Q2 Antipsychotic Drugs Flashcards

1
Q

many psychotherapeutic drugs produce their effects by increasing or decreasing the rate of

A
  • neuronal circuit output
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2
Q

antipsychotic drugs in schizophrenia only treat ______ symptoms

which symptoms

A
  • positive

- delusions and hallucinations

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3
Q

antipsychotic drugs are _______ of multiple receptors found throughout the brain and in peripheral tissues

A
  • competitive antagonists
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4
Q

what receptors do antipsychotic drugs antagonize

A
  • D2 dopamine
  • 5HT2A serotonin
  • M2/3 acetylcholine
  • alpha 1 NE
  • H1 histamine
  • K+ channel in cardiac tissue
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5
Q

the therapeutic effect of antipsychotic drugs is mediated by their _______ of _____ and ______ receptors

A
  • antagonism
  • dopamine
  • serotonin
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6
Q

some antipsychotic drugs are partial _______ for ____ and _____ receptors

A
  • agonists
  • dopamine
  • serotonin
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7
Q

first generation antipsychotic drugs are callled

second generation antipsychotic drugs are called

A
  • typical

- atypical

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8
Q

examples of first gen antipsychotic drugs

which are high potency and which are low potency

what does high potency/low potency mean

A
  • fluphenazine (HP)
  • haloperidol (HP)
  • chlorpromazine (LP)
  • high potency - low doses needed
  • low potency - high doses needed
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9
Q

examples of second gen antipsychotic drugs

A
  • clozapine
  • olanzapine
  • risperadone
  • aripiprazole

CORA (that creepy cartoon who needed an antipsychotic)

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10
Q

all antipsychotic drugs antagonize or partially agonize the ____ receptor in the _____ pathway which is though to be primarily responsible for their therapeutic inhibition of positive symptoms

A
  • D2 dopamine receptor

- mesocortical

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11
Q

in schizophrenia, hyperstimulation of the ______ pathway which connects the ventral tegmental area to the prefrontal cortex causes excessive ___ to be released into the _____

A
  • mesocorticol dopaminergic
  • dopamine
  • prefrontal cortex
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12
Q

the correlation between a drug’s affinity for the ____ receptor and its clinical effectiveness is extremely strong

A
  • D2 receptor
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13
Q

drugs with higher D2 receptor affinity require _____ doses to be therapeutically effective

A
  • lower
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14
Q

research has shown that only ____% of the D2 receptors in the prefrontal cortex need to be occupied by a drug in order to produce a maximal clinical response

this is an example of _____ and it indicates that the dose of. drug can be titrated either up or down in order to find an optimal dose for each patient

A
  • 60%

- receptor reserve

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15
Q

while all antipsychotic drugs antagonize the 5HT2A serotonin receptor, the _____ generation drugs do so with higher affinity than the _____ drugs

  • this explains
A
  • second generation does so better than first generation

- explains inhibition of positive symptoms by second generation drugs

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16
Q

what toxicity results from antagonism of D2 receptors in non-therapeutic dopamine pathways

  • is this more prominent in first or second generation drugs? why?
A
  • extrapyramidal symptoms
  • more prominent in first
  • second generation has lower affinity for D2 dopamine receptor and antagonize with lower potency than 1st generation drugs
17
Q

extrapyramidal symptoms involve loss of

examples

A
  • skeletal muscle control
  • pseudoparksonism
  • acute dystonia
  • akathisia
  • tardive dyskinesia
18
Q

inhibition of the _____ pathway is responsible for the extrapyramidal symptoms of antipsychotic drugs

why

A
  • nigrostriatal

- responsible for skeletal muscle movement

19
Q

antipsychotic drug-induced changes in pituitary hormone secretion particularly _____ may also result from inhibition of dopamine receptors.

is this more common with first or second generation antipsychotic drugs

A
  • prolactin

- more common with first generation antipsychotic drugs

20
Q

inhibition of the _______ pathway is responsible for the hormonal effects of antipsychotic drugs

how

A
  • tuberoinfundibular pathway

- dopamine released from pituitary gland from tuberoinfundibular neurons to inhibit release of prolactin

21
Q

effects of hyperprolactinemia

A
  • gynecomastia
  • amenorrhea
  • decreased libido and sexual function
22
Q

Also associated with inhibition of dopaminergic (DA) pathways * is ____________ another important potential toxicity of __________ drugs

A
  • neuroleptic malignant syndrome (NMS)

- anti-epileptic drugs

23
Q

what condition is characterized by muscle rigidity, hyperthermia, and mental status changes such as agitation and dysautonomia

what treats the agitation

what treats the dopamine antagonism

what treats the muscle rigidity and hyperthermia

A
  • neuroleptic malignant syndrome
  • Benzodiazepines
  • Bromocriptine
  • Dantrolene
24
Q

how does Dantrolene treat muscle rigidity and hyperthermia

A
  • inhibits Ca2+ flow through ryanodine receptor

- reduces skeletal muscle contraction and reduces heat

25
Q

_____ is a constellation of symptoms including weight gain, dyslipidemia, hyperglycemia, and T2DM

results from inhibition of _____ pathways

  • seem more often in first/second generation antipsychotic drugs
A
  • metabolic syndrome
  • serotenergic
  • seen more often with 2nd generation drugs
26
Q

___ generation drugs caused more weight gain than ____ generation drugs

A
  • 2nd generation causes more weight gain than first generation drugs
27
Q

anti-cholinergic/parasympathetic effects are more common with ____ potency ____ generation and some _____ generation drugs than ___ potency ________ generation drugs

A
  • low potency first generation and 2nd generation drugs

- than high potency first generation drugs

28
Q

most common anticholinergic toxicities of antipsychotic drugs

A
  • xerostomia
  • constipation
  • urinary retention
  • blurred vision
29
Q

antipsychotic drugs also produce toxicities through inhibition of the alpha 1 receptor with ______ being the most common

these toxicities are more prevalent with _____ potency ____ drugs and _____ drugs

how

A
  • orthostatic hypotension
  • low potency first generation
  • second generation
  • inhibit binding of NE and EPI
  • induce vasodilation and lower BP
30
Q

_____ is common due to H1 receptor blockade

most common with ___ potency ____ generation drugs and _____ generation drugs

how?

A
  • sedation
  • low potency 1st generation
  • second generation
  • cross the blood brain barrier
31
Q

prolonged QT is common first 1st and 2nd generation antipsychotic drugs due to _________

A
  • cardiac K+ blockade
  • slow efflux of K+ from myocytes
  • extends repolarization which prolongs AP and QT
32
Q

important toxicity of clozapine

A
  • agranulocytosis

- neutropenia