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36 Cards in this Set
- Front
- Back
Function of MAO-B in the brain?
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Converts DA to DOPAC
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Name a selective MAO-B inhibitor?
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Selegiline
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Possible ways that selegiline can be administered?
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May be given w/ L-dopa to increase L-dopa efficacy or it can be given alone to treat very mild PD w/c will delay L-Dopa introduction.
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What is the oral dosage for Selegiline?
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<10mg/day to inhibit only MAO-B in the brain. If >10mg/day were given, it will also inhibit peripheral MAO-B & cause severe SE.
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How effective is L dopa therapy in PD pts?
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Initially in the honeymoon phase, it’s very effective but becomes less effective after 3-5yr where it starts to wear off.
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What SE are seen after the honeymoon phase of L dopa & why are these signs seen?
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Dyskinesia, akinesia, on & off, freezing. These SE occur b/c there is continuing loss of SN DA neurons; w/ loss L dopa can’t do its job b/c it relies on surviving DA to convert L dopa to DA
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Define On-off SE of L dopa?
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Unpredictable onset and offset of L dopa response
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What is the freezing SE of L dopa?
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Total lack of voluntary movements
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What are some possible solutions of L dopa SE?
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more frequent dosing, introduce COMTI, MAO-B inhibitor &/or DA agonists as combo Tx.
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What are the 5 DA R agonists?
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Apomorphine, bromocriptine, pramipexole, ropinirole, & rotigotine
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w/c DA agonist is injection only?
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Apomorphine
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w/c DA agonist is a skin patch?
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Rotigotine
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what are the similiarities of Pramipexole & Ropinirole?
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They can be used alone in early stage of PD or used w/ L-dopa in advanced PD. SE is falling asleep during daily activities.
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w/c DA agonists can be given w/ L-dopa in advanced PD?
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Bromocriptine, pramipexole, & ropinirole
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w/c DA agonist has blood pressure irregularities?
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Bromocriptine
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why are DA agonists more selective for D2 than D1?
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When D2 is stimulated, Gi is activated w/c decreases cAMP & therefore decreases GABA and also more D2 is found in the striatum.
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What is the increasing trend or preference w/ DA agonists?
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Is now given to new pts to delay L-dopa introduction so now given as monotherapy.
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These drugs are useful in late stage pts after long term L dopa use?
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DA agonists
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This DA agonist is given to pts in the “off” state of L dopa therapy?
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Apomorphine
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w/c DA agonist must always be used w/ L dopa Tx?
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Bromocriptine
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why has rotigotine been recalled by manufacturer?
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Drug crystallizes in the patch
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what SE do we see w/ DA agonists?
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N/V, postural hypotension.
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SE of DA agonist are more severe in who? Solution to this?
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Older pts suffer more from these SE so first line drugs should be L-dopa
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SE of pergolide?
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w/drawn from the market b/c it can cause serious damage to heart valves in a high percentage of pts
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When should anti-cholinergic agents be used in PD?
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Useful in pts not responding to L-dopa or agonists
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Anti-chol are primary used to treat what in PD?
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Tremor & rigidity
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What are the 3 anti-Ach drugs?
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Trihexyphenidyl, bentropine, & ethopropazine
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What is the MOA in treating PD?
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1)increases DA release, 2) inhibit reuptake of 5HT, 3) stimulate DA R, 4)may be anti-excitatory
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When is amantadine used?
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Monotherapy in early & mild PD. Can also be used in combo w/ L-dopa for pts in “wearing off”
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SE of amantadine?
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N, insomnia, hallucinations
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The role of GDNF in PD treatment?
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Since it’s essential for development, guidance, and maintenance of DA neurons, clinical trial study shows continuous delivery seems to produce benefit to early PD benefits
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Relate NSAIDS & anti-oxidants to PD?
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Both may be beneficial for treatment. Coenzyme Q10 possible anti-oxidant
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Relate caffeine & Estrogen to PD?
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Caffeine & Emay be neuroprotective; more Men have PD
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What is the pathology of Huntington Dz?
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There is a decrease in GABA in striatum & an increase in DA in nigra leading to excess DA activity and chorea movement
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How are symptoms managed in HD?
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1) Haloperidol to alleviate chorea, 2) reserpine to deplete pre-syn DA. 3) BZ used to increase GABA however their efficacy decreases as dz progresses. 4) tranquilizers to help control anxiety & 5) Li to combat pathological excitement & sever mood swings
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Relate # of GLU repeats to HD development?
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40 GLU repeats is the threshold for dz development; the more a pt has after 40, the early the dz will show up
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