Med. praxi. 2026;23(2):85-89 | DOI: 10.36290/med.2026.018

The role of cytisinicline in the treatment of nicotine dependence

doc. MUDr. Jiří Slíva, Ph.D., MBA
Ústav farmakologie, 3. LF UK, Praha

Cytisinicline is a plant‑derived alkaloid with a long history of pharmacological use, primarily acting through modulation of nicotinic acetylcholine receptors. Initially employed as a respiratory stimulant, it has been used since the mid‑20th century for the treatment of tobacco dependence, particularly in Central and Eastern Europe. As a partial agonist of α4β2 and α6β2 nicotinic receptors, cytisinicline reduces withdrawal symptoms while attenuating the reinforcing effects of inhaled nicotine. Its clinical efficacy in smoking cessation has been demonstrated in multiple randomized controlled trials and meta‑analyses, showing non‑inferiority or superiority to nicotine replacement therapy and comparable efficacy to varenicline with a more favorable safety profile. Cytisinicline therefore represents an effective, safe, and cost‑efficient pharmacological option for smoking cessation when integrated into comprehensive behavioral support strategies.

Keywords: nicotine, dependence, smoking, cytisine, nicotinic receptors, cytisinicline.

Accepted: April 23, 2026; Published: April 28, 2026  Show citation

ACS AIP APA ASA Harvard Chicago Chicago Notes IEEE ISO690 MLA NLM Turabian Vancouver
Slíva J. The role of cytisinicline in the treatment of nicotine dependence. Med. praxi. 2026;23(2):85-89. doi: 10.36290/med.2026.018.
Download citation

References

  1. Etter JF. Cytisine for smoking cessation: a literature review and a meta-analysis. Arch Intern Med. 2006 Aug 14-28;166(15):1553-9. Go to original source...
  2. Yu L, Jiang B, Chen Z, et al. Cytisine induces endoplasmic reticulum stress caused by calcium overload in HepG2 cells. Oncol Rep. 2018 Mar;39(3):1475-1484. Go to original source...
  3. Dale HH, Laidlaw PP. The physiological action of cytisine, the active alkaloid of laburnum(cytius-laburnum), J. Physiol. Exp. Ther. 1912; 3:205-221. Go to original source...
  4. Alzarea S, Rahman S. Alpha-7 nicotinic receptor allosteric modulator PNU120596 prevents lipopolysaccharide-induced anxiety, cognitive deficit and depression-like behaviors in mice. Behav Brain Res. 2019 Jul 2;366:19-28. Go to original source... Go to PubMed...
  5. Tutka P, Vinnikov D, Courtney RJ, Benowitz NL. Cytisine for nicotine addiction treatment: a review of pharmacology, therapeutics and an update of clinical trial evidence for smoking cessation. Addiction. 2019 Nov;114(11):1951-1969. Go to original source... Go to PubMed...
  6. Thun MJ, Carter BD, Feskanich D, et al. 50-year trends in smoking-related mortality in the United States. N Engl J Med. 2013 Jan 24;368(4):351-64. Go to original source...
  7. Pistillo F, Clementi F, Zoli M, Gotti C. Nicotinic, glutamatergic and dopaminergic synaptic transmission and plasticity in the mesocorticolimbic system: focus on nicotine effects. Prog Neurobiol. 2015 Jan;124:1-27. Go to original source...
  8. Grando SA. Connections of nicotine to cancer. Nat Rev Cancer. 2014 Jun;14(6):419-29. Go to original source... Go to PubMed...
  9. Prochaska JJ, Benowitz NL. The Past, Present, and Future of Nicotine Addiction Therapy. Annu Rev Med. 2016;67:467-86. Go to original source... Go to PubMed...
  10. Gendy MNS, Ibrahim C, Sloan ME, Le Foll B. Randomized Clinical Trials Investigating Innovative Interventions for Smoking Cessation in the Last Decade. Handb Exp Pharmacol. 2020;258:395-420. Go to original source... Go to PubMed...
  11. Rollema H, Shrikhande A, Ward KM, et al. Pre-clinical properties of the alpha4beta2 nicotinic acetylcholine receptor partial agonists varenicline, cytisine and dianicline translate to clinical efficacy for nicotine dependence. Br J Pharmacol. 2010 May;160(2):334-45. Go to original source...
  12. Etter JF, Lukas RJ, Benowitz NL, West R, Dresler CM. Cytisine for smoking cessation: a research agenda. Drug Alcohol Depend. 2008 Jan 1;92(1-3):3-8. Go to original source...
  13. Zatonski W, Cedzynska M, Tutka P, West R. An uncontrolled trial of cytisine (Tabex) for smoking cessation. Tob Control. 2006 Dec;15(6):481-4. Go to original source... Go to PubMed...
  14. West R, Zatonski W, Cedzynska M. Placebo-controlled trial of cytisine for smoking cessation. N Engl J Med. 2011 Sep 29;365(13):1193-200. Go to original source... Go to PubMed...
  15. Walker N, Howe C, Glover M, et al. Cytisine versus nicotine for smoking cessation. N Engl J Med. 2014 Dec 18;371(25):2353-62. Go to original source... Go to PubMed...
  16. Walker N, Smith B, Barnes J, et al. Cytisine versus varenicline for smoking cessation in New Zealand indigenous Māori: a randomized controlled trial. Addiction. 2021 Oct;116(10):2847-2858. Go to original source...
  17. Rigotti NA, Benowitz NL, Prochaska JJ, et al. Cytisinicline for Smoking Cessation: The ORCA Phase 3 Replication Randomized Clinical Trial. JAMA Intern Med. 2025 Jun 1;185(6):648-655. Go to original source...
  18. Ofori S, Lu C, Olasupo OO, et al. Cytisine for smoking cessation: A systematic review and meta-analysis. Drug Alcohol Depend. 2023 Oct 1;251:110936. Go to original source...
  19. Rigotti NA, Benowitz NL. An evaluation of cytisinicline for smoking cessation in adult smokers. Expert Opin Pharmacother. 2026 Apr 6:1-9. Go to original source... Go to PubMed...
  20. Tang E, Rodriguez RM, Srivastava A, et al. Impact of short duration smoking cessation on post-operative complications: A systematic review and meta-analysis. J Clin Anesth. 2025 Sep;106:111967. Go to original source... Go to PubMed...
  21. Alhabdan S, Alashjaai A, Adebisi YA. Preoperative smoking cessation interventions and their effects on smoking abstinence and postoperative outcomes: a systematic review and meta-analysis. Updates Surg. 2025 Sep 15. Ahead of Print. Go to original source... Go to PubMed...
  22. Mills E, Eyawo O, Lockhart I, et al. Smoking cessation reduces postoperative complications: a systematic review and meta-analysis. Am J Med. 2011 Feb;124(2):144-154.e8. Go to original source...
  23. Majo García R, Espinosa Villoria MG, Fernández-Martínez MN, et al. Evidence Update on the Efficacy of Cytisinicline by Treatment Regimen: A Rapid Review. Open Respir Arch. 2025 Jul 23;7(3):100472. Go to original source...




Medicine for Practice

Madam, Sir,
please be aware that the website on which you intend to enter, not the general public because it contains technical information about medicines, including advertisements relating to medicinal products. This information and communication professionals are solely under §2 of the Act n.40/1995 Coll. Is active persons authorized to prescribe or supply (hereinafter expert).
Take note that if you are not an expert, you run the risk of danger to their health or the health of other persons, if you the obtained information improperly understood or interpreted, and especially advertising which may be part of this site, or whether you used it for self-diagnosis or medical treatment, whether in relation to each other in person or in relation to others.

I declare:

  1. that I have met the above instruction
  2. I'm an expert within the meaning of the Act n.40/1995 Coll. the regulation of advertising, as amended, and I am aware of the risks that would be a person other than the expert input to these sites exhibited


No

Yes

If your statement is not true, please be aware
that brings the risk of danger to their health or the health of others.