Antipsychotics Flashcards
phenothiazines
MOA: strong D2 antagonists
side effects due to alpha adrenergic, muscarinic and 5-HT receptor blockade
chlorpramazine (thorazine)
fluphenazine (Prolixin)
thioridizine (Mellaril)
slightly less potent than phenothiazines
thiothixene (Narvane)
more potent than phenothiazines but with fewer side effects
Adverse: severe muscle stiffness
haloperidol
Atypical antipsychotics
serotonin-dopamine antagonists
MOA: greater potency for 5-HT2a receptors
Use: negative and positive symptoms of schizophrenia
Mood stabilizers in autism and bipolar disorder
-fewer EPS because don’t bind to D2 receptors with as high affinity as typical antipsychotics
side effect: weight gain from H1 receptor blockade & hypercholesterolemia (first 2 listed)
clozapine olanzapine quetiapine ziprasidone risperidone aripiprazole
other uses for atypical antipsychotics
acute mania bipolar disorder Tourette's syndrome OCD control aggression in self-injurious children
associated with psychosis
- increased dopaminergic activity in limbic system
- increased D2 receptor density in nucleus accumbens, caudate & putamen (schizophrenia)
side effects of antipsychotics
- dopamine release into the portal circulation by the arcuate & PVN decreases prolactin secretion. If inhibit DA neurons will get increased release of prolactin
- tardive dyskinesia (D2 blockade in nigrostriatal pathway)
receptors blocked by antipsychotics
D2, alpha, muscarinic, H1 and 5-HT2
What makes an antipsychotic atypical?
equal receptor occupancy for D2 and 5-HT2a