B7-082 Antipsychotics Flashcards
antipsychotic drugs are […] based on their tendency to produce neurological side effects
neuroleptics
the original name of antipsychotics was […] which were used to quiet institutionalized mental patient
major tranquilizers
positive symptoms of schizophrenia [2]
hallucinations (typically auditory)
delusions
pathogenesis of schizophrenia is unknown but thought to have […] and […] components
neurodevelopmental
heritable
all antipsychotics are antagonists of
D2 dopamine receptor
what interaction contributes to the side effects of antipsychotics
other receptors a, ACh, histamine, etc
most important receptors of antipsychotics
D2
5HT
(but extensively interact with other receptors causing side effects)
initial pharmacologic effects of antipsychotics [2]
sedation
decreased agitiation
antipsychotics improve […] symptoms of schizophrenia over weeks to months of treatment
positive
(very delayed effect, presents a problem with the Dopamine hypothesis of schizophrenia)
do older, “typical” antipsychotics improve negative symptoms of shizophrenia?
no
positive may see improvement over time
How do antipsychotics cause parkinsonism?
blocks the striatal dopamine receptors
extrapryramidal effects of antipsychotics [3]
dystonia
akathisia
Parkinsonian symptoms
[…] can help prevent the extrapyramidal effects of antipsychotics
anticholinergics
antipsychotics cause increased prolactin release via inhibition of […] receptors
D2
(can cause amenorrhea, gynecomastia, and lactation)
newer antipsychotics cause significant […] gain
weight
can cause metabolic syndrome, diabetes
olanzepine
can cause blurred vision and retinitis pigmentosum
thioridazine
neuroleptic malignant syndrome can be treated with
(fever, rigidity, myoglobinuria)
bromotriptine
dantrolene
used to treat tardive dyskinesia
valbenazine
long term side effects of antipsychotics
tardive dyskinesias
perioral tremor
blood dyscrasias
agranulocytosis can occur with long term used of […]
clozapine
any drugs that are sedative will have […] CNS effects
additive
effective against positive, but not negative schizophrenia symptoms
typical antipsychotics
produce EPS and tardive dyskinesia
typical antipsychotics
typical antipsychotics: phenothiazines [3]
chlorpromazine
fluphenazine
thioridazine
-azine
phenothiazines (typical antipsychotics)
haloperidol and thiotixene are […] antipsychotics
typical
[…] has the highest incidence of causing EPS
typical antipsychotics
first antipsychotic drug
clorpromazine (phenothiazine)
(typical antipsychotic)
all typical antipsychotics are […] agonists
D2
no EPS or tardive dyskinesia
atypical antipsychotics
atypical antipsychotics are […] antagonists
5 HT receptors (higher affinity)
(also D2, but lower affinity)
prototypical atypical antipsychotic
clozapine
activity at a broad spectrum of receptors
“busiest drug out there”
clozapine
some effect on negative shizophrenic symptoms
clozapine (atypical antipsychotic)
major side effect of clozapine
agranulocytosis
(approved for used ONLY in patients that are treatment resistant, must receive routine blood tests)
approved only for treatment resistant patients who must receive regular blood tests
clozapine (atypical antipsychotic)
newer “atypical” antipsychotics have significant […] antagonist activity
5HT2
generally have an improved side effect profile
newer “atypical” antipsychotics
atypical antipsychotics that produce less EPS and tardive dyskinesia
risperidone (causes EPS at high doses)
lerasidone
paliperidone
high incidence of weight gain and metabolic syndrome [2]
olanzapine
quetiapine
(newer atypical antipsychotics)
D2 partial agonist
5HT2 antagonist
aripriprazole
generally less sedating than other antipsychotics
aripriprazole
(newer atypical antipsychotics)
other uses of antipsychotics
management of agitation and psychotic symptoms
antipsychotics can be used to treat […] but associated with increased risk of mortality
dementia
antipsychotics can be used to treat alcoholic hallucinosis but only when
actively drinking
(when in withdrawal, can cause seizures)
early side effects of haloperidol that occur in the first few weeks [2]
dystonia
Parkinsonism
use of what medication requires monitoring for agranulocytosis?
clozapine
olazapine and quetiapine have a low liability for causing EPS, but can cause [2]
weight gain
metabolic syndrome
atypical antipsychotics 5-HT2 […] D2
[higher affinity for which receptor?]
5-HT2 > D2
typical antipsychotics 5-HT2 orD2
[higher affinity for which receptor?]
5-HT2 < D2
typical antipsychotics have a tendency to cause [2]
EPS (parkinsonism)
tardive dyskinesia
antipsychotics with strong […] effects are the most likely to cause orthostatic hypotension and erectile dysfunction
alpha antagonist
(chlorpromazine)
has the side effect of retinitis pigementosa
thiordazine
which class of antipsychotics is more likely to cause EPS?
typicals
delirium results from blockade of […] receptors
muscarinic
erectile dysfunction and orthostatic hypotension results from blockade of […] receptors
alpha
sedation results from blockade of […] receptors
histamine
galactorrhea results from blockade of […] receptors
D2
less likely to produce EPS than typical antipsychotics, but EPS can still occur at high doses
risperidone
decrease EPS by blocking the input of cholinergic striatal interneurons to ascending GABAergic projection from the caudate to the globus pallidue
anticholinergics (benzotropine)
(used to lessen EPS)
