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8. Psychopharmacology > Antipsychotics III (specific antipsychotics, tables) > Flashcards

Antipsychotics III (specific antipsychotics, tables) Flashcards

1
Q

what is the half life of haldol

A

12-38 hours PO

3 weeks IM (long acting)

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2
Q

indications for haldol use

A

schizophrenia

bipolar disorder

behavioural disturbances in dementia

acute agitation

tics and vocal utterances in Tourettes disorder

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3
Q

starting dose of haldol

A

2mg po

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4
Q

titration of haldol

A

2mg po q2weeks

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5
Q

maximum dose of haldol

A

15mg po (max 25mg)

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6
Q

what is the dose of haldol to use if using it to manage acute agitation

A

2-5mg q1h PO/IM (max 20mg/24hours)

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7
Q

which is the most second generation-like FGA

A

loxapine

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8
Q

which is the most first generation-like SGA

A

risperidone

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9
Q

which APs are approved by health canada for pediatric uses

A

chlorpromazine

haldol

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10
Q

which AP has been banned by health canada for cardiac arrhythmia risk

A

thioridazine

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11
Q

loxapine is not recommended below what age

A

below 16

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12
Q

in general, how is metabolism of APs different in children from adults

A

quicker metabolism in children compared to adults (i,e which is why you see BID/TID dosing of APs in kids… they have shorter half life in kids)

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13
Q

what is the T1/2 of risperidone in kids compared to adults

A

kids–> 2 hours

adults–> 12-24 hours

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14
Q

which SGAs need to be taken with food

A

ziprazidone and lurasidone

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15
Q

which AP is the LEAST toxic in the context of liver failure

A

paliperidone

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16
Q

what should you think if someone is on clozapine and has elevated prolactin

A

theyre probably SEIZING

clozapine shouldnt cause much, if any, prolacting increase but DOES markedly lower seizure threshold

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17
Q

what side effect is quite specific to quetiapine

A

hypothyroid

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18
Q

what side effect is quite specific to olanzapine

A

impaired insulin

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19
Q

what enzymes metabolize risperidone

A

CYP 2D6 and 3A4

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20
Q

does risperidone have higher affinity for 5HT2A receptors or D2 receptors?

A

higher affinity for 5HT2A

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21
Q

on which receptors does risperidone act

A

D2

5HT2A

alpha 1

alpha 2

H1

(antagonism)

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22
Q

list indications for risperidone

A

schizophrenia

bipolar I

bipolar II

MDD (adjunctive)

OCD

BPSD

ASD (risperidone–should use low doses)

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23
Q

what is the maximum dose of risperidone

A

16mg

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24
Q

how long does it take for risperidone consta (IM long acting) to take effect

A

21 days

therefore requires 21 days of oral supplementation when starting treatment with IM formulation

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25
Q

what is the oral equivalent of 25mg IM risperidone

A

risperidone 25mg IM is = to about 2-3mg oral risperidone

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26
Q

care must be taken when prescribing risperidone with a particular SSRI. which SSRI is this? why?

A

fluoxetine

because concomitant Rx can increase plasma concentrations of risperidone by 2-3x as fluoxetine is CYP 2D6 inhibitor (which metabolizes risperidone)

*sertraline is also a moderate inhibitor but may increase levels of risperidone but not levels of the active metabolite

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27
Q

at what doses dose risperidone act more like a FGA

A

6-8 mg (higher doses)

this is a dose responsive relationship with dose and incidence of EPS

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28
Q

do you need to be careful with risperidone in renal impairment

A

yes–> start lower, use split doses, slower titration

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29
Q

why do we consider the blockade of 5HT2A receptors a positive thing with risperidone

A

causes enhancement of dopamine release in certain brain areas–> thus reduces motor side effects and possibly improves cognitive and affective symptoms

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30
Q

list 5 FDA approved indications for risperidone

A

schizophrenia

delaying relapse in schizophrenia

other psychotic disorders

acute mania (oral, monotherapy or with lithium/valproate)

ASD related irritability in kids 5-16

also indicated for:
bipolar maintenance
bipolar depression
behavioural disturbances in dementias
behavioural disturbances in kids and teens
disorders associated with impulse control

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31
Q

how quickly should you up-titrate risperidone

A

about 1mg per week on inpatient

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32
Q

what is the therapeutic range of risperidone for acute psychosis and bipolar disorder

A

2-8mg per day PO (risk of EPS higher above 6mg)

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33
Q

what is the therapeutic range for risperidone in kids or the elderly

A

0.5-2mg po daily

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34
Q

what is the starting dose of risperidone consta

A

25mg IM q2weeks

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35
Q

what is the max dose of risperidone consta

A

50mg IM q2weeks

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36
Q

what monitoring should be done for risperidone

A

weight/BMI

waist circumference

BP

lipid profile

fasting glucose

prolactinn levels when indicated

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37
Q

is risperidone generally lethal in monotherapy overdose

A

rarely

could see sedation, rapid HR, convulsions, low BP, difficulty breathing

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38
Q

other than fluoxetine and sertraline, what other antidepressant should be used with caution with risperidone

A

buproprion (also CYp 2D6 inhibitor)

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39
Q

how many LAI injections of risperidone are needed to achieve steady state

A

4

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40
Q

does risperidone prevent recurrences of mania in bipolar disorder

A

yes

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41
Q

what is the most frequently used AP in kids

A

risperidone

*but safety and efficacy not well established in data

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42
Q

what is the increased risk of cerebrovascular events in the elderly when using risperidone

A

base 1/100 per year to 2/100 per year

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43
Q

what is the increased mortality associated with dementia related psychosis

A

from base 1/100 per year to 2/100 per year….

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44
Q

what do the early findings show with regard to risperidone use in pregnancy

A

early findings show infants exposed to risperidone in utero do not show adverse consequences

may be preferable to anticonvulsant mood stabilizers if tx required during pregnancy

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45
Q

where does a significant portion of paliperdone metabolism occur

A

in the kidneys

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46
Q

why is paliperidone best in patients with hepatic failure

A

because it is an active metabolite so does not undergo much metabolism in the liver

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47
Q

starting dose of paliperidone

A

3mg po daily

increase by 3mg every 7 days

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48
Q

what is the maximum dose of paliperidone PO

A

12mg

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49
Q

where must invega sustenna IM doses be given to achieve higher plasma concentrations

A

in the deltoid

NOT the gluteal

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50
Q

how are paliperidone loading doses administered

A

standard for all patients

150mg IM day 1 and 100mg IM day 8

(150mg of paliperidone is given as 234 mg of paliperidone palmitate)

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51
Q

when should the 1st monthly maintenance dose of paliperidone be given

A

5 weeks after the very first injection (regardless of when second loading dose given)

52
Q

what must be trialled before invega trinza can be started

A

must have used invega sustenna for at least 4 months prior

53
Q

does the product monograph for paliperidone recommend PO bridging when starting a LAI?

A

no–> BUT these studies were done in people already at steady state on the PO

thus, if patient is AP naive or not adherent to meds it “makes clinical sense” to do oral bridge for period of first two loading doses as long as no side effect concerns

54
Q

what are the benefits of IM paliperidone over IM risperidone

A

IM paliperidone has:

smaller needle

can be delivered into deltoid (risperidone is just gluteal)

monthly injection vs every 2 weeks

can be stored at room temp (consta must be refridgerated)

55
Q

what is the half life of abilify

A

75-94 hours (LONG!!)

56
Q

what is the starting dose of abilify

57
Q

what is the maximum dose of abilify

A

30 mg–> 20mg is typical dose

58
Q

how quickly do you titrate PO abilify

A

2-5 mg every 2-3 weeks

59
Q

is there a bleeding risk with abilify

A

doesnt seem to be but can have leucopenia/neutropenia/thrombocytopenia

60
Q

what side effects should you monitor for related to abilify’s partial dopamine agonism

A

may induce increase impulsivity (similar to those on L-dopa)

pathological gambling, compulsive eating, compulsive shopping, and compulsive sexual behaviour have been reported in those on abilify but its rare

61
Q

why was brexpiprazole developed

A

due to concerns about impulsive behaviours with abilify

62
Q

what is the recommended dose of lurasidone

A

40-80mg po daily (single dose)

63
Q

is titration needed when starting lurasidone

64
Q

what else must be taken with lurasidone

A

a meal/food of at least 350 calories

(if not, absorption is reduced by 50%)

65
Q

what blood test may be possible biomarker for treatment response to lurasidone

A

CRP

responses to high or low dose lurasidone are linearly related to baseline CRP levels–> possible biomarker for response

66
Q

is there QTc prolongation risk with lurasidone

A

no–> its an “improved” ziprasidone

67
Q

half life of quetiapine

A

6-12 hours

68
Q

what is a key feature that distinguishes all SGAs

A

antagonist at serotonin 5HT2A receptor

69
Q

at what receptor is quetiapine a partial agonist

A

serotonin 5HT1A

70
Q

which AP has the lowest affinity for the D2 receptor

A

quetiapine

71
Q

what is the effective target dose for treating acute mania with quetiapine

A

600mg po daily (range 400-800mg)

72
Q

indications for quetiapine

A

bipolar I and II
MDD
schizophrenia

73
Q

how quickly can you increase quetiapine in bipolar mania?

A

IR–> start at 50mg and increase by 100-200mg per day

XR–> start at 300mg daily and can increase by 300mg per day

74
Q

which has lower side effect profile, quetiapine IR or XR

A

XR (IR is more sedating)

75
Q

which AP is used in the treatment of parkinsons related psychosis

A

pimavanserin –> not yet approved in canada

76
Q

what is the mechanism of action of pimavanserin

A

NOT a dopamine receptor antagonist

it is a highly selective serotonin 5TH2A receptor antagonist

77
Q

is asenapine a good medication choice in the treatment of schizophrenia? why or why not?

A

no

very poor PO bioavailability if ingested–> must be taken SL

patient needs to avoid food + liquids for 10 min after SL admin

requires BID dosing

78
Q

which two antipsychotics are associated with greater risk of QTc prolongation

A

chlorpromazine and pimozide

79
Q

what benefits does loxapine have over haldol

A

more sedation (good for PRN)

less akathesia

lower risk of QTc prolongation

80
Q

what SGA is health canada approved for BPSD

A

risperidone

81
Q

what is one benefit of amisulpride

A

essentially no cholinergic, histaminergic or alpha adrenergic antagonism

82
Q

should you use risperidone in pregnancy

83
Q

risperidone is first line therapy for which 3 conditions other than psychosis

A

1st line monotherapy mania

1st line ADJUNCT for MDD

1st line ADJUNCT for OCD

84
Q

is risperidone first line for tics

A

no 2nd line

85
Q

what AP is commonly used in anorexia nervosa

A

olanzapine

86
Q

is olanzapine first line monotherapy for mania

A

no–> 2nd line monotherapy

87
Q

olanzapine is second line for bipolar I depression when combined with what other medication

A

fluoxetine

88
Q

are FGAs effective for treating negative symptoms of schizophrenia

A

generally no. effective for positive symptoms only

89
Q

is there a particular set of APs that are first line in schizophrenia

A

all APs are first line in schizophrenia but atypicals tend to be better tolerated

90
Q

max dose of olanzapine

91
Q

max dose of loxapine

A

100mg /day

92
Q

max dose of paliperidone

A

12mg / day

93
Q

max dose of lurasidone

A

160mg / day

94
Q

what is the only AP to be excreted by the kidneys

A

paliperidone

95
Q

does paliperidone affect QTc more or less than risperidone

96
Q

what are particular side effects with lurasidone

A

nausea

elevated triglycerides

97
Q

what is likely the most weight neutral AP

A

ziprasidone

98
Q

how do you dose ziprasidone

A

must be BID

99
Q

max dose of ziprasidone

100
Q

can paliperidone be used for mania

A

yes–1st line monotherapy

101
Q

can lurasidone be used for mania

A

no–but is first line monotherapy for bipolar depression

102
Q

can ziprasidone be used for mania

A

yes–2nd line monotherapy for mania

103
Q

what effect does abilify have on prolactin

A

lowers prolactin–> due to partial D2 agonism

can combine with other APs when developing elevated prolactin on an otherwise effective agent

104
Q

name the ONLY 1st line treatment for bipolar II depression

A

quetiapine

105
Q

what AP might you consider if someone is complaining about sexual side effects from other APs

106
Q

in addition to psychosis, what disorders does the following AP treat:

abilify

A

mania–> 1st line monotherapy

bipolar maintenance 1st line

MDD–> 1st line adjunct

OCD–> 1st line adjunct

tics–> 2nd line

irritability/aggression in autism

107
Q

in addition to psychosis, what disorders does the following AP treat:

quetiapine

A

MDD–> 2nd line monotherapy and 1st line adjunct

mania–> 1st line monotherapy

bipolar II + II depression–> 1st line monotherapy

bipolar maintenance

GAD–> 2nd line

108
Q

in addition to psychosis, what disorders does the following AP treat:

ziprasidone

A

mania–> 2nd line monotherapy

109
Q

in addition to psychosis, what disorders does the following AP treat:

lurasidone

A

bipolar I depression–> monotherapy + in combo

110
Q

in addition to psychosis, what disorders does the following AP treat:

paliperidone

A

mania–> 1st line monotherapy

111
Q

in addition to psychosis, what disorders does the following AP treat:

risperidone

A

mania–> 1st line monotherapy

MDD–> 1st line adjunct

OCD–> 1st line adjunct

tics–> 2nd line

irritability/aggression with autism

112
Q

in addition to psychosis, what disorders does the following AP treat:

olanzapine

A

mania–> 2nd line monotherapy

bipolar I depression–> 2nd line in combo with fluoxetine

MDD–> 2nd line adjunct

used in anorexia nervosa

113
Q

what medical issue do most APs address

A

nausea/vomiting

especially in cyclical vomiting associated with cannabis use

114
Q

in addition to psychosis, what disorders does the following AP treat:

brexpiprazole

A

MDD–> 2nd line adjunct

115
Q

in addition to psychosis, what disorders does the following AP treat:

asenapine

A

mania–> 1st line monotherapy

bipolar maintenance 1st line

116
Q

in addition to psychosis, what disorders does the following AP treat:

cariprazine

A

mania–> 1st line monotherapy

bipolar I depression–> 2nd line

117
Q

what is the max dose of brexpiprazole

118
Q

what is the starting dose of brexpiprazole

A

0.5-1mg / day

119
Q

what is the half life of brexpiprazole

A

90 hours (longer than abilify)

120
Q

what are the side effects of brexpiprazole

A

similar yo abilify

121
Q

what are the side effects of abilify

A

EPS

insomnia

rare impulse control disorders

minimal effect on QTc

few sexual side effects

less weight gain

122
Q

how do you dose asenapine

123
Q

name an AP that has a study showing its efficacy for negative symptoms of schizophrenia

A

cariprazine

124
Q

what is unique about cariprazine’s dopamine receptor action

A

it is a D3-preferring D3/D2 receptor partial agonist

125
Q

how does pimavanserin work at the 5HT2 receptor

A

inverse agonist

126
Q

does pimavanserin have affinity for D2 receptor

A

no affinity

nor does it have affinity for the muscarinic, histaminergic or adrenergic receptors

127
Q

what is the dosing of clopixol acuphase

A

50-150mg IM–> lasts 2-3 days

8. Psychopharmacology (21 decks)

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