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Pharma 3: Treatment Of Parkinsons Flashcards

1
Q

Levodopa

Precursor of:

A

Precursor of dopamine which crosses BBB

Dopamine is peripheral product of levodopa

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2
Q

LEVODOPA

T1/2 and consequence on dose

A

T1/2 very short (1-2hrs)—> fluctuations in plasma concentration

There4 need large doses

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3
Q

LEVODOPA

Adverse effects

A
  1. Dyskinesia ie involuntary movements result from:OVERACTIVITY of dopamine on receptors of basal ganglia
  2. “On-off)” effects due to t1/2–>fluctuations in plasma concentrations
  3. N/V + anorexia due to stimulation of CHEMORECEPTOR ZONE OF MEDULLA
  4. Tachycardia due to dopaminergic effects on heart
  5. Behavioral changes eg, confusion + hallucinations similar to schizophrenia due to increased dopamine activity in brain
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4
Q

How do you optimize levodopa treatment

A

Combining it with drugs that enhance central effects and MINIMIZE PERIPHERAL EFFECTS.

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5
Q

Dopa decarboxylase inhibitors MOA

A

They decrease dopa metabolism peripherally and its metabolism in GI leading to fewer side effects by inhibiting dopa decarboxylase

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6
Q

Dopa decarboxylase inhibitors

A

Carbidopa

Benserazide

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7
Q

Result of taking levodopa with Carbidopa/Benserazide

A
  1. Minimize PERIPHERAL SE ONLY (arrhythmia, nausea) ie Dyskinesia still present
  2. Use dopa at lower dose (80%less)
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8
Q

Carbidopa/Benserazide adminstration

A

Orally with levodopa

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9
Q

Peripherally acting dopamine ANTAGONIST

A

DOMPERIDONE

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10
Q

Domperidone MOA

A

Peripheral Dopamine antagonist that does NOT cross bbb but can act on the chemoreceptor trigger zone (outside bbb) to prevent Nausea + anorexia

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11
Q

Domperidone useful for

A
  1. Nausea
  2. Headache
  3. Dizziness
  4. Dry mouth
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12
Q

MAO-B inhibitor

A

SELEGILINE

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13
Q

Selegiline MOA

A

Selectively blocks MAO-B to selectively inhibit dopamine metabolism in brain

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14
Q

Effect of Selegiline

A

Reduces motor complications of Levodopa

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15
Q

SELEGILINE administration

A

Orally with levodopa-carbidopa

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16
Q

Selegiline metabolism

A

Metabolized into amphetamine and methamphetamine—>cause insomnia if taken later than mid afternoon

17
Q

Selegiline can possibly

A

Neuroprotective ie slow progression of newly diagnosed patients

18
Q

COMT inhibitor

A

Entacapone

Tolcapone

19
Q

Entacapone/Tolcapone

MOA

A

When peripheral dopamine decarboxylase is inhibited by CARBIDOPA, a byproduct; 3-0methyldopa is formed. 3-0-methyldopa competes with levodopa for actuve transport into CNS.

Nutshell: levodopa+carbidpoa—

20
Q

Entacapone/tolcapone

Effect

A

Reduce symptoms of “waring off” in patients taking levodopa-carnidopa

21
Q

Entacapone/tolcapone

Administration

A

Orally

With levodopa-carbidopa +/- selegiline

22
Q

Entacapone/tolcapone

Adverse effects

A
  1. Postural hypotension
  2. Nausea
  3. Anorexia
  4. Dyskinesia
  5. Hallucinations
  6. Sleep disorders

“Similar to levodopa-carbidopa”

23
Q

Levodopa’s effect on dopaminergic neurotransmisison

A

Enhances it by enhancing synthesis of dopamine in surviving substansia nigra cells

24
Q

Pros of DOPAMINE RECEPTOR AGONISTS

A
  1. Duration of action > levodopa
  2. Can be used as a single agent early in disease or with levodopa/carbidpoa in later stages
  3. Effective in early treatment of motor symptoms of pd
  4. Controls motor fluctuations associated with levodopa (newer drugs are at less risk of causing motor dyskinesia)
25
Q

Pramipexole + Ropinirole

MOA

A

Potent agonists of D2 receptors

26
Q

Pramipexole and Ropinirole

Administration

A

Added to levodopa if levodopa ineffective or to prevent on off fluctuations

27
Q

Pramipexole and Ropinirole

Adverse effects

A

Less likely to cause dyskinesia

*CAN CAUSE:

  1. Hallucinations
  2. Confusion
  3. SWELLING OF ANKLES
  4. COMPULSIVE BEHAVIOR eg uncontrolled shopping and eating
28
Q

Rotigotine

MOA

A

Dopamine receptor agonist

29
Q

Rotigotine

Administration

A

Once daily transdermal patch changed every 24 hrs

30
Q

Rotigotine

Side effects

A

Mild skin irritation that can be avoided by rotating the sites of adhering the patch

31
Q

Apomorphine

MOA

A

Dopamine receptor agonist

32
Q

Apomorphine administration

A

Self injectable (up to five times a day)

AS A RESCUE for advanced pd or sever “off” episodes

33
Q

Apomorphine side effects

34
Q

Amantadine MOA

A

Increases dopamine release AND blocks cholinergic receptors

35
Q

Amantadine administered

A
  1. Prescribed alone for short term relief of mild ie early pd
    • Carbidopa/levodopa during late stages to control the dykinesias caused by carbidopa/levodopa

“Less effacious than levodopa or ropinirole ie only for mild reflief”

36
Q

Amantidine adverse effects

A
  1. Purple mottling of skin
  2. Ankle swelling
  3. Restlessness
  4. Agitation
  5. Confusion
  6. Hallucinations
  7. At high dose—> acute toxic psychosis
37
Q

MUSCARINIC ACETYLCHOLINE RECEPTOR ANTAGONIST

A

Atropine

Benztropine—> less peripheral effects than atropine

38
Q

Atropine, Benztropine

Therapeutic use

A

Less than levodopa

Reduce tremor more than rigidity and bradykinesia

+SIDE EFFECTS

There4 used in pts on antipsychotic drugs, which are dopamine antagonists

39
Q

Benztropine

Side effects

A
  1. Dry mouth
  2. Constipation
  3. Impaired vision
  4. Urinary retention

CNS (28 decks)

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