As a smoking cessation aid
Adult: 500 mcg once daily for the 1st 3 days, followed by 500 mcg bid for the next 4 days. Maintenance (wk 2-12): 1 mg bid. Initiate dose 1-2 wk prior to target quit date; may temporarily reduce dose to 500 mcg bid if adverse effects are not tolerable. Usual treatment duration: 12 wk. May continue for another 12 wk to reduce relapse in patients who have successfully quit after the initial treatment course.
Renal impairment: Haemodialysis: Max: 500 mcg once daily.
CrCl (ml/min)Dosage Recommendation
<30Max: 500 mcg bid.
Warnings / Precautions
Monitor for signs of suicidal ideation or behaviour, or changes in behaviour. May affect performance of skilled tasks. Not recommended for use in children <18 yr. Pregnancy, lactation.
Adverse Reactions
Nausea, headache, dizziness, somnolence, fatigue, sleep disturbances, increased appetite and GI disturbances including vomiting, constipation and flatulence.
Overdose Reactions
General supportive measures should be instituted.
Drug Interactions
Cimetidine may increase the plasma levels of varenicline.
See Below for More varenicline Drug Interactions
Mechanism of Actions
Varenicline is a partial neuronal α4 β2 nicotinic receptor agonist. It works as a smoking cessation aid by preventing nicotine stimulation of mesolimbic dopamine system. It also stimulates dopamine activity but to a much lesser extent than nicotine does, resulting in reduced craving and withdrawal symptoms.
Absorption: Well absorbed from the GI tract; plasma concentrations peak 3-4 hr after admin.
Metabolism: Minimal metabolism.
Excretion: About 92% of a dose is excreted unchanged in the urine. Elimination half-life: About 24 hr.
Storage Conditions
Oral: Store between 15-30°C.
ATC Classification
N07BA03 - varenicline ; Belongs to the class of drugs used in the management of nicotine dependence.
Oral: Store between 15-30°C.
Available As
  • Varenicline 0.5 mg
  • Varenicline 1 mg
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