Varenicline in smoking cessation

Expert Review of Respiratory Medicine

Volumn 4, Issue 3, 2010, Pages 291-299

  Tonstad, Serena ^a   Rollema, Hans ^b  

^a LOMA LINDA UNIVERSITY   (United States)

^b PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Pharmacology; Safety; Smoking cessation; Tobacco addiction; Varenicline

Indexed keywords

AMFEBUTAMONE; NICOTINE; NICOTINE GUM; NICOTINE PATCH; PLACEBO; VARENICLINE;

ABNORMAL DREAMING; ANXIETY; BEHAVIOR THERAPY; CARDIOVASCULAR DISEASE; CIGARETTE SMOKING; DEPRESSION; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BRAIN LEVEL; DRUG DISPOSITION; DRUG DISTRIBUTION; DRUG DOSE TITRATION; DRUG EFFICACY; DRUG EXCRETION; DRUG FATALITY; DRUG HALF LIFE; DRUG INDUCED HEADACHE; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG SELECTIVITY; DRUG TARGETING; DRUG TOLERABILITY; DRUG WITHDRAWAL; EYE DISEASE; GASTROINTESTINAL DISEASE; HUMAN; IC 50; INSOMNIA; MAXIMUM PLASMA CONCENTRATION; MENTAL DISEASE; MOTIVATION; NAUSEA; NICOTINE REPLACEMENT THERAPY; NONHUMAN; PHARMACODYNAMICS; POSTMARKETING SURVEILLANCE; RECOMMENDED DRUG DOSE; REVIEW; SIDE EFFECT; SLEEP DISORDER; SMOKELESS TOBACCO; SMOKING CESSATION; SUICIDAL IDEATION; SUICIDE ATTEMPT; TOBACCO DEPENDENCE; UNSPECIFIED SIDE EFFECT;

EID: 77953255862     PISSN: 17476348     EISSN: 17476356     Source Type: Journal    
DOI: 10.1586/ers.10.27     Document Type: Review

References (69)

1. Fiore MC, Jaén CR, Baker TB et al. Treating Tobacco Use and Dependence: 2008 Update. Clinical Practice Guideline. Executive Summary. Department of Health and Human Services. Public Health Service, MD, USA (2008).
2. Picciotto MR, Zoli M, Rimondini R et al. Acetylcholine receptors containing the beta2 subunit are involved in the reinforcing properties of nicotine. Nature 391, 173-177 (1998).
3. Pontieri FE, Tanda G, Orzi F, Di Chiara G. Effects of nicotine on the nucleus accumbens and similarity to those of addictive drugs. Nature 382, 255-257 (1996).
4. Murray RP, Bailey WC, Daniels K et al.; the Lung Health Study Research Group. Safety of nicotine polacrilex gum used by 3,094 participants in the Lung Health Study. Lung Health Study Research Group. Chest 109, 438-445 (1996).
5. West R, Hajek P, Foulds J, Nilsson F, May S, Meadows A. A comparison of the abuse liability and dependence potential of nicotine patch, gum, spray and inhaler. Psychopharmacology 149, 198-202 (2000).
6. Paterson NE, Balfour DJ, Markou A. Chronic bupropion attenuated the anhedonic component of nicotine withdrawal in rats via inhibition of dopamine reuptake in the nucleus accumbens shell. Eur. J. Neurosci. 25, 3099?3108 (2007).
7. Hughes JR, Stead LF, Lancaster T. Antidepressants for smoking cessation. Cochrane Database Syst. Rev. 1, CD000031 (2007).
8. Stead LF, Perera R, Bullen C, Mant D, Lancaster T. Nicotine replacement therapy for smoking cessation. Cochrane Database Syst. Rev. 1, CD000146 (2008).
9. Gonzales D, Rennard SI, Nides M et al. Varenicline, an a4b2 nicotinic acetylcholine receptor partial agonist, vs sustained-release bupropion and placebo for smoking cessation: a randomized controlled trial. JAMA 296, 47-55 (2006).
10. Nakamura M, Oshima A, Fujimoto Y et al. Efficacy and tolerability of varenicline, an a4b2 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. 29, 1040-1056 (2007).
11. Benowitz NL. Nicotine absorption and cardiovascular effects with smokeless tobacco use: comparison with cigarettes and nicotine gum. Clin. Pharmacol. Ther. 44, 23-28 (1988).
12. Rose JE, Behm FM, Westman EC, Coleman RE. Arterial nicotine kinetics during cigarette smoking and intravenous nicotine administration: implications for addiction. Drug Alcohol Depend. 56, 99-107 (1999).
13. Di Chiara G. Role of dopamine in the behavioural actions of nicotine related to addiction. Eur. J. Pharmacol. 393, 295-314 (2000).
14. Nestler EJ. Is there a common molecular pathway for addiction? Nat. Neurosci. 8, 1445-1449 (2005).
15. Benowitz NL. Pharmacology of nicotine: addiction, smoking-induced disease, and therapeutics. Annu. Rev. Pharmacol. Toxicol. 49, 57-71 (2009).
16. Laviolette SR, Van der Kooy KD. The neurobiology of nicotine addiction: bridging the gap from molecules to behaviour. Nat. Rev. Neurosci. 5, 55-65 (2004).
17. Taly A, Corringer PJ, Guedin D, Lestage P, Changeux JP. Nicotinic receptors: allosteric transitions and therapeutic targets in the nervous system. Nat. Rev. Drug Discov. 8, 733-750 (2009).
18. Maskos U, Molles BE, Pons S et al. Nicotine reinforcement and cognition restored by targeted expression of nicotinic receptors. Nature 436, 103-107 (2005).
19. Marubio LM, Gardier AM, Durier S et al. Effects of nicotine in the dopaminergic system of mice lacking the a4 subunit of neuronal nicotinic acetylcholine receptors. Eur. J. Neurosci. 17, 1329-1337 (2003).
20. Tapper AR, McKinney SL, Nashmi R et al. Nicotine activation of a4* receptors: sufficient for reward, tolerance and sensitization. Science 306, 1029-1032 (2004).
21. Exley R, Clements MA, Hartung H, McIntosh JM, Cragg SJ. a6-containing nicotinic acetylcholine receptors dominate the nicotine control of dopamine neurotransmission in nucleus accumbens. Neuropsychopharmacology 33, 2158-2166 (2008).
22. Gotti C, Clementi F, Fornari A et al. Structural and functional diversity of native brain neuronal nicotinic receptors. Biochem. Pharmacol. 78, 703-711 (2009).
23. Coe JW, Brooks PR, Vetelino MG et al. Varenicline: an a4b2 nicotinic receptor partial agonist for smoking cessation. J. Med. Chem. 48, 3474-3477 (2005).
24. 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. 306, 407-420 (2003).
25. Rollema H, Coe JW, Chambers LK, Hurst RS, Stahl SM, Williams KE. Rationale, pharmacology and clinical efficacy of partial agonists of a4b2 nACh receptors for smoking cessation. Trends Pharmacol. Sci. 28, 316-325 (2007).
26. Coe JW, Rollema H, O'Neill BT. Case history: Chantix™/ Champix™ (varenicline tartrate), a nicotinic acetylcholine receptor partial agonist as a smoking cessation aid. Ann. Rep. Med. Chem. 44, 71-101 (2009).
27. 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 52, 985-994 (2007).
28. Rollema H, Shrikhande A, Ward KM et al. Preclinical properties of the a4b2 nAChR partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependence. Br. J. Pharmacol. 160, 334-345 (2010).
29. Smith JW, Mogg A, Tafi E et al. Ligands selective for alpha4beta2 but not a3b4 or a7 nicotinic receptors generalise to the nicotine discriminative stimulus in the rat. Psychopharmacology 190, 157-170 (2007).
30. O'Connor EC, Parker D, Rollema H, Mead AN. The a4b2 nicotinic acetylcholine-receptor partial agonist varenicline inhibits both nicotine self-administration following repeated dosing and reinstatement of nicotine seeking in rats. Psychopharmacology 208, 365-376 (2010).
31. Obach RS, Reed-Hagen AE, Krueger SS et al. Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab. Dispos. 34, 121-130 (2006).
32. Faessel HM, Gibbs MA, Clark DJ, Rohrbacher K, Stolar M, Burstein AH. Multiple-dose pharmacokinetics of the selective nicotinic receptor partial agonist, varenicline, in healthy smokers. J. Clin. Pharmacol. 46, 1439-1448 (2006).
33. Mihalak KB, Carroll FI, Luetje CW. Varenicline is a partial agonist at a4b2 and a full agonist at a7 neuronal nicotinic receptors. Mol. Pharmacol. 70, 801-805 (2006).
34. Rollema H, Hajós M, Seymour PA et al. Preclinical pharmacology of the a4b2 nAChR partial agonist varenicline related to effects on reward, mood and cognition. Biochem. Pharmacol. 78, 813-824 (2009).
35. Nides M, Oncken C, Gonzales D et al. Smoking cessation with varenicline, a selective alpha4beta2 nicotinic receptor partial agonist: results from a 7-week, randomized, placebo- and bupropion-controlled trial with 1-year follow-up. Arch. Intern. Med. 166, 1561-1568 (2006).
36. Oncken C, Gonzales D, Nides M et al. Efficacy and safety of the novel selective nicotinic acetylcholine receptor partial agonist, varenicline, for smoking cessation. Arch. Intern. Med. 166, 1571-1577 (2006).
37. Jorenby DE, Hays JT, Rigotti NA et al. Efficacy of varenicline, an a4b2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA 296, 56-63 (2006).
38. Tsai ST, Cho HJ, Cheng HS et al. A randomized, placebo-controlled trial of varenicline, a selective a4b2 nicotinic acetylcholine receptor partial agonist, as a new therapy for smoking cessation in Asian smokers. Clin. Ther. 29, 1027-1039 (2007).
39. Wang C, Xiao D, Chan KP et al. Varenicline for smoking cessation: a placebo-controlled, randomized study. Respirology 14, 384-392 (2009).
40. Niaura R, Hays JT, Jorenby DE et al. The efficacy and safety of varenicline for smoking cessation using a flexible dosing strategy in adult smokers: a randomized controlled trial. Curr. Med. Res. Opin. 24, 1931-1941 (2008).
41. Rigotti NA, Pipe A, Benowitz NL, Arteaga C, Garza D, Tonstad S. Efficacy and safety of varenicline for smoking cessation in patients with cardiovascular disease: a randomized trial. Circulation 121, 221-229 (2010).
42. Tonstad S, Tonnesen P, Hajek P et al. Effect of maintenance therapy with varenicline on smoking cessation: a randomized controlled trial. JAMA 296, 64-71 (2006).
43. Williams KE, Reeves KR, Billing Jr CB et al. A double-blind study evaluating the long-term safety of varenicline for smoking cessation. Curr. Med. Res. Opin. 23, 793-801 (2007).
44. Aubin HJ, Bobak A, Britton JR et al. Varenicline versus transdermal nicotine patch for smoking cessation: results from a randomised open-label trial. Thorax 63, 717-724 (2008).
45. Tashkin DP, Rennard S, Hays JT, Ma W, Lee TC. Efficacy and safety of varenicline for smoking cessation in patients with mild to moderate chronic obstructive pulmonary disease. Presented at: CHEST - American College of Chest Physicians. San Diego, CA, USA, 31 October-5 November 2009.
46. Metcalfe M, Gilljam H, Lund KE, Tonstad S, Fagerström K. A randomized, multicentre, double blind, placebo controlled study evaluating the efficacy of varenicline in cessation of oral tobacco use. Presented at: Meeting of the Society for Research on Nicotine and Tobacco. Baltimore, MD, USA, 24-28 February 2010.
47. Tsukahara H, Noda K, Saku K. A randomized controlled open comparative trial of varenicline vs nicotine patch in adults smokers. Circ. J. 74(4), 771-778 (2010).
48. Eisenberg MJ, Filion KB, Yavin D et al. Pharmacotherapies for smoking cessation: a meta-analysis of randomized controlled trials. CMAJ 179, 135-144 (2008).
49. Cahill K, Stead L, Lancaster T. A preliminary benefit-risk assessment of varenicline in smoking cessation. Drug Saf. 32, 119-135 (2009).
50. Nides M, Glover ED, Reus VI et al. Varenicline versus bupropion SR or placebo for smoking cessation: a pooled analysis. Am. J. Health Behav. 32, 664-675 (2008).
51. Fagerström K, Hughes JR. Varenicline in the treatment of tobacco dependence. Neuropsychiatr. Dis. Treat. 4, 353-363 (2008).
52. Hajek P, Tønnesen P, Arteaga C, Russ C, Tonstad S. Varenicline in prevention of relapse to smoking: effect of quit pattern on response to extended treatment. Addiction 104, 1597-1602 (2009).
53. 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 103, 146-154 (2008).
54. Yeh HC, Duncan BB, Schmidt MI, Wang NY, Brancati FL. Smoking, smoking cessation and risk for type 2 diabetes mellitus: a cohort study. Ann. Intern. Med. 152, 10-17 (2010).
55. Ferry LH. The power of the press in smokers' attempts to quit. Br. Med. J. 324, 1346-1347 (2002).
56. Gunnell D, Irvine D, Wise L, Davies C, Martin RM. Varenicline and suicidal behavior: a cohort study based on data from the General Practice Research Database. Br. Med. J. 339, b3805 (2009).
57. Kasliwal R, Wilton LV, Shakir SA. Safety and drug utilization profile of varenicline as used in general practice in England: interim results from a prescription-event monitoring study. Drug Saf. 32, 499-507 (2009).
58. Harrison-Woolrych M. Safety data from New Zealand. Br. Med. J. 340, 117-118 (2010).
59. Moore TJ, Furberg CD. Risk of psychiatric side effects with varenicline. Br. Med. J. 339, b4964 (2009).
60. Gunnell D, Irvine D, Wise L, Davies C, Martin RM. Authors' reply. Br. Med. J. 339, b4969 (2009).
61. Stapleton J. Do the 10 UK suicides among those taking the smoking cessation drug varenicline suggest a causal link? Addiction 104, 862-865 (2009).
62. Cahill K, Stead LF, Lancaster T. Nicotine receptor partial agonists for smoking cessation. Cochrane Database Syst. Rev. (3) CD006103 (2008).
63. Tonstad S, Davies S, Flammer M, Russ C, Hughes JR. Psychiatric disorders in ten placebo-controlled clinical trials of varenicline: a pooled analysis. Drug Saf. 33, 289-301 (2010).
64. Garza D, Murphy M, Tseng LJ, Riordan H, Chatterjee A. Neuropsychiatric symptoms in smokers quitting with varenicline or placebo: a double-blind, randomized, controlled pilot study. Presented at: European Congress of Psychiatry. Munich, Germany, 27 February-2 March 2010.
65. McClure JB, Swan GE, Jack L et al. Mood, side-effects and smoking outcomes among persons with and without probably lifetime depression taking varenicline. J. Gen. Intern. Med. 24, 563-569 (2009).
66. Rollema H, Guanowsky V, Mineur YS et al. Varenicline has antidepressant-like activity in the forced swim test and augments sertraline's effect. Eur. J. Pharmacol. 605, 114-116 (2009).
67. Blak BT, Wilson K, Metcalfe M, Maguire A, Hards M. Evaluation of varenicline as an aid to smoking cessation in UK general practice - a THIN database study. Curr. Med. Res. Opin. 26(4), 861-870 (2010).
68. Shah SD, Wilken LA, Winkler SR, Swu-Jane L. Systematic review and meta-analysis of combination therapy for smoking cessation. J. Am. Pharm. Assoc. 48, 659-665 (2008).
69. Ebbert JO, Croghan IT, Sood A, Schroeder DR, Hays JT, Hurt RD. Varenicline and bupropion sustained-release combination therapy for smoking cessation. Nic. Tob. Res.11, 572-576 (2009).