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Varenicline

Generic Name
Varenicline
Brand Names
Champix, Chantix, Tyrvaya
Drug Type
Small Molecule
Chemical Formula
C13H13N3
CAS Number
249296-44-4
Unique Ingredient Identifier
W6HS99O8ZO
Background

Varenicline is a prescription medication used to treat smoking addiction. This medication is the first approved nicotinic receptor partial agonist. Specifically, varenicline is a partial agonist of the alpha4/beta2 subtype of the nicotinic acetylcholine receptor. In addition it acts on alpha3/beta4 and weakly on alpha3beta2 and alpha6-containing receptors. A full agonism was displayed on alpha7-receptors.

On March 9, 2015, the U.S. Food and Drug Administration warned that Varenicline, in the form of Pfizer Inc's quit-smoking drug, Chantix, has been associated with seizures and that some patients who drink while taking the drug may become aggressive or black out. Pfizer is conducting an additional safety study of the drug, results of which are expected in late 2015. The FDA said it is keeping the black box in place at least until the results of the trial are announced.

Indication

For use as an aid in smoking cessation.

Varenicline as a nasal spray is indicated for the symptomatic treatment of dry eye disease.

Associated Conditions
Dry Eye Syndrome (DES)
Associated Therapies
Smoking, Cessation
Clinical Trials
Related News

Varenicline Shows Promising Results for Youth Vaping Cessation in Landmark Trial

• A groundbreaking clinical trial reveals varenicline combined with remote behavioral counseling achieved 51% vaping abstinence rates in youth compared to 14% with placebo during the final four weeks of treatment. • The study, published in JAMA, is the first pharmacotherapy trial for nicotine vaping cessation specifically targeting individuals aged 16-25, addressing a critical gap in treatment options for this vulnerable population. • Despite some adverse events like nausea and vivid dreams, varenicline was generally well-tolerated, offering a potential evidence-based intervention for the 7.8% of high school students and 24.1% of young adults who reported recent e-cigarette use.

Genetic Variants Influence Success of Smoking Cessation Drug Varenicline, Landmark Study Finds

• University of Leicester researchers conducted the first genome-wide study revealing genetic variations affect varenicline's effectiveness in smoking cessation, offering new insights into personalized treatment approaches. • The comprehensive analysis utilizing UK Biobank and international health records identified specific DNA variants linked to successful smoking cessation with varenicline treatment. • The groundbreaking findings illuminate the biological mechanisms underlying varenicline-aided smoking cessation, though researchers emphasize the need for larger confirmatory studies.

GLP-1 Agonists Show Promise in Addiction Treatment: Beyond Weight Loss

• GLP-1 agonists, initially for diabetes and obesity, are being explored for their potential in treating substance use disorders by targeting brain mechanisms. • Studies suggest GLP-1 agonists may reduce cravings for addictive substances by impacting the brain's reward system, showing potential in reducing binge drinking and opioid overdoses. • Clinical trials are underway to investigate the efficacy of GLP-1 agonists like semaglutide in treating various substance use disorders, with results expected in the coming years. • Experts emphasize that while promising, GLP-1 medications should be part of a comprehensive treatment plan, including community support and therapy, for individuals with addiction.
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