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Pharmacology 3 > Neuro 2 Parkinsons > Flashcards

Neuro 2 Parkinsons Flashcards

1
Q

What is Parkinsons?

A

degeneration of substantial nigra in the cerebellum

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2
Q

Why does it occur?

A

loss of dopamine producing neurons

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3
Q

What may worsen symptoms?

A

Mismatch between Ach and DA

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4
Q

Classic triad of disease?

A
  • Bradykinesia
  • Rigidity
  • Tremor
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5
Q

What is the phenomenon?

A

“on-off”, periods of dyskinesia (on, hyper movement) and alternating hypokinesia (off, no movement) so disease is difficult to manage

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6
Q

6 Therapeutic Maneuvers

A
  • Replenish dopamine supply
  • Agonize dopaminergic stimulation
  • Inhibit dopamine metabolism
  • Release dopamine for stores
  • Inhibit dopamine reuptake
  • Reduce cholinergic over-play
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7
Q

What may antipsychotics do?

A

antidopaminergics, may precipitate “drug-induced parkinsonism”

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8
Q

What is Levodopa?

A

naturally occurring amino acid precursor (l dopa) of dopamine

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9
Q

Why not use dopamine? (2)

A

rapidly metabolized in the gut, blood, and liver.

DA will NOT cross BBB

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10
Q

What 2 things metabolizes dopamine?

A

COMT & MAO

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11
Q

Does IV dopamine work centrally?

A

NO- poor lipophilicity

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12
Q

L-dopa is rapidly absorbed where? What converts it to dopamine?

A

Gut, transported across BBB within CNS, converted to DA via Central Dopa Decarboxylase

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13
Q

What is a cofactor in the peripheral conversion of L-dopa to DA?

A

Vitamin B6 (pyridoxine)

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14
Q

What is the therapeutic limitation?

A

As mono therapy, most of l-dopa metabolized by peripheral dopadecarboxylase

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15
Q

How can you prevent this limitation?

A

co-administor with decarboxylase inhibitors

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16
Q

Do you want decarboxylase inhibitor to cross BBB?

A

NO, you want l-dopa to be metabolized once it gets through BBB

17
Q

Decarboxylase inhibitor drug interactions? what happens?

A

Non-selective MAO, can lead to HTN urgency / emergency

Also antipsychotics

18
Q

Bromocriptine is what? Used how?

A

D2 agonist (dopamine receptor)

Dosed in combination with L-dopa

19
Q

How is Bromocriptine administered

A

PO- rapidly absorbed so dosed multiple times/day

20
Q

Bromocriptine A/E?

A

N/V (low doses)

Hallucinations, confusion (high dose)

21
Q

What is another use of Bromocriptine? Who may use this? What is the drug called?

A

Hyperprolactinemia- dopamine hates prolactin

Galactorhhea, pituitary adenoma

Cabergoline (NOT for Parkinsons)

22
Q

What is Rotigotine? Indicated for what? Administered how?

A

Dopamine agonist for Parkinson’s and Restless Leg Syndrome

QD transdermal patch

23
Q

A/E of Rotigotine? (2)

A
  • Psychosis

- Acute compulsive behavior

24
Q

Entacapone works how?

A

COMT inhibitor (enzyme that metabolizes DA)

Prolongs the activity of l-dopa

25
Q

Entacapone dosed with what?

A

L-dopa, crosses BBB and keeps L-dopa around longer

26
Q

Who should get Entacapone?

A

patients with L-dopa end dose phenomenon

27
Q

A/E of Entacapone?

A

increased incidence of dyskinesias

28
Q

What is Tolcapone?

A

similar to Entacapone, with greater lipophilicity and CNS penetration but increased risk of hepatic necrosis

29
Q

Amantidine works how?

A

Increases the synthesis and release of DA, may also block reuptake

30
Q

Is Amantidine or L-dope more effective?

A

L-dopa

31
Q

What is Amantidine used for?

A

limited efficacy as an anti-viral agent (Influenza A, but now resistant) by weak neuraminidase inhibitor

32
Q

A/E of Amantidine?

A
  • Insomnia

- Hallucinations

33
Q

What is Rimantidine?

A

Hydrophilic analogue of Amantidine, it does not cross BBB so not for Parkinsons

34
Q

How do Anticholinergics work?

A

Redress issue of CNS dopaminergic/cholinergic imbalance

35
Q

Give examples of Anticholinergics

A
  • Diphenhydramine
  • Benztropine
  • Trihexyphenidyl
36
Q

How do you treat essential tremor?

A

Propranolol

tremor of intent

37
Q

How do you treat RLS?

A

Ropinirole

Pramipexole

Pharmacology 3 (10 decks)

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