Selegiline and Rasagiline

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Summary

Selegiline and Rasagiline are drugs used in the treatment of Parkinson's disease. They inhibit monoamine oxidase-B, increasing the availability of dopamine in the brain. They can also be used in conjunction with levodopa to treat Parkinson’s disease and specifically combat the “wearing off” effect of levodopa. Selegiline and Rasagiline can also have a protective effect on the brain by preventing damage of dopaminergic neurons by a toxin called MPTP.  Lastly, it’s worth noting that these drugs may also be used to treat atypical depression by increasing the amount of dopamine in the brain.

Key Points

  • Selegiline, Rasagiline 
    • Drug Names
      • -giline suffix (selegiline, rasagiline)
    • Mechanism
      • Acts as  Monoamine Oxidase - B (MAO-B) inhibitor → increases dopamine availability
        • Block conversion of dopamine into DOPAC (Dihydroxyphenylacetic acid) by selectively inhibiting MAO-B  in the CNS → increase dopamine availability
    • Clinical use
      • Treat Parkinson's disease
        • Used as adjunctive agent to L-DOPA in the treatment of Parkinson disease
        • Helps combat the “wearing off” effect of long-term L-DOPA use
        • Slows clinical progression of Parkinsons
        • Can prevent MPTP-induced damage of dopaminergic neurons (neuroprotective effect)
      • Treat Atypical Depression
    • Adverse effects
      • May enhance adverse effects of L-DOPA