Cytisine – The Old, New Quit Smoking Therapy

Cytisine, a plant derived alkaloid similar to Varenicline (Champix/Chantix), is structurally similar to nicotine and acts on nicotinic receptors, again in a similar way that Varenicline does.  Cytisine is thought to aid smoking cessation by reducing the severity of withdrawal symptoms and reducing the reward and smoking satisfaction.  The biggest advantage of Cytisine is affordability.  In Europe, Cytisine costs just $20 – $30 USD for a complete 25 day course.  This is much less than the recommended 12 week course of NRT, Varenicline and others.  Here is a summary of what you need to know:

  1. Cytisine (Tabex) has been available over-the-counter and by prescription for the treatment of smoking dependence in central and eastern Europe since the 1960’s.
  2. Cytisine releases approximately 40% of the dopamine that nicotine consumption would, when studied in rats.
  3. It is taken orally in tablet form at 1.5 mg per tablet in a tapering dose over 25 days.  Clients start with 1.5 mg, or one tablet, every 2 hours on days 1 to 3 (9mg/day), and taper to 1 tablet every six hours on day 21 to 25 (3mg/day). Users are advised to reduce the number of cigs they smoke over the first 5 days, and assign Day 5 as their official quit date.
  4. The half-life of Cytisine is 4.8 hours, compared to Varenicline which is 17 hours.
  5. Cytisine is not metabolised, but is readily absorbed through the gastrointestinal tract, and excreted by the kidneys (may need to reduce dose in compromised kidney function)
  6. There is limited data regarding interactions with other drugs, however in a small sample of 17 adults, cytisine showed no unfavorable interactions with insulin, antidepressants or neuroleptics.  There is also limited data regarding contraindications however the manufacturers list the following: arterial hypertension, advanced atherosclerosis, and pregnancy/breastfeeding.
  7. Cytisine was found to be superior to placebo and NRT at one week, 2 months, and six months, and time to relapse back to smoking was significantly delayed in the cytisine group compared to NRT.  Studies are currently underway to compare Cytisine with behavioral therapy alone, and other smoking cessation therapies such as Varenicline and Nortriptyline.
  8. Cytisine is well tolerated at therapeutic doses (1.5 mg to 9 mg /day/ 25 days), and few adverse events were noted, however if noted adverse events were primarily gastrointestinal and included things like nausea, vomiting and sleep disturbance.

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