Tabex film-coated tablets 1.5 mg 5 blisters of 20 pcs.

Mechanism of action. Cytisine is an alkaloid obtained from the plant Cytisus laburnum.

It has a chemical structure similar to that of nicotine and lobeline. It selectively and competitively binds to receptors, having partial agonist activity towards nicotinic acetylcholine receptors and, in particular, high affinity for the α4β2 subtype. Thus, it prevents the binding of nicotine to α4β2 receptors and the stimulation of the central mesolimbic dopamine system, which is associated with the mechanisms of nicotine addiction, due to the ability of nicotine to activate these receptors.

Pharmacodynamics. The effect of the drug is to disrupt the ganglia of the autonomic nervous system, disrupt reflex breathing, release of adrenaline from the medullary part of the adrenal glands, and increase blood pressure. The mechanism of action of cytisine is close to the mechanism of action of nicotine, but with much less toxicity and a greater therapeutic effect. Cytisine competitively inhibits the interaction of nicotine with the corresponding receptors, which leads to a gradual decrease and disappearance of nicotine dependence.

Pharmacokinetics. Absorption: cytisine is rapidly absorbed from the gastrointestinal tract after oral administration. Plasma С _max – 15.55 ng / ml is achieved within 0.92 hours.

Distribution: There are no data on the extent of distribution in humans.

Biotransformation and excretion: Cytisine is not metabolized in the body. Up to 64% of the administered dose is excreted unchanged in the urine within 24 hours. T _½ is approximately 4 hours. The mean retention time (MRT) of cytisine in the body is approximately 6 hours.

Tabex is prescribed for chronic nicotinism to help quit smoking.

Adults. The drug is used according to the following scheme: from the 1st to the 3rd day – 1 tablet every 2 hours (6 tablets per day). At the same time, gradually reduce the number of cigarettes smoked. If the result is unsatisfactory, the treatment is stopped and can be resumed after 2-3 months. With a positive effect, the therapy is continued according to the following scheme:

• from the 4th to the 12th day – 1 tablet every 2.5 hours (5 tablets per day);
• from the 13th to the 16th day – 1 tablet every 3 hours (4 tablets per day);
• from the 17th to the 20th day – 1 tablet every 5 hours (3 tablets per day);
• from the 21st to the 25th day – 1-2 tablets per day.

The tablets are taken whole, washed down with sufficient liquid.

Final cessation of smoking should occur by the 5th day from the start of treatment. After completion of treatment, the patient should show willpower and not allow himself to smoke a single cigarette.

Duration of treatment – according to the scheme.

Patients over 65 years of age. The drug is not recommended for use in this age group of patients.

Tabex is contraindicated in case of hypersensitivity to the active or any of the excipients of the drug, in acute myocardial infarction, unstable angina, cardiac arrhythmia, recent cerebrovascular disease, atherosclerosis; severe hypertension, during pregnancy and breastfeeding.

The drug is usually well tolerated. Side effects of mild to moderate severity are rare. Most of them appear at the beginning and disappear during treatment. Most often they are associated with quitting smoking and are manifested by dizziness, headache and insomnia.

On the part of the endocrine system: increased sweating, weight loss.

From the nervous system: headache, dizziness, insomnia, drowsiness, increased irritability.

Cardiac: tachycardia, palpitations.

Vascular: slight increase in blood pressure.

Respiratory, thoracic and mediastinal disorders: dyspnea.

On the part of the digestive system: change in taste and appetite, dry mouth, abdominal pain, nausea, constipation, diarrhea, upper abdominal pain, dyspepsia, vomiting.

Musculoskeletal and connective tissue disorders: myalgia.

General disorders and administration site conditions: chest pain.

Tabex should only be used if the patient is serious about quitting smoking. Using the drug and smoking at the same time can lead to increased side effects of nicotine (nicotine intoxication).

There is no sufficient clinical experience with the use of Tabex in patients with ischemic heart disease, heart failure, arterial hypertension, cerebrovascular disease, obliterating arterial diseases, hyperthyroidism, gastric ulcer, diabetes mellitus, renal or hepatic insufficiency. The drug should be prescribed to these categories of patients only after a careful assessment of the benefit/risk ratio by the doctor.

Due to the lack of adequate safety studies, the use of the drug in patients with some forms of schizophrenia, patients with chromaffin tumors of the adrenal glands and gastroesophageal reflux disease is possible only after a careful assessment of the benefit/risk ratio.

There is insufficient clinical experience regarding the safe use of Tabex in children (under 18 years of age) and the elderly (over 65 years of age), therefore its use in these age groups is not recommended.

The use of the drug is contraindicated during pregnancy and breastfeeding.

Children. Do not use in children.

Ability to influence the reaction rate when driving vehicles or working with other mechanisms. The use of the drug Tabex usually does not affect the reaction rate when driving vehicles or working with other mechanisms.

Given that rarely, sensitive patients may experience adverse reactions (drowsiness, dizziness) when using the drug, at the beginning of treatment you should refrain from driving vehicles and working with other mechanisms.

Increased activity of CYP 1A2 is observed in smoking. After cessation of smoking, the activity of this isoenzyme may decrease, which may cause increased plasma concentrations of drugs that are metabolized by CYP 1A2, such as theophylline, ropinirole, clozapine and olanzapine. In these cases, their adverse reactions may increase, since these drugs have a narrow therapeutic range.

With simultaneous use of Tabex with cholinomimetics and anticholinesterase drugs, increased cholinomimetic side effects are possible.

Concomitant use with antihyperlipidemic drugs (statins) increases the risk of myalgia.

Simultaneous use of Tabex with antihypertensive drugs may weaken their effect.

Symptoms: nausea, vomiting, profuse sweating, tremors, visual disturbances, general weakness, tachycardia, clonic convulsions, respiratory paralysis.

Treatment: gastric lavage, if the patient is conscious, infusion of water-salt solutions, use anticonvulsants, cardiotonics, analeptics and other symptomatic agents. Monitor breathing, blood pressure and heart rate.

In the original packaging to protect from moisture, at a temperature not exceeding 25 °C.