CNS Agents Flashcards

(79 cards)

1
Q

what drugs are a part of CNS pharmacology?

A

opioids

anti-parkinsonism meds

psychopharmacology

antiepileptic meds

anti-spasmodic meds

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2
Q

PD causes a decrease in ___ and an increase in ____ influence

A

dopamine, acetylcholine

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3
Q

what happens with damage to the substantia nigra?

A

death of dopamine producing cells (PD)

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4
Q

t/f: in PD the amount of ACh is not increased, but it’s relative influence is increased

A

true

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5
Q

pharmacology for PD increases ____ or takes away ____

A

dopamine, Ach

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6
Q

what are the 3 classifications of anti-parkinson agents?

A

carbidopa/Levodopa 25/100 (Sinemet 25/100): dopamine replacement

pramipexole (Mirapex): dopamine agonist

rasagiline (Azilect): monoamine oxidase-B (MOAB) inhibitor

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7
Q

what is Levodopa (l-dopa)?

A

dopamine replacement

precursor to dopamine

attempts to increase dopamine levels in the basal ganglia

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8
Q

what kind of drug is carbidopa/Levodopa?

A

a dopamine replacement

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9
Q

what kind of drug is pramipexole?

A

dopamine agonist

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10
Q

what kind of drug is rasagiline?

A

monoamine oxidase-B (MOAB) inhibitor

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11
Q

why can’t dopamine be used to treat PD?

A

bc dopamine can’t cross the blood brain barrier (BBB)

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12
Q

what converts L-dopa into dopamine?

A

DOPA (decarboxylase)

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13
Q

why is carbidopa given with l-dopa?

A

bc l-dopa can be converted into dopamine in the periphery before it reaches the brain, so it still won’t be able to cross the BBB.

carbidopa prevents the premature transformation of L-dopa to dopamine before crossing the BBB by inhibiting decarboxylase in the periphery

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14
Q

what pill combines L-dopa and carbidopa?

A

Sinemet

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15
Q

what is pramipexole?

A

a dopamine agonist that binds and activates dopaminergic receptors in the striatum

boosts the action of available dopamine

given earlier in disease progression

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16
Q

what drugs fall under the category of promipexole (Mirapex)?

A

Rotigotine (Neupro)

Apomorphine (Apokyn)

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17
Q

what is Rasagiline (Azilect)?

A

a MOAB inhibitor that reduces the breakdown of dopamine, resulting in increased levels of dopamine in the brain

often used with L-dopa

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18
Q

will Rasagiline (azilect) be effective if the brain is depleted of all dopamine?

A

no

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19
Q

t/f: the use of Rasagiline with L-dopa can decrease the dose of L-dopa required

A

true

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20
Q

why is it beneficial that Rasagiline with L-dopa can reduce the dose of L-dopa required?

A

bc L-dopa has a lot of side effects and if a long-term drug

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21
Q

t/f: Rasagiline has a lot of side effects

A

false, Rasagiline has relatively few side effects

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22
Q

what is Selegiline (Eldepryl)?

A

a non-selective MAOI

also used as an antidepressant bc it can stop the breakdown of other NTs like serotonin

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23
Q

what is the desired therapeutic effect of carbidopa/Levodopa (sinemet)?

A

more dopamine in the brain–> more movement

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24
Q

what is the desired therapeutic effect of pramipexole (Mirapex)?

A

activate dopamine receptors in the brain–>more movement

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25
what is the desired therapeutic effect of rasagiline (azilect)?
less dopamine broken down in the brain-->more movement
26
when is the peak plasma concentration of carbidopa/Levodopa (sinemet)?
0.5-2 hours
27
when is the peak plasma concentration of pramipexole (mirapex)?
1-3 hours
28
when is the peak plasma concentration of rasagiline (azilect)?
0.5-1 hour
29
what is the half life of carbidopa/Levodopa (sinemet)?
1.5 hours
30
what is the half life of pramipexole (Mirapex)?
8-12 hours
31
what is the half life of rasagiline (azilect)?
1.5-3.5 hours
32
t/f: carbidopa/Levodopa (sinemet) has minimal hepatic metabolism
true
33
t/f: pramipexole (Mirapex) has minimal hepatic metabolism
true
34
t/f: rasagiline (azilect) has minimal hepatic metabolism
false, it has extensive hepatic metabolism
35
what are common side effects of carbidopa/levodopa (sinemet)?
orthostatic hypotension, confusion, movement disorders, nausea, hallucinations
36
what are common side effects of pramipexole (mirapex)?
inappropriate urges (sexual, gambling, etc), edema (usually peripheral below the knees)
37
t/f: pramipexole (mirapex) can be used to treat restless leg syndrome
true
38
what are common side effects of rasagiline (azilect)?
headache, nausea, joint pain, upset stomach, depression, falls, constipation, orthostatic hypotension, dry mouth, rash, hallucinations, vomiting, and difficulty moving
39
t/f: there are a lot of movement and behavioral side effects of meds targeting dopaminergic receptors
true
40
t/f: meds with overlapping side effects make those side effects more likely
true
41
what is a very common side effect of PD meds
dyskinesia (unwanted movement)
42
t/f: orthostatic hypotension is already a symptom of PD, so PD meds may make it worse as it is a common side effect
true
43
are hallucinations associated with PD meds usually visual or auditory?
visual
44
t/f: hallucinations from PD meds can cause psychosis like symptoms
true
45
what are serious side effects of carbidopa/levodopa (sinemet)?
dyskinesia orthostatic hypotension MI arrhythmias/depression
46
what are serious side effects of pramipexole (mirapex)?
hallucinations, vision changes, SOB/chest pain ongoing safety review regarding possible risk of heart failure
47
why is it especially important to monitor cardiac symptoms if a pt is on pramipexole (mirapex)?
bc there is a risk for heart failure
48
what are serious side effects of rasagiline (azilect)?
HTN MI arryhthmias dyskinesia
49
what is a potential drug interaction with carbidopa/Levodopa (sinemet)?
MAOI antidepressants with carbidopa/Levodopa can severely increase BP protein with carbidopa/levodopa can have negative interactions
50
why should carbidopa/Levodopa (sinemet) be taken at least an hour after a meal (especially high protein meals)?
bc it can have negative interactions with protein
51
what are potential drug interactions with pramipexole (mirapex)?
acetaminophen, aspirin, caffeine, opioid analgesics can increase the side effects of pramipexole (mirapex)
52
what are potential drug interactions with rasagiline (azilect)?
antidepressants that increase serotonin levels can lead to serotonin syndrome amphetamines (stimulants) vasoconstrictors interactions lead to an increased risk of CV events
53
what are the symptoms associated with serotonin syndrome?
arrhythmias, seizures, confusion, increased reflexes, dilated pupils, etc)
54
what is the on-off phenomenon?
motor symptoms fluctuate w/in dose cycle of PD meds end-of-dose akinesia/dyskinesia peaks (side effects) and valleys (no therapeutic effect) decreased therapeutic window after prolonged drug use
55
what can we do for a pt experiencing symptoms of the on-off phenomenon?
decrease dosage, increase frequency give dif drug with dif action powder form of l-dopa can be inhaled for the off periods to get them through until the next dose (when in the valley)
56
what are other classes of drugs commonly used for PD?
anticholinergics COMT inhibitors NMDA receptor blockers
57
what do anticholinergic drugs do?
combat the increased influence of Ach decrease excessive movement (rigidity and tremors and drooling)
58
what kind of drugs are Trihexyphenidyl (artane), Benztropine (cogentin), and Biperiden (Akineton)?
anticholinergic
59
what are the side effects of anticholinergic drugs?
dry mouth, blurred vision, photophobia, urinary retention, constipation
60
are the side effects of anticholinergic drugs related to sympathetic or parasympathetic overactivation?
sympathetic overactivation
61
anticholinergic drugs down regulate ____ and up regulate ____
parasympathetic, sympathetic
62
what is COMT (catechol-O-methyltransferase)?
an enzyme that breaks down L-dopa in peripheral tissues
63
what do COMT inhibitors do?
prevent L-dopa from breaking down in the periphery by blocking COMT similar actions to carbidopa
64
what kind of drugs are Tolcapone (Tasmar) and Entacapone (Comtan)?
COMT inhibitors
65
t/f: COMT inhibitors can be combined with l-dopa and carbidopa
true
66
what drug is a combo of COMT inhibitors, L-dopa, and carbidopa?
Stalevo
67
what are the side effects of COMT inhibitors?
abdominal pain, back pain, constipation, nausea, diarrhea, and hematuria (blood in urine)
68
NMDA receptors are a subtype of ___ receptors, which are ___?
glutamate, excitatory
69
what do NMDA receptor blockers do?
the exact mechanism is unknown but it is believed to increase dopamine release or decrease glutamate influence
70
what type of drug is Amantadine (symmetrel, Gocoril)?
NMDA receptor blockers
71
t/f: Amantadine is an antidyskinetic agent, NMDA antagonists, dopamine agonist, and anticholinergic
true
72
what does NMDA receptor blockers treat?
tremors and dyskinesia
73
t/f: NMDA receptor blockers are given in conjunction with Levodopa in pts with excessive movements like tremors
true
74
what are the side effects of NMDA receptor blockers?
orthostatic hypotension, depression, confusion, rashes
75
what are the PT implications of CNS agents?
scheduling of PT recognize synergistic effects of physical rehab and drug therapy pt education pt safety advocacy
76
when should PT be scheduled for a pt with PD?
30-60 minutes after meds are taken may see pts in off periods
77
what can we educate pts on?
dosing schedule keeping an hourly log of symptoms
78
what pt safety risks should we keep in mind?
OH, falls, syncope
79
how can we advocate for our pts?
document responses and side effects to med changes communicate with the pt and neurologist for optimizing meds