PD Meds Flashcards

1
Q

What are the 2 types of drugs used for PD?

A
  • Dopaminergic agents: activate dopamine receptors

- Anticholinergic agents: block acetylcholine

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2
Q

What drugs treat mild symptoms?

A

MAOB-inhibitor (Dopaminergic agents):

-selegiline or rasagiline

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3
Q

What drugs treat severe symptoms?

A

Levodopa with carbidopa and possibly with entacapone

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4
Q

percursor to dopamine

A

levodopa

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5
Q

What happens to Levodopa over time?

A
  • benefits diminish over time
  • gradual wearing off: prevent by shortening dosing interval and give meds that prolog levodopa half life
  • Abrupt loss: “on-off” phenomenon, lasts hours to minutes
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6
Q

Explain the mechanism of action of Levodopa.

A
  • crosses BBB
  • converts to dopamine in CNS and periphery
  • activates post-synaptic dopaminergic receptor; increases dopamine at receptor site
  • administer with decarboxylase inhibitors to increase bioavailability
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7
Q

What are some important adverse affects of Levodopa?

A
  • difficulty with impulse control
  • insomnia and nightmares
  • darkens sweat and urine
  • dyskinesias: involuntary movements
  • anxiety, hallucinations, paranoia
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8
Q

What are the drug interactions with Levodopa?

A
  • 1st gen antipsychotics
  • MAOIs
  • Anticholinergic drugs (benztropine (congentin) and Trihexyphenidyl (Artane).
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9
Q

What is the mech of action for carbidopa?

A
  • inhibits decarboxylase leaving more levodopa available in the CNS
  • does not allow metabolism in GI or peripheral tissue
  • but then is unable to cross BBB so it won’t prevent conversion of levodopa to dopamine
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10
Q

What are the advantages of carbidopa?

A
  • levodopa dosage can be reduced

- reduces N/V and cardiovascular response (dysrhythmias) caused by levodopa

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11
Q

What is one disadvantage of the levodopa and carbidopa combination?

A

abnormal movements and psychiatric disturbances can occur sooner and be more intense

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12
Q

What is sinemet?

A

Levodopa and Carbidopa

  • take on empty stomach
  • food reduces absorption
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13
Q

First line drug for PD for mild to moderate symptoms.

A

dopamine agonists

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14
Q

What are the 2 dopamine agonists (drugs)?

A

pramipexole (Mirapex)

apomorphine (Apokyn)

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15
Q

What are the serious side effects of dopamine agonists pramipexole (Mirapex) apomorphine (Apokyn)?

A

hallucinations
day time sleepiness
postural hypotension

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16
Q

What are the 2 types of dopamine agonists?

A
  • derivatives of ergot: less selective

- non-ergot derivatives: highly selective for dopamine receptors

17
Q

When is pramipexole (Mirapex) used?

A
  • early on in PD used alone for motor improvement

- late in PD used with levodopa to reduce levodopa dosage

18
Q

What else is pramipexole (Mirapex) used for?

A

RLS

19
Q

What are the adverse effects of pramipexole (Mirapex) alone and with levodopa?

A
  • monotherapy: nausea, dizziness, insomnia, constipation, hallucinations
  • combined with levodopa: orthostatic hypotension, dyskinesias, increase in hallucinations, compulsive behaviors,
20
Q

What are the characteristics of the non-ergot (highly selective) dopamine agonist
apomorphine (Apokyn)?

A
  • used during “off” periods to treat hypo mobility for advanced PD pt’s
  • not for routine PD management (no given PO)
  • derivative of morphine but devoid of typical opioid effects
21
Q

What are the adverse effects of apomorphine (Apokyn)?

A
  • injection site reaction
  • hallucinations
  • drowsiness
  • dyskinesias
  • rhinorrhea
  • N/V
  • sleep attacks
  • rare: priapism
22
Q

What are the 2 COMT inhibitors and what do they do?

A
  1. entacapone (safer and more effective)
  2. Tolcapone
    - inhibit metabolism of levodopa in the periphery and GI
    - prolongs time levodopa is available to the brain
23
Q

What are some important adverse effects of entacapone (Comtan)?

A

-yellow orange discoloration of urine

24
Q

When are anticholinergics (benztropine (congentin) and Trihexyphenidyl (Artane) used for?

A

-used for second line therapy for tremor

25
Q

These block cholinergic receptors in the periphery.

A

(benztropine (congentin) and Trihexyphenidyl (Artane)