Varenicline

Chantix

Smoking cessation • Nicotinic receptor partial agonist

Half-life

24 hours

Protein Binding

<20%

Metabolized By

Minimal metabolism

External

Partial agonist at alpha-4/beta-2 nicotinic receptors; reduces craving and withdrawal

Drug Class

Smoking cessation

Subclass

Nicotinic receptor partial agonist

Chantix

Half-life

24 hours

Time for plasma concentration to decrease by 50%

Protein Binding

<20%

Fraction bound to plasma proteins

Therapeutic Index

Wide

Margin between therapeutic and toxic doses

•Neuropsychiatric events (behavior changes, hostility, suicidal ideation) — boxed warning removed in 2016 but monitor closely