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Specialized Pharmacology MN650 > Parkinson Disease Drugs > Flashcards

Parkinson Disease Drugs Flashcards

1
Q

What are the 3 ways a nuerotrasmitter is removed from the synaptic cleft?

A
  • reuptake
  • enzymatic degradation
  • diffusion
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2
Q

What types of drugs cannot cross the blood brain barrier?

A

protein bound and highly ionized

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3
Q

What types of drugs can cross the blood brain barrier?

A
  • lipid soluble

- drugs that use transport systems

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4
Q

Monoamine neurotransmitters of the CNS include?

A
  • dopamine
  • epi
  • NE
  • serotonin
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5
Q

Opioid peptides of the CNS include?

A
  • dynorphins
  • endorphins
  • enkephalins
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6
Q

What is the term for a decreased response that occurs with prolonged drug use?

A

tolerance

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7
Q

What are the cardinal symptoms of Parkinson Disease?

A
  • resting tremor
  • rigidity
  • postural instability
  • bradykinesia
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8
Q

What is the cause of the motor symptoms in parkinsons disease?

A

loss of dopamine releasing neurons in the substantia nigra resulting in excessive stimulation of acetylcholine

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9
Q

What is dyskinesia?

A

disorder of movement

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10
Q

What is the term for slowed body movements?

A

bradykinesia

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11
Q

What is the term for complete loss of movement?

A

akinesia

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12
Q

In persons with PD, what two neurotransmitters are out of balance?

A
  • dopamine

- acetylcholine

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13
Q

What is dopamine’s MOA?

A

GABA inhibition

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14
Q

What two classes of drugs are used to treat PD?

A
  • anticholinergic agents

- dopaminergic agents

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15
Q

What are the 4 mechanisms of action for the dopaminergic drugs?

A
  • direct dopamine receptor activation
  • monoamine oxidase B inhibitors
  • increase release of dopamine
  • prevent dopamine reuptake
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16
Q

What is levodopa’s MOA?

A
  • direct dopamine receptor agonist

- enters into dopaminergic neuron in the striatum of the brain, where it is converted to dopamine

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17
Q

What is the drug of choice for the initial treatment of mild PD symptoms?

A

MOA-B inhibitor

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18
Q

Rasagiline is what type of drug?

A

MOA-B inhibitor

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19
Q

Selegiline is what type of drug?

A

MOA-B inhibitor

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20
Q

What does monoamine oxidase-B do?

A

breaks down dopamine

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21
Q

What is the drug of choice for the initial treatment of severe PD symptoms?

A

Levodopa/carbidopa or dopamine agonist

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22
Q

What is the only drug recommended for levodopa induced diskinesias?

A

amantadine

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23
Q

What is Entacapones MOA?

A

inhibits breakdown of levodopa by COMT

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24
Q

Long-term use of these drugs are associated with “off times” or loss of symptom relief and drug-induced diskinesia

A

levodopa and dopamine agonists

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25
Q

Pramipexole is what type of drug?

A

nonergot dopamine agonist

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26
Q

Ropinirole is what type of drug?

A

nonergot dopamine agonist

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27
Q

Rotigotine is what type of drug?

A

nonergot dopamine agonist

28
Q

Bromocriptine is what type of drug?

A

ergot dopamine agonist

29
Q

What is Amantadine MOA?

A

promotes release of dopamine and may block reuptake

30
Q

How long does it take for full PD symptom relieve with levodopa use?

A

months

31
Q

Gradual loss of symptom relief or “wearing off” with levodopa is due to what?

A

subtherapeutic plasma levels

32
Q

How to minimize wearing off with levodopa?

A
  • shorten dosing interval
  • add drug that prolongs half-life (entacapone)
  • add direct acting dopamine agonist
33
Q

Abrupt loss of symptom relief or “on-off” phenomenon with levodopa is due to what?

A

thought to reflect disease progression and not tolerance to the drug

34
Q

Drugs that can help reduce on-off phenomenon with levodopa?

A
  • entacapone

- rasagiline

35
Q

GI considerations for levodopa use?

A
  • food delays absorption by delaying gastric emptying

- high protein foods reduce therapeutic effects

36
Q

How is levodopa metabolized?

A
  • decarboxylase enzymes convert levodopa to dopamine in the periphery and brain
37
Q

True or False: Dopamine can not cross the BBB?

A

true

38
Q

Pyridoxone enhances the effects of which enzyme?

A

decarboxylase

39
Q

What are the adverse effects of levodopa?

A
  • N/V
  • Dyskinesias
  • postural hypotension
  • arrhythmias
  • psychosis
  • CNS effects
  • dark sweat or urine
40
Q

What psychosis symptoms present with levodopa?

A
  • hallucinations
  • vivid dreams/nightmares
  • paranoid
41
Q

How to reduce the pyschosis AE of levodopa?

A

reduce dose

42
Q

Treatment of levodopa induced psychosis?

A

clozapine and quetiapine

43
Q

CNS side effects of levodopa?

A
  • anxiety
  • agitation
  • memory loss
  • cognitive impairment
44
Q

Hypertensive crisis can occur with concurrent use of levodopa with?

A

MAOi

45
Q

Which drug type are the first choice of treatment for mild to moderate PD?

A

dopamine agonist

46
Q

Apomorphine is what type of drug?

A

nonergot dopamine agonist

47
Q

cabergoline is what type of drug?

A

ergot dopamine agonist

48
Q

Drugs for Parkinson Disease?

A
  • levodopa
  • carbidopa
  • pramipexole
  • entacapone
  • selegiline
  • amantadine
  • benztropine
49
Q

Pramipexole is used to treat what?

A
  • PD
  • mod-severe restless leg syndrome
  • highly selective for dopamine 2 and D3 receptors
50
Q

Ropirinole is used to treat what?

A
  • PD

- restless leg syndrome

51
Q

Rotigotine is used to treat what?

A
  • PD

- mod-severe restless leg syndrome

52
Q

What is apomorphine used to treat?

A
  • hypomobility during off episodes in advance PD
  • NOT for routine treatment of PD
  • given by injection
53
Q

What type of drug is entacapone and tolcapone?

A

Catechol-O-Methyltransferase Inhibitors (COMTi)

54
Q

What is entacapone used to treat?

A

PD by inhibiting the metabolism of levodopa

55
Q

Entacapone adverse effects?

A
  • vomitting

- yellow-orange urine

56
Q

Talcapone adverse effects?

A
  • liver failure

- yellow-orange urine

57
Q

Selegiline is what type of drug?

A
  • selective, irreversible MAO-B inhibitor

- prevents destruction of dopamine

58
Q

What is Selegiline used to treat?

A

PD

59
Q

What can occur when you combine selegiline with an SSRI (prozac)?

A

fatal serotonin syndrome

60
Q

SSRI’s should be withdrawn how long before giving selegiline?

A

at least 5 weeks

61
Q

Rasagiline is what type of drug?

A
  • selective, irreversible MAO-B inhibitor

- prevents destruction of dopamine

62
Q

Why does selegiline cause insomnia?

A

it is metabolized into l-amphetamine and l-methamphetamine

63
Q

What foods should be avoided when taking selegiline and rasagiline?

A

tyramine rich foods, cause hypertensive crisis

64
Q

Amantadine MOA?

A
  • inhibition of dopamine uptake
  • stimulation of dopamine release
  • anticholinergic
  • NMDA antagonist
  • glutamate receptor blocker
65
Q

What is tested for in a BMP?

A

a. Bicarb
b. BUN
c. Creatinine
d. Calcium
e. Chloride
f. Glucose
g. Potassium
h. Sodium

66
Q

What is tested for in a CMP?

A

a. Albumin
b. Alkaline phosphatase (ALP)
c. ALT
d. AST
e. Bicarb
f. Bilirubin
g. BUN
h. Creatinine
i. Calcium
j. Chloride
k. Glucose
l. Potassium
m. Sodium
n. Total protein

Specialized Pharmacology MN650 (28 decks)

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