Neurology Book

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Gepant

Aka: Gepant, Oral Calcitonin Gene-Related Peptide Blocker, Oral CGRP Inhibitor, Ubrogepant, Ubrelvy, Rimegepant, Nurtec
  1. See Also
    1. Calcitonin Gene-Related Peptide Blocker
  2. Indications
    1. Acute Migraine Headache
      1. Third-line agent in acute Migraine Headaches refractory to NSAIDS and Triptans
      2. Avoid for acute Migraines if also using Injectable CGRP Inhibitor for Migraine Prophylaxis
    2. Migraine Prophylaxis
      1. Rimegepant (Nurtec) is FDA approved for Migraine Prophylaxis in 2021 (third-line agent)
      2. Injectable CGRP Inhibitors are also indicated in Migraine Prophylaxis
  3. Mechanism
    1. Blocks CalcitoninGene-Related Peptide (CGRP)
      1. CGRP is a vasodilator and pain sensitizer that increases during Migraine Headaches
  4. Preparations
    1. Ubrogepant (Ubrelvy)
      1. Dose: 50-100 mg orally
        1. May repeat a second dose 2 hours after first)
        2. Maximum: 200 mg/24 hours
      2. Costs $85 per tablet (contrast with 70 cents per Sumatriptan tablet)
      3. May be repeated 2 hours after first dose if inadequate effect
    2. Rimegepant (Nurtec)
      1. Migraine Abortive Treatment
        1. Dissolving oral tablet: 75 mg taken as single dose (maximum 75 mg/day)
      2. Migraine Prophylaxis
        1. Dissolving oral tablet: 75 mg taken every OTHER day (maximum 18 days per month)
        2. Breakthrough acute Migraine Headache should not be treated with Rimegepant
          1. Use another type of Migraine Abortive Treatment
        3. Cost: $1800/month (contrast with $630/month for Injectable CGRP Inhibitors)
  5. Efficacy
    1. Migraine Abortive Treatment
      1. NNT 10 for one patient to be pain free at 2 hours
        1. Contrast with NNT 5 for Sumatriptan
    2. Migraine Prophylaxis
      1. Rimegepant prevents 1 Migraine more than Placebo per month in those with 10 Migraines/month on average
      2. Similar efficacy to other Migraine Prophylaxis agents including Injectable CGRP Inhibitors
  6. Adverse Effects
    1. Nausea
    2. Somnolence
    3. Dry Mouth
  7. Drug Interactions
    1. CYP3A4 Agents
      1. Drug levels may be increased by strong CYP3A4 inhibitors
      2. Drug levels may be decreased by CYP3A4 inducers (e.g. Phenytoin, Rifampin, St. John's Wort)
  8. References
    1. (2020) Presc Lett 27(3): 13
    2. (2021) Presc Lett 28(8): 43-4
    3. LoVecchio (2020) Crit Dec Emerg Med 34(2):28

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