Neuro Flashcards

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1
Q

Levodopa

A

Indication: parkinsons (early stages)

Route: oral - absorbed by AT - in comp with amino acids (high protein meals)

  • standard dosage
  • controlled release preparations
  • dispersible madopar - liquid so easier to swallow

Action:

  • cross BBB
  • taken up by dopaminergic cells in the substantia nigra
  • converted to dopamine by dopa decarboxylase
  • highly effacious (lost over time due to loss of neurones)

Adverse effects:

  • nausea/vomiting
  • hypotension
  • psychosis
  • tachycardia
  • involuntary movements
  • motor complications

Interactions: pyridoxine/vitamin B6 increases peripheral breakdown of levodopa

Other:

  • 90% inactivated in intestinal wall due to monoamine oxidase and dopa decarboxylase
  • 9% converted to dopamine in peripheral tissues
  • used in combo with a peripheral dopa decarboyxlase inhibitor (reduces dose required, side effects, increase levodopa reaching brain)
  • short half life (2hrs) - short dose interval and fluctulations in blood levels and symptoms
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2
Q

Sinemet, madopar

A

Levodopa in combination with peripheral dopa decarboxylase inhibitor

Sinemet = levodopa + carbidopa
Madopar = levodopa + benserazide
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3
Q

Entacapone, opicapone, stalevo

A

Indication: parkinsons

Class: Catechol-o-methyl transferase (COMT) inhibitors

Action: reduce peripheral breakdown of levodopa to 3-O-methyldopa - levodopa sparing effect

Other:
- no therapeutic effect alone - always with levodopa (and dopa decarboxylase inhbitor)

Stalevo = levodopa, peripheral dopa decarboxylase inhibitor, COMT inhibitor

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4
Q

Ropinirole, pramipexole, rotigotine, apomorphine

A

Indication: parkinsons

  • de novo therapy
  • add on therapy
  • apomorphine for severe motor fluctuations

Class: dopamine receptor agonists - less efficacy than levodopa

Route:

  • Oral = ropinirole, pramipexole
  • patch = rotigotine
  • subcutaneous = apomorphine

Adverse effects:

  • impulse control disorders e.g pathological gambling, punding
  • more pyschiatric side effects e.g hallucinations
  • sedation
  • confusion
  • nausea
  • hypotension

Other:

  • less dyskinesias/motor problems than levodopa
  • possible neuroprotection
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5
Q

Rasagaline, safinamide

A

Indication: parkinsons

  • used alone
  • used alongside levodopa to prolong action

Class: monoamine oxidase B inhibitors

Action: prevent metabolism of dopamine

Adverse effects: at high dose can risk hypertensive crisis

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6
Q

Trihexyphenidydyl, orphenarine, procylidine

A

Indication: parkinsons
- treat tremors

Class: anticholinergics - not acting via dopamine system so does not rely on neuron number

Disadvantages:

  • no effecr on bradykinesia
  • confusion and drowsiness
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7
Q

Amantadine

A

Indication: parkinsons
- levodopa induced dyskinaesia

Can cause hallucinations and confusion

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8
Q

Pyridostigmine

A

Indication: myasthenia gravis

Class: acetycholineesterase inhibitor

Route: oral

  • onset = 30 mins
  • peak = 60-120 mins
  • Duration = 3-6 hrs
  • dose interval and timing crucial

Action:

  • prevent breakdown of Ach
  • higher conc remains in the synaptic cleft
  • enahnce neuromuscular transmission

Adverse effects:

  • SSLUDGE syndrome (muscarinic side effect)
  • excess dose = cholinergic crisis

Other: manage the autoimmune side of myasthenia gravis via normal routes e.g corticosteroids, azathioprine

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