rimegepant

General

Pronunciation:
ri-meg-je-pant


Trade Name(s)

  • Nurtec

Ther. Class.

vascular headache suppressants

Pharm. Class.

calcitonin gene-related peptide receptor antagonists

Indications

  • Acute treatment of migraine with or without aura.
  • Preventive treatment of episodic migraines.

Action

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

Therapeutic Effect(s):

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

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 and 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)

ROUTEONSETPEAKDURATION
PO0.5 hr2 hrup to 48 hr

Contraindication/Precautions

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.

Adverse Reactions/Side Effects

GI: nausea

Misc: hypersensitivity reactions

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

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.

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.

Availability

Orally disintegrating tablets (ODTs) (menthol flavor): 75 mg

Assessment

  • 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.

Implementation

  • Use dry hands when opening blister pack. Peel back foil covering of one blister and gently remove the 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.

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 nurtecpregnancyregistry@ppd.com, or visit nurtecpregnancyregistry.com.

Evaluation/Desired Outcomes

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