Gepants are a class of small-molecule, orally administered calcitonin gene-related peptide (CGRP) receptor antagonists developed for the acute treatment of migraine.
- Mechanism: They block the CGRP receptor, preventing the vasodilation and neurogenic inflammation associated with migraine.
- Examples:
-Atogepant (Qulipta): Approved for preventive treatment; blocks CGRP receptor.
- Rimegepant (Nurtec ODT) – FDA-approved for acute migraine.
- Ubrogepant (Ubrelvy) – FDA-approved for acute migraine.
- Rationale: Gepants offer an alternative to triptans, with a favorable side-effect profile (e.g., no vasoconstriction) and potential for use in patients with cardiovascular risk factors.
- Guidelines: Recommended in the 2021 AHS guidelines for acute migraine treatment, particularly for patients with contraindications to triptans.
- Dosage
Rimegepant: Typically 75 mg orally for acute migraine treatment. Ubrogepant: Typically 50 mg or 100 mg orally for acute migraine treatment.
- Route of Administration
Oral: Both rimegepant and ubrogepant are administered orally.
- Side Effects
Common Side Effects: Nausea Dysgeusia (taste disturbances) Fatigue Dizziness Less Common Side Effects: Leukopenia (low white blood cell count) Thrombocytopenia (low platelet count) Hypersensitivity reactions Hearing impairment Hypoglycemia (low blood sugar)
- Special Instructions
May be taken with food to decrease gastric distress. Use with caution in patients with hepatic dysfunction, kidney disease, serious gastrointestinal problems, heart diseases, and asthma. Efficacy Both rimegepant and ubrogepant have been shown to be efficacious in achieving greater freedom from headache pain and absence of the most bothersome symptoms in clinical trials. They do not cause vasoconstriction, making them suitable for patients with vascular disease, including those who are triptan non-responders. Warnings Contraindications: None specific to vascular diseases, but caution is advised in patients with hepatic dysfunction, kidney disease, serious GI problems, heart diseases, and asthma. Pregnancy and Breastfeeding: Not recommended for use in pregnant or breastfeeding women unless clearly necessary.
- Additional Notes
Dosage recommendations may vary based on individual patient response and local availability. Always check the package insert for any changes in indications, dosage, and additional warnings.