Gepants represent a newer class of medication offering targeted relief for individuals experiencing migraine. These small-molecule drugs have emerged as a significant advancement in migraine treatment, providing options for both acute symptom management and long-term prevention. Their development addresses previously unmet needs in migraine care, offering a different approach to managing this often-debilitating neurological condition.
What Gepants Are
Gepants are a class of small molecule drugs that act as calcitonin gene-related peptide (CGRP) receptor antagonists. CGRP is a protein naturally found in the body that plays a role in transmitting pain signals, causing inflammation, and dilating blood vessels during a migraine attack. During a migraine, nerve endings in the brain release CGRP, which then binds to specific receptors, leading to the characteristic pain and other symptoms.
Gepants work by blocking CGRP from binding to its receptors, thereby disrupting the pain signaling pathway associated with migraine attacks. This targeted action prevents CGRP-mediated effects like pain perception and neurogenic inflammation. By blocking these receptors, gepants can stop or prevent a migraine attack.
Who Benefits From Gepants
Gepants are approved for treating both acute migraine attacks and for preventing migraines in adults. Some gepants, like ubrogepant and zavegepant, are used for acute treatment, while atogepant is specifically for prevention. Rimegepant is unique as it has indications for both acute and preventive use.
These medications are particularly suitable for individuals who cannot tolerate or have medical conditions that prevent them from using other common migraine medications, such as triptans. Triptans, for example, can cause blood vessel constriction, making them unsuitable for people with certain cardiovascular diseases or those at risk of stroke or heart attack. Gepants do not cause this vasoconstriction, offering a safer alternative for these patient populations. Furthermore, gepants do not appear to cause medication overuse headache, a common issue with frequent use of other acute migraine treatments.
How Gepants are Used and Their Common Effects
Gepants are available in various forms, including oral tablets, orally disintegrating tablets, and nasal sprays. For acute migraine treatment, a gepant is typically taken as soon as a migraine attack begins, or when symptoms are still mild. For instance, ubrogepant is available in 50 mg or 100 mg tablets, with an option for a second dose at least two hours after the initial dose, up to a maximum of 200 mg in 24 hours. Rimegepant is often prescribed as a 75 mg orally disintegrating tablet, taken at the onset of an attack for acute relief or every other day for prevention. Zavegepant is administered as a nasal spray, offering pain relief within two hours and potentially lasting up to 48 hours.
When used for migraine prevention, a gepant like atogepant is taken daily, or rimegepant can be taken every other day. These preventive regimens aim to reduce the frequency and severity of migraine attacks over time. Gepants are generally well-tolerated, with common side effects being mild and temporary. These can include nausea, fatigue, dry mouth, constipation, dizziness, or decreased appetite.
Gepants Alongside Other Migraine Therapies
Gepants offer a distinct therapeutic option when compared to other established migraine treatments like triptans and CGRP monoclonal antibodies. Triptans work by constricting blood vessels and affecting serotonin receptors in the brain, which can be a concern for patients with cardiovascular conditions.
CGRP monoclonal antibodies (mAbs) also target the CGRP pathway but are larger molecules typically administered by injection or intravenous infusion, often on a monthly or quarterly basis for prevention. Gepants, being small molecules, are generally taken orally, offering a more convenient administration method for many patients. While both gepants and CGRP mAbs block CGRP signaling, gepants can be used for both acute and/or preventive treatment, whereas CGRP mAbs are primarily for prevention. The availability of gepants provides an important option for patients seeking alternatives or additional therapies for their condition.