Tabex^® (Cytisine) Instruction

International Non-Proprietary Name (INN): cytisine
Dosage form: tablets
Structure
In 1 tablet:
Active ingredient: cytisine 1.5 mg;
Excipients: lactose monohydrate, microcrystalline cellulose, talc, magnesium stearate;
Composition of the film shell: opadry II brown (hypromellose, lactose monohydrate, titanium dioxide (E171), macrogol 3000, triacetin, iron dye yellow oxide (E172), iron dye red oxide (E172), iron dye black oxide (E172)).
Description
Round biconvex film-coated tablets of light brown color.
Pharmacological classification: drugs used in addictive disorders, drugs used in nicotine dependence
ATC code: N07BA04
Pharmacological action: drugs used in addictive disorders, drugs used in nicotine dependence

Pharmacodynamics

Cytisine is an agonist of the choline receptors in the vegetative ganglia and belongs to the group of gangliostimulating drugs. Tabex^® excites the nicotine-sensitive choline receptors of the postsynaptic membranes in the vegetative ganglia, chromaffin cells in the molecular part of the suprarenal gland and sinocarotid reflexogenic zone, which results in excitation of the respiratory center, predominantly through the reflexes, simulation of adrenaline release by the medullar part of the suprarenal glands and a rise in the blood pressure. After its absorption in the gastrointestinal tract, cytisine plays the part of a nicotine-substitute substance which decreases the period of interaction between nicotine and the corresponding receptors. This in turn leads to a gradual decrease and interruption of the smokers’ psychic and physical nicotine dependence.

Intended uses

Tabex^® is a drug of choice for the treatment of chronic nicotinism. It is particularly appropriate for the treatment of risk groups of smokers with health problems on the part of the cardiovascular and respiratory systems, as well as smokers professionally subjected to tension and stress that are predisposed to seek a “false comfort” in nicotine or other drugs causing dependence.

Contraindications

Advanced atherosclerosis, some forms of schizophrenia, pheochromocytoma, conditions connected with severe impairment of the cardiovascular system and malignant hypertension.

Dosage and administration

The drug is administered perorally according to the following schedule:

First 3 days: 1 tablet 6 times daily (every 2 hours) with a parallel reduction of the number of cigarettes smoked. If the result is unsatisfactory, the treatment is discontinued and a new therapy can be resumed after 2-3 months.

In case of good effect, the treatment should continue according to the following schedule:
from the 4th to the 12th day – 1 tablet every 2.5 hours (5 tablets daily);
from the 13th to the 16th day – 1 tablet every 3 hours (4 tablets daily);
from the 21st to the 25th day – 1-2 tablets daily.

Complete discontinuation of smoking must occur by the 5th day of treatment.

Precaution

The drug should be administered carefully to patients with exacerbated peptic ulcer. After completing the treatment course, the patients should refrain from smoking even one cigarette, in order to obtain a lasting effect.

Side effects

The high doses may provoke nausea, vomiting, dizziness, tachycardia, and muscle weakness. These effects pass quickly after the dose is decreased.

Overdose

Symptoms of nicotine intoxication are observed in Tabex^® overdose. The toxic effects are manifested in nausea, vomiting, pupil dilation, tachycardia, general weakness, clonic convulsions, paralysis of respiration. The communications of overdose with the drug are scarce. Lavage of the stomach, monitoring of respiration, arterial pressure, and heart rate are initiated as in all cases of overdose. Infusion, reanimation is undertaken with saline and glucose solutions, anticonvulsants, cardiotonics, analeptics, etc. symptomatic agents.

Pregnancy and lactation

The intraovular application of cytisine substance to hen embryos induced no embriotoxic and teratogenic effect within the limits of the single therapeutic doses. Higher doses of the drug lead to embryotoxic action. On the basis of the experimental data obtained, Tabex^® is recommended (with cytisine as the basic component) not to be taken by pregnant women, due to the potential risk of embryotoxic action in case of uncontrolled administration. The drug should not be administered during breastfeeding.

Interaction with other drugs

The analeptic effect of cytisine decreases during combined therapy with antituberculosis drugs (PASA, streptomycin, etc.).

Manufacturer

Sopharma, Bulgaria. https://www.sopharmagroup.com/