Pharmacokinetics of cytisine, an α4β2 nicotinic receptor partial agonist, in healthy smokers following a single dose

Drug Testing and Analysis

Volumn 7, Issue 6, 2015, Pages 475-482

  Jeong, Soo Hee ^a   Newcombe, David ^a   Sheridan, Janie ^a   Tingle, Malcolm ^a  

^a UNIVERSITY OF AUCKLAND   (New Zealand)

Author keywords

Cytisine; Human plasma; LC MS; Pharmacokinetics; 4 2 nicotinic partial agonist

Indexed keywords

HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY; METABOLITES; NICOTINE; PLASMA (HUMAN); SMOKE;

CYTISINES; HISTORY OF USE; HUMAN FOLLOWING; HUMAN PLASMAS; LIQUID CHROMATOGRAPHY - MASS SPECTROMETRIES; NICOTINIC RECEPTOR; PLANT ALKALOIDS; SINGLE-DOSE; SMOKING CESSATIONS; Α4Β2 NICOTINIC PARTIAL AGONIST;

PHARMACOKINETICS;

CYTISINE; ALKALOID; AZOCINE DERIVATIVE; NICOTINIC RECEPTOR; NICOTINIC RECEPTOR BETA2; NICOTINIC RECEPTOR BLOCKING AGENT; QUINOLIZINE DERIVATIVE;

ACCURACY; ADULT; ARTICLE; BLOOD ANALYSIS; DOSE RESPONSE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DETERMINATION; DRUG DISTRIBUTION; DRUG EFFECT; DRUG ELIMINATION; DRUG EXCRETION; DRUG HALF LIFE; DRUG URINE LEVEL; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; HUMAN EXPERIMENT; MALE; MASS SPECTROMETRY; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; PRIORITY JOURNAL; QUANTITATIVE ANALYSIS; SINGLE DRUG DOSE; ULTRAVIOLET SPECTROSCOPY; BLOOD; METABOLISM; PARTIAL AGONISM; URINE; VALIDATION STUDY; YOUNG ADULT;

ADULT; ALKALOIDS; AZOCINES; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DRUG PARTIAL AGONISM; HUMANS; MALE; NICOTINIC ANTAGONISTS; QUINOLIZINES; RECEPTORS, NICOTINIC; YOUNG ADULT;

EID: 84930241644     PISSN: 19427603     EISSN: 19427611     Source Type: Journal    
DOI: 10.1002/dta.1707     Document Type: Article

References (47)

1. P. Jha. Avoidable global cancer deaths and total deaths from smoking. Nat. Rev. Cancer 2009, 9, 655.
2. U.S. Department of Health and Human Services, The health consequences of smoking: a report of the Surgeon General. Atlanta: Centers for Disease Control and Prevention, National Center for Chronic Disease Prevention and Health Promotion, Office on Smoking and Health; Washington, D.C., 2004.
3. R. Peto. Smoking, smoking cessation, and lung cancer in the UK since 1950: Combination of national statistics with two case-control studies. Brit. Med. J. 2000, 321, 323.
4. J.R. Hughes, J. Keely, S. Naud. Shape of the relapse curve and long-term abstinence among untreated smokers. Addiction 2004, 99, 29.
5. S. Stoyanov. Treatment of nicotinism with the Bulgarian drug Tabex. Med. Biol. Inform. 1967, 1.
6. S. Stoyanov, M. Yanachkova. Treatment of Nicotinism with the Bulgarian Drug Tabex. Chimpharm, Sofia, 1965, pp. 2.
7. P. Tutka. Nicotinic receptor partial agonists as novel compounds for the treatment of smoking cessation. Expert Opin. Inv. Drug 2008, 17, 1473.
8. P. Hajek, H. McRobbie, K. Myers. Efficacy of cytisine in helping smokers quit: Systematic review and meta-analysis. Thorax 2013, 68, 1037.
9. P. Aveyard, R. West. Cytisine and the failure to market and regulate for human health. Thorax 2013, 68, 989.
10. J.M. Samet. Cytisine is effective for smoking cessation: Should clinicians use it? Evid. Based Med. 2014.
11. J.J. Prochaska, S. Das, N.L. Benowitz. Cytisine, the world's oldest smoking cessation aid. Brit. Med. J. 2013, 347, f5198.
12. J. Leaviss, W. Sullivan, S. Ren, E. Everson-Hock, M. Stevenson, JW. Stevens, M. Strong, A. Cantrell. What is the clinical effectiveness and cost-effectiveness of cytisine compared with varenicline for smoking cessation? A systematic review and economic evaluation. Health Technol. Assess. 2014, 18, 1.
13. H.P. Klocking, M. Richter, G. Damm. Pharmacokinetic studies with 3H-cytisine. Arch. Toxicol. Suppl. 1980, 4, 312.
14. H. Astroug. Pharmacokinetics of cytisine after single intravenous and oral administration in rabbits. Interdiscip. Toxicol. 2010, 3, 15.
15. H. Wang. Comparative analysis of quinolizidine alkaloids from different parts of Sophora alopecuroides seeds by UPLC-MS/MS. J. Pharm. Biomed. Anal. 2012, 67/68, 16.
16. P.L. Ding, Y.Q. Yu, D.F. Chen. Determination of quinolizidine alkaloids in Sophora tonkinensis by HPCE. Phytochem. Anal. 2005, 16, 257.
17. S.W. Ng. Simultaneous detection of 22 toxic plant alkaloids (aconitum alkaloids, solanaceous tropane alkaloids, sophora alkaloids, strychnos alkaloids and colchicine) in human urine and herbal samples using liquid chromatography-tandem mass spectrometry. J. Chromatogr. B 2013, 942/943, 63.
18. J. Pietsch. Simultaneous determination of thirteen plant alkaloids in a human specimen by SPE and HPLC. J. Sep. Sci. 2008, 31, 2410.
19. J. Beyer. Detection and validated quantification of toxic alkaloids in human blood plasma--comparison of LC-APCI-MS with LC-ESI-MS/MS. J. Mass Spectrom. 2007, 42, 621.
20. US Department of Health and Human Services FDA, Guidance for industry: bioanalytical method validaton. Centre for Drug Evaluation and Research, Centre for Veterinary Medicine, 2001.
21. T.F. Heatherton. The fagerstrom test for nicotine dependence: A revision of the fagerstrom tolerance questionnaire. Brit. J. Addict. 1991, 86, 1119.
22. A.H. Burstein. Pharmacokinetics, safety, and tolerability after single and multiple oral doses of varenicline in elderly smokers. J. Clin. Pharmacol. 2006, 46, 1234.
23. P. Ravva. Population pharmacokinetic analysis of varenicline in adult smokers. Brit. J. Clin. Pharmacol. 2009, 68, 669.
24. H. Rollema. Pre-clinical properties of the alpha4beta2 nicotinic acetylcholine receptor partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependence. Brit. J. Pharmacol. 2010, 160, 334.
25. C. Romano, A. Goldstein, N.P. Jewell. Characterization of the receptor mediating the nicotine discriminative stimulus. Psychopharmacology (Berl) 1981, 74, 310.
26. Y.S. Mineur. Cytisine-based nicotinic partial agonists as novel antidepressant compounds. J. Pharmacol. Exp. Ther. 2009, 329, 377.
27. C. Reavill. Behavioural and pharmacokinetic studies on nicotine, cytisine and lobeline. Neuropharmacology 1990, 29, 619.
28. D. Gonzales. Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs sustained-release bupropion and placebo for smoking cessation: A randomized controlled trial. JAMA 2006, 296, 47.
29. D.E. Jorenby. Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: A randomized controlled trial. JAMA 2006, 296, 56.
30. C.C. Boido. Cytisine derivatives as ligands for neuronal nicotine receptors and with various pharmacological activities. Farmaco 2003, 58, 265.
31. Tabex. Product monograph, Sophia, Bulgaria: Sopharma, 2006.
32. R.S. Obach. Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab. Dispos. 2006, 34, 121.
33. K. Venkatakrishnan, L.L. von Moltke, D.J. Greenblatt. Nortriptyline E-10-hydroxylation in vitro is mediated by human CYP2D6 (high affinity) and CYP3A4 (low affinity): Implications for interactions with enzyme-inducing drugs. J. Clin. Pharmacol. 1999, 39, 567.
34. L.M. Hesse. CYP2B6 mediates the in vitro hydroxylation of bupropion: Potential drug interactions with other antidepressants. Drug Metab. Dispos. 2000, 28, 1176.
35. Pfizer. Champix (varenicline tartrate)- Product Monograph. Quebec, Canada: C.P. Pharmaceuticals International C.V. Pfizer Canada Inc., 2014.
36. B. Feng. Effect of human renal cationic transporter inhibition on the pharmacokinetics of varenicline, a new therapy for smoking cessation: An in vitro-in vivo study. Clin. Pharmacol. Ther. 2008, 83, 567.
37. W. Zatonski. An uncontrolled trial of cytisine (Tabex) for smoking cessation. Tob. Control 2006, 15, 481.
38. R. West. Placebo-controlled trial of cytisine for smoking cessation. New Engl. J. Med. 2011, 365, 1193.
39. D. Vinnikov, N. Brimkulov, A. Burjubaeva. A double-blind, randomised, placebo-controlled trial of cytisine for smoking cessation in medium-dependent workers. J. Smok. Cess. 2008, 3, 57.
40. P. Tutka, W. Zatonski. Cytisine for the treatment of nicotine addiction: From a molecule to therapeutic efficacy. Pharmacol. Rep. 2006, 58, 777.
41. H. Faessel, P. Ravva, K. Williams. Pharmacokinetics, safety, and tolerability of varenicline in healthy adolescent smokers: A multicenter, randomized, double-blind, placebo-controlled, parallel-group study. Clin. Ther. 2009, 31, 177.
42. H.M. Faessel. Single-dose pharmacokinetics of varenicline, a selective nicotinic receptor partial agonist, in healthy smokers and nonsmokers. J. Clin. Pharmacol. 2006, 46, 991.
43. D. Schrenk. A distribution study of CYP1A2 phenotypes among smokers and non-smokers in a cohort of healthy Caucasian volunteers. Eur. J. Clin. Pharmacol. 1998, 53, 361.
44. W. Kalow, B.K. Tang. Caffeine as a metabolic probe: Exploration of the enzyme-inducing effect of cigarette smoking. Clin. Pharmacol. Ther. 1991, 49, 44.
45. L. Bertilsson. Clozapine disposition covaries with CYP1A2 activity determined by a caffeine test. Brit. J. Clin. Pharmacol. 1994, 38, 471.
46. K.L. Shirley. Correlation of cytochrome P450 (CYP) 1A2 activity using caffeine phenotyping and olanzapine disposition in healthy volunteers. Neuropsychopharmacology 2003, 28, 961.
47. J. de Leon, F.J. Diaz. A meta-analysis of worldwide studies demonstrates an association between schizophrenia and tobacco smoking behaviors. Schizophr. Res. 2005, 76, 135.