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Drugs reference index «Varenicline»



Pronunciation: (var-EN-I-kleen TAR-trate)Class: Smoking deterrent

Trade Names:Chantix- Tablets 0.5 mg- Tablets 1 mg

Champix (Canada)


Binds with high affinity and selectivity to neuronal nicotinic acetylcholine receptors, which produces agonist activity while preventing nicotine binding to receptors.



Absorption is virtually complete and exhibits linear pharmacokinetics. C max occurs within 3 to 4 h. Steady state is reached within 4 days.


Plasma protein binding is 20% or less.


Minimal metabolism occurs.


Elimination half-life is approximately 24 h. Excretion is 92% unchanged in the urine.

Special Populations

Renal Function ImpairmentMild Renal Function Impairment

Pharmacokinetics unchanged.

Moderate Renal Function Impairment

Drug exposure increased 1.5-fold.

Severe Renal Function Impairment

Drug exposure increased 2.1-fold.

End-Stage Renal Disease

Drug exposure increased 2.7-fold.

Hepatic Function Impairment

Pharmacokinetics should not be affected.


Pharmacokinetics in elderly patients (65 to 75 yr of age) are similar to that of younger patients.


Pharmacokinetics not affected.


Pharmacokinetics not affected.

Smoking status

Pharmacokinetics not affected.

Indications and Usage

Aid to smoking cessation.


Standard considerations.

Dosage and Administration


PO 1 mg twice daily subsequent to the following titration: days 1 to 3, 0.5 mg once daily; days 4 to 7, 0.5 mg twice daily; day 8 to end of treatment, 1 mg twice daily.

Severe Renal ImpairmentAdults

PO Start with 0.5 mg once daily, then titrate as needed to a max of 0.5 mg twice daily.

End-stage renal disease

0.5 mg once daily max.

General Advice

  • Take after eating and with a full glass of water.
  • Consider dosage reduction in patients unable to tolerate the adverse reactions.
  • Treat for 12 wk. For patients who have successfully stopped smoking after 12 wk, an additional 12-wk course may increase the likelihood of long-term abstinence.
  • Encourage patients who do not succeed in stopping smoking after 12 wk of initial therapy or who relapse to make another attempt once factors contributing to the failure have been identified and addressed.


Store at 59° to 86°F.

Drug Interactions


Coadministration increased the systemic exposure of varenicline by 29%.

Transdermal nicotine

The incidence of adverse reactions may be increased with coadministration.

Laboratory Test Interactions

None well documented.

Adverse Reactions


Hypertension (at least 1%).


Headache, insomnia (19%); abnormal dreams (13%); dysgeusia (8%); fatigue/malaise/asthenia (7%); sleep disorder (5%); increased appetite (4%); somnolence (3%); decreased appetite, lethargy, nightmare (2%); anxiety, depression, disturbances in attention, dizziness, emotional disorder, irritability, restlessness, sensory disturbance (at least 1%); agitation, depressed mood, suicidal ideation, suicide (postmarketing).


Rash (3%); pruritus (1%); hot flush, hyperhidrosis (at least 1%).


Rhinorrhea (1%).


Nausea (30%); flatulence (9%); constipation (8%); abdominal pain (7%); dry mouth (6%); dyspepsia, vomiting (5%); gastroesophageal reflux disease (1%); diarrhea, gingivitis, thirst (at least 1%).


Menstrual disorder, polyuria (at least 1%).

Lab Tests

LFT abnormalities (at least 1%).


Arthralgia, back pain, muscle cramp, musculoskeletal pain, myalgia (at least 1%).


Upper respiratory tract disorder (7%); dyspnea (2%); epistaxis (at least 1%).


Chest pain, edema, influenza-like illness (at least 1%).



Observe patients for neuropsychiatric symptoms, including agitation, changes in behavior, depressed mood, suicidal behavior, and suicidal ideation.


Category C .




Safety and efficacy not established.


Use with caution because of the greater frequency of decreased renal function.

Renal Function

Use with caution.


Serious neuropsychiatric symptoms have been reported.



None listed.

Patient Information

  • Instruct patient to set a date to quit smoking and to initiate varenicline treatment 1 wk before the date.
  • Advise patient to take the dose after eating and with a full glass of water.
  • Instruct patient on the recommended dosage regimen.
  • Inform patient that the adverse reactions from treatment are usually transient and to notify health care provider if the reactions are persistently bothersome so that dosage modification can be considered.
  • Provide patient with educational material and necessary counseling to support smoking cessation.
  • Inform patient that some medications may require dose adjustment after smoking cessation.
  • Advise women to notify health care provider if pregnant, planning to become pregnant, or breast-feeding because of the risks of smoking, and risks and benefits of smoking cessation.
  • Instruct patients and caregivers to stop the product and contact health care provider if agitation, depressed mood, or changes in behavior that are not typical for the patient are observed, or if suicidal ideation or suicidal behavior develops.

Copyright © 2009 Wolters Kluwer Health.

  • Varenicline MedFacts Consumer Leaflet (Wolters Kluwer)
  • Varenicline Detailed Consumer Information (PDR)
  • varenicline Advanced Consumer (Micromedex) - Includes Dosage Information
  • Chantix Prescribing Information (FDA)
  • Chantix Consumer Overview

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