Atypical Antipsychotics

Question 1

Asenapine

Answer 1

*SHE DOESN'T LIKE (taste terrible and expensive) brand only)
Sublingual only, poor bioavailability
MWG
QTc prolongation
P450 1A2 substrate 
Metallic taste
Unit dosing, hard for pts
Smoking dec concentration, caffeine inc concentration
for neg sympts, some pos

Question 2

Brexpiprazole

Answer 2

QD, MWG, akathisia (less than arip), high binding affinity
P450 2D6 3A4 substrate
Dosing adjustments for 2D6/3A4 inhib. And 3A4 induc.
Hepatic dysfunction or Cr Cl

Question 3

Cariprazine

Answer 3

QD, MWG, High akathisia
P450 3A4 substrate
No recommended in renal impairment
Max 6 mg, higher doses more effective, but greater risk of akathisia

Question 4

Clozapine

Answer 4

MOST EFFECTIVE, many SE (need to dose titrate to try and minimize)
REMS monitoring bc of agranulocytosis (neutrophil count needs to be 1500) monitor weekly for 6 mon, biweekly for 6 mon, then Q4w
Cardiomyopathy, hypersalvation, hypotension, metabolic syndrome, dose-related seizures, QTc prolongation, constipation, sedation.
P450 1A2 substrate

Question 5

Iloperidone

Answer 5

QTc prolongation BBW
Slow dose titration bc orthostatic hypotension (BID)
MWG
P450 2D6 3A4 substrate
Expensive
Must have an EKG, no evidence in use with children

Question 6

Lurasidone

Answer 6

**First line for early onset
MUST TAKE W FOOD
Akathisia
LWG
P450 3A4 substrate
Usual max 160 mg, CrCl

Question 7

Olanzipine

Answer 7

QD (give at bedtime, high sedation) or BID
HWG
Hyperglycemia, hyperlipemia
Acts as an AntiCH at high doses (15mg/day)
P450 1A2 substrate
LAI- Zyprexa Relprevv REMS monitoring

Question 8

Paliperidone

Answer 8

9-OH metabolite of Risperidone
QD
Oral form is ER and has ghost tablets in renal elimination
Dose adj in renal impaired
EPS and hyperprolactemia
MWG
QTc prolongation 
LAI- invega sustenna=IM Q4w
LAI- invega Trinza=IMM Q12w

Question 9

Quetiapine

Answer 9

300mg-800mg dose range, short 1/2 life but given QD if poss.
Significant sedation
**QTc prolongation BBW
MWG
P450 3A4 substrate 
*Abuse potential
Used to "come down" from stimulants 
Similar to benzos

Question 10

Risperidone

Answer 10

Often seen as 1st line treatment, QD
Higher risk of EPS and Hyperprolactemia 
MWG
P450 2D6 substrate 
**Can produce paliperidone 
LAI- Risperdal consta=IM Q2w

Question 11

Ziprasidone

Answer 11

BID but can be give QD
MUST TAKE W FOOD
LWG
Low risk of akathisia 
No significant P450 metabolism
QTc prolongation warning
DRESS warning from post-marketing surveillance

Question 12

Aripiprazole

Answer 12

QD, akathisia, low wt gain or metabolic syn, high binding affinity
P450 2D6 and 3A4 substrate
Dosing adjustments with strong 2D6 or 3A4 inhibitors or 3A4 inducers
LAI must have 2 or 3 oral overlap