Exam 4 spring P2 Flashcards
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1st generation antipsychotics
-movement problems: EPS and tardive dyskinesia
- very effective for treating positive symptoms ( worse negative/ cognitive symptoms)
chlorpromazine (thorazine)
-antihistamine effects
- 1st antipsychotic
promethazine (phenergan)
-antihistamine effects
-antiemetic
fluepenazine (oermitil,proxilin)
-eps
thoridazine (mellaril)
-anticholingeric AEs
-sedation
-sexual dysfunction
- cv risk
prochlorperazine (compazine)
-antiemetic
perpehnazine (trilafon)
-CATIE studies-> combo with anticholinergics
thiothixene (navane)
-modest EPS
Haloperidol (haldol)
-EPS
-most commonly used routine and PRN
-most common standing order
haloperidol decanoate
IM injection
-z-track technique
Milindone (Moban)
-moderate EPS
Pimozide (orap)
-used in tourettes to supress tics
2nd gen antipsychotics
- reduced EPS but more metabolic side effects
- D2 (postsynaptic) and 5HT2A (presynaptic) antagonism -> increased synthesis and release of DA
-13
clozapine (clozaril)
-weight gain, sedation, dry mouth, constipation, hypersalvation, GI hypomobility
- 1st atypical antipsychotic (very effective)
-agranulocytosis-> weekly blood monitoring
-third line
- risk of diabetes
- 1A2 substrate
- warning: neutropenia, orthostasis, bradycardia, syncope, seizures, myocarditit, cardiomyipathy
-QTc prolongation
-REMS: weekly, biweekly then every 4 weeks
Olanzapine (zyprexa)
-significant weight gain
-sedation
-risk of diabetes
-1A2 substrate
-high risk metabolic syndrome
-DRESS warning
Olanzapine/ samidorphan (lybalvi)
combo mitigates metabolic syndrome
zyprexa relpravv
-IM injection
-REMS program
-post dose delirium sedation syndrome -> Over dose (CNS depressant)
-can happen 24h later
loxapine (loxitane)
-older agent
-NET Inhibitor
adasuve (loxapine)
nasal spray for inhalation
-not commonly used
Quetiapine (seroquel)
-hypotension (alpha)
-sedation (H1)
-weight gain
-metabolite with antidepressant activity
-decent antipsychotic
-risk of diabetes
-3A4 substrate
-boxed warning -> suicidal ideation
risperidal consta
IM weekly
-must supplement with oral risperidone for first 4 weeks of treatment
perseris (risperidone)
q4w subQ injection
-abdominal
-3A4 inducer - 120mg dose
-may need oral supplementation
rykindo (risperidone)
q2w IM injection
-oral dose overlap is shorter than costa (7 days vs 21-28 days)
Uzedy (risperidone)
-abdominal or upper arm SubQ injection
-monthly or every other month
Risperidone (risperidol)
-low eps
-weight gain
-sedation
-hyperprolactinemia
-orthostasis
- designed to be both 5HT2A and D2 receptor antagonist A24
-2D6 substrate
paliperidone (invega)
-eps
-weight gain
- sedation
- hyperprolactinemia
-orthostasis
-renally eliminated (dose adjustment)
-QTc prolongation
invega sustenna (paliperidone)
-IM injection
-loading dose and booster w/in 7 days then every 4 weeks
-initial loading and booster given in deltoid
-no need for oral overlap
-may require dose adjustment -> renally eliminated
invega trinza (paliperidone)
-q3 months
- deltoid injection
-may be given to patient after 4 months of sustenna
-recommended for deltoid
-renal considerations
invega hafyra (paliperidone)
q6m gluteal IM injection
-may be initiated after sustenna 4 months or 1 dose of trinza
-gluteal only
IIoperidone (fanapt)
-structurally related to risperidone
-very potent at alpha 1 receptors
-high risk for orthostasis and syncope
-QTc prolongation
-2D6 substrate
aloperidone
sucks
ziprasidone (Geodon/ Zeldox)
- QT prolongation
-5HT2A, D2, alpha 1 affinity
-QTc prolongation
-DRESS warning - take with food
-3A4 substrate
asenapine (saphris)
-antihistamine
-dopaminergic
-alpha antimuscarinic AE
-5HT2A
-D2 antagonist
-Sublingual ONLY
-and patch formulations
-1A2 substrate
-QTc prolongation
asenapine transdermal patch
apply every 24h
-reduce dose if given with strong 1A2 inhibitors-> fluvoxamine
lurasidone (latuda)
-less weight gain and metabolic effects
-fast onset
-low doses effectiveness similar to high dose
-rapid titration
-3A4 substrate
-higher risk for akathisia
-warning for suicide
-take with food
pimavanserin (nuplazid)
-inverse 5HT2A agonist
-used for PD psychosis
-3A4 substrate
D2/D3 receptor partial agonist
-stabilize DA transmission
- associated with more akathisia
-adjunct in depression
-warning for suicide
brexpiprazole (rexulti)
-moderate akathesis
-low moderate weight gain
-2D6 and 3A4 substrate
cariprazine (vraylar)
-akathesia
-low moderate weight gain
-3A4 substrate
lumateperone (caplyta)
-low risk for weight gain
-metabolic side effects
-EPS
-akathesia
-3A4 susbtrate
-once daily
aripiprazole (abilify)
-weight gain
-low risk for D2 effets
-moderate akathesia
-high affinity to 5HT2 and D2
-partial agonist at 5HT1A receptors (depression)
-prodrugs
-2D6 and 3A4 substrate -> interactes with fluoxetine
abilify maintena
-IM deltoid or gluteal q4w
-must overlap with oral aripiprazole for at least 14 days
abilify asimtufii
- gluteal IM q2m
-continue oral aripiprazole for 2 weeks after 1st injection
aristada
-prodrug of aripiprazole
- overlap with oral aripiprazole for 1st 3 weeks
aristada initio
-avoids 21 day overlap of antipsychotic
-avoid in pts who are poor 2D6 metabolizers
-avoid with strong 3A4 or 2D6 inhibitors
VMAT inhibitors
-inhibit VMAT to decrease storage/ increase release DA serotonin and NE
-treat TD
-dose adjustment for 2D6 inhibitors or 3A4 inducers
valbenazine (ingrezza)
-QTc prolongation
-weight gain
- rash
-anxiety
2D6 and 3A4 substrate
Deutetrabenazine (austedo)
-QTc prolongation
-anxiety
-2D6 substrate
Antipsychotics
increased risk of death in elderly pts with dementia with related behaviors
-fall risk assessment
2D6
fluoxetine, paroxetine are inhibitors
1A2
cigarette smoke decreases antipsychotic serum concentrations
-FLUVOZAMINE is a 1A2 inhibitor