General

Pronunciation:
za-ve-je-pant

Trade Name(s)

• Zavzpret

Ther. Class.

vascular headache suppressants

Pharm. Class.

calcitonin gene-related peptide receptor antagonists

Indications

Acute treatment of migraine with or without aura.

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.

Pharmacokinetics

Absorption: 5% absorbed following intranasal administration.

Distribution: Extensively distributed to tissues.

Protein Binding: 90%.

Metabolism and Excretion: Primarily metabolized in liver via the CYP3A4 isoenzyme and to a lesser extent by the CYP2D6 isoenzyme. Primarily excreted as unchanged drug in feces (80%) and urine (11%).

Half-life: 6.55 hr.

TIME/ACTION PROFILE (relief of migraine pain)

Contraindication/Precautions

Contraindicated in:

• Hypersensitivity;
• Severe renal impairment;
• Severe hepatic impairment.

Use Cautiously in:

• Hypertension;
• Raynaud phenomenon;
• OB:   Safety not established in pregnancy;
• Lactation:  Safety not established in breastfeeding;
• Pedi:   Safety and effectiveness not established in children.

Adverse Reactions/Side Effects

CV: hypertension, Raynaud phenomenon

EENT: nasal discomfort

GI: taste disorders, nausea, vomiting

Misc: hypersensitivity reactions

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

Interactions

Drug-Drug

•  Organic anion transporting polypeptide 1B3 (OATP1B3) inhibitors  or  sodium taurocholate cotransporting polypeptide (NTCP) transporter inhibitors, including  rifampin, may ↑ levels and risk of toxicity; avoid concurrent use.
•  Organic anion transporting polypeptide 1B3 (OATP1B3) inducers  or  sodium taurocholate cotransporting polypeptide (NTCP) transporter inducers  may ↓ levels and effectiveness; avoid concurrent use.
•  Intranasal decongestants  may ↓ absorption of zavegepant; avoid concurrent use. If concurrent use unavoidable, administer intranasal decongestant ≥1 hr after zavegepant.

Route/Dosage

Intranasal (Adults): Single dose of 10 mg in one nostril.

Availability

Nasal spray: 10 mg/spray

Assessment

• Assess pain location, character, intensity, duration, and associated symptoms (photophobia, phonophobia, nausea, vomiting) of migraine pain.
• Monitor frequency of migraine headaches.
• Monitor BP periodically and more frequently in patients with pre-existing HTN.
• Monitor for signs and symptoms of hypersensitivity reactions (anaphylaxis, dyspnea, rash, pruritus, urticaria, facial edema).  If hypersensitivity reaction occurs,  discontinue zavegepant and treat appropriately.

Implementation

• Intranasal Administer a single 10 mg spray in one nostril, as needed. Do not administer more than one spray in each 24 hr period.

Patient/Family Teaching

• Instruct patient to administer zavegepant as directed. Do not test or prime the nasal spray before use. Advise patient to read the  Patient Information  before starting therapy and with each Rx refill in case of changes.
• Advise patient to avoid using intranasal decongestants with zavegepant; may ↓ absorption of zavegepant. If concurrent use is unavoidable, administer intranasal decongestants ≥1 hr after zavegepant administration.
• Advise patient to notify health care provider immediately if signs or symptoms of hypersensitivity reactions (shortness of breath; rash; swelling of the face, mouth, tongue, or throat) occur.
• Advise patient to report symptoms of ↑ BP or worsening pre-existing hypertension.
• 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.
• Rep:  Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.

Evaluation/Desired Outcomes

Decrease in pain and symptoms associated with migraine headaches.