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Pharmacology > Parkinsons > Flashcards

Parkinsons Flashcards

1
Q

Name 6 treatment options Parkinson’s and examples

A
  • Dopamine precursor: levodopa and carbidopa/benserazide
  • dopamine agonists: pramipexole, ropinirole
  • increase release endogenous dopamine: amantadine
  • inhibit COMT: tolcapone, entacapone
  • inhibit mao-b: selegiline, rasagiline
  • affect cholinergic system: benzhexol, benztropine
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2
Q

Name 3 long term side effects of dopaminergics

A
  • Motor fluctuations: with Cp drop, “wearing off phenomena”
  • Freezing
  • dyskinesia: dystonia, akathisia, chorea, myoclonus
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3
Q

First line treatment Parkinson’s?

A 
Levodopa with carbidopa or benserazide: better to improve motor disability
Dopamine agonists (ropinirole, pramipexole): better to lessen motor complications
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4
Q

Name 2 drug interactions with selegiline

A
  • High doses: hypertension, especially with tyramine foods
  • amantidine (increase release endogenous dopamine) and centrally active antimuscarinic agents: potentiate anti-pd effects
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5
Q

Name a dopamine precursor

A

Levodopa

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6
Q

Name 2 dopamine agonists

A

• Pramipexole
• ropinirole
(Bromocriptine, cabergoline, pergolide, apomorphine)

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7
Q

Name an anti-parkinsons drug that stimulate endogenous release dopamine

A

Amantadine

Therefore not enzyme inhibitor like others.

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8
Q

Name a COMT inhibitor

A

Entacapone
(tolcapone)
For Parkinson’s

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9
Q

Name a mao-b inhibitor

A

Selegiline
(Rasagiline)
Parkinson’s

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10
Q

Name 2 anti. Parkinson’s drugs that affect cholinergic system

A
  • Benzhexol

* benztropine

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11
Q

Name indications selegiline

A

• Parkinson’s mild symptomatic relief prior to initiating methyldopa

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12
Q

Drug interactions with levodopa?

A

Maoi: hypertension (especially with tyramine)

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13
Q

Name 2 peripheral decarboxylase inhibitors that need to be given with levodopa to prevent metabolism before crossing BBB

A
  • Carbidopa

* benserazide

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14
Q

Name 4 adverse effects levodopa

A
  • Nausea and vomiting ( chemoreceptor trigger zone outside BBB so improve with decarboxylase inhibitor addition)
  • psychiatric: schizo like
  • CV: arrhythmia, postural hypotension ( improve with decarboxylase inhibitor addition)
  • dyskinesias, especially face and limbs
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15
Q

Which medications reduce off time of levodopa? (2)

A

Entacapone (comt I )

Rasagiline (maob-i)

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16
Q

Indication anticholinergics for Parkinson’s?

A

First line for Parkinsonism caused by antipsychotics

17
Q

Which Parkinson’s medication reduce dyskinesia?

A

Amantadine (stimulate release endogenous dopamine)

18
Q

Which neurotransmitter is pertinent in Parkinson’s

A

Dopamine (decrease)

19
Q

Moa levodopa?

A
  • Dopamine precursor that can cross BBB.
  • transported into brain via system L amino acid transporters
  • enters nerve terminals in basal ganglia where it’s decarboxylated to form dopamine by dopa decarboxylase
20
Q

Moa pramipexole?

A

Dopaminergic (d2) agonist that mimic dopamine

Longer acting than levodopa

21
Q

Moa selegiline?

A
  • Selective irreversible inhibitor of intraneuronal mao-b

* prevent breakdown dopamine

22
Q

Moa entacapone?

A
  • Reversible, competitive COMT inhibitor specific for cns

* prevent levodopa break down leading to increase bioavailability at nigrostriatal nerve fibres

23
Q

Moa amantadine?

A
  • Stimulate release endogenous dopamine!
  • other proposed moa: dopamine agonist, monoamine reuptake inhibitor, anticholinergic, NMDA r antag
  • also reported to inhibit reuptake dopamine presynaptically and have direct action on dopamine R
24
Q

Moa benzhexol?

A
  • Anticholinergic or antimuscarinic
  • ach inhibit dopamine response
  • restore balance between dopaminergic and cholinergic pathways
  • reduction tremors
25
Q

Name 2 long term effects of dopaminergics

A
  • Motor fluctuations (decreased levels): wearing off phenomena ( off time), freezing
  • Drug induced dyskinesia (increased levels): dystonia, akathisia, chorea, myoclonus
26
Q

Which anti-parkinsons drugs offer most favourable long term motor complication profile?

A

Dopamine 2 receptor agonist: pramipexole, ropinirole

27
Q

Ropinirole adverse effects? (4)

A
  • Somnolence and sleep episodes
  • Nausea
  • orthostatic hypotension, syncope
  • nightmares and hallucinations
28
Q

Describe metabolism selegiline and active metabolites (4)

A
  • Single oral dose or transdermal
  • extensively metabolised in liver but also intestine via n-dealkylation, carbon hydroxylation, ring hydroxylation.
  • active metabolites = amphetamine and methamphetamine
  • long half life 39 hours
29
Q

Name 3 adverse effects selegiline

A
  • Agitation and involuntary movements
  • confusion, insomnia, hallucinations
  • Nausea
30
Q

Which 2 factors predict the outcome of deep brain stimulation of subthalamic nucleus for Parkinson’s?

A
  • Intensity to which pt responds to levodopa rx (pre-op) serves as predictor motor improvement. Not helpful for symptoms that don’t respond.
  • younger patients with shorter disease duration or shorter motor fluctuations
31
Q

Name 5 beneficial effects of deep brain stimulation in Parkinson’s

A
  • effective control fluctuating responses to levodopa
  • Control dyskinesia that doesn’t improve with med adjustment
  • reduce tremor
  • reduce rigidity
  • improve slowing of movement
32
Q

Which release formulation is better for levodopa?

A

At rx initiation, no difference in rate of motor complications seen between extended and immediate release formulations

33
Q

Half life levodopa-carbidopa combination?

A

2 hours

34
Q

Ropinirole drug interaction?

A
  • cyp1a2 metabolise Ropinirole

* cyp1a2 inhibitors eg. ciprofloxacin, flavoxamine, reduce clearance Ropinirole

35
Q

Which drug has both antiviral and anti Parkinson’s activity?

A

Amantidine

36
Q

What percentage levodopa enter brain unaltered?

A

1-3%

Pharmacology (34 decks)

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