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DPT 530 > CNS Agents > Flashcards

CNS Agents Flashcards

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
Q

what is the desired therapeutic effect of rasagiline (azilect)?

A

less dopamine broken down in the brain–>more movement

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26
Q

when is the peak plasma concentration of carbidopa/Levodopa (sinemet)?

A

0.5-2 hours

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27
Q

when is the peak plasma concentration of pramipexole (mirapex)?

A

1-3 hours

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28
Q

when is the peak plasma concentration of rasagiline (azilect)?

A

0.5-1 hour

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29
Q

what is the half life of carbidopa/Levodopa (sinemet)?

A

1.5 hours

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30
Q

what is the half life of pramipexole (Mirapex)?

A

8-12 hours

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31
Q

what is the half life of rasagiline (azilect)?

A

1.5-3.5 hours

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32
Q

t/f: carbidopa/Levodopa (sinemet) has minimal hepatic metabolism

A

true

33
Q

t/f: pramipexole (Mirapex) has minimal hepatic metabolism

A

true

34
Q

t/f: rasagiline (azilect) has minimal hepatic metabolism

A

false, it has extensive hepatic metabolism

35
Q

what are common side effects of carbidopa/levodopa (sinemet)?

A

orthostatic hypotension, confusion, movement disorders, nausea, hallucinations

36
Q

what are common side effects of pramipexole (mirapex)?

A

inappropriate urges (sexual, gambling, etc), edema (usually peripheral below the knees)

37
Q

t/f: pramipexole (mirapex) can be used to treat restless leg syndrome

A

true

38
Q

what are common side effects of rasagiline (azilect)?

A

headache, nausea, joint pain, upset stomach, depression, falls, constipation, orthostatic hypotension, dry mouth, rash, hallucinations, vomiting, and difficulty moving

39
Q

t/f: there are a lot of movement and behavioral side effects of meds targeting dopaminergic receptors

A

true

40
Q

t/f: meds with overlapping side effects make those side effects more likely

A

true

41
Q

what is a very common side effect of PD meds

A

dyskinesia (unwanted movement)

42
Q

t/f: orthostatic hypotension is already a symptom of PD, so PD meds may make it worse as it is a common side effect

A

true

43
Q

are hallucinations associated with PD meds usually visual or auditory?

A

visual

44
Q

t/f: hallucinations from PD meds can cause psychosis like symptoms

A

true

45
Q

what are serious side effects of carbidopa/levodopa (sinemet)?

A

dyskinesia

orthostatic hypotension

MI

arrhythmias/depression

46
Q

what are serious side effects of pramipexole (mirapex)?

A

hallucinations, vision changes, SOB/chest pain

ongoing safety review regarding possible risk of heart failure

47
Q

why is it especially important to monitor cardiac symptoms if a pt is on pramipexole (mirapex)?

A

bc there is a risk for heart failure

48
Q

what are serious side effects of rasagiline (azilect)?

A

HTN

MI

arryhthmias

dyskinesia

49
Q

what is a potential drug interaction with carbidopa/Levodopa (sinemet)?

A

MAOI antidepressants with carbidopa/Levodopa can severely increase BP

protein with carbidopa/levodopa can have negative interactions

50
Q

why should carbidopa/Levodopa (sinemet) be taken at least an hour after a meal (especially high protein meals)?

A

bc it can have negative interactions with protein

51
Q

what are potential drug interactions with pramipexole (mirapex)?

A

acetaminophen, aspirin, caffeine, opioid analgesics can increase the side effects of pramipexole (mirapex)

52
Q

what are potential drug interactions with rasagiline (azilect)?

A

antidepressants that increase serotonin levels can lead to serotonin syndrome

amphetamines (stimulants)

vasoconstrictors

interactions lead to an increased risk of CV events

53
Q

what are the symptoms associated with serotonin syndrome?

A

arrhythmias, seizures, confusion, increased reflexes, dilated pupils, etc)

54
Q

what is the on-off phenomenon?

A

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
Q

what can we do for a pt experiencing symptoms of the on-off phenomenon?

A

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
Q

what are other classes of drugs commonly used for PD?

A

anticholinergics

COMT inhibitors

NMDA receptor blockers

57
Q

what do anticholinergic drugs do?

A

combat the increased influence of Ach

decrease excessive movement (rigidity and tremors and drooling)

58
Q

what kind of drugs are Trihexyphenidyl (artane), Benztropine (cogentin), and Biperiden (Akineton)?

A

anticholinergic

59
Q

what are the side effects of anticholinergic drugs?

A

dry mouth, blurred vision, photophobia, urinary retention, constipation

60
Q

are the side effects of anticholinergic drugs related to sympathetic or parasympathetic overactivation?

A

sympathetic overactivation

61
Q

anticholinergic drugs down regulate ____ and up regulate ____

A

parasympathetic, sympathetic

62
Q

what is COMT (catechol-O-methyltransferase)?

A

an enzyme that breaks down L-dopa in peripheral tissues

63
Q

what do COMT inhibitors do?

A

prevent L-dopa from breaking down in the periphery by blocking COMT

similar actions to carbidopa

64
Q

what kind of drugs are Tolcapone (Tasmar) and Entacapone (Comtan)?

A

COMT inhibitors

65
Q

t/f: COMT inhibitors can be combined with l-dopa and carbidopa

A

true

66
Q

what drug is a combo of COMT inhibitors, L-dopa, and carbidopa?

A

Stalevo

67
Q

what are the side effects of COMT inhibitors?

A

abdominal pain, back pain, constipation, nausea, diarrhea, and hematuria (blood in urine)

68
Q

NMDA receptors are a subtype of ___ receptors, which are ___?

A

glutamate, excitatory

69
Q

what do NMDA receptor blockers do?

A

the exact mechanism is unknown but it is believed to increase dopamine release or decrease glutamate influence

70
Q

what type of drug is Amantadine (symmetrel, Gocoril)?

A

NMDA receptor blockers

71
Q

t/f: Amantadine is an antidyskinetic agent, NMDA antagonists, dopamine agonist, and anticholinergic

A

true

72
Q

what does NMDA receptor blockers treat?

A

tremors and dyskinesia

73
Q

t/f: NMDA receptor blockers are given in conjunction with Levodopa in pts with excessive movements like tremors

A

true

74
Q

what are the side effects of NMDA receptor blockers?

A

orthostatic hypotension, depression, confusion, rashes

75
Q

what are the PT implications of CNS agents?

A

scheduling of PT

recognize synergistic effects of physical rehab and drug therapy

pt education

pt safety

advocacy

76
Q

when should PT be scheduled for a pt with PD?

A

30-60 minutes after meds are taken

may see pts in off periods

77
Q

what can we educate pts on?

A

dosing schedule

keeping an hourly log of symptoms

78
Q

what pt safety risks should we keep in mind?

A

OH, falls, syncope

79
Q

how can we advocate for our pts?

A

document responses and side effects to med changes

communicate with the pt and neurologist for optimizing meds

DPT 530 (14 decks)

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