Antipsychotics Flashcards
how do pre synaptic serotonin receptors impact dopamine?
decrease synaptic dopamine
what happens when we block post synaptic dopamine receptors?
movement disorders
(seen in typical antipsychotics)
what happens when we block dopamine and serotonin receptors
increase synaptic dopamine
competition between drug and dopamine
reduced motor side effects
possible etiologies of schizophrenia
neurodevelopmental
genetics
environmental
gene - environment interactions
neurodevelopment-environment interactions
which receptor mediator of hallucinations
5HT2a
which agents were originally identified as 5HT agonists
LSD and mescaline
5HT2a receptors modulate what
glutamate release and NMDA receptors
dopamine release
5HT2a ____ are beneficial in schizophrenia
antagonists
what is glutamate
major excitatory neurotransmitter
whats part of the glutamate theory that exacerbates psychosis and cognition
ketamine and phencyclidine which are noncompetitive inhibitors of NMDA receptors
patients with schizophrenia have increased _____ receptor density
D2
which region responsible for motor side effects (EPS)
basal ganglia
which region is primary therapeutic effects
mesolimbic
which region has hypofunction in schizoprenia
mesocortical
which region helps anti-emetic
medulla
when do we see EPS symptoms?
early, days/weeks
drug therapy for EPS
anticholinergics (benztropine, trihexphenidyl, akineton)
benadryl
amantadine
propranolol
how do EPS side effects happen?
since we blocking inhibitory and D2, we get excess excitatory so we need anticholinergic
when may tardive dyskinesia occur?
late, months to years
is tardive dyskinesia reversible
no
irreversible
treatment of tardive dyskinesia
prevention
how does tardive dyskinesia happen
unknown MOA
new therapies target VMAT2
new drugs for tardive dyskinesia treatment
tetrabenazine
valbenazine
deutetrabenazine
VMAT2 inhibitors
when does neuromalignant syndrome happen
serious and rapid
treatment is to stop drugs and restore dopamine through diazepam
what drug treats Tourettes
pimozide
alpha receptor blockade adverse effects?
hypotension, impotence, failure to ejaculate
dopamine receptor blockade side effects
Parkinsons, EPS
histamine receptor blockade side effects
weight gain, sedation
hyperprolacinemia side effects
infertility, impotence, amenorhhea
typical/first gen antipsychotics
increased EPS and tardive dyskinesia
phenothiazine structure
chlorpromazine
1st antipsychotic, antihistamine side effects
which drugs for N/V
promethazine
prochlorperazine
thioridazine
many SEs
anticholinergic, sedation, cardiovascular
1st gens with EPS
fluephenazine
thiothixene
haloperidol
molindrone
perphenazine
combo with anticholinergic
atypical/second gen antipsychotics
reduced EPS
more metabolic problems
enhanced 5HT antagonism
which agents linked to diabetes in pts less than 50
olanzapine
clozapine
clozapine
clozapine has a risk of
agranulocytosis and diabetes
olanzapine
loxapine
risperidone
which drug has a prodrug and is a partial agonist at 5HT1a
aripiprazole
what does aripiprazole do to dopamine activity
brings it down with psychosis
brings it up with EPS
drugs that are D2/D3 partial agonists
brexiprazole, cariprazine, lumateperone
olanzapine
risk weight gain and diabetes
quetiapine
antidepressant, hypotension, sedation
risperidone
5HT2a/D2 antagonistz
ziprasidone
5HT2a/D2 antagonist, prolong QT interval, alpha affinity
lurasidone
5HT2A/D2, reduced metabolic effects, rapid titration
aripiprazole
partial agonist activity
5HT2a/D2 affinity
