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Pharm > Parkinson Meds > Flashcards

Parkinson Meds Flashcards

1
Q

Characteristic features of Parkinson

A

Tremor
Rigidity
Badykinesia
Postural instability

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2
Q

What happens as a result of complications of Parkinson

A

Death

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3
Q

What is the pathophys of Parkinson

A

Loss of dopaminergic neurons in substantia nigra

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4
Q

What percent of pts develop motor complications of Parkinson

A

50-90% of pts on levodopa >5 years develop motor complications

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5
Q

How to deal with wearing off of levodopa effect

A

Initially: treat by more frequent dosing
Later: add dopamine agonist

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6
Q

How to deal w/ on-off effect of levodopa

A

Treat w/ rescue apomorphine or adjust dose/frequency of dosing

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7
Q

Describe the physical disability associated with Parkinson

A

Progressive
Unavoidable
Highly individualized***

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8
Q

Levoadopa (LD)

A

Mainstay of tx since the 1960s

DOES cross blood brain barrier (BBB)

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9
Q

Does LD have peripheral effects?

A

Yes

Ex: dyskinesias, NV, etc.

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10
Q

What do you always administer LD with?

A

Peripheral dopa decarboxylase (DDC) inhibitor

Ex: Carbidopa

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11
Q

What does LD compete w/ for absorption?

A

Other amino acids

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12
Q

GI upset with LD?

A

Yes, but minimized

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13
Q

How is LD best absorbed

A

W/ low protein meals

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14
Q

Peripheral dopa decarboxylase inhibitor agent

A

Carbidopa

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15
Q

COMT-Inhibitor Agents

A

Entacapone
Tolcapone
**good peripherally and centrally

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16
Q

MAO-B Inhibitor Agents

A

Selegiline

Rasagline

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17
Q

Carbidopa

A

Available alone or in combo w/ Levodopa

Sinemet

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18
Q

Carbidopa dosing

A

75-100 mg CD/d usually needed to inhibit peripheral DDC

*Usually start w/ IR product of 25/100 mg Sinemet TID

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19
Q

What dose of Levodopa do most pts respond to?

A

750-1000 mg of LD

After 8 Tabs/day of 25/100 mg Sinemet -> switch to to 1 tab of 25/250 TID

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20
Q

Carbidopa/Levodopa (SInemet) forms

A 
Immediate release (generic)
Sustained release (generic)
Orally disintegrating (generic)
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21
Q

Carbidopa form

A

Brand = Lodosyn

Allows greater individualization for pts w/ advanced Parkinson

22
Q

Entacapone dosing and cost

A

Generic
Available as 200 mg tabs or combo w/ Sinemet
Generic is significantly less expensive than brand Tolcapone

23
Q

What is the combo of Entacapone and Sinemet called?

A

Stalevo

24
Q

Tolcapone dosing and AE

A

Dosed as single drug TID
Associated w/ fatal cases of acute liver failure
So limited clinical use

25
Q

MAO-B Inhibitors for Parkinson

A 
Prolong dopamine agonist affects
Modest effects
Adjunct therapy in most cases
Minimized tyramine intake
Dont use SSRIs at the same time (Serotonin syndrome)
26
Q

What are selegiline advantages and what is it less effective at?

A

Early use may delay need for LD by 9 months
May improve wearing off effects
Less effective in improving on off effects

27
Q

Selegiline dosing

A

Generic (least expensive): BID
Brand Zelapar: daily-decreased 1st pass effect
Brand Emsam: only FDA approved for depression

28
Q

Rasagiline inhibition strenght and cost

A

More potent inhibition of MAO-B than selegiline

Brand and generic are expensive

29
Q

What is safinamide useful for treating and how is it used?

A

Use adjunct to levadopa/carbidopa

Useful for treatment of off episodes

30
Q

Adverse effects off Safinamide

A

severe HTN
Hypersexual behavior
Retinal degeneration

31
Q

Dopamine Agonists

A

Cross BBB and stimulate the dopamine receptors
Can be use as monotherapy early in disease, or adjunct later on
ADLs improve on these 30%
Monotherapy more effective with younger pts
Early use my postpone use of levodopa

32
Q

Dopamine Agonist Agents

A 
Bromocriptine
Pramipexole
Ropinirole
Apomorphine
Rotigotine
33
Q

Bromocriptine

A

1st generation ergot-derivative (wheat)
Rarely used
Adverse effects: pericardial and cardiac valve fibrosis

34
Q

Pramipexole

A

2nd generation
Fewer dyskinesias
Fewer wearing off effects
Fewer motor complications

35
Q

Ropinirole

A

Equally efficacious per indirect comparisons

Dosing: generic = TID; brand = daily

36
Q

Apomorphine

A

Injectable but expensive

Rescue therapy of hypomoblility or off episodes

37
Q

What drug is contraindicated for apomorphine

A 
Serotonin RAs (ondasetron-Zofran)
Can cause severe hypotension and syncope
38
Q

Dosing of IV apomorphine

A

SC 2-6 mg -> Higher than book recommends

IV administration is contraindicated

39
Q

Rotigotine

A

Only one available as transdermal patch

very expensive

40
Q

Anticholinergics

A

Mainstay of tx until 1960s

Reserved for resting tremor early in disease

41
Q

Side effects of anticholinergics

A 
Constipation
Dry mouth
Blurred vision
Confusion
Urinary retention
42
Q

Benzotropin

A

Anticholinergic
May inhibit reuptake of dopamine
Divided BID or single dose at hs
IV/IM injection solution

43
Q

Trihexyphenidyl

A

Anticholinergic
Divided 3-4x/day
Oral elixir

44
Q

Amatadine

A

Primarily antiviral agent found to have anti-PD activity
Previously used as monotherapy
Now and add-on for levodopa-induced dyskinesias

45
Q

Pramipexole dosing

A

Generic TID

Brand TID or daily

46
Q

How is pramipexole eliminated?

A

Renally

Its the only dopamine agonist that is!

47
Q

What is the recommended taper for pramipexole when d/cing it?

A

None!

48
Q

Anticholinergic agents

A

Benzotropin

Trihexyphenidyl

49
Q

Ropinirole taper

A

Taper over 7 days if D/Cing

50
Q

How is ropinirole metabolized and if there is an issue w/ this organ is there a dose adjustment?

A

Hepatically metabolized

No dose adjustment

51
Q

Apomorphine SE

A

Severe emesis

Will need an antiemetic

Pharm (32 decks)

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