USMLE

Selegiline and Rasagiline

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Other Neuro Pharm
  1. Ramelteon
  2. Triptans
  3. Benzodiazepines - Function
  4. Zolpidem Zaleplon Eszopiclone
  5. Suvorexant
  6. Bromocriptine (Ergot Dopamine Agonists)
  7. Pramipexole, Ropinirole
  8. Amantadine
  9. Levodopa, Carbidopa
  10. Entacapone, Tolcapone
  11. Selegiline and Rasagiline
  12. Benztropine, Trihexyphenidyl
  13. Tetrabenazine
  14. Baclofen
  15. Memantine
  16. Riluzole
  17. Full Opioid Agonists
  18. Partial Opioid Agonists
  19. Dextromethorphan
  20. Tramadol
  21. Naloxone
  22. Naltrexone

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