Cytisine — Tabex (Quinolizidine Alkaloid · Nicotinic Partial Agonist · Smoking Cessation)
| Compound | Cytisine (Baptitoxine / Sophorine) |
| Chemical class | Alkaloid — Quinolizidine (Lupane-type bicyclic quinolizidine) |
| CAS | 485-35-8 |
| Primary source | Laburnum anagyroides (golden chain tree), Cytisus scoparius (Scotch broom), Sophora spp. |
| Key applications | Nicotinic partial agonist, smoking cessation, cognitive (preclinical), respiratory stimulant |
| Claim strength | High (smoking cessation RCTs) |
| Typical form | Tabex® (cytisine tablet, Eastern European pharmaceutical); cytisine isolate; Laburnum extract |
| Buy from Herbuno | Request availability and bulk pricing → |
Name origin: From Cytisus (Scotch broom genus). Also known as baptitoxine (from Baptisia) and sophorine (from Sophora) — reflecting its occurrence across multiple plant genera. Cytisine is a bicyclic quinolizidine alkaloid structurally related to nicotine — it occupies the same nicotinic acetylcholine receptor (nAChR) binding site with partial agonist activity. This structural and pharmacological relationship to nicotine has made cytisine the most clinically studied natural nicotinic partial agonist for smoking cessation. Traditional use: Laburnum (Laburnum anagyroides) and Scotch broom (Cytisus scoparius) have been used in European traditional medicine as emetics, purgatives, and for respiratory conditions. The toxic potential of cytisine at higher doses (from Laburnum especially — the “golden chain” is one of the most toxic UK garden plants) was well-known historically. Cytisine’s smoking cessation application emerged from Eastern European phytopharmacology research in the 1960s. Research trajectory: Cytisine has an excellent and growing RCT evidence base for smoking cessation, including several large well-powered trials (CASCADES, 2014, n=1310; Walker et al. 2020 meta-analysis of 12 RCTs). It is approved and widely used as the pharmaceutical Tabex® in several Eastern European countries (Bulgaria, Poland, Russia) and is under review in Western markets as a low-cost smoking cessation pharmaceutical. Cytisine is the natural prototype for varenicline (Champix/Chantix) — the most effective prescription smoking cessation drug — which was designed with cytisine as the lead compound. Commercial source: Not currently in the Herbuno catalogue. Contact Herbuno for availability assessment.
Evidence for Cytisine Applications
Smoking cessation — multiple RCTs (High claim strength): A 2020 meta-analysis (Walker et al.) of 12 RCTs (n=3,784 participants) confirmed cytisine (1.5 mg tablets, tapering 25-day course) significantly increased 6-month continuous abstinence rates versus placebo (RR 3.98; 95% CI 2.01–7.87). Head-to-head RCTs show cytisine is comparable to nicotine replacement therapy and potentially superior. Cytisine is substantially cheaper than varenicline or NRT — making it a high-evidence, low-cost smoking cessation option with potential global public health impact. Claim strength: High.
Nicotinic receptor pharmacology: Cytisine is a partial agonist at α4β2 nicotinic acetylcholine receptors — binding with high affinity but producing submaximal receptor activation. This partial agonism simultaneously provides mild nicotinic stimulation (reducing withdrawal symptoms) and competitively blocks nicotine from achieving full receptor activation (reducing the reward from smoking). This is the same mechanism as varenicline — cytisine is the natural template. Claim strength: High (mechanism confirmed).
Respiratory stimulant: Cytisine has direct respiratory stimulant activity via carotid body nAChR activation — historically studied for respiratory depression. At sub-toxic doses, it stimulates breathing. This respiratory stimulant property underlies some traditional respiratory uses of cytisine-containing plants. Claim strength: Moderate (pharmacological mechanism; no clinical supplement data).
Request availability and bulk pricing →
Browse Standardised Extract Powders →
Dosage & Formulator Specification
Tabex® (approved pharmaceutical) dosing: 1.5 mg cytisine 6×/day for 3 days, then reducing to 1.5 mg 3×/day through day 25. Total course: ~100 mg cytisine over 25 days. The therapeutic dose range for smoking cessation (1.5 mg multiple times daily) is well above doses producing GI side effects (nausea at higher single doses) — the tapering schedule manages side effects while maintaining efficacy. As a natural partial agonist, cytisine does not undergo the extensive CYP1A2-mediated metabolism that makes nicotine’s pharmacokinetics complex. Contact Herbuno for cytisine extract availability from Laburnum or Sophora sources.
Frequently Asked Questions — Cytisine
Is cytisine approved for smoking cessation in Western markets?
Not widely — cytisine is approved as Tabex® in several Eastern European countries (Bulgaria, Poland, Russia) where it has been marketed since the 1960s. In Western markets (US, UK, EU), cytisine has not achieved regulatory approval despite its evidence base, primarily due to regulatory pathway and commercial disincentives (it is off-patent and inexpensive to produce). A 2021 Lancet editorial called for urgent action to make cytisine available given its evidence base and low cost. New Zealand approved cytisine (Desmoxan) in 2022. UK MHRA approval is under consideration.
How does cytisine compare to varenicline for smoking cessation?
Varenicline (Champix/Chantix) was designed with cytisine as the structural lead — it is a synthetic cytisine analogue with optimised pharmacokinetics (longer half-life, better oral bioavailability). Meta-analyses suggest varenicline has marginally greater efficacy than cytisine for smoking cessation, but cytisine is approximately 20× cheaper than varenicline per treatment course. Given similar mechanisms and comparable efficacy, cytisine’s cost advantage makes it a highly attractive public health smoking cessation option for low-to-middle-income country populations.
Is laburnum poisoning from cytisine common?
Laburnum (Laburnum anagyroides, golden chain tree) is one of the most poisonous garden plants in the UK and Northern Europe — all parts contain cytisine, with seeds having the highest concentration. Children are the primary at-risk group for laburnum poisoning, typically from ingesting the attractive seed pods. Symptoms: nausea, vomiting, salivation, convulsions, and respiratory failure at high doses. UK Poison Information Centre handles laburnum exposure regularly. The toxicity reflects cytisine’s nicotinic agonist effects at above-therapeutic doses — the same mechanism that makes it pharmacologically valuable at controlled therapeutic doses.
Can cytisine be positioned as a natural alternative to nicotine patches?
Yes — this positioning is supported by the clinical evidence base (comparable efficacy to NRT in RCTs) and mechanistic rationale (partial nAChR agonism). However, regulatory compliance is critical: smoking cessation product claims typically trigger the pharmaceutical regulatory pathway rather than dietary supplement pathway in most markets. Formulators should seek specific regulatory advice on the supplement-versus-drug boundary for cytisine products in each target market. Natural origin and lower cost versus NRT/varenicline are genuine differentiating factors in the correct regulatory framework.
Related compounds: Sparteine, Vasicinone, Capsaicin, Colchicine
Claim-strength scale – High = multiple human RCTs; Moderate = limited trials or strong preclinical convergence; Emerging = early-stage lab or animal data.
← HerbIQ Compound Index · HerbIQ P02: Extraction · HerbIQ P03: Delivery