Nicozam, tablets 1.5mg

Package Insert for the Medicinal Product Nicozam

Registration Number: LP-007262

Brand Name: Nicozam 

International Nonproprietary Name (INN): Cytisine 

Dosage Form: Film-coated tablets 

Composition per one tablet:

Active substance: Cytisine – 1.50 mg;

Excipients: Lactose monohydrate – 52.30 mg, Pregelatinized corn starch – 15.00 mg, Povidone K-17 – 2.4 mg, Talc – 2.00 mg, Magnesium stearate – 1.00 mg, Microcrystalline cellulose – to obtain a core tablet weighing 100.00 mg;

Excipients for the coating: Film Coating Mixture "Opadry® II 85F26948 Brown" [Polyvinyl alcohol – 40.00 %, Titanium dioxide – 21.81 %, Macrogol (PEG) – 20.20 %, Talc – 14.80 %, Iron oxide yellow – 2.06 %, Iron oxide red – 0.61 %, Iron oxide black – 0.52 %] – to obtain a coated tablet weighing – 106.00 mg.

Description: 

Round, biconvex, light brown film-coated tablets. The core in cross-section is white to light brown.

Pharmacotherapeutic Group: Medicinal products for the treatment of nicotine dependence.

ATC Code: [N07BA04]

Pharmacological Properties

Pharmacodynamics

The alkaloid cytisine is the active substance of the drug and has an n-cholinomimetic effect. Its effects are as follows: it excites 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 mechanism of action closely similar to nicotine, cytisine has significantly lower toxicity and a greater therapeutic index. Cytisine competitively inhibits the interaction of nicotine with corresponding receptors, leading to a gradual reduction and eventual disappearance of nicotine (tobacco) dependence.

Pharmacokinetics

The pharmacokinetic parameters of cytisine were studied in 36 healthy volunteers after oral administration of a single 1.5 mg dose (one tablet of the drug).

Absorption

Cytisine is rapidly absorbed from the gastrointestinal tract after oral administration. The maximum plasma concentration of the drug is 15.55 ng/ml and is achieved within 0.92 hours.

Distribution

Clinical data on the distribution of the drug in humans are not available.

In mice, high plasma concentrations of cytisine after oral and intravenous administration are established in the liver, kidneys, and adrenal glands. The volume of distribution (Vd) in rabbits after oral and intravenous administration is 6.21 L/kg and 1.02 L/kg, respectively.

Biotransformation and Elimination

Cytisine is not metabolized in the body. Up to 64% of the administered dose is excreted unchanged in the urine within 24 hours. The elimination half-life is approximately 4 hours. The mean residence time (MRT) of cytisine in the body is approximately 6 hours.

Indications for Use

Treatment of tobacco dependence (to facilitate smoking cessation).

Physical and psychological dependence on nicotine is considered a specific type of disease that leads to an inability to refrain from smoking, even while understanding its negative effects.

Contraindications

Hypersensitivity to the active substance or any of the excipients of the drug, acute myocardial infarction, unstable angina, cardiac arrhythmia, recent stroke (within 1 month prior to starting the drug), atherosclerosis, severe arterial hypertension, pregnancy and breastfeeding, age under 18 years and patients over 65 years of age, lactase deficiency, galactosemia, glucose-galactose malabsorption syndrome (the drug contains lactose).

Use with Caution

The drug should be used with caution in other forms of coronary artery disease (stable angina, silent myocardial ischemia, vasospastic angina, syndrome X (microvascular angina)), in heart failure, elevated blood pressure, cerebrovascular diseases, obliterative arterial diseases, hyperthyroidism, gastric ulcer, diabetes mellitus, renal or hepatic insufficiency, in some forms of schizophrenia, in the presence of pheochromocytoma of the adrenal glands, gastroesophageal reflux disease, individuals with a long history of smoking and individuals over 40-45 years of age (see "Special Instructions" section).

Use of the drug in patients with the conditions listed in the "Use with Caution" section is possible only after consultation with a physician.

Use during Pregnancy and Breastfeeding

The drug should not be used by women during pregnancy and breastfeeding.

Dosage and Administration

The tablets are taken orally, whole, with a sufficient amount of fluid. Do not exceed the recommended doses.

It is advisable to start taking the medication after the patient has committed to complete smoking cessation.

The medication should be used according to the following schedule: from Day 1 to Day 3 – 1 tablet 6 times a day, every 2 hours, while gradually reducing the number of cigarettes smoked. The tablet should be taken between smoking episodes to lengthen the intervals between cigarettes and minimize their consumption. The 2-hour dosing interval must be observed.

If a reduction in daily cigarette consumption cannot be achieved, treatment should be discontinued. It can be restarted after 2-3 months.

If the effect is good, continue treatment according to the following schedule:

from Day 4 to Day 12 – 1 tablet 5 times a day, every 2.5 hours;

from Day 13 to Day 16 – 1 tablet 4 times a day, every 3 hours;

from Day 17 to Day 20 – 1 tablet 3 times a day, every 5 hours;

from Day 21 to Day 25 – 1-2 tablets per day.

It is strongly recommended to quit smoking no later than the 5th day of treatment.

Combining medication therapy with counseling, including psychological support measures for the patient, significantly increases treatment effectiveness.

Adverse Reactions

Clinical trial data show good tolerability of the drug. The observed adverse reactions are mild or moderate. Most of them occur at the beginning of treatment and resolve on their own. Most often they are associated with smoking cessation and manifest as dizziness, headache, and insomnia.

At recommended doses, the drug does not cause serious adverse effects.

The following adverse reactions are possible:

Cardiovascular system: Tachycardia, slight increase in blood pressure, palpitations;

Nervous system: Headache, dizziness, insomnia or drowsiness, increased irritability;

Respiratory system: Shortness of breath;

Gastrointestinal tract: Dry mouth, nausea, abdominal pain, constipation, diarrhea, changes in taste and appetite;

Musculoskeletal and connective tissue: Muscle pain;

Metabolism and nutrition: Weight loss, increased sweating;

Other: Chest pain.

Overdose

Symptoms of Overdose: Nausea, vomiting, dilated pupils, general weakness, tachycardia, clonic convulsions, respiratory paralysis.

Symptoms of overdose occur if the patient does not follow the dosage regimen and takes the drug in doses several times higher than the therapeutic ones.

In case of overdose, it is necessary to consult a doctor immediately!

Treatment: Administration of activated charcoal, gastric lavage, infusion of saline solutions, as well as 5% or 10% glucose solution, anticonvulsants, cardiotonic agents, respiratory analeptics, and other symptomatic treatments. Respiratory function, blood pressure, and heart rate should be monitored.

Drug Interactions

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

Concurrent use of cytisine with acetylcholine, carbachol, galantamine, pyridostigmine, rivastigmine, distigmine may enhance cholinomimetic side effects (salivation, lacrimation, bronchial secretion with cough and risk of asthma attack, pupil constriction, colic, nausea, vomiting, frequent urination, increased muscle tone or sudden muscle contractions).

The use of cytisine concurrently with lovastatin, simvastatin, fluvastatin, pravastatin, etc., increases the risk of muscle pain.

Concurrent use of cytisine with antihypertensive agents (propranolol, etc.) may weaken their effect.

Special Instructions

Treatment with the drug should only be started when the patient has a serious intention to quit smoking.

Individuals with a long history of smoking and individuals over 40-45 years of age should use the drug only after consultation with a physician.

If you miss a dose, take it as soon as possible. If it is time for the next dose, take it as usual. Do not take a double dose to make up for a missed one. Continue taking the drug according to the schedule described in this instruction.

The recommended doses should not be exceeded during drug use.

Treatment with the drug and continued smoking may lead to an enhancement of nicotine's side effects (nicotine intoxication).

The medicinal product contains the excipient lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency, or glucose-galactose malabsorption should not take this medicinal product.

Effects on Ability to Drive and Use Machines

Although no negative influence on the ability to drive vehicles or operate machinery was observed during the use of the drug, caution should be exercised in these situations due to the possible occurrence of drowsiness and other adverse reactions.

Packaging

Film-coated tablets, 1.5 mg.

10 or 20 tablets in a blister strip made of polyvinyl chloride (PVC) or polyvinyl chloride/polyvinylidene chloride (PVC/PVDC) and printed, lacquered aluminum foil.

100 tablets in a polypropylene polymer jar with a low-density polyethylene snap-on lid featuring a first-opening control and a desiccant insert, OR in a low-density polyethylene polymer jar with a polypropylene screw cap featuring a first-opening control and a desiccant insert.

A self-adhesive label is affixed to the jar.

One jar, OR 10 blister packs of 10 tablets, OR 5 blister packs of 20 tablets, along with the package insert, are placed into a cardboard carton for consumer packaging or equivalent quality packaging.

Shelf Life

2 years.

Do not use after the expiration date printed on the packaging.

Storage Conditions

In the original packaging (carton) at a temperature not exceeding 25 °C.

Keep out of reach of children.

Prescription Status

Available without a prescription.

Marketing Authorization Holder / Consumer Claims Organization:

JSC "AVVA RUS", Russia, 121614,

Moscow, ul. Krylatskie Kholmy, 30, building 9.

Tel.: +7 (495) 956-75-54.

avva-rus.ru

Manufacturer:

JSC "AVVA RUS",

Kirov region, Kirov, ul. Luganskaya, 53A.

Tel.: +7 (8332) 25-12-29; +7 (495) 956-75-54.