med chem III test III anticonvulsant - MS

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  1. 2.5 million Americans are afflicted with epilepsies with more than 40 distinct types identified means?
    wear a medic alert identification
  2. 3 general physiologic mechanisms of drugs to treat seizures
    1. limit the sustained repetitive firing by promoting the inactivated Na channel

    2. enhance GABA

    3. less commonly limiting the T-current Ca channel
  3. 5 off label uses of anti convulsants
    • migraines
    • neuropathic pain
    • mood disorders
    • schizo
    • neuromuscular disorders
  4. 4 drugs used for partial seizures
    • carbamazepine
    • clonazepam
    • phenytoin
    • valproic acid
  5. 2 drugs used for absence seizures
    • valproic acid
    • clonazepam
  6. 3 drugs used for tonic clonic seizure
    • carbamazepine
    • diazepam
    • phenytoin
  7. 2 drugs used for status epilepticus
    • diazepam
    • phenytoin
  8. hydantoin
    ineffective in absence seizures
    use single manufactures product
    small therapeutic window 5-20 micrg/mL
    phenytoin - dilantin
  9. hydantoin
    no sedative property  in normal doses
    overdose = ataxia
    many drug interactions
    never IM
    phenytoin - dilantin
  10. major side effet of phenytoin
    gingival hyperplasia
  11. hydantoin
    ind - SE
    water soluble injectable phosphate prodrug
    must be diluted into 5% dextrose
    must monitor resp, ECG & BP during admin
  12. hydantoin
    tabs taken in 4-6 divided doses per day
    indiviudalize dosing, <2grams/day
    usually ineffective in adults
    ethotoin - peganone
  13. succinimide
    only for absence
    preferred for children
    may increase frequency of grand mal
    suppression of 3/cycle spike
    monitor for blood dyscrasias
    • ethosuximide - zarontin
    • methsouximide - celontin
  14. oxazolidinedione
    does not raise the seizure threshold
    metab - demethylation to metabs
    monitor blood dyscrasias
    tell MD if visual disturbances or infection
    trimethadione - tridione
  15. benzo
    be aware of additive sedative effects
    alone or adjunct
    clonazepam - klonopin
  16. benzo
    ind - adjunct in partial & alcohol withdrawl
    not for children <9yo
    clorazepate - gen-Xene
  17. benzo
    oral - adjunct
    rectally - refractory pts
    parenterally - SE
    diazepam - valium
  18. benzo
    2 yo and up for lennox-gastaut syndrome
    alcohol increases blood levels by 50%
    metab by 3A4
    clobazam - onfi
  19. azepine
    SE - agranulocytosis, Steven johnson syndrome (BBW)
    best for partial seizures
    MOA - reduce polysynaptic response and block post-tetanic potentials
    metab 3A4 to the epoxide
    carbamazepine - tegretol
  20. azepine
    ind - 4-16 yo w/ partial, atypical disorders
    moa-reduction of ketones to hydroxy group
    metab - glucuronide conjugation
    biphasic half life - parent 2hrs, metab 9 hrs
    oxcarbazepine - trileptal
  21. adjunct for petit mal
    tolerance develops rapidly
    moa - inhibit caronic anhydrase
    CI - sulfa allergy
    acetazolamide - diamox
  22. ind - convulsions due to hyomagnesiumia
           inhibition of premature labor
    injection only (IV,IM)
    moa - decrease amount of ACh at the end plate
    magnesium sulfate
  23. adjunct
    adverse effects - aplastic anemia, use in pts refractory to other therapies for partials
    felbamate - felbatol
  24. adjunct
    ind - 3-6yo w/ partial
           postherpetic neuralgia
           restless leg syndrome in adults
    moa - analog of GABA
    >12 yo dose function of CrCl
    gabapentin - neurontin
  25. analog of GABA but doesn't bind it
    ind - partial onset seizures in adults
           first approved for fibromyalgia
    moa - binds alpha2-delta site
    metab - negligible in humans
    pregabalin - lyrica
  26. adjunct
    ind - sole therapy in adults and adjunct in peds
    SE - stevens johnson syndrome
    often confused w/ other meds with similar names
    lamotrigine - lamictal
  27. adjunct
    hepatotoxicity, teratogenic, pancreatitis
    ind - mixed seizures and petit mal
    moa - increase GABA levels
    metab - glucuronidaton and CYP mediated b-oxidation
    will interfer with urine ketone tests
    >5 years decreased bone density in young children
    valproic acid - depakene
  28. adjunct
    ind - partial
    should be taken with food
    moa - binds GABA
    teratogenic in animals and excreted into breat milk
    tiagabine - gabitril
  29. adjunct
    partial onset and lennox gastaut in kids
    dose on CrCl
    moa - sulfamate monosaccharide, blocks Na channel action and increase GABA action and antaonizes glutamate
    maintain fluid intake due to stone formation
    topiramate - topomax
  30. adjunct
    partial in adults
    individualized dosing on CrCl
    possible teratogen
    levetiracetam - keppra
  31. adjunct
    grand mal, benign familial tremor
    not recommended in <8, individualized dosing
    bioequivalence issues among manufactures
    metab - to phenylethylmalonamide and phenobarbital
    primidone - mysoline
  32. adjunct
    partial in adults
    unrelated to any other
    moa - reduce T-type Ca channels
    metab - glucuronidation
    sulfonamide - watch for rash
    pediatric hyperthermia and oligohidrosis has occured
    drowsiness at high doses
    zonisamide - zonegran
  33. triazole
    ind - adjunct in lennox-gastaut in children 4 yo and up and adults
    use alternative BC
    moa? - prolongation of the inactive state of Na channels
    metab - not CYP, carboxylesterase mediated hydrolysis of carboxamide
    CI - pts w/ familial short QT syndrome
    watch for suicidal behavior and ideation
    rufinamide - banzel
  34. functionalized serine amino acid
    ind - partial onset seizure
    tab - pts >17yo
    inj - short term replacement when oral is not feasible
    moa - enhances slow inactivation of Na channels
    metab - CYP2C19
    watch for suicidal behavior and PR prolongation
    lacosamide - vimpat
  35. racemic agent, (S) pcol active
    ind - infantile spasms in 1mo - 2yo
           complex partial in adults
    available under SHARE program
    moa - irreversible inhibition of GABA-T
    metab - 2C9
    SE - irreversible damage to peripheral vision
    vigabatrin - sabril
  36. adjunct
    partial onset >18yo
    moa - K channel opener, via KCNG channel
    metab - N-acetylation, NO CYP
    SE - urinary retention, QT prolongation, possible teratogen
    ezogabine - potiga
  37. new in 2012
    partial onset w/ or w/o secondarily generalzed >12yo
    moa - non-competitve antagonist of AMPA
    metab - oxidation by 3A4/5
    SE - psychiatric can be serious, gait disturbances and falls
    perampanel - fycompa
  38. anti-alcoholic
    management of chronic alcoholics
    enforced sobriety
    inhibits alcohol dehydrogenase
    disulfiram - antabuse
  39. Tx of alcohol dependence
    decreases the craving
    moa - opioid antagonist
    injectable suspension
    CI - narcotic
    naltrexone - vivitrol
  40. Tx of alcohol dependence
    maintenance of abstinence
    moa - may interact with GABA & glutamate
    acamprosate - campral
  41. smoking deterrent
    works best with high physical addiction
    dispose of patches properly
    good pesticide
    nicotine - habitrol
  42. smoking cessation aid
    moa - maybe prevent NE and DA reuptake
    SE - seizures increased in anorexia nervousa
           insomnia common
    bupropion - zyban
  43. smoking cessation
    most effective to treat tobacco dependence
    moa - agonist for alpha4beta2 nicotinic ACh receptors
    BBW - neuropsychiatric symptoms
    varencline tartrate - chantix
  44. For MS
    ind - reduction with relapsing-remitting MS
    moa - possible modification of immune response
    glatiramer - copaxone
  45. MS drug
    ind - improves walking speed in pts
    moa- K channel antagonist
    CI - renal failure and seizure history
    ampyra - dalfampridine
  46. MS drug
    ind - oral Tx for relapsing
    moa - sphingosine 1-phosphate modulator
    CI - class Ia and III antiarrhytmics, beta blockers (additive effect), azole antifungals
    takes 2 months to eliminate from the body
    fingolimod - gilenya
  47. MS drug
    moa - humanized recombinant monoclonal antibody, by grafting murine antibody
    natalizumab - tysabri
  48. MS drug
    ind - pseudobulbar affects (laughter or crying) and amyotrophic lateral sclerosis
    dextromethorphan & quinidine - nuedexta
  49. MS drug
    ind - treat relaps
    moa - inhibits dihydroorotate dehydrogenase
    metab - hydrolysis with oxidation
    watch for liver failure
    teriflunomide - aubagio
  50. ALS CNS agent
    ind - amyotrophic later sclerosis and lou gehrig's
    moa - prevents glutamate release, inactivation of voltage dependent Na channels
    metab - hepatic hydroxylation
    discourage drinking and report febrile illness
    riluzole - rilutek
  51. misc PNS agent
    modified drooling scale used
    ind - reduce chronic drooling
    moa - ACh agent, competitive inhibitor
    DI - increases digoxin, atenolol metformin
         decreases haloperidol and levodopa
    CI - solid oral KCl
    glycopyrrolate - cuvposa

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med chem III test III anticonvulsant - MS
2013-04-09 16:04:35
med chem III test anticonvulsant MS

med chem III test III anticonvulsant - MS
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