UNIT 2 PD DRUGS

Question 1

What are the two major categories of PD drugs?

Answer 1

1. Dopamine agents
2. Anticholinergic agents

Question 2

What is the MOA for dopamine agents?

Answer 2

1. Promote activation of dopamine receptors

Question 3

What is the MOA of anticholinergic agents?

Answer 3

1. Prevent activation of cholinergic rectors

Question 4

How is Levodopa absorbed?

Answer 4

Orally administered and rapidly absorbed from small intestine

Question 5

What is the most important patient teaching for a patient taking levodopa?

Answer 5

1. Food delays absorption esp. protein
2. High-protein foods reduce therapeutic effects
3. Teach patients not to eat protein at the same time as medication

Question 6

What is important to know about neutral amino acids and levodopa?

Answer 6

1. Neutral amino acids compete w/levodopa for intestinal absorption and for transport across the blood brain barrier

Question 7

What is the MOA of Levodopa/carbidopa (Sinemet)?

Answer 7

1. Levodopa is converted into dopamine in the CNS. Carbidopa prevents peripheral destruction of levodopa.

Question 8

What are adverse effects of Levodopa/Carbidopa?

Answer 8

1. N/V
2. Dyskinesias
3. Postural hypotension
4. Dysrhythmias
5. Psychosis
6. Impulse control
7. darkened sweat and urine loss

Question 9

Due to the “on and off” effect of PD drugs what is important to monitor?

Answer 9

Blood levels

Question 10

What do we need to know about dopamine agonists?

Answer 10

1. 1st drug of choice for mild to moderate symptoms

Question 11

What is the MOA of dopamine agonists?

Answer 11

1. direct activation of dopamine receptors
2. Not dependent on enzymatic conversion to be active
3. Does not compete w/dietary proteins

Question 12

Are dopamine agonists more or less effective than levodopa?

Answer 12

Less

Question 13

What should we know about the Dopamine agonists Pramipexole (Mirapex)?

Answer 13

1. Used alone in EARLY PD and w/levodopa in advanced PD
2. Max benefits take several weeks

Question 14

What are adverse effects of the Dopamine agonist Pramipexole (mirapex)

Answer 14

Monotherapy:
1. Sleep attacks***
2. Nausea
3. Dizziness
4. Daytime somnolence
5. Insomnia
6. constipation
7. Weakness
8. Hallucinations

Combined Therapy:
1. orthostatic hypotension
2. Dyskinesia
3. Increased hullucinations

Question 15

What is a rare side effect of the dopamine agonist pramipexole (mirapex)

Answer 15

If pathologic gambling and other compulsive self-rewarding behaviors

Question 16

What are some anticholinergic drugs?

Answer 16

1. Trinexlphendyl
2. Benziropine

Question 17

What is the MOA of anticholinergic drugs?

Answer 17

1. Blocks muscarinic receptors in stratum. Decreases ach. activity

Question 18

What are some adverse effects of anticholinergic drugs?

Answer 18

1. Dry mouth
2. Urinary retention
3. Tachycardia
4. Blurred vision
5. Constipation
6. Photophobia
7. Confusion
8. Hallucinations

Question 19

Never do what with PD drugs?

Answer 19

Stop taking abruptly

Question 20

What is the MOA of COMT inhibitors?

Answer 20

Inhibit metabolism of levodopa in the periphery. NO direct theraputic effects on their own.

Question 21

What are two examples of COMT inhibitors?

Answer 21

Entracapone (comtan)
Tolcapone (tasmar)

Question 22

What should we know about COMT inhibitor Entacapone (comtan)

Answer 22

Indicated for use with levodopa

Question 23

What is the MOA of Entacapone (comtan)? COMT inhibitors

Answer 23

1. Inhibits breakdown of levadopa in the periphery

Question 24

What are some adverse effects of entacapone (comtan)? COMT inhibitors

Answer 24

1. Dyskinesia
2. Orthostatic hypotension
3. N/V/D
4. hallucinations
5. Sleep disturbances
6. impulse control disorders
7. Yellow and orange discoloration of urine

Question 25

What should we know about tolcapone (tasmar) COMT inhibitor?

Answer 25

1. Used only in conjunction with levodopa 2. Only used if safer agents are ineffective or inappropriate

Question 26

What are some adverse effects of tolcapone (tasmar) COMT inhibitors?

Answer 26

1. Liver failure 2. Dyskinesia 3. Orthostatic hypotension 4. Nausea 5. Hallucination 6. sleep disturbance 7. Yellow and orange discoloration of urine

Question 27

What should we know about MOA-B inhibitors?

Answer 27

1. Considered 1st line drugs for PD 2. Benefits are modest 3. Combination w/levodopa can reduce the wearing off effect

Question 28

What are the two MOA-b inhibitors?

Answer 28

1. Selegline 2. Rasagline

Question 29

What is the MOA of selegline (eldepryl) a MOA-b inhibitor?

Answer 29

1. inhibits breakdown of dopamine

Question 30

What are adverse effects of the MOA-b inhibitor Selegline (eldpryl)?

Answer 30

1. Insomnia 2. Dry mouth 3. Orthostatic hypotension 4. Dizziness 5. Hypertension crisis 6. GI symptoms

Question 31

What should we know about Rasagline (azilect)? MOA-b inhibitors

Answer 31

1. Approved for initial therapy and for combined use with levodopa 2. Benefits derived from preserving dopamine in the brain 3. Avoid tyramine

Question 32

What are some adverse effects of rasagline (azilect) MOA-b inhibitor?

Answer 32

1. orthostatic hypotension 2. insomnia 3. irritation of buccal muscosa 4. hypertensive crisis

Question 33

What are other agents used to treat PD?

Answer 33

1. Antihistamine w/anticholinergic or b-adrenergic blockers are used to manage tremors 2. Antiviral agent- amantadine 3. Apomorphine for hypomobility