No Ifs, Ands or Butts - Continuing Medical Education

VareniclineVarenicline: A Highly Selective α4β2 ReceptorPartial Agonist• Approved by FDA in May, 2006• Marketed as Chantix• A non-nicotine medication• A selective α4β2 NicotinicAcetylcholine Receptor Partial Agonist• “Like methadone for smokers”• Black Box for Depression and SuicideRisk49NicotineBinding of nicotine at the α4β2 nicotinic receptor inthe Ventral Tegmental Area (VTA) is believed tocause release of dopamine at the Nucleus Accumbens(nAcc)ChantixChantix is an α4β2 nicotinic receptor partial agonist, acompound with dual agonist and antagonistactivities. This is believed to result in both a lesseramount of dopamine release from the VTA at thenAcc as well as the prevention of nicotine binding atthe α4β2 receptors50Varenicline Phase 3 Studies: EfficacyMeasurements: CO-Confirmed ContinuousAbstinence Rates Wks 9-52Varenicline: MostCommon Adverse EventsFrom 12-Week Fixed-Dose, Placebo-Controlled Studies5152Rates of DiscontinuationVarenicline – Prescribing Information400350300250200150100500Varenicline Bupropion SR PlaceboRandomizedDiscontinuedAE• Start varenicline one week before the quit date formaximum effectiveness• Recommended treatment is 12 weeks:– Days 1-3………..1 pill (0.5 mg) per day– Days 4-7………..1 pill (0.5 mg) twice a day (am & pm)– Day 8-end………1 pill (1 mg) twice a day (am & pm)• An additional course of 12 weeks for maintenance can beconsidered• First Month – starter month pak• Subsequent Months – continuing month pak53549