Antipsychotics

Question 1

chlorpromazine

Answer 1

typical

even worse EPS than olanapine

Question 2

thioridazine

Answer 2

typical
worst autonomic effects (orthox htx, no ejac)
worst muscarinic block (urinary retention)/toxic confusional state

metabolite is more effective than active

Question 3

trifluoperazine

Answer 3

typical

HUGE EPS RISK

Question 4

fluphenazine

Answer 4

typical

HUGE EPS RISK

Question 5

thiothixene

Answer 5

typical

Question 6

haloperidol

Answer 6

typical
HUGE EPS RISK (most D receptor blockade)
weakest autonomic effects
@high dose-completely block D

Question 7

clozapine

Answer 7

atypical
agranulocytosis
bad weight gain
NO EPS
high affinity for D4 receptor and 5HT2 block
trx resistant schizo
CYP3a4
CYP2d6

Question 8

risperidone

Answer 8

atypical
CYP3a4
CYP2d6

Question 9

olanapine

Answer 9

atypical
worst weight gain
CYP2d6

Question 10

quetiapine

Answer 10

atypical
QT prolongation
6 hour half life
CYP3a4

Question 11

ziprasidone

Answer 11

atypical
QT prolongation
8 hour half life
CYP3a4

Question 12

aripiprazole

Answer 12

atypical
partial D2 and 5HT agonist
-get to 25% Dopamine Emax=never completely block D (no bad EPS)

75 hour half life

CYP3a4
CYP2d6

Question 13

typical vs atypical

Answer 13

Typicals=EPS and only positive sx

Atypical-reduced EPS risk, postitive and negative sx (5HT2R antagonism)

Question 14

EPS

Answer 14

PD like sx=bradykinesia, rigidity, tremor
Akathisia, dystonias=painful

due to D receptor blockade (typicals)
small in all atypicals except clozapine

Question 15

Tardive dyskinesia

Answer 15

choreatheoid movements of lips and buccal cavity=might be irreversible

• @6 mo to several years
• elim antichoniergics and add Diazepam (GABA agonist)

Question 16

Neuroleptic Malignant Syndrome

Answer 16

muscle rigidity, excess switching, fever, life threatening autonomic instability (due to D in hypothalamus messed up)

@pts particularly sensitive to EPS

trx is dantrolene (muscle relaxant) and bromociptine (D agonist)

Question 17

Endocrine effects

Answer 17

Due to D2 pituitary blockade

hyperprolactinemia, gynecomastia, ammernoeria, infertility

Question 18

Metabolic effects

Answer 18

ESPICALLY ATYPICALS

sig weight gain and hyperglycemia and hyperlipidemia

DM

antagonized 5HT2c receptors/leptin disreg?

Question 19

D receptor blockade increase

Answer 19

EPS risk increase

Question 20

Autonomic effects

• mech
• typicals vs atypical
• sx

Answer 20

due to block of peripheral alpha adrenergic/muscarinic receptors

typicals
thioridazine worst, haloperidol weakest

atypicals all have intermediate effects

ortho htx and ejaculation failure

Question 21

Muscarinic block

Answer 21

atropine like effects (PSNS up!) @ thiorzidaine/most

-toxic confessional state, urinary retention

Question 22

typical and atypical

• protein binding
• avg t1/2

Answer 22

bound

12-24 hours