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DT II Exam 1 > Egleton: Movement Disorder Drugs > Flashcards

Egleton: Movement Disorder Drugs Flashcards

1
Q

Parkinsonism causes

A

Dopaminergic tract: Substantia nigra
Genetics, Environment, MPTP
Oxidative stress theory

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2
Q

Levodopa (L-Dopa):definition

A

For Parkinson
Dopamine precursor
GI absorption
Peripheral decarboxylation

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3
Q

Levodopa: actions

A

Decrease rigidity and tremor

Alleviate motor dysfnction

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4
Q

Levodopa: ADR

A

Occasional psychotic symptoms
Dyskinesia
On-Off phenomenon

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5
Q

Levodopa: contra

A

MAOI (14 days)
Narrow angle glaucoma
Avoid high protein/ high B6 (Pyridoxine) {promote decarboxylation]
Rapid discontinuation [confusion, rigidity, fever, autonomic dysfunction]

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6
Q

Carbidopa

A

For Parkinson
Inhibitor of Aromatic L-amino acid decarboxylase
Doesn’t cross BBB
Decrease peripheral side effects of L-Dopa
Reduce L-Dopa dose (x10)
No side effects

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7
Q

Entacapone: action

A

Inhibit metabolism of L-Dopa to 3-OMD (only peripheral)
Increase L-Dopa blood level
3-OMD= Competitive substrate for LNAA (increase brain uptake)
Adjunct to Leveodopa/ Carbidopa

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8
Q

Entacapone: ADR

A

Delayed diarrhea

Hallucination (unique)

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9
Q

Talcapone: action

A

For Parkinson
Inhibit metabolism of L-Dopa to 3-OMD (both peripheral and brain)
Increase L-Dopa blood level
Increase CNS uptake of L-Dopa
Decrease frequency of On-Off phenomeon
3-OMD= Competitive substrate for LNAA (increase brain uptake)
Adjunct to Leveodopa/ Carbidopa

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10
Q

Talcapone: ADR

A

Fulminating hepatic necrosis
If no improvement after 3wk, discontinue
Black box warning

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11
Q

Selegiline/ Rasagiline

A 
For Parkinson 
Monoamine oxidase B inhibitors
Inhibit MAO-B only (only in Brain)
Increase Dopamine level
Reduce DOPAC (reduce ROS in MPTP model)
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12
Q

Selegiline

A

Reduces L-Dopa dose when used together (Ameliorates on-off)
Less hypertensive crisis (if high dose= inhibit MAO-A too)
Metabolized to Amphetamine [potentiating effect of DA in brain]

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13
Q

Selegiline: contra

A

Avoid Meperidine
Avoid TCA and SSRI (serotinin syndrome)
Avoid Tryramine foods (cheese, wine, beer, red meat)

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14
Q

Rasagiline

A

For Parkinson
More potent than Selegiline
Can be used as monotherapy in early stage Parkinson
Adjunct therapy with Levodopa/ Carbidopa in advanced patients
Similar ADR with Selegiline

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15
Q

Bromocriptine

A

For Parkinson
D2 agonist, weak partial D1 agonist
Ergot derivative= Valvular heart disease
Used with L-Dopa

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16
Q

Pramiprexole

A 
For Parkinson
D3 agonist
Not Ergot derivative
Rapid oral absorption
Renal excretion (lower dose for renal defect)
Monotherapy for mild Parkinson
Adjunct with Levodopa [reduce fluctuations and Levodopa dose]
Treat Restless leg syndrome
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17
Q

Pramiprexole: ADR

A

Orthostatic hypotension, Nausea, Hallucination, Insomnia, Diziness, Constipation

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18
Q

Ropinirole

A

For Parkinson
D2 agonist
Extended release formulation (Roprinrole XL)
Effective monotherapy for mild Parkinson
Adjunct for advanced or response fluctuations

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19
Q

Apomorphine

A

For Parkinson
Dopamine agonist
Subcutaneous
Rapid intake to brain (fast, 10 min)
Rescue to treat Off
Nausea (control with Trimethobenzomide, 3 days prior, continue for a month)
Avoid Serotonin agonist and Dopamine angatonist

20
Q

Pergolide

A

For Parkinson
D1 and D2 agonist
Ergot derivative (Valvular heart disease)
More effective than Bromocriptine (D1 and D2 agonist)
WIthdrawn

21
Q

Rotigone

A 
For Parkinson
Dopamine receptor agonist
Skin patch
Minimize On-Off
Withdrawn because of crystal formation at site of patch
22
Q

Amantadine

A

Used for Parkinson and Drug induced extrapyramidal symptoms
Antiviral drug
Enhance DA synthesis and release
Inhibit reuptake

23
Q

Amantadine: ADR

A

For Parkinson
Restlessness, Agination, Confusion, Orthostatic hypotension, Urinary retention, Hallucination, Dry mouth
Acute toxic psychosis when high dose
Less efficacious than L-Dopa/ Less side effects tho
More effective for rigidity and Bradykinesia than anticholinergics
Used in early stage or L-Dopa supplement

24
Q

Antimuscarinics

A

Trihexyphenidyl, Benztropine, Biperiden
Used before L-Dopa for Parkinson
ADR: Cycloplesia, Constipation, Urinary retention, Confusion, Delirium, Hallucinations

25
Q

Reserpine/ Tetrabenazine

A

Used for Huntington’s mild chorea
Block Dopamine reuptake in presynaptic vesicle
(Reduce dopamine released)
ADR: dopamine deficiency related

26
Q

Reserpine/ Tetrabenazine: drug interaction

A

Enhance QTc prolongation drug effect
Enhance CNS depressants
MAOI

27
Q

Reserpine/ Tetrabenazine: contra

A

Suicidal/ Depression
Liver problem
MAOI use (14 days)
Reserpine use w/in 20 days

28
Q

Chlorpromazine, Haloperidol

A

DA antagonists
Antipsychotics
For severe chorea and psychosis treatment

29
Q

Balclofen

A 
For Huntingon AND MS
Antispasmodic, GABA B agonist
Muscle relaxant (hyperpolarize primary afferent fiber terminals)
Slow metabolism, Low and slow for brain
Spasticity of MS reduced
30
Q

Baclofen: ADR

A

Drowsiness, vertigo, dizziness, psychiatric disturbance, insomnia, slurred speech, ataxia
Muscle weakness

31
Q

Baclofen: drug interaction

A

Enhance CN depression (like alchohol)

32
Q

Balclofen: contra

A

Elderly (more CNS effects)

33
Q

Rilzole

A 
ALS treatment
Protect from Glutamate neurotoxicity
Inhibit Glutamic acid release
Noncompetitive bloc of NMDA receptor response
Direct effect on vol-dep Na channel

Prolong time before life support
Absorption decreased with fatty food (hepatic metabolism (CYP1A2)

34
Q

Rilzole: ADR

A

Neutropenia, etc

35
Q

Rilzole: contra

A

Hepatic impairment

Liver enzyme defect

36
Q

Tacrine, Donepezil, Rivastigmine, Galantamine

A

AChEI
Treat Alzheimer
Improve cognition, activation, mood, behavior
ADR: Insomnia, Anorexia, Diarrhea, Nausea, Fatigue, Muscle cramps
Treat in am to avoid insomnia
Titrate dose slowly for adjustment

37
Q

Tacrine, Donepezil, Rivastigmine, Galantamine: Drug interaction

A

Succinylcholine (increase muscle relaxation with neuromuscular blockage)
NSAIDs: increase stomach ulcers

38
Q

Memantine

A

For Alzheimer
NMDA antagonist
Binds to Mg site and block the channel
45% protein bound
Elimination reduced by high urine pH
ADR: Hypertension, Cardiac failure, TIA, Dizziness, Confusion, Headache
Drug interactino: CA inhibitor= inhibit excretion
Contra: avoid food/ drug that change urine pH

39
Q

Vitamin E

A

For Alzheimer
Slow progression
1000 IM twice daily

40
Q

Methylene blue

A

For Alzheimer
Strange pee color
Strong MAOI
For ich of fish (fungal infection)

41
Q

Interferon beta

A

For RRMS MS
Reduce BBB breakdown by inflammation
Bind T cell VLA-4, prevent adhesion to BBB endothelial cells
Inhibit T cell expression of MMP
Reduces T cell activation
Changes cytokine profile
ADR: Flu-like symptom, Elevated ALT and AST, UTI

42
Q

Glattiramer

A

For RRMS MS
Glutamic acid, Lysine, Alanine, Tyrosine (glat)
Imitate myelin basic protein
Induce Th2 cell effect to enter CNS
Mediate bystander suppression of inflammation of site
ADR: Vasodilation, chest pain, pain, anxiety, injection site rxn, Neuromuscular weakness, Infection

43
Q

Mitoxantrone

A

For RRMS/PMS MS
Anti-neoplastic agent
Suppress cellular and humoral immune response
Only for really worsening patient

44
Q

Natiluzamab

A

For RRMS MS
Antibody to Alpha-4 integrins on inflammatory lymphocytes and monocytes
Prevent binding to endothelial cells
Reduces CNS entry
Reduces new lesion and size by 83% but…
Cause PML***
(Progressive multifocal leukoencephalopathy)

45
Q

Methylprednisolone

A 
For PMS/ Acute relapse MS
Suppress immune response
Tighten BBB
First choice in acute relapse
Use in conjunction with other agents

DT II Exam 1 (5 decks)

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