138
Views
13
CrossRef citations to date
0
Altmetric
Review

Preclinical pharmacology, efficacy, and safety of varenicline in smoking cessation and clinical utility in high risk patients

Pages 39-48 | Published online: 14 Apr 2010

References

  • Cigarette smoking among adults, United States 2006MMWR Morb Mortal Wkly Rep2007561157116117989644
  • 2008 PHS Guideline Update Panel, Liaisons, and StaffTreating tobacco use and dependence: 2008 update US Public Health Service Clinical Practice Guideline executive summaryRespir Care2008531217122218807274
  • Smoking-attributable mortality, years of potential life lost, and productivity losses, United States 2000–2004Morb Mortal Wkly Rep20085712261228
  • EtterJFCytisine for smoking cessation: a literature review and a meta-analysisArch Intern Med20061661553155916908787
  • HaysJTEbbertJOSoodAEfficacy and safety of varenicline for smoking cessationAm J Med20081214 Suppl 1S32S4218342165
  • GarrisonGDDuganSEVarenicline: a first-line treatment option for smoking cessationClin Ther20093146349119393839
  • GoldbergSRSpealmanRDGoldbergDMPersistent behavior at high rates maintained by intravenous self-administration of nicotineScience19812145735757291998
  • JonesSSudweeksSYakelJLNicotinic receptors in the brain: correlating physiology with functionTrends Neurosci19992255556110542436
  • DaniJABiasiMDCellular mechanisms of nicotine addictionPharmacol Biochem Behav20017043944611796143
  • Le NovèreNCorringerPJChangeuxJPThe diversity of subunit composition in nAChRs: evolutionary origins, physiologic, and pharmacologic consequencesJ Neurobiol20025344745612436412
  • McGeheeDSRoleLWPhysiological diversity of nicotinic acetylcholine receptors expressed by vertebrate neuronsAnnu Rev Physiol1995575215467778876
  • WonnacottSPresynaptic nicotinic ACh receptorsTrends Neurosci19972092989023878
  • ClarkePBPertAAutoradiographic evidence for nicotine receptors on nigrostriatal and mesolimbic dopaminergic neuronsBrain Res19853483553584075093
  • ZhouFMWilsonCDaniJAMuscarinic and nicotinic cholinergic mechanisms in the mesostriatal dopamine systemsNeuroscientist20039233612580337
  • WiseRADopamine, learning, and motivationNat Rev Neurosci2004548349415152198
  • WatkinsSSEpping-JordanMPKoobGFBlockade of nicotine self-administration with nicotinic antagonists in ratsPharmacol Biochem Behav19996274375110208381
  • PicciottoMRZoliMRimondiniRAcetylcholine receptors containing the beta2 subunit are involved in the reinforcing properties of nicotineNature19983911731779428762
  • MarubioLMGardierAMDurierSEffects of nicotine in the dopaminergic system of mice lacking the alpha4 subunit of neuronal nicotinic acetylcholine receptorsEur J Neurosci2003171329133712713636
  • WooltortonJRPidoplichkoVIBroideRSDifferential desensitization and distribution of nicotinic acetylcholine receptor subtypes in midbrain dopamine areasJ Neurosci2003233176318512716925
  • PicciottoMRZoliMLénaCAbnormal avoidance learning in mice lacking functional high-affinity nicotine receptor in the brainNature199537465677870173
  • XiZXSpillerKGardnerELMechanism-based medication development for the treatment of nicotine dependenceActa Pharmacol Sin20093072373919434058
  • CarrozziLPistelliFViegiGPharmacotherapy for smoking cessationTher Adv Respir Dis2008230131719124379
  • SilagyCLancasterTSteadLNicotine replacement therapy for smoking cessationCochrane Database Syst Rev20043CD00014615266423
  • LancasterTSteadLFMecamylamine (a nicotine antagonist) for smoking cessationCochrane Database Syst Rev20002CD00100910796584
  • RoseJELevinEDConcurrent agonist-antagonist administration for the analysis and treatment of drug dependencePharmacol Biochem Behav1992412192261539072
  • RoseJEBehmFMWestmanECMecamylamine combined with nicotine skin patch facilitates smoking cessation beyond nicotine patch treatment aloneClin Pharmacol Ther19945686998033499
  • ChildressARO’BrienCPDopamine receptor partial agonists could address the duality of cocaine cravingTrends Pharmacol Sci2000216910637646
  • CoeJWBrooksPRWirtzMC3, 5-Bicyclic aryl piperidines: a novel class of alpha4beta2 neuronal nicotinic receptor partial agonists for smoking cessationBioorg Med Chem Lett2005154889489716171993
  • BarlowRBMcLeodLJSome studies on cytisine and its methylated derivativesBr J Pharmacol1969351611744387392
  • BenndorfSScharfenbergGKempeGSmoking withdrawal treatment with Cytisine (Tabex). Results of a semi-annual survey of former smokers after 4 weeks of therapyDtsch Gesundheitsw1970247747765524300
  • ScharfenbergGBenndorfSKempeGCytisine (Tabex) as a pharmaceutical aid in stopping smokingDtsch Gesundheitsw1971264634654930772
  • EtterJFLukasRJBenowitzNLCytisine for smoking cessation: a research agendaDrug Alcohol Depend2008923817825502
  • PapkeRLHeinemannSFPartial agonist properties of cytisine on neuronal nicotinic receptors containing the β2 subunitMol Pharmacol1994451421498302273
  • StolermanIPGarchaHSMirzaNRDissociations between the locomotor stimulant and depressant effects of nicotinic agonists in ratsPsychopharmacology (Berl)19951174304377604144
  • ReavillCWaltherBStolermanIPBehavioral andpharmacokinetic studies on nicotine, cytisine, and lobelineNeuropharmacology1990296196242385332
  • MuseoEWiseRAPlace preference conditioning with ventral tegmental injections of cytisineLife Sci199455117911867934614
  • ChandlerCJStolermanIPDiscriminative stimulus properties of the nicotinic agonist cytisinePsychopharmacology (Berl)19971292572649084064
  • RasmussenTSwedbergMDReinforcing effects of nicotinic compounds: intravenous self-administration in drug-naive micePharmacol Biochem Behav1998605675739632242
  • RollemaHChambersLKCoeJWPharmacological profile of the alpha4beta2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aidNeuropharmacology20075298599417157884
  • RollemaHCoeJWChambersLKRationale, pharmacology, and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessationTrends Pharmacol Sci20072831632517573127
  • CarrollFIYokotaYMaWSynthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3′-(substituted phenyl) deschloroepibatidine analogsBioorg Med Chem20081674675417964169
  • SpillerKXiZXLiXVarenicline attenuates nicotine-enhanced brain-stimulation reward by activation of alpha4beta2 nicotinic receptors in ratsNeuropharmacology200957606619393252
  • O’ConnorECParkerDRollemaHThe alpha4beta2 nicotinic acetylcholine-receptor partial agonist varenicline inhibits both nicotine self-administration following repeated dosing and reinstatement of nicotine seeking in ratsPsychopharmacology2009125 [Epub ahead of print]
  • SmithJWMoggATafiELigands selective for alpha4beta2 but not alpha3beta4 or alpha7 nicotinic receptors generalize to the nicotine discriminative stimulus in the ratPsychopharmacology200719015717017115136
  • ZaniewskaMMcCrearyACStefan ′skiREffect of varenicline on the acute and repeated locomotor responses to nicotine in ratsSynapse20086293593918798299
  • MihalakKBCarrollFILuetjeCWVarenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptorsMol Pharmacol20067080180516766716
  • BrioniJDKimDJBO’NeillABNicotine cue: lack of effect of the alpha7 nicotinic receptor antagonist methyllycaconitineEur J Pharmacol1996301158773440
  • GommansJStolermanIPShoaibMAntagonism of the discriminative and aversive stimulus properties of nicotine in C57BL/6J miceNeuropharmacology2000392840284711044754
  • StolermanIPChamberlainSBizarroLThe role of nicotinic receptor alpha7 subunits in nicotine discriminationNeuropharmacology20044636337114975691
  • FaesselHMSmithBJGibbsMASingle-dose pharmacokinetics of varenicline, a selective nicotinic receptor partial agonist, in healthy smokers and nonsmokersJ Clin Pharmacol20064699199816920893
  • FaesselHMGibbsMAClarkDJMultiple-dose pharmacokinetics of the selective nicotine receptor partial agonist, varenicline, in healthy smokersJ Clin Pharmacol2006461439144817101743
  • FengBObachRSBursteinAHEffect of human renal cationic transporter inhibition on the pharmacokinetics of varenicline, a new therapy for smoking cessation: An in vitro-in vivo studyClin Pharmacol Ther20088356757617971819
  • TsaiSTChoHJChengHSA randomized, placebo-controlled trial of varenicline, a selective alpha4beta2 nicotinic acetylcholine receptor partial agonist, as a new therapy for smoking cessation in Asian smokersClin Ther2007291027103917692719
  • GarrisonGDDuganSEVarenicline: a first-line treatment option for smoking cessationClin Ther20093146349119393839
  • NidesMOnckenCGonzalesDSmoking cessation with varenicline, a selective alpha4beta2 nicotinic receptor partial agonist: results from a 7-week, randomized, placebo-, and bupropion-controlledtrialwith1-yearfollow-upArchInternMed200616615611568
  • OnckenCGonzalesDNidesMEfficacy and safety of the novel selective nicotinic acetylcholine receptor partial agonist, varenicline, for smoking cessationArch Intern Med20061661571157716908789
  • GonzalesDRennardSINidesMVarenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs sustained-release bupropion and placebo for smoking cessation: a randomized controlled trialJAMA2006296475516820546
  • JorenbyDEHaysJTRigottiNAEfficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trialJAMA2006296566316820547
  • TonstadSTønnesenPHajekPEffect of maintenance therapy with varenicline on smoking cessation: a randomized controlled trialJAMA2006296647116820548
  • NakamuraMOshimaAFujimotoYEfficacy and tolerability of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, in a 12-week, randomized, placebo-controlled, dose-response study with 40-week follow-up for smoking cessation in Japanese smokersClin Ther2007291040105617692720
  • NiauraRHaysJTJorenbyDEThe efficacy and safety of varenicline for smoking cessation using a flexible dosing strategy in adult smokers: a randomized controlled trialCurr Med Res Opin2008241931194118513462
  • AubinHJBobakABrittonJRVarenicline versus transdermal nicotine patch for smoking cessation: results from a randomized openlabel trialThorax20086371772418263663
  • NidesMGloverEDReusVIVarenicline versus bupropion SR or placebo for smoking cessation: a pooled analysisAm J Health Behav20083266467518442345
  • WestRBakerCLCappelleriJCEffect of varenicline and bupropion SR on craving, nicotine withdrawal symptoms, and rewarding effects of smoking during a quit attemptPsychopharmacology (Berl)200819737137718084743
  • CahillKSteadLFLancasterTNicotine receptor partial agonists for smoking cessationCochrane Database Syst Rev200816CD00610318646137
  • MillsEJWuPSpurdenDEfficacy of pharmacotherapies for short-term smoking abstinance: a systematic review and meta-analysisHarm Reduct J200962519761618
  • WangCXiaoDChanKPPothiratCGarzaDDaviesSVarenicline for smoking cessation: a placebo-controlled, randomized studyRespirology20091438439219192221
  • WilliamsKEReevesKRBillingCBJrA double-blind study evaluating the long-term safety of varenicline for smoking cessationCurr Med Res Opin20072379380117407636
  • MooreTJCohenMRFurbergCDInstitute for Safe Medication PracticesStrong safety signal seen for new varenicline risks2008521 Available from: http://www.ismp.org/docs/vareniclinestudy.asp. Accessed 2008 May 29.
  • Institute for Safe Medication Practices Quarter Watch (3rd Quarter 2008): Safety concerns with generics, Chantix aggressive behavior, and more. 2009 May 7. Available from: http://www.ismp.org/Newsletters/acutecare/articles/20090507.asp. Accessed 2010 March 29.
  • US Food and Drug Administration Safety alerts for human medical products: Chantix (varenicline). 2007 November 20. Available from: http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm152098.htm. Accessed 2007 November 23.
  • US Food and Drug Administration Public health advisory: important information on Chantix (varenicline). May 16, 2008. Available from: http://www.fda.gov/cder/drug/advisory/varenicline.htm. Accessed 2008 May 29.
  • LyonGJPossible varenicline-induced paranoia and irritability in a patient with major depressive disorder, borderline personality disorder, and methamphetamine abuse in remissionJ Clin Psychopharmacol20082872072119011454
  • KintzPEvansJVillainMSmoking cessation with varenicline: a suicidal fatalityJ Anal Toxicol20093311812019239738
  • KutscherECStanleyMOehlkeKChantix-induced mental status changes in a young healthy femaleS D Med20096219319519489343
  • PurvisTLMambourgSEBalvanzTMSafety and effectiveness of varenicline in a veteran population with a high prevalence of mental illnessAnn Pharmacother20094386286719383936
  • KasliwalRWiltonLVShakirSASafety and drug utilization profile of varenicline as used in general practice in England: interim results from a prescription-event monitoring studyDrug Saf20093249950719459717
  • US Dept of Transportation, Federal Motor Carrier Safety Administration Statement from administrator. 2008 May 23. Available from: http://www.fmcsa.dot.gov/statement-5-23-08.htm. Accessed 2008 May 28.
  • Federal Aviation Administration Anti-smoking medicine Chantix banned. 2008 May 23. Available from: http://www.faa.gov/news/updates/index.cfm?newsld=56363. Accessed 2008 May 28.