FKLG 312:

SU 8:

Blog 10

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

Anticholinergic drugs

Dopamine agonists

• In what way does amantadine act as a antiparkinsonism drug?

Amantadine is an antiviral, NMDA antagonist and anticholinergic drug. Amantadine has the following mechanism of action to counter Parkinson's:

• Increase dopamine release.
• Increase dopamine synthesis.
• Inhibits the re-recording of dopamine.

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

Selective MAO – B inhibitors increase the dopamine concentration in an indirect manner through potent inhibition of MAO – B, thereby inhibiting the re-uptake of dopamine.

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

Ergot derivate = bromocriptine

Not ergot derivative = Pramipexole and Ropinirole

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

Bromocriptine = D2 receptors (partial agonist)

Pramipexole = D3

Ropinirole = D2

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

Pramipexole (Pexola) and selective MAO-B reuptakers are considered neuroprotective because it reduces affective symptoms and causes disease progression to decrease. Neuroprotective drugs meaning is that it reduces the symptoms of depression that can occur.

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

MAO-B inhibitors increase dopamine concentration in the central nervous system in that it has a specific substrate for dopamine.

• How do the COMT-inhibitors act in Parkinsonism?

COMT inhibitors metabolizes L-dopa to 3-O-methyldopa (3OMD)

3OMD competes with L-dopa for active transport.

COMP prolongs L-dopa's duration of action, lowers metabolism, and promotes the bioavailability of L-dopa.

• How does istradephyline act?

Adenosine A2 antagonist – D2 function is inhibited by adenosine.

• Discuss the MOA of safinamide

Safinamide has two-pronged mechanisms.

• It Increases dopamine function by potent MAO-B inhibition and dopamine re-uptake inhibition.
• And it Lowers glutamate release.