Rimegepant
Generic Name: Rimegepant
Brand Names: Nurtec ODT
Rimegepant is an oral CGRP antagonist approved for both acute treatment and prevention of migraine.
Drug Class
Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist (Gepant)
Pregnancy
Not recommended during pregnancy. Animal studies showed adverse developmental effects at high doses. Insufficient human data. Women of childbearing potential should be counseled about potential risks.
Available Forms
Orally Disintegrating Tablet (ODT)
What It's Used For
Dosage Quick Reference
These are general dosage guidelines. Your doctor will determine the appropriate dose for your specific situation.
| Condition | Starting Dose | Maintenance Dose |
|---|---|---|
| Acute Treatment of Migraine | 75 mg as needed (max 1 dose per day) | 75 mg as needed; max 1 dose in 24 hours |
| Episodic Migraine Prevention | 75 mg every other day | 75 mg every other day |
Side Effects
Common Side Effects:
- Nausea
- Abdominal pain
- Dyspepsia
Serious Side Effects:
- Hypersensitivity reactions (dyspnea, rash, urticaria)
- Severe hypersensitivity reactions (may be delayed)
Drug Interactions
Major Interactions:
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin) — Significantly increase rimegepant levels; avoid concomitant use
- Strong or moderate CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine, St. John’s Wort, efavirenz) — Significantly decrease rimegepant levels, potentially reducing effectiveness; avoid concomitant use
- P-glycoprotein (P-gp) inhibitors (e.g., cyclosporine, verapamil) — May increase rimegepant levels; avoid concurrent use with strong P-gp inhibitors
- BCRP inhibitors (e.g., eltrombopag, curcumin at high doses) — May increase rimegepant exposure; use with caution
Additional Information
Rimegepant is a small molecule calcitonin gene-related peptide (CGRP) receptor antagonist (gepant) used for both acute treatment of migraine and preventive treatment in adults. It offers a targeted approach to migraine management without the cardiovascular concerns of triptans.
Mechanism of Action
Rimegepant works by targeting the CGRP pathway:
- CGRP receptor antagonist: Competitively blocks CGRP binding to its receptor
- Inhibits trigeminovascular activation: CGRP is released during migraine attacks and causes vasodilation and neurogenic inflammation
- Central and peripheral effects: Blocks CGRP signaling in trigeminal ganglion and central pain pathways
- No vasoconstrictor activity: Safe for patients with cardiovascular disease
CGRP is elevated during migraine attacks and plays a key role in migraine pathophysiology.
Available Formulations
Rimegepant is available as:
- Orally disintegrating tablets (ODT): 75 mg (Nurtec ODT)
ODT dissolves on the tongue without water and should not be pushed through the blister pack.
Medical Uses
FDA-Approved Indications:
- Acute treatment of migraine with or without aura in adults
- Preventive treatment of episodic migraine in adults
It is the first CGRP receptor antagonist approved for both acute and preventive treatment.
Dosing Guidelines
Acute Treatment:
- 75 mg as needed
- Maximum: 75 mg per day
- Safety of treating more than 18 migraines in a 30-day period has not been established
Preventive Treatment:
- 75 mg every other day
Administration:
- Place on or under the tongue
- Allow to dissolve (typically within seconds)
- Can be taken with or without food
- Do not take with liquids
Important Safety Information
Contraindications:
- History of hypersensitivity reaction to rimegepant
Warnings and Precautions:
- Hypersensitivity reactions: Dyspnea, rash, and urticaria have occurred; may occur days after administration
- Delayed serious hypersensitivity: Severe hypersensitivity reactions can occur even with prior tolerance
Hepatic Considerations:
- Avoid in patients with severe hepatic impairment
Drug Interactions
Strong CYP3A4 Inhibitors (ketoconazole, itraconazole, clarithromycin):
- Avoid concurrent use or limit to single dose within 48 hours
Moderate CYP3A4 Inhibitors:
- Avoid another dose within 48 hours
Strong or Moderate CYP3A4 Inducers (rifampin, phenobarbital, St. John's Wort):
- Avoid concurrent use (reduces rimegepant efficacy)
P-gp and BCRP Inhibitors:
- Avoid concurrent use or limit to single dose within 48 hours
Special Populations
- Hepatic Impairment:
- Mild to moderate: No adjustment needed
- Severe: Avoid use
- Renal Impairment:
- Mild to moderate: No adjustment
- Severe/ESRD: Avoid use (not studied)
- Pregnancy: Limited data; use only if benefit outweighs risk
- Lactation: Unknown if excreted in milk
- Elderly: No dose adjustment needed
Frequently Asked Questions
Questions to Ask Your Doctor
Consider discussing these topics at your next appointment:
- ✓Ask your doctor whether rimegepant is best used for acute treatment, prevention, or both in your case.
- ✓Discuss whether any of your current medications are CYP3A4 inhibitors or inducers that could affect rimegepant.
- ✓Ask how to track your migraine frequency to assess whether preventive treatment with rimegepant is working.
- ✓Discuss what to do if rimegepant alone does not adequately control your migraines.
Related Health Conditions
This medication is commonly used to treat or manage the following conditions:
Medical Disclaimer: This information is for educational purposes only and should not be considered medical advice. Always consult with your healthcare provider before starting, stopping, or changing any medication. Your doctor can provide personalized recommendations based on your specific health condition and medical history.
Related Medications
Other medications in the same category
Questions About This Medication?
Talk to your doctor or pharmacist about whether Rimegepant is right for you.
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