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Class: Calcitonin Gene-related Peptide (CGRP) Antagonists
Chemical Name: [(5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl] 4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate
Molecular Formula: 2C28H28F2N6O3•H2SO4•3H2O
CAS Number: 1374024-48-2
Brands: Nurtec ODT

Medically reviewed by Last updated on March 16, 2020.


Rimegepant sulfate is a calcitonin gene-related peptide (CGRP) receptor antagonist.

Uses for Rimegepant

Rimegepant sulfate has the following uses:

Rimegepant sulfate is indicated for the acute treatment of migraine with or without aura in adults.1

Rimegepant sulfate has the following limitations of use:

Rimegepant sulfate is not indicated for the preventive treatment of migraine.1

Rimegepant Dosage and Administration


Rimegepant sulfate is available in the following dosage form(s) and strength(s):

Rimegepant sulfate orally disintegrating tablets: 75 mg (of rimegepant).1


It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:


Dosage and Administration
  • The recommended dose is 75 mg taken orally, as needed.1

  • The maximum dose in a 24-hour period is 75 mg.1

  • The safety of treating more than 15 migraines in a 30-day period has not been established.1

Cautions for Rimegepant


Patients with a history of hypersensitivity reaction to rimegepant sulfate or to any of its components.1


Hypersensitivity Reactions

Hypersensitivity reactions, including dyspnea and rash, have occurred with rimegepant sulfate in clinical studies. Hypersensitivity reactions can occur days after administration, and delayed serious hypersensitivity has occurred. If a hypersensitivity reaction occurs, discontinue rimegepant sulfate and initiate appropriate therapy.1

Specific Populations


Risk Summary: There are no adequate data on the developmental risk associated with the use of rimegepant sulfate in pregnant women. In animal studies, oral administration of rimegepant during organogenesis resulted in adverse effects on development in rats (decreased fetal body weight and increased incidence of fetal variations) at exposures greater than those used clinically and which were associated with maternal toxicity. The evaluation of developmental effects following oral administration of rimegepant throughout pregnancy and lactation was inadequate.1

In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively. The estimated rate of major birth defects (2.2 to 2.9%) and miscarriage (17%) among deliveries to women with migraine are similar to rates reported in women without migraine.1

Published data have suggested that women with migraine may be at increased risk of preeclampsia and gestational hypertension during pregnancy.1

Animal Data: Oral administration of rimegepant (0, 10, 60, or 300 mg/kg/day) to pregnant rats during the period of organogenesis resulted in decreased fetal body weight and an increased incidence of fetal variations at the highest dose tested (300 mg/kg/day), which was associated with maternal toxicity. Plasma exposures (AUC) at the no-effect dose (60 mg/kg/day) for adverse effects on embryofetal development were approximately 45 times that in humans at the maximum recommended human dose (MRHD) of 75 mg/day.1

Oral administration of rimegepant (0, 10, 25, or 50 mg/kg/day) to pregnant rabbits during the period of organogenesis resulted in no adverse effects on embryofetal development. The highest dose tested (50 mg/kg/day) was associated with plasma exposures (AUC) approximately 10 times that in humans at the MRHD.1

The prenatal and postnatal development study in rats, in which rimegepant (0, 10, 25, or 60 mg/kg/day) was orally administered throughout gestation and lactation, was inadequate to assess for adverse effects of rimegepant during these periods of development.1


There are no data on the presence of rimegepant or its metabolites in human milk, the effects of rimegepant on the breastfed infant, or the effects of rimegepant on milk production. There are no animal data on the excretion of rimegepant in milk. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for rimegepant sulfate and any potential adverse effects on the breastfed infant from rimegepant sulfate or from the underlying maternal condition.1

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.1

Geriatric Use

In pharmacokinetic studies, no clinically significant pharmacokinetic differences were observed between elderly and younger subjects. Clinical studies of rimegepant sulfate did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger patients.1

Hepatic Impairment

No dosage adjustment of rimegepant sulfate is required in patients with mild (Child-Pugh class A) or moderate (Child-Pugh class B) hepatic impairment. Plasma concentrations of rimegepant were significantly higher in subjects with severe (Child-Pugh class C) hepatic impairment. Avoid use of rimegepant sulfate in patients with severe hepatic impairment.1

Renal Impairment

No dosage adjustment of rimegepant sulfate is required in patients with mild, moderate, or severe renal impairment. Rimegepant sulfate has not been studied in patients with end-stage renal disease and in patients on dialysis. Avoid use of rimegepant sulfate in patients with end-stage renal disease (Clcr <15 mL/min).1

Common Adverse Effects

The adverse reaction reported in ≥1% of patients treated with rimegepant sulfate is nausea.1

Drug Interactions

Specific Drugs

It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:

  • Strong CYP3A4 Inhibitors: Avoid concomitant administration.1

  • Moderate CYP3A4 Inhibitors: Avoid another dose of rimegepant sulfate within 48 hours when administered with a moderate CYP3A4 inhibitor.1

  • Strong and Moderate CYP3A Inducers: Avoid concomitant administration.1

  • Inhibitors of P-glycoprotein (P-gp) or breast cancer resistance protein (BCRP): Avoid concomitant administration.1


Rimegepant is a CGRP receptor antagonist.1

Advice to Patients

Advise patients to read the FDA-approved patient labeling (Patient Information).1

Handling of Orally Disintegrating Tablets Packaging

Instruct patients not to remove the blister from the outer aluminum pouch until ready to use the orally disintegrating tablet inside.1

Hypersensitivity Reactions

Inform patients about the signs and symptoms of hypersensitivity reactions and that these reactions can occur days after administration of rimegepant sulfate. Advise patients to contact their healthcare provider immediately if signs or symptoms of hypersensitivity reactions occur.1

Additional Information

AHFSfirstRelease. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.


Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Rimegepant Sulfate


Dosage Forms


Brand Names



Tablet, Orally Disintegrating

75 mg (of rimegepant)

Nurtec ODT

Biohaven Pharmaceuticals Inc

AHFS Drug Information. © Copyright 2021, Selected Revisions March 16, 2020. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.


1. Biohaven Pharmaceuticals, Inc. NURTEC ODT (rimegepant sulfate) ORAL prescribing information. 2020 Mar.

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