Cytisine
Common Name(s): Baptitoxine, Sophorine
Medically reviewed by Drugs.com. Last updated on Feb 21, 2022.
Clinical Overview
Use
Limited clinical data support a place in therapy for cytisine use in smoking cessation.
Dosing
Limited clinical studies are available to guide dosage. In studies of smoking cessation, the suggested dosing regimen was one cytisine dose (tablet or capsule: 1.5 mg; oral strip: 1 mg) every 2 hours initially (6 doses per day), then titrated downward over 25 days to 2 doses per day.
Contraindications
Contraindications for use include pregnancy and breastfeeding, advanced atherosclerosis, and uncontrolled hypertension.
Pregnancy/Lactation
Avoid use. Information regarding use in pregnancy and lactation is lacking.
Interactions
Information is limited. Data are lacking regarding use with other smoking cessation agents; concurrent use should be avoided.
Adverse Reactions
GI disorders (dyspepsia and nausea), headache, increased appetite, dry mouth, nightmares, and irritability have been reported.
Toxicology
Cytisine toxicity is considered to be dose dependent, and reports of fatalities due to respiratory failure following consumption of L. anagyroides plant material exist.
Scientific Family
- Fabaceae (pea)
- Leguminosae
Source
Cytisine is an alkaloid that exists naturally in the seeds of plants belonging to the Leguminosae/Fabaceae family, particularly L. anagyroides.Rouden 2014, Stead 2007 L. anagyroides, a small decorative garden tree (also called the Golden Rain Acacia due to its golden yellow flowers), is common in Central and Southern Europe. A synonym for L. anagyroides is Cytisus laburnum.USDA 2018, Rouden 2014
The plant species Ulex europaeus L., Baptisia tinctoria, and Sophora secundiflora contain chemicals previously identified as unique compounds (ulexine, sophorine, baptitoxine) but later determined to be identical to cytisine.Rouden 2014
Cytisine-type alkaloids have also been identified in other plant species, including Maackia amurensis, Sophora tonkinensis, and Ormosia hosiei.Pouny 2014, Rouden 2014
History
Traditional use of Laburnum seeds for their emetic effects, and use of the leaves of L. anagyroides as a tobacco substitute have been documented. By the late 19th century, the chemical structure and synthesis of cytisine was developed. Cytisine has been marketed for use in treatment of tobacco dependence in Central and Eastern Europe since the 1960s. Since the 1990s, a resurgence in interest in cytisine chemistry and potential therapeutic applications has resulted in a rise in the number of published studies evaluating its use; however, clinical trial data are lacking. Products containing cytisine are available in Russia and Poland, in other former Soviet countries, in Canada, and via the internet.Aveyard 2013, Gross 2015, Hajek 2013, Prochaska 2016, Rouden 2014
Chemistry
The chemical structure of cytisine has been described, and methods for identification of the compound have been published.Perez 2012, Rouden 2014
Methods of cytisine extraction from the seeds of L. anagyroides have been elucidated. Cytisine is a partial nicotinic agonist, similar to the FDA-approved drug varenicline.Astroug 2010, Aveyard 2013, Jeong 2015,
