the trigeminovascular system is now known to have a significant role in the initiation of migraines, including the release of pain mediators such as calcitonin gene-related peptide (CGRP) and substance P (1)
when administered, calcitonin gene-related peptide (CGRP) has been shown to cause mast cell degranulation and cerebral vasculature vasodilation leading directly to the development of migraine
two main classes of CGRP modulators have been developed:
CGRP receptor antagonists (gepants)
CGRP monoclonal antibodies
both gepants and CGRP monoclonal antibodies are believed to target peripheral CGRP receptors
rimegepant is a second-generation gepant that was first introduced in 2012
is a CGRP receptor antagonist approved for the acute treatment of migraine with or without aura in adults, and for the preventive treatment of episodic migraine in adults (2)
a 75mg once-daily dose in orally disintegrating tablet (ODT) formulation was approved by the FDA in February 2020, with a maximum dose of 75mg per 24 hours (1)
offers convenience and a potentially faster response time than the conventional tablet formulation (2)
ODT formulation is ingested by placement under the patient’s tongue and will dissolve in saliva, allowing for ingestion without additional fluid, making administration comfortable even during a severe migraine attack
a review states (2):
rimegepant was also more effective than placebo at reducing the number of monthly migraine days when taken every other day for the preventive treatment of migraine
beneficial effects of rimegepant in reducing migraine frequency and improving quality of life were maintained over the longer term (up to 52 weeks)
was generally well tolerated, with no evidence of hepatotoxicity or cardiovascular toxicity in clinical trials
as the first dual agent approved for both treatment and prevention of migraine, rimegepant represents a useful option for the management of migraine in adults
NICE state (3):
Rimegepant is recommended as an option for preventing episodic migraine in adults who have at least 4 and fewer than 15 migraine attacks per month, only if at least 3 preventative treatments have not worked
Stop rimegepant after 12 weeks of treatment if the frequency of migraine attacks does not reduce by at least 50%
Reference:
Berger AA, Winnick A, Carroll AH, Welschmeyer A, Li N, Colon M, Paladini A, Ramírez GF, Hasoon J, Cornett EM, Song J, Varrassi G, Kaye AM, Kaye AD, Ganti L. Rimegepant for the treatment of migraine. Health Psychol Res. 2022 Oct 12;10(5):38534. doi: 10.52965/001c.38534. PMID: 36262478; PMCID: PMC9560892.
Blair HA. Rimegepant: A Review in the Acute Treatment and Preventive Treatment of Migraine. CNS Drugs. 2023 Mar;37(3):255-265. doi: 10.1007/s40263-023-00988-8. Epub 2023 Feb 4. Erratum in: CNS Drugs. 2023 Jul 4;: PMID: 36739335; PMCID: PMC10299922.
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