Rimegepant
CGRP antagonists (gepants and anti-CGRP antibodies)
CGRP antagonists (gepants and anti-CGRP antibodies)
An oral CGRP receptor blocker that dissolves on or under the tongue. It treats migraine attacks and can also prevent them.
Quick facts
- Group
- CGRP antagonists (gepants and anti-CGRP antibodies)
- Target
- CGRP receptor (calcitonin receptor-like receptor, CALCRL, with RAMP1)
- Used for
- Acute treatment of migraine attacks
- Key effects
- Nausea · Stomach pain · Indigestion
- Monitor
- Headache diary · Blood pressure
- ATC
- N02CD06
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows telcagepant, an earlier gepant that was never marketed, bound to the extracellular domains of the human CGRP receptor (CLR with RAMP1), where small-molecule gepants block the receptor; there is no structure with this drug.
Rimegepant is a small-molecule antagonist of the CGRP receptor (a gepant). Calcitonin gene-related peptide (CGRP), released by trigeminal nerves during migraine, dilates meningeal vessels and drives neurogenic inflammation. Gepants bind at the junction of the two receptor subunits (CLR and RAMP1) and stop CGRP from activating it. Unlike triptans, they do not constrict blood vessels.
- Rimegepant binds the CGRP receptor
- Trigeminal CGRP can no longer act
- Less vasodilation and neurogenic inflammation
- The attack eases, or attacks become fewer
Indications
- Acute treatment of migraine attacks Migraine →
- Prevention of episodic migraine Migraine →
Adverse effects
Common
- Nausea
- Stomach pain
- Indigestion
Contraindications
- Hypersensitivity to rimegepant or any component of the product
Key interactions
- St John's wort
- Can lower rimegepant levels
- Grapefruit and grapefruit juice
- Their use is discussed with the treating team before starting
- Other medicines (some interacting medicines cannot be combined)
- The full medication list is reviewed before starting
What is monitored
- Headache diary: attacks and use of acute medicines
- Blood pressure
- Fingers and toes for Raynaud symptoms
Administration and safety
- The tablet dissolves on or under the tongue without water
- For an attack it is used at the first sign of migraine; no more than one dose in 24 hours
- Kidney and liver problems are reported before starting
Pregnancy and breastfeeding
There is little information in pregnancy; it is a decision for the treating team.
Nursing care
- Ask about hypertension, Raynaud phenomenon, kidney and liver disease
- Review all medicines and supplements, including St John's wort
- Teach to report headaches that do not improve or become more frequent
Pharmacokinetics
- Absorption
- Orally disintegrating tablet placed on or under the tongue
Test yourself
Think of the answer, then tap the question to see it.
How does rimegepant work?
It is a small-molecule antagonist of the CGRP receptor (a gepant).
Which two uses does rimegepant have in migraine?
Acute treatment of attacks and prevention of episodic migraine.
Do gepants constrict blood vessels like triptans?
No; they block CGRP signalling without vasoconstriction.
Connections
← Back to the class: CGRP antagonists (gepants and anti-CGRP antibodies)
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Rimegepant: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); RCSB PDB - 3N7R: Crystal structure of the ectodomain complex of the CGRP receptor, a Class-B GPCR, reveals the site of drug antagonism (RCSB Protein Data Bank, 2026).
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Representative model, for educational purposes only.