Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Pharmacology Test 4 > Antiparkinson Drugs > Flashcards

Antiparkinson Drugs Flashcards

1
Q

What are the 4 main symptoms of Parkinson’s? secondary sxs?

A

bradykinesia, resting tremor, rigidity, postural instability. secondary: depression, dementia, autonomic dysfunction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is the pathology?

A

loss of a lot of DA in neurons in the Substantia Nigra. Also Lewy inclusion bodies in neurons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What drug is used to restore dopaminergic function?

A

Levodopa = L-DOPA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

1) what converts tyrosine to L-DOPA?

A

Tyrosine hydroxylase (TH)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

2) what converts L-DOPA to Dopamine?

A

aromatic-amino acid decarboxylase (AAD)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

what is the rate-limiting enzyme?

A

TH tyrosine hyroxylase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

3) which enzymes between Dopamine and Metabolites?

A

MAO-B (monoamine oxidase) and COMT (catechol O-methyltransferase)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Does Dopamine cross the blood brain barrier?

A

no

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Does tyrosine increase dopamine levels? why/why not?

A

no because TH (tyrosine hydroxylase) is already saturated with normal tyrosine levels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

what happens when L-DOPA is administered alone?

A

the majority of it is converted to DA by AAD in peripheral tissues before entering the brain.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is administered with L-DOPA and why?

A

Carbidopa because it inhibits peripheral AAD and can’t cross the blood brain barrier…it stops L-DOPA from being converted to dopamine by AAD in peripheral tissues before the brain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is carbidopa?

A

a peripheral AAD inhibitor administered with Levodopa

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What does Carbidopa do to L-DOPA levels?

A

it permits more L-DOPA to enter the brain where it can be converted to DA by AAD in brain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Therefore, Carbidopa (2):

A

1) increases the potency of L-DOPA (decreases required daily dose)
2) decreases production of DA in peripheral tissues, reducing peripheral side effects

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What are the peripheral side effects?

A

nausea, vomiting, postural hypotension

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What is the L-DOPA + Carbidopa drug?

A

Sinemet (like “cinema”)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What is another name for vitamin B6?

A

pyridoxine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What do high doses of pyridoxine do?

A

activates peripheral AAD which decreases L-DOPA levels

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

how many patients actually respond to L-DOPA?

A

~2/3

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

L-DOPA loses its effectiveness in about 5 years…why?

A

further loss of DA neurons and lack of new Da synthesis from L-DOPA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What is the on-off phenomenon? why?

A

L-DOPA effectiveness is on-off. dietary reason, persistent loss of DA neurons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What are the major side effects of L-DOPA (4)?

A

extrapyramidal dyskinesias, nausea and vomiting, postural hypotension, sleep disturbances

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What are the COMT inhibitors?

A

entacapone, tolcapone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Which COMT inhibitors work in the periphery?

A

entacapone and tolcapone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Which COMT inhibitors work in the CNS?

A

tolcapone

26
Q

How do COMT inhibitors work?

A

inhibit L-DOPA metabolism in peripheral tissues and/or DA metabolism in the brain (Tolcapone)

27
Q

Are COMT inhibitors used alone?

A

NO! Always used in combo with L-DOPA

28
Q

What are the side effects of COMT inhibitors?

A

diarrhea, increased sensitivity to L-DOPA

29
Q

What’s special about Tolcapone?

A

hepatotoxicity, peripheral and central

30
Q

What’s special about Entacapone?

A

peripheral COMT only, shorter duration

31
Q

What is the Levodopa + Carbidopa + Entacapone drug?

A

Stalevo

32
Q

What is Stalevo?

A

levodopa + carbidopa + entacapone

33
Q

What are the MAO-B Blockers?

A

Selegiline, Rasagiline

34
Q

Where do the MAO-B inhibitors work?

A

CNS (striatum)

35
Q

What is the mechanism of MAO-B blockers?

A

block DA metabolism by inhibiting MAO in striatum

36
Q

What does MAO-B do?

A

preferentially metabolizes DA

37
Q

What are the drug interactions with MAO-B blockers (2)?

A

1) contraindicated with Meperidine or Tricyclid antidepressants because of hyperthermic or hypertensive interactions
2) potential hypertension if used with L-DOPA

38
Q

What are the DA receptor agonists (3)?

A

Bromocriptine, Pramipexole, Ropinirole

39
Q

What are the older DA receptor agonists?

A

Bromocriptine

40
Q

What are the newer DA receptor agonists?

A

Pramipexole, Ropinirole

41
Q

What are the side effects of bromocriptine?

A

hypotension, nausea, dyskinesia

42
Q

Why are pramipexole and ropinirole better?

A

longer duration of action (less on and off) and good efficacy, side effects are less severe

43
Q

what are the side effects of pramipexole and ropinirole?

A

hypotension, nausea, dyskinesia, sleep disturbance, hallucination/confusion, risky behaviors. (less severe than bromocriptine)

44
Q

What are the muscarinic receptor antagonists?

A

Benztropine

45
Q

What does DA normally do to Ach?

A

DA released from nigrostriatal neurons activates D2 receptors on cholinergic neurons in the striatum and inhibits the release of Ach

46
Q

What does coordination of movement rely on?

A

balance of Ach and DA

47
Q

What happens to cholinergic activity in Parkinson’s?

A

Reduced DA activity leads to cholinergic hyperactivity

48
Q

What do muscarinic receptor antagonists do (benztropine)?

A

counteract cholinergic hyperactivity in PD

49
Q

What are the side effects of benztropine?

A

anti-parasympathetic: dry mouth, reduced sweating, increased heart rate

50
Q

What is benztropine especially effective against?

A

tremor

51
Q

What antiviral agent works for Parkinsons?

A

Amantadine

52
Q

What does Amantadine do?

A

increases DA release

53
Q

Downsides of amantadine?

A

beneficial effects are not as pronounces as L-DOPA and tolerance occurs within weeks

54
Q

What are the side effects of Amantadine?

A

(usually mild) restlessness, depression, livedo reticularis (purplish mottled skin discoloration), edema, hypotension, hallucinations

55
Q

What is the DA precursor?

A

L-DOPA

56
Q

What is the peripheral AAD inhibitor?

A

Carbidopa

57
Q

What are the COMT inhibitors?

A

Entacapone, Tolcapone

58
Q

What are the MAO-B inhibitors?

A

Selegiline, Rasagiline

59
Q

What is the anti-viral agent?

A

Amantadine

60
Q

What is the muscarinic receptor antagonist?

A

Benztropine

61
Q

What are the DA receptor agonists?

A

Bromocriptine, Pramipexole, Ropinirole

Pharmacology Test 4 (10 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions