antipsychotics Flashcards
What is the indication for clozapine?
recurrent suicidal behavior
multi-drug resistant disease
What is the indication for pimavanserin?
hallucinations/delusions associated with parkinson disease psychosis
Positive symptoms of schizophrenia are related to what pathway
overactivity of the mesolimbic pathway
Negative symptoms of schizophrenia are related to what pathway
mesocortical pathway dysfunction
What are the positive symptoms of schizophrenia
hallucinations, delusions, disorganized speech/thinking, agitation, abnormal motor behavior
What are the negative symptoms of schizophrenia
apathy, avolition (decreased motivation), alogia (complete lack of speech), cognitive deficits, social withdrawal
Nigrostriatal pathway
projections from substantia nigra to basal ganglia
- -stimulation of purposeful movement
- -D2 antagonism induces extrapyramidal symptoms (pseudoparkinsonism & tardive dyskinsea)
Tuberoinfundibular pathway
projections from hypothalamus to infundibular region
- -dopamine is released & tonically inhibits prolactin release
- -D2 antagonism increases prolactin levels
How long must therapy be before evaluating for response
2-3 weeks
remission may take several months
First generation antipsychotics block what
dopamine type-2 post synaptic receptors
also, block muscarinics, histaminics, alphas, D2s in nigrostriatal & tuberoinfundibular pathways
1st gen SEs
dry mouth, constipation, urinary retention, blurred vision
ortho hypotension, dizziness/syncope
sedation
risk of QTc prolongation & seizure activity
hyperprolactinemia
extrapyrimidal symptoms (movement)
Which are the 1st gen low potency agents
chlopromazine
thioridazine
more sedation, hypotension, & seizure-threshold reducation
Which are the 1st gen high potency agents
fluphenazine
haloperidol
more movement & endocrine effects
What are the treatments for the extrapyramidal symptoms
- anticholinergic agents: benztropine & trihexyphenidyl
2. antihistamine agents: diphenhydramine
What are the treatments for tardive dyskinesia
- selective vesicular monoamine transporter 2 inhibitors: valbenazine & deutetrabenazine
What receptors do the 2nd gen antipsychotics block
D2 & 5HT2A
–stronger serotonin blockers than dopamine
List the SGA 5HT-2A/DA receptor antagonists
lurasidone (partial 5HT-1A agonist)
risperidone
ziprasidone
List the SGA partial DA/5HT-1A receptor agonists
aripiprazole
brexpiprazole
List the SGA multi-acting receptor target agents
clozapine
olanzapine
quetiapine
What does pimavanserin do
inverse serotonin agonist/antagonist
used for parkinson’s psychosis
MOA of cariprazine
5HT-2A/DA antagonist & partial DA/5HT-1A agonist
SEs of SGAs
weight gain, hyperglycemia/insulin resistance, hyperlipidemia
QTc prolongation/EKG changes
rare SE of clozapine
agranulocytosis
rare SE of olanzapine
drug reaction w/ eosinophilia & systemic symptoms–skin eruption, hematologic abnormalities, lymphadenopathy & internal organ involvement
Neuroleptic malignant syndrome
severe parkison’s like movement disorder with widespread muscle contraction
- AMS
- muscle rigidity, increased muscle metabolism, rhabdo
- hyperthermia
- dehydration
treatment of neuroleptic malignant syndrome
dantrolene (malignant hyperthermia)
1st gen SGAs we have to know
chlorpromazine
fluphenazine
haloperidol
thioridazine
Before giving antipsychotics, check these
serum glucose, lipids, weight, BP, waist circumference & personal/family history of metabolic & CV disease
What are the long-acting injectable agents?
risperidone
olanzapine
aripiprazole lauroxil
paliperidone palmitate
