Drugs For Parkinsons Disease (24) Flashcards

1
Q

Parkinsons disease affects

A

Dopamine producing neurons in the brain

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2
Q

Symptoms of Parkinson’s are caused by

A

An imbalance of dopamine and acetylcholine

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3
Q

Dopamine vs ACh in Parkinson’s

A

Dopamine: inhibitory

ACh: excitatory

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4
Q

Direct vs indirect drugs affecting the dopamine system

A

Direct: dopamine receptor agonists

Indirect: levodopa-carbidopa selegiline amantidine

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5
Q

Precursor to dopamine

A

Levodopa

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6
Q

MAOI prevents

A

DA metabolism

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7
Q

Anticholingeric agents example

A

Benztropine

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8
Q

BBB does not allow

A

Exoganeously supplied dopamine to enter, but it does allow levodopa

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9
Q

Levodopa is taken up by

A

Dopaminergic terminal and converted into dopamine and then released

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10
Q

Levodopa therapy is aimed at

A

Increasing dopamine release form surviving DA neurones

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11
Q

Levodopa therapy maintains function mobility for

A

Years
-prolongs quality of life and expectancy

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12
Q

How long does it take for full therapeutic response

A

Several months

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13
Q

Therapy for Parkinson’s does not

A

Cure or stop progression of disease

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14
Q

As PD progresses

A

It becomes more and more difficult to control symptoms with levodopa

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15
Q

Where is levodopa metabolized outside of CNS

A

GI and liver

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16
Q

Combination therapy with levodopa therapy

A

Carbidopa

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17
Q

Why is carbidopa given if it Cant cross the BBB?

A

Prevents levodopa breakdown in the periphery

18
Q

Levodopa can also be metabolized by COMT, how does one stop this

A

Use COMT inhibitors

19
Q

Example of COMT inhibitors

A

Entacapone

20
Q

Entacapone

A

Inhibits COMT
-more levodopa available to enter brain
-used to reduce on-off phenomenon

21
Q

Wearing off effect of levodopa therapy

A

Gradual loss
-subtherapeutic levels near end of dosing interval

22
Q

On off phenomenon

A

Abrupt loss of drug effect even at high drug levels
-lasts from minutes to hours
-unknown reason

23
Q

AE of levodopa

A

-nausea and vomiting
-dyskinesia
-CV
-psychosis

24
Q

Dyskinesia as AE of levodopa

A

Involuntary muscle movements
-oral, facial muscle, writhering and flinging movement of arms and legs

25
Q

Dopaminergic therapy

A

Prevents DA metabolism
-MAO B inhibitor
-inhibiting DA breakdown in neurones

26
Q

MAO-B inhibitor

A

Selegiline

27
Q

Amantadine

A

Promotes DA release from nerve endings

28
Q

selegiline

A

Irreversible MAOI that selectively inhibits MAO-B

29
Q

Selegiline is a

A

MAO-B inhibitor

30
Q

Selegiline causes an increase

A

In the levels of dopaminergic stimulation in the CNS

31
Q

Selegiline indications

A

Milder symptoms or earlier

32
Q

Selegiline has a ___ agent and it is helpful

A

Adjunctive agent, helping response to levodopa flucting on-off

33
Q

AE of Selegiline

A

Mild: nausea, abdominal pain, dry mouth, lightheaded mess, dizziness, insomnia,

34
Q

Indirect dopaminergic therapy: amantadine

A

Release of dopamine from the storage sites at the end of nerve cells that are still intact

35
Q

Indirect dopaminergic therapy: amantadine also blocks

A

The reputable of dopamine into the nerve endings

36
Q

Indirect dopaminergic therapy: amantadine does not

A

Stimulate dopamine receptors directly

37
Q

Indirect dopaminergic therapy: amantadine may help with

A

Levodopa induced dyskinesias

38
Q

Direct acting dopaminergic therapy

A

DA receptor agonists
-directly stimulate dopamine receptors

39
Q

What is the first line treatment for PD in younger patients, mild/moderate symptoms, reduce wearing off effect, less effective than levodopa

A

Dopaminergic therapy

40
Q

Anticholingeric drugs do not relieve

A

Bradykinesia