Parkinsons Flashcards

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
Q

What is a uncommon but unique AE of dopamine receptor agonists?

A

gambling

-especially ropinirole

26
Q

In what situation would dopamine receptor agonists may be used as first line?

A

to treat early onset PD to delay the use of levodopa

-avoid dyskinesias

27
Q

Bromocriptine is a dopamine ____________

A

agonist

28
Q

What kind of drug is pramirexole?

A

dopamine receptor agonist

29
Q

Which of the dopamine receptor agonists are given in subQ form?

A

apomorphine

30
Q

Dopamine receptor agonists are also used in the treatment of __________

A

RLS

-i have no idea what this is but it was in his slides

31
Q

In what situation is apomorphine useful?

A

acute

32
Q

Dopamine is ____________

A

inhibitory

33
Q

Acetlycholine is _________

A

excitatory

34
Q

What regulates voluntary movement?

A

substantia nigra in basal ganglia of midbrain

35
Q

What two drugs are inhibitors of dopamine metabolism?

A

selegiline

rasagiline

36
Q

Where is selegiline active?

A

CNS-not periphery

37
Q

MOA of rasagiline

A

inhibits breakdown of dopamine

38
Q

Selegiline and rasagiline are ___________ inhibitors

A

MAO-B

39
Q

MAO-A vs MAO-B

A

MAO-A: tyramine, NE, epi, serotonin

MAO-B: dopamine

40
Q

What is the difference between selegiline/rasagiline and COMT inhibitors?

A

COMT acts in periphery

selegiline/rasagiline act in CNS

41
Q

Selegiline may last for _____________

A

months

42
Q

Is rasagiline selective for MAO-B?

A

nope

43
Q

Which is more potent, selegiline or rasagiline?

A

rasagiline is x5 more potent

44
Q

What kind of drug inhibits the metabolism of dopamine?

A

selegiline/rasagiline

-inhibitors of dopamine metabolism

45
Q

In advanced disease you can give selegiline/rasagiline with _____________ to enhance effect

A

levodopa

46
Q

What kind of drug is amantadine?

A

dopamine reuptake inhibitor

47
Q

MOA of amantadine

A

stimulates presynaptic release of dopamine

inhibits presynaptic reuptake of dopamine

48
Q

What is a unique con about amantadine?

A

starts working in a few weeks and stops after a few months

-given in 1-2 week periods during exacerbations

49
Q

Amantadine vs. levodopa

A

not as effective but fewer AE

50
Q

Amantadine is ___________ effective than anticholinergics

A

less

51
Q

What kind of drug is benztropine?

A

anticholinergic

52
Q

What kind of drug is trihexyphenidyl?

A

anticholinergic

53
Q

What kind of drug is diphenhydramine?

A

anticholinergic

54
Q

MOA of benztropine

A

reduces the relative excess of ACh vs dopamine

55
Q

What are could you give to treat tremors, salivation and spasticity associated with PD?

A

anticholinergics

  • benztropine
  • trihexyphenidyl
  • diphenhydramine
56
Q

What drug essentially “replaces” dopamine?

A

levodopa

57
Q

What drugs stimulate dopamine receptors?

A

bromocriptine
ropinirole
pramiprexole
rotigotine

58
Q

What drugs inhibit the breakdown of CNS dopamine?

A

selegiline

rasagiline

59
Q

What drug increases the levels of CNS dopamine?

A

amatadine

60
Q

What kind of drugs may exacerbate PD?

A
antipsychotics
antiemetics
-promethasize, metoclopramide, prochlorperizine 
DA depleting Rx
-reserpine, methyldopa
61
Q

What agents decreased the metabolism of levodopa?

A

AADC inhibitors

COMT inhibitors