031315 antipsychotics Flashcards

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1
Q

dopamine hypothesis

A

schizophrenia results from hyperactivity of dopaminergic neurons or their receptors, particularly those w terminals in limbic areas of brain

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2
Q

all antipsychotics interact w

A

dopamine systems

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3
Q

dopaminergic pathways

A

mesolimbic tract (dopamine hyperactivity leads to positive symptoms)

mesocortical tract (diminished dopaminergic activity leads to negative symptoms)

nigrostriatal pathway (dopamine blockade here results in increased extrapyramidal symptoms. blockade of 5HT2a results in decreased extrapyramidal symptoms)

tuberoinfundibular tract (dopamine blockade increases prolactin release)

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4
Q

newer antipsychotics block

A

serotonin 5HT2 receptors in forebrain and striatum in addition to dopamine, so EPS decreased

have greater potency with 5HT2 than w dopamine receptors

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5
Q

chlorpromazine

A

little potency (less affinity for dopamine D2 receptor)

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6
Q

in addition to dopamine receptors, what to typical antipsychotics bind to?

A

block histamine, muscarinic receptors (thus the side effects)

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7
Q

actions of antipsychotic drugs

A

decrease in psychotic behavior
sedation
extrapyramidal effects (dystonias, Parkinsonism, akathisia, tardive dyskinesia)

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8
Q

early vs late EPS side effects of antipsychotics

A

early: acute dystonia, parkinsonism, akathisia
late: tardive dyskinesia

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9
Q

newer atypicals have decreased

A

risk of extrapyramidal symptoms

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10
Q

other than EPS, what other side effects do antipsychotics have

A

anticholinergic

orthostatic hypotension (blockade of alpha receptors)

neuroendocrine effects (result of DA receptor blockade, causing increased prolactin)

allergic and idiosyncratic effects: liver, blood, cutaneous (esp newer drugs)

cardiac effects: thioridazine

decreased seizure threshold (esp phenothiazines)

weight gain, diabetes (more in atypicals-esp olanzapine, risperidone, clozapine, quetiapine)

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11
Q

neuroleptic malignant syndrome

A

potentially lethal hypodopaminergic side effct of antipsychotic drugs

hyperthermia, Parkinson-like symptoms, mutism, possible death

tx includes cooling and hydration, bromocriptine (DA agonist) and dantrolene (sk musc relaxer b/c musc rigidity is causing body temp to rise)

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12
Q

typical antipsychotics

A

phenothiazines
thioxanthine derivatives
butyrophenone derivative
pimozide

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13
Q

thioxanthine derivatives

A

pharm is similar to phenothiazines

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14
Q

butyrophenone derivatives

A

pharmacologically similar to high potency piperazine derivatives

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15
Q

pimozide’s use

A

antipsychotic

tx of Tourette’s (used when haloperidol doesn’t work)

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16
Q

advantages of atypical antipsychotics over typicals

A
  • lower risk of EPS (better compliance)
  • poossible lower incidence of tardive dyskinesia
  • improve negative symptoms perhaps
  • improve positive symptoms in many antipsychotic-resistant pts
  • perhaps less impact on cognitive functioning
  • perhaps more cost effective
17
Q

clozapine’s MOA

A

blocks D4 and 5HT2 receptors
muscarinic antagonist

improves neg symptoms

18
Q

side effects of clozapine

A

lowers seizure threshold more than other antipsychotics

fatal agranulocytosis

so it’s used when other drugs don’t work

19
Q

olanzapine’s MOA

A

5HT2 antagonist

D1 and D2 antagonist, some D4

20
Q

side effects of olanzapine

A
weight gain, diabetes
olanzapine abuse (b/c of sedating effects)
21
Q

intramuscular depot preps of atypical antipsychotics

A

risperidone

paliperidone

22
Q

quetiapine

A

similar to risperidone and olanzapine in effects on schizophrenia symptoms and side effects

23
Q

shorter half life drug

A

quetiapine (good for elderly)

24
Q

use of quetiapine

A

antipsychotic

augmentation in depression

25
Q

aripiprazole MOA

A

partial D2 agonist and 5HT2 antagonist

26
Q

use of aripiprazole

A

adjunct in depression

antipsychotic

27
Q

uses of antipsychotic drugs

A

acute psychotic episodes
chronic schizophrenia
manic episodes, bipolar disorder (aripiprazole, olanzapine, quetiapine, ziprasidone, rispierdone, asenapine, lurasidone)

schizoaffective disorder (paliperidone)

augmentation in depression (aripiprazole, olanzapine, quetiapine)

Tourette’s-haloperidol, pimozide

antiemesis-not thioridazine