varenicline intranasal

Action and Spectrum

Actions and Spectrum: 

Through activation of the trigeminal parasympathetic nerve pathway, varenicline intranasal enhances the stimulation of nicotinic cholinergic receptors and promotes an increase in basal tear film production, ultimately resulting in enhanced outcomes pertaining to tear film production. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Cough (16%) 

Sneezing (82%) 

Throat irritation (13%) 

1-10% 

Nasal irritation (8%) 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

• Hypersensitivity: varenicline should not be used in individuals with known hypersensitivity/allergy to varenicline or its components. 
• History of psychiatric disorders: varenicline has been associated with neuropsychiatric symptoms such as changes in behavior, agitation, depression, suicidal ideation, and suicide attempts. Individuals with a history of psychiatric disorders should be closely monitored while taking varenicline. 
• Pregnancy and breastfeeding: Safety of varenicline during pregnancy condition and breastfeeding has not been established. Avoiding varenicline use in these situations is typically recommended unless potential benefits outweighs the risks. Pregnant or breastfeeding individuals should consult with their healthcare provider for guidance. 

Caution 

• Psychiatric effects: varenicline has been associated with neuropsychiatric symptoms such as changes in behavior, agitation, depression, suicidal ideation, and suicide attempts. Individuals should be closely monitored for these symptoms, particularly those with a history of psychiatric disorders.  
• Cardiovascular events: There have been post-marketing reports of cardiovascular events, like the heart attack and stroke, in patients taking varenicline. Individuals with a history of cardiovascular disease should use varenicline cautiously, and healthcare providers should weigh the potential risks against the benefits before prescribing the medication. 
• Seizures: varenicline has been associated with seizures in some individuals. Caution is advised in patients with a prior history of seizures or other factors that may increase the risk of seizures. 
• Renal impairment: varenicline is primarily excreted through the kidneys. Patients with moderate-severe renal impairment should use varenicline cautiously, and dosage adjustments may be necessary. 
• Use in elderly patients: Elderly patients may be more susceptible to the adverse effects of varenicline. Careful monitoring and appropriate dose adjustments should be considered. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• 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 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: 

varenicline intranasal stimulates nicotinic cholinergic receptors and basal tear film production through the trigeminal parasympathetic nerve pathway, leading to improved outcomes related to tear film production. This intranasal formulation provides an effective alternative for managing DED, particularly for patients who struggle with ophthalmic product administration. 

Pharmacodynamics: 

Mechanism of action: The action of varenicline intranasal in dry eye disease involves the activation of the trigeminal parasympathetic pathway. By activating this pathway, varenicline increases tear film production, which helps alleviate the symptoms of dry eye disease.  

Pharmacokinetics: 

Absorption 

The absorption of varenicline intranasal occurs through the nasal mucosa. Once it is administered, the drug is absorbed into the bloodstream, allowing it to exert its pharmacological effects on the body. 

Distribution 

After absorption, varenicline is distributed throughout the body via the bloodstream. The drug reaches various tissues and organs, including the target tissues involved in dry eye disease. 

Metabolism 

varenicline undergoes metabolism primarily in the liver. 

Elimination and Excretion 

varenicline, including the intranasal formulation, is primarily eliminated from the body through renal excretion. The drug is excreted in the urine without undergoing significant metabolism. 

Adminstartion

Administration: 

The standard recommended dosage for varenicline is to start with a low dose and gradually increase it over several days to reach the maintenance dose. The specific dosing instructions and duration of treatment may vary depending on individual factors and the prescribing healthcare provider’s recommendations. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: varenicline intranasal 

Pronounced: [ ver-EN-e-kleen ] 

Why do we use varenicline intranasal? 

varenicline intranasal is a medication for dry eye disease (DED). It is administered as a liquid spray in the nose and works by increasing tear production. 

• Dry Eye Disease (DED): varenicline intranasal has been specifically developed and approved by the FDA as a treatment for DED. Clinical studies have shown that varenicline intranasal significantly improves DED’s signs and symptoms over four weeks. It enhances tear production, which helps alleviate the dryness and discomfort associated with the condition. The medication offers an alternative for patients who struggle with the administration of ophthalmic products such as eye drops