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New Pharmacotherapies for Assisting Smokers in Their Cessation Efforts. Frank Vocci, Ph.D. Director, DPMCDA December 7, 2005. Varenicline. Partial agonist at the 4ß2 nicotine receptor Partial agonists have some effects like nicotine but can also act like antagonists - PowerPoint PPT Presentation
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New Pharmacotherapies for Assisting Smokers in Their Cessation Efforts
Frank Vocci, Ph.D.Director, DPMCDADecember 7, 2005
Varenicline• Partial agonist at the 4ß2 nicotine
receptor• Partial agonists have some effects like
nicotine but can also act like antagonists
• A dual mechanism of action is proposed:– Partial nicotine-like effects– Nicotine blockade from cigarette smoking
Varenicline
Varenicline Phase II Trials- Tonstad study
Drug 12 WeekQuit Rate %
52 WeekQuit Rate %
placebo 18 10
Bupropion 30 16
Varenicline 44 22
Rimonabant
• CB1 inverse agonist/ antagonist• Stratus-US Study ( unpublished)• Quit rates in the 20 mg group were
double that of placebo• Weight gain in the 20 mg group was 0.4
kg for 12 weeks versus 3.6 kg for placebo• The 20 mg group also had attenuated
weight gain 1.5 kg versus and additional 3.5 kg for placebo
Rimonabant
• May be sought after by smokers who want to quit but don’t want to gain weight
• Could be tested with other therapies, especially NRT for additive effects
• Has other metabolic effects which can independently reduce cardiovascular disease risk
Nicotine Vaccine
• Being produced by three companies
• Potential indications:– Aid to cessation– Prevention of relapse– And prevention of smoking
Nicotine Vaccine
Nicotine Vaccine
Nicotine Vaccine Blocks Nicotine Self-
Administration
New Therapies
• Offer new prospects for smokers looking for an assist to quit smoking
• Each may have distinct advantages• The vaccine may be useful for relapse
prevention• Other medications are also being
developed