CNS - Parkinson's and neurodegenerative

Question 1

Selegine, Rasagiline

1. mechanism?
2. use?
3. Adverse effects?

Answer 1

1. inhibits Monoamine Oxidase B (dopamine)
2. Parkinson’s with Levodopa
3. Serotonin syndrome with SSRIs/ TCAs
   Insomnia, mood change, dyskinesias, GI distress

Question 2

Tolcapone, Entacapone

1. mechanism?
2. use?
3. Adverse effects?

Answer 2

1. COMT inhibitors (Levodopa -> 3OMD)
   - 3OMD competes for uptake to CNS with Levodopa
2. Adjunct to Levodopa-carbidopa
3. ORANGE urine, sleep disturbances, liver failure

Question 3

Treatment of Wilson’s?

Answer 3

Penicilamine (Dimethylcysteine)
- chelates copper

Trientine, tetrathiomolybdate has been used

Question 4

Restless leg syndrome treatment?

Answer 4

Dopaminergic therapy

• Pramipexole
• Ropinirole

(Benzos, Gabapentin)

Question 5

Mechanism and use of Memantine?

Answer 5

Neuroprotective agent:

NMDA receptor antagonist
- limits Ca2+ influx

use: ALzheimer

Question 6

Restless leg syndrome treatment?

Answer 6

Dopaminergic therapy

• Pramipexole
• Ropinirole

Question 7

Levodopa

1. mechanism?
2. use?
3. Adverse effects?
4. contraindication?

Answer 7

1. Dopamine precursor
2. Reduce symptoms & mortality in Parkinson’s
3. Nausea, vomiting, emesis, postural hypotension
4. Contraindicated if history of psychosis

Question 8

Bromocriptine

1. mechanism?
2. use?
3. Adverse effects?

Answer 8

1. ergot alkaloid partial D2 agonist
2. Parkinson’s - +- levodopa
3. Nausea, vomiting, dyskinesia, postural hypoT
   Hallucinations, confusion, delusions

Question 9

Pramipexole

1. mechanism?
2. use?
3. Adverse effects?

Answer 9

1. Non-ergot D3 agonist
2. Mild parkinson’s - alone
   advanced parkinson’s - with levodopa
3. anorexia, nausea, vomiting, postural hypoT

Question 10

Ropinirole

1. mechanism?
2. use?
3. Adverse effects?

Answer 10

1. non ergot D2 agonist
2. monotherapy / with levodopa
3. CYP1A2 interactions + like Pramipexole

Question 11

Apomorphine

1. mechanism?
2. use?
3. Adverse effects?

Answer 11

1. Potent dopamine agonist
2. subc. rapid temporaly relief of “off-periods”
3. Severe nausea (3d pretreat with antiemetic)

Question 12

Amantadine

1. mechanism?
2. use?
3. Adverse effects?

Answer 12

1. enhances dopaminergic neurotransmission
   muscarinic blocking
2. Parkinson’s, antiviral
3. Livedo reticularis, psychosis, insomnia, edema

Question 13

Benzotropine
Biperiden
Orphenadrine

1. mechanism?
2. use?
3. Adverse effects?

Answer 13

1. Decrease Ach effect in striatum
2. Reversal of drug extrapyramidal sympt.
   adjunctivly in primary parkinson’s
3. drowsiness, confusion, peripheral atropine like

Question 14

Drugs used for treatment of Huntington’s? (2)

Answer 14

Amine depleting: (Reserpine, Tetrabenazine)

Dopamine antagonists: (Haloperidol, Perphenazine)

Question 15

Treatment of Tourette’s? (1)

Answer 15

Dopamine antagonists (Haloperidol)

Question 16

Carbidopa

1. Mechanism?

Answer 16

1. Inhibits peripheral dopa decarboxylase