16- Antipsychotics Flashcards
chlorpromazine (Thorazine)
typical antipsychotic- D2 antagonist
- returns DA balance in nucleus accumbens (positive symptoms)
- higher clinical potency than atypicals
- multiple side effects d/t activity at muscarinic, adrenergic, DA, serotonin and histamine receptors
- can induce/inhibit CYP metabolism
- metabolized by CYP2D6 and CYP3A4
fluphenazine (Permitil, Prolixin)
typical antipsychotic- D2 antagonist
- returns DA balance in nucleus accumbens (positive symptoms)
- higher clinical potency than atypicals
- multiple side effects d/t activity at muscarinic, adrenergic, DA, serotonin and histamine receptors
- can induce/inhibit CYP metabolism
- metabolized by CYP2D6 and CYP3A4
thiothixene (Navane)
typical antipsychotic- D2 antagonist
- returns DA balance in nucleus accumbens (positive symptoms)
- higher clinical potency than atypicals
- multiple side effects d/t activity at muscarinic, adrenergic, DA, serotonin and histamine receptors
- can induce/inhibit CYP metabolism
- metabolized by CYP2D6 and CYP3A4
haloperidol (Haldol)
typical antipsychotic- D2 antagonist
- returns DA balance in nucleus accumbens (positive symptoms)
- higher clinical potency than atypicals
- multiple side effects d/t activity at muscarinic, adrenergic, DA, serotonin and histamine receptors
- can induce/inhibit CYP metabolism
- metabolized by CYP2D6 and CYP3A4
aripiprazole (Abilify)
atypical antipsychotic
- inhibit serotonin receptors (2A & 2C)
- lower affinity for DA receptors than typical drugs
- blocking serotonin receptors leads to both a decrease in glutamate release and inc. DA release in the cortex
- Less EPS and NMS
- many side effects because of off-target effects
- metabolized by CYP1A2, 3A4, 2D6
- induce/inhibit CYPs
clozapine (Clozaril)
atypical antipsychotic
- inhibit serotonin receptors (2A & 2C)
- lower affinity for DA receptors than typical drugs
- blocking serotonin receptors leads to both a decrease in glutamate release and inc. DA release in the cortex
- Less EPS and NMS
- many side effects because of off-target effects
- metabolized by CYP1A2, 3A4, 2D6
- induce/inhibit CYPs
- increased risk of metabolic syndrome, ganulocytosis, leukopenia
olanzapine (Zyprexa)
atypical antipsychotic
- inhibit serotonin receptors (2A & 2C)
- lower affinity for DA receptors than typical drugs
- blocking serotonin receptors leads to both a decrease in glutamate release and inc. DA release in cortex
- Less EPS and NMS
- many side effects because of off-target effects
- metabolized by CYP1A2, 3A4, 2D6
- induce/inhibit CYPs
- increased risk of metabolic syndrome
paliperidone (Invenga)
atypical antipsychotic
- inhibit serotonin receptors (2A & 2C)
- lower affinity for DA receptors than typical drugs
- blocking serotonin receptors leads to both a decrease in glutamate release and inc. DA release in cortex
- Less EPS and NMS
- many side effects because of off-target effects
- metabolized by CYP1A2, 3A4, 2D6
- induce/inhibit CYPs
quetiapine (Seroquel)
atypical antipsychotic
- inhibit serotonin receptors (2A & 2C)
- lower affinity for DA receptors than typical drugs
- blocking serotonin receptors leads to both a decrease in glutamate release inc. DA release in cortex
- Less EPS and NMS
- many side effects because of off-target effects
- metabolized by CYP1A2, 3A4, 2D6
- induce/inhibit CYPs
risperidone (Risperdal)
atypical antipsychotic
- inhibit serotonin receptors (2A & 2C)
- lower affinity for DA receptors than typical drugs
- blocking serotonin receptors leads to both a decrease in glutamate release and inc. DA release in cortex
- Less EPS and NMS
- many side effects because of off-target effects
- metabolized by CYP1A2, 3A4, 2D6
- induce/inhibit CYPs
Neuroleptic Malignant Syndrome (NMS)
rare, but life threatening
occurs shortly after beginning typical drug
-Hyperthermia
-Mental Status Changes
-Rigidity
-Autonomic Instability
treatment: d/c neuroletpic use, life support, Bromocriptine, Dantrolene
Mesolimbic Pathway
ventral tegmental area to NUCLEUS ACCUMBENS
-role- motivation, reward, emotional behaviors
hallucinations, delusions & thought disorder
-HYPERACTIVITY in pathway causes POSITIVE symptoms of schizophrenia
Mesocortical Pathway
ventral tegmental area to CORTEX
- role- cognition, executive function, emotions
- HYPOACTIVITY leads to NEGATIVE symptoms of schizophrenia
Nigrostriatal Pathway
substantia nigra to striatum
- role- motor planning and purposeful movement
- isn’t believed to be involved in schizophrenia, but antipsychotics can interfere with this pathway leading to movement disorder side effects
Tuberoinfundibular Pathway
hypothalamus to pituitary gland
- role- inhibition of prolactin release
- normal in schizophrenia, but hypoactivity can lead to galactorrhea, amenorrhea, sexual dysfunction
