rimegepant

Contraindicated in:

Hypersensitivity;
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.

Adv. Reactions/Side Effects ⬆ ⬇

GI: nausea

Misc: hypersensitivity reactions

Interactions ⬆ ⬇

Drug-drug:

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, including cyclosporine or quinidine, may ↑ levels and risk of toxicity; avoid another dose of rimegepant within 48 hr during concurrent use.

Availability ⬆ ⬇

Orally disintegrating tablets (ODTs) menthol flavor: 75 mg

Route/Dosage ⬆ ⬇

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.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Binds to and inhibits the calcitonin gene-related peptide (CGRP) receptor, which reduces the neuroinflammatory and vasodilatory effects of CGRP.

Therapeutic effects:

Reduction in pain and other bothersome symptoms associated with migraine.
Reduction in number of monthly migraine days.

Classifications ⬆ ⬇

Therapeutic Classification: vascular headache suppressants

Pharmacologic Classification: calcitonin gene-related peptide receptor antagonists

Pharmacokinetics ⬆ ⬇

Absorption: 64% absorbed following oral administration. High-fat foods may delay and ↓ extent of absorption.

Distribution: Extensively distributed to tissues.

Protein Binding: 96%.

Metabolism/Excretion: Primarily metabolized in liver via the CYP3A4 isoenzyme, and to a lesser extent by the CYP2C9 isoenzyme. Primarily excreted as unchanged drug in feces (42%) and urine (51%).

Half-Life: 11 hr.

Time/Action Profile ⬆ ⬇

(relief of migraine pain)

ROUTE	ONSET	PEAK	DURATION
PO	0.5 hr	2 hr	up to 48 hr

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. 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 take >75 mg in any 24-hr period.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
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 patient of potential for hypersensitivity reactions and that these reactions can occur days after administration of rimegepant. Advise patient to notify health care provider immediately if signs or symptoms of hypersensitivity reactions (shortness of breath, rash) occur. Rimegepant should be discontinued if hypersensitivity reaction occurs.
Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding. Inform patient of the pregnancy exposure registry that monitors outcomes in women exposed to Nurtec during pregnancy. For more information, health care providers or patients are encouraged to contact 1-877-366-0324, email [email protected], or visit nurtecpregnancyregistry.com.

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Indications ⬇

Contraind./Precautions ⬆ ⬇