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Rimegepant

Medically reviewed by Drugs.com. Last updated on Sep 22, 2020.

Pronunciation

(ri ME je pant)

Index Terms

  • Nurtec ODT
  • Rimegepant sulfate

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet Disintegrating, Oral, as sulfate:

Nurtec: 75 mg [contains menthol]

Brand Names: U.S.

  • Nurtec

Pharmacologic Category

  • Antimigraine Agent
  • Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist

Pharmacology

Rimegepant is a calcitonin gene-related peptide receptor antagonist.

Absorption

Cmax decreased 42% to 53% and AUC decreased 32% to 38% following a high fat meal.

Distribution

Vdss: 120 L.

Metabolism

Primarily hepatic via CYP3A4 and to a lesser extent by CYP2C9.

Excretion

Urine (51% as unchanged drug); feces (42% as unchanged drug).

Onset of Action

≤2 hours (Croop 2019).

Time to Peak

1.5 hours; delayed 1 hour following a high fat meal.

Duration of Action

Up to 48 hours (Croop 2019).

Half-Life Elimination

~11 hours.

Protein Binding

~96%.

Special Populations: Hepatic Function Impairment

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.

Use: Labeled Indications

Migraine, treatment: Acute treatment of migraine with or without aura in adults.

Limitations of use: Not indicated for the preventive treatment of migraine.

Contraindications

Hypersensitivity to rimegepant or any component of the formulation.

Dosing: Adult

Migraine, treatment: Oral: 75 mg as a single dose; maximum: 75 mg/24 hours. The safety of treating >15 migraines in a 30-day period has not been established.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Administration

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).

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F).

Drug Interactions

Abametapir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

BCRP/ABCG2 Inhibitors: May increase the serum concentration of Rimegepant. Avoid combination

Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

CYP3A4 Inducers (Moderate): May decrease the serum concentration of Rimegepant. Avoid combination

CYP3A4 Inducers (Strong): May decrease the serum concentration of Rimegepant. Avoid combination

CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Rimegepant. Management: Avoid a second dose of rimegepant within 48 hours when used concomitantly with moderate CYP3A4 inhibitors. Consider therapy modification

CYP3A4 Inhibitors (Strong): May increase the serum concentration of Rimegepant. Avoid combination

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Erdafitinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Larotrectinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Lasmiditan: May increase the serum concentration of BCRP/ABCG2 Substrates. Avoid combination

Palbociclib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

P-glycoprotein/ABCB1 Inhibitors: May increase the serum concentration of Rimegepant. Avoid combination

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Stiripentol: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

Tafamidis: May increase the serum concentration of BCRP/ABCG2 Substrates. Monitor therapy

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Voxilaprevir: May increase the serum concentration of BCRP/ABCG2 Substrates. Avoid combination

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10%: Gastrointestinal: Nausea (2%)

<1%:

Dermatologic: Skin rash

Hypersensitivity: Hypersensitivity reaction

Respiratory: Dyspnea

Frequency not defined: Hypersensitivity: Type IV hypersensitivity reaction

Warnings/Precautions

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.

Pregnancy Considerations

Adverse events were observed in some animal reproduction studies at doses that also caused maternal toxicity.

Agents other than rimegepant are preferred for the management of acute migraine in pregnant women (Burch 2019).

Patient Education

What is this drug used for?

• It is used to treat migraine headaches.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Nausea

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine’s uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Frequently asked questions

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.