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Cytisine – Smoking Cessation Active Ingredient

Cytisine is a plant-derived active ingredient used to support smoking cessation. It works similarly to nicotine and helps reduce cravings for cigarettes.

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Things worth knowing about "Cytisine"

Cytisine is a plant-derived active ingredient used to support smoking cessation. It works similarly to nicotine and helps reduce cravings for cigarettes.

What is Cytisine?

Cytisine is a naturally occurring plant alkaloid extracted from the seeds of the laburnum shrub (Laburnum anagyroides). It has been used for decades in Eastern Europe as a smoking cessation aid and is now approved in several countries, including European Union member states, under the brand name Todacitan.

Mechanism of Action

Cytisine acts as a partial agonist at nicotinic acetylcholine receptors in the brain, particularly at the α4β2 subtype — the same receptors targeted by nicotine. This dual action provides two key therapeutic effects:

Reduction of withdrawal symptoms: By partially activating the receptors, cytisine decreases the urge to smoke and relieves nicotine cravings.
Blocking the reward effect of nicotine: If the individual does smoke, nicotine produces a significantly reduced pleasurable effect because the receptors are already occupied.

This combination makes cytisine an effective pharmacological tool for smoking cessation.

Usage and Dosage

Cytisine is typically taken over a 25-day course with a gradually decreasing dose schedule:

Days 1–3: 6 tablets daily (every 2 hours, 1.5 mg per tablet)
Days 4–12: 5 tablets daily
Days 13–16: 4 tablets daily
Days 17–20: 3 tablets daily
Days 21–25: 1–2 tablets daily

Patients are advised to stop smoking by the 5th day of treatment at the latest. The course may be repeated upon medical advice if needed.

Indication

Cytisine is indicated for adult smokers who wish to quit smoking. It is considered a plant-based alternative to synthetic agents such as varenicline and may be suitable for individuals who have not responded sufficiently to nicotine replacement therapy.

Side Effects

Cytisine is generally well tolerated. Possible side effects include:

Nausea and vomiting
Dry mouth
Sleep disturbances
Headache
Elevated blood pressure

Since cytisine is an alkaloid, overdose can be toxic. It must always be taken strictly as directed by a healthcare professional.

Contraindications

Cytisine should not be used in:

Pregnancy and breastfeeding
Severe cardiovascular disease
Arterial hypertension (high blood pressure)
Known hypersensitivity to the active ingredient

Scientific Evidence

Clinical studies, including a landmark trial published in the New England Journal of Medicine, confirm the efficacy of cytisine for smoking cessation. Participants taking cytisine showed significantly higher abstinence rates compared to placebo. Its effectiveness is comparable to that of varenicline, while being considerably more cost-effective.

References

Walker N. et al. - Cytisine versus Nicotine for Smoking Cessation. New England Journal of Medicine, 2014; 371:2353–2362.
European Medicines Agency (EMA) - Todacitan (cytisine) Assessment Report, 2023. URL: https://www.ema.europa.eu
West R. et al. - Placebo-controlled trial of cytisine for smoking cessation. Thorax, 2011; 66:998–1000.

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