Drugs for Neurodegenerative Disease Flashcards

1
Q

Malfunction of substantia nigra causes (hyper/hypo)kinetic

Which disease?

A

Hypokinetic

Parkinsonism

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2
Q

Malfunction of striatum causes (hyper/hypo)kinetic

Which disease?

A

Hyperkinetic

Huntington’s disease

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3
Q

What disease?

Involve muscle weakness and atrophy due to degeneration of motor neurons in spinal cord and cerebral cortex

A

Amyotrophic lateral sclerosis (ALS)

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4
Q

Alzheimer’s disease is due to degeneration of neurons in what parts of the brain?

A

hippocampus and cerebral cortex

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5
Q

Lewy bodies are characteristic of what disease?

A

Parkinson’s disease

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6
Q
Which of the following is a characteristic of Parkinson's disease?
A. Hyperkinesia
B. Intentional tremor
C. Muscular flaccidity
D. Mask-like face, shuffling gait
E. Unaffected speech
A

D

A. Bradykinesia
B. Resting tremor
C. Muscular rigidity
E. Impaired speech

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7
Q

D1 receptor controls ____ in the basal ganglia

A

direct pathway: accelerates movement

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8
Q

D2 receptor controls ____ in the basal ganglia

A

indirect pathway: slows movement

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9
Q

A reduction in dopamine acting at D1 and D2 causes

A

Inhibition of direct pathway

Activation of indirect pathway

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10
Q

Name the drugs that increase DA synthesis (3)

A

L-DOPA (levodopa)
Levodopa/Carbidopa (Sinemet)
Entacapone/Levodopa/Carbidopa (Stalevo)

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11
Q

Which of the following is TRUE about L-DOPA (levodopa)?
A. Poor oral availability
B. 8-10 hour half life
C. Good brain penetration
D. Metabolized peripherally by aromatic I-amino acid decarboxylase
E. Effect does not wane long term

A

D

A. Good oral availability: quick absorption from small intestine
B. Short half life: 1-2 hrs
C. Poor brain penetration (1-3%)
E. “Wearing off” effect after 3-5 years

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12
Q
Which of the following is NOT a side effect of L-DOPA?
A. Nausea/vomiting, anorexia 
B. Cardiac arrhythmias
C. Visual and auditory hallucination
D. Memory impairment
E. Dyskinesia
A

D

Also orthostatic hypotension and mood changes (depression, psychosis, anxiety)

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13
Q

Medication of choice for Parkinson’s

A

Sinemet (Levodopa/Carbidopa)

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14
Q

Aromatic I-amino acid decarboxylase inhibitor

A

Carbidopa

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15
Q

Name the drug:
o Blocks peripheral metabolism of L-DOPA → increase L-DOPA availability in brain
o Allow reduced dose of L-DOPA by 4-5x → reduce side effects of peripheral DA

A

Sinemet (Levodopa/Carbidopa)

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16
Q

Inhibitor of catechol-O-methyltransferase

A

Entacapone

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17
Q

Name the drugs that decrease DA catabolism (2)

A

Selegiline

Rasagiline

18
Q

Which of the following is TRUE about Selegilline?
A. Inhibits I-amino acid decarboxylase
B. IV administration
C. Liver excretion
D. Limits formation of neurotoxic free radical

A

D by decreasing production of byproduct of dopamine, hydrogen peroxide

A. Carbidopa does this. Selegilline inhibits monoamine oxidase type B
B. Oral administration
C. Renal excretion

19
Q

Used adjunctive w/ levodopa

A

Selegiline

Very little benefit when taken alone

20
Q

Is metabolized to methamphetamine and amphetamine causing insomnia

A

Selegiline

21
Q

What are the advantages of Rasagiline over Selegiline?

A

More potent

Not metabolized to amphetamine-like substance

22
Q

D2 agonist, D1 partial agonist

A

Bromocriptine

23
Q

D2, D3 agonist

A

Ropinirole

Pramipexole

24
Q

Name the dopamine receptor agonists (4)

A

Ropinirole
Pramipexole
Bromocriptine
Apomorphine

25
Q

Longer half life (6-8 hours) than L-DOPA so it reduces motor control fluctuation

A

Dopamine receptor agonists

26
Q

Emergency treatment of pts w/ advanced Parkinson’s for “off periods”

A

Apomorphine

27
Q

Apomorphine administration

A

SubQ injection

do NOT use IV –> would cause thrombus and PE

28
Q

Name the type of drug:
Benztropine
Trihexyphenidyl

A

Muscarinic antagonist

29
Q

Muscarinic antagonists (Benztropine, Trihexyphenidyl) used to alleviate what symptoms of Parkinsons?

A

Tremor and rigidity

NOT bradykinesia

30
Q

Amantadine used to alleviate what symptoms of Parkinsons?

A

Bradykinesia and rigidity

NOT tremor

31
Q

Used by patients with mild-moderate disease before using L-DOPA

A

Amantadine

32
Q

Name the drug:

Block cholinergic muscarinic receptors and glutamatergic NMDA receptors

A

Amantadine

33
Q
Which of the following is NOT a side effect of Amantadine?
A. Hallucinations, confusion
B. Nausea
C. Rash of upper extremities 
D. Dizziness
A

C. Rash of LOWER extremities

34
Q
Which of the following is NOT an AChE inhibitor
A. Donepezil
B. Memantine
C. Galantamine
D. Rivastigmine
E. Tacrine
A

B. Memantine is a NMDA receptor antagonist

35
Q

Which AChE inhibitor has the longest half life?

A

Donepezil (70 hrs)

36
Q

Which AChE inhibitor has the shortest half life?

A

Rivastigmine (1.5 hrs)

37
Q

AChE inhibitors used to treat

A

Alzheimer’s

38
Q

Donepezil, galantamine, tacrine is metabolized by ____

A

P450 liver enzymes

39
Q

Rivastigmine metabolized by ____

A

plasma cholinesterase

40
Q

All AChE inhibitors are overall safe except for ____

A

Tacrine: hepatotoxicity

41
Q

Type of drug:

Memantine

A

NMDA receptor antagonist –> protect neurons form Ca2+ overload, neuronal death