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2010-09-19 17:55:12

Pharmacotherapy 3 test 1 parkinsons
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  1. Dopamine Release onto Striatal Neurons Pic
  2. Treatment Strategies
    • Symptomatic: improves symptoms
    • Neuroprotective: slows nerve cell loss
    • Restorative: restores cell function or increases the number of cells
  3. Restorative Thereapies-Under study- probably not on exam
    • Intraputamenal GDNF: demonstrated improvement in 6 weeks, double blind trial results were disappointing
    • CERE-120: Intrastriatal neurturin (NTN) therapy funded by ceregene phase II planned

    These are surgical interventions
  4. Neuroprotection for PD-Under study- probably not on exam
    • Coenzyme Q 10: provacative data using 1200mg/day (about $200/month)
    • Selegiling (Eldepryl): not neuroprotective in over 800 patients in DATATOP Trial
    • Vitamin E: DATATOP study, not neuroprotective
    • Creatinine: Further study merited
    • Isradipine (Dynacirc): Ca+ channel blocker, (calcium channels present in dopamine cells), shown to affect disease progression Mike Lee does work with transgenic mice models for parkinsons in the football stadium
  5. Symptomatic Research Therapies-Under study- probably not on exam
    • Adenosin A2a antagonists: provide a dopaminergic effect. e.g.. istradefylline
    • Dopamine agonists: SLV-208 or once daily ropinirole
    • AMPA blockers: E2000
    • Gene Thereapies: shown some benifit but maybe placebo

    Under study- probably not on exam
  6. What are the current symptomatic medication options?
    • Levodopa/carbidopa (Sinemet): Gold Standard sinemet is latin for without vomiting
    • Anticholinergics: trihexyphenidyl (Artane) and beztropine (cogentin)
    • Amantadine (symmetrel):
    • Selegiline (Eldepryl):
    • Rasagiline (Azilect):
  7. What are the two classes of Dopamine Agonists?
    Ergots and Non-ergots
  8. Dopamine Agonists - Ergots
    Bromocriptine (Parlodel): may cause fibrosis
  9. Dopamine Agonist- Non-ergots
    • Pramipexole (Mirapex):
    • Ropinirole (Requip):
    • Apomorphine (Apokyn):
  10. COMT Inhibitors
    • entacapone (comtan):
    • tolcapone (Tasmar):
    • entacapone/carbidopa/levodopa (Stalevo):
  11. How do the medications work? -Memorize this pic
  12. Levodopa/Carbidopa (Sinemet): Dose, S/Es, Notes
    • Most effective treatment for all features
    • Controversial as to when to begin and the most appropriate dose.
    • Doses: 10/100, 25/100, 25/250
    • S/Es: nausea, light-headedness, dyskinesias, hallucinations, sleep attacks
  13. Sinemet CR
    • Doses: 25/100 and 50/200
    • Half life longer
    • improves motor fluctuations
    • slower absorption
    • good for dosing at night
  14. COMT Inhibitors
    • COMT metabolizes L-dopa primarily in the GI tract
    • Peripheral COMT blockade improves CNS L-dopa levels
    • Central COMT inhibition is of unclear benefit

    Stalevo: carbidopa + l-dopa + entacapone
  15. COMT Inhibitors-Mechanism, S/Es, indication, dosing
    • Mechanism: more l-dopa gets into the brain
    • S/Es: the increase l-dopa may result in side-effects such as dykinesias
    • Clinical indication: to improve motor fluctuations in chronic PD
    • Dosing: l-dopa dose reduction is often required after starting COMT inhib.
  16. Tolcapone:
    • Rarely used.
    • More effective than entacapone but rarely used.
    • Liver failure.
    • Must carefully monitor.
  17. Stalevo
    • Doses: 50, 100, 150mg
    • Doses reflect mgs of levodopa combined with 200 mg entacapone and varying amounts of carbidopa
    • comptan and sinemet together
  18. Entacapone (comtan): MOA, S/Es, Cost, dose
    • MOA: peripheral blockade of COMT
    • S/Es: diarrhea, increased dyskinesias
    • Cost: $166/month
    • Dose: 200 mg entacapone with each l-dopa dose
  19. Dopamine Agonists MOA
    Simulate the action of dopamine
  20. Dopamine Agonist Half-lives
    • Levodopa: 1 hour
    • Bromocriptine: 3-8 hours
    • Ropinirols: 4-6 hours
    • Pramipexole: 8-12 hours
    • Cabergoline: 65-72 hours (for breast feeding mothers)
  21. Dopamine Agonists Side Effects
    • Orthostatic hypotension:
    • hallucinations: are more frequent with agonists than levodopa
    • somnolence:
    • sleep attacks: (resulting in Motor Vehicle Accidentss)
    • nausea:
    • increase dyskinesias:
    • compulsive behaviors:
  22. Dopamine Agonist Doses
  23. Are MOAb inhibitors neuroprotective or symptomatic?
  24. MAOb Inhibitors
    • Selegiline: alleviate Sxs by MAO-B blockade, SSRI and TCA interaction
    • Rasagiline: made by same company that makes the generic seleginline
  25. Anticholinergics: MOA, Indications, S/Es
  26. Anticholinergic Meds
    • Trihesyphenidyl (Artane):
    • Cogentin (benztropine):
  27. Amantadine (Symmetrel):
    • Not conclusive if this works!
  28. Motilium (domperidone)
    • Indication: management of nausea associated with levodopa
    • Mech: Peripheral dopamine antagonist
  29. Lodosyn (carbidopa)
    Indication: nausea for when more carbidopa is needed
  30. Whats the most effective drug for parkinsons disease? (key question)
  31. What drug causes compulsive gambling?
    Dopamine Agonists
  32. What causes splotcy legs?
  33. What drug interactions should you be careful for with selegiline?
    • 1. SSRIs and TCAs: serotonin syndrome
    • 2. Meperidine (demorol):
    • 3. Tyramine containing foods: hypertensive crisis