Varenicline is a smoking cessation drug that acts as a partial agonist/antagonist at nicotinic acetylcholine receptors in the brain. It reduces dopamine release and the rewarding effects of smoking, while also blocking nicotine from binding to receptors. This prevents the satisfaction from smoking. Common side effects include nausea, sleep disturbances, and changes in behavior. Clinical trials found varenicline increased quit rates compared to placebo at weeks 12 and 52. However, a new meta-analysis found an increased risk of serious cardiovascular adverse events with varenicline use.

1. Vareniclina
Andrea Isabel Arteaga

2. Action at 42 nicotine receptor
Partial agonist/antagonist
Releases lower amounts of dopamine into
brain than smoke
• Reduces withdrawal
• Not as addictive as smoke
Blocks nicotine from binding to receptor
• Prevents reward of smoking

3. Mecanismo de acción

6. Efectos adversos
Sleep
Nausea Constipation
Disturbance
changes in
Vomiting Gas
behavior

7. Evidencia

8. Varenicline phase 2 trial
CO-confirmed 4-week continuous quit rates,
at week 12
60
50.6
50 45.1
40
0.5 mg 2/day
30 1.0 mg 2/day
Placebo
20
12.4
10
0 p<0.0001

9. Varenicline clinical trial
CO-confirmed 4-week continuous quit rates,
at week 7
45 40.8
40
35 31
30
28.6 0.3 mg 1/day
25.4
1.0 mg 1/day
25
1.0 mg 2/day
20
13.8 Zyban 150*2
15
Placebo
10
5
0 p<0.05

10. Varenicline 12 semaines + si succès encore
12 semaines varenicline ou placebo
80
71
70
60
50
50 12 sem +
placebo
40
12+12 sem
30
20
10
0
Communiqué de presse du 15 nov
2005, Pfizer

12. Increased CV risk with smoking cessation
drug varenicline: New meta-analysis
Sources
1. Singh S, Loke YK, Spangler JG, et al. Risk of serious adverse cardiovascular events associated with
varenicline: a systematic review and meta-analysis. CMAJ 2011. Available at:http://www.cmaj.ca
2. Hays JT. Varenicline for smoking cessation: Is it a heartbreaker? CMAJ 2011.