Antipsychotics Flashcards
definition: psychosis
denotes a variety of mental disorder with multiple causes and manifestations
systemic and psychiatric diseases
toxic manifestations of chemical agents
what are the positive symptoms of schizophrenia?
delusions hallucinations (auditory) agitation paranoia aberrant thinking intrusion of thoughts
what are the negative symptoms of schizophrenia?
emotional apathy (flat affect)
socially withdrawn
inattentiveness
what is the dopamine hypothesis of schizophrenia pathophysiology?
hyperactivity of the mesolimbic / mesocortical system - excessive limbic DA activity leading to psychosis
cannot explain cognitive impairment
what is the key MOA of the main class of atypical antipsychotic drugs?
blockage of 5HT2a receptor
what is the glutamate hypothesis of schizophrenia pathophysiology?
hypofunction of NMDA receptors located on GABAergic interneurons
many antipsychotic drugs block what receptors?
D2
neuroleptic drugs have side effects on what brain system?
extrapyramidal
what are the main therapeutic indications for antipsychotic drugs?
schizophrenia
psychotic behavior
severe mania
antiemetic
what are the typical antipsychotic agents?
chlorpromazine
thioridazine
fluphenazine
haloperidol
what are the atypical antipsychotic agents?
clozapine olanzapine risperidone aripiprazole quetiapine ziprasidone
chlorpromazine is what class of antipsychotic?
typical
olanzapine is what class of antipsychotic?
atypical
thioridazine is what class of antipsychotic?
typical
quetiapine is what class of antipsychotic?
atypical
ziprasidone is what class of antipsychotic?
atypical
risperidone is what class of antipsychotic?
atypical
fluphenazine is what class of antipsychotic?
typical
haloperidol is what class of antipsychotic?
typical
clozapine is what class of antipsychotic?
atypical
aripiprazole is what class of antipsychotic?
atypical
what are the pharmacokinetics of antipsychotics?
low bioavailability
depot forms
what is the distribution of antipsychotics?
large volume of distribution
how are the antipsychotics metabolized? what are the products?
CYP450 - liver
clinically significant metabolites
what is the MOA of the typical antipsychotic drugs?
dopamine receptor antagonist (post synaptic D2)
what is the MOA of the atypical antipsychotic drugs?
antagonist at 5HT2a and D2 receptors
clozapine has strong binding to what receptor?
serotonin
D2 affinity is correlated to what side effects?
extrapyramidal
antipsychotic drugs act mostly on what brain system?
mesolimbic-mesocortical
VTA - limbic system and neocortex
what are the anti-dopaminergic effects of antipsychotic drugs?
cognitive motor - EPS - parkinsonian, dystonia, TDK nausea and vomiting endocrine - hyperprolactinemia weight gain - mostly with atypicals
what are the pharmacologic effects of antipsychotic drugs?
anticholinergic
antihistaminic
antiadrenergic (primarily a1)
neuroleptic malignant syndrome is a side effect of antipsychotic drugs acting on what system?
DA
the newer atypical antipsychotics are better at relieving which side effects?
less EPS
less hypotensive
less sedation
which antipsychotics are LEAST strongly associated with EPS effects?
clozapine and quetiapine
which antipsychotic drug is MOST strongly associated with EPS effect?
risperidone
which age group is higher risk for developing TDK following antipsychotic therapy?
older
which antipsychotic drugs are heavily associated with weight gain? are they typicals or atypicals?
clozapine and olanzapine
atypicals
