vascular headache suppressants
calcitonin gene-related peptide receptor antagonists
- Acute treatment of migraine with or without aura.
- Preventive treatment of episodic migraines.
Binds to and inhibits the calcitonin gene-related peptide (CGRP) receptor, which reduces the neuroinflammatory and vasodilatory effects of CGRP.
- Reduction in pain and other bothersome symptoms associated with migraine.
- Reduction in number of monthly migraine days.
Absorption: 64% absorbed following oral administration. High-fat foods may delay and reduce extent of absorption.
Distribution: Extensively distributed to tissues.
Protein Binding: 96%.
Metabolism and Excretion: Primarily metabolized in liver via CYP3A4 isoenzyme, and to a lesser extent by CYP2C9 isoenzyme. Primarily excreted as unchanged drug in feces (42%) and urine (51%).
Half-life: 11 hr.
TIME/ACTION PROFILE (relief of migraine pain)
|PO||0.5 hr||2 hr||up to 48 hr|
- Severe hepatic impairment
- End-stage renal disease (CCr <15 mL/min).
Use Cautiously in:
- OB: Safety not established in pregnancy;
- Lactation: Safety not established in breastfeeding;
- Pedi: Safety and effectiveness not established in children.
Adverse Reactions/Side Effects
Misc: hypersensitivity reactions
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
- Strong CYP3A4 inhibitors, including itraconazole may significantly ↑ levels and risk of toxicity; avoid concurrent use.
- Moderate CYP3A4 inhibitors may ↑ levels and risk of toxicity; avoid another dose of rimegepant within 48 hr during concurrent use.
- Strong CYP3A4 inducers, including rifampin or moderate CYP3A4 inducers , may ↓ levels and effectiveness; avoid concurrent use.
- P-glycoprotein inhibitors or breast cancer resistance protein (BCRP) inhibitors, including itraconazole may significantly ↑ levels and risk of toxicity; avoid concurrent use.
Acute Migraine Treatment
PO (Adults): 75 mg as single dose (max dose = 75 mg/24 hr). Should not be used to treat >18 migraines in 30–day period.
Preventive Treatment of Episodic Migraines
PO (Adults): 75 mg every other day.
Orally disintegrating tablets (menthol-flavor): 75 mg
- Assess pain location, character, intensity, duration, and associated symptoms (photophobia, phonophobia, nausea, vomiting) during migraine attack.
- Monitor frequency of migraine headaches in patients using rimegepant for prophylaxis.
- Use dry hands when opening blister pack. Peel back foil covering of one blister and gently remove the orally disintegrating tablet (ODT). Do not push ODT through foil. As soon as blister is opened, remove ODT and place on tongue; ODT may also be placed under tongue. ODT will disintegrate in saliva so that it can be swallowed without additional liquid. Take ODT immediately after opening blister pack. Do not store ODT outside the blister pack for future use.
- PO Treatment: Administer ODT once daily as needed for migraine attacks. Limit dose to one ODT/day and no more than 18 doses in a 30–day period.
- Prophylaxis: Administer one ODT every other day for prevention of migraine headaches.
- Instruct patient to take rimegepant as soon as symptoms of a migraine attack appear, but it may be administered any time during an attack. Do not use more than 75 mg in any 24-hr period.
- Instruct patient using rimegepant for prevention to take as directed.
- Advise patient to avoid alcohol, which aggravates headaches, during rimegepant use.
- Advise patient that lying down in a darkened room following rimegepant administration may further help relieve headache.
- Inform patients of potential for hypersensitivity reaction and that these reactions can occur days after administration of rimegepant. Advise patients to notify health care professional immediately if signs or symptoms of hypersensitivity reactions (shortness of breath, rash) occur. Rimegepant should be discontinued if hypersensitivity reaction occurs.
- Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
- Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
- Relief of migraine attack.
- Reduction in frequency of migraine headaches.
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