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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
Q

Do FGA’s or SGA’s cause serious EPS?

A

1st generation antipsychotics

26
Q

What is the important trend seen with FGA and SGA?

A

Low potency = High sedation

High potency = Strong EPS

27
Q

Most neuroleptic drugs are metabolized by what enzymes in the liver and brain?

A

Cytochrome P-450s

28
Q

What are the four major dopamine related pathways that are associated with adverse effects of typical neuroleptics?

A
  1. Mesolimbic pathway
  2. Mesocortical pathway
  3. Nigrostriatal pathway
  4. Tuberoinfundibular pathway
29
Q

Negative symptoms are associated with what pathway?

A

Meso-cortical pathway

30
Q

Positive symptoms are associated with what pathway?

A

Meso-limbic pathway

31
Q

What are two positive symptoms?

A
  1. Delusions

2. Hallucinations

32
Q

What are three negative symptoms?

A
  1. Withdrawal
  2. Lack of motivation
  3. Lack of pleasure
33
Q

Which pathway is associated with coordination of body movements?

A

Nigrostriatal pathway

34
Q

Which pathway inhibits the release of prolactin?

A

Tuberoinfundibular pathway

35
Q

What is Tardive Dyskinesia and how is it treated?

A

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
Q

Name five symptoms associated with anti-dopaminergic side effects.

A
  1. Acute dystonia
  2. Akathisia
  3. Pseudoparkinsonism
  4. Tardive dyskinesia
  5. Hyper-prolactinemia
37
Q

Name five general adverse effects of typical neurlopetics.

A
  1. Anti-dopaminergic side effects
  2. Anticholinergic/antimuscarininc side effects
  3. Antiadrenergic side effects
  4. Antihistaminergic side effects
  5. Photosensitivity
38
Q

What is acute dystonia and what is it associate with?

A

It is involuntary muscle contraction and it is associated with anti-dopaminergic side effects.

39
Q

What is akathisia?

A

Inner restlessness and constant urge to move; restless leg syndrome.

40
Q

What is pseudoparkinsonism?

A

Bradykinesia, tremor, rigidity, postural instability

41
Q

What is hyper-prolactinemia?

A

Increased prolactin secretion

42
Q

Neuoleptic Malignant Syndrom is associated with adverse effects of what drugs?

A

Antipsychotic drugs

43
Q

The acronym F.E.V.E.R is associated with what syndrome?

A

Neuroleptic Malignant Syndrome

44
Q

What does the acronym F.E.V.E.R stand for?

A 
F: Fever
E: Encephalopathy 
V: Vital signs
E: Enzymes
R: Rigidity of muscles
45
Q

Name two drugs that can be used to treat Neuroleptic Malignant syndrome and give their effect.

A
  1. Dentrolene: muscle relaxant

2. Bromocriptine: increase dopamine neurotransmission

46
Q

T or F. Patients treated with antipychotic drugs may elicit severe forms of neurotoxicity.

A

True. Neuroleptic Malignant Syndrome

47
Q

What are four properties of 2nd generation antipsychotic drugs?

A
  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
Q

What are the two main side effects when taking the SGA clozapine?

A
  1. Weight gain

2. Agranulocytosis

49
Q

What are the two main sites where clozapine acts?

A
  1. Dopamine D1 receptor antagonist

2. 5-HT(2A) receptor antagonist

50
Q

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?

51
Q

What SGA is structurally and pharmacologically similar to Clozapine, but without the liability to cause aganulocytosis?

A

Olanzapine

52
Q

Which SGA has a high potential for abuse?

A

Quetiapine

53
Q

What is the first of 3rd generation antipsychotic drugs?

A

Aripirazol

54
Q

What antipsychotic drug would be best to use if the patient is bipolar, anxious, and overweight?

A

Aripirazol - Used for bipolar and autism spectrum disorders and has lower liability for weight gain.

55
Q

What are the three most frequently prescribed FGA drugs?

A
  1. Haloperidol
  2. Chlorpromazine
  3. Thioridazine
56
Q

What are the three most commonly prescribed SGA drugs?

A
  1. Risperidone
  2. Olanzapine
  3. Aripiprazole
57
Q

What is the monitoring mnemonic for atypical neuroleptic drugs?

58
Q

What does E-FALCON stand for?

A 
E: EKG
F: Fasting glucose
A: AIMS (parkinson like symptoms)
L: Lipids
C: CBS
O: Obesity
N: Noncompliance
S: Seizures
59
Q

Why would Risperidone, Olanzapine, and Aripiprazole have greater appeal than some other SGA drugs?

A

These drugs alleviate both negative and positive symptoms of schizophrenia and they lower the liability of EPS.

Pharmacology (9 decks)

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