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Nervous System Pharmacology > Movement Disorder Drugs > Flashcards

Movement Disorder Drugs Flashcards

1
Q

Levodopa:
MOA
Therapeutic Use

A

Metabolized by DOPA-Decarboxylase–> Dopamine in the brain/periphery (crosses BBB)

Treats Parkinsons: Requires Large Dose

  • Peripheral decarboxylation
  • 40% metabolized in gut
  • Rarely given alone
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2
Q

Carbadopa:
MOA
Therapeutic Use

A

Inhibits Peripheral DOPA-Decarboxylase (NO cross BBB)
Inhibits peripheral L-Dopa metabolism
Given with L-Dopa= SINIMET

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3
Q

PRAMIPREXOLE:
MOA
Therapeutic Use
* Which patient population is ideal for this drug?

A

D3 agonist
1) Monotherapy mild Parkinsons
2) Restless Leg
Good for liver disease patients because not metabolized

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4
Q

Sinimet

A

Levodopa + Carbadopa

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5
Q

Contraindications to Levodopa Use (3 + caveat)

A

1) Narrow angle glaucoma
2) MAOis –> HTN crisis
3) Vitamin B6 –> INCREASES L-dopa breakdown in periphery
* Avoid rapid discontinuation

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6
Q

Adverse Drug Reactions to Levodopa:

GI, Cardio, Ocular, Psych

A

1) Nausea, vomiting, anorexia
2) Arrhythmias, hypotension
3) Mydriasis
4) Mood changes, depression, anxiety, psychosis
5) Hallucinations/ Dyskinesia Titrate dose

*Due to dopamine in periphery

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7
Q

Dopamine agonists that are ergot derivatives

A

Bromocriptine

Pergolide

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8
Q

Ropinirole:
MOA
Therapeutic Use

A

D2 agonist

Monotherapy mild Parkinsons or adjunct in severe disease

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9
Q

Apomorphine
MOA
Therapeutic Use
ADR*

A

Dopamine agonist rapidly taken up into brain
Parkinson’s Rescue therapy
Severe nausea, give antiemetic prior to admin.- not DA based

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10
Q

Rotigone:
MOA
Therapeutic Use
ADR*

A

Skin patch delivers continuous Dopamine agonist
Used to treat parkinsons
Discontinued
Crystallization at patch site

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11
Q

Antimuscarinic Drugs Used to Treat Parkinson’s

A

Trihexylphenidyl

Benzotropine

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12
Q

Rasageline:
MOA
Therapeutic Use

A

MAO-B Inhibitor: Stop Dopamine–> DOPAC–> Increase Dopamine, Decrease Oxidative Stress

Parkinson’s:

1) Monotherapy early on/ w sinemet
2) Combo tx. In late disease

  • More potent than selegiline
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13
Q

Selegiline:
MOA
Therapeutic Use
ADR

A

MAO-B Inhibitor: Stop Dopamine–> DOPAC–> Increase Dopamine, Decrease Oxidative Stress

Parkinson’s: Prevents On/Off symptoms of L-Dopa tx.

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14
Q

Which drugs interact with MAOB’s (3)?

Which foods should these patients avoid (1) ?

A
  • Many drug interactions: SSRis/TCAs, meperidine

- Avoid tyramine (cheese, beer)

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15
Q

Etacopone:
MOA
Does it cross BBB?
Therapeutic Use

A

NO cross BBB (Inhibits peripheral COMT)
Parkinson’s: Prevents 3-OMD formation competitive inhibition w/ L-DOPA for entry @ BBB

Therapeutic Use:
w/ sinemet only for “wearing off”
*alone dopamine formation in periphery

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16
Q

Tolcapon:
MOA
Does it Cross BBB?
Therapeutic Use

A

YES cross BBB (Inhibits peripheral & CNS COMT)
Parkinson’s: Prevents 3-OMD formation competitive inhibition w/ L-DOPA for entry @ BBB

Therapeutic Use:
w/ sinemet only for “wearing off”
*alone dopamine formation in periphery

17
Q

Amantadine

A

Antiviral used to treat parkinsons; increases dopamine and NE

18
Q

What is the salient side effect associated with Etacapone use?

A

Delayed Diarrhea 2-12 weeks

19
Q

Why is Tolcapone discontinued after three weeks without symptomatic improvement?

A

Fulminating Hepatic Necrosis; remove drug from regimen after 3 weeks if no symptomatic improvement

20
Q

Typical Antipsychotics used to treat Huntington’s (2)

A

CHLORPROMAZINE

HALOPERIDOL

21
Q

Atypical Antipsychotics Used to treat Huntington’s Disease (2)

A

RISPERIDOME

OLANZAPINE

22
Q

Reserpine:
MOA
Therapeutic Use
ADRs

A

Inhibits uptake of dopamine into vesicles cytosolic–> Increases metabolism of dopamine
Huntingtons: mild chorea

ADR: MAOI’s; QT prolonging agents (increase efficacy)

23
Q

Absolute contraindications to Reserpine Use

A

actively suicidal/ depressed patients

24
Q

BACLOFEN:
MOA
Metabolism
Therapeutic Use

A

Muscle relaxant used to treat spasticity in Huntington’s Disease and MS

*Limited metabolism, low and slow in brain

25
Q

ADRs with Baclofen

Which population of patients is most sensitive to the drug’s effects?

A

Drug Interactions:
All depressant drugs (benzos, ETOH, etc.)
*Elderly more prone to effects.

26
Q

Riluzole:
Metabolism + Contraindications
Therapeutic Use

A

Hepatic Metabolism CYP1A2
Contraindications: hepatic impairment
Prolongs time before need for life support in patients with ALS

27
Q

AchE Inhibitors used to treat Alzheimer’s Disease

A
  1. Tacarine
  2. Donepazil
  3. Rivastigmine
  4. Galantamine
28
Q

What is a possible side effect to using AchE inhibitor to treat Alzheimer’s Disease? How might you combat this problem?

What are 2 possible ADRs asstd. with AchE Inhibitors?

A

Insomnia- Give Dose Early, titrate

Avoid succinylcholine/ NSAIDs

29
Q

How do AchE Inhibitors help treat Alzheimer’s disease?

A
  • 40-70% inhibition Early cognitive improvement

- Slow course of disease

30
Q

MEMANTINE:
MOA
Therapeutic use
How is it excreted?

A

NMDA Antagonist; Bings Mg site to block Ca++ channel
Used to treat Alzheimers

Excreted in Alkalized urine, so avoid carbonic anhydrase inhibitors or any other drug that might decrease using pH

31
Q

Methylene Blue:
MOA
Weird side effect

A

Strong MAOI

Alzheimers patients may get this over the counter and it will turn their urine funny colors

32
Q

IFNS:
MOA
Therapeutic Use
Side effects

A

Change cytokine profile in brain + Strengthen BBB
Treat RRMS
Flu symptoms

33
Q

Glatramir:
MOA
Therapeutic Use
Side Effects

A 
Angelically similar to myelin basic protein--> Stimulates bystander effects 
Treats RRMS (w/ IFN)

Pain, anxiety, weakness, chest pain

34
Q

Mitoxantrone:
MOA
Therapeutic use
How is it administered?

A

Antineoplastic agent used to treat aggressive and unresponsive RRMS
IV admin every 3 mos

35
Q

Natiluzamab:
MOA
Therapeutic Use
Side Effect*

A

Monoclonal Ab against alpha 4 integrins on lymphocytes
Treats RRMS (second line agent)
IV infusion every 4 weeks
Reduces size of lesions

ADR: PML*

36
Q

Methylprednisone:
MOA
Therapeutic Use
Side Effect*

A

Decreases Inflammation, suppresses immune system,
Tightens BBB
Treats Acute Attacks in Progressive MS; reduces relapse

ADR: Cushings

Nervous System Pharmacology (3 decks)

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