Varenicline

Indications
 Oral
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.
Storage
 Oral: Store between 15-30°C.
Available As
  • Varenicline 0.5 mg
  • Varenicline 1 mg

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