Antipsychotics - Linger Flashcards

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1
Q

aripiprazole

A

atypical antipsychotic

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2
Q

lurasidone

A

atypical antipsychotic

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3
Q

olanzapine

A

atypical antipsychotic

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4
Q

quetiapine

A

atypical antipsychotic

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5
Q

risperidone

A

atypical antipsychotic

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6
Q

ziprasidone

A

atypical antipsychotic

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7
Q

clozapine

A

special use atypical antipsychotic

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8
Q

chlorpromazine

A

typical low potency antipsychotic

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9
Q

haloperidol

A

typical high potency antipsychotic

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10
Q

atypical

A

because dramatic reductionin extrapyramidal side effects

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11
Q

dopamine hypothesis

A

evidence for:

  • antipsychotics - some block D2 receptors postsynaptic
  • drugs increase DA - aggravate schizophrenia or trigger psychosis
  • DA receptors - more in brain of schizophrenic
  • post-mortem - more DA and D2 receptorrs in schizophrenic nucleus accumbens, caudate, putamen

evidence against:

  • decreased cortex/hippocampus DA activity - underlie cognitive impairment and negative sx of schizophrenia
  • many atypicals - lower affinity for D2 receptors - but effective for schizophrenia tx

dopamine hypothesis - oversimplification

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12
Q

serotonin hypothesis

A

hallucinogenics - LSD, mescalin

-serotonin receptor agonists

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13
Q

bio basis of schizophrenia

A

DA, serotonin, glutamate imbalance

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14
Q

glutamate hypothesis

A

low function NMDA receptors

  • on GABA internerous
  • induce disinhibition of glutamatergic activity - hyperstimulation
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15
Q

atypical antipsychotics

A

greater effect at 5-HT2a than D2 receptors

-dissociation of EPS and antipsychotic efficacy

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16
Q

phenothiazine derivative

A

chlorpromazine

aliphatic

more sedation and weight gain

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17
Q

butyrophenone derivative

A

haloperidol

high level of EPS

more potent, fewer autonomic effects

  • but more EPS
  • compared to phenothiazines
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18
Q

cholinergic rebound and withdrawal movement disorders

A

clozapine

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19
Q

cholinergic rebound

A

also with chlorpromazine and thioridazine

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20
Q

relapse to schizo after stop taking drug

A

most - 6 months

except - clozapine - rapid and severe relapse

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21
Q

efficacy of typical antipsychotics

A

D2 receptor affects

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22
Q

atypical antipsychotics

A

block 5-HT2A more potently than inhibit D2 receptors

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23
Q

mesolimbic mesocortical pathway

A

behavior and cognition

VTA - projection to limbic system and neocortex

inhibition of DA activity - antipsychotic effect

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24
Q

nigrostriatal pathway

A

coordination of movement

substantia nigra to dorsal striatum (caudate/putamen)

inhibit - EPS

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25
Q

tuberoinfundibular system

A

PRL release

DA inhibits

arcuate nucleus and periventricular neurons
-to hypothalamus and posterior pituitary

pathway inhibited by antipsychotics - PRL release

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26
Q

D1-like

A

D1 and D5

increase cAMP - activate Gs and adenylyl cyclase

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27
Q

D2-like

A

D2, D3, and D4

decreased cAMP - Gi - inhibit Ca channels, open K channels

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28
Q

D2 receptors

A

role in action of antipsychotics

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29
Q

D2 binding affinity

A

strong correlation with antipsychotic potency and EPS

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30
Q

typical antipsychotics

A

need 60% occupancy of striatal D2 receptors for antipsychotic

EPS at 80%

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31
Q

atypical antipsychotics

A

need 30-50% occupancy of striatal D2 receptors for antipsychotic

bc concurrent high occupancy at 5-HT2A receptors

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32
Q

aripiprazole

A

high D2 occupancy - without EPS

partial agonist at D2

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33
Q

catatonic schizo tx

A

benzos

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34
Q

reduce risk of suicide in schizoaffective pt

A

clpzapine

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35
Q

non-psych indications of antipsychotics

A

antiemetic

neuroleptanesthesia

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36
Q

first line tx of schizophrenia

A

atypical antipsychotics

-except clozapine and olanzapine

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37
Q

effective drug tx

A

both positive and negative sx improve

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38
Q

acute control uncoop patient

A

haloperidol

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39
Q

autonomic side effect

A

chlorpromazine

40
Q

severe EPS

A

haloperidol

41
Q

agranulocytosis

A

clozapine

42
Q

lower seizure threshold

A

clozapine

43
Q

QT prolongation

A

ziprasidone

44
Q

dibenzothiazepine

A

quetiapine

45
Q

dihydroindolone

A

ziprasidone

46
Q

dihydrocarbostyril

A

aripiprazole

47
Q

thienobenzodiazepine

A

olanzapine

48
Q

benzisoxazole

A

risperidone

49
Q

dibenzodiazepine

A

clozapine

50
Q

butyrophenone

A

haloperidol

51
Q

weight gain

A

olanzapine

52
Q

atypicals

A

wide therapeutic index

53
Q

adverse of clozapine

A

agranulocytosis and myocarditis

only patients refractory high dose other agents
-or suicidal

54
Q

full effect of tx

A

16-20 weeks

55
Q

electroconvulsive therapy

A

adjunct for tx of mood sx and positive sx

augment - clozapine - max dose of clozapine ineffective

56
Q

anhedonia

A

inablity to experience pleasure

57
Q

akathisia

A

uncontrolled restlessness - can’t sit still

58
Q

tx of EPS

A

anticholinergic

antimuscarinic (antihistamine - diphenhydramine)

59
Q

early motor effects antipsychotics

A

EPS - 1-3 days
parkinsonism, increased activity

akathisia - can’t sit still

acute dystonic rxns

EPS and dystoni tx - anticholinergic or antihistamine

never use levodopa in these patients

60
Q

later motor effects of antipsychotics

A

tardive dyskinesia

with chronic tx - months/years

writhing movements of tongue, face body - choreoathetoid

imbalance of cholinergic vs. dopaminergic activity in motor pathways

61
Q

lower risk of tardive dyskinesia

A

clozapine or quetiapine

62
Q

seizure threshold

A

lowered with most antipsychotics

clozapine - seizures in 2-5% of patients

63
Q

typical antipsychotics

A

affinity for muscarinic cholinergic and a1 adrenergic receptors

anti-PS effect

loss of accomodation, dry mouth, difficulty urinating, constipation

orthostatis hypotension, dizzy, sedated, impotent, failure to ejaculate

switch to newer typical agent

64
Q

high risk of weight gain

A

clozapine

olanzapine

65
Q

intermediate risk of weight gain

A

iloperidone
paliperidone
quetiapine
risperidon

66
Q

low risk weight gain

A

asenapine

67
Q

lowest risk of weight gain

A

lurasidone
aripiprazole
ziprasidone

68
Q

weight gain

A

follow food intake, BMI, blood sugars, and lipids

hyperglycemia and hyperlipidemia common problems

69
Q

hyperPRL

A

with antipsychotic use

loss of DA inhibition of PRL secretion

amenorrhea-galactorrhea, infertile, osteoporosis - women
infertility, loss of libido, impotent, gynecomastia - men

more with older typical antipsychotics
-as well as risperidone and paliperidone

70
Q

agranulocytosis

A

with clozapine

need to monitor CBC

  • weekly first 6 months
  • every 3 weeks thereafter
71
Q

QT prolongation

A

with several antipsychotics

risk sudden death

avoid antiarrhythmics and erythromycin (prolong QT)

72
Q

antipsychotics in pregnancy

A

atypical preferred

considered relatively safe - category C

73
Q

neuroleptic malignant syndrome

A

life-threatening acute severe parkinsonism, muscle rigid, autonomic instability, HTN, hyperthermia, stress leukocytosis (infection misdiagnosis)

side effect of antipsychotics

tx - supportive - cool body, muscle relaxants

74
Q

positive sx

A

excess DA - mesolimbic system

75
Q

negative sx

A

loss of DA - mesolimbic system

76
Q

dopamine receptors

A

GPCRs

77
Q

typical vs atypical

A

typical - positive sx treatment

atypical - positive/negative sx treatment

78
Q

loss of accomodation, dry mouth, difficulty urinating, constipation

A

muscarinic cholinoceptor blockade

79
Q

orthostatic hypotension, dizzy, sedation, failure to ejaculate

A

a-adrenoreceptor blockade

80
Q

parkinsons syndrome, akathisia, dystonia

A

dopamine receptor blockade

81
Q

weight gain

A

combined H1 and 5-HT2 blockade

82
Q

endocrine changes

A

dopamine receptor blockade

83
Q

acute motor effects

A

D2 blockade basal ganglia - EPS

treatable

84
Q

late onset motor effects

A

tardive dyskinesia

imbalance - cholinergic deficiency and dopaminergic supersensitivity

may be irreversible

85
Q

tx tardive dyskinesia

A

decrease dose - initially get worse - improve over weeks

switch - quetiapine or clozapine

86
Q

more severe with haloperidol

A

EPS

87
Q

chlorpromazine

A

has activity at many receptors

so get unwanted effects

cholinergic, a-adrenergic, H1

low potent at D2

88
Q

tx bipolar depression

A

aripiprazole

less weight gain and hyperglycemia

89
Q

olanzapine

A

bind 5-HT2a, Ma, and H1 high affinity

severe weight gain

90
Q

aripiprazole

A

partial D2 agonist

91
Q

lurasidone

A

tx schizo and bipolar

D2 and 5-HT2 - high affinity

no QT prolongation

92
Q

quetiapine

A

low affinity D2 and 5-HT2

higher affinity H1 and alpha1 - sedation and orthostatic

off label use as sleep aid

QT prolongation - poor choice for those with heart issue

93
Q

risperidone

A

high affinity 5-HT2a, D2 and alpha1

highest EPS and hyperPRL

floppy iris syndrome before cataract surgery

94
Q

ziprasidone

A

high affinity 5-HT2a - lower affinity D2

CI - patient with recent MI - QT prolongation

95
Q

antiemesis

A

DA blockade

96
Q

neuroleptanesthesia

A

analgesia and amnesia

droperidol
fetanyil
nitrous oxide