Pfizer; patent expires 2018.
Dual mechanism of action: 1) Partial agonist at nicotinic receptors, mimicking nicotine
effects on the brain; 2) Blocks nicotine from binding to these receptors, thereby decreasing the
reinforcing effect of smoking.
Supplied as 0.5 mg white tablet and 1 mg light blue tablet.
Because of high risk of nausea, titrate slowly: Days 1-3: 0.5 mg/day; Days 4-7: 0.5 mg BID;
thereafter: 1 mg BID. Continue for 12-24 weeks depending on response.
Most convenient way to prescribe: “Starting Month Pak,” which contains 0.5 mg x 11 tablets
and 1 mg x 42 tablets.
Price varies depending on pharmacy, but a month-long course costs around $130.00.
Patients should take it after eating and with a full glass of water.
Quit rates about 40% after 3 to 4 months, vs. 30% with Zyban and 20% with placebo.
Most common: nausea (30%-40% of patients), insomnia, constipation, flatulence.
Not a controlled substance, no abuse potential.
Can be combined with Zyban.
When combined with nicotine replacement therapy, causes a high incidence of nausea,
headache, vomiting, and dizziness.
No other drug interactions
Half-life 24 hours.
Excreted unchanged in urine, no hepatic metabolism.
Patients should set a quit date and start Chantix one week before quitting.