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Rimegepant

An oral disintegrating tablet formulation, which is a small molecule calcitonin gene-related peptide(CGRP) receptor antagonist.

It is used for the acute treatment of migraine with or without aura in adults.
 

Data from a long-term study of adults with migraine and a history of triptan treatment failure revealed that long-term treatment with rimegepant 75 mg up to once daily is safe and well-tolerated.

 

Nurtec tradename.

it is an orally administered small molecule calcitonin-related peptide (CGRP) receptor antagonist.

Rimegepant comes as an orally disintegrating tablet to take by mouth.

If used to prevent a migraine, it is usually taken every other day.

If used to treat a migraine, it is usually taken as a single dose at the first sign of a migraine headache.

It binds selectively to and antagonizes the CGRP receptor.
CGRP is a potent vasodilator and pain signaling neurotransmitter that is especially coming in trigeminal and spinal ganglia, but is also prevalent throughout the central and peripheral nervous systems.
CGRP levels of CGRP increase during migraine attacks, and IV CGRP induces migraine like headaches.
Resolves headache pain at two hours post those in 20% of patients, compared with 11-12% with placebo.
Nausea is the most common adverse effect in clinical trials.The most common adverse reactions were nausea (2.7% in patients who received Nurtec ODT compared to 0.8% in patients who received placebo) and abdominal pain/dyspepsia (2.4% in patients who received Nurtec ODT compared to 0.8% in patients who received placebo).
Hypersensitivity, including dyspnea and rash, occurred in less than 1% of patients treated.

Avoid concomitant administration with strong inhibitors of CYP3A4, or strong or moderate inducers of CYP3A.

It is not known if rimegepant can harm an unborn baby.

The transfer of rimegepant into breastmilk is low (<1%).

Avoid use in persons with severe hepatic impairment.

Avoid use in patients with end-stage renal disease.

Should not be taken with strong CYP 3A for inhibitors, strong or moderate CYP3A inducers.

Does not have vasoconstrictive effects, and can be used in patients with vascular disease.
Appears to be similarly effective to irbogepant.
The recommended dosage is 75 mg placed on or under the tongue and allow to disintegrate in saliva.
 
 

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