varenicline (Rx)

Brand and Other Names:Chantix
  • Print

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 0.5mg
  • 1mg

Smoking Cessation

Set a date to stop smoking and begin varenicline 1 week before this date

Alternatively, the patient can begin varenicline and then quit smoking between days 8 and 35 of treatment

Also see Administration

Quit smoking date regimen

  • Initiate regimen 1 week before quit smoking date
  • Days 1-3: 0.5 mg PO qDay
  • Days 4-7: 0.5 mg PO BID
  • Day 8 to end of treatment: 1 mg PO BID
  • If quitting is successful after 12 weeks, continue another 12 weeks at 1 mg q12hr

Gradual approach to quitting

  • For patients who are sure that they are not able or willing to quit abruptly, consider a gradual approach to quitting smoking with varenicline
  • Begin dosing and reduce smoking by 50% from baseline within the first 4 weeks, by an additional 50% in the next 4 weeks, and continue reducing with the goal of reaching complete abstinence by 12 weeks
  • Continue varenicline for an additional 12 weeks, for a total of 24 weeks of treatment
  • Encourage patients to attempt quitting sooner if they feel ready

Dosage Modifications

Consider a temporary or permanent dose reduction in patients who cannot tolerate the adverse effects

Renal impairment

  • Mild-to-moderate (CrCl ≥30 mL/min): No dosage adjustment required
  • Severe (CrCl <30 mL/min): 0.5 mg PO qDay initially; may increase to 0.5 mg PO q12hr
  • ESRD on hemodialysis: Not to exceed 0.5 mg PO qDay

<18 years: Safety and efficacy not established

Next:

Interactions

Interaction Checker

and varenicline

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            All Interactions Sort By:
             activity indicator 
            Previous
            Next:

            Adverse Effects

            >10%

            Nausea (15-40%; dose related)

            Abnormal dreams

            Headache

            Insomnia

            1-10%

            Appetite changes

            Chest pain

            Constipation

            Dry mouth

            Dyspepsia

            Dyspnea

            Flatulence

            Gastroesophageal reflux disease (GERD)

            Fatigue or lethargy

            Pruritus

            Rash

            Somnolence

            Rhinorrhea

            Vomiting

            Upper respiratory tract disorder

            Frequency Not Defined (selected)

            Abnormal liver function tests

            Anemia

            Anxiety

            Arrhythmia

            Arthralgia

            Depression

            Diarrhea

            Dizziness

            Epistaxis

            Hypertension

            Myocardial infarction (MI)

            Polyuria

            Respiratory disorder

            Postmarketing Reports

            Depression, mania, psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed suicide, somnambulism

            Serious skin reactions, including Stevens-Johnson syndrome

            Cerebrovascular accident

            Seizures

            MI

            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%)

            Irritability

            Agitation

            Somnambulism

            Previous
            Next:

            Warnings

            Contraindications

            Documented hypersensitivity or skin reactions to drug or components of formulation

            Nonsmokers

            Cautions

            May cause nausea; reduce dose if nausea occurs

            Somnambulism reported, including cases describing harmful behavior to self, others, or property; instruct patients to discontinue varenicline and notify their healthcare professional

            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

            Neuropsychiatric adverse effects

            • Serious neuropsychiatric adverse events reported; these postmarketing reports include changes in mood (including depression and mania), psychosis, hallucinations, paranoia, delusions, homicidal ideation, aggression, hostility, agitation, anxiety, and panic, as well as suicidal ideation, suicide attempt, and completed suicide
            • Some patients who stopped smoking may have been experiencing symptoms of nicotine withdrawal, including depressed mood
            • Depression, rarely including suicidal ideation, has been reported in smokers undergoing a smoking cessation attempt without medication; however, some of these adverse events occurred in patients taking varenicline who continued to smoke
            • Neuropsychiatric adverse events occurred in patients without and with pre-existing psychiatric disease; some patients experienced worsening of their psychiatric illnesses
            • Some neuropsychiatric adverse events, including unusual and sometimes aggressive behavior directed to oneself or others, may have been worsened by concomitant use of alcohol
            • Advise patients and caregivers that the patient should stop taking varenicline and contact a healthcare provider immediately if agitation, depressed mood, or changes in behavior or thinking that are not typical are observed, or if the patient develops suicidal ideation or suicidal behavior

            Alcohol interaction

            • 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

            Cardiovascular risk

            • 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
            Previous
            Next:

            Pregnancy & Lactation

            Pregnancy

            Available data have not suggested increased risk for major birth defects following exposure to varenicline in pregnancy, compared with women who smoke; smoking during pregnancy causes increased risks of orofacial clefts, premature rupture of membranes, placenta previa, placental abruption, ectopic pregnancy, fetal growth restriction and low birth weight, stillbirth, preterm delivery and shortened gestation, neonatal death, sudden infant death syndrome and reduction of lung function in infants; it is not known whether quitting smoking with varenicline during pregnancy reduces these risks

            Lactation

            Because there are no data on presence of varenicline in human milk and effects on breastfed infant, breastfeeding women should monitor their infant for seizures and excessive vomiting, which are adverse reactions that have occurred in adults that may be clinically relevant in breastfeeding infants

            Pregnancy Categories

            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.

            Previous
            Next:

            Pharmacology

            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

            Absorption

            Completely absorbed

            Bioavailability: High

            Peak plasma time: 3-4 hr

            Distribution

            Protein bound: <20%

            Metabolism

            Minimally metabolized

            Elimination

            Excretion: Urine (92%)

            Half-life: 24 hr

            Excretion: Urine (92%)

            Previous
            Next:

            Administration

            Oral Administration

            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

            Previous
            Next:

            Images

            Previous
            Next:

            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Additional Offers
            Email to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Email Forms to Patient

            From:

            To:

            The recipient will receive more details and instructions to access this offer.

            By clicking send, you acknowledge that you have permission to email the recipient with this information.

            Previous
            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.