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Expert Opinion on Investigational Drugs Volume 17, 2008 - Issue 10
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Review

Nicotinic receptor partial agonists as novel compounds for the treatment of smoking cessation

Piotr Tutka Medical University of Lublin, Department of Experimental and Clinical Pharmacology, Lublin, Poland +48 81 7187351; +48 81 7408744; [email protected]
, MD PhD
Pages 1473-1485 | Published online: 22 Sep 2008

Bibliography

  • Peto R, Lopez AD, Boreham J, Thun M. Mortality from smoking in developed countries 1950 – 2000. Available from: http://www.ctsu.ox.ac.uk/∼tobacco [Last accessed 22 July 2008]
  • WHO Report on the Global Tobacco Epidemic, 2008. Available from: http://www.who.int/tobacco/mpower/mpower_report_full_2008.pdf [Last accessed 22 July 2008]
  • Benowitz NL. Nicotine addiction. Prim Care 1999;26:611-31
  • Tutka P, Mosiewicz J, Wielosz M. Pharmacokinetics and metabolism of nicotine. Pharmacol Rep 2005;57:143-53
  • Hughes JR, Higgins ST, Bickel WK. Nicotine withdrawal versus other drug withdrawal syndromes: similarities and dissimilarities. Addiction 1994;89:1461-70
  • Benowitz NL. Clinical pharmacology of nicotine: implications for understanding, preventing, and treating tobacco addiction. Clin Pharmacol Ther 2008;83:531-41
  • Anthonisen NR, Skeans MA, Wise RA, et al. The effects of smoking cessation intervention on 14.5-year mortality: a randomized clinical trial. Arch Intern Med 2005;142:233-9
  • West R, McNeill A, Raw M. Smoking cessation guidelines for health professionals: an update. Health Education Authority. Thorax 2000;55:987-99
  • Nides M. Update on pharmacologic options for smoking cessation treatment. Am J Med 2008;121:S20-31
  • Treating Tobacco Use and Dependence: 2008 Update. A US Public Health Service-sponsored Clinical Practice Guideline. The Tobacco Use and Dependence Guideline Panel, Consortium Representatives, and Staff. Available from: http://www.surgeongeneral.gov/tobacco/treating_tobacco_use08.pdf [Last accessed 22 July 2008]
  • Fagerström K, Balfour DJ. Neuropharmacology and potential efficacy of new treatments for tobacco dependence. Expert Opin Investig Drugs 2006;15:107-16
  • Hurt RD, Sachs DPL, Glover ED, et al. A comparison of sustained-release bupropion and placebo for smoking cessation. N Engl J Med 1997;337:1195-202
  • Jorenby DE, Leischow SJ, Nides MA, et al. A controlled trial of sustained-release bupropion, a nicotine patch, or both for smoking cessation. N Engl J Med 1999;340:685-91
  • Silagy C, Lancaster T, Stead L, et al. Nicotine replacement therapy for smoking cessation. Cochrane Database Syst Rev 2004;(4):CD000146
  • Hughes J, Stead L, Lancaster T. Antidepressants for smoking cessation. Cochrane Database Syst Rev 2007;(1):CD000031
  • Etter JF, Stapleton JA. Nicotine replacement therapy for long-term smoking cessation: a meta-analysis. Tob Control 2006;15:280-5
  • Britton J, Jarvis MJ. Bupropion: a new treatment for smokers. BMJ 2000;321:65-6
  • Le Foll B, George TP. Treatment of tobacco dependence: integrating recent progress into practice. CMAJ 2007;177:1373-80
  • Breining SR, Mazurov AA, Miller SH. Neuronal nicotinic acetylcholine receptor modulators: recent advances and therapeutic potential. Ann Rep Med Chem 2005;40:3-16
  • Picciotto MR, Zoli M, Rimondini R, et al. Acetylcholine receptors containing the beta2 subunit are involved in the reinforcing properties of nicotine. Nature 1998;391:173-7
  • Cohen C, Bergis OE, Galli F, et al. SSR591813, a novel selective and partial alpha4beta2 nicotinic receptor agonist with potential as an aid to smoking cessation. J Pharmacol Exp Ther 2003;306:407-20
  • Coe JW, Brooks PR, Vetelino MG, et al. Varenicline: an α4β2 nicotinic receptor partial agonist for smoking cessation. J Med Chem 2005;48:3474-7
  • Rollema H, Coe JW, Chambers LK, et al. Rationale, pharmacology and clinical efficacy of partial agonists of α4β2 nACh receptors for smoking cessation. TiPS 2007;28:316-25
  • Rollema H, Chambers LK, Coe JW, et al. Pharmacological profile of the a4b2 nicotinic acetylcholine receptor partial agonist varenicline, an effective smoking cessation aid. Neuropharmacology 2007;52:985-94
  • Champtiaux N, Gotti C, Codero Erausquin M, et al. Subunit composition of functional nicotinic receptors in dopaminergic neurons investigated with knock-out mice. J Neurosci 2003;21:7820-9
  • Laviolette SR, Van der Kooy D. The neurobiology of nicotine addiction: bridging the gap from molecules to behavior. Nat Rev Neurosci 2004;5:55-65
  • Hildebrand BE, Nomikos GG, Hertel B, et al. Reduced dopamine output in the nucleus accumbens but not in the medial prefrontal cortex in rats displaying a mecamylamine-precipitated nicotine withdrawal syndrome. Brain Res 1998;779:214-25
  • Epping Jordan MP, Watkins SS, Koob GF, Markou A. Dramatic decreases in brain reward function during nicotine withdrawal. Nature 1998;393:76-9
  • Malin DH, Lake JR, Newlin Maultsby P, et al. Rodent model of nicotine abstinence syndrome. Pharmacol Biochem Behav 1992;43:779-84
  • Izaddoost M, Harris BG, Gracy RW. Structure and toxicity of alkaloids and amino acids of Sophora secundiflora seeds. J Pharm Sci 1976;65:352-4
  • Adovasio JM, Fry GF. Prehistoric psychotropic drug use in Northern Mexico and Trans-Pecos Texas. Econ Bot 1976;30:94-6
  • Tutka P, Zatonski W. Cytisine for the treatment of nicotine addiction: from a molecule to therapeutic efficacy. Pharmacol Rep 2006;58:777-98
  • Tutka P, Mroz K, Zatonski W. Cytisine – renaissance of well known alkaloid. Pharmacological aspects of efficacy in the treatment of tobacco dependence [in Polish]. Farmakoterapia Psych Neurol 2006;22:33-9
  • Tabex®. Product monograph. Sopharma; 2006
  • Etter JF. Cytisine for smoking cessation, a literature review and a meta-analysis. Arch Intern Med 2006;166:1553-9
  • Tutka P. Pharmacological properties of cytisine. Conference: cytisine – a natural plant extract for tobacco dependence treatment [in Polish], Cracow; 2004
  • Zatonski W, Cedzynska M, Tutka P, West R. An uncontrolled trial of cytisine (Tabex) for smoking cessation. Tob Control 2006;15:481-4
  • Lukas RJ. Pharmacological effects of nicotine and nicotinic receptor subtype pharmacological profiles. In: George TP, editor. Medication treatments for nicotine dependence. CRC Press, Boca Raton; 2006. p. 3-23
  • Smith JW, Mogg A, Tafi E, et al. Ligands selective for α4β2 but not α3β4 or α7 nicotinic receptors generalise to the nicotine discriminative stimulus in the rat. Psychopharmacology 2007;190:157-70
  • Imming P, Klaperski P, Stubbs MT, et al. Syntheses and evaluation of halogenated cytisine derivatives and of bioisosteric thiocytisine as potent and selective nAChR ligands. Eur J Med Chem 2001;36:375-88
  • Boido CC, Tasso B, Boido V, Sparatore F. Cytisine derivatives as ligands for neuronal nicotine receptors and with various pharmacological activities. Farmaco 2003;58:265-77
  • Grady SR, Murphy KL, Cao J, et al. Characterization of nicotinic agonist-induced [3H]dopamine release from synaptosomes prepared from four mouse brain regions. J Pharmacol Exp Ther 2002;301:651-60
  • Abin Carriquiry JA, Voutilainen MH, Barik J, et al. C3-halogenation of cytisine generates potent and efficacious nicotinic receptor agonists. Eur J Pharmacol 2006;536:1-11
  • Reavill C, Walther B, Stolerman IP, Testa B. Behavioural and pharmacokinetic studies on nicotine, cytisine and lobeline. Neuropharmacology 1990;29:619-24
  • Chandler CJ, Stolerman IP. Discriminative stimulus properties of the nicotinic agonist cytisine. Psychopharmacology (Berl) 1997;129:257-64
  • Rasmussen T, Swedberg MD. Reinforcing effects of nicotinic compounds: intravenous self-administration in drug-naive mice. Pharmacol Biochem Behav 1998;60:567-73
  • Benndorf S, Kempe G, Scharfenberg G, et al. Results of pharmacological smoking cessation using cytisine (Tabex®)[in German]. Dtsch Gesundheitsw 1968;23:2092-6
  • Paun D, Franze J. Breaking the smoking habit using cytisin containing “Tabex” tablets [in German]. Dtsch Gesundheitsw 1968;23:2088-91
  • Scharfenberg G, Benndorf S, Kempe G. Cytisine (Tabex) as a pharmaceutical aid in stopping smoking [in German]. Dtsch Gesundheitsw 1971;26:463-5
  • Schmidt F. Medical support of nicotine withdrawal. Report on a double blind trial in over 5000 smokers [in German]. Munch Med Wochenschr 1974;116:557-64
  • Ostrovskaia TP. Results of clinical investigations of anti-nicotine drug patches [in Russian]. Med Tekh 1994;3:42-3
  • Ostrovskaia TP. Clinical trial of antinicotine drug-containing films. Biomed Eng 1994;28:168-71
  • Cahill K, Stead LF, Lancaster T. Nicotine receptor partial agonists for smoking cessation. Cochrane Database Syst Rev 2007;24:CD006103
  • West R, Hajek P, Stead L, Stapleton J. Outcome criteria in smoking cessation trials: proposal for a common standard. Addiction 2005;100:299-303
  • Monova D, Nikolov R. Safety and tolerability of cytisine as a treatment to assist smoking cessation. 8th European Conference of the Society for Research on Nicotine and Tobacco; 2006; Kusadasi, Turkey
  • Vinnikov D, Brimkulov N, Burjubaeva A. A double-blind, randomised, placebo-controlled trial of cytisine for smoking cessation in medium-dependent workers. J Smoking Cessation 2008;3:57-62
  • Gonzales D, Rennard SI, Nides M, et al. Varenicline, an α4β2 nicotinic acetylocholine receptor partial agonist, vs sustained-release bupropion and placebo for smoking cessation. A randomized controlled trial. JAMA 2006;296:47-55
  • Paun D, Franze J. Tabex, registering and treatment of smokers with chronic bronchitis in the consultation against tobacco smoking. Med Biol Inform 1970;3:14-9
  • Maliszewski L, Straczynski A. On the use of Tabex [in Polish]. Wiad Lek 1972;25:2207-10
  • Stoyanov S, Yanachkova M. Tabex – therapeutic efficacy and tolerance [in Bulgarian]. Savr Med 1972;23:30-3
  • Hughes JR, Shiffman S, Callas P, Zhang J. A meta-analysis of the efficacy of over-the-counter nicotine replacement. Tob Control 2003;12:21-7
  • Chaloupka FJ, Tauras JA. The impact of nicotine replacement therapies on cigarette demand. J Econ Finance 2004;28:395-403
  • Naboko D, Dimitrova Z. Accessibility of nicotine dependence therapy. J Public Health 2007;15:433-50
  • Bulgarian Drug Agency, BDA. Available from: http://www.bda.bg [Last accessed 22 July 2008]
  • Drugs Index MP OnLine [in Polish]. Available from: http://www.mp.pl/leki [Last accessed 22 July 2008]
  • Wiggers LC, Smets EM, Oort FJ, et al. Adherence to nicotine replacement patch therapy in cardiovascular patients. Int J Behav Med 2006;13:79-88
  • Etter JF, Lukas RJ, Benowitz NL, et al. Cytisine for smoking cessation: a research agenda. Drug Alcohol Depend 2008;92:3-8
  • Rose JE, Corrigall WA. Nicotine self-administration in animals and humans: similarities and differences. Psychopharmacology 1997;130:28-40
  • Zatonski W, West R, Cedzynska M, et al. The Tabex Smoking Cessation Trial (TASC); 2006
  • European Public Assessment Report for Champix. European Medicines Agency, EMEA. Available from: http://www.emea.europa.eu/humandocs/Humans/EPAR/champix/champix.htm [Last accessed 22 July 2008]
  • Burstein AH, Clark DJ, O'Gorman M, et al. Lack of pharmacokinetic and pharmacodynamic interactions between a smoking cessation therapy, varenicline, and warfarin: an in vivo and in vitro study. J Clin Pharmacol 2007;47:1421-9
  • Pfizer Press Releases (22 April 2008). Available from: http://www.pfizer.com/news/press_releases/pfizer_press_releases.jsp [Last accessed 22 July 2008]
  • Faessel HM, Gibbs MA, Clark DJ, et al. Multiple-dose pharmacokinetics of the selective nicotinic receptor partial agonist, varenicline, in healthy smokers. J Clin Pharmacol 2006;46:1439-48
  • Potts LA, Garwood CL. Varenicline: the newest agent for smoking cessation. Am J Health Syst Pharm 2007;64:1381-4
  • Mihalak KB, Carroll FI, Luetje CW. Varenicline is a partial agonist at α4β2 and a full agonist at α7 neuronal nicotinic receptors. Mol Pharmacol 2006;70:801-5
  • Burstein AH, Fullerton T, Clark DJ, Faessel HM. Pharmacokinetics, safety and tolerability following single and multiple oral doses of varenicline in elderly smokers. J Clin Pharmacol 2006;46:1234-40
  • Faessel HM, Smith BJ, Gibbs MA, et al. Single-dose pharmacokinetics of varenicline, a selective nicotinic receptor partial agonist, in healthy smokers and nonsmokers. J Clin Pharmacol 2006;46:991-8
  • Chantix™: full prescribing information. Pfizer Labs. Available from: http://www.pfizer.com/files/products/uspi_chantix.pdf [Last accessed 22 July 2008]
  • Tonstad S, Tonnesen P, Hajek P, et al. Effect of maintenance therapy with varenicline on smoking cessation: a randomized controlled trial. JAMA 2006;296:64-71
  • Jorenby DE, Hays JT, Rigotti NA, et al. Efficacy of varenicline, an α4β2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation. JAMA 2006;296:56-63
  • Nides M, Oncken C, Gonzalez D, et al. Smoking cessation with varenicline, a selective α4β2 nicotinic receptor partial agonist. Arch Intern Med 2006;166:1561-8
  • Oncken C, Gonzalez D, Nides M, et al. Efficacy and safety of the novel selective nicotinic acetylcholine receptor partial agonist varenicline, for smoking cessation. Arch Intern Med 2006;166:1571-7
  • Williams KE, Reeves KR, Billing CB, et al. A double-blind study evaluating the long-term safety of varenicline for smoking cessation. Curr Med Res Opin 2007;23:793-801
  • Aubin HJ, Bobak A, Britton JR, et al. Varenicline versus transdermal nicotine patch for open-label trial smoking cessation: Results from a randomized open-label trial. Thorax 2008;63(8):717-24
  • McColl SL, Burstein AH, Reeves KR, et al. Human abuse liability of the smoking cessation drug varenicline in smokers and nonsmokers. Clin Pharmacol Ther 2008;83:607-14
  • Stapleton JA, Watson L, Spirling LI, et al. Varenicline in the routine treatment of tobacco dependence: a pre-post comparison with nicotine replacement therapy and an evaluation in those with mental illness. Addiction 2008;103:146-54
  • Nakamura M, Oshima A, Fujimoto Y, et al. Efficacy and safety of varenicline, an alpha-4 beta-2 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 smokers. Clin Ther 2007;29:1040-56
  • Tsai ST, Cho HJ, Cheng HS, et al. A randomized, placebo-controlled trial of varenicline, a selective alpha-4 beta-2 nicotinic acetylcholine receptor partial agonist, as a new therapy for smoking cessation in Asian smokers. Clin Ther 2007;29:1027-39
  • West R, Baker CL, Cappelleri JC, Bushmakin AG. Effect of varenicline and bupropion SR on craving, nicotine withdrawal symptoms, and rewarding effects of smoking during a quit attempt. Psychopharmacology (Berl) 2008;197:371-7
  • Early communication about an ongoing safety review: varenicline (marketed as Chantix). Food and Drug Administration, FDA/Center for Drug Evaluation and Research. Available from: http://www.fda.gov/cder/drug/early_comm/varenicline.htm [Last accessed 22 July 2008]
  • Effectiveness and safety of varenicline in smokers with cardiovascular disease who wish to quit smoking. A 12-week, double-blind, placebo-controlled, multicenter study with a 40 week follow up evaluating the safety and efficacy of varenicline tartrate 1 mg bid for smoking cessation in subjects with cardiovascular disease. Pfizer A3051049. Available from: http://www.clinicaltrials.gov/ct2/search; identifier: NCT00282984 [Last accessed 22 July 2008]
  • Smoking cessation in subjects with mild-to-moderate chronic obstructive pulmonary disease (COPD). A 12-week, randomized, double-blind, placebo-controlled, multicenter trial with 40-week follow-up evaluating the safety and efficacy of varenicline tartrate for smoking cessation in patients with mild-to-moderate chronic obstructive pulmonary disease. Pfizer A3051054. Available from: http://www.clinicaltrials.gov/ct2/search; identifier: NCT00285012 [Last accessed 22 July 2008]
  • Freedman R. Exacerbation of schizophrenia by varenicline. Am J Psychiatry 2007;164:1269
  • Kohen I, Kremen N. Varenicline-induced manic episode in a patient with bipolar disorder. Am J Psychiatry 2007;164:1269-70
  • Lexchin J, Bero LA, Djulbegovic B, Clark O. Pharmaceutical industry sponsorship and research outcome and quality: systematic review. BMJ 2003;326:1167-76
  • Cassels BK, Bermudez I, Dajas F, et al. From ligand design to therapeutic efficacy: the challenge for nicotinic receptor research. Drug Discov Today 2005;10:1657-65
  • sanofi-aventis Press Releases (17 September 2007). Available from: http://en.sanofi-aventis.com/press/ppc_18851.asp [Last accessed 22 July 2008]
  • sanofi-aventis Press Releases (12 February 2008). Available from: http://en.sanofi-aventis.com/press/ppc_20303.asp [Last accessed 22 July 2008]

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