. Weight gain | 2. Agranulocytosis
49
What are the two main sites where clozapine acts?
1. Dopamine D1 receptor antagonist | 2. 5-HT(2A) receptor antagonist
50
What is a SGA that blocks serotonin 5-HT(2A) and dopamine D2 receptors, is not as effective as clozapine, has low incidence of EPS, and is well absorbed orally?
Risperdal
51
What SGA is structurally and pharmacologically similar to Clozapine, but without the liability to cause aganulocytosis?
Olanzapine
52
Which SGA has a high potential for abuse?
Quetiapine
53
What is the first of 3rd generation antipsychotic drugs?
Aripirazol
54
What antipsychotic drug would be best to use if the patient is bipolar, anxious, and overweight?
Aripirazol - Used for bipolar and autism spectrum disorders and has lower liability for weight gain.
55
What are the three most frequently prescribed FGA drugs?
1. Haloperidol 2. Chlorpromazine 3. Thioridazine
56
What are the three most commonly prescribed SGA drugs?
1. Risperidone 2. Olanzapine 3. Aripiprazole
57
What is the monitoring mnemonic for atypical neuroleptic drugs?
E-FALCON
58
What does E-FALCON stand for?
``` E: EKG F: Fasting glucose A: AIMS (parkinson like symptoms) L: Lipids C: CBS O: Obesity N: Noncompliance S: Seizures ```
59
Why would Risperidone, Olanzapine, and Aripiprazole have greater appeal than some other SGA drugs?
These drugs alleviate both negative and positive symptoms of schizophrenia and they lower the liability of EPS.

Pharmacology (9 decks)

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