Cytisine is an agonist of nicotinic receptors; in particular, it binds strongly with α4β2 nicotinic receptors. Cytisine has been used to treat tobacco dependence for 40 years in Eastern Europe. The objective of this study was to review the literature on the effect of cytisine on smoking cessation.
Review of PubMed, EMBASE, Psychological Abstracts, BIOSIS, Google.com, and Scholar.google.com, using the keywords cytisine, cytisin, zytisin, cytisinum, Tabex, and smoking cessation. Experts and the manufacturer of Tabex were contacted. Placebo-controlled trials were included in a meta-analysis.
Ten studies reported the effects of cytisine on smoking cessation, including 4 controlled studies (3 placebo controlled). Nine studies used the Bulgarian drug Tabex, containing 1.5 mg of cytisine per tablet, and one Russian study used buccal films containing either 1.5 mg of cytisine or 0.75 mg of cytisine plus 0.75 mg of anabasine. All studies were published between 1967 and 2005 in Bulgaria, Germany, Poland, and Russia. There were 4404 smokers treated with cytisine and 3518 in control conditions. The pooled odds ratio after 3 to 8 weeks in the 3 placebo-controlled trials (2 were double blind and 1 was randomized) was 1.93 (95% confidence interval, 1.21-3.06). For the 2 placebo-controlled double-blind trials with a longer follow-up, the pooled odds ratio after 3 to 6 months was 1.83 (95% confidence interval, 1.12-2.99). One placebo-controlled double-blind trial had follow-up after 2 years (odds ratio, 1.77; 95% confidence interval, 1.29-2.43). Some adverse effects were reported. Most trials were, however, of poor quality.
Cytisine may be effective for smoking cessation. This fact remained largely unnoticed in the English-language literature.