zavegepant

Action and Spectrum

Actions and Spectrum: 

Actions: 

• zavegepant binds to and blocks the CGRP receptor, which prevents the activation of the receptor by CGRP. 
• By blocking CGRP signaling, zavegepant can inhibit the release of neuropeptides that are involved in migraine pain. 
• zavegepant is highly selective for the CGRP receptor and does not interact with other receptors in the brain, which reduces the risk of side effects. 

Spectrum: 

• zavegepant is being developed as a potential treatment for acute migraine attacks. 
• Clinical studies have shown that zavegepant can provide rapid and sustained relief of migraine pain, as well as reduce the incidence of adverse events. 
• zavegepant has also been evaluated for the treatment of cluster headache, another type of headache disorder. 
• zavegepant has the potential to be used as a first-line therapy for migraine, or as an alternative for patients who do not respond to other treatments or who experience side effects from those treatments. 

Drug Interaction

Adverse Reaction

Frequency defined 

<1%  

Hypersensitivity 

1-10%  

Vomiting (2%) 

Nasal discomfort (3%) 

Nausea (4%) 

>10%  

Taste disorder (18%) 

Black Box Warning

None

Contraindication / Caution

Contraindication / Caution: 

Contraindications: 

Hypersensitivity: zavegepant should not be used in patients who have a known hypersensitivity or allergy to the medication or any of its components. 

Severe liver impairment: zavegepant is primarily metabolized in the liver, and its safety and efficacy have not been established in patients with severe liver impairment.  

Precautions: 

Pregnancy and lactation: The safety and efficacy of zavegepant have not been established in pregnant or lactating women.  

Renal impairment: zavegepant is eliminated primarily by the kidneys. Its safety and efficacy have not been established in patients with severe renal impairment. 

Drug interactions: zavegepant can interact with other medications that are metabolized by the same liver enzymes, such as rifampin or cimetidine.  

Allergic reactions: Allergic reactions, including anaphylaxis, have been reported with zavegepant. Patients should be monitored for signs and symptoms of allergic reactions during and after administration of the medication. 

Cardiovascular effects: zavegepant can cause changes in heart rate and blood pressure. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category

Pharmacology

Pharmacology: 

zavegepant has been shown to be effective in reducing the frequency and severity of migraine headaches.  

Pharmacodynamics: 

It works by blocking the activity of calcitonin gene-related peptide (CGRP), a neuropeptide that is involved in the pathophysiology of migraines. 

Pharmacokinetics: 

Absorption 

When administered intranasally, zavegepant is absorbed through the nasal mucosa and enters the bloodstream. The absorption of zavegepant from the nasal cavity is rapid, and peak plasma concentrations are achieved within 30 minutes to 2 hours after administration. 

Distribution 

zavegepant is distributed throughout the body after it enters the bloodstream. It is highly bound to plasma proteins, primarily albumin, which may limit its distribution to tissues. The volume of distribution of zavegepant is not yet known. 

Metabolism 

zavegepant is metabolized in the liver by enzymes known as cytochrome P450s (CYPs).  

Elimination and Excretion 

zavegepant and its metabolites are excreted primarily in the urine.  

Adminstartion

Administration: 

It is administered intranasally and has a rapid onset of action, with relief of migraine symptoms occurring within two hours of dosing. 

zavegepant is generally well-tolerated, with the most common side effects being nausea, dry mouth, and dizziness. It has not been associated with any significant cardiovascular or hepatic toxicity and does not appear to have any significant drug interactions. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: zavegepant 

Why do we use zavegepant? 

zavegepant is a calcitonin gene-related peptide (CGRP) receptor antagonist that is used for the treatment of acute migraine. CGRP is a neuropeptide that is released during a migraine attack and is believed to play a key role in the pathogenesis of migraine. By blocking the CGRP receptor, zavegepant can reduce inflammation and pain associated with a migraine attack.