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CYTISINICLINE
Generic Name: CYTISINICLINE
ABSTRACT -
Cytisinicline, also known as cytisine, is a plant-derived alkaloid that acts as a partial agonist at nicotinic acetylcholine receptors, especially alpha4beta2 receptors. It is used or investigated to reduce nicotine cravings and support smoking cessation.
DOSAGE -
Where approved as 1.5 mg tablets, one 25-day course may be used with tapering frequency: days 1-3 one tablet every 2 hours, days 4-12 every 2.5 hours, days 13-16 every 3 hours, days 17-20 every 5 hours, and days 21-25 one to two tablets daily. Smoking should stop no later than day 5, or per the approved label.
SIDE EEFECTS -
- Nausea, dry mouth, abdominal pain, dyspepsia, constipation, or diarrhea
- Headache, dizziness, irritability, mood changes, or sleep disturbance
- Appetite change, weight change, or taste disturbance
- Fast heartbeat, palpitations, or increased blood pressure
- Rash, sweating, muscle aches, fatigue, or malaise
ALLERGIC REACTIONS -
(These symptoms may indicate an allergic reaction and require medical attention.)
- Rash, itching, hives, or widespread redness
- Swelling of the face, lips, tongue, or throat
- Wheezing, chest tightness, or breathing difficulty
- Severe dizziness, fainting, or anaphylaxis
DRUG INTERACTIONS-
- Concurrent smoking or nicotine products can intensify adverse reactions and undermine cessation goals
- Smoking cessation can change exposure to CYP1A2 substrates such as theophylline, clozapine, olanzapine, and some caffeine effects
- Avoid or review use with anti-tuberculosis medicines where the product label warns against coadministration
- Hormonal contraceptive reliability may require additional barrier contraception according to some labels
PREAUTONS–
- Use only when the patient is motivated to stop smoking or reduce nicotine dependence
- Use caution in cardiovascular disease, hypertension, gastrointestinal ulcer disease, hyperthyroidism, diabetes, renal/hepatic impairment, and psychiatric illness
- Contraindicated in pregnancy and breastfeeding in some labels
- Review all medicines affected by smoking cessation before therapy
- Regulatory approval status and dosing schedules vary by country
WARNINGS –
- Do not use after recent myocardial infarction, recent stroke, unstable angina, or significant arrhythmia unless a specialist determines otherwise
- Stop smoking during treatment as instructed; continued smoking may worsen side effects
- Seek urgent care for chest pain, severe palpitations, neurologic symptoms, or allergic reaction
- As of June 2026, cytisinicline was not FDA-approved in the United States; availability differs internationally
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