Nicotinell - instructions for use, dose, side effects, contraindications

Excipients, maltitol 880 mg, sodium carbonate 10 mg, sodium hydrogen carbonate 20 mg, methyl methacrylate and ethyl acrylate copolymer [1: 2] 50 mg, xanthan gum 40 mg, silicon dioxide colloid 15 mg, levomenthol 3 mg, peppermint leaves 5 mg butter, aspartame 10 mg, magnesium stearate 20 mg.

Each tablet for resorption [mint] 2 mg contains:

Active substance, nicotine bitartrate dihydrate 6.144 mg (corresponding to 2 mg nicotine).

Excipients: maltitol 880 mg, sodium carbonate 10 mg, sodium bicarbonate 20 mg, methyl methacrylate and ethyl acrylate copolymer [1: 2] 50 mg, xanthan gum 40 mg, silicon dioxide colloid 15 mg, levomenthol 9 mg, peppermint leaves 5 mg butter, aspartame 10 mg, magnesium stearate 20 mg.

Description:Round biconvex tablets from white to slightly yellowish color with the smell of mint.

Pharmacotherapeutic group:Means for the treatment of nicotine addiction.

ATX: & nbsp

N.07.B.A Drugs used in nicotine addiction

N.07.B.A.01 Nicotine

Pharmacodynamics:

After a sharp quitting, patients may develop a withdrawal syndrome, which includes: dysphoria, insomnia, increased irritability, anxiety, impaired concentration, reduced heart rate, increased appetite, or weight gain.An important symptom of the syndrome of "withdrawal" is also the desire to smoke. Contained in tablets nicotine replaces part of the nicotine that enters the body during smoking, and reduces the severity of the "withdrawal" syndrome, and also reduces the craving for smoking.

In the treatment of tobacco addiction, nicotine replacement therapy reduces the need for the number of cigarettes smoked, reduces the symptoms of "withdrawal" symptoms that occur with complete quitting from those who choose to quit, facilitates temporary abstinence from smoking, and also helps to reduce the number of smoked cigarettes from those who can not or do not want to completely stop smoking.

Pharmacokinetics:

When placed in the mouth, a resorption tablet [mint] Nicotinell® slowly breaks down during resorption, and dissolves in saliva. Free nicotine then absorbed through the mucosa of the oral cavity and enters the systemic circulation.

Some of the nicotine enters with saliva into the stomach and intestines, where it is inactivated. Due to the effect of the first passage through the liver, the systemic bioavailability of nicotine is low.For this reason, after the use of tablets to resorb [mint] Nicotinell®, there is rarely a similar rapid increase in the concentration of nicotine in the systemic bloodstream, as in smoking.

The volume of distribution after intravenous nicotine intake is approximately 2-3 l / kg, the half-life period is 2 h. Nicotine metabolism occurs mainly in the liver, its average plasma clearance is about 70 l / h. Nicotine also metabolized in the kidney and lung. More than 20 metabolites, which are less active than nicotine. Nicotine penetrates the blood-brain barrier. The connection of nicotine with plasma proteins is less than 5%. In this regard, violations of the binding of nicotine with the simultaneous use of other drugs or changes in plasma protein levels in various diseases should not have a significant effect on the kinetics of nicotine.

The primary metabolite of nicotine in plasma - cotinine - has a half-life of 15-20 hours, and its concentration exceeds that of nicotine by a factor of 10.

Urine is excreted mainly cotinine (15% dose) and trans-3-hydroxy-cotinine (45% dose). From 10% to 30% of the dose of nicotine is excreted in the urine unchanged. Progressive deterioration of kidney function is accompanied by a decrease in overall nicotine clearance.Its pharmacokinetics does not change in patients with cirrhosis of the liver with negligible hepatic impairment (5 on the Child-Pugh scale) and decreases in patients with cirrhosis of the liver with moderate impaired hepatic function (7 on the Child-Pugh scale). Smokers with concomitant chronic renal failure treated with hemodialysis, noted the increase in nicotine concentration in the blood plasma.

In elderly patients there is a slight decrease in total nicotine clearance, which does not require dose adjustment.

Indications:

Treatment of tobacco dependence and alleviation of symptoms arising from quitting smoking, by reducing the need for nicotine in the following cases:

- reducing the symptoms of "lifting" that arise when full smoking cessation in patients who have decided to quit smoking;

- with a temporary cessation of smoking;

- reduction in the number of cigarettes smoked from those who can not or do not want to completely give up smoking.

Nicotinella tablets for resorption [mint] 2 mg are indicated in cases of more pronounced tobacco dependence on the background of quitting smoking.

Contraindications:

Hypersensitivity to nicotine or other components of the drug, severe arrhythmia, arterial hypertension, unstable angina, myocardial infarction and cerebral circulation (recently transferred), phenylketonuria (t.the preparation contains aspartame).

The drug should not be used by non-smokers.

Disinfecting tablets [mint] Nicotinell® should not be used by persons under the age of 18 without appropriate doctor's advice.

Carefully:

The drug should be used only after consultation with a doctor, after assessing the risk / benefit ratio:

- patients with cardiovascular disorders, in particular, suffered serious cardiovascular diseases during the last month (especially, such as stroke, unstable angina, arrhythmia, myocardial infarction, shunting or angioplasty) or with uncontrolled arterial hypertension;

- patients with moderate or severe impairment of liver function, severe renal failure, exacerbation of esophagitis, peptic ulcer of the duodenum and stomach, inflammatory diseases of the oral cavity or larynx;

- patients with cerebrovascular disease;

- patients with intolerance to fructose;

- Nicotine, entering the human body with replacement therapy or smoking, causes the release of catecholamines from the adrenal medulla. In this regard, Nicotinell® should be used with caution in patients with uncontrolled hyperthyroidism, pheochromocytoma, and diabetes mellitus. The use of Nicotinell® is associated with less risk than smoking.

Pregnancy and lactation:

Nicotine enters the body of a pregnant, in any form (cigarettes, drugs, nicotine replacement therapy, etc.) can have a negative effect on the fetus. Nicotine penetrates the placenta and excretes with human milk, and therefore its use may pose a risk to the fetus or the child. Pregnant women are recommended to quit without using nicotine replacement therapy.

In the case of failure of such attempts, the decision to conduct therapy is taken after comparing the possible positive effects for the mother and the potential harm to the fetus, as well as breastfeeding.Pregnant and lactating women are admitted only after consultation with the attending physician.

Lactation

Nicotine is excreted in breast milk in quantities that can have an effect on the newborn. Therefore, in the lactation period, the use of tablets for resorption of [mint] Nicotinell® is not recommended.

The use of tablets for resorption of [mint] Nicotinell® during lactation is carried out only under strict indications and directly under the supervision of the doctor after assessing the risk / benefit ratio. In order to reduce the negative effect of nicotine on the baby, the Nicotinell® drug should be used immediately after feeding.

Dosing and Administration:

Children and teenagers.

The experience of using Nicotinella® in adolescents under the age of 18 is not available, so Nicotinell® should be administered by persons under the age of 18 strictly according to the doctor's prescription.

Adults.

Tablets should be resorbed until completely dissolved - about 30 minutes. During the first days after the beginning of treatment, unpleasant sensations in the oral cavity in the throat may occur. After a while these sensations are invisible.

The initial dose should be selected individually.The optimal dose is selected depending on the severity of nicotine dependence and the number of cigarettes smoked.

Nicotinell® tablets for resorption [mint] 1 mg is recommended for use with an average degree of nicotine dependence, this dosage should not be used in case of pronounced nicotine dependence.

Nicotinell® tablets for resorption [mint] 2 mg is recommended for severe and very strong nicotine addiction, as well as for those who attempted to quit smoking earlier.

The initial dose should be selected individually, depending on the degree of tobacco dependence. Patients with a low degree of dependence treatment should start with 1 tablet Nicotinell® at the reception. Smokers with a higher degree of dependence (Fagerstrom test for nicotine dependence> 6 points, or the number of cigarettes smoked per day exceeds 20) and patients who failed to quit using 1 tablet of 2 mg should begin treatment with a 2- x tablets of 2 mg per reception. At the beginning of the course of treatment, the tablets should be taken every 1-2 hours; 8-12 tablets of 2 mg per day, usually enough.During the day should not take more than 30 tablets of 2 mg.

Full and sharp refusal of smoking:

The duration of therapy is set individually. Usually the course of treatment is at least 3 months. After 3 months of treatment, it is necessary to gradually reduce the daily dose of taking tablets or switch to taking 1 mg tablets, also gradually reducing the number of tablets taken per day.

If a strategy for a complete and abrupt quitting is chosen, then patients should completely stop smoking during treatment with pills for resorption with [mint] Nicotinell®.

It is necessary to dissolve one tablet when there is a need to smoke a cigarette. At the initial stage, one tablet should be resorbed every 1 -2 hours.

If you select tablets for resorption [mint] 1 mg, then the daily dose is usually 8-12 tablets, the maximum daily dose - up to 30 tablets per day.

If you select tablets for resorption [mint] 2 mg, then the daily dose is usually 8-12 tablets, the maximum daily dose - up to 15 tablets per day.

Dosage of the drug must be adjusted in accordance with individual needs, without exceeding the maximum permissible level.

Recommendations for use:

1. The tablet should be rassevat until the appearance of a pronounced taste in the mouth.

2. Then the tablet should be placed between the gum and cheek.

3. If the taste disappears, you should again begin to dissolve the tablet.

4. Such actions should be repeated until the tablet is completely resorbed (about 30 minutes).

Reducing the number of smoked cigarettes to complete quitting in 3 stages:

1. Disinfecting tablets [mint] Nicotinella® should be used to relieve an acute desire to smoke and to extend the intervals between smoking a cigarette in order to minimize the amount of cigarettes smoked. It is necessary to dissolve 1 tablet, when there is a growing desire to smoke a cigarette. If the number of cigarettes smoked per day does not decrease within 6 weeks, you should consult a doctor.

2. Continue to use the drug during nicotine addiction, gradually reducing the number of cigarettes to 0. When the patient feels ready to quit, you should try to completely quit smoking, but no later than 6 months after the start of therapy. If you can not quit smoking within 9 months after starting therapy, you should consult your doctor.

3. When it is possible to completely stop smoking, gradually reduce the amount of taken tablets for resorption. When taking 1-2 tablets a day, you should stop taking the drug.

The patient should try to quit smoking when he is ready for it, but no later than 6 months after the start of treatment. If within 9 months after the beginning of therapy to quit smoking failed, you should consult a specialist.

It is not recommended to take the medication regularly for more than 12 months. Some people who manage to quit smoking may need a longer time to take the drug in order to minimize the risk of resumption of smoking. After the end of the course of treatment, however, it is desirable for the patient to have several tablets, because at any time there may be a spontaneous desire to smoke. Simultaneous medical counseling and psychological support usually improve the effectiveness of therapy.

Temporary cessation of smoking:

Tablets can be used in periods when you need to temporarily give up smoking, for example, when you are in places where smoking is prohibited, or in other situations when you need to refrain from smoking.

In the case of forced intermittent smoking cessation, one tablet should be taken to dissolve [mint] Nicotinell when a strong need to smoke occurs.

For a dosage of 1 mg: should dissolve about 8-12 tablets a day, but not more than 30 tablets a day.

For a dosage of 2 mg: should dissolve about 8-12 tablets a day, but not more than 15 tablets a day.

Do not exceed the indicated dose!

Side effects:

Undesirable reactions when taking tablets for resorption of [mint] Nicotinella are similar to those when taking nicotine in other dosage forms and are dose-dependent. Most adverse reactions occur in patients on 3-4 week of treatment with the drug.

Side effects that do not depend on the dose: hypersensitivity, angioedema and anaphylactic reactions.

Dizziness, headache, insomnia, may be manifestations of the "cancellation" syndrome caused by the refusal of smoking. If you quit smoking, the incidence of aphthous stomatitis may increase. Nicotinecontained in the resorption tablets can sometimes cause mild irritation of the mouth and throat and increase salivation at the beginning of treatment.Excessive ingestion of nicotine released into saliva may initially cause hiccups. Sometimes there are cases of indigestion or heartburn, in such cases, a slower resorption of tablets can reduce discomfort.

The relationship of these phenomena with the use of the drug Nicotinell® is not obvious.

Classification of incidence of adverse reactions:

very often (> = 1/10); often (> = 1/100, <1/10); infrequently (> = 1/1000, <1/100); rarely (> = 1/10000, <1/1000); very rarely (<1/10000), including individual messages.

From the central nervous system:

Often: dizziness, headache.

From the gastrointestinal tract:

Often: gastrointestinal discomfort, nausea, flatulence, gastritis, dry mouth, stomatitis and esophagitis.

From the respiratory system:

Often: cough, rhinitis.

From the side of the cardiovascular system:

Often: heart palpitations.

Rarely: atrial fibrillation.

Very rarely: arrhythmia.

Others:

Often: sore throat, irritation of the oral mucosa, dryness in the throat.

From the immune system:

Very rarely: hypersensitivity, angioedema and anaphylactic reactions.

Certain symptoms (dizziness,headache and insomnia) may be associated with withdrawal syndrome due to quitting and, consequently, insufficient intake of nicotine in the body.

Overdose:

Excessive intake of nicotine with substitution therapy and / or smoking can cause symptoms of overdose.

Overdose Symptoms are similar to those in acute nicotine poisoning and include nausea, increased salivation, abdominal pain, diarrhea, hyperhidrosis, headache, dizziness, hearing impairment and severe weakness. When applying high doses of nicotine, arterial hypotension, a weak and irregular pulse, shortness of breath, vascular collapse, coma and generalized convulsions can be noted.

Treatment.

First aid - reception of activated carbon, gastric lavage for 1 hour after poisoning, if necessary, inpatient treatment with symptomatic therapy.

Nicotine in doses carried by adult smokers, is dangerous for children, because it causes symptoms of poisoning right up to a lethal outcome. In case of an accidental overdose of nicotine, a child needs emergency medical assistance.

Interaction:

There are no data on the interactions of tablets for resorption of [mint] Nicotinell® with other drugs.

Smoking (but not nicotine) leads to an increase in the activity of the enzyme CYT1A2. Thus, a complete cessation of smoking can lead to a decrease in clearance for a given enzyme, which in turn causes an increase in plasma concentrations of narrow-spectrum drugs, such as theophylline, Tacrine, clozapine and ropinirole.

Plasma concentrations of other active substances subject to metabolism involving cytochrome CYT1A2, such as caffeine, paracetamol, phenazone, phenylbutazone, pentazocine, lidocaine, benzodiazepines, warfarin, estrogens and vitamin B12 can also increase. However, the clinical significance of this effect on the effect of these active substances has not yet been established.

Smoking can reduce the analgesic effect of propoxyphene, reduce the diuretic effect of furosemide, weaken the effect of propranolol on blood pressure and heart rate, and lead to a slower cicatrization of the ulcer when using H₂antagonists.

Under the influence of smoking and the introduction of nicotine, the levels of yortysol and catecholamines in the blood can increase; this can lead to a decrease in the effect of taking nifedipine or adrenergic receptor antagonists and increasing the effect of adrenoreceptor agonists.

As a result of an increase in the level of subcutaneous absorption of insulin that occurs after smoking cessation, patients may need to reduce the dose of insulin.

Special instructions:

Nicotinell® tablets for resorption [mint] do not contain sugar.

Patients with diabetes after smoking cessation may need to lower their insulin doses.

In each Nicotinell tablet® is contained aspartame, the source of phenylalanine formation, its content corresponds to 5 mg / dose and can harm the health of patients with phenylketonuria.

Since Nicotinell® tablets contain maltitol, a source of fructose, patients with a rare hereditary disease associated with impaired fructose tolerance should not use this drug. Due to the presence of maltitol, some patients may have mild laxative effect. One tablet for resorption [mint] Nicotinell® 1 mg or 2 mg contains 9.8 mg of sodium.

The concomitant intake of acid-containing beverages (eg, coffee) can affect the absorption rate of nicotine, so refrain from taking acidic beverages for 15 minutes before using resorption tablets.

If the medicine has become unusable or the expiration date has expired, do not throw it into sewage or into the street! Place the drug in a bag and put it in the trash. These measures will help protect the environment.

Effect on the ability to drive transp. cf. and fur:

When using Nicotinella® in accordance with the recommendations, there is no effect on the ability to drive or operate machinery. However, it must be remembered that the need for smoking can cause changes in behavior.

Form release / dosage:

Nicotinell® tablets for resorption [mint] 1 mg, 2 mg. For 12 tablets in a blister of combined material (PVC / PE / PVDC / PE / TEX) and aluminum foil. One, three or eight blisters together with the instruction for use are placed in a cardboard pack.

Packaging:(12) - blisters (1) - packs cardboard
(12) - blisters (3) - packs cardboard
(12) - blisters (8) - packs cardboard

Storage conditions:

Store at a temperature of no higher than 25 ° C in the original packaging. Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiry date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-002738

Date of registration:02.12.2014

The owner of the registration certificate:Новартис Консьюмер Хелс САНовартис Консьюмер Хелс СА Switzerland

Manufacturer: & nbsp

SwissCo Servises, AG Switzerland

Representation: & nbspNOVARTIS CONSUMER HELS S.A. (part of Novartis groups) NOVARTIS CONSUMER HELS S.A. (part of Novartis groups) Switzerland

Information update date: & nbsp09.08.2015

Illustrated instructions

Instructions

Nicotinell® (Nicotinell®)