Zavegepant (Zavzpret): Uses, Dose, MOA, Side effects

Drug: Zavegepant

Brand Name: Zavzpret

Class: CGRP antagonist

Manufacturer: Pfizer Pharmaceuticals

Date of FDA Approval: 09th March 2023

Indication: Rapid relief of migraine headache

Formulation: Nasal Spray

The United States Food and Drug Administration (FDA) has granted approval to Zavegepant (Zavzpret, Pfizer) nasal spray for the immediate relief of migraine headaches with or without aura in adults.

It belongs to the class of drugs called CGRP antagonists (calcitonin-gene-related peptide antagonists).

Other drugs from the same class which have already been approved are:

Zavegepant (Zavzpret) Indications:

ZAVZPRET, a medicine made by Pfizer, is given to quickly help with migraine headaches in grown-ups, whether or not there are warning signs.

This medicine is meant for dealing with migraines that are happening right away.

It's not proven to stop migraines from starting.

So, it's not suggested for preventing migraine headaches.

Dosage and administration of Zavzpret:


ZAVZPRET is available in the form of a nasal spray, with a strength of 10 mg of Zavegepant per device.

Recommended dose strength:

  • For adults dealing with migraine headaches, the suggested amount of the medicine is one spray, which has 10 mg of Zavegepant.

  • You spray it into one nostril whenever you need quick relief.
  • The most you should use in a day is 10 mg, which equals one spray.
  • Also, don't use the spray for more than 8 migraine days (meaning 8 sprays) within a 30-day period.

The following table summarizes the dosing information and the dosage form of ZAVZPRET:



Recommended Dose 10 mg as a single spray in one nostril
Maximum Daily Dose 10 mg (one spray) per day
Safety Information No more than 8 migraines in a 30-day period.

Before using the spray, get proper advice regarding its use from your prescriber.

Contraindications to Zavegepant (Zavzpret):

If someone has had an allergic reaction to Zavegepant or any parts of ZAVZPRET before, it's not advised for them to use this medicine.

This caution is because there's a risk of severe allergic reactions in people who are highly sensitive to the medication.

Warning And Precautions

  • Hypersensitivity Reactions:

Using ZAVZPRET may lead to hypersensitivity reactions, which are potential side effects.

In studies, patients treated with this medication experienced skin rashes, hives, swelling of the face, and urticaria.

It's crucial to know that hypersensitivity reactions can be serious and, in some cases, life-threatening.

If someone using ZAVZPRET has a hypersensitivity reaction, it's advised to stop the medication right away and seek appropriate treatment.

This might involve giving medications to ease the symptoms of the allergic reaction or consulting with an allergy specialist for further assessment and care.

Side effects caused by Zavegepant (Zavzpret):

Zavzpret can lead to side effects in some people, so it's important to know about them before using the medication.

Common side effects that some people might experience include:

  • Nausea
  • Fatigue
  • Dry mouth
  • Dizziness
  • Dysgeusia (a taste disturbance)

These side effects are usually mild and temporary. Most people don't need any special treatment for them.

However, there's a possibility of more serious allergic reactions with Zavzpret, showing up as:

  • Facial swelling
  • Urticaria (hives)
  • Angioedema (swelling deeper in the skin)

If someone using Zavzpret notices serious symptoms like facial swelling, hives, or deep skin swelling, it's crucial to get medical help right away.

People experiencing any of these symptoms while using Zavzpret should stop taking the medication immediately and seek appropriate medical attention.

Using Zavzpret has been linked to an increase in heart rate and blood pressure in clinical studies.

While rare, it may also lead to severe cardiovascular events like a heart attack or stroke.

Patients with a history of heart-related issues should be vigilant for any signs or symptoms indicating a potential heart problem.

Other possible side effects of Zavzpret include respiratory tract infection, nasal discomfort, and nasal congestion.

These effects are typically mild and don't usually require specific treatment.

Drug Interaction:

Drug Interaction

Effect of Interaction


Inhibitors of OATP1B3 or NTCP transporters Significant increase in Zavegepant exposure Avoid combining Zavzpret and drugs that inhibit OATP1B3 or NTCP transporters
Inducers of OATP1B3 or NTCP transporters Decrease in Zavegepant exposure Avoid combining Zavzpret with drugs that induce OATP1B3 or NTCP transporters
Intranasal decongestants Decrease in the absorption of zavegepant Avoid or administer at least one-hour of Zavzpret administration

Use in Specific population:


There haven't been studies on the use of Zavzpret in pregnant women, so we don't know the potential risks to the fetus.

Women who experience migraines are already at a higher risk of developing conditions like preeclampsia and gestational hypertension during pregnancy.

Before giving Zavzpret to pregnant women, it's important for healthcare providers to carefully consider clinical factors and potential risks.

Use in breastfeeding:

It's unclear whether Zavegepant or its byproducts are present in human breast milk.

Because there hasn't been a study on mothers using Zavzpret and its potential impact on breastfeeding infants, it's essential to carefully consider the risks and benefits before prescribing it to nursing mothers.

Old aged patients:

The clinical trials for Zavzpret didn't include many people aged 65 and older, so it's not clear if there are differences in how they respond compared to younger adults.

However, a small number of elderly patients were studied, and it was found that there were no notable differences in how the drug is processed and metabolized in their bodies compared to younger individuals.

Liver disease patient:

For individuals with mild (Child-Pugh Class A) or moderate (Child-Pugh Class B) liver impairment, no changes in the dose of the medication are needed.

However, in patients with severe liver impairment (Child-Pugh Class C), it's advisable to avoid using the medication.

This is because the drug hasn't been studied in these patients, and its effects are uncertain.

Kidney disease patient:


Dosage adjustment

≥ 30 mL/min Not necessary
< 30 mL/min Avoid use

Mechanism of action of Zavegepant (Zavzpret):

Zavegepant works as a blocker of the calcitonin gene-related peptide (CGRP) receptor.

Importantly, it doesn't have any significant effects on normal blood pressure or the QT interval, even when taken at a dose up to four times the recommended daily amount.

After a single 10 mg dose using the nasal spray, the highest concentration in the blood is reached around 30 minutes later.

About 5% of the drug is absorbed into the bloodstream (absolute bioavailability).

Using ZAVZPRET once a day for 14 days doesn't show any build-up of the drug in the body.

Around 90% of the drug attaches to proteins in the blood.

In terms of how the body processes it, Zavegepant undergoes metabolism, primarily by CYP3A4, and to a lesser extent by CYP2D6 in laboratory studies.

Its effective half-life, which indicates how long it remains active in the body, is about 6.55 hours.

When the body gets rid of the drug, the major route is through bile (feces), with a smaller amount being eliminated through urine.

Nonclinical Toxicology

Test Name Test Results
Carcinogenesis None detected in animal studies
Mutagenesis None detected in animal studies
Impairment of Fertility No effects on fertility or reproductive performance.