Pharm: Movement Disorders - Kruse

Question 1

apomorphine

Answer 1

DA agonist

Question 2

bromocriptine

Answer 2

DA agonist

Question 3

pramipexole

Answer 3

DA agonist

Question 4

ropinirole

Answer 4

DA agonist

Question 5

rasagiline

Answer 5

MAOI

Question 6

selegiline

Answer 6

MAOI

Question 7

safinamide

Answer 7

MAOI

Question 8

entacapone

Answer 8

catehol-O-methyltransferase inhibitor

Question 9

tolcapone

Answer 9

catechol-O-methyltransferase inhibitor

Question 10

benztropine

Answer 10

anticholinergic

Question 11

biperiden

Answer 11

anticholinergic

Question 12

orphenadrine

Answer 12

anticholinergic

Question 13

procyclidine

Answer 13

anticholinergic

Question 14

trihexyphenidyl

Answer 14

anticholiergic

Question 15

riluzole

Answer 15

misc agent

Question 16

reserpine, tetrabenazine

Answer 16

misc agents

Question 17

what med agents can be used for pts with PD?

Answer 17

DA agonists and/or anticholinergics

Question 18

immediate metabolic precursor to DA, 1-3 hr half life

• approved for the use in Parkinsonian syndrome
• hallmark side effect is development of dyskinesia (distortion/impairment of voluntary movement)

Answer 18

levodopa

Question 19

what are the adverse effects of levodopa?

Answer 19

1. GI: N/V
2. CV: postural hypotension, or HTN
3. dyskinesias occur in 80% of pts (choreoathetosis of face and distal extremities)
4. behavioral: depression, anxiety, agitation, insomnia, somnolence, confusion
5. fluctuations in response, on/off phenomenon: periods of marked akinesia alternate over the course of a few hours with periods of improved mobility

Question 20

what drug class can be administered in addition to levodopa/carbidopa, and those who have end-of-dose akinesia or on/off phenomenon?

Answer 20

DA receptor agonists

Question 21

which DA agonist have extensive first pass metabolism with CYP34?

Answer 21

bromocriptine

Question 22

which DA agonist has preferential affinity for D3 receptors, and is approved from treatment of moderate-severe restless leg syndrome

Answer 22

pramipexole

Question 23

which DA agonist may require as dose adjustment in pts with renal insufficiency

Answer 23

pramipexole - KNOW this

Question 24

which DA agonist has preferential affinity for D2 receptors, and is metabolized primarily by CYP1A2?

Answer 24

ropinirole

Question 25

what are the adverse effects of DA agonists?

Answer 25

1. GI: anorexia, N/V, constipation 2. CV: postural hypotension 3. dyskinesias 4. mental disturbances: confusion, hallucination, delusions

Question 26

what are the contraindications of DA agonists?

Answer 26

pts with hx of **PSYCHOTIC ILLNESS, RECENT MI, OR ACTIVE PEPTIC ULCERTATION**

Question 27

what does MAO-A preferentially metabolize?

Answer 27

NE and 5HT

Question 28

what does MAO-B preferentially metabolize?

Answer 28

phenylethylamine and benzylamine

Question 29

what are equally metabolized by MAO-A and B?

Answer 29

DA and tryptamine

Question 30

which MAO-I is a selective irreversible MAO-B inhibitor?

Answer 30

selegiline

Question 31

what is the precaution with MAO-I's?

Answer 31

- pts taking meperidine, TCA's, or SSRI's -> **RISK OF SEROTONIN SYNDROME** - also, do NOT combine levodopa and nonselective MAO-I treatment -> **RISK OF HYPERTENSIVE CRISIS**

Question 32

these meds prolong the activity of levodopa by inhibiting peripheral metabolism, which decreases clearance and increases bioavalability

Answer 32

catechol-O-methyltransferase (COMT) inhibitors | - tolcapone, entacapone

Question 33

DA agonist at D2 receptors | - injected subQ -> clinical benefits in 10 mins!

Answer 33

apomorphine SA's: nausea, dyskinesias, drowsiness, sweating, hypotension, injection site bruising

Question 34

antiviral agent whose MOA in parkinsonism in unknown - may cause **livedo reticularis** (vascular condition w/purplish mottled discoloration of the skin, usually the legs); restlessness, depression, irritability, hallucinations, insomnia, HA, heart failure

Answer 34

amantadine

Question 35

what drug class may improve tremor and rigidity in PD, but have little effect on bradykinesia?

Answer 35

anticholinergic drugs | - adverse effects: common peripheral anchicolinergic effects)

Question 36

what drugs used to treat: | - tremor

Answer 36

- metoprolol, propranolol - topirimate - alprazolam - botulinum toxin A

Question 37

what drugs used to treat: | - HD

Answer 37

no current therapy slows disease progression | - but reserpine and tetrabenazine can alleviate chorea

Question 38

what drugs used to treat: | - tics

Answer 38

- tetrabenazine, haloperidol, pimozide -> EPS :( | - clonidine, guanfacine (effective w/fewer adverse effects)

Question 39

what drugs used to treat: | - restless leg syndrome

Answer 39

- pramipexole, ropinirole | - gabapentin, pregabalin (a2-Ca channel ligands)

Question 40

what drugs used to treat: | - ALS

Answer 40

riluzole (only drug w/impact on survival) | - inhibits glutamate release and blocks NMDA-r, inhibiting voltage-gated Na channel

Question 41

what drugs used to treat: | - Wilson disease

Answer 41

1. penicillamine (chelating agent, surrounds copper) 2. potassium disulfide (reduces intestinal absorption of copper) 3. trientine, zinc acetate, zinc sulfate (increase fecal excretion)