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[Pharmacology](https://durgical.com/en/pharmacology/) · [Smoking cessation medicines](https://durgical.com/en/pharmacology/classes/smoking-cessation-medicines/)

# Cytisine

A plant alkaloid that is a nicotinic partial agonist, used to quit smoking. WHO added it to the essential medicines list in 2025.

Updated 2026-11-01

- Class: [Smoking cessation medicines](https://durgical.com/en/pharmacology/classes/smoking-cessation-medicines/)
- Receptor: Nicotinic acetylcholine receptor α4β2
- ATC code: N07BA04
- WHO Model List of Essential Medicines

Also called: Cytisinicline (INN)

◎**Nicotinic acetylcholine receptor α4β2**Cytisine

ⓘ The figure shows nicotine, which binds the same site, in the human α4β2 nicotinic receptor; cytisine has only been solved with model proteins (acetylcholine-binding proteins), not the human receptor.

**Target in 3D:** Nicotinic acetylcholine receptor α4β2. PDB structure 6CNJ (RCSB PDB, public domain). [View the structure at RCSB PDB](https://www.rcsb.org/structure/6CNJ) · Drag to rotate · pinch to zoom

## Mechanism of action

Cytisine is a plant alkaloid and a partial agonist at nicotinic acetylcholine receptors, with affinity for the α4β2 subtype. Like varenicline, which was developed from it, it eases craving and blocks part of nicotine's reward.

- Binds α4β2 nicotinic receptors as a partial agonist
- Partial stimulation eases craving
- Nicotine from smoking rewards less

## Pharmacokinetics

**Absorption**
Taken by mouth

**Half-life**
About 5 hours

## Indications

- Aid to stopping smoking and tobacco use, with counselling and behavioural support [Tobacco use disorder →](https://durgical.com/en/conditions/tobacco-use-disorder/)

## Adverse effects

### Common

- Gastrointestinal upset (mostly mild)
- Sleep disturbance

### Serious (rare, important)

- Serious adverse events did not differ from placebo in the reviewed trials

## Contraindications

- Hypersensitivity to cytisine

## Key interactions

**Theophylline, warfarin, insulin (effect of quitting smoking)**
Their effects may change after stopping smoking; doses may need review

**Continued smoking**
Less benefit; the plan is to stop tobacco completely

## What is monitored

- Smoking status
- Gastrointestinal and sleep complaints

## Administration and safety

- Given by mouth over a set course, with a planned quit date
- Combined with counselling or behavioural support

## Nursing care

- Agree on a quit date and follow-up
- Ask about nausea, stomach upset and sleep
- Review medicines whose effect changes when smoking stops

## Pregnancy and breastfeeding

Not established in pregnancy; behavioural support comes first.

## Memory aid

Cytisine: «the original from the plant» – varenicline's ancestor, same partial-agonist trick, shorter half-life.

## Test yourself

Think of the answer, then tap the question to see it.

## What is the relation between cytisine and varenicline?

Varenicline was developed from cytisine; both are nicotinic partial agonists.

## In which year did cytisine enter the WHO essential medicines list?

2025, on the core list.

## Which adverse effects are reported most often with cytisine?

Gastrointestinal upset and sleep disturbance.

[Add to my cards (3)](https://durgical.app/estudiar/?add=/en/pharmacology/cytisine/)

## Related drugs

- [Varenicline](https://durgical.com/en/pharmacology/varenicline/)
- [Nicotine (replacement therapy)](https://durgical.com/en/pharmacology/nicotine/)

## Related conditions

- [Tobacco use disorder](https://durgical.com/en/conditions/tobacco-use-disorder/)

[← Back to the class: Smoking cessation medicines](https://durgical.com/en/pharmacology/classes/smoking-cessation-medicines/)

Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: [Cytisine (cytisinicline)](https://list.essentialmeds.org/recommendations/1472) (World Health Organization (eEML), 2025); Goodman & Gilman's The Pharmacological Basis of Therapeutics, 14th ed., ch. 13 (McGraw Hill, 2023); [WHO releases first-ever clinical treatment guideline for tobacco cessation in adults](https://www.who.int/news/item/02-07-2024-who-releases-first-ever-clinical-treatment-guideline-for-tobacco-cessation-in-adults) (World Health Organization, 2024); [ATCDDD - ATC/DDD Index](https://atcddd.fhi.no/atc_ddd_index/?code=N07BA04) (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

## **Spotted a mistake?** We are always improving for the community. Tell us what is wrong and our team will review it. Report a mistake

Representative model, for educational purposes only.

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Source: https://durgical.com/en/pharmacology/cytisine/
License: CC BY 4.0 (https://creativecommons.org/licenses/by/4.0/). Cite as: DurgiPedia (durgical.com), https://durgical.com/en/pharmacology/cytisine/