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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.

 

 

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

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.
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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