Parkinson Disease Drugs Flashcards

(66 cards)

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
Pramipexole is what type of drug?
nonergot dopamine agonist
26
Ropinirole is what type of drug?
nonergot dopamine agonist
27
Rotigotine is what type of drug?
nonergot dopamine agonist
28
Bromocriptine is what type of drug?
ergot dopamine agonist
29
What is Amantadine MOA?
promotes release of dopamine and may block reuptake
30
How long does it take for full PD symptom relieve with levodopa use?
months
31
Gradual loss of symptom relief or "wearing off" with levodopa is due to what?
subtherapeutic plasma levels
32
How to minimize wearing off with levodopa?
- shorten dosing interval - add drug that prolongs half-life (entacapone) - add direct acting dopamine agonist
33
Abrupt loss of symptom relief or "on-off" phenomenon with levodopa is due to what?
thought to reflect disease progression and not tolerance to the drug
34
Drugs that can help reduce on-off phenomenon with levodopa?
- entacapone | - rasagiline
35
GI considerations for levodopa use?
- food delays absorption by delaying gastric emptying | - high protein foods reduce therapeutic effects
36
How is levodopa metabolized?
- decarboxylase enzymes convert levodopa to dopamine in the periphery and brain
37
True or False: Dopamine can not cross the BBB?
true
38
Pyridoxone enhances the effects of which enzyme?
decarboxylase
39
What are the adverse effects of levodopa?
- N/V - Dyskinesias - postural hypotension - arrhythmias - psychosis - CNS effects - dark sweat or urine
40
What psychosis symptoms present with levodopa?
- hallucinations - vivid dreams/nightmares - paranoid
41
How to reduce the pyschosis AE of levodopa?
reduce dose
42
Treatment of levodopa induced psychosis?
clozapine and quetiapine
43
CNS side effects of levodopa?
- anxiety - agitation - memory loss - cognitive impairment
44
Hypertensive crisis can occur with concurrent use of levodopa with?
MAOi
45
Which drug type are the first choice of treatment for mild to moderate PD?
dopamine agonist
46
Apomorphine is what type of drug?
nonergot dopamine agonist
47
cabergoline is what type of drug?
ergot dopamine agonist
48
Drugs for Parkinson Disease?
- levodopa - carbidopa - pramipexole - entacapone - selegiline - amantadine - benztropine
49
Pramipexole is used to treat what?
- PD - mod-severe restless leg syndrome - highly selective for dopamine 2 and D3 receptors
50
Ropirinole is used to treat what?
- PD | - restless leg syndrome
51
Rotigotine is used to treat what?
- PD | - mod-severe restless leg syndrome
52
What is apomorphine used to treat?
- hypomobility during off episodes in advance PD - NOT for routine treatment of PD - given by injection
53
What type of drug is entacapone and tolcapone?
Catechol-O-Methyltransferase Inhibitors (COMTi)
54
What is entacapone used to treat?
PD by inhibiting the metabolism of levodopa
55
Entacapone adverse effects?
- vomitting | - yellow-orange urine
56
Talcapone adverse effects?
- liver failure | - yellow-orange urine
57
Selegiline is what type of drug?
- selective, irreversible MAO-B inhibitor | - prevents destruction of dopamine
58
What is Selegiline used to treat?
PD
59
What can occur when you combine selegiline with an SSRI (prozac)?
fatal serotonin syndrome
60
SSRI's should be withdrawn how long before giving selegiline?
at least 5 weeks
61
Rasagiline is what type of drug?
- selective, irreversible MAO-B inhibitor | - prevents destruction of dopamine
62
Why does selegiline cause insomnia?
it is metabolized into l-amphetamine and l-methamphetamine
63
What foods should be avoided when taking selegiline and rasagiline?
tyramine rich foods, cause hypertensive crisis
64
Amantadine MOA?
- inhibition of dopamine uptake - stimulation of dopamine release - anticholinergic - NMDA antagonist - glutamate receptor blocker
65
What is tested for in a BMP?
a. Bicarb b. BUN c. Creatinine d. Calcium e. Chloride f. Glucose g. Potassium h. Sodium
66
What is tested for in a CMP?
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