Medically reviewed on Nov 15, 2018
(var EN i kleen)
- Varenicline Tartrate
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Chantix: 0.5 mg, 1 mg
Chantix Continuing Month Pak: 1 mg
Chantix Starting Month Pak: 0.5 mg x 11 & 1 mg x 42
Brand Names: U.S.
- Chantix Continuing Month Pak
- Chantix Starting Month Pak
- Partial Nicotine Agonist
- Smoking Cessation Aid
Partial neuronal α4 β2 nicotinic receptor agonist; prevents nicotine stimulation of mesolimbic dopamine system associated with nicotine addiction. Also binds to 5-HT3 receptor (significance not determined) with moderate affinity. Varenicline stimulates dopamine activity but to a much smaller degree than nicotine does, resulting in decreased craving and withdrawal symptoms.
Well absorbed; unaffected by food
Minimal (<10% of clearance is through metabolism)
Urine (92% as unchanged drug)
Time to Peak
Plasma: ~3 to 4 hours
Special Populations: Renal Function Impairment
Moderate renal impairment (CrCl ≥30 to ≤50 mL/minute): Drug exposure increased 1.5-fold
Severe renal impairment (CrCl <30 mL/minute): Drug exposure increased 2.1-fold
End-stage renal disease (ESRD) requiring hemodialysis: Drug exposure increased 2.7-fold
Use: Labeled Indications
Smoking cessation: As an aid to smoking cessation treatment
Serious hypersensitivity reactions or skin reactions to varenicline or any component of the formulation
Smoking cessation: Oral:
Days 1 to 3: 0.5 mg once daily
Days 4 to 7: 0.5 mg twice daily
Maintenance (≥ Day 8): 1 mg twice daily for 11 weeks; may consider a temporary or permanent dose reduction if usual dose is not tolerated.
Note: Start 1 week before target quit date. Alternatively, patients may consider setting a quit date up to 35 days after initiation of varenicline according to the manufacturer; some data suggests that an extended pretreatment regimen may result in higher abstinence rates (Hajek 2011). For patients who are sure that they are not able or willing to quit abruptly, begin treatment with varenicline 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 complete abstinence by 12 weeks. If patient successfully quits smoking at the end of the 12 weeks, may continue for another 12 weeks to help maintain success. Patients who are motivated to quit and do not succeed in stopping smoking during prior therapy, or who relapse after treatment, should be encouraged to make another attempt with varenicline once factors contributing to the failed attempt have been identified and addressed.
Refer to adult dosing.
Dosing: Renal Impairment
CrCl ≥30 mL/minute: No dosage adjustment necessary.
CrCl <30 mL/minute: Initiate: 0.5 mg once daily; maximum dose: 0.5 mg twice daily
End-stage renal disease (ESRD) (receiving hemodialysis): Maximum dose: 0.5 mg once daily
Dosing: Hepatic Impairment
No dosage adjustment necessary.
Dosing: Adjustment for Toxicity
Patients who cannot tolerate adverse events may require temporary (or permanent) reduction in dose.
Administer after eating and with a full glass of water.
Take after eating and with a full glass of water to decrease gastric upset.
Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).
Alcohol (Ethyl): Varenicline may enhance the adverse/toxic effect of Alcohol (Ethyl). Specifically, alcohol tolerance may be decreased and the risk for neuropsychiatric adverse effects may be increased. Monitor therapy
Histamine H2 Receptor Antagonists: May increase the serum concentration of Varenicline. Management: Monitor for increased varenicline adverse effects with concomitant use of cimetidine or other H2-antagonists, particularly in patients with severe renal impairment. International product labeling recommendations vary. Consult appropriate labeling. Monitor therapy
Nicotine: Varenicline may enhance the adverse/toxic effect of Nicotine. Monitor therapy
Quinolones: May increase the serum concentration of Varenicline. Management: Monitor for increased varenicline adverse effects with concurrent use of levofloxacin or other quinolone antibiotics, particularly in patients with severe renal impairment. International product labeling recommendations vary. Consult appropriate labeling. Monitor therapy
Tafenoquine: May increase the serum concentration of OCT2 Substrates. Management: Avoid use of OCT2 substrates with tafenoquine, and if the combination cannot be avoided, monitor closely for evidence of toxicity of the OCT2 substrate and consider a reduced dose of the OCT2 substrate according to that substrate's labeling. Consider therapy modification
Trimethoprim: May increase the serum concentration of Varenicline. Management: Monitor for increased varenicline adverse effects with concomitant use of trimethoprim, particularly in patients with severe renal impairment. International product labeling recommendations vary. Consult appropriate labeling. Monitor therapy
Central nervous system: Headache (12% to 19%), insomnia (9% to 19%), abnormal dreams (8% to 13%), irritability (11%), suicidal ideation (11%), depression (4% to 11%)
Gastrointestinal: Nausea (16% to 40%), vomiting (5% to 11%)
1% to 10%:
Cardiovascular: Angina pectoris (4%), chest pain (3%), peripheral edema (2%), myocardial infarction (≤1%)
Central nervous system: Anxiety (8%), malaise (7%), agitation (5% to 7%), sleep disorder (3% to 5%), tension (4%), drowsiness (3%), hostility (2% to 3%), lethargy (1% to 2%), nightmares (1% to 2%)
Dermatologic: Skin rash (3%)
Gastrointestinal: Flatulence (6% to 9%), constipation (5% to 8%), dysgeusia (5% to 8%), abdominal pain (7%), diarrhea (6%), xerostomia (6%), dyspepsia (5%), increased appetite (3% to 4%), anorexia (≤2%), decreased appetite (≤2%), gastroesophageal reflux disease (1%)
Respiratory: Upper respiratory tract infection (5% to 7%), dyspnea (2%), rhinorrhea (≤1%)
<1%, postmarketing, and/or case reports: Abnormal hepatic function tests, abnormality in thinking, abnormal urinalysis, accidental injury, acne vulgaris, acute coronary syndrome, acute renal failure, aggressive behavior, allergic rhinitis, altered sense of smell, amnesia, anemia, angioedema, arthralgia, asthma, atrial fibrillation, back pain, behavioral changes, Bell palsy, blurred vision, bradycardia, cardiac arrhythmia, cardiac flutter, cataract (subcapsular), cerebrovascular accident, chills, conjunctivitis, cor pulmonale, coronary artery disease, deafness, decreased libido, decreased mental acuity, decreased visual acuity, delusions, diabetes mellitus, difficulty thinking, disorientation, dissociative disorder, dizziness, dysarthria, dysphagia, ECG abnormality, eczema, edema, elevation in serum levels of skeletal-muscle enzymes, emotional disturbance, emotional lability, enterocolitis, epistaxis, equilibrium disturbance, erectile dysfunction, eructation, erythema, erythema multiforme, esophagitis, euphoria, eye irritation, eye pain, fever, flu-like symptoms, flushing, gallbladder disease, gastric ulcer, gastritis, gastrointestinal hemorrhage, hallucination, homicidal ideation, hyperglycemia, hyperhidrosis, hyperlipidemia, hypersensitivity reaction, hypoglycemia, hypokalemia, intestinal obstruction, lack of concentration, leukocytosis, loss of consciousness, lymphadenopathy, mania, Meniere disease, menstrual disease, migraine, multiple sclerosis, muscle cramps, musculoskeletal pain, myalgia, myositis, nephrolithiasis, nocturia, nocturnal amblyopia, nystagmus, ophthalmic vascular disease, oral mucosa ulcer, osteoporosis, palpitations, pancreatitis, panic, paranoia, photophobia, pleurisy, pollakiuria, polyuria, psoriasis, psychomotor agitation, psychomotor retardation, psychosis, pulmonary embolism, respiratory tract disease, restless leg syndrome, seizure, sensory disturbance, sexual difficulty, skin photosensitivity, somnambulism, splenomegaly, Stevens-Johnson syndrome, syncope, tachycardia, thrombocytopenia, thrombosis, thyroid disease, tinnitus, toothache, transient blindness, transient ischemic attacks, tremor, upper respiratory tract inflammation, urethral disease, urinary retention, urine abnormality, urticaria, ventricular premature contractions, vertigo, visual field defect, vitreous opacity, weight gain, xeroderma, xerophthalmia
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving). There have been postmarketing reports of traffic accidents, near-miss incidents in traffic, or other accidental injuries in patients taking varenicline.
• Hypersensitivity reactions: Postmarketing reports of hypersensitivity reactions (including angioedema) and rare cases of serious skin reactions (including Stevens-Johnson syndrome and erythema multiforme) have been reported. Patients should be instructed to discontinue use and contact healthcare provider if signs/symptoms occur.
• Nausea: Dose-dependent nausea may occur; both transient and persistent nausea has been reported. Dosage reduction may be considered for intolerable nausea.
• Neuropsychiatric effects: Post-marketing cases of serious neuropsychiatric events (including depression, suicidal thoughts, and suicide) have been reported in patients with or without preexisting psychiatric disease; some cases may have been complicated by symptoms of nicotine withdrawal following smoking cessation. Subsequent controlled trials in patients with or without psychiatric disorders; however, have not identified significant differences in neuropsychiatric effects for patients taking varenicline, bupropion, nicotine patches, or placebo (Anthenelli 2013; Anthenelli 2016; Gibbons 2013; Thomas 2015). Monitor all patients for behavioral changes and psychiatric symptoms (eg, agitation, depression, suicidal behavior, suicidal ideation); inform patients to discontinue treatment and contact their health care provider immediately if they experience any behavioral and/or mood changes. Of post-marketing cases, many resolved following therapy discontinuation.
• Somnambulism: Cases of somnambulism, involving harmful behavior to self, others or property, have been reported. Discontinue treatment if somnambulism occurs.
• Cardiovascular events: Treatment may increase risk of cardiovascular events. A meta-analysis of 15 clinical trials, including a placebo-controlled trial in patients with stable cardiovascular disease, showed an increased incidence of major cardiovascular events (combined outcome of cardiovascular-related death, nonfatal MI, nonfatal stroke) in patients using varenicline compared with placebo. Cardiovascular events were uncommon in both the varenicline and placebo groups. These findings did not reach statistical significance, although data was consistent. Events occurred primarily in patients with known cardiovascular disease. The meta-analysis also showed a lower incidence of all-cause and cardiovascular mortality in varenicline-treated patients, although this was not statistically significant either. Patients should be instructed to contact their health care provider if cardiovascular symptoms occur.
• Renal impairment: Use with caution in patients with renal impairment; dosage adjustment required with severe impairment.
• Seizures: Seizures have been reported in patients with or without a history of seizures. Seizures generally occurred within the first month of therapy. Consider the risks against the benefits before initiating in patients with a history of seizures or other factors that can lower the seizure threshold; discontinue use if seizures occur during therapy.
Concurrent drug therapy issues:
• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.
Monitor for behavioral changes and psychiatric symptoms (eg, agitation, depression, suicidal behavior, suicidal ideation).
Information related to the use of varenicline in pregnancy is limited (Harrison-Woolrych 2013; Kaplan 2014; Richardson 2017).
Nicotine exposure is associated with adverse events to both the mother and fetus. All pregnant females should be encouraged to stop smoking. However, data is insufficient to recommend varenicline for smoking cessation during pregnancy (ACOG 721 2017).
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience flatulence, insomnia, headache, nightmares, constipation, dry mouth, abdominal pain, change in taste, common cold symptoms, or loss of strength and energy. Have patient report immediately to prescriber signs of depression (suicidal ideation, anxiety, emotional instability, or confusion), hallucinations, psychosis, anxiety, agitation, mood changes, behavioral changes, signs of angioedema, signs of severe cerebrovascular disease (change in strength on one side is greater than the other, difficulty speaking or thinking, change in balance, or vision changes), signs of a heart attack (angina; pain in arms, back, neck, jaw, or abdomen; shortness of breath; cold sweats; severe dizziness; passing out; or severe nausea or vomiting), shortness of breath, severe nausea, vomiting, seizures, confusion, sleepwalking, or signs of Stevens-Johnson syndrome/toxic epidermal necrolysis (red, swollen, blistered, or peeling skin [with or without fever]; red or irritated eyes; or sores in mouth, throat, nose, or eyes) (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
More about varenicline
- Varenicline Side Effects
- During Pregnancy or Breastfeeding
- Dosage Information
- Drug Interactions
- Support Group
- En Español
- 1363 Reviews
- Drug class: smoking cessation agents
- FDA Alerts (6)
Other brands: Chantix