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varenicline (Rx)Brand and Other Names:Chantix

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 0.5mg
  • 1mg
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Smoking Cessation

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

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; may increase to 0.5 mg PO q12hr
  • ESRD on hemodialysis: Not to exceed 0.5 mg PO qDay

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

<18 years: Safety and efficacy not established

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Interactions

Interaction Checker

varenicline and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            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

            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%)

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            Warnings

            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

            Contraindications

            Documented hypersensitivity or skin reactions to drug or components of formulation

            Nonsmokers

            Cautions

            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

            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
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            Pregnancy & Lactation

            Pregnancy category: C

            Lactation: Unknown whether drug is excreted in breast milk; discontinue drug, or do not nurse

            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.

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            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%)

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            Images

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            Formulary

            FormularyPatient Discounts

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            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.
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