Alzheimer's and Parkinson's

Question 1

Dopamine and acetylcholine role in smooth movements

Answer 1

dopamine inhibits, acetylcholine excites

Question 2

neurotransmitters involved in parkinson’s

Answer 2

dopamine and acetylcholine

Question 3

Most effective drug for Parkinson’s

Answer 3

Levodopa/carbidopa=sinemet

Question 4

Levodopa mechanism of action

Answer 4

lifts dopamine levels by converting to dopamine in the brain

Question 5

carbidopa MOA

Answer 5

drives levodopa across the BBB by decreasing breakdown of levodopa in the periphery by DDC.

Question 6

how long does levodopa have an effect

Answer 6

about 5 years – often won’t use it in 60 year olds

Question 7

What enzyme breaks down levodopa, allowing only 2% of blood to reach the brain

Answer 7

DDC. When carbidopa blocks that enzyme, 10% of it goes across the BBB

Question 8

SE of levodopa/carbidopa

Answer 8

MOST COMMON: n/v (don’t take with high-protein meals), dyskenesia
Other systems: CV postural hypotension, dysrhythmias; NEURO psychosis 20%, anxiety, agitation, memory but don’t use 1st gen antipsychotic; GU darkened sweat and urine; activate malignant melanoma

Question 9

Most common SE of levodopa/carbidopa

Answer 9

n/v, dyskinesia

Question 10

Cardiovascular SE of Levodopa/Carbidopa

Answer 10

postural hypotension, dysrhythmias – sometimes need salt pills

Question 11

CNS effects of levodopa/carbidopa

Answer 11

psychosis (but don’t use a 1st gen antipsychotic), anxiety, agitation, memory issues

Question 12

Integumentary/excretion SE of levodopa/carbidopa

Answer 12

• darkened sweat and urine

- maybe activate malignant melanoma

Question 13

Acute loss of effect for levodopa/carbidopa

Answer 13

• wears off at end of the dosing interval

- minutes to hours where it stops working (avoid high protein meals)

Question 14

Dopamine agonist prototype

Answer 14

pramipexole (Mirapex)

Question 15

1st line therapy for mild to moderate symptoms and for younger patients who are more likely to handle side effects

Answer 15

dopamine agonists: pramipexole

younger patients – the babies get pushed in the pram

Question 16

weird side effect of pramipexole

Answer 16

pathological gambling and other compulsive self-rewarding behavior

Question 17

SE of monotherapy pramipexole

Answer 17

daytime sleepiness (sleep attack), insomnia, hallucinations, nausea, dizziness, constipation, weakness

Question 18

SE of levadopa + pramipexole

Answer 18

orthostatic hypotension, dyskinesia, double rate of hypotension

Question 19

what else is pramipexole used for

Answer 19

restless leg syndrome

Question 20

COMT inhibitor prototype

Answer 20

entacapone (comtan)

Question 21

Levodopa booster

Answer 21

COMT inhibitor – no direct therapeutic effects on their own

Question 22

SE of COMT inhibitors (entacapone)

Answer 22

increased levo SE, GI distress, yellow/orange discoloration of urine

Question 23

MAO-B inhibitors prototype

Answer 23

selegiline (Eldepryl)

Question 24

Why are MAO-B inhibitors used in parkinson’s

Answer 24

Reduce levodopa wearing-off effect, suppress destruction of dopamine and prolong the effects of levodopa

Question 25

SE of selegiline (MAO-B inhibitors)

Answer 25

insomnia, orthostatic hypotension, dizziness, GI symptoms

Question 26

Unexpected drug for parkinson’s

Answer 26

amantadine (antiviral)

Question 27

Why does an antiviral help with Parkinson’s

Answer 27

can help with dyskinesias caused by levodopa

Question 28

SE of amantadine for Parkinson’s

Answer 28

CNS, anticholinergic, benign livedo reticularis (mottled skin discoloration)

Question 29

anticholinergic prototype

Answer 29

benztropine (cogentin)

Question 30

who gets an anticholinergic for parkinson’s

Answer 30

younger patients – it’s on the BEERS list

Question 31

function of cholinesterase

Answer 31

breaks down acetylcholine

Question 32

MOA of cholinesterase inhibitors

Answer 32

Inhibits cholinesterase, making ACh available to neurons

Question 33

are cholinesterase inhibitors effective?

Answer 33

Ummm, statistically but not clinically. They also don’t bring back anything that’s already been lost.

Question 34

SE of cholinesterase inhibitors

Answer 34

pro-cholinergic: rest and digest, bronchoconstriction, n/d, bradycardia, fainting, falls

Question 35

Administration considerations for cholinesterase inhibitors

Answer 35

give at night, slowly titrate up

Question 36

NMDA receptor antagonists prototype

Answer 36

memantine (namenda)

Question 37

MOA for NMDA receptor antagonists (memantine)

Answer 37

allows calcium influx into neuron

Question 38

SE of memantine

Answer 38

related to toooooo much calcium entering: dizziness, headache, confusion, constipation (but very well tolerated)