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. Farmacocinética
Concentración Vida media 17-
máxima 4h 24h
Mucosa
Excreción renal
gástrica
Vareniclina

5. Mecanismo de acción

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

10. Evidencia

11. 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 p<0.0001
0

13. 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
p<0.05
0

15. 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

17. 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.