EXAM #3: ANTIPARKINSON'S DRUGS Flashcards Preview

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Flashcards in EXAM #3: ANTIPARKINSON'S DRUGS Deck (38):
1

What is the aggregate found in PD?

Intracytoplasmic aggregates of alpha-synuclein

2

When does PD typically onset?

50's and 60's

3

What is PD characterized by from a pathologic standpoint?

Progressive loss of dopaminergic neurons in the basal ganglia

4

What are the cardinal symptoms of PD?

1) Bradykinesia
2) Muscular rigidity
3) Resting tremor
4) Postural instability

5

Specifically what dopaminergic neurons are lost in PD?

Dopaminergic neurons in the SN that project into the Striatum

6

What is the definition of the Striatum i.e. what are the parts of the Basal Ganglia that compose the Striatum?

Putamen
Caudate Nucleus

7

Describe the pathophysiology of PD.

- Alpha-synuclein accumulates into Lewy Bodies
- Lewy body formation generates free radicals

8

What is the specific part of the Basal Ganglia that is degenerative in PD?

Substantia Nigra Pars Compacta

9

What is the outcome of SN pars compacta degeneration in PD?

- OVERACTIVITY of the indirect pathway leading to:
1) Inhibition of the VA/L thalamus
2) Reduced excitatory input to the cortex
3) Diminished execution of movement

10

What is the role of ACh in PD?

- Imbalance of DA and ACh in PD
- Thus, there is too much ACh in PD

11

What is the most common drug used to treat PD?

L-DOPA

12

Why is L-DOPA given instead of DA?

DA cannot cross the BBB

13

What enzyme converts L-DOPA into DA?

Dopa carboxylase

14

What symptoms does L-DOPA specifically improve in PD?

Bradykinesia
Rigidity

15

What drug is L-DOPA typically co-administered with?

Carbidopa

16

What is the MOA of Carbidopa?

Carbidopa is an inhibitor of Dopa Decarboxylase in the periphery

17

What is the effect of inhibiting Dopa Decarboxylase?

Inhibits the premature breakdown of L-DOPA in the periphery

18

What are the adverse effects associated with L-DOPA adminstration?

1) Dyskinesias
2) Response fluctuations
- Wearing off reactions
- On-off phenomenon
3) GI disturbance
4) Postural hypotenion/ tachycardia
5) Behavioral disturbances

19

What can be done to prevent the response fluctuations of L-DOPA?

Drug holidays i.e. periodic cessation

20

What is the drug interaction of L-DOPA with Pyridoxine?

This is Vitamin B6, a DOPA decarboxylase cofactor that enhances L-DOPA metabolism in the periphery

21

What is the drug interaction of L-DOPA with antipsychotics?

DA receptor blockade limits efficacy

22

What is the drug interaction of L-DOPA with MAO-inhibitors?

Hypertensive response (NE)

23

List the three DA receptor agonists.

Pramipexole
Ropinirole
Apomorphine

24

What is the clinical use of Apomorphine?

Given subcutaneously for rescue of L-DOPA induced dyskinesias

25

What is the MOA of the DA receptor agonists

D2 receptors agonsit

26

What are the two MAO-B inhibitors used to treat PD?

Rasagiline
Selegiline

27

What is the MOA of the MAO-B inhibitors?

Decreases breakdown of dopamine

28

What is the major behavioral issue seen with the administration of DA agonsits?

Impaired impulse control leading to:
- Compuslive gambling
- Shopping
- Betting
- Sex

29

What is the dose of MAO-B inhibitor that is needed to have a therapeutic effect in PD?

Low

30

What are the two drugs used as COMT inhibitors in the treatment of PD?

Entacapone
Tolcapone

31

What is the difference between Entacapone and Tolcapone?

Entacapone= peripheral COMT inhibitor ONLY

Tolcapone= central and peripheral COMT inhibition

32

What is the MOA of COMT inhibitors?

Block peripheral breakdown of L-DOPA--used as an adjunct

33

What is the MOA of Amantadine?

Increased DA release

34

What class of drug is Amantadine?

Anti-viral

35

What is the major adverse effect associated with Amantadine administration?

Livedo Reticularis

36

What are the anticholinergic agents used to treat PD?

Benztropine
Trihexyphenidyl

37

What is the MOA of Benztropine and Trihexyphenidyl?

Muscarinic antagonists

38

What is the general picture of muscarininc antagonist overdose?

"Dry-picture"

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