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Flashcards in Antipsychotic Drugs Deck (19):
1

Arises in the ventral tegmental area (VTA)

Projects to the frontal cortex (cortical limb)
Too little DA activity (negative and cognitive symptoms)
Do not want to block DA receptors here

Projects to the nucleus accumbens (limbic limb)
Too much dopaminergic activity (positive symptoms)
Want to block DA receptors here

Mesocorticolimbic projection is involved in schizophrenia

Mesocorticolimbic projection

2

Blockade of D2 receptors in the striatum produces parkinsonian-like effects (extrapyramidal symptoms)

Do not want to block DA receptors here

Nigrostriatal projection

3

Arcuate nucleus of the hypothalamus pituitary

Endocrinological side effects due to D2 block in this location
DA suppresses prolactin, blocking D2 increases prolactin

Tuberoinfundibular system

4

Motor nucleus of the vagus areas around ventricles

Deals with eating behavior, blockade is associated with weight gain

Medullary-periventricular neurons

5

blockage results in antiemetic properties

dopamine receptors in chemotrigger zone

6

Typical phenothiazine antipsychotic
First agent to specifically address psychosis as opposed to simple sedation
Potentiates anesthesia
No longer often used but may be used in acute treatment of psychotic episode
Sedation, alpha 1 block (bad in the elderly)
Skin reactions, photosensitivity, cardiotoxicity, anticholinergics
Increased risk of tardive dyskinesia

chlorpromazine

7

Typical butyrophenone antipsychotic
Major drug in schizophrenia treatment
Lower sedation and less alpha block than phenothiazines
Parenteral form available
Severe extrapyramidal symptoms

haloperidol

8

First atypical antipsychotic
No extrapyramidal symptoms due to DPI selectively in mesolimbic pathway
High potency at 5HT2, better against negative symptoms than typicals
No D2 super-sensitivity
Agranulocytosis and diabetes risk, weight gain
Anticholinergic effects can cause confusion, dry mouth, orthostatic hypotension, urinary

clozapine

9

Atypical antipsychotic
Low risk of extrapyramidal symptoms with low doses
No evidence of agranulocytosis risk

risperidone

10

Atypical antipsychotic
No evidence of agranulocytosis risk
Associated with weight gain, risk of diabetes, and hyoptension
Smaller increase in serum prolactin that with haloperidol
Anticholinergic effects can cause confusion, dry mouth, urinary retention, constipation, blurred vision

olanzepine

11

Atypical antipsychotic
QT prolongation

ziprasidone

12

Atypical antipsychotic
Partial agonist at D2
Modest affinity at 5HT2 receptors (antagonist)
Partial agonist at 5HT1A receptors
No apparent risk of diabetes, lesser effect on prolactin levels
Used when depressive symptoms are present

aripiprazole

13

early neurological side effect of antipsychotics
Appears in 1-5 days
Anticholinergics are diagnostic and curative
Readily treatable but alarming to patient

acute dystonia (spastic retrocollis or torticollis)

14

early neurological side effect of antipsychotics
Occurs in 5-60 days
Reduce drug or change treatment
Anticholinergic or propranolol may help
Occurs early, tends to persist

akasthisia (motor restlessness)

15

early neurological side effect of antipsychotics
Occurs in 5-30 days of treatment
Bradykinesia, rigidity, mask facies, shuffling gait
Caused by antagonism of DA in striatum
Can treat with anticholinergics

parkinsonism (EPS)

16

early neurological side effect of antipsychotics
Catatonia, stupor, fever, unstable blood pressure, myoglobinemia
May be fatal
Can occur within weeks, and can persist after stopping treatment likely due to D2 block in the hypothalamus
Stop drug immediately, high mortality
Bromocriptine or dantrolene may help
Do not use anticholinergics

neuroleptic malignant syndrome

17

early neurological side effect of antipsychotics
Especially with low potency antipsychotics and clozapine
Use with caution in epilepsy and patient withdrawing from CNS depressant

lower seizure threshold

18

late neurological side effect of antipsychotics
May be a late variant of Parkinsonism
Can occur after months or years of treatment
Mechanism is unknown
Antiparkinson drugs are not often helpful

perioral syndrome (rabbit syndrome)

19

late neurological side effect of antipsychotics
Oral facial dyskinesias, widespread chorioathetosis or dystonia
Occurs after months or years of treatment
Occurs in 20% of patients
Mechanism is dopamine receptor supersensitivity due to prolonged D2 block
Increased DA sensitivity increases GABA inhibition which increases movement
Prevention is crucial, treatment is unsatisfactory
Do not use anticholinergics

tardive dyskinesia