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Pharmacology > Antipsychotics > Flashcards

Antipsychotics Flashcards

1
Q

what is schizophrenia?

A

chronic psychotic disorder c:

  • disturbed behavior
  • thinking
  • emotions
  • perceptions
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2
Q

what are some schizo (+) sx’s?

A
  1. hallucinations/delusions
  2. thought disorder
  3. perceptual disturbances
  4. incongruous mood
  5. increased motor function
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3
Q

what are some schizo (-) sx’s?

A
  1. blunted affect
  2. poverty of speech
  3. diminished motivation
  4. social withdrawal
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4
Q

what are some cognitive sx’s of schizo?

A

deficits in memory and cognitive control of behavior

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5
Q

schizo (+) sx’s biological basis?

A

linked to overactivity of mesolimbic pathway.

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6
Q

Schizo (-) and cognitive sx’s biological basis?

A

hypoactivity of the mesocortical pathway

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7
Q

what is the dopamine hypothesis of schizo?

A

excessive dopaminergic activity plays a role.
rx’s increase activity = increase/produce (+) psychotic sx’s
- ex) amphetamine and cocaine
rx’s decrease activity = decrease/stop (+) sx’s.

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8
Q

what are 4 well-defined dopamine pathways in the brain?

A
  1. mesolimbic pathway
  2. nigrostriatal pathway
  3. mesocortical pathwya
  4. tuberoinfundibular pathway
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9
Q

describe mesolimbic pathway

A

midbraine to limbic system.
role: emotional behaviors
hyperactive = (+) psychotic sx’s
block D2 receptors = antipsychotic effects

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10
Q

describe nigrostriatal pathway

A

substantia nigra to basal ganglia
role: controls motor movements
block D2 recpetors = disorders of movement can appear
part of extrapyramidal nervous system.
- blck dopamine recpetors can give motor a.e AKA extrapyramidal rxns.

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11
Q

describe mesocortical pathway

A

midbrain to prefrontal cortex.
reduce activity = (-) and cognitive sx’s.
block D2 recptors = cause/worsen sx’s

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12
Q

Describe tuberoinfundibular pathway

A

hypothalamus to anterior pituitary.
dopamine released from these neurons inhibits prolactin secretion.
when blocked = prolactin level rise, can cause galactorrhea.

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13
Q

what are some classical antipsychotic drugs?

A
  1. chlorpromazine
  2. fluphenazine
  3. haloperidol
  4. thioridazine
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14
Q

what are some atypical antipsychotic drugs?

A
  1. clozapine
  2. risperidone
  3. olanzapine
  4. quetiapine
  5. ziprasidone
  6. aripiprazole
  7. paliperidone
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15
Q

what are HIGH potency classical antipsychotic drugs?

A
  1. fluphenazine

2. haloperidol

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16
Q

what are LOW potency classical antipsychotic drugs?

A
  1. chlorpromazine

2. thioridazine

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17
Q
  1. chlorpromazine
  2. fluphenazine
  3. haloperidol
  4. thioridazine

MOA?

A

block D2 receptors in the mesolimbic pathway

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18
Q

what are atypical antipsychotics drugs?

A

they have higher affinities for other receptors than D2 receptors

ex)

  1. clozapine: high affinity for D1, D4, 5HT2, musc, and a-adrenergic
  2. risperidone: 5HT2
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19
Q

what are some common properties of atypical antipsychotics?

A
  1. dual antagonism at 5HT2A and D2
  2. part of action is d/t 5HT block
  3. less likely to cause EPRs than classical agents
  4. less likely to cause tardive dyskinesea
  5. less likely to cause increases prolactin
  6. more effective at treating (-) sx’s
  7. effective in refractory populations
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20
Q

properties of clozapine?

A

prototype of the atypical agents

21
Q

properties of risperidone?

A

causes EPR, rare at therapeutic doses

22
Q

properties of paliperidone?

A

9-hydroxyrisperidone, active metabolite of risperidone

23
Q

properties of aripiprazole?

A

partial agonist at D2 and 5HT1A

antagonist at 5HT2A

24
Q

what are two atypical antipsychotics least likely to induce EPR?

A
  1. clozapine

2. quetiapine

25
Q

antipsychotics actions?

A
  • reduce hallucination/agitation
  • calming effect
  • don’t depress intellectual function
  • motor incoordination is minimal
  • onset is
26
Q

antipsychotics antiemetic effects?

A

block D2 receptors of the chemoreceptor trigger zone in the medulla.

exceptions: aripiprazole and thioridazine (no antiemetic)

27
Q

antipsychotic metabolisM?

A

CYP2D6, CYP1A2, CYP3A4

don’t interfere c the metabolims of other drugs.

28
Q

causes of antipsychotic extrapyramidal rxns?

A
  • assoc c high D2 potency.
    • rx: haloperidol and fluphenazine

less likely with:

  1. low D2 potency: clorpromazine or thioridazine
  2. strong anticholinergic: thioridazine and chlorpromazine
  3. atypical antipsychotics
29
Q

what are some Extrapyramidal rxns?

A
  1. parkinsonism
  2. dystonia
  3. akathisia
30
Q

tx for parkinsonism?

A

antimuscarinics:

  1. benztropine
  2. trihexyphnidyl
  3. diphenhydramine
  4. amantadine

Levodopa should never be used in these pts.

31
Q

tx for dystonia?

A
  1. benztropine
  2. trihexyphenidyl
  3. diphenhydramine
32
Q

tx for akathisia?

A
  1. reduction of dosage or change rx
  2. clonazepam
  3. propranolol.
33
Q

what is tardive dyskinesia?

A

late-occuring syndrome of abnl chreoathetoid movements.

unwanted effect of antipsychotics
potentially irreversible
may be d/t dopamine receptor up-regulation

34
Q

management of tardive dyskinesia?

A
  1. d/c or reduce rx.
  2. eliminate all rx’s c central anticholinergic action (antiparkinsonian and TCAs)
  3. diazepam

clozapine is rec’d for pts c tardive dyskinesia who require antipsychotics.

35
Q

what is neuroleptic malignant syndrome?

A

rare and life-threatening disorder.

  • rigidity, tremor, hyperthermia
  • altered mental status
  • autonomic instability
  • elevated WBC and CK
  • myoglobinemia c potential nephrotoxicity
36
Q

tx of neuroleptic malignant syndrome?

A
  1. dantrolene

2. bromocriptine

37
Q

what antipsychotics cause sedation?

A

low-potency and atypical agents

d/t block central H1 receptrs.

38
Q

which antipsychotics cause seizures?

A
  1. chlorpromazine

2. clozapine

39
Q

how can antipsychotics produce autonomic effects?

A

block musc receptors, producing anticholinergic effects.

  1. block alpha1 receptors = orthostatic hypotension, impaired ejaculation.
40
Q

which antipsychotics cause toxic and allergic rxns?

A

clozapine causes agranulocytosis

regular blood cell counts are mandatory.

41
Q

what are some endocrine and metabolic effects c antipsychotics?

A
  1. prolactin secretion (less c atypical)
    - block D2 recpetors in pituitary.
    - women: amenorrhea-galactorrhea, infertility
    - men: loss libido, infertility and impotence
  2. weight gain
    - majority atypical
42
Q

which antipsychotics cause high incidence of cardiac toxicity?

A
  1. thioridazine (QTc- and T-wave changes)

2. ziprasidone (prolong QTc)

43
Q

which antipsychotics cause ocular complications?

A
  1. chlorpromazine - deposits in corean and lens.

2. thioridazine - retinal deposits.

44
Q

what are some psychiatric indications for antipsychotics?

A
  1. schizo
  2. bipolar
  3. suppression of tics in tourretts
  4. control disturbed behavior in alzheimers
  5. adjuncts to antidepressants in tx-resistant major depression.
  6. combo c antidepressants in psychotic depression
  7. irritability assoc c autism (DOC risperidone)
45
Q

what are some non-psychiatric indications for antipsychotics?

A
  1. nausea and vomiting

2. droperidol is used in combo c fentanyl in neurolept-anesthesia

46
Q

what are DOC for antipsychotics?

A
  1. atypical preferred d/t:
    - benefit (-) sx’s and cognition
    - diminished risk of EPRs and tardive dyskinesia
    - lesser increase in prolactin levels.
  2. risperidone - most prescribed
  3. clozapine - d/t potential for agranulocytosis is reserved for refractory pts.
47
Q

antipsychotic in pregancy?

A

cat C
clozapine is catB

risks (greater c atypicals):

  1. hyperglycemia
  2. weight gain
48
Q

define psychosis?

A

sustained mental state of impaired contact c reality

Pharmacology (13 decks)

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