Drugs affecting Neurologic Functioning: Part 1

Question 1

Parkinson’s Disease is a ___________ disease

Answer 1

Neurodegenerative

Question 2

Parkinson’s Disease is a disorder of the _____ system

Answer 2

Extrapyramidal (EPS)

Question 3

Dopamine is produced in the _______ _____ and supplied to the ____ of the EPS

Answer 3

Substantia nigra

Striatum

Question 4

EPS is the part of the brain responsible for…

Answer 4

Movement

Question 5

What is the issue with Parkinson’s?

Answer 5

There is not enough dopamine

Question 6

Balance between Acth and dopamine

Answer 6

70-80% of neurons in the substance nigra are destroyed before symptoms are evident
Imbalance between dopamine (inhibitory neurotransmitter) and acetylcholine (excitatory neurotransmitter)

Question 7

Main two clinical symptoms of Parkinson’s Disease

Answer 7

Dyskinesias

Psychologic disturbances

Question 8

Dyskinesias

Answer 8

Tremor at rest
Rigidity
Postural instability
Bradykinesia

Question 9

Psychologic disturbances (Parkinson’s)

Answer 9

Dementia
Depression
Impaired memory

Question 10

Is there currently a treatment for Parkinson’s that reverses nerve degeneration and prevents further degeneration?

Answer 10

NO

Question 11

Current treatment for Parkinson’s…..

Answer 11

Aimed at improving patients ability to carry out ADLs, only symptomatic

Question 12

Drug classifications for Parkinson’s

Answer 12

Dopaminergic agents
Dopamine agonists
MAO-B inhibitors
COMT Inhibitors 
Anticholinergic Agents

Question 13

Levodopa (Dopar)

Answer 13

Dopamine replacement

Question 14

Levodopa (Dopar) effects

Answer 14

Converts to dopamine in the brain

Promotes synthesis of dopamine in the striatum

Question 15

Most patients experience ____ reduction in symptom severity with Levodopa

Answer 15

50%

Question 16

How long does it take for Levodopa to decrease symptoms?

Answer 16

Several months

Question 17

Why is Levodopa given in an inactive form?

Answer 17

It would cause renal perfusion and excitation of the heart

Question 18

Over time, Levodopa…

Answer 18

Loses effectiveness

Question 19

“On-off” phenomenon with Levodopa

Answer 19

Any time during dosing interval
“Off” times may last minutes to hours
“Off” periods increase in intensity & frequency

Question 20

Administered alone, what happens with Levodopa?

Answer 20

98% is metabolized in the intestines (only 2% reaches the brain)

Question 21

What do we administer with Levodopa and why?

Answer 21

Carbidopa - 10% of Levodopa reaches the brain

Question 22

Levodopa + Carbidopa =

Answer 22

Sinemet

Question 23

Adverse effects of Levodopa

Answer 23

N&V
Dyskinesias
Cardiovascular
Psychosis 
Severe depression with suicidal ideation

Question 24

Adverse effects of Levodopa: Dyskinesias

Answer 24

Minor:
-Head bobbing
-Tics 
-Grimacing
Disabling: 
-Ballismus (arm swinging) 
-Choreoathetosis (constant shoulder movement)

Question 25

Adverse effects of Levodopa: Cardiovascular

Answer 25

Postural hypotension

Question 26

Levodopa drug interactions

Answer 26

Conventional antipsychotics MAO inhibitors Anticholinergic drugs (increase toxicity)

Question 27

Levodopa food interactions

Answer 27

Meals with high protein can reduce therapeutic responses (amino acids compete with the drug for absorption)

Question 28

Dopamine agonists are for...

Answer 28

Mild to moderate symptoms - Drug of first choice

Question 29

How do dopamine agonists work?

Answer 29

Direct activation of dopamine receptors in the striatum

Question 30

Compatred to Levodopa, dopamine agonists are ____ effective

Answer 30

Less

Question 31

Compared to Levodopa, dopamine agonists have a ___ incidence of response failures

Answer 31

Lower (Less on-off & losing effectiveness over time)

Question 32

Compared to Levodopa, dopamine agonists are _____ likely to cause disabling dyskinesias

Answer 32

Less

Question 33

Dopamine agonists meds

Answer 33

``` Pramipexole (Mirapex) Ropinirole (Requip) Amantadine hydrochloride (Symmetrel) Bromocriptine (Parlodel) Apomorphine (Apokyn) Pergolide (Permax) ```

Question 34

Pramipexole (Mirapex) binds selectively to...

Answer 34

D2 and D3 receptors

Question 35

The binding of Pramipexole (Mirapex) to D2 and D3 receptors causes..

Answer 35

Significant improvement in motor skills early in disease process

Question 36

Use of Pramipexole (Mirapex) may allow for...

Answer 36

Reduction of Levodopa later in disease process

Question 37

Early stage Parkinson's Drug

Answer 37

Mirapex used alone

Question 38

Advanced Parkinson's drug

Answer 38

Mirapex + Levodopa

Question 39

Adverse effects of Pramipexole (Mirapex)

Answer 39

``` Sleep attacks (take away ability to drive) Nausea Dizziness Daytime somnolence Insomnia ~Hallucinations ~ ```