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HLSC 220 - Pharmacotherapeutics for Healthcare Professionals > Chapter 24 - Drugs for Parkinson's Disease > Flashcards

Chapter 24 - Drugs for Parkinson's Disease Flashcards

(80 cards)

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1
Q

What is Parkinson’s Disease?

A

a neurodegenerative disorder of the extrapyramidal system associated with the disruption of neurotransmission

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2
Q

PD is characterized by __________ and __________

A

dyskinesia and akinesia

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3
Q

PD causes an imbalance between ___________ and _____ due to the degeneration of neurons

A

dopamine and ACh

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4
Q

Why does inadequate dopamine affect neurons?

A

no dopamine means ACh causes excessive stimulation of neurons that release GABA

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5
Q

What causes motor symptoms of PD?

A

overactiivity of GABA neurons

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6
Q

What are symptoms dyskinesias?

A

-tremor at rest
-rigidity
-postural instability
-bradykinesia (slowed movement)

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7
Q

What are non-motor symptoms of PD?

A

-autonomic disturbances
-depression
-psychosis
-dementia

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8
Q

What is the therapeutic goal of PD?

A

improve patient’s ability to carry out ADLs

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9
Q

Is there a treatment that reverses neuronal degeneration?

A

no

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10
Q

What are the two drug categories for PD?

A

-dopaminergic agents
-anticholinergic agents

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11
Q

What are the most commonly used drugs for PD?

A

dopaminergic agents

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12
Q

What do dopaminergic agents do?

A

promote activation of dopamine receptors

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13
Q

What is the prototype dopaminergic agent?

A

levodopa

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14
Q

What do anticholinergic agents do?

A

prevent activation of cholinergic receptors

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15
Q

What is the prototype anticholinergic for PD?

A

Benztropine

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16
Q

What drug is used for mild symptoms of PD?

A

monoamine oxidase-B (MAO-B) inhibitor like SELEGILINE or RASAGILINE

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17
Q

What drugs are used for more severe PD symptoms?

A

Levodopa combined with carbidopa or benserazide

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18
Q

What is a long-term risk of Levodopa?

A

disabling dyskinesias

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19
Q

“OFF” times for motor fluctuations can be reduced with…

A

dopamine agonists, COMT inhibitors, MAO-B inhibitors

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20
Q

Are there drugs that provide neuroprotection for PD?

A

no

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21
Q

___________ is only given in combination with carbidopa or benserazide

A

Levodopa

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22
Q

How does Levodopa act?

A

-increases dopamine synthesis in the brain to restore the balance between dopamine and ACh

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23
Q

What is Levodopa?

A

the biological precursor of dopamine

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24
Q

What breaks levodopa down into dopamine?

A

enzyme dopa-decarboxylase (DDA)

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25
How does levodopa enter the brain?
via an active transport system
26
What enhances the activity of decarboxylase?
pyridoxine (Vitamin B6)
27
Levodopa is useful for PD for ___ years before losing efficacy after 5 years
2
28
How is levodopa administered?
orally
29
What are food restrictions of Levodopa?
-food delays absorption
30
What kind of foods reduce therapeutic effects of levodopa?
high-protein foods
31
How can you minimize the wearing off effect of levodopa?
-shorten dosing interval -give drug that prolongs half life -give a direct-acting dopamine agonist
32
What are the adverse effects of Levodopa?
-N&V -orthostatic hypotension -palpitations -agitation -anxiety -psychosis -dyskinesias -vivid dreams -nightmares -impulsivity -memory impairment -darkened sweat and urine -activates malignant melanoma (SKIN ASSESSMENTS!!)
33
What does Levodopa interact with?
-1st gen. antipsychotics -MAOIs (htn crisis) -anticholinergics
34
How do 1st gen antipsychotics interact with levodopa?
block DA receptors and decrease therapeutic effects
35
How do MAOIs interact with levodopa?
htn crisis
36
How do anticholinergic drugs interact with levodopa?
contribute to dyskinesias, cause enhanced response to levodopa
37
Do carbidopa and benserazide have therapeutic effects of their own?
no
38
What do carbidopa and benserazide do?
inhibit decarboxylation of levodopa in intestine (helps inhibit conversion of levodopa into DA allowing it to be available in the CNS), thus decreasing the needed dosage by 75%
39
Carbidopa reduces what adverse effects of levodopa?
-CV -N&V
40
Dopamine agonists are _____-line drugs for PD
first
41
How do dopamine agonists act?
directly activate dopamine receptors
42
How do dopamine agonists compare to Levodopa?
-are less effective -don't depend on enzymatic conversion to be ACTIVE -lower incidence of response failure -less likely to cause dyskinesia
43
What are the two types of dopamine agonists?
-derivatives of ergot -non-ergot derivatives
44
What kind of dopamine agonist is Pramipexole?
non-ergot
45
How does pramipexole act?
D2 (some D3) receptor agonist
46
When is pramipexole used?
-early PD -with levodopa in advancing PD
47
What are the adverse effects of pramipexole used alone?
-nausea -dizziness -somnolence -insomnia -constipation -weakness -hallucinations
48
What are the adverse effects of pramipexole used in combo?
-orthostatic hypotension -dyskinesias -hallucinations
49
What are rare adverse effects of pramipexole?
-impulse control disorders (gambling, shopping, eating) -sleep attacks
50
What kind of dopamine agonist is rotigotine?
non-ergot
51
How does rotigotine act?
D2 and D3 receptor agonist, some action on other dopamine, alpha, and serotonin receptors
52
When is rotigotine used?
-early in tmt -with or without levodopa
53
What are side effects of rotigotine?
-N&V -dizziness -somnolence -site reactions
54
How is rotigotine applied?
patch - do not cut to get lower dose
55
What is a limitation of Bromocriptine?
poorly tolerated
56
What kind of dopamine agonist is Bromocriptine?
ergot derivative
57
How does Bromocriptine act?
direct dopamine agonist (activates dopamine receptors)
58
How is Bromocriptine used?
-early PD -in combo with levodopa for advance PD
59
What are the adverse effects of Bromocriptine?
-nausea -confusion -nightmares -hallucinations -delusions -retroperitoneal fibrosis -pulmonary infiltrates -Raynaud like phenomenon -valvular heart disease
60
How do COMT inhibitors act?
inhibit metabolism of levodopa in the periphery by inhibiting the COMT enzyme
61
What are the direct therapeutic effects of COMTIs?
none. lol.
62
What category is Entacapone?
COMT inhibitor
63
Entacapone is combined with levodopa to:
-prolong the time levodopa is available in the brain -inhibit levodopa metabolism in the intestine and periphery
64
What are the adverse effects of Entacapone?
-dyskinesias -orthostatic hypotension -nausea -hallucinations -sleep disturbances -impulse control disorders -vomiting -diarrhea -constipation -yellow-orange discolouration of urine
65
What kind of drug is Selegiline?
a MAO-B inhibitor
66
Selegiline causes...
modest improvement of motor function
67
Benefits of Selegiline decline dramatically in ___ to ___ months
12-24 months
68
When is selegiline used?
early in PD progression
69
High doses of selegiline can interact with ___________
tyramine
70
How does amantadine act?
-inhibits DA uptake and stimulates DA release -blocks cholinergic receptors -blocks glutamate receptors
71
Is amantadine a first line agent?
no
72
How long is the amantadine response?
starts in 2-3 days, diminishes in 3-6 months
73
What is amantadine used for?
dyskinesias caused by levodopa
74
What are the adverse effects of amantadine?
-confusion -anxiety -blurred vision -urinary retention -dry mouth -constipation -livedo reticularis
75
Livedo reticularis
a condition characterized by mottle discolouration of the skin
76
How do centrally acting anticholinergics act?
block muscarinic receptors in the striatum
77
What are come centrally acting anticholinergic drugs?
-Benztropine -Trihexyphenidyl -Procyclidine
78
How do centrally acting anticholinergic drugs compare to levodopa and dopamine agonists?
-less effective -better tolerated
79
Which drugs are used for younger patients with mild symptoms?
centrally acting anticholinergic drugs
80
centrally acting anticholinergic drugs should be avoided in...
elderly patients

HLSC 220 - Pharmacotherapeutics for Healthcare Professionals (18 decks)

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