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Neuro Quiz 3 > Dopamine Enhancing Agents > Flashcards

Dopamine Enhancing Agents Flashcards

1
Q

How do we increase dopaminergic action in striatum?

A 
Augmentation of the synthesis of brain DA
Stimulation of DA release
Direct stimulation of DA receptor
Decreasing DA reuptake
Decreasing metabolism of DA and DOPA
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2
Q

Secondary therapeutic goal in PD

A

Decrease endogenous ACh action

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3
Q

Why worry about ACh?

A

ACh has an overall stimulating effects on muscle contraction (while DA inhibits muscle contracting so not enough = tremor)

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4
Q

So what happens in PA?

A

Not enough DA to counteract ACh

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5
Q

Why can’t you administer DA?

A

It is completely destroyed during digestion
It cannot be absorbed by the gut wall
Must be given IV and even then it can’t cross BBB

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6
Q

So L-dopa works how?

A

It is decarboxylated to DA

L-dopa is transported across BBB via large neutral amino acid transporter (LAT)

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7
Q

L-dopa half life and problems

A

0.5-2 hrs
Has to compete with neutral amino acids so don’t take it with lots of proteins
Also rapid peripheral decarboxylation so always given with an inhibitor

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8
Q

Levodopa SE

A

Nausea
Dyskinesias
Hallucinations, postural hypoTN

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9
Q

Long-term treatment with levodopa leads to

A

Motor complications

  • Waring off and response fluctuations
  • Dyskinesias (involuntary movements)
  • Feeling stuck to the floor
  • Therapeutic window becomes narrower with longer treatment
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10
Q

Levodopa Absorption

A

Bioavailablity of 30% but doubled when given with a decarboxylase inhibitor
Delayed/reduced with food

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11
Q

Levodopa Metabolism and Excretion

A

M: Liver/gut/kidney
E: Kidneys

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12
Q

Decarboxylase Inhibitor =

A

Carbidopa

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13
Q

Decarboxylase Inhibitor MOA

A

Inhibits the peripheral metabolism of L-dopa to DA which increases amount of levadopa which increase the amount of DA in the brain

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14
Q

Carbidopa Brands

A

Sinernel
Rytary
Lodosyn (monotherapy)

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15
Q

Carbidopa helps to

A

Relieve nausea and other side effects of Levadopa

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16
Q

COMT Inhibitors do what?

A

Diminish response fluctuations
Adjunct to L-dopa/carbidopa
Blocks L-DOPA to 3-o-MD

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17
Q

COMT Inhibitors Drugs

A

Talcapone (Tasmar)

Entacapone (Comtan)

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18
Q

Talcapone Brand

A

Tasmar

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19
Q

Talcapone MOA

A

Inhibits COMT centrally and peripherally

Long duration of action

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20
Q

Talcapone SE

A

jaundice, upset stomach, extreme tiredness, hepatotoxicity

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21
Q

Talcapone Black Box Warning

A

Risk of potentially fatal, acute fulminant liver failure so requires blood test

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22
Q

Talcapone Use

A

Only used in patients not responding to other treatments

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23
Q

Entacapone Brand

A

Comtan

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24
Q

Entacapone MOA

A

Inhibits COMT peripherally

Preferred over Tolcapone

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25
Q

Carbidopa + Levodopa + Entacapone =

A

Stalevo

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26
Q

Entacapone SE

A

Nausea
Orthostatic hypotension
0 Less severe

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27
Q

Entacapone + MAOI?

A

Only selegiline

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28
Q

MAO-A

A

Preferentially deaminates serotonin, epinephrine and NE leading to unwanted serious side effects

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29
Q

MAO-B

A

Resonsible for oxidative deamination of DA in the brain

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30
Q

So is MAOB or A more desired?

A

MAO-B should be selectively inhibited

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31
Q

MAO-B Inhibitors

A

Selegiline (Eldepryl, Emsam, Zelapar)

Rasagiline (Azilect)

32
Q

Selegiline

A

Eldepryl
Emsam
Zelapar

33
Q

Selegiline is what type of inhibitor?

A

Irreversible MAO-B Inhibitor

34
Q

Low dose verse high dose Selegiline

A

Low: MAOB
High: both A and B

35
Q

Selegiline Use

A

1st drug of choice in pts under 65
Monotherapy in early PD
Adjunct in advanced PD

36
Q

Metabolites of Selegiline

A

Amphetamine and methamphetamine

37
Q

Selegiline SE

A

Anxiety and insomnia

Hallucinations

38
Q

Selegiline Drug Interactions

A

Meperidine (serotonin syndrome, CV instability)

39
Q

Transdermal patch and orally disintegrating pill of selegiline?

A

Reduce 1st pass metabolism and limits the formulation of metabolites so there are less side effects

40
Q

Rasagiline brand

A

Azilect

41
Q

Rasagiline MOA

A

irreversible MAO-B Inhibitor

42
Q

Rasagiline upside

A

Not metabolized to amphetamines so less side effects

43
Q

Rasagiline use

A

Monotherapy in early or adjunct with levadopa in advanced PD

44
Q

Ergot derivatives that are Dopamine Receptor Agonists

A

Bromocriptine

- Rarely used nowadays bc they are older

45
Q

Most common Dopamine Receptor Agonists

A

Pramipexole

Rapirnirole

46
Q

Define Indirect Pathway

A

Inhibits movement

47
Q

Define Direct Pathway

A

Enables movement

48
Q

What does Dopamine do to the pathways?

A

It inhibits the indirect pathway (blocks inhibition of movements) and stimulates the direct pathway (increase movement)

49
Q

So how do dopamine agonist work?

A

Directly stimulates dopamine receptors

50
Q

Dopamine Agonists upsides

A

Longer half lives
No toxic metabolites
No competition for transporter

51
Q

Dopamine Agonist Uses

A

Initial therapy esp in young and adjunct to levadopa

52
Q

Monotherapy dopamine agonist

A

Ropinirole and pramipexole

53
Q

Dopamine agonists SE

A 
N/V
Dizziness
Drowsiness/somnolence
Confusion hallucinations
Dyskinesias with levadopa
Fibrosis (ergots)
54
Q

Ropinirole brand

A

Requip

55
Q

Ropinrole MOA

A 
D2 class receptor selectivity
6 hr half life and last 8-24 hours
56
Q

Ropinirole SE

A

Somnolence
Hallucination/confusion
Orthostatic hypotension

57
Q

Ropinirole Use

A

Treating on/off effects

58
Q

Pramipexole Brand

A

Mirapex

59
Q

Pramipexole MOA

A

D2 class receptor selectivey
8 hr half life
90% bioavailability

60
Q

Pramipexole AE

A

N
Somnolence
Sleepiness (sudden falling asleep)

61
Q

Apomorphine brand

A

Apokyn

- Oldest and most potent dopamine agonist

62
Q

Apomorphine Use

A 
SC injection 
Rescue medication (pts with irregular off periods)
63
Q

Apomorphine SE

A

Highly nauseating

Orthostatic hypotension

64
Q

Rotigotine Brand and dosage form

A

Neupro

- Transdermal patch

65
Q

Rotigotine MOA

A

Selective D2 receptor agonist

halflife 5-7 hrs

66
Q

Rotigotine Use

A

PD and restless leg syndrome

67
Q

Anti-cholinergic agent MOA

A

Anti-PD blcoks msucarinic receptors or inhibit DA reuptake

DA depletion leads to increased cholinergic activity (tremor)

68
Q

Decreased dopaimine leads too

A

Inhibited ACh through D2

Increased ACh which leads to tremor

69
Q

Muscarinic receptor antagonists?

A

Benzlropine (Cogentin)

Trihexyphenidyl (Artane)

70
Q

Anticholinergic agent Use

A

Tremor

71
Q

Anticholinergic agents + older pts

A

Worsening dementia so CI in alzheimer’s

72
Q

Anticholinergic SE

A 
Dry mouth
Constipation
Urinary retention
Sedation/confusion
Delirium
73
Q

Amantadine brand

A

Symmetrel

74
Q

Amantadine MOA

A

Antiviral drug used for flu
Enhances DA release and inhibits its reuptake
Has anticholinergic properties
Blocks NMDA receptors

75
Q

Amantadine Use

A

Mild PD

76
Q

Amantadine SE

A 
Confusion
Dizziness
Hallucinations
Dry mouth
Livedo reticularis (mottling of skin)

Neuro Quiz 3 (3 decks)

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