Antiparkinson Drugs Flashcards

1
Q

Parkinsonism refers to the presence of ________, ______and ________ (slowness of movement). Collectively, these 3 make up the 3 cardinal features of Parkinson’s Disease.

A
  1. rest tremors
  2. rigidity
  3. bradykinesia
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2
Q

Young-onset PD starts at age ____, affects 5-10% of PD patients

A

21-40

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3
Q

Juvenile-onset PD starts before age ___ years. Higher frequency of _____ PD amongst this group

A
  1. 20

2. genetically inherited

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4
Q

All types of PD share a common mechanism: Impaired clearing of _______ proteins by _______ system. This can lead to the accumulation of aggresomes and apoptosis.

A
  1. abnormal/damaged intracellular

2. ubiquitin-proteasomal

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5
Q

Characteristic ______ (≈ aggresome), containing α-synuclein and ubiquitin are seen in PD.

A

Lewy bodies

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6
Q

In PD, there is degeneration of _______ neurons with Lewy body inclusions in substantia nigra, which has _______ projections to _______ (Facilitates and modulates motor movements initiated by motor cortex).

A
  1. dopaminergic
  2. dopaminergic
  3. basal ganglia
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7
Q

There are no reliable diagnostic markers for PD. Diagnosis and diagnostic criteria are based on the _______ of clinical features, and the _______ of alternative diagnoses

A
  1. presence

2. exclusion

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8
Q

PD is the main cause of parkinsonism, but _____% of patients with parkinsonian syndromes do not have PD. Common differential diagnoses are the atypical parkinsonian disorders

A

10-25

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9
Q

Common* non-motor manifestations for PD include autonomic, _______, ______ and _____ manifestations. They are more prominent in later stages of PD.

*as many as 88% with 1 sx, 11% with 5 sx

A
  1. neuropsychiatric (similar to Alzheimer’s)
  2. olfactory
  3. sensory
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10
Q

Non-motor manifestations of PD are relatively resistant to, and may be worsened by _____ agents. They cause significant disability and are often neglected in PD management.

A

dopaminergic

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11
Q

PD is a progressive disorder and rate of disability progression is most marked in the ____ years of the disease. Significant disability can happen 10-15 years after onset.

A

early

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12
Q

The key treatment principle for PD is to 1. _______ treatment and to 2. ______.

A
  1. individualize

2. start low, go slow

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13
Q

Patients with early symptomatic disease without complications may not even need _______ if coping well. The preferred plan includes physiotherapy and exercise, healthy balanced diet, providing knowledge on disease and social support.

A

oral medications

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14
Q

The 4 main classes of oral medications used in PD are – _______ agents (eg Artane)
– _______ inhibitors (eg Selegiline)
– _______ agonists (eg Bromocriptine)
– _______ (eg Madopar)

A
  1. Anticholinergic
  2. MAO-B / COM-T
  3. Dopamine
  4. Levodopa
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15
Q

The ‘Gold standard’ in PD treatment is _______ (dopamine precursor). It may come in 2-in-1 preparations with ________ inhibitors to increase dopamine conversion in brain.

A
  1. Levodopa

2. peripheral decarboxylase

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16
Q

Levodopa is available as regular form or long acting form (HBS or CR).
Brand names:
– Levodopa + benserazide: ______
– Levodopa + carbidopa: ______

A
  1. madopar

2. sinemet

17
Q

Levodopa has serious long term side effects such as ________ and _______ (10%/yr), which persists even after lowering levodopa dose.

A
  1. motor fluctuations

2. dyskinesia

18
Q

To prevent long term side effects of levodopa, we have to ______ as much as possible. (i.e. use _____ medications)

A
  1. lower its dose

2. adjunct

19
Q

Trihexyphenidyl (Artane) is an anticholinergic agent with side effects such as Dry _____, sedation, ______, _____ retention, delirium, confusion, hallucinations (especially in elderly).

A
  1. mouth
  2. constipation
  3. urinary
20
Q

Trihexyphenidyl (Artane) has 2 advantages in that it may be effective in controlling ____ and that peripherally acting agents may be useful in treating ______ .

A
  1. tremor

2. sialorrhea (excessive salivation)

21
Q

Trihexyphenidyl (Artane) dose is ____mg/day. It may be used as symptomatic ________ or as an adjunct to _______ to treat tremors and stiffness in Parkinson’s disease.

A
  1. 2 - 15
  2. monotherapy
  3. levodopa
22
Q

Selegiline (Jumex®) is a ______ that reduces breakdown of dopamine. It has mild antiparkinson activity but laboratory studies suggest that it may delay the ________ (potential disease modifying effect).

A
  1. MAO-B inhibitor

2. nigral brain cell degeneration

23
Q

Side effects of Selegiline (Jumex®) include: heartburn, loss of _____, nausea, constipation, dizziness, anxiety, headache, palpitation, ______, confusion, ______, visual hallucination.

A
  1. appetite
  2. insomnia
  3. nightmares
24
Q

Selegiline (Jumex®) is efficacious as a symptomatic ________ and may be used in ____ stages of Parkinson’s disease.

A
  1. monotherapy

2. early

25
Q

Entacapone (Comtan®) and Tolcapone (Tasmar®) are _______ (COMT) inhibitors that block an enzyme that converts levodopa into an _____ form. This allows more levodopa to enter the brain.

A
  1. Catechol-O-methyltransferase

2. inactive

26
Q

Entacapone (Comtan®) and Tolcapone (Tasmar®) increases ______ of each dose of levodopa, beneficial in treating “wearing off” responses (i.e. when the duration of action for levodopa gradually reduces). But they are only effective if used with ______.

A
  1. duration

2. levodopa

27
Q
COMT inhibitors' side effects include: 
– increase abnormal movements (dyskinesias)
– \_\_\_\_\_ dysfunction (Tolcapone Tasmar®)
– nausea, diarrhea
– \_\_\_\_\_ discoloration
– visual hallucinations
– daytime drowsiness, \_\_\_\_\_ disturbances
A
  1. liver
  2. urinary
  3. sleep
28
Q

Dopamine agonists can be used as both adjunct or monotherapy with Antiparkinsonian effects ________ compared to levodopa. It can prevent or delay onset of ______________.

A
  1. not superior

2. motor complications

29
Q

Dopamine agonists such as ______ and _______ can cause somnolence while Pergolide can cause ______ disease as an side effect.

A
  1. ropinirole
  2. pramipexole
  3. restrictive valvular heart
30
Q

Dopamine agonists have similar side effects as Levodopa but also include other side effects such as ______ and _______. As ‘ergot’ derivatives, they can cause ______ in regular users.

A
  1. pedal edema
  2. arrhythmia
  3. fibrosis
31
Q

In younger Parkinson’s disease patients, therapy should commence first with ________ rather than ______, due to milder side effects.

A
  1. dopamine agonists

2. levodopa

32
Q

Dopamine agonists are efficacious as symptomatic ________ and may also be used as an adjunct to ________ in the treatment of Parkinson’s disease

A
  1. monotherapy

2. levodopa

33
Q

Amantadine is an antiviral agent, accidentally discovered to have mild antiparkinsonian effect (tremor, rigidity, bradykinesia, dyskinesia). It is given as ______________ to levodopa.

A

monotherapy or adjunct

34
Q

Amantadine may be considered as therapy to reduce dyskinesia in patients with Parkinson’s disease who have motor fluctuations as it has _______ effects.

A

Anti-dyskinetic

35
Q

Amantadine works via:

  1. Enhance release of stored _______
  2. Inhibit presynaptic uptake of ________
  3. _____ receptor agonist
  4. ______ receptor antagonist (anti-glutamate)
A
  1. dopamine
  2. catecholamine
  3. Dopamine
  4. NMDA
36
Q

The usefulness of Amantadine is limited by the need to screen pts for hx of _______ symptoms. ______ limit its use in advanced disease.

A
  1. seizures/psychiatric

2. Side effects

37
Q

The side effects of Amantadine include: ________ (inability to concentrate), hallucination, insomnia, nightmares, ________ (Venule swelling due to thromboses, mottled reticulated discoloration of limbs).

A
  1. Cognitive impairment

2. livedo reticularis

38
Q

The CNS side effects of Amantadine are likely due to ________ and ________ activity and to a lesser extent its _______ activity

A
  1. dopaminergic
  2. adrenergic
  3. anti-cholinergic
39
Q
Brand names of Dopamine agonists:
– Bromocriptine (\_\_\_\_\_\_)
– Pergolide (Celance®, Permax®)
– \_\_\_\_\_\_\_ (Trivastal Retard®)
– Ropinirole (\_\_\_\_\_\_)
– \_\_\_\_\_\_ (Sifrol®)
A
  1. Parlodel®
  2. Piribedil
  3. Requip®
  4. Pramipexole