med chem III quiz 6 anti-psychotics - hypnotics

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med chem III quiz 6 anti-psychotics - hypnotics
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med chem III quiz anti psychotics hypnotics
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med chem III quiz 6 anti-psychotics - hypnotics
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  1. first gen
    phenothiazine
    aliphatic
    anit-emetic
    ind - pediatric behavioral problems
    high sedative effects
    chlorpromazine - thorazine
  2. first gen
    phenothiazine
    piperazine
    low sedative effects
    50X more potent than chlorpromazine
    prodrug ester
    fluphenazine
  3. first gen
    phenothiazine
    piperazine
    IV only
    10X more potent than chlorpromazine
    reduce dose for elderly
    perphenazine
  4. first gen
    phenothiazine
    piperazine
    short term only
    20X more potent than chlorpromazine
    promethazine
  5. first gen
    phenothiazine
    piperazine
    commonly used anti-emetic
    suppositories as well
    7.5X more potent than chlorpromazine
    prochlorperazine - compro
  6. first gen
    piperdine
    prodrug discontinued
    metabolite of thioridazine
    mesoridazine - serentil
  7. first gen
    phenothiazine
    piperdine
    parent drug
    cardiotoxic agent
    equipotent to chlorpromazine
    thioridazine - mellaril
  8. first gen
    thioxanthene
    25X as potent than chlorpromazine
    not for children <12
    thiothixene - navan
  9. first gen
    butyrophenone
    DOC for tourette's
    for PCP overdose
    SE severe extrapyramidal effects
    50X as potent as chlorpromazine
    haloperidol
  10. first gen
    diphenylbutylpiperdine
    ind - tourette's, not first line though
    monitor ECG
    pimozide - orap
  11. may have a role in the tourette's syndrome
    L-Histadine
  12. second gen
    thienobenzodiazepine
    ind - schizo, BPD, dementia related to alzheimers
    oral disintegrating tabs
    heavy sedation
    less weight gain
    olanzapine - zyprexa
  13. second gen
    dibenzothiazepine
    multi receptor antagonist
    no anticholinergic side effects
    increased heart issues
    less weight gain
    extended release form
    quetiapine fumarate - seroquel
  14. second gen
    dibenzodiazpine
    ind - if not responding to other agents
    agranulocytopenia - must do blood work for refill
    only dispense 1 week at a time
    available through patient management system
    clozapine - clozaril
  15. second gen
    benzisoxazole
    ind - demential from alzheimers
          delay of relapse in long term Tx of schizo
    no anticholinergic effects
    risperidone - risperdal
  16. second gen
    benzthiazole
    80 mg dose max --> QT elongation
    metabolized by 3A4 & 1A2
    no inhibition on CYP
    ziprasidone - geodon
  17. second gen
    agonist and antagonist properties
    metabolized by 2D6
    steady state reached in 14 days
    aripiprazole - abilify
  18. second gen
    benzisoxazole
    active metabolite of risperidone
    ER and injectable
    antagonism of D2 and 5HT2A receptors
    T1/2 - 23 hours, watch for accumulation in elderly
    • paliperidone - invega --> ER
    • sustenna - invega --> injectable
  19. second gen
    benzisoxazole
    D2 and 5HT2A antagonism
    alpha1 - antagonist --> titrate dose (severe orthostatic hypotension)
    iloperidone - fanapt
  20. second gen
    ind - acute adult schizo, bipolar 1 disorder
    moa - very promiscuous
    < 2% bioavailability orally
    35% bioavailability sublingual
    asenapine - saphris
  21. second gen
    benzoisothiazol derivative
    ind - adult schizo
    black box warning - cerebrovascular AE
    metabolized by 3A4
    lurasidone - latuda
  22. anti-psychotic
    manic episodes
    increase neutrophil count in chemo pts
    competes with Mg possibly
    watch for dehydration - toxic
    lithium
  23. 1st drug for chorea
    black box warning - increase risk of suicide
    moa - reversible depletor of monoamines
             reversible VMAT2 inhibitor
    significant CYP induction
    tetrabenzine - xenazine
  24. increased Cu in the brain
    treated with zinc acetate or D-penicillamine
    wilson's disease
  25. anti-parkinson's
    anti-cholinergic
    not for children <3yo
    benztropine mesylate - cogentin
  26. anti-parkinson's
    anticholinergic
    idiopathic
    T1/2 - 18-24 hours
    biperiden - akineton
  27. antiparkinson's
    anticholinergic
    best tolerated in elderly with mild PK
    lower incidence of peripheral SE
    diphenhydramine - benadryl
  28. anitparkinson's
    anticholinergic
    quatenary
    reduce other drugs dose when used adjunct
    trihexyphenidyl
  29. antiparkinsons
    dopaminergic
    direct agonist unstable photochemically
    pramipexole - mirapex
  30. antiparkinson
    dopaminergic
    direct agonist D3 & D2 only
    SE - hallucinations
          teratogenic
    extensive 1A4 metabolism
    restless leg syndrome
    once daily Tx
    ropinirole - requip
  31. antiparkinson
    DOC - carbon monoxide poisoning
    moa - produces increased dopamine release
    amantadine
  32. antiparkinson
    moa - dopamine agonist
    use if unresponsive to levodopa
    ergot
    • cycloset
    • higher dose bromocriptine - parlodel
  33. antiparkinsons
    inhibits peripheral decarboxylase enzyme
    does not cross BBB
    SE - watch for blepharospasm
    carbidopa - lodosyn
  34. antiparkinsons
    ind - relief of herpes zoster shingle pain and restless leg syndrome
    prodrug converted in CNS
    SE - dark urine and sweat
    levodopa
  35. antiparkinson
    used with wearing off syndrome
    moa - selective and reversible inhibitor of COMT
    entacapone - comtan
  36. antiparkinson
    watch for fulminant liver failure
    selective and reversible competitive inhibitor of COMT
    metabolized by methyl hydroxylation and glucuronidation
    tolcapone - tasmar
  37. antiparkinson
    moa - irreversible monoamine oxidase type B suicide substrate inhibitor - CNS only enzyme
    selegiline - eldepryl
  38. orally disintegrating MOA inhibitor
    zelapar
  39. antiparkinson
    adjunct or alone
    irreversible MAO type B inhibitor
    metabolized by 1A2
    monitor for melanoma
    rasagiline - azilect
  40. combo product for parkinsons
    stalevo
  41. possible used to slow the progression of parkinsons
    coenzyme Q10
  42. antiparkinsons
    used for end of dose wearing off episodes
    used for severe emesis in poisoning cases
    MOA - stimulates post synaptic D2 receptors
    subQ only
    apomorphine - apokyn
  43. antiparkinsons
    non-ergot DA agonist
    continuously delivered to avoid DA pulsation
    transdermal
    rotigotine - neupro
  44. alzheimers
    cholinesterase inhibitor
    discontinued
    monitor serum transaminase levels
    tacrine - cognex
  45. alzheimers
    cholinesterase inhibitor
    centrally acting
    has active metabolites
    dose based on serum transaminase levels
    donepezil - aricept
  46. alzheimers
    cholinesterase inhibitor
    centrally acting
    metabolized by decarbamoylation
    SE - N/V, anorexia and weight loss
    transdermal patch available
    rivastigmine - exelon
  47. alzheimers
    first drug for severe stages
    moa - blocks glutamate, uncompetitive open-channel antagonist
    excreted unchanged in the urine
    memantine - namenda
  48. alzheimers
    extracted from the bulbs of daffodil narcissus pseudonarcissus
    cholinesterase inhibitor
    metabolized by 2D6 & 3A4
    SE - bradycardia
    galantamine - razadyne
  49. hypnotic
    imidoazopyridine
    ind - short term Tx of insomnia
    MOA - modulation of GABA receptor
    reduce dose in hepatic impairment
    zolpidem - ambien
  50. sublingual zolpidem
    edluar
  51. oral spray zolpidem
    zolpimist
  52. sublingual zolpidem for middle of the night awakening
    intermezzo
  53. hypnotic
    pyrazolopyrimidine
    short term management of insomnia
    moa - specific binding to GABA omega1 receptor
    japanese subjects have increased levels
    zaleplon - sonata
  54. hypnotic
    ind - sedation of ICU pts
    moa - relative selective alpha 2 agonist
    injection only
    dexmedetomidine - precedex
  55. hypnotic
    hospital used
    moa - similar to BZ's w/ less selectivity and higher abuse potential
    CI in epileptics
    meprobamate
  56. benzo with shortest half life
    flurazepam
  57. benzo with longest half life
    quazepam - doral
  58. benzo with lowest hypnotic dose
    triazolam - halcion
  59. benzo with quickest onset
    flurazepam
  60. benzo to be used if a full night sleep is obtained
    triazolam - halcion
  61. first barb
    can cause CNS depression and decreased IQ tests in kids
    very long half life 50h
    phenobarbital
  62. barb hypnotic
    intermediate acting
    onset of action 45 - 60 minutes
    decrease dose in hepatic problems
    T1/2 - 66-140 minutes
    butabarbital - butisol
  63. 2 - barb sedative & hypnotic
    short acting
    onset of action 10-15 min.
    • pentobarbital - nembutal
    • secobarbital - seconal
  64. pyrrolopyrazine derivative for insomnia
    moa - allosterically coupled to BZ receptor
    safer for long term use
    eszopiclone - lunesta
  65. idenofuran used of insomnia
    moa - melatonin receptor agonist
    ind - Tx of adults w/ trouble falling asleep
    watch w/ hepatic deficiency
    ramelteon - rozerem
  66. TCA for insomnia
    doxepin - silenor

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