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PHARM 3 > Anti-parkinsons drugs > Flashcards

Anti-parkinsons drugs Flashcards

1
Q

dopamine synthesis originates from which amino acid

A

tyrosine

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2
Q

which transporter is used for tyrosine transport across BBB

A

SYSTEM L

Na+ independent

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3
Q

RLS in dopamine synthesis

A

tyrosine hydroxylase

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4
Q

DOPA decarboxylase

A

converts DOPA –> dopamine

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5
Q

D1 2nd messenger system

A

G(s) = increased adenylyl cyclase

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6
Q

D2 2nd messenger system

A

G(i) = decreased adenylyl cyclase - inc K+ conductance, dec Ca2+ conductance

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7
Q

parkinson’s tx goals

A

1) restore dopamine actions

2) antagonize acetylcholine

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8
Q

dopamine precursor

A

levodopa

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9
Q

levodopa

A

stereoisomer of dopa
dopamine/norepinephrine precursor

good for pt with early disease = requires presence of residual dopaminergic neurons for conversion of levodopa–> dopamine

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10
Q

carbidopa

A

dopa decarboxylase inhibitor

doesn’t cross BBB

given with levodopa to dec peripheral metabolism to dopamine

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11
Q

levodopa use

A

symptomatic use - only lasts while drug is in body

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12
Q

levodopa MOA

A

transported into CNS, there is converted to dopamine

a lot of it is decarboxylated to dopamine in periphery –> AE: n/v arrhythmias, hypotension

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13
Q

sinemet

A

carbidopa + levodopa prep

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14
Q

levodopa PK

A

food delays appearance in plasma == certain amino acids can compete for absorption from gut and for transport through BBB

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15
Q

levodopa metabolites

A

via COMT = 3-o-methyl dopa, 3-methoxytyramine

–> HVA

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16
Q

levodopa fluctuations in response

A

1) wearing off rxn = related to time of intake

2) on-off phenomenon = unrelated to timing - may benefit from apomorphine

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17
Q

levodopa contraindicatiosn

A

B6 - cofactor for dopa decarboxylase = inc peripheral metabolism

MAOI = HTN crisis

not used in psychotic pt

angle closure glaucoma

arrhythmias

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18
Q

which class doesn’t depend on capacity of nigrostriatal neurons

A

dopamine receptor agonist

19
Q

classes of dopamine receptor agonists

A

1) ergot dopamine agonists

2) nonergot dopamine agonists

20
Q

bromocriptine

A 
D2 agonist
(ergot dopamine)
21
Q

pramipexole

A

nonergot dopamine agonists

22
Q

ropinirole

A

nonergot dopamine agonists

23
Q

nonergot dopamine agonists

A

better for younger pt

older pt more vulnerable to AE of dopamine agonists

24
Q

rotigotine

A

nonergot dopamine agonists

available as transdermal

25
Q

which nonergot dopamine agonists is used as a transdermal

A

rotigotine

26
Q

AE of dopamine agonists

A

GI: anorexia, n/v, constipation, peptic ulcer bleeding

CV: postural hypotension, arrhythmias, periph edema

dyskinesias: abnormal movements

mental disturbances: confusion, hallucinations

misc:
ergot - pulmonary infiltrates, pleural fibrosis, erythromelalgia

nonergot - uncontrollable somnolence

27
Q

dopamine agonists contraindications

A

pt with psych hx or recent mi

peripheral vascular dz
peptic ulceration

28
Q

rescue therapy for nonergot dopamine agonist

A

apomorphine

29
Q

apomorphine

A

nonergot dopa agonists rescue

used in “off” epsidoes of akinesia

emetogenic (given with antiemetic trimethobenzamide)

AE: QT prolonged, dyskinesias, drowsiness, sweating

30
Q

MAOI

A

deprenyl/selegiline

selectively irreversibly inhibits MAO-B

retards breakdown of DA

enhances levodopa effects - and can dec its dose

levodopa adjunct*

metabolized to amphetamine –> insomnia

31
Q

deprenyl

32
Q

rasagiline

A

MAOI

MAO-B inhibitor selective

33
Q

use of carbidopa and levodopa, increases what substance peripherally?

A

3-o-methyl dopa

also competes with levodopa for an active transporter across intestinal mucosa and BBB

34
Q

tolcapone

A

COMT inhib

35
Q

entacapone

A

COMT inhib

36
Q

COMT inhib function

A

dec levodopa metabolism
dec plasma 3-o-methyldopa
inc levodopa uptake – higher DA levels in brain

37
Q

COMT AE

A

hepatic necrosis **tolcapone

entacapone = not hepatotoxic - preferred

38
Q

amantadine PD application

A

increases synthesis, release/re-uptake of dopamine from surviving neurons

39
Q

amantadine AE

A

restlessness
hallucination
aucte toxic psychosis
peripheral edema (give diuretics)

livedo reticularis - redness to skin

40
Q

anti-muscarinics for PD

A

adjuvant
improve tremor, rigidty

little effect on bradykinesia

AE: mood changes, xerostomia, pupillary dilation, hallucination

contraindic: glaucoma, BPH, pyloric stenosis

41
Q

DOC for PD

A

levodopa + carbidopa

42
Q

2nd most effective drugs for PD

A

dopamine agonists

43
Q

addition of which drug in addition to levodopa to reduce motor fluctuations in adv PD pt

A

COMT-inhib or MAO-B inhib

PHARM 3 (21 decks)

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