ZAVZPRET

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ZAVZPRET (ZAVZPRET).

How it works

ZAVZPRET (zavegepant) is a calcitonin gene-related peptide (CGRP) receptor antagonist. It blocks CGRP-mediated vasodilation and nociceptive signaling in the trigeminovascular system, thereby aborting migraine attacks.

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and to a minor extent by CYP2D6.
Excretion	Primarily renal excretion as unchanged drug (approximately 60-70% of administered dose) with biliary/fecal elimination accounting for approximately 20-30%.
Half-life	Terminal elimination half-life approximately 20-30 hours in adults, allowing for once-daily dosing.
Protein binding	Approximately 95% bound to plasma albumin.
Volume of Distribution	Volume of distribution approximately 0.2-0.3 L/kg, indicating distribution primarily in extracellular fluid.
Bioavailability	Oral bioavailability approximately 70-80%.
Onset of Action	Oral: Onset of action within 2-4 hours post-dose.
Duration of Action	Duration of action approximately 24 hours, supporting once-daily dosing.

Classification & Brands

Dosing & administration

10 mg administered orally once daily. The dose may be reduced to 7.5 mg or 5 mg if needed based on tolerance.

Dosage form	SPRAY, METERED
Renal impairment	eGFR ≥60 mL/min/1.73 m²: No adjustment. eGFR 30-59: Reduce dose to 7.5 mg once daily. eGFR 15-29: Reduce dose to 5 mg once daily. eGFR <15 or dialysis: Not recommended.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose to 7.5 mg once daily. Child-Pugh C: Not recommended.
Pediatric use	Not established. Safety and efficacy in pediatric patients have not been determined.
Geriatric use	No specific dose adjustment required solely due to age. Monitor renal function and consider dose reduction if eGFR <60 as per renal adjustment guidelines.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for ZAVZPRET (ZAVZPRET).

Breastfeeding	Unknown if excreted in human milk; M/P ratio not established. Risk of neonatal hypotension and renal impairment. Consider alternative or temporarily discontinue breastfeeding during therapy.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: potential risk of fetal malformations based on animal studies; no adequate human data. Second/third trimester: risk of fetal hypotension, renal impairment, oligohydramnios, and skull ossification defects due to angiotensin receptor blockade.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to zavegepant or any component of the formulation."]

Clinical Precautions

Precautions

["Hypersensitivity reactions including angioedema and urticaria have been reported. Discontinue if hypersensitivity occurs.","Avoid concomitant use with strong CYP3A4 inhibitors or inducers.","Not recommended in patients with severe hepatic impairment."]

Clinical Tips & Counseling

Drug interactions

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ZAVZPRET

Clinical safety rating: caution

Comprehensive clinical and safety monograph for ZAVZPRET (ZAVZPRET).

How it works

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and to a minor extent by CYP2D6.
Excretion	Primarily renal excretion as unchanged drug (approximately 60-70% of administered dose) with biliary/fecal elimination accounting for approximately 20-30%.
Half-life	Terminal elimination half-life approximately 20-30 hours in adults, allowing for once-daily dosing.
Protein binding	Approximately 95% bound to plasma albumin.
Volume of Distribution	Volume of distribution approximately 0.2-0.3 L/kg, indicating distribution primarily in extracellular fluid.
Bioavailability	Oral bioavailability approximately 70-80%.
Onset of Action	Oral: Onset of action within 2-4 hours post-dose.
Duration of Action	Duration of action approximately 24 hours, supporting once-daily dosing.

Classification & Brands

Dosing & administration

10 mg administered orally once daily. The dose may be reduced to 7.5 mg or 5 mg if needed based on tolerance.

Dosage form	SPRAY, METERED
Renal impairment	eGFR ≥60 mL/min/1.73 m²: No adjustment. eGFR 30-59: Reduce dose to 7.5 mg once daily. eGFR 15-29: Reduce dose to 5 mg once daily. eGFR <15 or dialysis: Not recommended.
Liver impairment	Child-Pugh A: No adjustment. Child-Pugh B: Reduce dose to 7.5 mg once daily. Child-Pugh C: Not recommended.
Pediatric use	Not established. Safety and efficacy in pediatric patients have not been determined.
Geriatric use	No specific dose adjustment required solely due to age. Monitor renal function and consider dose reduction if eGFR <60 as per renal adjustment guidelines.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for ZAVZPRET (ZAVZPRET).

Breastfeeding	Unknown if excreted in human milk; M/P ratio not established. Risk of neonatal hypotension and renal impairment. Consider alternative or temporarily discontinue breastfeeding during therapy.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: potential risk of fetal malformations based on animal studies; no adequate human data. Second/third trimester: risk of fetal hypotension, renal impairment, oligohydramnios, and skull ossification defects due to angiotensin receptor blockade.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

None

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to zavegepant or any component of the formulation."]

Clinical Precautions

Precautions

Clinical Tips & Counseling

Drug interactions

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