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Flashcards in Parkinson Meds Deck (51):
1

Characteristic features of Parkinson

Tremor
Rigidity
Badykinesia
Postural instability

2

What happens as a result of complications of Parkinson

Death

3

What is the pathophys of Parkinson

Loss of dopaminergic neurons in substantia nigra

4

What percent of pts develop motor complications of Parkinson

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

5

How to deal with wearing off of levodopa effect

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

6

How to deal w/ on-off effect of levodopa

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

7

Describe the physical disability associated with Parkinson

Progressive
Unavoidable
Highly individualized***

8

Levoadopa (LD)

Mainstay of tx since the 1960s
DOES cross blood brain barrier (BBB)

9

Does LD have peripheral effects?

Yes
Ex: dyskinesias, NV, etc.

10

What do you always administer LD with?

Peripheral dopa decarboxylase (DDC) inhibitor
Ex: Carbidopa

11

What does LD compete w/ for absorption?

Other amino acids

12

GI upset with LD?

Yes, but minimized

13

How is LD best absorbed

W/ low protein meals

14

Peripheral dopa decarboxylase inhibitor agent

Carbidopa

15

COMT-Inhibitor Agents

Entacapone
Tolcapone
**good peripherally and centrally

16

MAO-B Inhibitor Agents

Selegiline
Rasagline

17

Carbidopa

Available alone or in combo w/ Levodopa
(Sinemet)

18

Carbidopa dosing

75-100 mg CD/d usually needed to inhibit peripheral DDC
*Usually start w/ IR product of 25/100 mg Sinemet TID

19

What dose of Levodopa do most pts respond to?

750-1000 mg of LD
After 8 Tabs/day of 25/100 mg Sinemet -> switch to to 1 tab of 25/250 TID

20

Carbidopa/Levodopa (SInemet) forms

Immediate release (generic)
Sustained release (generic)
Orally disintegrating (generic)

21

Carbidopa form

Brand = Lodosyn
Allows greater individualization for pts w/ advanced Parkinson

22

Entacapone dosing and cost

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

23

What is the combo of Entacapone and Sinemet called?

Stalevo

24

Tolcapone dosing and AE

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

25

MAO-B Inhibitors for Parkinson

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

26

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

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

27

Selegiline dosing

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

28

Rasagiline inhibition strenght and cost

More potent inhibition of MAO-B than selegiline
Brand and generic are expensive

29

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

Use adjunct to levadopa/carbidopa
Useful for treatment of off episodes

30

Adverse effects off Safinamide

severe HTN
Hypersexual behavior
Retinal degeneration

31

Dopamine Agonists

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

Dopamine Agonist Agents

Bromocriptine
Pramipexole
Ropinirole
Apomorphine
Rotigotine

33

Bromocriptine

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

34

Pramipexole

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

35

Ropinirole

Equally efficacious per indirect comparisons
Dosing: generic = TID; brand = daily

36

Apomorphine

Injectable but expensive
Rescue therapy of hypomoblility or off episodes

37

What drug is contraindicated for apomorphine

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

38

Dosing of IV apomorphine

SC 2-6 mg -> Higher than book recommends
IV administration is contraindicated

39

Rotigotine

Only one available as transdermal patch
very expensive

40

Anticholinergics

Mainstay of tx until 1960s
Reserved for resting tremor early in disease

41

Side effects of anticholinergics

Constipation
Dry mouth
Blurred vision
Confusion
Urinary retention

42

Benzotropin

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

43

Trihexyphenidyl

Anticholinergic
Divided 3-4x/day
Oral elixir

44

Amatadine

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

45

Pramipexole dosing

Generic TID
Brand TID or daily

46

How is pramipexole eliminated?

Renally
Its the only dopamine agonist that is!

47

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

None!

48

Anticholinergic agents

Benzotropin
Trihexyphenidyl

49

Ropinirole taper

Taper over 7 days if D/Cing

50

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

Hepatically metabolized
No dose adjustment

51

Apomorphine SE

Severe emesis
Will need an antiemetic