zavegepant

Contraindicated in:

Hypersensitivity;
Severe hepatic impairment;
Severe renal impairment (CCr <30 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 ⬆ ⬇

EENT: nasal discomfort

GI: taste disorders, nausea, vomiting

Misc: hypersensitivity reactions

Interactions ⬆ ⬇

Drug-drug:

Organic anion transporting polypeptide 1B3 (OATP1B3) inhibitors or sodium taurocholate co-transporting 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 co-transporting 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.

Availability ⬆ ⬇

Nasal spray: 10 mg/spray

Route/Dosage ⬆ ⬇

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

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.

Classifications ⬆ ⬇

Therapeutic Classification: vascular headache suppressants

Pharmacologic Classification: calcitonin gene-related peptide receptor antagonists

Pharmacokinetics ⬆ ⬇

Absorption: 5% absorbed following intranasal administration.

Distribution: Extensively distributed to tissues.

Protein Binding: 90%.

Metabolism/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)

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

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 decrease the absorption of zavegepant. If concurrent use is unavoidable, administer intranasal decongestants at least 1 hr after zavegepant administration.
Advise patient to notify health care professional immediately if signs or symptoms of hypersensitivity reactions (shortness of breath, rash, swelling of the face, mouth, tongue, or throat) occur.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Rep: Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

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Indications ⬇

Contraind./Precautions ⬆ ⬇