How do prophylactic medications for migraine work?

Updated: Oct 21, 2019
  • Author: Jasvinder Chawla, MD, MBA; Chief Editor: Helmi L Lutsep, MD  more...
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Currently, the major prophylactic medications for migraine work via one of the following mechanisms:

  • 5-HT2 antagonism - Methysergide

  • Regulation of voltage-gated ion channels - Calcium channel blockers

  • Modulation of central neurotransmitters - Beta blockers, tricyclic antidepressants

  • Enhancing gamma-aminobutyric acid-ergic (GABAergic) inhibition - Valproic acid, gabapentin

  • Prevention of acetylcholine from presynaptic membrane – Botulinum toxin

  • Calcitonin gene-related peptide (CGRP) inhibitors – Erenumab, fremanezumab, galcanezumab

Another notable mechanism is alteration of neuronal oxidative metabolism by riboflavin and reduction of neuronal hyperexcitability by magnesium replacement.

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