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Dopamine Release onto Striatal Neurons Pic
- Symptomatic: improves symptoms
- Neuroprotective: slows nerve cell loss
- Restorative: restores cell function or increases the number of cells
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
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
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
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):
What are the two classes of Dopamine Agonists?
Ergots and Non-ergots
Dopamine Agonists - Ergots
Bromocriptine (Parlodel): may cause fibrosis
Dopamine Agonist- Non-ergots
- Pramipexole (Mirapex):
- Ropinirole (Requip):
- Apomorphine (Apokyn):
- entacapone (comtan):
- tolcapone (Tasmar):
- entacapone/carbidopa/levodopa (Stalevo):
How do the medications work? -Memorize this pic
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
- Doses: 25/100 and 50/200
- Half life longer
- improves motor fluctuations
- slower absorption
- good for dosing at night
- 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
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.
- Rarely used.
- More effective than entacapone but rarely used.
- Liver failure.
- Must carefully monitor.
- Doses: 50, 100, 150mg
- Doses reflect mgs of levodopa combined with 200 mg entacapone and varying amounts of carbidopa
- comptan and sinemet together
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
Dopamine Agonists MOA
Simulate the action of dopamine
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)
Dopamine Agonists Side Effects
- Orthostatic hypotension:
- hallucinations: are more frequent with agonists than levodopa
- sleep attacks: (resulting in Motor Vehicle Accidentss)
- increase dyskinesias:
- compulsive behaviors:
Are MOAb inhibitors neuroprotective or symptomatic?
- Selegiline: alleviate Sxs by MAO-B blockade, SSRI and TCA interaction
- Rasagiline: made by same company that makes the generic seleginline
Anticholinergics: MOA, Indications, S/Es
- Trihesyphenidyl (Artane):
- Cogentin (benztropine):
- Not conclusive if this works!
- Indication: management of nausea associated with levodopa
- Mech: Peripheral dopamine antagonist
Indication: nausea for when more carbidopa is needed
Whats the most effective drug for parkinsons disease? (key question)
What drug causes compulsive gambling?
What causes splotcy legs?
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
What would you like to do?
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