Movement disorders pharm Flashcards

1
Q

dopamine agonists (DA)

A
bromocriptine
pramipexole
ropinirole
rotigotine
apomorphine
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2
Q

monoamine oxidase inhibitors

A

rasagiline

selegiline

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3
Q

COMT inhibitors

A

entacapone

tolcapone

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4
Q

antimuscarinic agents

A
benztropine
biperiden
orphenadrine
procyclidine
trihexyphenidyl
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5
Q

levodopa MOA

A

agonist at D2R

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6
Q

levodopa PK

A

take 30-60min before meals
only 1-3% reaches brain
combo w/carbidopa reduces peripheral meta of levodopa

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7
Q

levodopa GI

A

w/o 80% experience anorexia, nausea, and vomiting

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8
Q

levodopa CV

A

postural hypotension
tachycardia, ventricular extrasystoles, rarely afib
d/t increased peripheral catecholamines
HTN can occur w/large doses

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9
Q

levodopa behavioral

A
depression
anxiety
agitation
insomnia
somnolence
confusion
delusions
hallucinations
nightmares
euphoria
more common w/combo
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10
Q

levodopa dyskinesia

A

80% of pt taking drug >10yrs

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11
Q

wearing off phenomenon

A

each dose of L-dopa effective for 1-2hrs with rapid return of rigidity and akinesia

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12
Q

on-off phenomenon

A

marked akinesia alternating with improved movement with no coordination to timing of drugs

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13
Q

DDIs levodopa

A

Pyridoxine- increases extracerebral metabolism may prevent therapeutic effect unless peripheral decarboxylase inhibitor
MAOIs-HTN, do not give if taking MAOIs or w/in 2 wks of discontinuation

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14
Q

DA MOA

A

act directly on postsynaptic DRs
do not require enzymatic conversion
no potentially toxic metabolites
do not compete w/another substance for transport across BBB

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15
Q

uses of DAs

A

certain pts respond better to certain drugs
1st line therapy for parkinsons
use is associated w/less fluctuations and dyskinesias then L-dopa
generally those who do not respond to L-dopa do not respond to DAs
can be added to L-dopa

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16
Q

bromocriptine

A

ergot alkaloid derivative
D2 agonists
extensive first pass
can also be used for endocrine disorders

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17
Q

pramipexole

A

D3Rs
renal insufficiency- must be dose adjusted
RLS

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18
Q

ropinirole

A

D2Rs

RLS

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19
Q

rotigotine

A

DA

may have serious site application rxns

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20
Q

DA GI

A

anorexia, nausea, vomiting (should be taken w/meals)

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21
Q

DA CV

A
postural hypotension
ergot derivatives (bromocriptine)- painless digital vasospasm
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22
Q

DA dyskinesias

A

dose dependent

23
Q

DA mental disturbances

A

confusion, hallucinations, delusions

disorders of impulse control

24
Q

DA misc ADRs

A

HA, nasal congestion
increased arousal
pulmonary infiltrates, pleural and retroperitoneal fibrosis
pramipexole and ropinirole can cause pts to fall asleep at inappropriate times

25
Q

DA CIs

A
history of psychotic illness, recent MI, active peptic ulcer disease
ergot derivatives (bromocriptine)- should be avoided in peripheral vascular disease
26
Q

MAO types

A

monoamine oxidase A- metabolizes NE, serotonin, and dopamine

monoamine oxidase B- metabolizes dopamine selectively

27
Q

selegiline MOA

A

selective inhibitor of MAO B decreasing dopamine breakdown

28
Q

selegiline uses

A

adjuct for declining effectiveness of L-dopa

should be taken and breakfast and lunch to prevent insomnia

29
Q

rasagiline MOA

A

irreversible inhibitor MAO-B

more potent then selegiline

30
Q

rasagiline uses

A

neuro-protective and early parkinsons

31
Q

MAOI DDIs

A
non-selective MAOIs should not be combined w/L-dopa b/c can cause HTN crisis 
cannot be combined w/:
-meperdine
-tramadol
-methasone
-propoxyphene
-cyclobenzaprine
-st. johns wort
-dextropmethorphan
-OTC cold preps
32
Q

COMT inhibitors

A

inhibitions of dopa decarboxylase is associated w/compensatory activation of other pathways of L-dopa metabolism, especially COMT which increases 3-O-methyldopa which competes w/L-dopa to cross BBB

33
Q

COMT inhibitors MOA

A

prolong action of L-dopa by diminishing peripheral metabolism

34
Q

uses of COMT inhibitors

A

pts who have developed response fluctuations
tolcapone- central and peripheral effects
entacpone- peripheral only

35
Q

COMT inhibitors ADRs

A
related to increased L-dopa
diarrhea
abdominal pain
orthostatic hypotension
sleep disturbances
orange urine
tolcapone- rare acute hepatic failure
36
Q

apomorphine MOA

A

potent non-ergot dopamine agonists

post synaptic D2R in caudate and putamen

37
Q

uses of apomorphine

A

temporary relief (rescue) of off perioids

38
Q

ADRs of apomorphine

A

nausea at drug initiation
can preTx with trimethobenxamide
dyskinesias, drowsiness, sweating, hypotension, injection site bruising

39
Q

amantadine MOA

A

antiviral

unclear, but may potentiate dopamangeric fnx

40
Q

uses of amantadine

A

less efficasious then L-dopa
benefits short lived (wks)
may favorably impact bradykinesia, rigidity, tremor
may help reduce iatrogenic dyskinesias in advanced disease

41
Q

amantadine ADRs

A

restlessness, depression, irritability, insomnia, agitation, excitement, hallucinations, and confusion, as well as HA, heart failure, postural hypotension, urinary retention, and GI disturbances
may cause livedo reticularis

42
Q

amantadine CIs

A

Hx of seizures or heart failure

43
Q

antimuscarinic MOA

A

centrally actin, mAChR antagonists

44
Q

antimuscarinic use

A

may improve tremor and rigidity of parkinsonism, but little effect on bradykinesia

45
Q

antimuscarinic ADRs

A

common peripheral antimuscarinic effects:

sedation, mental confusion, constipation, urinary retention, blurred vision

46
Q

parkinson’s disease

A

dopaminergic therapy early stage
avoid Tx until disability
start w/one of these: rasafiline, amantadine, and antimuscarinic
w/progression switch to DA +/- carbidopa-levodopa
end-stage ass COMT inhibitor

47
Q

tremor

A
beta blockers
antiepileptic drug primidone (small dose)
topiramate
alprazolam
botulinum toxin A
48
Q

Huntingtons Tx

A

reserpine and tetrabenzine to deplete dopamine stores
block DRs: olanzapine, pehnothiazine, butyrophenones,
can also use: GABA, glutamic acid decarboxylase, and choline acetyltransferase

49
Q

Tics

A

ANTIPSYCHOTICS
alpha adrengerics
botulinum toxins

50
Q

RLS

A
DAs
levodopa
diazepam
clonazepam
opitates
51
Q

wilsons disease

A

penicillamine

potassium disulfide

52
Q

penicillamine MOA

A

chelating agent

53
Q

penicillamine ADRs

A

nausea, vomiting, neprhotic syndrome, myastehnia, optic neuropathy, blood disorders

54
Q

potassium disulfide

A

reduces intestinal absorption of Cu