Stopadix^® (Tablets) Instructions for Use

Marketing Authorization Holder

Promomed Rus LLC (Russia)

Manufactured By

Biokhimik, JSC (Russia)

ATC Code

N07BA (Drugs used for nicotine dependence)

Active Substance

Cytisine (Grouping Name)

Dosage Form

Stopadix®

Film-coated tablets, 1.5 mg: 50 or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets light brown in color, round, biconvex; on the cross-section, the core is white or almost white.

Excipients: lactose monohydrate – 28 mg, microcrystalline cellulose – 67.5 mg, talc – 2 mg, magnesium stearate – 1 mg.

Film coating composition Opadry^® II 85F26948 brown – 3 mg (partially hydrolyzed polyvinyl alcohol – 40%, titanium dioxide – 21.8%, macrogol 4000 – 20.2%, talc – 14.8%, iron oxide yellow (E172) – 2.1%, iron oxide red (E172) – 0.6%, iron oxide black (E172) – 0.5%).

10 pcs. – blister packs (5) – cardboard box.
20 pcs. – blister packs (5) – cardboard box.
100 pcs. – jars – cardboard packs.

Clinical-Pharmacological Group

Drug for the treatment of nicotine dependence

Pharmacotherapeutic Group

Other agents for the treatment of nervous system diseases; agents used for addictive disorders; agents used for nicotine dependence

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, cytisine has much lower toxicity and a greater therapeutic index.

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

Pharmacokinetics

After oral administration, cytisine 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.

Cytisine 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 retention 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. The single dose is 1.5 mg (one tablet).

Begin treatment only when you have a firm intention to quit smoking.

From day 1 to day 3, take one tablet every 2 hours (6 times daily).

From day 4 to day 12, take one tablet every 2.5 hours (5 times daily).

From day 13 to day 16, take one tablet every 3 hours (4 times daily).

From day 17 to day 20, take one tablet every 4-5 hours (3 times daily).

From day 21 to the end of the course (day 25), take one tablet every 6-8 hours (1-2 times daily).

If the urge to smoke is not reduced by the 5th day of treatment, discontinue therapy and attempt a new course after 2-3 months.

If smoking cessation is successful before the end of the course, you may stop taking the drug.

Do not exceed the recommended dosage. Continue smoking during the initial treatment phase, but gradually reduce the number of cigarettes smoked.

If smoking is resumed after a period of abstinence, repeat the course immediately.

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 obliterating 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 insufficiency.

Use in Renal Impairment

Use with caution in renal insufficiency.

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 cytisine 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 the 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.

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

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

Concomitant 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.