Note: Concurrent use of rimegepant for both migraine treatment and prevention has not been evaluated (Croop 2021).
Migraine, moderate to severe, acute treatment (alternative agent):
Note: Consider use if triptans are contraindicated (eg, cardiovascular risk factors), ineffective, or poorly tolerated. Administration early in the course of a migraine attack, at the first sign of pain, may improve response to treatment (AHS [Ailani 2021]).
Oral: 75 mg as a single dose. Maximum: 75 mg per 24 hours (Croop 2019; manufacturer’s labeling).
Migraine, prevention (alternative agent):
Note: Avoid use in patients with recent cardiovascular or cerebrovascular ischemic events. Limit use to patients with significant disability from frequent migraines who are unable to tolerate or do not respond to adequate trials of other preventive therapies (Loder 2018; Schwedt 2022). An adequate trial for assessment of effect is considered to be at least 8 weeks at a therapeutic dose (AHS [Ailani 2021]).
Oral: 75 mg every other day (Croop 2021; manufacturer’s labeling).
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
CrCl ≥15 mL/minute: No dosage adjustment necessary.
CrCl <15 mL/minute: Avoid use (has not been studied).
Patients on dialysis: Avoid use (has not been studied).
Mild to moderate impairment (Child-Pugh class A, B): No dosage adjustment necessary.
Severe impairment (Child-Pugh class C): Avoid use.
Refer to adult dosing.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet Disintegrating, Oral, as sulfate:
Nurtec: 75 mg [contains menthol]
No
Oral: Using dry hands, peel foil covering blister to remove tablet; do not push tablet through the foil. Immediately place tablet on or under tongue. The tablet will disintegrate in saliva (can be swallowed without additional liquid).
Migraine, prevention: Preventative treatment of migraine in adults (Croop 2021; manufacturer's labeling).
Migraine, moderate to severe, acute treatment: Acute treatment of migraine with or without aura in adults.
Rimegepant may be confused with rimonabant [multiple international markets].
Nurtec may be confused with Noctec brand name for chloral hydrate [United States, Australia, Canada, United Kingdom]; Nutren brand name for enteral nutrition preparation [multiple international markets]; Nutrex brand name for nutritional supplement [India, Italy].
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
1% to 10%: Gastrointestinal: Abdominal pain (≤2%), dyspepsia (≤2%), nausea (2% to 3%)
<1%:
Dermatologic: Skin rash
Hypersensitivity: Hypersensitivity reaction
Respiratory: Dyspnea
Frequency not defined: Hypersensitivity: Type IV hypersensitivity reaction
Hypersensitivity (including delayed serious hypersensitivity) to rimegepant or any component of the formulation.
Concerns related to adverse effects:
• Hypersensitivity: Hypersensitivity reactions, including dyspnea, rash, and delayed serious reactions, have been reported; discontinue therapy if hypersensitivity occurs.
Disease-related concerns:
• Hepatic impairment: Use is not recommended in patients with severe hepatic impairment.
• Renal impairment: Use is not recommended in patients with end-stage renal disease.
Other warnings and precautions:
• Appropriate use: The safety of using more than 18 doses in a 30-day period has not been established.
Substrate of BCRP/ABCG2, CYP2C9 (minor), CYP3A4 (major), P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Asciminib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor therapy
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
CYP3A4 Inducers (Moderate): May decrease the serum concentration of Rimegepant. Risk X: Avoid combination
CYP3A4 Inducers (Strong): May decrease the serum concentration of Rimegepant. Risk X: Avoid combination
CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Rimegepant. Management: If taking rimegepant for the acute treatment of migraine, avoid a second dose of rimegepant within 48 hours when used concomitantly with moderate CYP3A4 inhibitors. No dose adjustment needed if using rimegepant for prevention of episodic migraine. Risk D: Consider therapy modification
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Rimegepant. Risk X: Avoid combination
Erdafitinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Management: If coadministration with these narrow therapeutic index/sensitive P-gp substrates is unavoidable, separate erdafitinib administration by at least 6 hours before or after administration of these P-gp substrates. Risk D: Consider therapy modification
Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Futibatinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor therapy
Gilteritinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk C: Monitor therapy
Lasmiditan: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid combination
Pacritinib: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid combination
P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of Rimegepant. Management: Avoid administration of another dose of rimegepant within 48 hours if given concomitantly with a P-glycoprotein (P-gp) inhibitor. Risk D: Consider therapy modification
Taurursodiol: May increase the serum concentration of P-glycoprotein/ABCB1 Substrates (Narrow Therapeutic Index/Sensitive with Inhibitors). Risk X: Avoid combination
In general, preventive treatment for migraine in patients trying to become pregnant should be avoided; treatment should be individualized considering the available safety data and needs of the patient should pregnancy occur (AHS [Ailani 2021]).
Following oral administration of rimegepant to pregnant rats during the period of organogenesis, adverse fetal events were only observed at doses that also caused maternal toxicity; pre- and postnatal developmental studies in rats were inadequate. Adverse events were not observed following oral administration to pregnant rabbits during the period of organogenesis.
In general, preventive treatment for migraine in pregnant patients should be avoided; treatment during pregnancy should be individualized considering the available safety data, the potential for adverse maternal and fetal events, and needs of the patient (AHS [Ailani 2021]). Based on available data, other agents may be preferred for the management of acute migraine or the prevention of migraine in pregnant patients (Burch 2019).
Data collection to monitor pregnancy and infant outcomes following exposure to rimegepant is ongoing. Health care providers are encouraged to enroll patients exposed to rimegepant during pregnancy in the Nurtec Pregnancy Registry (877-366-0324 or nurtecpregnancyregistry.com).
Rimegepant is present in breast milk.
Data related to the presence of rimegepant in breast milk is available from 12 lactating patients 2 weeks to 6 months postpartum. Patients were administered a single dose of rimegepant 75 mg and breast milk was collected at specified intervals for 36 hours after the dose. The median time to peak concentrations of rimegepant in breast milk was 2 hours after the dose. The maximum concentrations of rimegepant in breast milk and maternal plasma were 169.6 ng/mL and 759.2 ng/mL, respectively. Using the mean milk concentration, authors of the study calculated the estimated exposure to the breastfeeding infant to be 0.005 mg/kg/day (relative infant dose [RID] 0.51% based on a mean maternal dose of 1.04 mg/kg/day). Infants were not breastfed during the study (Baker 2022). In general, breastfeeding is considered acceptable when the RID of a medication is <10% (Anderson 2016; Ito 2000).
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and the benefits of treatment to the mother. In general, preventive treatment for migraine in lactating patients should be avoided; when treatment is needed, therapy should be individualized considering the available safety data and needs of the patient (AHS [Ailani 2021]).
Rimegepant is a calcitonin gene-related peptide receptor antagonist.
Onset:
Migraine treatment: ≤2 hours (Croop 2019).
Migraine prevention: ≤4 weeks (Croop 2021).
Duration: Migraine treatment: Up to 48 hours (Croop 2019).
Absorption: Cmax decreased 42% to 53% and AUC decreased 32% to 38% following a high-fat meal. Cmax decreased 36% and AUC decreased 28% following a low-fat meal.
Distribution: Vdss: 120 L.
Protein binding: ~96%.
Metabolism: Primarily hepatic via CYP3A4 and to a lesser extent by CYP2C9.
Bioavailability: ~64%.
Half-life elimination: ~11 hours.
Time to peak: 1.5 hours; delayed 1 hour following a high-fat meal.
Excretion: Urine (51% as unchanged drug); feces (42% as unchanged drug).
Hepatic function: Cmax and AUC increased ~2-fold in patients with severe hepatic impairment (Child-Pugh class C) following a single 75 mg dose compared to healthy controls.
Tablet, orally-disintegrating (Nurtec Oral)
75 mg (per each): $137.89
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