Neurodegenerative and Movement Disorders Flashcards

1
Q

what are the 2 main purposes of pharmacotherapy of Parkinsons

A

increase dopaminergic activity
decrease cholinergic activity

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2
Q

dopamine doesn’t cross the BBB, however its precursor __ does

A

L-dopa

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3
Q

how is dopamine able to cross the BBB

A

the prodrug L-dopa crosses the BBB and is converted to dopamine by dopa decarboxylase

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4
Q

what is the effect of dopamine binding to D2 and D3 receptors in the CNS

A

opens K+channels

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5
Q

most of L-dopa is metabolized in the intestines by MAO and decarboxylation, however some is metabolized in the periphery (blood) by __ and __

A

COMT
decarboxylation

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6
Q

L-dopa is administered with __ which functions as a __

A

Carbidopa
peripheral decarboxylase inhibitor

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7
Q

what is the function of Carbidopa

A

inhibition of peripheral decarboxylase and its metabolism of L-dopa in GIT and blood, therefore increasing CNS bioavailability in the CNS

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8
Q

common side effects of L-dopa include …

A

nausea/vomiting
orthostatic hypotension
cardiac arrhythmia

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9
Q

what is the main adverse effect of L-dopa

A

dyskinesias

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10
Q

dyskinesias caused by L-dopa can be decreased by adding what drug

A

amantadine

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11
Q

wearing off reactions of L-dopa are related to

A

gradually, the duration of L-dopa effect is decreased

*related to timing

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12
Q

on-off phenomenon with L-dopa

A

sometimes patients response to L-dopa, sometimes they don’t

*fluctuation in clinical response

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13
Q

what is one of the main drug interactions of L-dopa

A

vitamin B6

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14
Q

how does vitamin B6 interact with L-dopa

A

increases dopa decarboxylase

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15
Q

what is the drug of choice for Parkinsons

A

L-dopa

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16
Q

if L-dopa is ineffective, what drug is used as a backup

A

dopamine receptor agonist

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17
Q

dopamine receptor agonists are used for ___ and __

A

response fluctuation
refractory to levodopa

18
Q

what is the main adverse effect of dopamine receptor agonists

A

pulmonary and retroperitoneal fibrosis

19
Q

Cabergoline is a dopamine receptor agonist that leads to what adverse effect

A

cardiac valvulopathy

20
Q

Pergolide is a dopamine receptor agonist that lead to what adverse effect

A

heart valve fibrosis
regurgitation

21
Q

what type of drug can be given to delay the need for L-dopa

A

non-ergot derivative dopamine receptor agonist

22
Q

what is the injectable dopamine agonist Apomorphine used for

A

advanced Parkinsons with intermittent off episodes

23
Q

what is given prior to injection of dopamine agonist Apomorphine

A

anti-emetic (Trimethobenzamide or Domeperidone)

24
Q

the injectable dopamine agonist Apomorphine is contradicted with use of what drugs

A

5-HT3 receptor blockers

*can lead to severe hypotension

25
Q

what is an adverse effect of the MAO-B inhibitor Selegiline

A

serotonin syndrome

26
Q

what is the function of Catechol-O-Methyltransferase (COMT)

A

inhibition of dopa decarboxylase so there will be a decrease in 3-OMD competing for the L-dopa transporter into the CNS

27
Q

what is the main use of COMT inhibitors

A

reduce the wearing off/on-off effects of L-dopa

28
Q

what is an adverse effect of the COMT inhibitor Tolcapone

A

fatal hepatotoxicity

29
Q

what type of drug is Tolcapone

A

COMT inhibitor

30
Q

what is the function of Amantadine in Parkinsons

A

enhances release of dopamine
blocks dopamine uptake

31
Q

what are 3 adverse effects of Amantadine

A

-livedo reticularis (bluing of skin+ankle edema)
-orthostatic hypotension
-Amantadine keratopathy (corneal edema)

32
Q

what is the function of central anticholinergics (muscarinic blockers) in Parkinsons

A

balance dopamine/acetylcholine activity

33
Q

what is the main use of anticholinergics for Parkinsons

A

drug induced Parkinsonism (mainly by antipsychotics)

34
Q

what is the most effective treatment for Parkinsons

A

L-dopa+Carbidopa

35
Q

what is the neurological cause of Huntingtons

A

degeneration of GABAnergic neurons in the neostriatum

36
Q

what is the mechanism of action of Tetrabenazine, a VMAT inhibitor used for Huntingtons

A

inhibitor of monoanime uptake and storage

37
Q

what is the neurological cause of Alzheimers

A

overstimulation of NMDA receptors

38
Q

therapy for Alzheimers include __ and __

A

cholinesterase inhibitors
NMDA antagonists

39
Q

what is the drug used for management of depression associated with Parkinsons

A

Rivastigmine

40
Q

what therapeutic use can be used for Tourette syndrome

A

Botulinism toxin for tics