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Kol- Pharm 323 Spring > Parkinsons > Flashcards

Parkinsons Flashcards

1
Q

Dopamine: inhib or excitatory

Parkinsons = too little or too much dopamine?

A

Inhibitory transmitter

Parkinsons = too little dopamine

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2
Q

Acetylcholine: inhib or excitatory ?

Parkinsons= too little or too much?

A

Acetylcholine (ACh)= Excitatory transmitter

Parkinsons = too much ACh

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3
Q

2 main categories of drugs to treat Parkinsons

A
  1. dopaminergic agents

2. Anticholinergic

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4
Q

5 types of dopaminergic agents

A

~Dopamine replacement: Promotes dopamine synthesis
(Levodopa )

~Dopamine agonists: Stimulate dopamine receptors directly
(pramipexole)

~COMT inhibitors: Enhance effects of levodopa by blocking its degradation
(entacapone)

~MAO-B inhibitors: Inhibit dopamine breakdown
(selegiline)

~Antiviral: Promotes dopamine release
(amantadine)

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5
Q

class promotes dopamine SYNTHESIS

A

~Dopamine replacement: Levodopa

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6
Q

class STIMULATES dopamine RECEPTORS directly

A

Dopamine agonists:(pramipexole)

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7
Q

class enhances effects of levodopa by BLOCKING its DEGRADATION

A

~COMT inhibitor: entacapone

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8
Q

Class INHIBITs dopamine BREAKDOWN

A

MAO-B inihibitor : selegiline

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9
Q

class promotes dopamine RELEASE

A

antiviral: amantadine

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10
Q

most effective drug for parkinsons disease

A

Levodopa/Carbidopa

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11
Q

How does Levodopa/Carbidopa fxn? What enzyme is at play here?

A

FXN:levodopa converts to dopamine in the brain (dopamine replacement)

  • leovdopa crosses BBB to convert to dopamine
  • Levodopa in peripheral circulation comes into contact with enzyme DDC
  • Enzyme DDC breaks down levodopa so only small portion (2%) can cross BBB
  • Add in CARBIDOPA to decrease the breakdown of levodopa in the periphery by DDC and increase the amount (10%) that crosses the BBB.
  • carbidopa = no other effect
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12
Q

Benefits of having Levodopa with Carbidopa

A
  • ->use less drug

- -> less side effect from levodopa

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13
Q

Levodopa/Carbidopa onset and duration

A
  • Delayed full effect (months)
  • Effect doesn’t last (<5 years)
  • –>reserved, don’t use in younger patients
  • –> no drug holiday anymore!
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14
Q

do we give young people Levodopa/Carbidopa

A

try not to

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15
Q

7 side effects of Levodopa/Carbidopa

A
  1. *Nausea/Vomiting: give with food initially. Avoid high-protein meals. start low dose and increase
  2. Dyskinesia: ie: dystonic movements
  3. Cardiovascular
    - *Postural hypotension: increase salt and water to prevent
    - Dysrhythmias
  4. Psychosis
    - No 1st generation antipsychotic meds w/ parkinsons b/c block dopamine receptors and make PD worse
    - use 2nd generation antipsychotic
  5. CNS Effects
    - Anxiety, agitation, memory issues
  6. Darkened sweat and urine
  7. Can activate malignant melanoma
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16
Q

2 aspects of “acute loss effect” of Levodopa/Carbidopa

A

“Wearing Off”
• sxs start returning at the end of the dosing interval
-Dosing must be on time

“On-Off” 
• Abrupt loss of effect
-Can occur at anytime
-Lasts from minutes to hours 
-Avoid high protein meals
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17
Q

minimize wearing off of levodopa/carbidopa by

A
  • Shorten interval
  • Give a drug to prolong half life
  • Give direct acting dopamine agonist
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18
Q

prototype for dopamine agonist

A

pramipexole (Mirapex)

19
Q

1st line therapy for mild to moderate sxs of parkinsons

A

pramipexole (Mirapex) (Dopamine AGONIST)

20
Q

how does pramipexole (Mirapex) fxn?

A

Direct activation of dopamine receptors in striatum

21
Q

indication for use of pramipexole (Mirapex)

A
  • Used in younger patients who are more likely to handle side effects
  • Also used in Restless legs syndrome
22
Q

onset of pramipexole (Mirapex)

A

weeks (quicker than carvidopa/levodopa)

23
Q

Adverse effect of pramipexole (Mirapex) as monotherpay vs combined with levodopa

A

-Monotherapy-
nausea, dizziness, *Sleep attack: daytime somnolence, insomnia, constipation, weakness, and *hallucinations

  • Combined with levodopa–
  • orthostatic hypotension & dyskinesia and double rate of hallucinations
24
Q

really unique side effect of pathologic gambling and other compulsive self-rewarding behaviors
with which drug?

A

pramipexole (Mirapex) (Dopamine AGONIST)

25
Q

prototype for COMT inhibitor?

A

entacapone (Comtan)

26
Q

how does entacapone (Comtan) fxn?

A
  • Increases the amount of levodopa that enters the brain
  • ->Inhibit the breakdown of levodopa in the periphery
  • When DDC is blocked by carbidopa body starts trying to break down levodopa w/ another enzyme COMT
  • No direct therapeutic effects of their own –> prevents breakdown of levodopa/carbadopa
  • ->Levodopa “Boosters”
27
Q

adverse effects of entacapone (Comtan)

A
  • Increased levodopa levels—dyskinesias; orthostatic hypotension, nausea, hallucinations, sleep disturbances, impulse control
  • GI distress; yellow/orange discoloration of urine
28
Q

prototype for MAO-B inhibitors

A

selegiline (Eldepryl)

29
Q

how does selegiline (Eldepryl) fxn?

A

Can suppress destruction of dopamine derived from levodopa and prolong the effects of levodopa

  • Combination with levodopa
  • can reduce the wearing-off effect
30
Q

duration of selegiline (Eldepryl)

A

1-2 weeks

31
Q

adverse effects of selegiline (Eldepryl)

A

Insomnia (give in am)
Orthostatic hypotension
Dizziness
GI symptoms

32
Q

prototype for antiviral parkinsons med?

A

amantadine

33
Q

what does amantadine due to dopamine?

A

promotes dopamine release in brain

34
Q

indication for using amantadine

A

used for dyskinesias caused by levodopa

35
Q

onset/duration of amantadine

A

works w/in 2-3 days, lasts several months

36
Q

adverse effects of amantadine

A
  • CNS (anxiety)
  • Anticholinergic
  • Livedo reticularis (mottled discoloration of skin)

“a man has a tic on his dick”

37
Q

anticholinergic prototype for parkinsons drugs?

A

benztropine (Cogentin)

38
Q

how does benztropine (Cogentin)

fxn?

A

Block muscarinic receptors

-Centrally acting

39
Q

indication for using benztropine?

A

Reduce tremors and rigidity

40
Q

is benztropine a first or 2nd line therapy for parkinsons?

A

2nd

41
Q

what patient population do we give benztropine to?

A

younger

42
Q

adverse effects for benztropine?

A

anticholingeric

agitation/hallucination in elderly

43
Q

how do we treat orthostatic hypotension with levodopa/carbidopa

A

give salt!

44
Q

how do we prevent “acute loss effect” of Levodopa/Carbidopa?

A

avoid high protein meals, give meds on time

Kol- Pharm 323 Spring (41 decks)

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