Cytisine

Brand names: Baptitoxine, Sophorine

Usage of Cytisine

Appetite suppressant effects

Animal data

A study in rats reported that cytisine-treated animals ate less and gained less weight than the control arm.Grebenstein 2013

Clinical data

Clinical trials evaluating the effect of cytisine on appetite are lacking; however, subjects in an open-label pharmacokinetic study in healthy adults conversely reported increased appetite.Jeong 2017

Cancer

In vitro data

Cytisine induced apoptosis in HepG2 cells via a mitochondrial pathway, suggesting potential chemotherapeutic applications.Yu 2018

CNS effects

Animal and in vitro data

In vitro studies suggest neuronal protective effects of cytisine through mechanisms that involve downregulation of N-methyl-D-aspartate (NMDA) receptors.Li 2013 Limited studies in rodents have reported efficacy in treating induced depression. Treatment with cytisine for 2 weeks relieved symptoms related to unpredictable chronic mild stress.Han 2016 In another study of a mouse model, fluoxetine and cytisine were shown to have synergistic effects on depression, whereas serotonin depletion blocked the antidepressant effects of cytisine.Mineur 2015 A study in rats suggested cytisine attenuated the mental discomfort associated with nicotine withdrawal.Igari 2014 A study in rodents showed cytisine modulates chronic voluntary ethanol consumption, suggesting a possible role in alcohol addiction.Sajja 2013, Sotomajor 2013

Diabetes

Animal data

A study in mice reported efficacy in treatment of type 2 diabetes with a combination preparation containing cytisine with a water-soluble analog of vitamin E (Trolox C).Jin 2014

Smoking cessation

Cytisine as an option in smoking cessation has been the topic of a number of supportive journal articles and editorials.Mulhall 2015, Prochaska 2016, Rigotti 2014, Stapleton 2015, Walker 2016, Zatonski 2015

Animal data

Studies in rodents suggest cytisine is a nicotinic receptor agonist, behaving as both a competitive partial agonist and full agonist, depending on the subunit of attachment. Cytisine appears to have weaker peripheral effects on the cardiovascular system than nicotine.Radchenko 2015, Rouden 2014

Clinical data

Meta-analyses of available clinical trial data have been conducted, with 2 quality clinical studies identifiedVinnikov 2008, West 2011 and up to 9 other clinical studies evaluated.Cahil 2013, Hajek 2013, Leaviss 2014, Samet 2014 No head-to-head trials comparing varenicline with cytisine had been conducted as of January 2013; however, further trials evaluating cytisine have been registered or are in progress.Leaviss 2014, NIH 2018

One quality clinical trial evaluating cytisine versus placebo in middle-age smokers reported no difference in abstinence at 8 weeks, but a significant difference in abstinence at 26 weeks (10.6% for the cytisine group compared to 1.2% with placebo [P=0.01]).Vinnikov 2008 A second quality clinical trial enrolled 740 participants in a single-center, randomized, double-blind, placebo-controlled trial and reported a sustained 12-month abstinence rate of 8.4% in the cytisine group compared with 2.4% in the placebo group (95% confidence interval [CI], 2.7% to 9.2%; P=0.001).West 2011 Pooled results from these 2 clinical trials show a risk ratio for successful cessation of 3.29 (95% CI, 1.84 to 5.9) with cytisine intervention.Hajek 2013, Samet 2014

Another open-label, noninferiority trial randomly assigned 1,310 adult daily smokers to oral cytisine for 25 days or nicotine replacement therapy for 8 weeks. Cytisine was superior to nicotine replacement therapy, with higher continuous abstinence rates at 1 week, 2 months, and 6 months.Walker 2014 This study was noted to have certain methodological limitations.Mulhall 2015

Cytisine side effects

Evidence supports the safety of cytisine; long periods of postmarketing surveillance exist in the European Medicines Authority database.Aveyard 2013, Hajek 2013 However, dose-dependent reports of toxicity exist (see Toxicology).

In an open-label pharmacokinetic study in healthy adults, no effects on blood pressure or respiratory rate were observed, and reported adverse effects included increased appetite, dry mouth, dream/nightmares, and irritability.Jeong 2017 Similar findings have been reported in a systematic review of the literature.Leaviss 2014

A Cochrane meta-analysis of 3 clinical trials using cytisine report a lack of significant adverse effects, with GI disorders (dyspepsia and nausea) and headache most commonly reported.Cahill 2013 Similarly, a review that included 8 clinical trials reported more adverse GI effects with cytisine than placebo (relative risk, 1.76; 95% CI, 1.28 to 2.42) but no significant safety concerns.Hajek 2013

Contraindications for use include pregnancy and breastfeeding, severe atherosclerosis, and uncontrolled hypertension.Prochaska 2013

Before taking Cytisine

Information regarding use in pregnancy or lactation is lacking. At 4 to 5 weeks' gestation, nicotinic receptor proteins and gene transcripts for nicotinic receptor subunits exist in the human prenatal brain, making the consequences of cytisine use during pregnancy potentially similar to that of smoking.Hellstrom 2001

How to use Cytisine

Cytisine is available as tablets and capsules (both containing cytisine 1.5 mg), and as oral strips (cytisine 1 mg).Jeong 2017 All 3 doseforms are associated with the same recommended dosing regimen for smoking cessation: One dose every 2 hours (6 doses per day) for days 1 through 3, with the dosing interval increased to every 2.5 hours (5 doses per day) days 4 through 12, to every 4 hours (4 doses per day) days 13 through 16, to every 5 hours (3 doses per day) days 17 through 20, and to every 6 hours (2 doses per day) days 21 through 25. The recommended target "quit day" is day 5.Jeong 2017, West 2011

Pharmacokinetic studies conducted in rabbitsAstroug 2010 and healthy human volunteersJeong 2017 reported rapid but incomplete absorption following oral administration. The half-life is estimated to be about 5 hours.Jeong 2017 A pharmacokinetic study reported cytisine is renally excreted, with no metabolites detected in plasma or urine.Jeong 2015

Warnings

Animal studies have shown that the leaves and seeds of L. anagyroides and related plants are toxic. A lethal dose in horses has been estimated to be 0.5 g/kg of L. anagyroides seedpods.Jeong 2017, Rouden 2014, Simeonova 2010

Cytisine toxicity is considered to be dose dependent, and reports of fatalities due to respiratory failure following consumption of L. anagyroides plant material exist.Jeong 2017, Musshoff 2009

No antidote to cytisine toxicity has been identified, and management is supportive.Rouden 2014

What other drugs will affect Cytisine

Theoretically, an interaction with varenicline, also used in smoking cessation, is possible, given that both act at the nicotinic receptor.

Studies in mice demonstrated inhibition of phenytoin and lamotrigine anticonvulsant activity by cytisine,Tutka 2013 as well as that of lacosamide, levetiracetam, and pregabalin.Tutka 2017

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