Rimegepant: A Newer Drug for the Management of Acute and Episodic Migraine

Asian Pain Academy
Aug 1
3 min read

Published by: Asian Pain Academy – Pain Management Training Academy

Introduction: Redefining Migraine Management, Rimegepant for Migraine

Migraine is a disabling neurological disorder that affects over one billion people globally. From throbbing pain to nausea and sensitivity to light or sound, the burden is physical, emotional, and financial. While triptans and NSAIDs have traditionally dominated migraine care, limitations remain, especially in patients with cardiovascular comorbidities or medication overuse.

Rimegepant, a novel oral CGRP receptor antagonist, is changing this landscape. At Asian Pain Academy, we train physicians through advanced pain fellowships and workshops. This article introduces Rimegepant, now approved for both acute migraine attacks and preventive treatment of episodic migraine.

What is Rimegepant?

Rimegepant is a second-generation, oral small-molecule calcitonin gene-related peptide (CGRP) receptor antagonist. It is indicated for:

Acute treatment of migraine with or without aura in adults.
Preventive treatment of episodic migraine in adults.

Unlike triptans, which act on serotonin receptors and cause vasoconstriction, Rimegepant blocks the CGRP receptor, a key mediator of migraine pathogenesis, without vascular effects.

Mechanism of Action: How Rimegepant Works for Migraine

Migraine attacks involve activation of the trigeminal nerve and release of CGRP, which causes vasodilation and inflammation of the meninges. Rimegepant blocks CGRP receptors, interrupting the neurovascular cascade, leading to pain relief and reduced sensitivity to photophobia, phonophobia, and nausea.

Dosage and Administration

Acute Treatment: 75 mg orally, as needed.✅ Maximum of one dose per 24 hours❌ Do not exceed 18 doses per month
Preventive Treatment: 75 mg orally every other day

Rimegepant is available as an orally disintegrating tablet (ODT) that dissolves quickly on or under the tongue, making it easy to use during migraine attacks, especially when nausea or vomiting is present.

Efficacy: Backed by Robust Clinical Evidence

✅ For Acute Migraine Relief

In a double-blind, placebo-controlled trial:

Pain freedom at 2 hours: 21.2% vs. 10.9% with placebo
Freedom from most bothersome symptom (MBS) at 2 hours: 35.1% vs. 26.8%
Significant improvement in functional ability and sustained pain freedom for up to 48 hours

✅ For Preventive Use

In another pivotal study:

Average reduction in monthly migraine days (MMD): 4.3 days vs. 3.5 with placebo
≥50% reduction in MMD: Achieved by 49.1% of patients vs. 41.5% with placebo

Advantages of Rimegepant for Migraine Over Traditional Therapies

Feature	Triptans	Rimegepant
CGRP Modulation	❌	✅ Yes
Vasoconstriction Risk	✅ Yes	❌ No
Safe in Cardiac Patients	❌ Limited	✅ Preferred
Route	Oral (some injectables)	✅ Orally disintegrating
Preventive Use	❌ No	✅ Yes (Every other day)

Safety and Side Effects

Well-tolerated in most patients. Common side effects include:

Nausea (2–3%)
Indigestion or abdominal discomfort

Rare but serious effects:

Hypersensitivity reactions (rash, dyspnea)
Hypertension (new onset or worsening)
Raynaud’s phenomenon

Contraindications:

Severe hepatic impairment (Child-Pugh Class C)
End-stage renal disease (CrCl <15 mL/min)
Known allergy to rimegepant or its excipients

Drug Interactions to Consider

Rimegepant is metabolized by CYP3A4 and a substrate of P-gp. Avoid use with:

Strong CYP3A4 inhibitors or inducers
P-gp inhibitors (space doses 48 hours apart if needed)

No significant interaction with:

Oral contraceptives
Sumatriptan (at recommended doses)
Metformin

Special Considerations in Clinical Practice

Elderly: No dose adjustment needed
Pregnancy: Insufficient human data; registry available
Lactation: Low transfer into breastmilk; <1% of maternal dose
Pediatrics: Safety and efficacy not established

Implications for Pain Physicians and Fellows

As pain physicians, we must adapt to therapies backed by solid evidence and patient-friendly profiles. Rimegepant offers:

Non-invasive administration
No vasoconstriction risks
Dual-use capability (acute + preventive)
Applicability in cardiac and hypertensive patients

At Asian Pain Academy, our training programs cover pharmacological updates, evidence-based protocols, and clinical decision-making strategies — empowering fellows to confidently use modern therapies like Rimegepant.

Conclusion: A Welcome Addition to the Migraine Armamentarium

Rimegepant is a powerful CGRP-targeting therapy that redefines the standard of care for migraine management. With its unique pharmacology, favorable safety, and easy-to-administer formulation, it is becoming a go-to option for both acute and preventive treatment of migraines.