-
pimozide
- FGA typical (Orap)
- High potency (highest FGA)
- Range 2-10mg/day
- Max dose 20mg/day
- Low sedation, anticholinergic, hypotensive
- High EPS
- 3A4 metabolized
- 2D6 inhibitor (MAJOR)
-
haloperidol
- FGA typical (Haldol, decanoate LAI)
- High potency
- Range 1-100mg/day
- Max dose 100mg/day
- Very low sedation, anticholinergic, hypotensive
- Very high EPS
- Half-life: 12-36 hr
- 2D6, 1A2 metabolized
- 2D6, 3A4 inhibitor
- LAI: q4wk
- Start 10-20x daily PO dose (max 100mg)
- Target 10-15x daily PO dose
- Max monthly dose 450mg
-
fluphenazine
- FGA typical (Prolixin, decanoate LAI)
- High potency
- Range 1-50mg/day
- Max dose 100mg/day
- Low sedation, anticholinergic, hypotensive
- Very high EPS
2D6 metabolized
- LAI: q2-4wk
- Start 12.5-25mg
- Target 12.5-50mg
- Max 100mg
- Overlap recommended
-
thiothixene
- FGA typical (Navane)
- Medium relative potency
- Range 5-60mg/day
- Max dose 100mg/day
- Low sedation, anticholinergic, hypotensive
- High EPS
1A2 metabolized
-
trifluoperazine
- FGA typical (Stelazine)
- Medium relative potency
- Range 2-80mg/day
- Max dose 100mg/day
- Low sedation, anticholinergic, hypotensive
- High EPS
- 1A2 metabolize
- Not known to inhibit any CYPs
-
perphenazine
- FGA typical (Trilafon)
- Medium relative potency
- Range 8-64mg
- Max dose 100mg/day
- Sedation, anticholinergic, hypotensive (low)
- High EPS
- 2D6 metabolized
- 2D6 inhibitor
-
molindone
- FGA typical (Moban)
- Medium relative potency
- Range 15-225mg/day
- Max dose 225mg/day
- Sedation (v. low)
- Anticholinergic, hypotensive (low)
- Moderate EPS
2D6 metabolized
-
loxapine
- FGA typical (Loxitane)
- Medium relative potency
- Range 20-250mg/day
- Max dose 250mg/day
- Sedation, hypotensive, EPS (moderate)
- Anticholinergic (low)
CYP450 metabolized
-
thioridizine
- FGA typical (Mellaril)
- Low potency
- Range 50-800mg/day
- Max dose 800mg/day
- Sedation, anticholinergic, hypotensive (high)
- EPS (low)
- QT prolongation
- 2D6 metabolized
- 2D6 [minor] inhibitor
-
chlorpromazine
- FGA typical (Thorazine)
- Lowest potency
- Start 100mg/day
- Range 60-800mg/day
- Max 2000mg/day
- Sedation, anticholinergic (high)
- Hypotensive (moderate - High IV)
- Low EPS
- 2D6 [major] metabolized (minor 1A2, 3A4)
- 2D6 [major] inhibitor (minor 2E1)
-
clozapine
- SGA atypical (Clozaril)
- Only FDA approved AS for refractory Sz
- Longest pt retention
- Start 12.5mg/day
- Range 300-450mg/day
- Max 900mg/day
1A2 [major] metabolized (2D6, 3A4, 2C19 etc minor)
- Moderate EPS, prolactin
- High seizure-threshold lowering, antimuscarinic, sedation, weight gain, hypotension, dyslipidemia, glucose intolerance
- Agranulocytosis:
- Monitoring qwk x6mo at first, q2wk x6mo, then q4wk
-
risperdone
SGA atypical (Risperdal, Consta LAI)
- Start 1-2mg/day titrate
- Range 2-6mg/day (6+ risks EPS)
- Max 16mg/day
2D6 [major] metabolized (3A4 minor)
+Prolactin (not dose-related)
- LAI: Start 25mg
- Range 25-50mg q2wk
-
olanzapine
- SGA atypical (Zyprexa, Relprevv LAI)
- Also for adolescent BPD and TRD
- Start 2.5-10mg/day titrate
- Range 5-20mg/day
1A2 [major] metabolized (2D6 minor)
- Anticholinergic, dyslipidemia, glucose intolerance (High)
- Highest weight gain
- Dose-dependent lowering of seizure threshold
- LAI: 150-300mg q2wk or
- 405mg q4wk
- No overlap required
- Monitor x3hr for PDSS
-
quetiapine
- SGA atypical (Seroquel)
- Also for acute BPD
- Start 25mg BID titrate
- Range 300-800mg/day
3A4 [major] metabolized (2D6 minor)
- Sedation, weight gain, glucose intolerance, dyslipidemia, hypotention (High-Mid)
- Anticholinergic (Mid-low)
-
ziprasidone
SGA atypical (Geodon)
- 500+Calorie meal required
- Start 20mg BID titrate
- Range 120-160mg/day
Metabolized [2/3] by aldehyde oxidase (3A4 remainder)
Low SE profile
-
aripiprazole
- SGA atypical (Abilify)
- Also approved for BPD and adjuct ADT
- Range 10-15mg/day titrate q2wk
- Max 30mg/day
2D6, 3A4 metabolized
- Low SE profile
- Lowest weight gain
-
paliperidone
- SGA atypical (Invega, Sustenna LAI)
- Active risperidone metabolite
- Food increases F by 60% but not required
- Start 6mg/day titrate
- Range 6-12mg/day
- Max 12mg/day
High EPS, +prolactin Moderate for other SEs
60% excreted unchanged
- LAI: q4wk
- Loading dose 234mg + day-8 156mg
- Range 29-234mg
- Overlap not required
-
iloperidone
SGA atypical (Fanapt)
- Titrate q2d min to avoid orthostatic hypotension
- Start 1mg BID titrate
- Range 12-24mg/day
2D6, 3A4 metabolized
Low/moderate SE profile
-
asenapine
SGA atypical (Saphris)
- Dose always 5mg SL BID
- Do not swallow, nor eat/drink x10min
1A2 [major] metabolized (3A4 minor)
Low SE profile
-
Which two SG antipsychotics have the highest risk for increased prolactin and dose-dependent EPS?
- risperidone (Risperdal)
- paliperidone (Invega)
-
Which SG antipsychotics are also approved for treatment-resistant depression (TRD)?
- aripiprazole (Abilify)
- olanzapine (Zyprexa)
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