Parkinsons Flashcards

(61 cards)

1
Q

MOA of levodopa

A

converted in the CNS to dopamine

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2
Q

What converts levodopa to dopamine?

A

AA decarboxylase

AADC

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3
Q

What is the DOC for primary PD?

A

Levodopa

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4
Q

What agents decreased enzymatic metabolism of levodopa?

A

AADC inhibitors

COMT inhibitors

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5
Q

How many times per day is levodopa given? why?

A

3-5

short 1/2 life

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6
Q

Levodopa has the fastest onset to treat_____________

A

bradykinesias

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7
Q

What is a con of treating with levodopa?

A

Duration of action becomes shorter, and risk of dyskinesias increased w/increasing dosage

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8
Q

Levodopa may activate _________________

A

malignant melanoma

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9
Q

What medications should you give with levodopa?

A

entacapone
tolcapone
carbidopa

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10
Q

MOA of entacapone

A

Inhibits COMT which INCREASES levodopa uptake

-enhances bioavailability

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11
Q

MOA of carbidopa

A

Inhibits AADC so levodopa is not broken down before it can pass the BBB

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12
Q

MOA of tolcapone

A

Inhibits COMT which INCREASES levodopa uptake

-enhances bioavailability

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13
Q

Carbidopa is only given with _____________

A

levodopa

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14
Q

You can ____________ levodopa dosage when combined with carbidopa

A

decrease

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15
Q

Carbidopa + levodopa

A

sinemet

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16
Q

What is AACD?

A

responsible for converting levodopa to dopamine in periphery and CNS
-which is why we want to inhibit it-prevents the breakdown

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17
Q

AE of tolcapone

A

diarrhea, liver issues

LFTs q2wks x 1 year

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18
Q

AE of entacapone

A

Confusion, dizziness, sedation, hallucinations

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19
Q

What is something unique about tolcapone?

A

Crosses the BBB so it also inhibits CNS metabolism of dopamine by COMT (in addition to its action on levodopa)

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20
Q

MOA of carbidopa

A

inhibits AADC

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21
Q
The following are what type of drug:
bromocriptine
pramiprexole
ropinirole
apomorphine
A

Dopamine receptor agonists

-Directly stimulates postsynaptic DOPAMINE receptors

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22
Q

Apomorphine is contraindicated in pt w/___________________

A

orthostatic hypotension

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23
Q

What is something unique about apomorphine?

A

Need an antiemetic to avoid severe nausea and vomiting

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24
Q

Apomorphine can be given with _____________ to reduce the risk of nausea and vomiting

A

trimethobenzamide

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25
What is a uncommon but unique AE of dopamine receptor agonists?
gambling | -especially ropinirole
26
In what situation would dopamine receptor agonists may be used as first line?
to treat early onset PD to delay the use of levodopa | -avoid dyskinesias
27
Bromocriptine is a dopamine ____________
agonist
28
What kind of drug is pramirexole?
dopamine receptor agonist
29
Which of the dopamine receptor agonists are given in subQ form?
apomorphine
30
Dopamine receptor agonists are also used in the treatment of __________
RLS | -i have no idea what this is but it was in his slides
31
In what situation is apomorphine useful?
acute
32
Dopamine is ____________
inhibitory
33
Acetlycholine is _________
excitatory
34
What regulates voluntary movement?
substantia nigra in basal ganglia of midbrain
35
What two drugs are inhibitors of dopamine metabolism?
selegiline | rasagiline
36
Where is selegiline active?
CNS-not periphery
37
MOA of rasagiline
inhibits breakdown of dopamine
38
Selegiline and rasagiline are ___________ inhibitors
MAO-B
39
MAO-A vs MAO-B
MAO-A: tyramine, NE, epi, serotonin | MAO-B: dopamine
40
What is the difference between selegiline/rasagiline and COMT inhibitors?
COMT acts in periphery | selegiline/rasagiline act in CNS
41
Selegiline may last for _____________
months
42
Is rasagiline selective for MAO-B?
nope
43
Which is more potent, selegiline or rasagiline?
rasagiline is x5 more potent
44
What kind of drug inhibits the metabolism of dopamine?
selegiline/rasagiline | -inhibitors of dopamine metabolism
45
In advanced disease you can give selegiline/rasagiline with _____________ to enhance effect
levodopa
46
What kind of drug is amantadine?
dopamine reuptake inhibitor
47
MOA of amantadine
stimulates presynaptic release of dopamine | inhibits presynaptic reuptake of dopamine
48
What is a unique con about amantadine?
starts working in a few weeks and stops after a few months | -given in 1-2 week periods during exacerbations
49
Amantadine vs. levodopa
not as effective but fewer AE
50
Amantadine is ___________ effective than anticholinergics
less
51
What kind of drug is benztropine?
anticholinergic
52
What kind of drug is trihexyphenidyl?
anticholinergic
53
What kind of drug is diphenhydramine?
anticholinergic
54
MOA of benztropine
reduces the relative excess of ACh vs dopamine
55
What are could you give to treat tremors, salivation and spasticity associated with PD?
anticholinergics - benztropine - trihexyphenidyl - diphenhydramine
56
What drug essentially "replaces" dopamine?
levodopa
57
What drugs stimulate dopamine receptors?
bromocriptine ropinirole pramiprexole rotigotine
58
What drugs inhibit the breakdown of CNS dopamine?
selegiline | rasagiline
59
What drug increases the levels of CNS dopamine?
amatadine
60
What kind of drugs may exacerbate PD?
``` antipsychotics antiemetics -promethasize, metoclopramide, prochlorperizine DA depleting Rx -reserpine, methyldopa ```
61
What agents decreased the metabolism of levodopa?
AADC inhibitors | COMT inhibitors