Parkinson's Drugs Flashcards

Dopaminergic Therapies

1
Q

List of drugs for Parkinson’s Disease

A

Dopamine Agonists
1. Levodopa/Benserazide
2. Levodopa/Carbidopa

Ergot-derived Dopamine Agonists: Bromocriptine

Non-ergot derived Dopamine Agonists:
1. Ropinirole
2. Pramipexole
3. Rotigotine

Irreversible MAO-B Inhibitor:
1. Selegiline
2. Rasagiline

Reversible COMT Inhibitor: Entacapone

NMDA Antagonist: Amantadine

Other Combination medications: Stalevo (Levodopa, Carbidopa, Entacapone)

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1
Q

Levodopa / Carbidopa Formulations used mainly in NUH and Max dosing

A

250/25 mg Tablet (Credanil)

Max dose: 8 tablets/day (Levodopa 2 g/day, Carbidopa 200 mg/day)

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2
Q

Levodopa/Benserazide Formulations used mainly in NUH

A

250 mg Tablet (Madopar)

Max dose: Levodopa
- 1200 mg/day for 1st year (6 tabs/day)
- 600 mg/day for subsequent years (3 tabs/day)

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3
Q

Counseling points for levodopa: How to take?

A
  1. Empty stomach (But can take with light snacks if irritated)
  2. Take on time to maintain the effect of medication
  3. Avoid high-protein diet while taking levodopa
  4. Other DDIs:
    - Space apart 2 hours: Iron, pyridoxine
    - Alternatives to consider for Metoclopramide, sulpiride
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4
Q

Counseling points for levodopa: ADRs?

A
  1. Orange coloration in body fluids (Harmless)
  2. Low BP
  3. Uncontrolled movement (On-off phenomenon, wearing off effect)
  4. Nausea, vomiting
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5
Q

What is the role of benserazide and carbidopa?

A

Prevent peripheral conversion of levodopa in the bloodstream so that more levodopa can enter the brain

This also reduces the side effects of nausea, vomiting

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6
Q

Ropinirole formulation and dosing

A

Form:
- 0.25 mg, 1 mg, 2 mg Tablets
- PR 2 mg, 4 mg Tablet (Requip PD)

IR: 0.25 mg TDS initially, then increase every 7 days
Max: 24 mg/day, 3 divided dose
Usual dose: 12 to 16 mg/day

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7
Q

Pramipexole formulation and dosing

A

Form
- 0.125 mg (Immediate)
- 0.375 mg (Extended)

IR: 0.125 mg TDS increase every 7 days up to 4.5 mg/day
ER: 0.375 mg QD up to 4.5 mg/day

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8
Q

Rotigotine Formulation and Dosing

A

Formulation
2 mg/24 hours
4 mg/24 hours
6 mg/24 hours
8 mg/24 hours

Dosing:
Early stage: Start with 2 mg
Advanced-stage: Start with 4 mg
Do not discontinue abruptly, decrease by 2 mg/24 h EOD

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9
Q

Bromocriptine Formulation and Dosing

A

Form: 2.5 mg Tablet

Dosing:
- Usual PD dose: 1.25 mg BD then 2.5 mg QD in 2-4 week interval
- Absolute max dose: 100 mg/day

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10
Q

ADRs of dopamine agonists (ergot/non-ergot)

A

Dopaminergic:
1. Nausea, vomiting
2. Orthostatic hypotension
3. Leg or arm swelling

Non-dopaminergic:
1. Hallucination, agitation
2. Compulsion (Urges)
3. Sleep attacks (Sudden)

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11
Q

MAO-B Inhibitors Place in therapy and dosing

A

Selegiline 5 mg tablets (Max: 1 tab BD)

Indication:
- PD adjunct
- PD monotherapy in young
- MDD

Rasagiline 1 mg tablets (Max: HALF to 1 tab QD)

Indication:
- PD adjunct
- PD monotherapy

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12
Q

What is the special point about selegiline dosing, relating to the ADR?

A

Take one dose in the morning and one in the afternoon (Liver metabolism to amphetamine causing difficulty sleeping)

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13
Q

What are the other ADRs of selegiline and the rationale?

A

MAO plays a major role in breaking down DA, 5HT, NE and epinephrine

  1. Nausea, abdominal pain, constipation, diarrhea (5HT)
  2. Low BP (NE)
  3. Dry mouth

Rare: Hallucinations

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14
Q

Entacapone formulation, place in therapy and dosing

A

Form: 200 mg Tablet

Indication: PD adjunct to levodopa (increase the effect of levodopa)

Maximum: 1600 mg/day

May need to reduce L-dopa dose

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15
Q

ADR to counsel to patients for entacapone

A

Red-brown urine (harmless)

NVD

Drowsiness

Hallucinations, compulsions

16
Q

DDIs of entacapone

A

Iron supplements (2h apart)

Some Antidepressants (e.g. Paroxetine, Moclobemide, Venlafaxine)

17
Q
A