Brand and Other Names:Chantix
- Classes: Smoking Cessation Aids
Dosing & Uses
Dosage Forms & Strengths
0.5 mg PO once daily for 3 days, then 0.5 mg PO q12hr for 4 days, then 1 mg PO q12hr for 11 weeks
If quitting is successful after 12 weeks, continue another 12 weeks at 1 mg q12hr
Consider a temporary or permanent dose reduction in patients who cannot tolerate the adverse effects
- Mild-to-moderate (CrCl ≥30 mL/min): No dosage adjustment required
- Severe (CrCl <30 mL/min): 0.5 mg PO qDay; may increase to 0.5 mg PO q12hr
- ESRD on hemodialysis: Not to exceed 0.5 mg PO qDay
Take dose after eating with full glass of water
Set date to stop smoking, and start varenicline 1 week before that date; alternatively, the patient can begin varenicline dosing and then quit smoking between days 8 and 35 of treatment
Patients who are motivated to quit, and who did not succeed in stopping smoking during prior varenicline therapy for reasons other than intolerability due to adverse events or who relapsed after treatment, should be encouraged to make another attempt with varenicline once factors contributing to the failed attempt have been identified and addressed
<18 years: Safety and efficacy not established
Serious - Use Alternative
Significant - Monitor Closely
Nausea (15-40%; dose related)
Gastroesophageal reflux disease (GERD)
Fatigue or lethargy
Upper respiratory tract disorder
Frequency Not Defined (selected)
Abnormal liver function tests
Myocardial infarction (MI)
Depression, mania, psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed suicide
Serious skin reactions, including Stevens-Johnson syndrome
Cardiovascular: During nontreatment follow-up to 52 weeks, adjudicated events comparing patients with stable cardiovascular disease to premarket studies included need for coronary revascularization (2.0% vs 0.6%), hospitalization for angina pectoris (1.7% vs 1.1%), and new diagnosis of peripheral vascular disease (PVD) or admission for PVD procedure (1.4% vs 0.6%)
Black Box Warnings
Serious neuropsychiatric events reported, including (but not limited to) depression, suicidal ideation, suicide attempt, and completed suicide; some reported cases may have been complicated by symptoms of nicotine withdrawal in patients who stopped smoking
Depressed mood may be symptom of nicotine withdrawal; depression, rarely including suicidal ideation, reported in smokers undergoing smoking cessation attempt without medication; however, some of these symptoms have occurred in patients taking varenicline who continued to smoke
All patients being treated should be observed for neuropsychiatric symptoms, including changes in behavior, hostility, agitation, depressed mood, and suicide-related events, including ideation, behavior, and attempted suicide
These symptoms have been reported in some patients attempting to quit smoking while taking varenicline in postmarketing experience; most often, symptoms occurred during treatment, but some followed discontinuance
These events have occurred in patients with and without preexisting psychiatric disease; safety and efficacy in patients with serious psychiatric illness (eg, schizophrenia, bipolar disorder, major depressive disorder) have not been established
Advise patients and caregivers that patient should stop taking varenicline and contact healthcare provider immediately if agitation, hostility, depressed mood, or atypical changes in behavior or thinking are observed or if patient develops suicidal ideation or suicidal behavior
Ongoing monitoring and supportive care should be provided until symptoms resolve; risks of varenicline therapy should be weighed against benefits
Documented hypersensitivity or skin reactions to drug or components of formulation
May cause nausea; reduce dose if nausea occurs
Possibility of serious neuropsychiatric disorder, including changes in mood (eg, depression, mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation, hostility, agitation, anxiety, abnormal dreams, and panic, as well as suicidal ideation, suicide attempt, and completed suicide
Seizures reported; some patients had no history of seizures, whereas others had a history of seizure disorder that was remote or well-controlled; in most cases, the seizure occurred within the first month of therapy; use with caution in patients with history of seizures or with other factors that might lower seizure threshold
May cause CNS depression; use caution when performing tasks requiring mental alertness, such as, operating heavy machinery or driving
Hypersensitivity reactions reported, including angioedema
Rare but serious skin reactions reported, including Stevens-Johnson Syndrome and erythema multiforme
- Patients should reduce amount alcohol they consume when initiating therapy until they know whether it increases intoxicating effects
- Postmarketing reports of patients experiencing increased intoxicating effects of alcohol while taking varenicline; some cases described unusual and sometimes aggressive behavior, and were often accompanied by amnesia for the events
- May increase risk of cardiovascular events in patients with underlying cardiovascular disease; randomized, double-blind, placebo-controlled study of 700 patients treated with varenicline for smoking cessation found increases in risk of nonfatal MI, need for revascularization, angina pectoris, and peripheral vascular disease
- In FDA meta-analysis, varenicline (compared with placebo) showed nonsignificant increase in risk for major adverse cardiovascular events (ie, combined outcome of cardiovascular-related death, nonfatal heart attack, and nonfatal stroke); these events were uncommon in both groups
Pregnancy & Lactation
Pregnancy category: C
Lactation: Unknown whether drug is excreted in breast milk; discontinue drug, or do not nurse
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Agonist at nicotinic receptors; acts on mesolimbic dopamine system associated with nicotine addiction, where it prevents nicotine stimulation; stimulates nicotine activity but to lesser degree than nicotine does
Peak plasma time: 3-4 hr
Protein bound: <20%
Excretion: Urine (92%)
Half-life: 24 hr
Excretion: Urine (92%)
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