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PSYCH > PHARM - Antipsychotics > Flashcards

PHARM - Antipsychotics Flashcards

1
Q

discuss the pathogenesis behind

  • positive schizophrenia symptoms
  • negative schizophrenia symptoms
A

both due to abnormal dopamine neurotransmission from dopraminergic neurons

  • positive symptoms: overactivity of mesolimbic pathway
  • negative symptoms: underactivity of mesocortical pathway
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2
Q

what major side effects can result from blockage of D2 receptors?

A
  • extrapyramidal system (EPS) AEs
  • hyperprolactinemia
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3
Q

what are the EPS adverse affects?

A
  • parkinson like symptoms
  • akathisia
  • acute dystonia
  • tardive dyskinesia
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4
Q

acute dystonia

  • early or late EPS effect?
  • presentation
A
  • early effect
  • presentation: severe spasm of back, neck, face and tongue
    • if progression to larynx → respiration impairment
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5
Q

parkinsonism

  • early or late EPS effect?
  • presentation
A
  • early EPS effect
  • presentation: bradykinesia
    • resting tremor
    • abrormal gait - stooped, shuffling
    • ridigity - often at elbow
    • facial weakness - mask-like, drooling
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6
Q

akasthia

  • early or late EPS effect?
  • presentation?
A
  • early EPS effect
  • presentation: pacing & squirming d/t an uncontrollable need to move
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7
Q

tardive dyskinesia

  • early or late EPS effect?
  • presentation
A
  • late effect
  • presentation: twisting, writhing, worm- like movements of the
    • tongue
    • face
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8
Q

discuss the mechanism of D2-blockage induced hyperprolactinemia

A

blockage of D2 receptors in the tuberoinfundibular pathway → no release of DA onto PRL-secreting neurons → no inhibition of PRL release → hyperprolactinemia

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9
Q

which anti-dopaminergic AE is due to

  • blockage of the infundibular pathway?
  • blockage of the nigrostratial pathway?
A
  • infundibular: hyperprolactinemia
  • nigrostriatal: akathisia (an EPS)
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10
Q

review the AE that results from histamine blockage

A

drowsiness / sedation

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11
Q

review the AEs that result from alpha-1 adrenergic receptor blockage

A

orthostatic hypotension

(resulting from blockage of compensatory vasoconstriction when patient stands)

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12
Q

review the AEs that result from muscarinic blockage

A
  • dry mouth
  • blurred vision
  • urinary retention
  • constipation
  • aggravation of glaucoma
  • tachycardia
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13
Q

typical anti-psychotics

  • include which drugs?
  • clinical uses?
  • MOA?
  • PK
  • AE/CI?
A
  • drugs: haloperidol, chlorpromazine
  • clinical uses: schizophrenia - both positive and negative symptoms
  • MOA: block D2 receptors + cross reactive with H1, M1 & alpha-1 receptors
  • PK:
    • narrow therapeutic range
    • various potencies, which dictate AE profile
  • AE:
    • high potency = AEs from D2 blockage
      • EPS side effects
      • hyperprolactinemia
    • low potency = AEs from cross reactiivty
      • anti-histaminergic - drowsiness
      • anti-a1 adrenergic - orthostatic hypotension
      • anti-cholinergic - u should know this by now
    • QT interval prolongation
    • neuroepileptic syndrome
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14
Q

constrast the adverse effect profiles of low potency vs high potency typical anti-psychotics

A

(haloperidol, chlorpomazine)

high potency: D2 predominante

  • EPS: tardive dyskinesia, akathisa, dystonia, parkinsonism
  • hyperprolactinemia

low potency: H1 / a1 / M1 predominate

  • drowiness (H1)
  • orthostatic hypotension (a1)
  • dry mouth, blurred vision, urinary retention / constipation, glaucoma, tachycardia (M1)

both = prolonged QT, neuroepileptic

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15
Q

summarize the AEs of high potency typical anti-psychotics

A

(haloperidol, chlorpromazine)

EPS & hyperprolactinemia > drowsiness, orthostatic hypotension, anticholinergic affects

+ prolonged QT, neuroepileptic syndrome

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16
Q

summarize the AEs of low potency typical anti-psychotics

A

(haloperidol, chlorpromazine)

drowsiness, orthostatic hypotension, anticholinergic affects > EPS & hyper-prolactinemia

+ prolonged QT, neuroepileptic syndrome

17
Q

chlorpromazine

  • is what kind of drug?
  • clinical uses?
  • MOA?
  • PK
  • AE/CI?
A
  • drugs: typical anti-psychotic
  • clinical uses: schizophrenia - both positive and negative symptoms
  • MOA: block D2 receptors + cross reactive with H1, M1 & alpha-1 receptors
  • PK:
    • narrow therapeutic range
    • various potencies, which dictae AE profile
  • AE:
    • high potency = AEs from D2 blockage
      • EPS side effects
      • hyperprolactinemia
    • low potency = AEs from cross reactiivty
      • anti-histaminergic - drowsiness
      • anti-a1 adrenergic - orthostatic hypotension
      • anti-cholinergic - u should know this by now
    • prolonged QT interval
    • neuroleptic malignant sydnrome
18
Q

haloperidol

  • is what kind of drug?
  • clinical uses?
  • MOA?
  • PK
  • AE/CI?
A
  • drugs: typical anti-psychotic
  • clinical uses: schizophrenia - both positive and negative symptoms
  • MOA: block D2 receptors + cross reactive with H1, M1 & alpha-1 receptors
  • PK:
    • narrow therapeutic range
    • various potencies, which dictae AE profile
  • AE:
    • high potency = AEs from D2 blockage
      • EPS side effects
      • hyperprolactinemia
    • low potency = AEs from cross reactiivty
      • anti-histaminergic - drowsiness
      • anti-a1 adrenergic - orthostatic hypotension
      • anti-cholinergic - u should know this by now
    • prolonged QT interval
    • neuroepileptic malignancy syndrome
19
Q

neuroepleptic malignant syndrome can arise following use of which drugs?

how is it treated?

A

from typical anti-psychotics (chlorpromazine, haloperidol)

tx = immediately discontinue treatment

20
Q

atypical anti-psychotics

  • includes what drugs?
  • clinical uses
  • MOA
  • PK
  • AE/CI
A
  • drugs: clozapine, asenapine, aripiprazole, lurasidone HCl
  • clinical uses: shizophrenia - positive symptoms > negative symptoms
  • MOA: 5-HT2A antagonism > D2 antagonism
  • AE:
    • key - increase metabolic syndrome markers
      • ​diabetes
      • obesity
      • dsylipidemia
    • +/- minor EPS, hyperprolactinemia
    • +/- minor anti-histaminergic, a1-adrenergic, muscarinic effects
21
Q

clozapine

  • what kind of drug?
  • clinical use
  • MOA
  • PK
  • AE
A
  • drug: atypical anti-psychotic
  • clinical uses: reserved for refractory shizophrenia only. as an atypical antipsychotic, treat mostly positive symptoms.
  • MOA: 5-HT2A antagonism > D2 antagonism
  • PK: narrow therapeutic range
  • AE:
    • increase metabolic syndrome markers
      • ​diabetes
      • obesity
      • dsylipidemia
    • agranulocytosis*
    • +/- minor EPS, hyperprolactinemia
    • +/- minor anti-histaminergic, a1-adrenergic, muscarinic effects
22
Q

aripiprazole

  • what kind of drug?
  • clinical use
  • MOA
  • PK
  • AE
A
  • drug: atypical anti-psychotic
  • clinical uses: schizophrenia: positive symptoms > negative symptoms
  • MOA: 5-HT2A antagonism > D2 antagonism
  • PK: narrow therapeutic range
  • AE:
    • increased metabolic syndrome markers
      • ​diabetes
      • obesity
      • dsylipidemia
    • +/- minor EPS, hyperprolactinemia
    • +/- minor anti-histaminergic, a1-adrenergic, muscarinic effects
23
Q

asenapine

  • what kind of drug?
  • clinical use
  • MOA
  • PK
  • AE
A
  • drug: atypical anti-psychotic
  • clinical uses: schizophrenia: positive symptoms > negative symptoms
  • MOA: 5-HT2A antagonism > D2 antagonism
  • PK: narrow therapeutic range
  • AE:
    • increased metabolic syndrome markers
      • ​diabetes
      • obesity
      • dsylipidemia
    • +/- minor EPS, hyperprolactinemia
    • +/- minor anti-histaminergic, a1-adrenergic, muscarinic effects
24
Q

lurasidone

  • what kind of drug?
  • clinical use
  • MOA
  • PK
  • AE
A
  • drug: atypical anti-psychotic
  • clinical uses: schizophrenia: positive symptoms > negative symptoms
  • MOA: 5-HT2A antagonism > D2 antagonism
  • PK: narrow therapeutic range
  • AE:
    • increased metabolic syndrome markers
      • ​diabetes
      • obesity
      • dsylipidemia
    • +/- minor EPS, hyperprolactinemia
    • +/- minor anti-histaminergic, a1-adrenergic, muscarinic effects
25
Q

which atypical anti-psychotic is considered to the “most effective”?

26
Q

blood counts must be monitored in patients taking which atypical anti-psychotic?

why?

A

clozapine

clozapine can cause agranulocytosis

27
Q

which anti-psychotics treat which schizophrenia symptoms?

A

typical: treat postive AND negative sx
atypitcal: positive sx mostly

28
Q

typical vs atypical anti-psychotics

  • schizophrenia symptoms treated
  • predominant AEs
A

typical

  • positive AND negative sx
  • AEs:
    • anti-D2 (EPS & hyperprolactinemia) - mostly high potency
    • anti-M1, H1, a1 - mostly low potency
    • prolonged QT
    • neuroepileptic malignancy

atypical

  • positive sx
  • AEs
    • increased metabolic markers - DM, obesity, disipdemia*
    • rarely anti-D2, M1, H1, or a1
29
Q

which drugs can be used to treat drug-induced parkinsonism?

A

anti-cholinergics

diphenhydramine*

PSYCH (7 decks)

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