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Calcitonin Gene-Related Peptide Blocker

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Calcitonin Gene-Related Peptide Blocker, CGRP Monoclonal Antibody, CGRP Antagonist, Injectable Calcitonin Gene-Related Peptide Blocker, Injectable CGRP Inhibitor, Erenumab, Ajovy, Fremanezumab, Emgality, Galcanezumab, Aimovig

  • Indications
  1. Migraine Prophylaxis if refractory to first-line agents
  • 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. CGRP Monoclonal Antibody agents that are injectable
    2. Contrast with Gepants which are oral or intranasal agents that block CGRP
  • Medications
  1. See Rimegepant (Nurtec)
  2. Erenumab (Aimovig)
    1. Autoinjector once monthly in Abdomen, thigh, upper arm
    2. Start 70 mg, and may increase as needed to 140 mg
    3. Adverse Effects: Constipation, myalgias
  3. Fremanezumab (Ajovy)
    1. May give 225 mg prefilled syringe dose once monthly OR
    2. Give 675 mg (3 injections from prefilled syringes) once every 3 months
  4. Galcanezumab (Emgality)
    1. Once monthly injection via pen
    2. Load 240 mg once, then 120 mg monthly
    3. Adverse Effects: back pain, Dizziness, swelling, Nausea, Pharyngitis
  • Adverse Effects
  1. Injection site mild reactions
  2. New onset or worsening Hypertension (Erenumab or Aimovig)
    1. Associated with 60 cases of systolic increase of 40 mmHg, diastolic increase of 30 mmHg
    2. Occurred within 1 week of first or second dose
    3. May be related to the blockade of CGRP which is a vasodilator
    4. Avoid in Uncontrolled Hypertension or significant Cardiovascular Risk
    5. Incorporate Home Blood Pressure Monitoring for the first few months after starting
    6. (2021) Presc Lett 28(4): 19-20
    7. Saely (2021) Headache 61(1):202-8 [PubMed]
  • Efficacy
  1. Reduces migraine Incidence by 2 fewer Migraine days/month
  • Disadvantages
  1. Limited safety data outside healthy patients without comorbidity at time of 2018 release
  2. Expensive: $6900 per year
  • References
  1. (2018) Presc Lett 25(8)
  2. (2018) Presc Lett 25(12): 70