Antipsychotics Flashcards
What is the dopamine receptor target for antipsychotics?
D2
What is the serotonin receptor target for antipsychotics?
5-HT2a
What is the off target receptor that antipsychotics hit in parasympathetic system?
M2/3
What is the off target receptor that antipsychotics hit in histamine?
H1
What is the off target receptor that antipsychotics hit in the heart?
K+c channels
Name the two first generation high potency anti psychotics
Fluphenazine
Haloperidol
Name the low potency first gen anti psychotic
Chlorpromazine
Name the four second generation antipsychotics
Risperidone
Olanzapine
Clozapine
Aripiprazole
What is the main difference between first and second generation antipsychotics?
First hit only dopamine, second hit dopamine and serotonin
What pathway do antipsychotics work in that inhibits positive symptoms of schizophrenia?
Mesocortical dopamine pathway
What characteristic of the antipsychotics helps minimize their toxicity?
They only have to occupy 60% of the receptors to achieve a 100% response
Do first generation or second generation have worse extrapyramidal symptoms?
First generation
What pathway leads to the EPS?
Inhibition of the nigrostriatal pathway
Inhibition of the tuberoinfundibular pathway from antipsychotics leads to what issue?
Hormonal effect of prolactinemia because dopamine inhibits the production of it so without dopamine you get more prolactin
What are the effects of hyperprolactinemia?
Gynecomastia
Amenorrhea
Decreased libido
Do first or second generation Aps cause worse prolactinemia?
First
What is neuroleptic malignant syndrome?
Hyperthermia, rigidity, mantal status changes, autonomic instability caused by antipsychotic medication
Do first or second generation Aps cause neuroleptic malignant syndrome?
Both cause it
What can you treat the muscle rigidity and hyperthermia with in neuroleptic malignant syndrome?
Dantrolene…calcium channel blocker to inhibit muscle
What side effect can be caused by the inhibition of serotonin receptors in AP meds?
Metabolic syndrome
What is metabolic syndrome symptoms?
Weight gain, dyslipidemia, hyperglycemia
Is metabolic syndrome more common in first or second gen Aps?
Second gen
Do AP drugs antagonize or agonize M2/M3 parasympathetic receptors?
Antagonize
What first gen antipsychotics cause antiparasympathetic issues?
Chlorpromazine (low potency)
What second gen antipsychotic is especially bad at causing antiparasympathetic issues?
Clozapine
Name the symptoms of anti parasympathetic issues caused by APs
Blurred vision
Xerostomia
Constipation
Urinary retention
What generation antipsychotics lead to orthostatic hypotension?
Low potency first gen and second generation
What second gen AP is really bad for orthostatic HypoTN?
Clozapine
Why do APs (low potency first gen and second gen) cause orthostatic HypoTN?
They can block alpha1 receptors which vasodilate
What classes of APs have issue with sedation?
First gen low potency and second gen
Why do APs cause sedation?
Because they block H1 (histamine) receptors and are in the brain
What first gen AP leads to prolonged QT ??
Haloperidol
What second generation APs leads to prolonged QT?
Risperidone
Olanzapine
What causes prolonged QT from first and second generation APs?
Inhibit K+efflux in the cardiac muscle therefore slowing repolarization
What AP drug has toxicity of agranulocytosis/neutropenia?
Clozapine
