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  • CLASSES

    Calcitonin Gene-Related Peptide (CGRP) Antagonists

    DEA CLASS

    Rx

    DESCRIPTION

    Oral, calcitonin gene-related peptide (CGRP) receptor antagonist
    Used for acute treatment of migraine with or without aura and preventative treatment of episodic migraine in adults
    Delayed serious hypersensitivity observed

    COMMON BRAND NAMES

    NURTEC ODT

    HOW SUPPLIED

    NURTEC ODT Oral Tab Orally Dis: 75mg
    NURTEC ODT Sublingual Tab Orally Dis: 75mg

    DOSAGE & INDICATIONS

    For the acute treatment of migraine with or without aura.
    Oral dosage
    Adults

    75 mg PO as a single dose. Max: 75 mg/day. The safety of using more than 18 doses in a 30-day period has not been established. Coadministration of certain other drugs may need to be avoided or dosage adjustments may be necessary; review drug interactions.[65052]

    For episodic migraine prophylaxis.
    Oral dosage
    Adults

    75 mg PO every other day. Coadministration of certain other drugs may need to be avoided or dosage adjustments may be necessary; review drug interactions.

    MAXIMUM DOSAGE

    Adults

    75 mg/day PO.

    Geriatric

    75 mg/day PO.

    Adolescents

    Safety and efficacy have not been established.

    Children

    Safety and efficacy have not been established.

    Infants

    Safety and efficacy have not been established.

    Neonates

    Safety and efficacy have not been established.

    DOSING CONSIDERATIONS

    Hepatic Impairment

    No dosage adjustment is needed in mild or moderate hepatic impairment (Child-Pugh Class A or B). Avoid rimegepant use in patients with severe hepatic disease (Child-Pugh Class C).

    Renal Impairment

    No dosage adjustment is needed with mild, moderate, or severe renal impairment (CrCl 15 mL/minute or more). Avoid rimegepant use in end-stage renal disease (CrCl less than 15 mL/minute).

    ADMINISTRATION

    Oral Administration
    Oral Solid Formulations

    Oral disintegrating tablets (ODT):
    With dry hands, peel back the foil covering of 1 blister and remove the tablet. Do not push the ODT through the foil.
    Place the tablet on the tongue, or alternatively, under the tongue.
    The ODT will dissolve in saliva and can be swallowed without additional liquid.
    Storage: Take the ODT immediately after opening the blister pack. Do not store the ODT outside the blister pack for future use.[65052]

    STORAGE

    NURTEC ODT:
    - Product should always be stored in the blister and only removed immediately before use
    - Store between 68 to 77 degrees F, excursions permitted 59 to 86 degrees F

    CONTRAINDICATIONS / PRECAUTIONS

    General Information

    Rimegepant is contraindicated in patients with a history of hypersensitivity to rimegepant or any of its excipients. Hypersensitivity reactions can occur days after rimegepant administration, and delayed serious hypersensitivity has occurred. If a hypersensitivity reaction occurs, institute appropriate therapy and discontinue rimegepant.[65052]

    Hepatic disease

    Avoid use of rimegepant in patients with severe hepatic disease (Child-Pugh C). Plasma concentrations of rimegepant were significantly higher in subjects with severe hepatic impairment.[65052]

    Dialysis, renal disease, renal failure

    Avoid use of rimegepant in patients with end-stage renal disease (CrCl less than 15 mL/minute). Rimegepant has not been studied in patients with end-stage renal disease (renal failure) or in patients on dialysis.

    Pregnancy

    There are no adequate data on the developmental risk associated with rimegepant use during human pregnancy. Women with migraine may be at increased risk of preeclampsia and gestational hypertension during pregnancy. Decreased fetal body weight and an increased incidence of fetal variations occurred at the highest dose tested (300 mg/kg/day) after oral administration of rimegepant (0, 10, 60, or 300 mg/kg/day) to pregnant rats during the period of organogenesis. 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. There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to rimegepant during pregnancy. Encourage participation and advise patients to get more information or enroll in the registry by visiting nurtecpregnancyregistry.com, emailing nurtecpregnancyregistry@ppd.com, or calling 1-877-366-0324.[65052]

    Breast-feeding

    There are no data on the presence of rimegepant in human milk, the effects on the breast-fed infant, or the effects on milk production. Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for rimegepant and any potential adverse effects on the breast-fed infant from rimegepant or the underlying maternal condition.[65052]

    ADVERSE REACTIONS

    Severe

    rash / Early / 0-1.0

    Moderate

    dyspnea / Early / 0-1.0

    Mild

    nausea / Early / 2.0-2.7
    dyspepsia / Early / 2.4-2.4
    abdominal pain / Early / 2.4-2.4

    DRUG INTERACTIONS

    Abrocitinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with abrocitinib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and abrocitinib is a P-gp inhibitor.
    Amiodarone: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with amiodarone; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; amiodarone is a moderate CYP3A4 inhibitor and P-gp inhibitor.
    Amobarbital: (Major) Avoid coadministration of rimegepant with amobarbital; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and amobarbital is a moderate CYP3A4 inducer.
    Amoxicillin; Clarithromycin; Omeprazole: (Major) Avoid coadministration of rimegepant with clarithromycin; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; clarithromycin is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Apalutamide: (Major) Avoid coadministration of rimegepant with apalutamide; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and apalutamide is a strong CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Aprepitant, Fosaprepitant: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with aprepitant; fosaprepitant; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and aprepitant; fosaprepitant is a moderate CYP3A4 inhibitor.
    Aspirin, ASA; Butalbital; Caffeine: (Major) Avoid coadministration of rimegepant with butalbital; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and butalbital is a moderate CYP3A4 inducer.
    Aspirin, ASA; Butalbital; Caffeine; Codeine: (Major) Avoid coadministration of rimegepant with butalbital; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and butalbital is a moderate CYP3A4 inducer.
    Atazanavir: (Major) Avoid coadministration of rimegepant with atazanavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and atazanavir is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Atazanavir; Cobicistat: (Major) Avoid coadministration of rimegepant with atazanavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and atazanavir is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold. (Major) Avoid coadministration of rimegepant with cobicistat; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate and cobicistat is a strong CYP3A4 inhibitor and a P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Belladonna Alkaloids; Ergotamine; Phenobarbital: (Major) Avoid coadministration of rimegepant with phenobarbital; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and phenobarbital is a strong CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Berotralstat: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with berotralstat; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; berotralstat is a moderate CYP3A4 inhibitor and a P-gp inhibitor.
    Bexarotene: (Major) Avoid coadministration of rimegepant with bexarotene; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and bexarotene is a moderate CYP3A4 inducer.
    Bosentan: (Major) Avoid coadministration of rimegepant with bosentan; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and bosentan is a moderate CYP3A4 inducer.
    Brigatinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with brigatinib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and brigatinib is a P-gp inhibitor.
    Butabarbital: (Major) Avoid coadministration of rimegepant with butabarbital; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and butabarbital is a moderate CYP3A4 inducer.
    Butalbital; Acetaminophen: (Major) Avoid coadministration of rimegepant with butalbital; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and butalbital is a moderate CYP3A4 inducer.
    Butalbital; Acetaminophen; Caffeine: (Major) Avoid coadministration of rimegepant with butalbital; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and butalbital is a moderate CYP3A4 inducer.
    Butalbital; Acetaminophen; Caffeine; Codeine: (Major) Avoid coadministration of rimegepant with butalbital; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and butalbital is a moderate CYP3A4 inducer.
    Cabozantinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with cabozantinib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and cabozantinib is a P-gp inhibitor.
    Cannabidiol: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with cannabidiol; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and cannabidiol is a P-gp inhibitor.
    Capmatinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with capmatinib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and capmatinib is a P-gp inhibitor.
    Carbamazepine: (Major) Avoid coadministration of rimegepant with carbamazepine; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and carbamazepine is a strong CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Carvedilol: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with carvedilol; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and carvedilol is a P-gp inhibitor.
    Cenobamate: (Major) Avoid coadministration of rimegepant with cenobamate; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and cenobamate is a moderate CYP3A4 inducer.
    Ceritinib: (Major) Avoid coadministration of rimegepant with ceritinib; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and ceritinib is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Chloramphenicol: (Major) Avoid coadministration of rimegepant with chloramphenicol; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and chloramphenicol is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Ciprofloxacin: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with ciprofloxacin; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and ciprofloxacin is a moderate CYP3A4 inhibitor.
    Clarithromycin: (Major) Avoid coadministration of rimegepant with clarithromycin; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; clarithromycin is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Cobicistat: (Major) Avoid coadministration of rimegepant with cobicistat; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate and cobicistat is a strong CYP3A4 inhibitor and a P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Conivaptan: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with conivaptan; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; conivaptan is a moderate CYP3A4 inhibitor and a P-gp inhibitor.
    Crizotinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with crizotinib; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and crizotinib is a moderate CYP3A4 inhibitor.
    Cyclosporine: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with cyclosporine; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; cyclosporine is a moderate CYP3A4 inhibitor and a P-gp inhibitor.
    Dabrafenib: (Major) Avoid coadministration of rimegepant with dabrafenib; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and dabrafenib is a moderate CYP3A4 inducer.
    Daclatasvir: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with daclatasvir; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and daclatasvir is a P-gp inhibitor.
    Danazol: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with danazol; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and danazol is a moderate CYP3A4 inhibitor.
    Darunavir: (Major) Avoid coadministration of rimegepant with darunavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and darunavir is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Darunavir; Cobicistat: (Major) Avoid coadministration of rimegepant with cobicistat; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate and cobicistat is a strong CYP3A4 inhibitor and a P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold. (Major) Avoid coadministration of rimegepant with darunavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and darunavir is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide: (Major) Avoid coadministration of rimegepant with cobicistat; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate and cobicistat is a strong CYP3A4 inhibitor and a P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold. (Major) Avoid coadministration of rimegepant with darunavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and darunavir is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir: (Major) Avoid coadministration of rimegepant with ritonavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; ritonavir is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Delavirdine: (Major) Avoid coadministration of rimegepant with delavirdine; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and delavirdine is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Dexamethasone: (Major) Avoid coadministration of rimegepant with dexamethasone; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and dexamethasone is a moderate CYP3A4 inducer.
    Dextromethorphan; Quinidine: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with quinidine; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and quinidine is a P-gp inhibitor.
    Diltiazem: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with diltiazem; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and diltiazem is a moderate CYP3A4 inhibitor.
    Dronedarone: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with dronedarone; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; dronedarone is a moderate CYP3A4 inhibitor and a P-gp inhibitor.
    Duvelisib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with duvelisib; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and duvelisib is a moderate CYP3A4 inhibitor.
    Efavirenz: (Major) Avoid coadministration of rimegepant with efavirenz; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and efavirenz is a moderate CYP3A4 inducer.
    Efavirenz; Emtricitabine; Tenofovir: (Major) Avoid coadministration of rimegepant with efavirenz; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and efavirenz is a moderate CYP3A4 inducer.
    Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate: (Major) Avoid coadministration of rimegepant with efavirenz; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and efavirenz is a moderate CYP3A4 inducer.
    Elagolix: (Major) Avoid coadministration of rimegepant with elagolix; concurrent use may alter rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate and elagolix is a weak to moderate CYP3A4 inducer and P-gp inhibitor.
    Elagolix; Estradiol; Norethindrone acetate: (Major) Avoid coadministration of rimegepant with elagolix; concurrent use may alter rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate and elagolix is a weak to moderate CYP3A4 inducer and P-gp inhibitor.
    Elexacaftor; tezacaftor; ivacaftor: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with ivacaftor; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and ivacaftor is a P-gp inhibitor.
    Eliglustat: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with eliglustat; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and eliglustat is a P-gp inhibitor.
    Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide: (Major) Avoid coadministration of rimegepant with cobicistat; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate and cobicistat is a strong CYP3A4 inhibitor and a P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate: (Major) Avoid coadministration of rimegepant with cobicistat; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate and cobicistat is a strong CYP3A4 inhibitor and a P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Enasidenib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with enasidenib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and enasidenib is a P-gp inhibitor.
    Enzalutamide: (Major) Avoid coadministration of rimegepant with enzalutamide; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and enzalutamide is a strong CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Erythromycin: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with erythromycin; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; erythromycin is a moderate CYP3A4 inhibitor and a P-gp inhibitor.
    Erythromycin; Sulfisoxazole: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with erythromycin; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; erythromycin is a moderate CYP3A4 inhibitor and a P-gp inhibitor.
    Eslicarbazepine: (Major) Avoid coadministration of rimegepant with eslicarbazepine; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and eslicarbazepine is a moderate CYP3A4 inducer.
    Etravirine: (Major) Avoid coadministration of rimegepant with etravirine; concurrent use may alter rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate and etravirine is a moderate CYP3A4 inducer and P-gp inhibitor.
    Fedratinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with fedratinib; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and fedratinib is a moderate CYP3A4 inhibitor.
    Flibanserin: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with flibanserin; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and flibanserin is a P-gp inhibitor.
    Fluconazole: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with fluconazole; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and fluconazole is a moderate CYP3A4 inhibitor.
    Fluvoxamine: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with fluvoxamine; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and fluvoxamine is a moderate CYP3A4 inhibitor.
    Fosamprenavir: (Major) Avoid coadministration of rimegepant with fosamprenavir; concurrent use may alter rimegepant exposure. Rimegepant is a CYP3A4 substrate and fosamprenavir is a strong CYP3A4 inhibitor and moderate CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Fosphenytoin: (Major) Avoid coadministration of rimegepant with fosphenytoin; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and fosphenytoin is a strong CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Fostamatinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with fostamatinib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and fostamatinib is a P-gp inhibitor.
    Gilteritinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with gilteritinib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and gilteritinib is a P-gp inhibitor.
    Glecaprevir; Pibrentasvir: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with glecaprevir; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and glecaprevir is a P-gp inhibitor. (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with pibrentasvir; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and pibrentasvir is a P-gp inhibitor.
    Grapefruit juice: (Major) Advise patients to avoid coadministration of rimegepant with grapefruit juice; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate and grapefruit juice is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Ibrutinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with ibrutinib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and ibrutinib is a P-gp inhibitor.
    Idelalisib: (Major) Avoid coadministration of rimegepant with idelalisib; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and idelalisib is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Imatinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with imatinib; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and imatinib is a moderate CYP3A4 inhibitor.
    Indinavir: (Major) Avoid coadministration of rimegepant with indinavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and indinavir is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Isavuconazonium: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with isavuconazonium; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; isavuconazonium is a moderate CYP3A4 inhibitor and a P-gp inhibitor.
    Isoniazid, INH; Pyrazinamide, PZA; Rifampin: (Major) Avoid coadministration of rimegepant with rifampin; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and rifampin is a strong CYP3A4 inducer. Coadministration of rimegepant with rifampin decreased rimegepant exposure by 80%.
    Isoniazid, INH; Rifampin: (Major) Avoid coadministration of rimegepant with rifampin; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and rifampin is a strong CYP3A4 inducer. Coadministration of rimegepant with rifampin decreased rimegepant exposure by 80%.
    Istradefylline: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with istradefylline; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and istradefylline is a P-gp inhibitor.
    Itraconazole: (Major) Avoid coadministration of rimegepant with itraconazole; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate and itraconazole is a strong CYP3A4 inhibitor and a P-gp inhibitor. Coadministration of rimegepant with itraconazole increased rimegepant exposure by 4-fold.
    Ivacaftor: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with ivacaftor; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and ivacaftor is a P-gp inhibitor.
    Ketoconazole: (Major) Avoid coadministration of rimegepant with ketoconazole; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; ketoconazole is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Lansoprazole; Amoxicillin; Clarithromycin: (Major) Avoid coadministration of rimegepant with clarithromycin; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; clarithromycin is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Lapatinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with lapatinib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and lapatinib is a P-gp inhibitor.
    Lasmiditan: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with lasmiditan; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and lasmiditan is a P-gp inhibitor.
    Ledipasvir; Sofosbuvir: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with ledipasvir; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and ledipasvir is a P-gp inhibitor.
    Lefamulin: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with oral lefamulin; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and oral lefamulin is a moderate CYP3A4 inhibitor. An interaction is not expected with intravenous lefamulin.
    Letermovir: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with letermovir; concurrent use may increase rimegepant exposure. Avoid concomitant use in patients also receiving cyclosporine because the magnitude of the interaction may be increased. Rimegepant is a CYP3A4 substrate. Letermovir is a moderate CYP3A4 inhibitor; however, when given with cyclosporine, the combined effect on CYP3A4 substrates may be similar to a strong CYP3A4 inhibitor.
    Levoketoconazole: (Major) Avoid coadministration of rimegepant with ketoconazole; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; ketoconazole is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Lomitapide: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with lomitapide; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and lomitapide is a P-gp inhibitor.
    Lonafarnib: (Major) Avoid coadministration of rimegepant with lonafarnib; concurrent use may increase rimegepant exposure. Rimegepant is a substrate of CYP3A4 and P-gp; lonafarnib is a P-gp and strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Lopinavir; Ritonavir: (Major) Avoid coadministration of rimegepant with ritonavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; ritonavir is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Lorlatinib: (Major) Avoid coadministration of rimegepant with lorlatinib; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and lorlatinib is a moderate CYP3A4 inducer.
    Lumacaftor; Ivacaftor: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with ivacaftor; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and ivacaftor is a P-gp inhibitor. (Major) Avoid coadministration of rimegepant with lumacaftor; ivacaftor; concurrent use may alter rimegepant exposure. Rimegepant is a CYP3A4 substrate; lumacaftor is a strong CYP3A4 inducer and ivacaftor is a P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Lumacaftor; Ivacaftor: (Major) Avoid coadministration of rimegepant with lumacaftor; ivacaftor; concurrent use may alter rimegepant exposure. Rimegepant is a CYP3A4 substrate; lumacaftor is a strong CYP3A4 inducer and ivacaftor is a P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Maribavir: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with maribavir; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and maribavir is a P-gp inhibitor.
    Mefloquine: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with mefloquine; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and mefloquine is a P-gp inhibitor.
    Methohexital: (Major) Avoid coadministration of rimegepant with methohexital; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and methohexital is a moderate CYP3A4 inducer.
    Midostaurin: (Major) Avoid coadministration of rimegepant with midostaurin; concurrent use may increase rimegepant exposure. Rimegepant is a substrate of BCRP and midostaurin is a BCRP inhibitor.
    Mifepristone: (Major) Avoid coadministration of rimegepant with mifepristone; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; mifepristone is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Mitapivat: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with mitapivat; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and mitapivat is a P-gp inhibitor.
    Mitotane: (Major) Avoid coadministration of rimegepant with mitotane; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and mitotane is a strong CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Modafinil: (Major) Avoid coadministration of rimegepant with modafinil; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and modafinil is a moderate CYP3A4 inducer.
    Nafcillin: (Major) Avoid coadministration of rimegepant with nafcillin; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and nafcillin is a moderate CYP3A4 inducer.
    Nefazodone: (Major) Avoid coadministration of rimegepant with nefazodone; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and nefazodone is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Nelfinavir: (Major) Avoid coadministration of rimegepant with nelfinavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; nelfinavir is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Neratinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with neratinib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and neratinib is a P-gp inhibitor.
    Netupitant, Fosnetupitant; Palonosetron: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with netupitant; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and netupitant is a moderate CYP3A4 inhibitor.
    Nevirapine: (Major) Avoid coadministration of rimegepant with nevirapine; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and nevirapine is a moderate CYP3A4 inducer.
    Nilotinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with nilotinib; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and nilotinib is a moderate CYP3A4 inhibitor.
    Nirmatrelvir; Ritonavir: (Major) Avoid coadministration of rimegepant with ritonavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; ritonavir is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Ombitasvir; Paritaprevir; Ritonavir: (Major) Avoid coadministration of rimegepant with ritonavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; ritonavir is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Omeprazole; Amoxicillin; Rifabutin: (Major) Avoid coadministration of rimegepant with rifabutin; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and rifabutin is a moderate CYP3A4 inducer.
    Osimertinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with osimertinib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and osimertinib is a P-gp inhibitor.
    Pacritinib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with pacritinib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and pacritinib is a P-gp inhibitor.
    Pexidartinib: (Major) Avoid coadministration of rimegepant with pexidartinib; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and pexidartinib is a moderate CYP3A4 inducer.
    Phenobarbital: (Major) Avoid coadministration of rimegepant with phenobarbital; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and phenobarbital is a strong CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Phenobarbital; Hyoscyamine; Atropine; Scopolamine: (Major) Avoid coadministration of rimegepant with phenobarbital; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and phenobarbital is a strong CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Phenytoin: (Major) Avoid coadministration of rimegepant with phenytoin; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and phenytoin is a strong CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Posaconazole: (Major) Avoid coadministration of rimegepant with posaconazole; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; posaconazole is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Primidone: (Major) Avoid coadministration of rimegepant with primidone; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and primidone is a strong CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Propafenone: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with propafenone; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and propafenone is a P-gp inhibitor.
    Quinidine: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with quinidine; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and quinidine is a P-gp inhibitor.
    Quinine: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with quinine; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and quinine is a P-gp inhibitor.
    Ranolazine: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with ranolazine; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and ranolazine is a P-gp inhibitor.
    Ribociclib: (Major) Avoid coadministration of rimegepant with ribociclib; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and ribociclib is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Ribociclib; Letrozole: (Major) Avoid coadministration of rimegepant with ribociclib; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and ribociclib is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Rifabutin: (Major) Avoid coadministration of rimegepant with rifabutin; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and rifabutin is a moderate CYP3A4 inducer.
    Rifampin: (Major) Avoid coadministration of rimegepant with rifampin; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and rifampin is a strong CYP3A4 inducer. Coadministration of rimegepant with rifampin decreased rimegepant exposure by 80%.
    Rifapentine: (Major) Avoid coadministration of rimegepant with rifapentine; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and rifapentine is a strong CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Rifaximin: (Major) Avoid coadministration of rimegepant with rifaximin; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and rifaximin is a moderate CYP3A4 inducer in vitro. However, in patients with normal liver function, rifaximin at the recommended dosing regimen is not expected to induce CYP3A4. It is unknown whether rifaximin can have a significant effect on the pharmacokinetics of concomitant CYP3A4 substrates in patients with reduced liver function who have elevated rifaximin concentrations.
    Ritonavir: (Major) Avoid coadministration of rimegepant with ritonavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; ritonavir is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Rolapitant: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with rolapitant; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and rolapitant is a P-gp inhibitor.
    Saquinavir: (Major) Avoid coadministration of rimegepant with saquinavir; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; saquinavir is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Sarecycline: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with sarecycline; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and sarecycline is a P-gp inhibitor.
    Secobarbital: (Major) Avoid coadministration of rimegepant with secobarbital; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and secobarbital is a moderate CYP3A4 inducer.
    Sofosbuvir; Velpatasvir: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with velpatasvir; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and velpatasvir is a P-gp inhibitor.
    Sofosbuvir; Velpatasvir; Voxilaprevir: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with velpatasvir; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and velpatasvir is a P-gp inhibitor. (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with voxilaprevir; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and voxilaprevir is a P-gp inhibitor.
    Sorafenib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with sorafenib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and sorafenib is a P-gp inhibitor.
    Sotorasib: (Major) Avoid coadministration of rimegepant with sotorasib; concurrent use may alter rimegepant exposure which may result in loss of efficacy or increased toxicity. Rimegepant is a CYP3A4 and P-gp substrate; sotorasib is a moderate CYP3A4 inducer and P-gp inhibitor.
    St. John's Wort, Hypericum perforatum: (Major) Avoid coadministration of rimegepant with St. John's Wort; concurrent use may significantly decrease rimegepant exposure which may result in loss of efficacy. Rimegepant is a CYP3A4 substrate and St. John's Wort is a strong CYP3A4 inducer. Coadministration of rimegepant with another strong CYP3A4 inducer decreased rimegepant exposure by 80%.
    Telithromycin: (Major) Avoid coadministration of rimegepant with telithromycin; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; telithromycin is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Temsirolimus: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with temsirolimus; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and temsirolimus is a P-gp inhibitor.
    Tepotinib: (Moderate) Avoid a second dose of rimegepant within 48 hours if coadministered with tepotinib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and tepotinib is a P-gp inhibitor.
    Tezacaftor; Ivacaftor: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with ivacaftor; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and ivacaftor is a P-gp inhibitor.
    Ticagrelor: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with ticagrelor; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and ticagrelor is a P-gp inhibitor.
    Tolvaptan: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with tolvaptan; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and tolvaptan is a P-gp inhibitor.
    Trandolapril; Verapamil: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with verapamil; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; verapamil is a moderate CYP3A4 inhibitor and a P-gp inhibitor.
    Tucatinib: (Major) Avoid coadministration of rimegepant with tucatinib; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 and P-glycoprotein (P-gp) substrate; tucatinib is a strong CYP3A4 inhibitor and P-gp inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Vemurafenib: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with vemurafenib; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and vemurafenib is a P-gp inhibitor.
    Venetoclax: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with venetoclax; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and venetoclax is a P-gp inhibitor.
    Verapamil: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with verapamil; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A4 and P-gp substrate; verapamil is a moderate CYP3A4 inhibitor and a P-gp inhibitor.
    Voclosporin: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with voclosporin; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and voclosporin is a P-gp inhibitor.
    Voriconazole: (Major) Avoid coadministration of rimegepant with voriconazole; concurrent use may significantly increase rimegepant exposure. Rimegepant is a CYP3A4 substrate and voriconazole is a strong CYP3A4 inhibitor. Coadministration of rimegepant with another strong CYP3A4 inhibitor increased rimegepant exposure by 4-fold.
    Voxelotor: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with voxelotor; concurrent use may increase rimegepant exposure. Rimegepant is a CYP3A substrate and voxelotor is a moderate CYP3A inhibitor.
    Zonisamide: (Major) Avoid a second dose of rimegepant within 48 hours if coadministered with zonisamide; concurrent use may increase rimegepant exposure. Rimegepant is a P-gp substrate and zonisamide is a P-gp inhibitor.

    PREGNANCY AND LACTATION

    Pregnancy

    There are no adequate data on the developmental risk associated with rimegepant use during human pregnancy. Women with migraine may be at increased risk of preeclampsia and gestational hypertension during pregnancy. Decreased fetal body weight and an increased incidence of fetal variations occurred at the highest dose tested (300 mg/kg/day) after oral administration of rimegepant (0, 10, 60, or 300 mg/kg/day) to pregnant rats during the period of organogenesis. 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. There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to rimegepant during pregnancy. Encourage participation and advise patients to get more information or enroll in the registry by visiting nurtecpregnancyregistry.com, emailing nurtecpregnancyregistry@ppd.com, or calling 1-877-366-0324.[65052]

    There are no data on the presence of rimegepant in human milk, the effects on the breast-fed infant, or the effects on milk production. Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for rimegepant and any potential adverse effects on the breast-fed infant from rimegepant or the underlying maternal condition.[65052]

    MECHANISM OF ACTION

    Rimegepant is a calcitonin gene-related peptide (CGRP) receptor antagonist. CGRP is distributed throughout the nervous system, and it is concentrated at anatomical sites, such as the trigeminovascular system, which are involved in migraine pathophysiology. Centrally, CGRP is involved in nociceptive transmission through second and third-order neurons and pain modulation in the brainstem. Peripherally, CGRP mediates vasodilation through smooth muscle receptors. CGRP concentrations are elevated during acute migraine attacks and may be chronically elevated in chronic migraineurs.[63169] [65052]

    PHARMACOKINETICS

    Rimegepant is administered orally or sublingually. Plasma protein binding of rimegepant is approximately 96%. The steady-state volume of distribution of rimegepant is 120 L. Rimegepant is eliminated mainly through metabolism, primarily by CYP3A4 and to a lesser extent by CYP2C9. Rimegepant is primarily eliminated in unchanged form (approximately 77% of the dose). No major metabolites have been detected in plasma. After oral administration of [14C]-rimegepant to healthy male subjects, 78% of the total radioactivity was recovered in feces and 24% in urine. Unchanged rimegepant is the major single component in excreted feces (42%) and urine (51%). The elimination half-life of rimegepant is approximately 11 hours.[65052]
     
    Affected cytochrome P450 isoenzymes and drug transporters: CYP2C9, CYP3A4, BCRP, OATP1B1, OATP1B3, OAT3, OCT2, P-gp, MATE1
    Rimegepant is a substrate for CYP2C9, CYP3A4, BCRP, and P-gp. Rimegepant is a weak inhibitor of CYP3A4 with time-dependent inhibition. Rimegepant is a weak inhibitor of OATP1B1 and OAT3 and an inhibitor of OATP1B3, OCT2, and MATE1. Administration of rimegepant with BCRP inhibitors is not expected to have a clinically significant impact on rimegepant exposure. In a dedicated interaction study, rimegepant coadministration had no clinically significant impact on the pharmacokinetics of a MATE1 transporter substrate. Clinically relevant drug interactions are not expected with OATP1B3 or OCT2 substrates.[65052]

    Oral Route

    The absolute oral bioavailability of rimegepant is approximately 64%. Peak plasma concentrations occur at approximately 1.5 hours after oral administration. Tmax was delayed by 1 to 1.5 hours when rimegepant was administered with a high-fat or low-fat meal. Cmax and AUC were reduced by 42% to 53% and 32% to 38%, respectively, when rimegepant was administered after a high-fat meal. A low-fat meal reduced rimegepant Cmax by 36% and AUC by 28%. The impact of the reduction in rimegepant exposure because of administration with food on its efficacy is unknown. Rimegepant was administered without regard to food in clinical studies.[65052]