CNS II Test 1 Antipsychotics

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Author:
Anonymous
ID:
49443
Filename:
CNS II Test 1 Antipsychotics
Updated:
2010-11-14 13:32:30
Tags:
Antipsychotics nervous system disorders
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Description:
Cards give drug class, brand name, dosing, metabolism, SE profile, and various unique considerations. A few quiz questions thrown in.
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  1. 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)
  2. 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
  3. 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
  4. thiothixene
    • FGA typical (Navane)
    • Medium relative potency

    • Range 5-60mg/day
    • Max dose 100mg/day

    • Low sedation, anticholinergic, hypotensive
    • High EPS

    1A2 metabolized
  5. 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
  6. perphenazine
    • FGA typical (Trilafon)
    • Medium relative potency

    • Range 8-64mg
    • Max dose 100mg/day

    • Sedation, anticholinergic, hypotensive (low)
    • High EPS

    • 2D6 metabolized
    • 2D6 inhibitor
  7. 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
  8. loxapine
    • FGA typical (Loxitane)
    • Medium relative potency

    • Range 20-250mg/day
    • Max dose 250mg/day
    • Sedation, hypotensive, EPS (moderate)
    • Anticholinergic (low)

    CYP450 metabolized
  9. 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
  10. 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)
  11. 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
  12. 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
  13. 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
  14. 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)
  15. 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
  16. 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
  17. 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
  18. 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
  19. asenapine
    SGA atypical (Saphris)

    • Dose always 5mg SL BID
    • Do not swallow, nor eat/drink x10min

    1A2 [major] metabolized (3A4 minor)

    Low SE profile
  20. Which two SG antipsychotics have the highest risk for increased prolactin and dose-dependent EPS?
    • risperidone (Risperdal)
    • paliperidone (Invega)
  21. Which SG antipsychotics are also approved for treatment-resistant depression (TRD)?
    • aripiprazole (Abilify)
    • olanzapine (Zyprexa)

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