Smoking cessation with varenicline, a selective α4β2 nicotinic receptor partial agonist

Results from a 7-week, randomized, placebo- and bupropion-controlled trial with 1-year follow-up

Mitchell Nides, Cheryl Oncken, David Gonzales, Stephen Israel Rennard, Eric J. Watsky, Rich Anziano, Karen R. Reeves

Research output: Contribution to journalArticle

302 Citations (Scopus)

Abstract

Background: Currently available smoking cessation therapies have limited success rates. Varenicline tartrate is a novel, selective nicotinic receptor partial agonist developed specifically for smoking cessation. This study evaluated the efficacy, tolerability, and safety of 3 varenicline doses for smoking cessation. Bupropion hydrochloride was included as an active control. Methods: A phase 2, multicenter, randomized, double-blind, placebo-controlled study of healthy smokers (18-65 years old). Subjects were randomized to varenicline tartrate, 0.3 mg once daily (n=128), 1.0 mg once daily (n=128), or 1.0 mg twice daily (n=127), for 6 weeks plus placebo for 1 week; to 150-mg sustained-release bupropion hydrochloride twice daily (n=128) for 7 weeks; or to placebo (n=127) for 7 weeks. Results: During the treatment phase, the continuous quit rates for any 4 weeks were significantly higher for varenicline tartrate, 1.0 mg twice daily (48.0%; P<.001) and 1.0 mg once daily (37.3%; P<.001), than for placebo (17.1%). The bupropion rate was 33.3% (P=.002 vs placebo). The carbon monoxide-confirmed continuous quit rates from week 4 to week 52 were significantly higher in the varenicline tartrate, 1.0 mg twice daily, group compared with the placebo group (14.4% vs 4.9%; P=.002). The bupropion rate was 6.3% (P=.60 vs placebo). Discontinuation owing to treatment-emergent adverse events was 15.9% for bupropion, 11.2% to 14.3% for varenicline, and 9.8% for placebo. No dose-related increases occurred in adverse events for varenicline. Conclusions: Varenicline tartrate demonstrated both short-term (1 mg twice daily and 1 mg once daily) and long-term efficacy (1 mg twice daily) vs placebo. Varenicline was well tolerated and may provide a novel therapy to aid smoking cessation.

Original languageEnglish (US)
Pages (from-to)1561-1568
Number of pages8
JournalArchives of Internal Medicine
Volume166
Issue number15
DOIs
StatePublished - Aug 28 2006

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Bupropion
Nicotinic Receptors
Smoking Cessation
Placebos
Varenicline
Therapeutics
Carbon Monoxide
Safety

ASJC Scopus subject areas

  • Internal Medicine

Cite this

Smoking cessation with varenicline, a selective α4β2 nicotinic receptor partial agonist : Results from a 7-week, randomized, placebo- and bupropion-controlled trial with 1-year follow-up. / Nides, Mitchell; Oncken, Cheryl; Gonzales, David; Rennard, Stephen Israel; Watsky, Eric J.; Anziano, Rich; Reeves, Karen R.

In: Archives of Internal Medicine, Vol. 166, No. 15, 28.08.2006, p. 1561-1568.

Research output: Contribution to journalArticle

Nides, Mitchell ; Oncken, Cheryl ; Gonzales, David ; Rennard, Stephen Israel ; Watsky, Eric J. ; Anziano, Rich ; Reeves, Karen R. / Smoking cessation with varenicline, a selective α4β2 nicotinic receptor partial agonist : Results from a 7-week, randomized, placebo- and bupropion-controlled trial with 1-year follow-up. In: Archives of Internal Medicine. 2006 ; Vol. 166, No. 15. pp. 1561-1568.
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abstract = "Background: Currently available smoking cessation therapies have limited success rates. Varenicline tartrate is a novel, selective nicotinic receptor partial agonist developed specifically for smoking cessation. This study evaluated the efficacy, tolerability, and safety of 3 varenicline doses for smoking cessation. Bupropion hydrochloride was included as an active control. Methods: A phase 2, multicenter, randomized, double-blind, placebo-controlled study of healthy smokers (18-65 years old). Subjects were randomized to varenicline tartrate, 0.3 mg once daily (n=128), 1.0 mg once daily (n=128), or 1.0 mg twice daily (n=127), for 6 weeks plus placebo for 1 week; to 150-mg sustained-release bupropion hydrochloride twice daily (n=128) for 7 weeks; or to placebo (n=127) for 7 weeks. Results: During the treatment phase, the continuous quit rates for any 4 weeks were significantly higher for varenicline tartrate, 1.0 mg twice daily (48.0{\%}; P<.001) and 1.0 mg once daily (37.3{\%}; P<.001), than for placebo (17.1{\%}). The bupropion rate was 33.3{\%} (P=.002 vs placebo). The carbon monoxide-confirmed continuous quit rates from week 4 to week 52 were significantly higher in the varenicline tartrate, 1.0 mg twice daily, group compared with the placebo group (14.4{\%} vs 4.9{\%}; P=.002). The bupropion rate was 6.3{\%} (P=.60 vs placebo). Discontinuation owing to treatment-emergent adverse events was 15.9{\%} for bupropion, 11.2{\%} to 14.3{\%} for varenicline, and 9.8{\%} for placebo. No dose-related increases occurred in adverse events for varenicline. Conclusions: Varenicline tartrate demonstrated both short-term (1 mg twice daily and 1 mg once daily) and long-term efficacy (1 mg twice daily) vs placebo. Varenicline was well tolerated and may provide a novel therapy to aid smoking cessation.",
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AU - Oncken, Cheryl

AU - Gonzales, David

AU - Rennard, Stephen Israel

AU - Watsky, Eric J.

AU - Anziano, Rich

AU - Reeves, Karen R.

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N2 - Background: Currently available smoking cessation therapies have limited success rates. Varenicline tartrate is a novel, selective nicotinic receptor partial agonist developed specifically for smoking cessation. This study evaluated the efficacy, tolerability, and safety of 3 varenicline doses for smoking cessation. Bupropion hydrochloride was included as an active control. Methods: A phase 2, multicenter, randomized, double-blind, placebo-controlled study of healthy smokers (18-65 years old). Subjects were randomized to varenicline tartrate, 0.3 mg once daily (n=128), 1.0 mg once daily (n=128), or 1.0 mg twice daily (n=127), for 6 weeks plus placebo for 1 week; to 150-mg sustained-release bupropion hydrochloride twice daily (n=128) for 7 weeks; or to placebo (n=127) for 7 weeks. Results: During the treatment phase, the continuous quit rates for any 4 weeks were significantly higher for varenicline tartrate, 1.0 mg twice daily (48.0%; P<.001) and 1.0 mg once daily (37.3%; P<.001), than for placebo (17.1%). The bupropion rate was 33.3% (P=.002 vs placebo). The carbon monoxide-confirmed continuous quit rates from week 4 to week 52 were significantly higher in the varenicline tartrate, 1.0 mg twice daily, group compared with the placebo group (14.4% vs 4.9%; P=.002). The bupropion rate was 6.3% (P=.60 vs placebo). Discontinuation owing to treatment-emergent adverse events was 15.9% for bupropion, 11.2% to 14.3% for varenicline, and 9.8% for placebo. No dose-related increases occurred in adverse events for varenicline. Conclusions: Varenicline tartrate demonstrated both short-term (1 mg twice daily and 1 mg once daily) and long-term efficacy (1 mg twice daily) vs placebo. Varenicline was well tolerated and may provide a novel therapy to aid smoking cessation.

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