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BMB Test 3 > B7-071 Drugs for Parkinsons Disease > Flashcards

B7-071 Drugs for Parkinsons Disease Flashcards

1
Q

what dopamine pathway modulates the extrapyrimidal motor system for controlled initiation of purposeful movement

A

nigrostriatal

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2
Q

what dopamine pathway functions in emotion, reward, and memory

A

mesolimbic

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3
Q

what dopamine pathway functions in attention and planning?

A

mesocortical

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4
Q

what dopamine pathway inhibits prolactin release from the anterior pituitary?

A

tuberoinfundibular (D2)

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5
Q

what dopamine pathway functions in emesis?

A

area postrema (d2)

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6
Q

D2 receptors function in the […] pathway of the basal ganglia

A

indirect

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7
Q

D1 receptors function in the […] pathway of the basal ganglia

A

direct

(D1rect)

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8
Q

which dopamine family of receptors is most important to therapeutic strategies in PD?

A

D2

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9
Q

primary strategy for PD therapy

A

replace or mimic dopamine

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10
Q

dopamine cannot cross the BBB, so it’s precursor […] is used to replace dopamine

A

L-DOPA

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11
Q

rate limiting step of dopamine synthesis

A

tyrosine hydroxylase

(why you can’t just take supplementary tyrosine for PD therapy)

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12
Q

reversal of rigidity, tremor, and bradykinesia in patients with PD

A

levodopa

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13
Q

levodopa works well for […] years of treatment

A

first few

(also only works really well for 1/3 of patients and doesn’t treat balance issues, etc)

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14
Q

most common side effects of levodopa [2]

A

nausea/vomiting via stimulation of D2 in CTZ
orthostatic hypotension

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15
Q

long term side effects of levodopa [3]

A

fluctuations in efficacy

abnormal involuntary movements (different than typical PD movements-80% of people develop this)

psychic side effects

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16
Q

fluctuations in efficacy of levodopa can be treated with [2]

A

opicapone- (COMT antagonist)
istradefylline (adenosine 2A antagonist)

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17
Q

levodopa can cause hallucinations, paranoia, mania, anxiety, depression, and impulse control via activation of […] pathways [2]

A

mesolimbic
mesocortical

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18
Q

management of psychic side effects of levodopa includes [3]

A

anti-psychotics that do not cause PD
lower dose of levodopa
pimavanserin

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19
Q

peak levels of levodopa occur […] to […] after administration

A

.5 - 2 hours

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20
Q

absorption of levodopa is dependent on

A

GI transit time

(less absorption with more time in transit)

anticholinergics decrease transit time

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21
Q

GI transit time is decreased by

A

anticholinergics

(may affect efficacy of levodopa)

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22
Q

half life of levodopa

A

1-3 hrs

23
Q

95% is decarboxylated in the periphery and excreted in urine

A

levodopa

24
Q

blocks AADC in periphery

A

carbidopa

25
Q

allows you to use a lower dose of levodopa and decreases side effect profile of levodopa

A

carbidopa

26
Q

levodopa is now only available in the US in formulation with

A

carbidopa

27
Q

levodopa + carbidopa =

A

sinemet

28
Q

other drugs used to increase dopaminergic activity [2]

(prevent LDOPA breakdown in either the brain or periphery)

A

MAO-B inhibitors
COMT inhibitors

29
Q

preferentially metabolizes dopamine

A

MAO-B

30
Q

MAO-B inhibitors [2]

A

selegeline
rassagaline

31
Q

COMT inhibitors [3]

A

tolcapone
entacapone
opicapone

(helps to protect LDOPA in the periphery)

32
Q

COMT inhibitor that only works in the periphery

A

entacapone

33
Q

absolute contraindications to drugs increasing dopamine bioavailability

A

abrupt discontinuation
closed-angle gluacoma (stimulate B receptors)
melanoma (precursor of melatonin)
breast feeding (inhibits prolactin secretion)

34
Q

drugs increasing dopamine bioavailability should be used with caution in patients with [2]

A

psychoses
open angle glaucoma

35
Q

dopamine agonists approved as monotherapy [3]

A

pramipexole
ropinerole
rotigotine

(all involve D3)

36
Q

add-on dopamine agonists with levodopa [2]

A

bromocriptine
apomorphine

37
Q

D2 agonist also used to treat hyperprolactinemia

A

bromocriptine

38
Q

anticholinergics [3]

A

benzotropine
procyclidine
trihexypheidyl

(secondary strategy)

39
Q

blocks actions of striatal cholinergic interneurons

can be used alone early in PD disease course, but not as effective as LDOPA

A

anticholinergics

40
Q

the anticholinergics used are all […] which gives better CNS penetration

A

tertiary amines

(over atropine, which has a lot of peripheral effects)

41
Q

mechanism is unknown
may release dopamine and/or have anticholinergic properties

A

amantadine

(secondary strategy)

42
Q

side effect is livedo reticularis

skin condition causing engorged capillaries and redness

A

amantadine

43
Q

antiviral that can be used as monotherapy or adjunct to LDOPA

A

amantadine

44
Q

late developing side effects of LDOPA [3]

A

abnormal movements
psychic symptoms (hallucinations, paranoia)
hypersexuality

45
Q

MOA of entacapone

A

blocks catabolism of L-DOPA in the periphery

(COMT inhibitor)

46
Q

inhibits AADC to block peripheral metabolism of levodopa

A

carbidopa

47
Q

D2/D3 agonist that can be used as monotherapy for PD [3]

A

pramipexole
ropinerole
rotigotine

all are D3

48
Q

is bromocriptine approved as monotherapy or add-on?

A

add on

49
Q

the psychic side effects that can occur after long-term used of levodopa are due to overactivation of the […] system

A

limbic and cortical

50
Q

used to block the catabolism of dopamine in patients treated with L-DOPA

A

MOA inhibitors

51
Q

[…] inhibitors are used to block the catabolism of dopamine in the brain and periphery in patients treated with LDOPA

A

COMT

52
Q

hepatotoxicity is a side effect of

A

tolcapone

53
Q

specifically indicated for treatment of Parkinson’s disease psychosis

A

Pimavanserin

BMB Test 3 (18 decks)

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