Anitpsychotic Drugs - Segars Flashcards

1
Q

what are the positive symptoms of schizophrenia?

A
  • hallucinations
  • delusions
  • disorganized speech/thinking
  • agitation
  • abnormal motor behavior
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2
Q

which drug class is more commonly utilized as first-line, initial therapy of psychotic disorders?

A

SGA’s

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3
Q

what is the minimum timeframe necessary to evaluate response to therapy of antipsychotics?

A

2-3 weeks

- maximum remission benefit may take several months

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4
Q

what do the first generation antipsychotics (FGA’s) primarily block?

A

dopamine type-2 (D2) post-synaptic receptors

- D2&raquo_space; 5HT

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5
Q

what are the other receptors that FGA’s block?

A
  • muscarinic
  • histaminic (H1)
  • alpha-adrenergic (a1)
  • D2 in nigrostriatal (EPS/movements) and tuberoinfundibular (prolactin) pathways
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6
Q

what are the muscarinic side effects of FGA’s?

A
  • dry mouth
  • constipation
  • urinary retention
  • blurred vision
  • sedation
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7
Q

what are the alpha-adrenergic effects of FGA’s?

A
  • orthostatic hypotension

- dizziness/syncope

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8
Q

what is the main histaminic effect of FGA’s?

A

sedation

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9
Q

what are the two important “other” effects of FGA’s?

A

risk of QT prolongation and seizure activity

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10
Q

what are the acute extrapyramidal symptoms (EPS)?

A
  • akathisia (restlessness)
  • dystonia
  • parkinsonism-like movements
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11
Q

when is there a high risk for EPS?

A

with high D2 occupancy (>78% of receptors occupied)

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12
Q

what are the 2 broad categories of FGA’s?

A
  1. low potency (more sedation, hypotension, seizure-threshold reduction)
  2. high potency (more movement and endocrine effects)
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13
Q
  • chlorpromazine

- thioridazine

A

low potency FGA’s

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14
Q
  • fluphenazine

- haloperidol

A

high potency FGA’s

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15
Q

what are the treatments for EPS? (acute maintenance)

A
  1. anticholinergic agents:
    - benztropine and trihexyphenidyl
  2. antihistamine agents:
    - diphenhydramine
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16
Q

what are the treatments for tardive dyskinesia (TD)

A

selective vesicular monoamine transporter 2 (VMAT2) inhibitors:

  • valbenazine
  • deutetrabenazine
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17
Q

what do second generation antipsychotics block along with D2 post-synaptic receptors?

A

5HT-2A&raquo_space; D2

NOTE: some SGA’s also block other DA receptors (D-1,3,5) and also have greater propensity to be an agonist/antagonist on one or more other 5HT receptors

18
Q

what are the 4 broad categories of SGA’s?

A
  1. 5HT-2A/DA receptor antagonists
  2. partial DA/5HT-1A receptor agonists
  3. multi-acting receptor-target agents
  4. inverse serotonin agonist/antagonist
19
Q
  • iloperidone
  • lurasidone
  • paliperidone
  • risperidone
  • ziprasidone
A

5HT-2A/DA receptor antagonists

20
Q
  • aripiprazole

- brexpiprazole

A

partial DA/5HT-1A receptor agonists

21
Q
  • asenapine
  • clozapine
  • olanzapine
  • quetiapine
A

multi-acting receptor-target agents

22
Q

primavanserin (parkinson’s psychosis)

A

inverse serotonin agonist/antagonist

23
Q

what are the common side effects of SGA’s?

A
  • weight gain
  • metabolic effects
  • stroke -> greater risk in elderly with dementia
24
Q
  • chlopromazine
  • fluphenazine
  • haloperidol
  • thioridazine
A

FGA’s

25
Q
  • aripiprazole
  • cariprazine
  • clozapine
  • lurasidone
  • olanzapine
  • quetiapine
  • risperidone
  • ziprasidone
A

SGA’s

26
Q

which FGA’s have the least effect on weight gain and DM?

A

fluphenazine and haloperidol

27
Q

which SGA’s have the least effect on weight gain and DM?

A

ziprasidone (null), aripiprazole (+)

28
Q

which FGA has the worst effect on weight gain and DM?

A

chlorpromazine

29
Q

which SGA’s have the worst effect on weight gain and DM?

A
  • clozapine and olanzapine (++++)

- quetiapine and risperidone (+++)

30
Q

which FGA’s have the least effect on EPS and TD?

A

chlorpromazine and thioridazine

31
Q

which FGA’s have the worst effect on EPS and TD?

A

fluphenazine and haloperidol

32
Q

which SGA’s have the least effect on EPS and TD?

A

clozapine and quetiapine

33
Q

which SGA’s have the worst effect on EPS and TD?

A

risperidone

34
Q

which SGA has the overall least side effects?

A

aripiprazole

35
Q

what is the rare-but-severe side effect of clozapine?

A

agranulocytosis

- monitor WBC, must be enrolled in REMS program

36
Q

what is the rare-but-severe side effect of olanzapine?

A

drug reaction with eosinophilia and systemic symptoms (DRESS)
- potentially life threatening drug-induced hypersensitivity reaction

37
Q

what is Neuroleptic Malignant Syndrome (NMS)?

A

rare, but potentially fatal, severe Parkinson’s-like movement disorder with wide-spread muscle contraction

38
Q

what is the tx for NMS?

A

dantrolene KNOW this muscle relaxer

39
Q

what baseline labs should be run before beginning antipsychotic medications?

A

serum glucose, lipids, BMI, blood pressure, waist circumference, family hx of metabolic and CV disease

40
Q

how can non-adherence to medication be managed?

A

long acting injectable agents (LAIA’s) every 2-12 weeks depending on agent/dose/patient

41
Q

what are the 3 LAIA’s Segars want’s us to know?

A
  • risperidone
  • olanzapine
  • aripiprazole