Antipsychotics III (specific antipsychotics, tables) Flashcards
(127 cards)
1
Q
what is the half life of haldol
A
12-38 hours PO
3 weeks IM (long acting)
2
Q
indications for haldol use
A
schizophrenia
bipolar disorder
behavioural disturbances in dementia
acute agitation
tics and vocal utterances in Tourettes disorder
3
Q
starting dose of haldol
A
2mg po
4
Q
titration of haldol
A
2mg po q2weeks
5
Q
maximum dose of haldol
A
15mg po (max 25mg)
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)
7
Q
which is the most second generation-like FGA
A
loxapine
8
Q
which is the most first generation-like SGA
A
risperidone
9
Q
which APs are approved by health canada for pediatric uses
A
chlorpromazine
haldol
10
Q
which AP has been banned by health canada for cardiac arrhythmia risk
A
thioridazine
11
Q
loxapine is not recommended below what age
A
below 16
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)
13
Q
what is the T1/2 of risperidone in kids compared to adults
A
kids–> 2 hours
adults–> 12-24 hours
14
Q
which SGAs need to be taken with food
A
ziprazidone and lurasidone
15
Q
which AP is the LEAST toxic in the context of liver failure
A
paliperidone
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
17
Q
what side effect is quite specific to quetiapine
A
hypothyroid
18
Q
what side effect is quite specific to olanzapine
A
impaired insulin
19
Q
what enzymes metabolize risperidone
A
CYP 2D6 and 3A4
20
Q
does risperidone have higher affinity for 5HT2A receptors or D2 receptors?
A
higher affinity for 5HT2A
21
Q
on which receptors does risperidone act
A
D2
5HT2A
alpha 1
alpha 2
H1
(antagonism)
22
Q
list indications for risperidone
A
schizophrenia
bipolar I
bipolar II
MDD (adjunctive)
OCD
BPSD
ASD (risperidone–should use low doses)
23
Q
what is the maximum dose of risperidone
A
16mg
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
25
what is the oral equivalent of 25mg IM risperidone
risperidone 25mg IM is = to about 2-3mg oral risperidone
26
care must be taken when prescribing risperidone with a particular SSRI. which SSRI is this? why?
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
27
at what doses dose risperidone act more like a FGA
6-8 mg (higher doses)
this is a dose responsive relationship with dose and incidence of EPS
28
do you need to be careful with risperidone in renal impairment
yes--> start lower, use split doses, slower titration
29
why do we consider the blockade of 5HT2A receptors a positive thing with risperidone
causes enhancement of dopamine release in certain brain areas--> thus reduces motor side effects and possibly improves cognitive and affective symptoms
30
list 5 FDA approved indications for risperidone
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
31
how quickly should you up-titrate risperidone
about 1mg per week on inpatient
32
what is the therapeutic range of risperidone for acute psychosis and bipolar disorder
2-8mg per day PO (risk of EPS higher above 6mg)
33
what is the therapeutic range for risperidone in kids or the elderly
0.5-2mg po daily
34
what is the starting dose of risperidone consta
25mg IM q2weeks
35
what is the max dose of risperidone consta
50mg IM q2weeks
36
what monitoring should be done for risperidone
weight/BMI
waist circumference
BP
lipid profile
fasting glucose
prolactinn levels when indicated
37
is risperidone generally lethal in monotherapy overdose
rarely
could see sedation, rapid HR, convulsions, low BP, difficulty breathing
38
other than fluoxetine and sertraline, what other antidepressant should be used with caution with risperidone
buproprion (also CYp 2D6 inhibitor)
39
how many LAI injections of risperidone are needed to achieve steady state
4
40
does risperidone prevent recurrences of mania in bipolar disorder
yes
41
what is the most frequently used AP in kids
risperidone
*but safety and efficacy not well established in data
42
what is the increased risk of cerebrovascular events in the elderly when using risperidone
base 1/100 per year to 2/100 per year
43
what is the increased mortality associated with dementia related psychosis
from base 1/100 per year to 2/100 per year....
44
what do the early findings show with regard to risperidone use in pregnancy
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
45
where does a significant portion of paliperdone metabolism occur
in the kidneys
46
why is paliperidone best in patients with hepatic failure
because it is an active metabolite so does not undergo much metabolism in the liver
47
starting dose of paliperidone
3mg po daily
increase by 3mg every 7 days
48
what is the maximum dose of paliperidone PO
12mg
49
where must invega sustenna IM doses be given to achieve higher plasma concentrations
in the deltoid
NOT the gluteal
50
how are paliperidone loading doses administered
standard for all patients
150mg IM day 1 and 100mg IM day 8
(150mg of paliperidone is given as 234 mg of paliperidone palmitate)
51
when should the 1st monthly maintenance dose of paliperidone be given
5 weeks after the very first injection (regardless of when second loading dose given)
52
what must be trialled before invega trinza can be started
must have used invega sustenna for at least 4 months prior
53
does the product monograph for paliperidone recommend PO bridging when starting a LAI?
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
what are the benefits of IM paliperidone over IM risperidone
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
what is the half life of abilify
75-94 hours (LONG!!)
56
what is the starting dose of abilify
2-5 mg
57
what is the maximum dose of abilify
30 mg--> 20mg is typical dose
58
how quickly do you titrate PO abilify
2-5 mg every 2-3 weeks
59
is there a bleeding risk with abilify
doesnt seem to be but can have leucopenia/neutropenia/thrombocytopenia
60
what side effects should you monitor for related to abilify's partial dopamine agonism
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
why was brexpiprazole developed
due to concerns about impulsive behaviours with abilify
62
what is the recommended dose of lurasidone
40-80mg po daily (single dose)
63
is titration needed when starting lurasidone
no
64
what else must be taken with lurasidone
a meal/food of at least 350 calories
(if not, absorption is reduced by 50%)
65
what blood test *may* be possible biomarker for treatment response to lurasidone
CRP
responses to high or low dose lurasidone are linearly related to baseline CRP levels--> possible biomarker for response
66
is there QTc prolongation risk with lurasidone
no--> its an "improved" ziprasidone
67
half life of quetiapine
6-12 hours
68
what is a key feature that distinguishes all SGAs
antagonist at serotonin 5HT2A receptor
69
at what receptor is quetiapine a partial agonist
serotonin 5HT1A
70
which AP has the lowest affinity for the D2 receptor
quetiapine
71
what is the effective target dose for treating acute mania with quetiapine
600mg po daily (range 400-800mg)
72
indications for quetiapine
bipolar I and II
MDD
schizophrenia
73
how quickly can you increase quetiapine in bipolar mania?
IR--> start at 50mg and increase by 100-200mg per day
XR--> start at 300mg daily and can increase by 300mg per day
74
which has lower side effect profile, quetiapine IR or XR
XR (IR is more sedating)
75
which AP is used in the treatment of parkinsons related psychosis
pimavanserin --> not yet approved in canada
76
what is the mechanism of action of pimavanserin
NOT a dopamine receptor antagonist
it is a highly selective serotonin 5TH2A receptor antagonist
77
is asenapine a good medication choice in the treatment of schizophrenia? why or why not?
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
which two antipsychotics are associated with greater risk of QTc prolongation
chlorpromazine and pimozide
79
what benefits does loxapine have over haldol
more sedation (good for PRN)
less akathesia
lower risk of QTc prolongation
80
what SGA is health canada approved for BPSD
risperidone
81
what is one benefit of amisulpride
essentially no cholinergic, histaminergic or alpha adrenergic antagonism
82
should you use risperidone in pregnancy
AVOID
83
risperidone is first line therapy for which 3 conditions other than psychosis
1st line monotherapy mania
1st line ADJUNCT for MDD
1st line ADJUNCT for OCD
84
is risperidone first line for tics
no 2nd line
85
what AP is commonly used in anorexia nervosa
olanzapine
86
is olanzapine first line monotherapy for mania
no--> 2nd line monotherapy
87
olanzapine is second line for bipolar I depression when combined with what other medication
fluoxetine
88
are FGAs effective for treating negative symptoms of schizophrenia
generally no. effective for positive symptoms only
89
is there a particular set of APs that are first line in schizophrenia
all APs are first line in schizophrenia but atypicals tend to be better tolerated
90
max dose of olanzapine
30mg
91
max dose of loxapine
100mg /day
92
max dose of paliperidone
12mg / day
93
max dose of lurasidone
160mg / day
94
what is the only AP to be excreted by the kidneys
paliperidone
95
does paliperidone affect QTc more or less than risperidone
less
96
what are particular side effects with lurasidone
nausea
elevated triglycerides
97
what is likely the most weight neutral AP
ziprasidone
98
how do you dose ziprasidone
must be BID
99
max dose of ziprasidone
80mg BID
100
can paliperidone be used for mania
yes--1st line monotherapy
101
can lurasidone be used for mania
no--but is first line monotherapy for bipolar depression
102
can ziprasidone be used for mania
yes--2nd line monotherapy for mania
103
what effect does abilify have on prolactin
lowers prolactin--> due to partial D2 agonism
can combine with other APs when developing elevated prolactin on an otherwise effective agent
104
name the ONLY 1st line treatment for bipolar II depression
quetiapine
105
what AP might you consider if someone is complaining about sexual side effects from other APs
abilify
106
in addition to psychosis, what disorders does the following AP treat:
abilify
mania--> 1st line monotherapy
bipolar maintenance 1st line
MDD--> 1st line adjunct
OCD--> 1st line adjunct
tics--> 2nd line
irritability/aggression in autism
107
in addition to psychosis, what disorders does the following AP treat:
quetiapine
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
in addition to psychosis, what disorders does the following AP treat:
ziprasidone
mania--> 2nd line monotherapy
109
in addition to psychosis, what disorders does the following AP treat:
lurasidone
bipolar I depression--> monotherapy + in combo
110
in addition to psychosis, what disorders does the following AP treat:
paliperidone
mania--> 1st line monotherapy
111
in addition to psychosis, what disorders does the following AP treat:
risperidone
mania--> 1st line monotherapy
MDD--> 1st line adjunct
OCD--> 1st line adjunct
tics--> 2nd line
irritability/aggression with autism
112
in addition to psychosis, what disorders does the following AP treat:
olanzapine
mania--> 2nd line monotherapy
bipolar I depression--> 2nd line in combo with fluoxetine
MDD--> 2nd line adjunct
used in anorexia nervosa
113
what medical issue do most APs address
nausea/vomiting
especially in cyclical vomiting associated with cannabis use
114
in addition to psychosis, what disorders does the following AP treat:
brexpiprazole
MDD--> 2nd line adjunct
115
in addition to psychosis, what disorders does the following AP treat:
asenapine
mania--> 1st line monotherapy
bipolar maintenance 1st line
116
in addition to psychosis, what disorders does the following AP treat:
cariprazine
mania--> 1st line monotherapy
bipolar I depression--> 2nd line
117
what is the max dose of brexpiprazole
4mg/day
118
what is the starting dose of brexpiprazole
0.5-1mg / day
119
what is the half life of brexpiprazole
90 hours (longer than abilify)
120
what are the side effects of brexpiprazole
similar yo abilify
121
what are the side effects of abilify
EPS
insomnia
rare impulse control disorders
minimal effect on QTc
few sexual side effects
less weight gain
122
how do you dose asenapine
BID
123
name an AP that has a study showing its efficacy for negative symptoms of schizophrenia
cariprazine
124
what is unique about cariprazine's dopamine receptor action
it is a D3-preferring D3/D2 receptor partial agonist
125
how does pimavanserin work at the 5HT2 receptor
inverse agonist
126
does pimavanserin have affinity for D2 receptor
no affinity
nor does it have affinity for the muscarinic, histaminergic or adrenergic receptors
127
what is the dosing of clopixol acuphase
50-150mg IM--> lasts 2-3 days
