Module 3 anti-parkinson

Question 1

D1 receptor family

Answer 1

D1 and D5
when activated second messenger systems
- inc. cAMP
- inc. PIP2 hydrolysis: Ca mobilization, PKC activation

Question 2

D2 receptor family

Answer 2

D2, D3, D4
when activated second messenger systems:
- dec. cAMP
- inc. K current
- dec. voltage gated Ca currents
-> hyperpolarization

Question 3

D1 stimulation

Answer 3

excitatory

- enables movement

Question 4

D2 stimulation

Answer 4

inhibitory

- inhibits movement

Question 5

Parkinson’s disease patho

Answer 5

direct pathway inhibited and indirect pathway activated, leading to reduced movement.

• dec. dopamine
• degeneration of dopaminergic neurons in substantia nigra

Question 6

s/s of parkinson’s

Answer 6

bradykinesia
rigidity
impaired postural balance
tremor

Question 7

Parkinson tx

Answer 7

symptomatic tx only
in. dopamine activity in brain
no change in underlying degenerative process

Question 8

levodopa MOA

Answer 8

dopamine precursor
- given with carbidopa
converted to DA in the CNS
inc. dopamine levels

Question 9

levodopa/carbidopa AE

Answer 9

dyskinesia: uncontrollable rhythmic movements of head and trunk

Question 10

levodopa/carbidopa education

Answer 10

continued use -> tolerance and desensitization

• need to inc. dose
• fluctuations between off and on periods

Question 11

Dopamine receptor agonist meds

Answer 11

bromocriptine
pramipexole
ropinirole

Question 12

dopamine Rc agonist MOA

Answer 12

directly target postsynaptic DA Rc

Question 13

dopamine Rc agonist administration

Answer 13

adjunct to levodopa
no coversion required
longer half-life: less blood level fluctulaiton

Question 14

dopamine Rc agonist AE

Answer 14

sedation
vivid dreams
hallucination

Question 15

MAO-BI drugs

Answer 15

selegiline

rasagiline

Question 16

MAO-BI MOA

Answer 16

inhibit breakdown of DA by MAO-B

Question 17

selegiline AE

Answer 17

toxic metabolite: amphetamine

-> sleeplessness, confusion

Question 18

COMT inhibitor drugs

Answer 18

tolcapone

entacapone

Question 19

COMT inhibitor MOA

Answer 19

inhibits DA breakdown by COMT

Question 20

entacapone MOA

Answer 20

works in periphery only

- inc. L-DOPA in periphery -> inc. CNS uptake

Question 21

tolcapone AE

Answer 21

hepatotoxicity

Question 22

nondopaminergic agents

Answer 22

amantadine
trihexyphenidyl
benztropine

Question 23

amantadine

Answer 23

tx of levodopa-induced dyskinesias

unknown MOA: blocks excitatory NMDA receptors

Question 24

trihexyphenidyl, benztropine

Answer 24

anti-cholinergics

reduction of tremor