CGRP Receptor Antagonists: Uses, most common brand names, and safety information
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It is estimated that more than 10% of people worldwide are affected by migraine headaches. Migraines are 3 times more common in women than in men and are most common in people 20 to 50 years of age.
Calcitonin gene-related peptide (CGRP) was discovered in 1982. Soon after, its role as a vasodilator in migraines was established. The first anti-CGRP medication, an IV CGRP-receptor antagonist called olcegepant was found to be effective in the acute treatment of migraines in 2004. However, it was not further developed due to the side effects including paresthesia (tingling), and because it had to be given intravenously. A monoclonal antibody, Aimovig (erenumab), received FDA approval for migraine prevention in 2018. There are currently several CGRP monoclonal antibodies and antagonists that are effective treatment options for migraines, with almost 33% of patients having complete symptom relief.
The list below includes CGRP receptor antagonists approved by the U.S. Food and Drug Administration (FDA) and their pricing:
List of CGRP receptor antagonists
Nurtec ODT (rimegepant)
Nurtec ODT is indicated for the treatment and prevention of migraines.
Qulipta is indicated to treat migraines.
Ubrelvy is indicated for the acute treatment of migraine with or without aura.
Vyepti is indicated to prevent migraines.
Emgality is indicated to prevent migraines and treat episodic cluster headaches.
Ajovy is indicated for the preventive treatment of migraines.
Aimovig is indicated to prevent migraines.
What are CGRP receptor antagonists?
CGRP receptor antagonists are a growing class of migraine treatment medications. They can be used to treat episodic migraine attacks or as a preventive treatment to reduce migraine frequency and headache days. These new drugs that block CGRP come in two forms, small molecules called gepants and larger molecules called monoclonal antibodies. Gepants are taken orally while monoclonal antibodies are given via a subcutaneous injection. CGRP receptor antagonists are an effective treatment that is typically used if you have failed other migraine therapies such as triptans or botox. According to the American Migraine Foundation, people usually see a reduction in migraine days within 1–4 weeks from CGRP treatment.
How do CGRP receptor antagonists work?
CGRP is found throughout your nervous system and is more concentrated at sites that are involved in migraine pathophysiology. CGRP levels are much higher during acute migraine attacks and may be chronically elevated in chronic migraine patients. By blocking CGRP, these migraine medications make blood vessels in your brain constrict which is thought to help relieve headache pain. This may also lead to cardiovascular side effects such as high blood pressure, although this has not been studied and proven.
What conditions are CGRP receptor antagonists used to treat?
CGRP receptor antagonists are used in several conditions, including:
- Treatment of acute migraine symptoms
- Migraine prophylaxis
- Treatment of cluster headaches
Are CGRP receptor antagonists safe?
The use of CGRP receptor antagonists is relatively safe and effective when taken as prescribed. Before beginning treatment with CGRP receptor antagonists, tell your doctor if you have any of the following medical conditions:
- Hypersensitivity to any ingredient in the CGRP receptor antagonist product
- Severe liver impairment
- End-stage kidney disease
What are the common side effects of CGRP receptor antagonists?
The adverse effects you experience from CGRP receptor antagonists will depend on several factors including the medication and dose. Some common adverse effects in clinical trials include:
- Injection site reactions
- Stomach pain
- Common cold symptoms
- Muscle cramps and spasms
- Allergic reactions including hives and shortness of breath
This is not a complete list of side effects and we encourage you to consult with your prescribing healthcare provider or neurologist for medical advice about any possible side effects.
Who should not take CGRP receptor antagonists?
You should not take CGRP receptor antagonists if you have a known hypersensitivity to any ingredients in the product’s formulation. You should also avoid these medications if you have advanced liver or kidney disease.
What blocks CGRP naturally?
In a 2014 study, 250mg of ginger was shown to stop migraines as well as Imitrex (sumatriptan). It also may reduce calcitonin gene-related peptide (CGRP) in migraine patients.
Is botox a CGRP receptor antagonist?
While it is not considered a CGRP receptor antagonist, botox is used as a migraine prophylactic and is thought to work through the inhibition of acetylcholine and CGRP release. It has been shown to be effective as a preventive medication for migraine patients.
How much do CGRP receptor antagonists cost?
CGRP receptor antagonists are very expensive with an average cost of around $10,000 per year.
You can purchase CGRP receptor antagonists for $49 per month from NiceRx if eligible for assistance. Prices at the pharmacy vary by location, strength, and quantity, as well as your insurance status.
Related resources for CGRP receptor antagonists
The content on this website is intended for information purposes only. It does not constitute medical advice. The information on this website should not be relied upon and is not a substitute for professional medical advice. You should always speak to your doctor regarding the risks and benefits of any treatment.