CNS 2 TEST 1

  1. PIMOZIDE
    1ST GEN TYPICAL ANTIPSYCH (ORAP)

    • HIGH POTENCY (HIGHEST 1ST GEN)
    • START DOSE ABOUT 2MG/DAY
    • MAX DOSE 20MG/DAY

    • LOW SEDATION
    • LOW ANTICHOLINERGIC
    • LOW HYPOTENSIVE
    • HIGH EPS

    • 3A4 METABOLIZED
    • 2D6 INHIBITOR (MAJOR!)
  2. HALOPERIDOL
    1ST GEN TYP ANTIPSYCH (HALDOL AND DECANOATE LAI)

    • HIGH POTENCY
    • START DOSE ABOUT 2MG/DAY
    • MAX DOSE 100MG/DAY

    • VERY LOW SEDATION
    • VERY LOW ANTICHOLINERGIC
    • VERY LOW HYPOTENSIVE
    • VERY HIGH EPS

    • 2D6 METABOLIZED
    • 2D6, 3A4 INHIBITOR

    • LAI: Q4WEEKS
    • 10-20X DAILY PO DOSE TO START
    • 10-15X DAILY PO DOSE FOR TARGET
    • 100MG MAX 1ST DOSE, AND THEN 450MG/MONTHMAX
  3. FLUPHENAZINE
    1ST GEN TYP ANTIPSYCH (PROLIXIN AND DECANOATE VERSION FOR LAI)

    • HIGH POTENCY
    • START DOSE ABOUT 2MG/DAY
    • MAX DOSE 100MG/DAY

    • LOW SEDATION
    • LOW ANTICHOLINERGIC
    • LOW HYPOTENSIVE
    • VERY HIGH EPS

    2D6 METABOLIZED

    • LAI: (Q2-4WEEKS)
    • 12.5-25MG START
    • 12.5-50MG TARGET DOSE
    • 100MG DOSE MAX
    • (PO OVERLAP RECOMMENDED, NOT REQUIRED)
  4. THIOTHIXENE
    1ST GEN TYP ANTIPSYCH (NAVANE)

    • HIGH POTENCY
    • START DOSE ABOUT 2MG/DAY
    • MAX DOSE 100MG/DAY

    • LOW SEDATION
    • LOW ANTCHOLINERGIC
    • LOW HYPOTENSIVE
    • HIGH EPS

    1A2 METABOLIZED
  5. TRIFLUOPERAZINE
    1ST GEN TYP ANTIPSYCH (STELAZINE)

    • HIGH POTENCY
    • START DOSE ABOUT 2MG/DAY
    • MAX DOSE 100MG/DAY

    • LOW SEDATION
    • LOW ANTICHOLINERGIC
    • LOW HYPOTENSIVE
    • HIGH EPS

    • 1A2 METABOLIZED
    • NOT KNOWN TO INHIBIT ANY CYPs
  6. PERPHENAZINE
    1ST GEN TYP ANTIPSYCH (TRILAFON)

    • MID/HIGH POTENCY
    • START DOSE ABOUT 10MG/DAY
    • MAX DOSE 100MG/DAY

    • LOW SEDATOIN
    • LOW ANTICHOLINERGIC
    • LOW HYPOTENSIVE
    • HIGH EPS

    • 2D6 METABOLIZED
    • 2D6 INHIBITOR
  7. MOLINDONE
    1ST GEN TYP ANTIPSYCH (MOBAN)

    • MID POTENCY
    • START DOSE ABOUT 10MG/DAY
    • MAX DOSE 225MG/DAY

    • VERY LOW SEDATION
    • LOW ANTICHOLINERGIC
    • LOW HYPOTENSIVE
    • MODERATE EPS

    • 2D6 METABOLIZED
    • NOT KNOW TO INHIBIT ANY CYPS
  8. LOXAPINE
    1ST GEN TYP ANTIPSYCH (LOXITANE)

    • MID POTENCY
    • START DOSE ABOUT 10MG/DAY
    • MAX DOSE 250MG/DAY

    • MODERATE SEDATION
    • LOW ANTICHOLINERGIC
    • MODERATE HYPOTENSIVE

    • EXTENSIVELY CYP METABOLIZED
    • INHIBITS NO KNOWN CYPS
  9. THIORIDAZINE
    1ST GEN TYP ANTIPSYCH (MELLARIL)

    • LOW POTENCY
    • START DOSE ABOUT 100MG/DAY
    • MAX DOSE 800MG/DAY

    • HIGH SEDATION
    • HIGH ANTICHOLINERGIC
    • HIGH HYPOTENSIVE
    • LOW EPS

    • 2D6 METABOLIZED
    • 2D6 INHIBITOR (MINOR)
  10. CHLORPROMAZINE
    1ST GEN TYP ANTIPSYCH (THORAZINE)

    • LOW POTENCY (LOWEST 1ST GEN)
    • START DOSE ABOUT 100MG/DAY
    • MAX DOSE 2000MG/DAY

    • HIGH SEDATION
    • HIGH ANTICHOLINERGIC
    • HIGH HYPOTENSIVE (IV)
    • MODERATE HYPOTENSIVE (ORAL)
    • LOW EPS

    • 2D6 METABOLIZED
    • 2D6 INHIBITOR
  11. CLOZAPINE
    2ND GEN ATYP ANTIPSYCH (CLOZARIL)

    *ONLY ANTIPSYCH FDA APPROVED FOR REFRACTORY SCHIZO (3RD CHOICE) AND HAS LONGEST PATIENT RETENTION DUE TO ABILITY TO ALLEVIATE POSITIVE SYMPTOMS

    • 12.5-25MG START THEN TITRATE UP
    • 300-450MG/DAY NORMAL DOSE RANGE
    • 900MG/DAY MAX
    • (NOTE THAT OF 2ND GENs ONLY SEROQUEL HAS RANGES EVEN NEARLY THIS HIGH)

    MID RANGE SGA FOR EPS, PROLACTIN

    HIGH RANGE SGA FOR *SEIZURE LOWERING THRESHOLD, *AGRANULOCYTOSIS(1%), ANTIMUSCARINIC, SEDATION, WEIGHT GAIN, ORTHOSTATIC HYPOTENSION, LIPID ABNORMALITIES, GLUCOSE INTOLERANCE
  12. RISPERIDONE
    2ND GEN ATYP ANTIPSYCH (RISPERDAL AND RISPERDAL CONSTA)

    • *RISK EPS OVER 6MG/DAY!
    • *IF GOING TO LAI, PO OVERLAP IS ABSOLUTELY REQUIRED DUE TO MICROSPHERE SLOW RELEASE!
    • *PRODRUG OF PALIPERIDONE (INVEGA) SO THEY HAVE VIRTUALLY THE SAME SEs

    • 1-2MG/DAY START THEN TITRATE UP
    • 2-6MG/DAY DOSE RANGE
    • 16MG/DAY MAX (*LIKELY EPS!)

    *HIGH DOSE RELATED EPS, AND NON-DOSE RELATED INCREASED PROLACTIN

    MODERATE IN ALL OTHER SEs AMONG SGAs

    • LAI:
    • 25MG + *3 WEEK PO OVERLAP (REQUIRED)
    • 25-50MG TARGET Q2WEEKS
    • 50MG MAX
  13. OLANZAPINE
    2ND GEN ATYP ANTIPSYCH (ZYPREXA AND ZYPREXA RELPREVV)

    • *POST INJECTION SYNDROME IS A HUGE CONCERN WITH LAI! SO RARELY GIVEN
    • *ALSO FOR ADOLESCENT BIPOLAR AND TREATMENT RESISTANT DEPRESSION

    • 2.5-10MG/DAY START THEN TITRATE UP
    • 5-20MG DOSE RANGE
    • 20MG MAX

    • HIGHLY ANTICHOLINERGIC
    • HIGHLY DOSE DEPENDANT SEIZURE THRESHOLD LOWERING
    • *HIGHEST WEIGHT GAIN ALONG WITH CLOZAPINE! BAD FOR DIABETICS!
    • HIGH LIPID ABNORMALITIES
    • HIGH GLUCOSE INTOLERANCE
    • *AGAIN, BAD FOR DIABETICS OR THOSE AT RISK!!!

    • LAI:
    • 150-300MG Q2WEEKS OR
    • 405MG Q4WEEKS
    • THIS APPLIES TO START, MAINTENANCE, AND MAX (NO ORAL OVERLAP NEEDED)

    CAN BE LARGELY GROUPED WITH CLOZAPINE IN MOST SE CATEGORIES. (NOT IN DOSING!)
  14. QUETIAPINE
    2ND GEN ATYP ANTIPSYCH (SEROQUEL)

    • *VERY SIMILAR TO CLOZAPINE IN DOSING, BUT NOT SE PROFILE
    • *POSSIBLY LOWEST PATIENT RETENTION
    • *ALSO FOR ACUTE BIPOLAR

    • 25MG BID START THEN TITRATE UP
    • 300-800MG/DAY DOSAGE RANGE
    • 800MG/DAY MAX

    SIDE EFFECTS LOW/MODERATE ACROSS THE BOARD EXCEPT RELATED TO WEIGHT GAIN AND ALL DIABETIC RISK AREAS (WHERE IT IS NOTABLY HIGH)

    REMEMBER QUETIAPINE AND CLOZAPINE HAVE VERY SIMILAR DOSING SCHEDULES
  15. ZIPRASIDONE
    2ND GEN ATYP ANTIPSYCH (GEODON)

    *ABSOLUTELY MUST BE TAKEN WITH A 500+ CALORIE MEAL!

    • 20MG BID W/ FOOD START THEN TITRATE
    • 120-160MG/DAY DOSAGE RANGE
    • 160MG/DAY MAX

    VERY LOW/MODERATE SE PROFILE
  16. ARIPIPRAZOLE
    2ND GEN ATYP ANTIPSYCH (ABILIFY)

    • *LIKELY BEST CHOICE SGA FOR DIABETICS BASED ON SE PROFILE!
    • *ONE OF 2 ANTIPSYCHS FDA APPROVED FOR ADJUNCT DEPRESSION THERAPY!

    • 10-15MG START THEN TITRATE UP QOW
    • 10-15MG DOSAGE RANGE
    • 30MG MAX

    HAS LOW/MODERATE SE PROFILE, SO SAFER, BUT NOT LIKELY AS EFFECTIVE FOR LOWERING POSITIVE SYMPTOMS AS CLOZAPINE AND SOME OTHERS
  17. PALIPERIDONE
    2ND GEN ATYP ANTIPSYCH (INVEGA AND INVEGA SUSTENNA)

    • *BAD EPS AND PROLACTIN SEs
    • *MORE ACTIVE METABOLITE OF RISPERIDONE (RISPERDAL) WITH SIMILAR SE PROFILE
    • *FOOD INCREASES BIOAVAILABILITY 60%, BUT IS NOT REQUIRED LIKE GEODON

    • 6MG/DAY START THEN TITRATE UP
    • 6-12MG/DAY DOSAGE RANGE
    • 12MG/DAY MAX

    MODERATE WEIGHT GAIN AND OTHER DIABETIC RISK FACTOR SEs, AND ORTHOSTATIC HYPOTENSION, BUT LOW IN ALL OTHER SEs

    • LAI: Q4WEEKS
    • 234MG DAY 1 + 156MG DAY 8
    • 117MG (39-234MG) DOSAGE TARGET
    • 234MG MAX
    • (PO OVERLAP NOT REQUIRED)
  18. ILOPERIDONE
    2ND GEN ATYP ANTIPSYCH (FANAPT)

    *TITRATE NO FASTER THAN 2MG/DAY TO AVOID ORTHOSTATIC HYPOTENSION

    • 1MG BID START THEN TITRATE UP
    • 12-24MG/DAY DOSAGE RANGE
    • 24MG MAX

    LOW/MODERATE SE PROFILE EXCEPT FOR POTENTIAL ORTHOSTATIC HYPOTENSION, WHICH IS WHY THE DOSE SHOULD BE INCREASED BY ONLY 2MG/DAY WHEN NEEDED
  19. ASENAPINE
    2ND GEN ATYP ANTIPSYCH (SAPHRIS)

    *5MG SUBLINGUAL TABLETS THAT ARE ALWAYS TAKEN TWICE DAILY!

    • 5MG BID START
    • 5MG BID DOSAGE RANGE
    • 5MG BID MAX

    LOW SE PROFILE

    DO NOT SWALLOW TABLETS, NOR EAT OR DRINK FOR 10 MINUTES TO ALLOW ABSORPTION
  20. WHAT IS AN APPROPRIATE STARTING DOSE FOR 1ST GEN ANTIPSYCHOTICS OF HIGH, MID, AND LOW POTENCY RESPECTIVELY?

    WHAT ARE THE LOW, MID, AND HIGH POTENCY 1ST GEN ANTIPSYCHs?
    2MG, 10MG, 100MG

    LOW POTENCY: CHLORPROMAZINE (THORAZINE), THIORIDAZINE (MELLARIL)

    MID POTENCY: LOXAPINE (LOXITANE), MOLINDONE (MOBAN), PERPHENAZINE (TRILAFON)

    HIGH POTENCY: PIMOZIDE (ORAP), HALOPERIDOL (HALDOL), FLUPHENAZINE (PROLIXIN), THIOTHIXENE (NAVANE), TRIFLUOPERAZINE (STELAZINE)
  21. WHAT'S THE ONLY ANTIPSYCHOTIC DRUG FDA APPROVED FOR REFRACTORY SCHIZOPHRENIA (A 3RD CHOICE WHEN OTHERS HAVE NOT WORKED)?
    CLOZAPINE (CLOZARIL)
  22. WHAT'S THE ANTIPSYCH DRUG THAT PATIENTS TEND TO STAY ON THE LONGEST WITHOUT QUITTING?
    CLOZAPINE
  23. WHICH ANTIPSYCHOTIC RISKS DOSE DEPENDANT EPS WHEN DOSING OVER 6MG/DAY?
    RISPERIDONE (RISPERDAL)
  24. WHICH ANTIPSYCH DRUG IS ABSOLUTELY REQUIRED TO BE TAKEN WITH A 500+ CALORIE MEAL?
    ZIPRASIDON (GEODON)
  25. WHICH ANTIPSYCH COMES IN 5MG SUBLINGUAL TABLETS ONLY, AND IS 5MG BID DOSING ALWAYS?
    ASENAPINE (SAPHRIS)
  26. WHICH 2 ANTIPSYCHs HAVE THE WORST PROLACTIN SEs AND DOSE DEPENDANT EPS?
    • RISPERIDONE (RISPERDAL)
    • PALIPERIDONE (INVEGA)
  27. WHICH ANTIPSYCH DRUG HAS BY FAR THE GREATEST ABILITY TO DOSE DEPENDENTLY LOWER SEIZURE THRESHOLD?
    CLOZAPINE (CLOZARIL)
  28. WHICH 2 ANTIPSYCH DRUGS CAUSE THE MOST WEIGHT GAIN AND ADDITIONAL RISKS TO DIABETICS (LIPID ABNORMALITIES AND GLUCOSE INTOLERANCE)?
    • CLOZAPINE (CLOZARIL)
    • OLANZAPINE (ZYPREXA)
  29. WHICH ANTIPSYCH DRUG HAS THE GREATEST OCCURANCE OF AGRANULOCYTOSIS?
    CLOZAPINE (CLOZARIL) WITH ABOUT 1%
  30. WHAT ARE THE ONLY 2 ANTIPSYCH DRUGS APPROVED ALSO FOR TREATMENT RESISTANT DEPRESSION?
    ARIPIPRAZOLE (ABILIFY)

    OLANZAPINE (ZYPREXA)
  31. WHICH ANTIPSYCH DRUG MUST BE MONITORED (WITH PATIENTS ON A REGISTRY) TO WATCH THEIR LIPID PROFILE?
    CLOZAPINE
  32. WHAT WOULD BE THE 3 BEST 2ND GEN ANTIPSYCH DRUGS TO SWITCH A PATIENT TO IF THEIR PSYCHIATRIST DECIDES THEY NEED TO SWITCH OFF OF CLOZAPINE AND LOSE WEIGHT?
    • 1. ARIPIPRAZOLE (ABILIFY)
    • 2. ZIPRASIDONE (GEODON)
    • 3. ASENAPINE (SAPHRIS)
  33. WHICH SGA WOULD LIKELY BE THE SAFEST FOR A DIABETIC?
    ARIPIPRAZOLE (ABILIFY)

    DUE TO LOWEST WEIGHT GAIN AND OTHER DIABETIC RISK FACTOR SEs
  34. WHICH 1ST GEN TYPICAL ANTIPSYCHOTICS ARE PRIMARILY METABOLIZED BY CYP 2D6? (MNEMONIC)
    "COMMON FELLOWS, HE'S MAKING PROGRESS THERE!" (C-F-H-M-P-T)

    • C-CHLORPROMAZINE (THORAZINE)
    • F-FLUPHENAZINE (PROLIXIN)
    • H-HALOPERIDOL (HALDOL)
    • M-MOLINDONE (MOBAN)
    • P-PERPHENAZINE (TRILAFON)
    • T-THIORIDAZINE (MELLARIL)

    • SINCE P AND T HAVE MULTIPLE 1ST GEN ANTIPSYCHs TO CHOOSE FROM, PICK THE ONE WITH LOWEST POTENCY.
    • EX: THIORIDAZINE HAS VERY LOW POTENCY, BUT THIOTHIXENE AND TRIFLUOPERAZINE HAVE HIGH POTENCY, SO THIORIDAZINE IS THE ONE METABOLIZED BY CYP-2D6.
  35. WHICH 2 1ST GEN ANTIPSYCHs ARE 1A2 METABOLIZED?
    • THIOTHIXENE (NAVANE)
    • TRIFLUOPERAZINE (STELAZINE)

    (T=1A2 IF HIGH POTENCY)

    BOTH HAVE NO/MINOR INHIBITION.
  36. WHICH 1ST GEN ANTIPSYCH IS METABOLIZED BY CYP-3A4, BUT HUGELY INHIBITS CYP-2D6?
    PIMOZIDE (ORAP)

    (THE MOST POTENT ONE IS ALSO THE MOST UNIQUE METABOLIZER.)
  37. WHICH 1ST GEN ANTIPSYCH MODERATELY INHIBITS CYP-3A4?
    HALOPERIDOL (HALDOL)

    IT ALSO INHIBITS CYP-2D6, WHICH IS ALSO THE PRIMARY ENZYME METABOLIZING HALDOL.
  38. WHICH 1ST GEN ANTIPSYCHs INHIBIT CYP-2D6 AT LEAST MODERATELY? (5)
    • PIMOZIDE (ORAP) - MAJOR INHIBITION!
    • HALOPERIDOL (HALDOL)
    • CHLORPROMAZINE (THORAZINE)
    • THIORIDAZINE (MELLARIL)
    • PERPHENAZINE (TRILAFON)

    TAKE YOUR 2 MOST POTENT, 2 LEAST POTENT, AND "TRY LAUGHIN" TO FIND YOUR 5 MODERATE/MAJOR CYP-2D6 INHIBITORS.
Author
cmg7737
ID
49116
Card Set
CNS 2 TEST 1
Description
CNS 2 TEST 1
Updated