Tabenova (Tablets) Instructions for Use

Marketing Authorization Holder

Pharmacor Production, LLC (Russia)

ATC Code

N07BA04 (Cytisinum)

Active Substance

Cytisinum (Grouping Name)

Dosage Form

Tabenova

Film-coated tablets, 1.5 mg: 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets brown in color, round, biconvex; the cross-section is white to white with a slightly yellowish tint.

Excipients: microcrystalline cellulose, lactose monohydrate, talc, magnesium stearate.

Film coating composition: Opadry II 85F265103 brown (partially hydrolyzed polyvinyl alcohol – 40%, macrogol/polyethylene glycol – 20.2%, talc – 14.8%, titanium dioxide (E171) – 14.65%, iron oxide yellow (E172) – 7.46%, iron oxide red (E172) – 1.89%, iron oxide black (E172) – 1%).

10 pcs. – blister packs (10) – cardboard boxes.
20 pcs. – blister packs (5) – cardboard boxes.
25 pcs. – blister packs (4) – cardboard boxes.
50 pcs. – blister packs (2) – cardboard boxes.

Clinical-Pharmacological Group

Drug for the treatment of nicotine dependence

Pharmacotherapeutic Group

Nicotine dependence treatment

Pharmacological Action

N-cholinomimetic. It stimulates the ganglia of the autonomic nervous system, reflexively stimulates respiration, causes the release of adrenaline from the adrenal medulla, and increases blood pressure.

Despite a close similarity to the mechanism of action of nicotine, Cytisinum possesses significantly lower toxicity and a greater therapeutic index.

Cytisinum competitively suppresses the interaction of nicotine with the corresponding receptors, which leads to a gradual reduction and disappearance of nicotine (tobacco) dependence.

Pharmacokinetics

After oral administration, Cytisinum is rapidly absorbed from the gastrointestinal tract.

The C_max of the active substance in blood plasma is 15.55 ng/ml and is achieved within 0.92 hours.

In mice, high plasma concentrations of cytisine after oral and intravenous administration are found in the liver, kidneys, and adrenal glands.

The V_d in rabbits after oral and intravenous administration is 6.21 l/kg and 1.02 l/kg, respectively.

Cytisinum is not metabolized in the body.

Up to 64% of the dose is excreted unchanged in the urine within 24 hours.

The T_1/2 is approximately 4 hours.

The mean residence time ( MRT) of cytisine in the body is approximately 6 hours.

Indications

Treatment of nicotine dependence (to facilitate smoking cessation).

ICD codes

Dosage Regimen

Take orally according to the following schedule. A single dose is 1.5 mg (one tablet).

Initiate treatment only after setting a target quit date. Completely stop smoking upon starting the regimen.

Days 1 to 3: Take 1 tablet every 2 hours (6 times daily). Do not exceed 6 tablets per day.

Days 4 to 12: Take 1 tablet every 2.5 hours (5 times daily). Do not exceed 5 tablets per day.

Days 13 to 16: Take 1 tablet every 3 hours (4 times daily). Do not exceed 4 tablets per day.

Days 17 to 20: Take 1 tablet every 4-5 hours (3 times daily). Do not exceed 3 tablets per day.

Days 21 to 25: Take 1-2 tablets daily. Space doses evenly throughout the day.

If the urge to smoke is not relieved, shorten the interval between tablets to a minimum of 1 hour.

The total treatment course is 25 days. If smoking cessation is not achieved, repeat the course after a several-month interval.

Do not exceed the recommended daily dosage. Treatment duration should not exceed the specified period.

Adverse Reactions

Metabolism and nutrition disorders: weight loss, increased sweating.

Nervous system disorders: headache, dizziness, insomnia or drowsiness, increased irritability.

Cardiac disorders: tachycardia, palpitations.

Vascular disorders: slight increase in blood pressure.

Respiratory, thoracic and mediastinal disorders: shortness of breath.

Gastrointestinal disorders: dry mouth, nausea, abdominal pain, constipation, diarrhea, changes in taste and appetite.

Musculoskeletal and connective tissue disorders: muscle pain.

General disorders and administration site conditions: chest pain.

Contraindications

Hypersensitivity to cytisine; acute myocardial infarction; unstable angina; cardiac arrhythmia; recent stroke (within 1 month prior to initiation of use); atherosclerosis; severe arterial hypertension; pregnancy, breastfeeding period; age under 18 years, patients over 65 years of age.

With caution

In the following forms of coronary artery disease: stable angina, asymptomatic (silent) myocardial ischemia, vasospastic angina, syndrome “X” (microvascular angina); in heart failure; in elevated blood pressure; in cerebrovascular diseases; in obliterative arterial diseases; in hyperthyroidism; in gastric ulcer disease; in diabetes mellitus; in renal failure; in hepatic failure; in some forms of schizophrenia; in the presence of pheochromocytoma of the adrenal glands; in GERD; patients with a long history of smoking and persons over 40-45 years of age.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

Use with caution in hepatic failure.

Use in Renal Impairment

Use with caution in renal failure.

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Contraindicated for use in elderly patients over 65 years of age.

Special Precautions

Administration of cytisine should be started only when the patient has a serious intention to quit smoking.

Persons with a long history of smoking and persons over 40-45 years of age should use Cytisinum only after consulting a doctor.

Do not exceed the recommended doses. Treatment with cytisine and continued smoking may lead to an increase in the side effects of nicotine (nicotine intoxication).

Effect on ability to drive vehicles and operate machinery

Due to the possible occurrence of drowsiness and other adverse reactions, caution should be exercised in the listed situations.

Drug Interactions

After smoking cessation, the side effects of theophylline, ropinirole, clozapine, and olanzapine may be enhanced.

With simultaneous use with acetylcholine, carbachol, galantamine, pyridostigmine, rivastigmine, distigmine, an enhancement of the cholinomimetic side effect is possible (salivation, lacrimation, bronchial secretion with cough and risk of an asthma attack, miosis, colic, nausea, vomiting, frequent urination, increased muscle tone or sudden muscle contractions).

Concomitant use with lovastatin, simvastatin, fluvastatin, pravastatin increases the risk of muscle pain.

Simultaneous use of cytisine with antihypertensive agents (including propranolol) may weaken their effect.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Over-the-Counter

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.