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Pharmacology > PARKISON'S > Flashcards

PARKISON'S Flashcards

1
Q

What is PD?

A
  • neurons connecting substantia nigra and striatum degenerate
  • Dopamine inputs inhibitory effect on GABA neuron in striatum
  • low levels of dopamine and high levels of GABA causes motor and cognitive imbalance
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2
Q

What is clinical presentations of PD?

A
  • coll wheel rigidity/bradykinesia
  • pill rolling tremors
  • stooped posture
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3
Q

What are therapies aimed at?

A
  • increasing dopamine levels
  • mimic dopamine action
  • antagonist to ACh colinergic neurons
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4
Q

What is MOA of Levydopa/Carbidopa? Why use levydopa over dopamine?

A
  • dopamine precursor and carbidopa prevents the fast metabolism of levydopa by blocking DDC enzyme
  • levydopa can cross blood brain barrier
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5
Q

What are drug interactions with Levydopa/Carbidopa?

A
  • COMT and MOA inhibitors
  • prolong effect of Levydopa
  • patient will exhibit excess dopamine
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6
Q

ADE of Levy/Carbidopa?

A
  • motor complications
  • dyskenisia
  • drowsiness
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7
Q

What % goes to the brain with Levy/Carbidopa?

A
  • 10%

- 1-3% without Levydopa/Carbidopa

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8
Q

What is MOA COMT Inhibitors?

A

they block the the conversion of L-Dopa into inactive 3-OMD in periphery

  • they block the conversion of dopamine into 3-MT in brain/glial cells
  • decrease metabolism of dopamine to increase the levels in the brain
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9
Q

Name two COMT inhibitors?

A

Entacapone
Tolcapone
-Entacapone only works at periphery
-Tolcapone: works on brain and periphery

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10
Q

What are ADE of COMT inhibitors?ADE?

A

Tolcapone: causes liver toxicity

  • dyskenisia
  • increased L-dopa levels
  • ADE: interact with anti-diarrhea meds
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11
Q

What should you monitor when using Tolcapone?

A

Liver function test

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12
Q

What is MAO-B inhibitors?

A
  • prolonged dopaminergic

- prevents metabolism of dopamine into DOPAC by irreversibly blocking MOA-B enzyme in glial cells/brain.

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13
Q

Name 2 drugs that are MAO-B inhibitors?

A
  • Rasaligine

- Selegiline

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14
Q

What are ADE of MOA-I?

A
  • N/V
  • insomnia
  • hallucinations
  • orthostatic hypotension
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15
Q

What is a drug interaction with MAO-I?

A
  • opiods analgesics
  • meperidine
  • serotonin syndrome: tachycardia, increased BP
  • Tremor
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16
Q

T/F SSRI’s anti-depressant cannot be used with MAO-I?

A

False

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17
Q

What is end product of selegiline?

A

amphetamine

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18
Q

What is 1 ADE of selegiline?

A

-increases effect of L-Dopa and can worsen dyskinesias and delusions

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19
Q

What is MOA of Safinamide?

A

-reversibly blocks MAO-B and is added AS ADJUNCT THERAPY to Levy/Carbidopa tx

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20
Q

What are ADE drug events Safinamide (5)?

A
  • impulse control disorder
  • hallucinations
  • falls
  • HTN
  • elevated LFT’s
  • very high tyramine foods
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21
Q

What is MOA for dopamine agonists?

A
  • dopamine agonist mimic dopamine

- stimulate dopamine receptors in nerves of sub. migra and striatum

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22
Q

T/F Seriligine and Rasagiline have a neuroprotective effect?

A

TRUE

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23
Q

Name 4 dopamine agonists?

A

-Apomorpine
-Rotigotine
-Ropinirole
Pramiprexole

24
Q

What are ADE of dopamine agonist (4)?

A
  • impulsive behaviors
  • postural hypotension
  • pulmonary fibrosis
  • psychosis: hallucinations, confusion,sedation, vivid dreaming
25
Q

What are the benefits to using Rotigotine?

A
  • transdermal patch
  • no renal or hepatic impairment
  • CYP mediated drug interactions are not significant
26
Q

What is MOA of Amantidine?

A
  • increases release of dopamine

- blocks NMDA receptors

27
Q

What are ADE of Amantidine? (3)

A
  • dry mouth
  • anti-cholinergic effects
  • livedo reticularis
28
Q

T/F Amantidine is useful add on agent to attenuate dyskinesias caused by levydopa

A

True

29
Q

Apomorphine ADE (1)?

A

N/V

-give anti-emetics before giving apomorpine

30
Q

T/F Apomorphine is derived from morphine but lacks its narcotic properties?

A

TRUE

31
Q

What is route of administration of apomorphine, half life, and drug metabolism?

A
  • sub Q injection
  • 40 min T 1/2
  • extensive hepatic first pass effect
32
Q

when should you use apomorphine?

A

patients with optimized therapy but frequent off response

“on response induced in 20 minutes

33
Q

T/F increased Ach causes the tremor in PD?

A

True

34
Q

What is MOA of Benztropine and Trihexylphenydyl?

A
  • block Ach muscarinic receptors

- balance Ach and Dopamine levels

35
Q

What are ADE of Benztropine and THP?

A

Hot as a hare

  • dry as a bone
  • red a beet
  • blind as bat
  • mad as hatter
36
Q

Which drug is used to tx the dyskinesias from use of Levydopa?

A

Amantidine

37
Q

Which drug is used to tx PD in asymptomatic patients?

A

MAO-B

  • Rasaligine
  • Selegiline
38
Q

What is peak dose dyskinesia?TX?

A
  • dyskinesia seen with peaked dose of l-dopa
  • lower dose of L-dopa
  • add amantidine
39
Q

What is freezing?Tx?

A
  • L-dopa complication
  • increase L-dopa
  • add MAO-I
40
Q

How do you tx delayed on response?

A
  • give L-dopa/Carbidopa on empty stomach

- add apomorphine

41
Q

How do you tx wearing off?

A
  • add COMT

- increase frequency of L-dopa/Carbidopa

42
Q

Eventually all pt will need Levy/Carbidopa?

A

TRUE

43
Q

What is Duopa?

A
  • gel form of levy/carbydopa that is administered into small intestine via enteral tube
  • reduced off symptoms
  • for pt who cant swallow
44
Q

What is Inbrija?

A

-inhaled levydopa/carbidopa
-used to tx off episodes
ADE: glaucoma, BF discoloration/urine sweat
-respiratory issues

45
Q

What is istradefylline?

A

A2A antagonist
-adenosine receptor antagonist
ADE: slight increase in dyskinesia
-tx wearing off adjunct therapy to levydopa

46
Q

What do you use to tx tremor in patient <65y/o?

A

Ach blockers

-Benztropine or Trihexyphenidyl

47
Q

What do you use to tx tremor in patient >65y/o?

A

Levydopa/Carbidopa

48
Q

What do you use to tx bradykinesia/rigidity in patient <65y/o?

A

dopamine agonist

49
Q

What do you use to tx bradykinesia/rigidity in patient >65y/o?

A

levydopa/carbidopa

50
Q

How do you tx motor complications?

A

deep brain stimulation

51
Q

How do you tx stooped posture in <65 y/o?

A

dopamine agonist: rotigotine, ropinilone,

PT

52
Q

How do you tx stooped posture in >65 y/o?

A

Levydopa/Carbidopa and PT

53
Q

Anti-cholinergic meds are used for what?

A
  • mild tremors-monotherapy less than 65y/o

- adjunct therapy for tremors when levydopa no longer useful as monotherapy

54
Q

What is the medical use of Levydopa/Carbydopa?

A
  • best tx for symptomatic PD

- used for tremors in >65 y/o or uncontrolled tremors

55
Q

What are the medical uses of COMT inhibitors?

A
  • attenuate motor fluctuations in levydopa/carbidopa

- good add on therapy for

56
Q

What are the uses of dopamine agonists?

A
  • mild to moderate PD

- reduces off time

Pharmacology (47 decks)

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