Vareniclina

Andrea Isabel Arteaga

Action at 42 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

Mecanismo de acción

Efectos adversos

Nausea Sleep

Disturbance Constipation

Gas Vomiting changes in behavior

Evidencia

Varenicline phase 2 trial

CO-confirmed 4-week continuous quit rates,

at week 12

45.1

50.6

12.4

0

10

20

30

40

50

60

0.5 mg 2/day

1.0 mg 2/day

Placebo

p<0.0001

Varenicline clinical trial

CO-confirmed 4-week continuous quit rates,

at week 7

25.4

40.8

28.6

13.8

31

0

5

10

15

20

25

30

35

40

45

0.3 mg 1/day

1.0 mg 1/day

1.0 mg 2/day

Zyban 150*2

Placebo

p<0.05

Varenicline 12 semaines + si succès encore

12 semaines varenicline ou placebo

50

71

0

10

20

30

40

50

60

70

80

12 sem +

placebo

12+12 sem

Communiqué de presse du 15 nov

2005, Pfizer

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.