1. Which two main groups of drugs are important in the treatment of Parkinsonism?

• Drugs that increase dopamine activity
• Drugs that decrease cholinergic activity

2. In what way does amantadine act as an antiparkinsonism drug?

• Metaffinoid potentiator of dopamine – increases the synthesis and release of dopamine but decreases the reuptake of dopamine
• It is an NMDA antagonist therefore having anti dyskinesia effects
• It is an adenosine A₂ antagonist – adenosine inhibits D₂ function

3. Discuss the mechanisms of action of the antiparkinsonism drugs that indirectly increase dopamine concentration.

• Enzymatic conversion to an active metabolite is not needed

4. Which of the dopamine agonists are ergot derivatives and which are not?

• Ergot derivatives: Bromocriptine and pergolide
• Non-ergot derivatives: Pramipexole, ropinirole and rotigotine

5. List the specific dopamine receptors that are stimulated by each agonist.

• Bromocriptine: D₂
• Pergolide: D₁ and D₂
• Pramipexole: D₃
• Ropinirole: D₂
• Rotigotine: no specificity

6. Which of these drugs are classified as neuron protecting drugs?  What does this mean?

• Rasagaline
• Neuroprotective means that the drug slowed down the disease progression

7. What is the importance of monoamine oxidase B (MAO-B) selective drugs in the treatment of Parkinsonism?

• These drugs selectively metabolise dopamine

8. How do the COMT-inhibitors act in Parkinsonism?

• Prolong levodopa’s action by diminishing its peripheral metabolism, thus decreasing the clearance but increasing the relative bioavailability

9. How does istradephyline act?

• It is an adenosine A₂ antagonist

10. Discuss the MOA of safinamide

• Safinamide – increases DA function
• It has a potent reversible inhibition of MAO-B and inhibits DA uptake
• But also decreases glutamate release

References: Katzung and Powerpoint notes