Dosing & Uses
Dosage Forms & Strengths
intranasal solution
- 10mg/spray
Migraine
Indicated for acute treatment of migraine with or without aura
10 mg single spray in 1 nostril PRN
Not to exceed 10 mg/24 hr period
Safety of treating >8 migraines/30 days has not been established
Dosage Modifications
Renal impairment
- CrCl ≥30 mL/min: No dosage adjustment necessary
- CrCl <30 mL/min: Avoid use; not studied
Hepatic impairment
- Mild or moderate (Child-Pugh A or B): No dosage adjustment necessary
- Severe (Child-Pugh C): Avoid use
Dosing Considerations
Limitation of use
- Not indicated for migraine prevention
Safety and efficacy not established
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (0)
Serious - Use Alternative (29)
- clarithromycin
clarithromycin will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- cyclosporine
cyclosporine will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 and NTCP inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP13B and NTCP substrate).
- daclatasvir
daclatasvir will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- encorafenib
encorafenib will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- erythromycin base
erythromycin base will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- erythromycin ethylsuccinate
erythromycin ethylsuccinate will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- erythromycin lactobionate
erythromycin lactobionate will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- erythromycin stearate
erythromycin stearate will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- ezetimibe
ezetimibe will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. NTCP inhibitors may result in a significant increase in systemic exposure of zavegepant (a NTCP substrate).
- fostemsavir
fostemsavir will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- glecaprevir/pibrentasvir
glecaprevir/pibrentasvir will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- indomethacin
indomethacin will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. NTCP inhibitors may result in a significant increase in systemic exposure of zavegepant (a NTCP substrate).
- irbesartan
irbesartan will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. NTCP inhibitors may result in a significant increase in systemic exposure of zavegepant (a NTCP substrate).
- levocarnitine
levocarnitine will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. NTCP inhibitors may result in a significant increase in systemic exposure of zavegepant (a NTCP substrate).
- naphazoline
naphazoline will decrease the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of intranasal decongestants with zavegepant intranasal. If unavoidable, administer intranasal decongestants at least 1 hr after zavegepant.
- oxymetazoline intranasal
oxymetazoline intranasal will decrease the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of intranasal decongestants with zavegepant intranasal. If unavoidable, administer intranasal decongestants at least 1 hr after zavegepant.
- phenylephrine nasal
phenylephrine nasal will decrease the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of intranasal decongestants with zavegepant intranasal. If unavoidable, administer intranasal decongestants at least 1 hr after zavegepant.
- pioglitazone
pioglitazone will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. NTCP inhibitors may result in a significant increase in systemic exposure of zavegepant (a NTCP substrate).
- propylhexedrine
propylhexedrine will decrease the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of intranasal decongestants with zavegepant intranasal. If unavoidable, administer intranasal decongestants at least 1 hr after zavegepant.
- rifampin
rifampin will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- rifamycin
rifamycin will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- rosiglitazone
rosiglitazone will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. NTCP inhibitors may result in a significant increase in systemic exposure of zavegepant (a NTCP substrate).
- simvastatin
simvastatin will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. NTCP inhibitors may result in a significant increase in systemic exposure of zavegepant (a NTCP substrate).
- sulfasalazine
sulfasalazine will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. NTCP inhibitors may result in a significant increase in systemic exposure of zavegepant (a NTCP substrate).
- trofinetide
trofinetide will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. Trofinetide (an OATP131 and OATP13B inhibitor) may increase plasma levels of OATP131 or OATP13B substrates. Avoid coadministration with sensitive substrates.
- velpatasvir
velpatasvir will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- voxilaprevir
voxilaprevir will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. OATP1B3 inhibitors may result in a significant increase in systemic exposure of zavegepant (an OATP1B3 substrate).
- xylometazoline
xylometazoline will decrease the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. Avoid coadministration of intranasal decongestants with zavegepant intranasal. If unavoidable, administer intranasal decongestants at least 1 hr after zavegepant.
- zafirlukast
zafirlukast will increase the level or effect of zavegepant intranasal by Other (see comment). Avoid or Use Alternate Drug. NTCP inhibitors may result in a significant increase in systemic exposure of zavegepant (a NTCP substrate).
Monitor Closely (0)
Minor (0)
Adverse Effects
>10%
Taste disorder (18%)
1-10%
Nausea (4%)
Nasal discomfort (3%)
Vomiting (2%)
<1%
Hypersensitivity, including facial swelling and urticaria
Warnings
Contraindications
History of hypersensitivity to zavegepant or other ingredients
Cautions
Hypersensitivity reactions reported, including facial swelling and urticaria; initiate appropriate therapy if hypersensitivity occurs
Ask patient to discuss prescription, OTC medications, or herbal supplements that they take or plan to take
Drug interaction overview
- Substrate of OATP1B3 and NTCP
-
OATP1B3 or NTCP inhibitors
- Avoid coadministration
- Inhibitors of organic anion transporting polypeptide 1B3 (OATP1B3) or sodium taurocholate cotransporting polypeptide (NTCP) transporters may significantly increase zavegepant exposure
-
OATP1B3 or NTCP inducers
- Avoid coadministration
- Inducers of OATP1B3 or NTCP transporters may decrease zavegepant exposure
-
Intranasal decongestants
- Dosage modification
- Avoid coadministration; if unavoidable, administer intranasal decongestants at least 1 hr after zavegepant
- Coadministration may decrease systemic exposure and efficacy of zavegepant
Pregnancy & Lactation
Pregnancy
Data are not available on developmental risk associated with the use in pregnant females
Animal studies
- No adverse developmental effects have been observed following SC administration to pregnant animals at doses associated with plasma exposures higher than those used clinically
Clinical considerations
- Data suggest that women with migraine may be at increased risk for preeclampsia and gestational hypertension during pregnancy
Lactation
Data are unavailable regarding the presence of zavegepant or its metabolites in human milk, effects on breastfed infants, or effects on milk production
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Calcitonin gene-related peptide (CGRP) receptor antagonist; binds to CGRP receptor, which is thought to be causally involved in migraine pathophysiology
Absorption
Peak plasma concentration: ~30 minutes
Absolute bioavailability: ~5%
Distribution
Protein bound: ~90%
Vd: 1774 L
Metabolism
Metabolized primarily by CYP3A4 and to a lesser extent by CYP2D6
Unchanged zavegepant was most prevalent (~90%) circulating component in human plasma
No major metabolites (ie, >10%) were detected in plasma
Elimination
Half-life: 6.55 hr
Clearance: 266 L/hr
Excretion
- Primarily excreted via biliary/fecal route
- Feces ~80%; urine 11% (recovered as unchanged drug after single 5-mg IV dose)
Administration
Intranasal Administration
Do not test spray, prime, or press plunger before use
Each individual unit only sprays 1 time and cannot be reused
For intranasal use only
Storage
Store at controlled room temperature, 20-25ºC (68-77ºF); excursions permitted to 15-30ºC (59-86ºF)
Do not freeze
Do not test spray, prime, or press plunger before use
Images
Formulary
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