Gepant

Aka: Gepant, Oral Calcitonin Gene-Related Peptide Blocker, Oral CGRP Inhibitor, Ubrogepant, Ubrelvy, Rimegepant, Nurtec, Zavegepant, Zavzpret

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II. 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

III. Mechanism

  1. Calcitonin Gene-Related Peptide (CGRP)
    1. CGRP is a neuropeptide that acts as a vasodilator and pain sensitization
    2. CGRP Is released by trigeminal Neurons in Migraine Headache, Cluster Headache and Trigeminal Neuralgia
  2. CGRP Inhibitors block CalcitoninGene-Related Peptide (CGRP)
    1. Gepants are oral or intranasal agents that block CGRP
    2. Contrast with CGRP Monoclonal Antibody agents that are injectable

IV. 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
    4. Resources: DailyMed
      1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=fd9f9458-fd96-4688-be3f-f77b3d1af6ab
  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)
    3. Resources: DailyMed
      1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=9ef08e09-1098-35cc-e053-2a95a90a3e1d&version=19
  3. Zavegepant (Zavzpret)
    1. Intranasal Gepant (useful when Nausea, Vomiting interferes with taking medication)
    2. Migraine Abortive Treatment Dosing
      1. One spray (10 mg/spray) intranasal per 24 hours as needed
    3. Pharmacokinetics
      1. Onset: 15 minutes
      2. Peak: 30 minutes
      3. Half-Life: 6.5 hours
    4. Adverse Effects
      1. Dysgeusia or Ageusia
      2. Nausea or Vomiting
      3. Nasal discomfort
    5. Safety
      1. Has not been studied in pregnancy, children, liver or renal Impairment
    6. References
      1. Lipton (2023) Lancet Neurol 22(3): 209-217 [PubMed]

V. 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

VI. Adverse Effects

  1. Nausea
  2. Somnolence
  3. Dry Mouth

VII. 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)

VIII. 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
  4. LoVecchio (2023) Crit Dec Emerg Med 37(5):32

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Related Studies

Cost: Medications

ubrelvy (on 1/14/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
UBRELVY 100 MG TABLET $90.07 each
UBRELVY 50 MG TABLET $89.78 each
nurtec (on 1/17/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
NURTEC ODT 75 MG TABLET $110.19 each
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Related Topics in Pharmacology

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