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Neuromusculoskeletal & Psychiatry II Exam #2 > Drugs for Movement Disorders > Flashcards

Drugs for Movement Disorders Flashcards

1
Q

MOA: “-dopa”

A

Levodopa and combinations

Levodopa
Carbidopa

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2
Q

What are the DA receptor agonists? (4)

A

Apomorphine
Bromocriptine
Pramipexole
Ropinirole

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3
Q

What are the MAO inhibitors used for Parkinson’s? (3)

A

Rasagiline
Selegiline
Safinamide

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4
Q

What are the catechol-O-methyltransferase inhibitors? (2)

A

Entacapone

Tolcapone

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5
Q

What are the anticholinergic drugs used in Parkinson’s? (5)

A 
Benztropine
Biperidin
Orphenadrine
Procyclidine
Trihexyphenidyl
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6
Q

What is the use of Carbidopa when used with Levodopa?

A

It is a DOPA decarboxylase inhibitor, thus it ensures that a greater amount of Levodopa crosses the BBB unscathed.

-reduces daily Levodopa needs by 75%

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7
Q

When is Carbidopa most effective?

A

The first few years of treatment.

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8
Q

What “phenomenon” can ensue after use of Levodopa?

How many people respond to the drug?

A

“Wearing-off” phenomenon: each dose of Levo effectively improves mobility for a period of time (12 hrs.), but rigidity and akinesia returns rapidly at the end of the dosing interval.

1/3 respond well, 1/3 respond less well, 1/3 are unable to take the medicine or don’t respond at all

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9
Q

What is a significant side-effect of Levodopa if not taken with Carbidopa?

A

GI-related: anorexia, nausea, vomiting (+ of chemoreceptor trigger zone) in 80% of patients.

If taken w/ Carbidopa, there is less risk for Gi-related problems.

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10
Q

What side-effects (aside from GI-related) are associated with Levodopa? (4 + GI)

A

CV effects - postural hypotension (often diminishes w/ repeated treatment). HTN may occur if taken in large doses or in combo w/ nonselective MAOIs/sympatheticomimetcs.

Dyskinesias - occurs in 80% of patients. Choreoathetosis of the face and distal extremities.

Behavioral effects - depression, anxiety, agitation, insomnia, etc. Atypical antipsychotics can help counteract behavioral problems.

Fluctuations in response and the “off and on” response.

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11
Q

What can help patients experiencing the “off and on” phenomenon?

A

Apomorphine

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12
Q

What are the contraindications of Levodopa use? (5)

A

Patients taking MAOIs (or within 2 wks. of discontinuation) may cause a HTN crisis.

Psychotic patients

Patients w/ closed-angle glaucoma

Patients with a history of melanoma/skin lesions

Use w/ caution in patients with active PUD

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13
Q

What is the indication for use of DA receptor agonists in patients taking Levodopa/Carbidopa?

A

End-of-dose akinesia or on-off phenomenon

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14
Q

What is the benefit of DA receptor agonists?

A

Less incidence of fluctuations and dyskinesias with long-term Levo therapy

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15
Q

What is the MOA of Bromocriptine?

What is it indicated for in addition to PD?

What is the unique problem with it?

A

Ergot alkaloid derivative that is a D2 agonist.

Endocrine disorders.

Extensive first-pass metabolism (28% bioavailability).

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16
Q

What is the MOA of Pramipaxole?

What is it indicated before in addition to PD?

In which patients must dosage be adjusted?

A

Affinity for D3 receptors.

Moderate to severe RLS.

Patients w/ renal insufficiency.

17
Q

What is the MOA of Ropinirole?

What is it indicated for in addition to PD?

A

Affinity for D2 receptors.

RLS.

18
Q

What are the adverse-effects of DA receptor agonists? (4)

A

GI-related (reduced if taken after meals).

CV effects

Dyskinesias - similar to Levo.

Mental disturbances - confusion, hallucinations, delusioms.

19
Q

What are the contraindications for DA receptor agonists? (4)

A

Psychotic illness

Recent MI

Active PUD

Peripheral vascular disease - vasoconstricting effects

20
Q

What does MAO-A and MAO-B preferentially metabolize?

A

MAO-A: NE and serotonin

MAO-B: phenylethylamine and benzylamine

DA and tryptamine are metabolized equally by the two.

21
Q

What is the MOA of Selegiline, Rasagiline and Safinamide?

What is the problem with it in terms of PKs?

In which patients should it be cautioned to take these drugs?

A

MAO-B inhibitor (will inhibit MAO-A at high doses); slows breakdpwn of DA and prolongs the antiparkinsonian effects of Levo.

10% bioavailability with peak plasma concentraion within an hour.

Patients taking Meperidine
Patients taking TCAs
Patients taking SSRIs (risk of serotonin syndrome)

22
Q

What can cause a HTN crisis in a patient taking Levo?

A

If coadministered with a non-selective (A + B) MAO inhibitor.

23
Q

What is the effect of inhibiting COMT?

How does it improve Parkinsonian symproms?

A

COMT metabolizes Levo to 3-O-methyldopa, which competes with Levo for transport in the intestines and across the BBB.

It inhibits peripheral metabolism, which decreases clearance and increases bioavailability.

24
Q

Which COMT inhibitor is central and peripheral acting?

Which is only peripheral acting?

A

Tolcapone

Entacapone

25
Q

What are the side-effects of COMT inhibitors? (4)

A

*Levodopa-like side-effects

Orange urine

Diarrhea/abdominal pain

Sleep disturbances

26
Q

What is the MOA of Apomorphine?

What is it best used for?

What are its adverse-effects?

A

DA agonist at D2 receptors.

SubQ injections for quick and temporary relief of akinesia in patients on DA therapy.

Nausea, dyskinesias, drowsiness, sweating, hypotension and injection-site bruising.

27
Q

What is Trimethobenzamine used for?

A

Pretreatment antiemetic for patients who need Apomorpine

28
Q

What is Amantadine?

What are the side-effects?

A

An antiviral agent whose MOA in parkinsonism is unknown.

Livedo reticularis in legs (purplish skin)
Mood changes
HA, HF and postural hypotension

29
Q

What do mAChR antagonists treat primarily in PD?

A

Tremor and rigidity, but little effect on bradykinesia.

Anticholinergic-like: sedation, confusion, constipation, urinary retention, blurred vision, etc.

30
Q

Which 2 drugs treat HD?

A

Reserpine and Tetrabenazine

31
Q

What is the only drug known to impact survival in ALS?

What is the MOA?

What are major side-effects?

A

Riluzole

Inhibition of glutamate release and blockage of NMDA and kainite glutamate receptors and VG Na+ channels.

Nausea and weakness.

Neuromusculoskeletal & Psychiatry II Exam #2 (15 decks)

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