Pharmacology > PARKISON'S > Flashcards

PARKISON'S Flashcards

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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?

Study These Flashcards
A

-Apomorpine
-Rotigotine
-Ropinirole
Pramiprexole

24
Q

What are ADE of dopamine agonist (4)?

Study These Flashcards
A
  • impulsive behaviors
  • postural hypotension
  • pulmonary fibrosis
  • psychosis: hallucinations, confusion,sedation, vivid dreaming
25
What are the benefits to using Rotigotine?
- transdermal patch - no renal or hepatic impairment - CYP mediated drug interactions are not significant
26
What is MOA of Amantidine?
- increases release of dopamine | - blocks NMDA receptors
27
What are ADE of Amantidine? (3)
- dry mouth - anti-cholinergic effects - livedo reticularis
28
T/F Amantidine is useful add on agent to attenuate dyskinesias caused by levydopa
True
29
Apomorphine ADE (1)?
N/V | -give anti-emetics before giving apomorpine
30
T/F Apomorphine is derived from morphine but lacks its narcotic properties?
TRUE
31
What is route of administration of apomorphine, half life, and drug metabolism?
- sub Q injection - 40 min T 1/2 - extensive hepatic first pass effect
32
when should you use apomorphine?
patients with optimized therapy but frequent off response | "on response induced in 20 minutes
33
T/F increased Ach causes the tremor in PD?
True
34
What is MOA of Benztropine and Trihexylphenydyl?
- block Ach muscarinic receptors | - balance Ach and Dopamine levels
35
What are ADE of Benztropine and THP?
Hot as a hare - dry as a bone - red a beet - blind as bat - mad as hatter
36
Which drug is used to tx the dyskinesias from use of Levydopa?
Amantidine
37
Which drug is used to tx PD in asymptomatic patients?
MAO-B - Rasaligine - Selegiline
38
What is peak dose dyskinesia?TX?
- dyskinesia seen with peaked dose of l-dopa - lower dose of L-dopa - add amantidine
39
What is freezing?Tx?
- L-dopa complication - increase L-dopa - add MAO-I
40
How do you tx delayed on response?
- give L-dopa/Carbidopa on empty stomach | - add apomorphine
41
How do you tx wearing off?
- add COMT | - increase frequency of L-dopa/Carbidopa
42
Eventually all pt will need Levy/Carbidopa?
TRUE
43
What is Duopa?
- gel form of levy/carbydopa that is administered into small intestine via enteral tube - reduced off symptoms - for pt who cant swallow
44
What is Inbrija?
-inhaled levydopa/carbidopa -used to tx off episodes ADE: glaucoma, BF discoloration/urine sweat -respiratory issues
45
What is istradefylline?
A2A antagonist -adenosine receptor antagonist ADE: slight increase in dyskinesia -tx wearing off adjunct therapy to levydopa
46
What do you use to tx tremor in patient <65y/o?
Ach blockers | -Benztropine or Trihexyphenidyl
47
What do you use to tx tremor in patient >65y/o?
Levydopa/Carbidopa
48
What do you use to tx bradykinesia/rigidity in patient <65y/o?
dopamine agonist
49
What do you use to tx bradykinesia/rigidity in patient >65y/o?
levydopa/carbidopa
50
How do you tx motor complications?
deep brain stimulation
51
How do you tx stooped posture in <65 y/o?
dopamine agonist: rotigotine, ropinilone, | PT
52
How do you tx stooped posture in >65 y/o?
Levydopa/Carbidopa and PT
53
Anti-cholinergic meds are used for what?
- mild tremors-monotherapy less than 65y/o | - adjunct therapy for tremors when levydopa no longer useful as monotherapy
54
What is the medical use of Levydopa/Carbydopa?
- best tx for symptomatic PD | - used for tremors in >65 y/o or uncontrolled tremors
55
What are the medical uses of COMT inhibitors?
- attenuate motor fluctuations in levydopa/carbidopa | - good add on therapy for
56
What are the uses of dopamine agonists?
- mild to moderate PD | - reduces off time
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