Partial nicotinic receptor agonist (smoking cessation) Pregnancy: Contraindicated during pregnancy and during breast-feeding. There are no or limited data from use in pregnant women and animal studies are insufficient with respect to reproductive toxicity. Women of childbearing potential must use highly effective contraception while taking cytisinicline, and women using systemically acting hormonal contraceptives should add a second barrier method. Fertility: no data.

Cytisinicline

Brand names: Tabex, Cytisine (specials)

Cytisinicline (cytisine) is an orally administered plant-derived aid to smoking cessation, taken as a short reducing course alongside behavioural support. A target stop date is set within the first few days of the regimen.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 25-day reducing course of 1.5 mg tablets: days 1-3, one tablet every 2 hours (maximum 6 tablets daily); days 4-12, one tablet every 2.5 hours (maximum 5 tablets daily); days 13-16, one tablet every 3 hours (maximum 4 tablets daily); days 17-20, one tablet every 5 hours (maximum 3 tablets daily); days 21-25, 1-2 tablets a day (maximum 2 tablets daily)

Route: Oral — taken with a suitable amount of water (source product: Cytisinicline 1.5 mg tablets)

Frequency: Fixed reducing schedule over 25 days as above; one package of 100 tablets is sufficient for a complete treatment course

Max: Maximum daily dose by treatment stage: 6 tablets (days 1-3), 5 tablets (days 4-12), 4 tablets (days 13-16), 3 tablets (days 17-20), 2 tablets (days 21-25)

Source: UK SPC (eMC) §4.2 for Cytisinicline 1.5 mg tablets (https://www.medicines.org.uk/emc/product/15789/smpc). The duration of therapy is 25 days. SMOKING CESSATION: 'Smoking should be stopped no later than on the 5th day of treatment. Smoking should not be continued during treatment as this may aggravate adverse reactions.' TREATMENT FAILURE: the treatment should be discontinued and may be resumed after 2 to 3 months. ELDERLY: due to limited clinical experience, cytisinicline is not recommended for use in elderly patients over 65 years of age. RENAL/HEPATIC: there is no clinical experience in patients with renal or hepatic impairment, therefore the product is not recommended for use in this patient population. PAEDIATRIC: safety and efficacy in persons under 18 years of age have not been established and cytisinicline is not recommended for use in persons under 18 years — no paediatric dose is stated, so paedDose is null; verify any under-18 use against a children's formulary. §4.4: should be taken only by those with a serious intention of weaning off nicotine; women of childbearing potential must use highly effective contraception while taking cytisinicline. Doses above are expressed in tablets exactly as the SPC states them (each tablet contains 1.5 mg).

Dose adjustments

Renal

There is no clinical experience of cytisinicline in patients with renal (or hepatic) impairment, therefore the product is not recommended for use in this patient population

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Hypersensitivity to the active substance or to any of the excipients listed in section 6.1
Unstable angina
A history of recent myocardial infarction
Clinically significant arrhythmias
A history of recent stroke
Pregnancy and breastfeeding

Side effects

Very common: change in appetite (mainly increase) and weight gain
Very common: dizziness, irritability, mood changes, anxiety, sleep disorders (insomnia, drowsiness, lethargy, abnormal dreams, nightmares) and headaches
Very common: tachycardia and hypertension (common: slow heart rate)
Very common gastrointestinal effects: dry mouth, diarrhoea, nausea, taste changes, heartburn, constipation, vomiting and abdominal pain (especially upper abdomen)
Very common: rash, myalgia and fatigue; uncommon: increase in serum transaminase levels

Interactions

Cytisinicline should not be used with anti-tuberculosis drugs; no other clinical data on significant interaction with other drugs
Simultaneous administration with smoking or use of products containing nicotine could lead to aggravated adverse reactions of nicotine
Effect of smoking cessation: polycyclic aromatic hydrocarbons in tobacco smoke induce CYP1A2 (and possibly CYP1A1) metabolism — stopping smoking may slow metabolism and raise blood levels of drugs with a narrow therapeutic window, e.g. theophylline, tacrine, clozapine and ropinirole
Plasma concentrations of other medicinal products partly metabolised by CYP1A2 (e.g. imipramine, olanzapine, clomipramine, fluvoxamine) may also increase on cessation of smoking; metabolism of flecainide and pentazocine may also be induced by smoking
Hormonal contraceptives: it is currently unknown whether cytisinicline may reduce the effectiveness of systemically acting hormonal contraceptives — women using them should add a second barrier method

Clinical monograph

How it works

It is a partial agonist at nicotinic acetylcholine receptors, partially stimulating them to ease withdrawal while reducing the reward from smoking. This dual action lessens craving and the satisfaction of any cigarette smoked.

Prescribing in practice

Use with caution in significant cardiovascular disease, as nicotinic receptor agonists can affect cardiovascular parameters; it is not recommended in pregnancy or breastfeeding.
Follow the staged dose-reduction schedule over the course and provide concurrent behavioural support.
Common adverse effects are gastrointestinal upset and altered sleep or appetite.

Monitoring

Monitor smoking status, tolerability, and any cardiovascular or neuropsychiatric symptoms during the course.

Counselling the patient

Follow the day-by-day schedule closely and stop smoking by your agreed early target date.
Take with care to reduce nausea and report troublesome stomach upset.
Combine the tablets with support or counselling for the best chance of quitting.

Evidence & guidelines

Cytisine is supported in UK smoking-cessation guidance as a licensed oral option that improves quit rates when combined with behavioural support.

Reference: NICE NG209; UKHSA smoking cessation guidance; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Pathways