Tabex Cytisine Introduction



Tabex is an original Bulgarian drug of vegetal origin for treatment of nicotinism. It is developed on the basis of the alkaloid contained in the plant Cytisus laburnum L., also called Golden Rain, widespread in the southern areas of Central Europe and Italy. All parts of the plant contain the alkaloid Cytisine, the greatest amount (up to 3%) being found in the seeds.

Fig. 1 Structural formula of cytisine

Fig. 1 Structural formula of cytisine

(1R-cis)-1,2,3,4,5,6-hexahidro-1,5-metano-8h-pyrido[1,2a][1,5]diazocin-8-on

Chemical characteristics and content of Tabex

Each tablet contains 0.0015 g cytisine

Empirical formula of cytisine: C11H14ON2

Ensuing from the molecular orbital calculations after Kier (1969), it is evident that the molecular configurations of nicotine and acetylcholine have a quaternary nitrogen atom which is with a negative charge and located at 4.85 +/- 0.1 A, considered to be responsible for the nicotine-like activity. In cytisine the nitrogen atom in ring C appears at 4.8-9 A from the oxygen atom of the pyridine group and is also negatively charged.

The prolonged clinical and toxicological studies in many countries all over the world have proved the enormous harm of smoking on all organs and systems of the human organism. The danger of cardiovascular incidents (myocardial infarction, stenocardia, peripheral vascular diseases), diseases of the respiratory system (lung cancer, tracheobronchitis, etc.), as well as psychic and physiological dependence of addictive type is mostly emphasized.

Fig. 2 Stereoisomeric formulae of cytisine and nicotine (after Barlow, R.B. and McLeod, L.J.)

Fig. 2 Stereoisomeric formulae of cytisine and nicotine (after Barlow, R.B. and McLeod, L.J.)

The treatment of nicotine addiction is a complex process in which drug therapy occupies an important part. Sopharma produces the drug Tabex, developed on the basis of the alkaloid Cytisine, which has an action similar to that of nicotine.

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