Antipsychotic Flashcards
Typical agents
older agents; metabolized in liver into INactivate metabolites. Binds to D2 receptors
only have effects on positive symptoms
Atypical agents
newer; less side side effects esp EPS effects at equal therapeutic doses.
Metabolized in liver to produce Active metabolites
Binds to D2 receptors and 5HT receptors
have effects on positive and negative symptoms
which system causes the hyperactivity of dopamine activity? and what is its clinical function?
Mesolimbic-mesocortical system; related to behavior and psychosis
Nigrostriatal system
coordination of voluntary movement; responsible for EPS
antidopaminergic effects on motor behavior
Blocks D2 receptors
if given high enough dose could cause EPS
-parkinson-like syndrome
-Akathesia:motor restlessness and anxiety
-dystonia
-Tardive dyskinesia
Tardive dyskinesia
due to supersensitivity of dopamine receptors– agents blocking D2 receptors.
involuntary movement of tongue, mouth, face, head
Irreversible
Affect ELDERLY more significantly
Neuroleptic malignant syndrome
hypertension, hyperthermia
positive symptoms of schizophrenia
manifesation of abnormal behavior: delusions, hallucination, agitation, paranoia, aberrant thinking, intrusion of thoughts
negative symptoms of schizophrenia
emotional apathy, socially withdrawn, inattentiveness
Anti dopaminergic effect on endocrine gland
Hyperprolactinemia
decrease testosterone production, gynecomastia, change in libido, and infertility
female: menstrual irregularities, gaactorrhea, infertility
What agents causes risk for diabetes?
Clozapine and olanzapine (atypical drugs)
Antihistamine effect
sedation, weight gain
Thioridazine
typical agent; poor antiemetic agent
Fluphenazine
typical; highly potent
Haloperidol
typical: highest potency –>increase EPS effect
Risperidone
Most strongly associated with EPS as atypical agent; tx for noncognitive symptom in AD
which drugs are used for non cognitive alzheimers
olanzapine, risperidone, quetiapine
arpiprazole
atypical agent
quetiapine
Atypical agent; least strongly associated w/ EPS; tx for non-cog AD
Ziprasidone
atypical agent
which antipsychotic drug is more prone for orthotic hypotension
chlorpromazine
EPS risk is influenced by
- Rapid dose escalation
- Target dose (concentration/receptor occupancy)
- patient vulnerability
What mechanism cause weight gain
combine H1 and serotonin blockade
what is the least potent typical agent? most potent?
least: chlorpromazine, highest: haloperidol
which atypical agent has most involvement with EPS? least effect to EPS?
most: Risperidone
least: Clozapine, quetiapine
what are antipsychotic agents used for?
schizophrenia, psychotic behavioral, severe mania, antiemetic,tourettes, chronic neuropathic pain
Schizophrenia pathophysiology
hyperactivity of mesolimbic mesocortical DA system–> excessive limbic DA activity–>psychosis
Blockade of serotonin receptor is KEY mechanism of action for atypical antipsychotic drugs’
Hypofunction of NMDA receptors located on GABAergic interneurons–>hyperstimulation of cortical nuerons–>psychosis
what is the key mechanism of action for atypical antipsychotic drugs
blocking serotonin receptors
antipsychotic effects on tuberoinfundibular
inhbit prolactin secretion from anterior pituitary–>amennorrhea/galactorrhea syndrome
antipsychotic effects on medullary periventricular area
antiemetic effects
