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

triglycerides (average chain length) 18.27 mg / 27.41 mg / 45.68 mg, copolymer of basic butyl methacrylate 14.58 mg / 21.87 mg / 36.45 mg, polyethylene terephthalate film, 19 pm (on the one hand, it may be lacquered) - the carrier of the layer containing the active substance Acrylate base:

acrylic adhesive solution 123.84 mg / 185.76 mg / 309.60 mg, potassium hydroxide 0.70 mg / 1.05 mg / 1.80 mg, croscarmellose sodium 5.00 mg / 7.49 mg / 12.50 mg, aluminum acetylacetonate 0.06 mg / 0.09 mg / 0.12 mg, polyethylene terephthalate film 100 rm, aluminized on one side and siliconized on both sides - the carrier, performs the function of protecting the adhesive layer (removable substrate), discarded before use.

Description:

The patch is rectangular with rounded corners, translucent, beige in color, on a rectangular aluminized and siliconized detachable substrate.

10 mg / 16 h with an area of 9 cm²+2 %, 27.7x33.2 mm

15 mg / 16 h with an area of 13.5 cm² ±2 %, 33.2x41.3 mm

25 mg / 16 h with an area of 22.5 cm² ±2 %, 43x53 mm

Pharmacotherapeutic group:treatment for nicotine addiction

ATX: & nbsp

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

N.07.B.A.01 Nicotine

Pharmacodynamics:

After a sharp quitting in patients who used tobacco products for a long time, a "cancellation" syndrome may develop, which includes: dysphoria, insomnia, increased irritability, anxiety, impaired concentration, decreased heart rate, increased appetite, or weight gain.An important symptom of the syndrome of "withdrawal" is also the desire to smoke.

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

Pharmacokinetics:

In the therapeutic range (10-25 mg / 16 hours), the relationship between the concentration of nicotine in the blood plasma and its dose is linear. Below are the values of maximum concentrations of nicotine (C_max ) when using different doses.

Dose of nicotine (mg / 16 hours)	Сmах (НГ / МЛ)
10	10
15	15,5
25	26,5

The maximum nicotine plasma concentrations calculated according to the model correspond to the measured values: 11 ng / ml for the transdermal patch 10 mg and 25 ng / ml for 25 mg. The value of the maximum concentration in blood plasma obtained by interpolation with the use of the transdermal patch 15 mg was 16 ng / ml.

Time to reach the maximum concentration in the blood plasma (t_max) is approximately 9 hours and is created in the afternoon or evening, when the risk of recurrence is maximal.

The volume of nicotine distribution is approximately 2-3 l / kg, its half-life is about 3 hours. Nicotine mainly excreted by the liver; the average plasma clearance is about 70 l / h. Nicotine also metabolized in the kidneys and lungs. More than 20 metabolites nicotine, the activity of which is inferior to the activity of the starting substance.

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 the content of plasma proteins for various diseases should not have a significant effect on the kinetics of nicotine.

The main metabolite of nicotine, cotunine, has a half-life of 15-20 hours and is found in blood plasma at a concentration 10 times greater than that of nicotine.

The main nicotine metabolites excreted in the urine are cotonine (12% of the administered dose) and trans-3-hydroxy-cotinine (37 % of the administered dose).

Approximately 10% of nicotine is excreted in the urine unchanged.Progression of renal failure may be accompanied by a decrease in overall nicotine clearance. In smokers with concomitant chronic renal failure who received hemodialysis treatment, an increase in the concentration of nicotine in the blood plasma was observed.

The pharmacokinetics of nicotine for mild hepatic insufficiency (Class A according to the Child-Pugh classification) does not change, with a moderate degree of hepatic insufficiency (class B according to Child-Pugh classification) nicotine clearance decreases.

A slight decrease in total nicotine clearance was noted in healthy elderly patients, which, however, does not require correction of its dose.

The concentration of nicotine in the blood plasma increases with the use of three types of transdermal patches in proportion to the dose.

Indications:

To treat tobacco dependence by reducing the need for nicotine, removing the symptoms of "cancellation" arising from quitting smoking in patients with appropriate motivation.

Contraindications:Hypersensitivity to nicotine or other components of the drug.

Carefully:

Patients who make up a cardiovascular risk group (who have had serious cardiovascular disease, hospitalization for cardiovascular disorders, such as stroke, myocardial infarction, unstable angina, cardiac arrhythmia, coronary artery bypass or angioplasty, for the 4 preceding weeks or uncontrolled arterial hypertension) should only be administered with Nicorette® after consultation with a physician.

The drug should be used with caution in patients with severe or moderate hepatic impairment, severe renal failure, as well as peptic ulcer of the stomach or duodenum in the acute stage. At the same time, the risk of nicotine replacement therapy should be correlated with the risk of continued smoking.

Nicotine, both released from substitution therapy, and absorbed by smoking, stimulates the release of catecholamines from the adrenal medulla. Therefore, the drug should be used with caution in patients with uncontrolled hyperthyroidism and pheochromocytoma.

Patients with diabetes may need to reduce their insulin dose after quitting.

Pregnancy and lactation:

Nicotine penetrates the placenta and affects the number of respiratory movements and hemocirculation in the fetus (the latter effect is dose-dependent). Smoking can have a serious adverse effect on the fetus and the newborn, and should therefore be discontinued. The use of the Nicorrette patch during pregnancy or during lactation is only possible after consultation with a doctor. The risk to the fetus when using Nicorette® is not fully understood. However, the benefits of nicotine replacement therapy in pregnant women who can not quit without such treatment significantly exceed the risk of continued smoking.

Nicotine penetrates into breast milk in small amounts and can adversely affect a child even when used in therapeutic doses.

Dosing and Administration:

Adults and Seniors

The patch is superimposed on undamaged skin immediately after

waking in the morning and removed before sleep. Treatment with this drug

simulates fluctuations in concentration nicotine during the day at the smoker; at

during the sleep of nicotine in the body does not occur. Application

transdermal nicotine patch in the course of the day does not cause violations,

observed when nicotine enters the body during sleep.

To heavy smokers (more than 20 cigarettes a day) it is recommended to start with 1 stage of therapy, applying 1 plaster 25 mg / 16 hours, daily, for 8 weeks.

Then start a gradual decrease in the dose of the drug: 1 patch 15 mg / 16 hours, daily, for 2 weeks, and then - 1 plaster 10 mg / 16 hours, daily, for 2 weeks.

Unnumbered smokers (10-20 cigarettes per day) are recommended to begin therapy with

2 stage (15 mg) for 8 weeks, then - reduce the dose to 3 stages (10 mg) for completing 4 weeks.

Inveterate smokers

Unplanned

smokers

Mode

dosage

the

Length

the

First 8 weeks

Mode

Tsozirova

the

Length

the

Stage

Nikore

tte plate 25 mg

Stage

Nikore

tte plate 15 mg

The next 2 weeks

Stage

Nikore

tte plate 15 mg

The first 8 weeks

Stage

Nikore

tte plate 10 mg

The last 2 weeks

Stage

Nikore

tte plas gyr 10 mg

After 4 weeks

In most cases, the use of a transdermal patch for more than 6 months is not recommended. However, some people may need longer therapy to not resume smoking.

How to apply a transdermal patch

Patch Nicorette® must

apply on a dry, clean, undamaged skin that does not contain hair, for example, the thigh, upper limb or chest. You need to change the location of the overlay every day: do not use the same area for the next two days.

1. Wash hands thoroughly before applying the patch.

2. Cut the packaging plaster scissors along the edge, as indicated on it. Choose a clean, dry area of the skin that does not contain hair (for example, the thigh, upper limb or chest).

Remove one half of the silvery aluminized protective film, not

while touching the adhesive surface of the patch.

4. Strengthen the freed from the protective

film the patch portion on the skin and remove the remaining half of the silvery aluminized

protective film.

5. Firmly press the patch to the skin with the palm or fingertips.

6. Slide your finger along the edge of the patch, making sure that it is tightly glued.

In combination with a chewing gum

The Nicorrette® patch can also be used in conjunction with the Nicorete® chewing gum with a dosage of 2 mg in those situations where, with the use of a patch human continues to

periodically feel irresistible urge to smoke, or if you can not quit using only chewing gums or just a band-aid. In combination with the Nicorrette® patch, the Nicorent® chewing gum with a dosage of 2 mg allows you to quickly remove strong urges to smoke when necessary.

Initial therapy:

Treatment should begin with a plaster 25mg / 16chasov (1 stage) in combination with chewing gum 2 mg. At the same time apply at least 4 chewing gum 2 mg per day; usually enough 5-6 chewing gums. The number of chewing gums should not exceed 15 pieces per day. Usually the general course of treatment lasts for 8 weeks. After that, the dose of nicotine should be reduced gradually. The plaster is applied immediately after waking up in the morning and is removed before bedtime. The Nicorette® patch should be applied to dry, clean, undamaged skin that does not contain hair, such as the hip, upper limb or chest. You need to change the location of the overlay every day: do not use the same area for the next two days.

After applying the patch, wash your hands thoroughly to avoid irritation of the eyes from possible exposure to nicotine.

Abolition of combination therapy: You can cancel combination therapy in two ways.

Method 1: Over the next 2 weeks, you need to switch from a 25 mg / 16 hour patch (Stage 1) to a 15 mg / 16 hour patch (Stage 2) and then for a further 2 weeks to a 10 mg / 16 hour patch (Stage 3) while maintaining the amount of chewing gum applied at a dosage of 2 mg, as in Initial therapy. Then gradually reduce the amount of chewing gums to a complete cancellation for the time that the person needs, depending on his needs, but no later than 12 months after the start of the combination therapy. Method 2: is to completely remove the patch immediately after the end of the step Initial therapy. Then gradually reduce the amount of chewing gum with a dosage of 2 mg to complete cancellation for the time that the person needs, depending on his needs, but no later than 12 months after the start of the combination therapy.

Initial therapy

Period

time

Patch

Chewing gum 2 mg

First 8 weeks	1 plaster 25 mg / 16 hours (stage 1) daily		If necessary. Recommended 5-6 chewing gums with a dosage of 2 mg per day
Cancel - Method 1
Next 2 Weeks	1 plaster 15 mg / 16 hours (2nd stage) daily		Continue application of chewing rubber bands with a dosage of 2 mg as needed
Next 2 Weeks	1 plaster 10 mg / 16 hours (stage 3) daily		Continue application of chewing rubber bands with a dosage of 2 mg as needed
Up to 12 months after the start of application combination of the of therapy			Gradual elimination of chewing gum with a dosage of 2 mg
Cancel - method 2
Up to 12 months after the start of application combination of the of therapy		Gradual elimination of chewing gum with a dosage of 2 mg

Side effects:

The Nicorrette ® patch can cause unwanted reactions, similar to those that develop with other methods of nicotine administration; most of them are dose-dependent.

Approximately 20% of patients develop unexpressed local skin reactions during the first weeks of therapy.
Some symptoms, including dizziness, headache and insomnia, can be caused by the "cancellation" syndrome in quitting smoking. The same circumstance may be due to an increase in the incidence of aphthous stomatitis, but the true cause-effect relationship is unclear.

Very often (> 1/10); often (> 1/100, but <1/10); infrequently (> 1/1 000, but <1/100); rarely (> 1/10 000, but <1/1000); very rarely (<1/10 000), including individual messages.

Impaired nervous system:	Often	dizziness, headache
Cardiological violations:	Infrequently	Heart palpitations
Cardiological violations:	Rarely	reversible atrial fibrillation
.Disruptions from the digestive system:	Often	gastrointestinal discomfort, nausea, vomiting.
Undesirable effects from the skin and subcutaneous tissue	Infrequently	hives
Systemic disturbances and. complications at the site of administration	Often	itchy skin
	Often	erythema

Overdose:

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

An overdose of nicotine can occur with the simultaneous use of several transdermal patches, in the presence of dependence on very low

doses, as well as when combining transdermal patches with other sources of nicotine, including smoking.

Signs of an overdose developing with acute nicotine poisoning include: nausea, increased salivation, abdominal pain, diarrhea, sweating, headache, dizziness, hearing impairment and severe weakness.When high doses are used, these symptoms can reduce blood pressure, weak and irregular heartbeat, difficulty breathing, prostration, collapse, and generalized seizures.

Nicotine in adult-dose smokers doses can cause severe symptoms of intoxication in children, including fatal ones.

Treatment of overdose: should immediately stop using nicotine and prescribe symptomatic treatment. Activated carbon reduces absorption of nicotine in the gastrointestinal tract

Interaction:

Smoking (but not nicotine) causes an increase in the activity of the isoenzyme CYP1A2. After cessation of smoking, a decrease in the clearance of the substrates of this isoenzyme may be observed. This may lead to an increase in the concentration of certain drugs in the blood plasma, which has potential clinical significance when using drugs with a narrow therapeutic range, such as theophylline, Tacrine, clozapine and ropinirole.

After cessation of smoking in the plasma, concentrations of other drugs that are partially metabolized by the isoenzyme may also increase CYP1A2, such as imipramine, olanzapine, clomipramine and fluvoxamine, although there is no evidence to support this hypothesis, and the possible clinical significance of this effect is not known.

Limited evidence suggests that smoking can induce the metabolism of flecainide and pentazocine.

Special instructions:Patients who make up a group of cardiovascular risk (who have suffered serious cardiovascular disease, hospitalization for cardiovascular disorders, for example, stroke, myocardial infarction, unstable angina pectoris, arrhythmia of the heart, shunting or angioplasty of the coronary arteries, in for 4 preceding weeks or with uncontrolled arterial hypertension), should apply a patch

It is only after consulting with Nicoletge® doctor.

Nicoretge® should be used with caution in patients with severe or severe moderate hepatic insufficiency, severe renal failure, and also peptic ulcer disease or duodenum in the stage exacerbation. In this case, the risk of nicotine replacement therapy should correlate with the risk of continuing smoking.

Nicotine, as released from the media substitution therapy, and absorbed during smoking, stimulates release of catecholamines from the brain adrenal glands. therefore

Nicoretge® should be used with caution in patients with uncontrolled hyperthyroidism and pheochromocytoma.

Patients with diabetes mellitus can need to reduce the dose of insulin after cessation of smoking.

Effect on the ability to drive transp. cf. and fur:It is necessary to take into account the profile of side effects of the drug (dizziness), which can worsen the ability to drive vehicles and engage in other activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Transdermal patch 10 mg / 16 h, 15 mg / 16 h, 25 mg / 16 h.

1 plaster 10 mg / 16 h, 15 mg / 16 h or 25 mg / 16 h in the sachet. For 7, 14 or 28 sachets, along with instructions for use in a cardboard pack.

Packaging:(1) - sachet (14) / 1 in the sachet. For 7, 14 or 28 sachets along with instructions for use in a cardboard bundle. / - cardboard pack
(1) is the sachet (28) / 1 in the sachet. For 7, 14 or 28 sachets along with instructions for use in a cardboard bundle. / - cardboard pack
(1) - sachet (7) / 1 in the sachet.For 7, 14 or 28 sachets along with instructions for use in a cardboard bundle. / - cardboard pack

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package!

Terms of leave from pharmacies:Without recipe

Registration number:LP-001122

Date of registration:03.11.2011

The owner of the registration certificate:Johnson & Johnson, LLC Johnson & Johnson, LLC Russia

Manufacturer: & nbsp

McNeil AB, Sweden

Representation: & nbspJohnson & Johnson LLC Johnson & Johnson LLC Russia

Information update date: & nbsp10.08.2015

Illustrated instructions

Instructions

Nicorette® (Nicorette®)