Risperidone Paliperidone Quetiapine Aripiprazole Olanzapine Clozapine

Init. Maint. Max. Init Maint Max Init Maint Max Init Maint Max Init Maint Max Init Maint Max
25BID 5-10
12.5
1-2mg 2-6mg 6mg 3 3-6 12 800 10-15 10-30 30 10-15
10-20 20 OD 900
XR 300 or BD
Dosage

No correlation b.w plasma
concentration & therapeutic
effect.
- Antagonist for 5HT2A, D2,
α1&2, H1
- low affinity on α & M
Pharmacology
Recommended 6mg
- derivative of
risperidone
- CYP→ limited role
- Maint→ lowest dose to - Initial 5-10 →psych - Maint: 150-300
maintain remission. - 10-15→ mania divided or 200 HS
- ↑dose every 2-3days - 30-40→ in
- need ECG in higher doses resistant pt.
- 25-300mg →ttt insomnia - >20→ not studied
- Antagonist for 5HT2&6, - antagonist 5HT2A, - Antagonist for - Antagonist for 5HT2A,
D2&1, α1&2, H1 D2, α1 5HT2A,1A, D2,1,4, H1, D1,2,3,4, αesp1
- don’t block M & benzo. - partial agonist D2 M1,5 - low potent on D2,

- potent on D2→ = to
haloperidol with less EPS if
dose below 6mg.
- extensive 1st pass
metabolism
- 1\2life 20h
- weak inhibitor of 2D6
- schz acute & maint in adult
& adolescent 13-17YO
-bipolarI acute manic or
mixed episode in adult &
children 13-17YO
* may combined ẽ lithium &
Indication
- no need for dose
adjunct in hepatic pt
- schz acute & maint.
- schizoaffective acute ttt
as monotherapy or
adjunct to mood
stabilizer or
antidepressants
- lower antagonism→ not - metabolize by 3A4 - 1\2life 31h Haldol block 80%-
associated with EPS & 2D6 - 40% of the dose clozapine 40-50%
- 1\2life 7h - modulator rather inactivated by 1st - 1\2life 12h
than blocker to pre- pass metabolism
post D2 - Steady state 1w
- elimination 1\2 life
75h
- schz - schz - schz - sever TD
- bipolarI acute mania as -bipolarI acute & - bipolarI: - suppress dyskinesia
mono or adjunct to maint. For manic or *acute manic\ mixed →return if Rx D\C
lithium or valproate. mixed episode, & *maintenance - pt intolerance to EPS
- bipolarI maintenance as may adjunct to *adjunct to lithium & - ttt-resistant mania
adjunct lithium\ valproate. lithium\ valproate valproate - sever psychotic dep.

valproate - bipolar depressive epi. As - MDD augment to *depressive epi. With - idiopathic Parkinson,
fluoxetine (sympyax)
- ASD irritability 5-16YO monotherapy. antidepressants Huntington.
- resistant depression
- for the XR formulation: - ASD irritability with sympyax, not
- suicide in schz,
* all previous indicated as mono. schizoaffective pt.
* MDD as adjunct with - acute agitation:
antidepressants. parenteral form,
combination with
benzo not approved
 - EPS→ dose dependent - ↓dose in renal pt. - orthostatic hypotension - ortho-hypotension - EPS dose related - GI→ constipation
- ↑prolactin - ↑sensitivity to ↑ dose gradually - less EPS - ↑wt. not dose - ↑salivation ↑@night
- wt gain children> adult temperature - the least SDAs cause EPS - akathisia related & continue - anticholinergic SE
- somnolence - ↑QTc - wt gain - insomnia over time. - m. weakness
- orthostatic hypotension - DM→ not established - no ↑wt, DM or - ↑appetite - risk of seizure 4% in
- EPS, akathisia, dystonia - rarely ↑prolactin ↑prolactin - somnolence dose >600mg
- cataract formation No significant ↑QTc - dry mouth -risk of leukopenia,
SE

- torsade de pointes if use - Seizure reported -2% ↑transaminase agranulocytosis,

* cardiac arrhythmia, level granulocytopenia 1%
↓HR - myocarditis,
*↓K & Mg cardiomyopathy (chesp
*with Rx that ↑QTc pain, fever, SOB) order
* congenital ↑QTc ECG, CPK, troponin
level

- Rx that inhibit 2D6 block - avoid with Rx ↑QTc e.g. - level ↓ by: - level ↓ by: - avoid in Rx cause BM
the formation of its class 1A & class III carbamazepine, Phenytoin, suppression or
metabolite antiarrhythmic, valproate, 2D6 carbamazepine agranulocytosis:
→fluoxetine, paroxetine antipsychotics, antibiotics inhibitors. - level ↑ by: carbamazepine,
- combination with SSRIs→ * FDA warning→ potential - level ↑by: Fluvox, cimitidne phenytoin, captopril,
significantly ↑prolactin ↑QTc if use above fluoxetine, parox, - Ethanol ↑Rx sulfonamide
recommended dose. quinidine, ketocona. absorption 25% → - ẽ lithium ↑seizure +
- phenytoin ↑ Quet. - level not affected ↑ sedation avoid in pt ẽ Hx of NMS
Clearance 5 times by: lithium, & - clomipramine ↑its
- valproate. level → ↓ seizure
threshold.
- Paroxetine ↑risk of
DDI

neutropenia
- level ↑by: fluoxetine,
fluvox, parox, risperid.
 Long acting IM Long acting IM\1m
- Starting 25\2w & Max - 1\2life 25- 49 days
50\2w - 1st & 2nd inject→ deltoid
- coad. Oral Rx. With IM for - then gluteal
3w - plasma concentration
28% higher with deltoid
Vs. gluteal injections
Notes
- low EPS & usefull to ttt = effective to - long acting IM box - plasma level of
Parkinson pt (DA induced haloperidol & warning of post- 350µg\ml ass. ẽ better
psychosis) risperidone in ttt injection delirium response→ test it if pt.
schz. sedation syndrome fail the ttt.
- clearance ↓ in (PDSS), observe the - ↑salivation ttt by
elderly pt for 3h after it. clonidine, amitriptyline
- execrated in milk - periodic assess - contraindicated to use
sugar+transaminase if WBCs <3500, BM ≠,
- FDA warning of past Hx of
↑stroke risk ẽ SDAs agranulocytosis ẽ
clozapine
- CBC\w for 6m
then\2w
- D\C if +hema consult.
* WBC <300
* granulocyte <1500
- for pt who tolerate
clozapine augment ẽ
risperidone→ dramatic
improvement.