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Cytisinicline for vaping cessation

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Cytisinicline is a partial agonist at α4β2 nicotinic acetylcholine receptors that mediate nicotine dependence, has shown efficacy for cigarette smoking cessation (1):

  • cytisinicline, historically known as cytisine, is a naturally occurring plant-based alkaloid that has been used as an over-the-counter smoking cessation product in Central and Eastern Europe for decades
  • cytisinicline, like varenicline, binds selectively to the α4β2 nicotinic acetylcholine receptor subtype that mediates nicotine dependence
    • cystisinicline acts as a partial agonist to reduce nicotine withdrawal symptoms while also blocking the reinforcement generated by nicotine when smoking cigarettes

A review notes (2):

  • a small, short-term, placebo-controlled trial evaluated whether cytisinicline (cytisine) plus behavioural support was more effective than behavioural support alone for vaping cessation.
  • a 12-week course of cytisinicline resulted in more people achieving short-term continuous abstinence from e-cigarettes than placebo (31.8% vs 15.1%)

NICE state with respect to cytisinicline and smoking cessation (3):

  • do not offer cytisinicline, varenicline or bupropion to people under 18
  • do not offer cytisinicline to people aged 66 and over
  • do not offer cytisinicline during pregnancy or breastfeeding
  • when using cytisinicline in smoking cessation, it is more likely to result in them successfully stopping smoking when combined with behavioural support
  • when using cytisinicline in smoking cessation, agree a quit date set within the first 5 days of treatment and reassess the person shortly before the prescription ends
  • cytisinicline is sometimes referred to as cytisine

Reference:

  1. Rigotti NA, Benowitz NL, Prochaska JJ, Cain DF, Ball J, Clarke A, Blumenstein BA, Jacobs C. Cytisinicline for Vaping Cessation in Adults Using Nicotine E-Cigarettes: The ORCA-V1 Randomized Clinical Trial. JAMA Intern Med. 2024 Aug 1;184(8):922-930.
  2. Cytisinicline for vaping cessation. Drug and Therapeutics Bulletin Published Online First: 30 January 2025.
  3. NICE (February 2025). Tobacco: preventing uptake, promoting quitting and treating dependence

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