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Vareniclina
Andrea Isabel Arteaga
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
Mecanismo de acción
Efectos adversos

                 Sleep
  Nausea                    Constipation
              Disturbance




 changes in
               Vomiting         Gas
  behavior
Evidencia
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
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
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
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.

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Vareniclina

  • 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
  • 4.
  • 5.
  • 6. Efectos adversos Sleep Nausea Constipation Disturbance changes in Vomiting Gas behavior
  • 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
  • 11.
  • 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.