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

Excipients: methacrylic acid and methyl methacrylate copolymer, polyester foil with aluminum coating, Matrix, layer 3: Duro-Tak® 387-2516, methacrylic acid and methyl methacrylate copolymer, middle-chain triglycerides (Miglyol 812); substrate - paper (26 g / m²), Matrix layers 1 and 2: Duro-Tak® 387-2516, methacrylic acid and methyl methacrylate copolymer, middle-chain triglycerides (Miglyol 812); Adhesive layer: Duro-Tak® 387-2516, medium-chain triglycerides (Miglyol 812); release layer - a polyester film, coated with silicone, with aluminum on one side.

Description:

TTS 7 mg / day: round beads of beige color with a diameter of about 36 mm. The adhesive is labeled CG CWC. Protective layer rectangular shiny on both sides, with a notch about 5 mm from one of the edges.

TTS 14 mg / day: round beads of beige color with a diameter of about 51 mm. The adhesive is labeled CG FEF. The protective layer is rectangular shiny on both sides, with a notch about 5 mm from one of the edges.

TTS 21 mg / day: round beads of beige color with a diameter of about 62 mm. The adhesive is labeled CG EME. Protective layer rectangular shiny on both sides, with a notch about 5 mm from one of the edges.

Pharmacotherapeutic group:a remedy for the treatment of nicotine addiction.

ATX: & nbsp

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

N.07.B.A.01 Nicotine

Pharmacodynamics:

N-holinostimuljator, reduces an inclination to smoking. It avoids the development of the "withdrawal" syndrome in people who quit smoking, which is expressed in a pronounced desire for smoking, dysphoria, irritability, frustration, anxiety, excitability, increased appetite or weight gain. Contained in plasters 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.

Pharmacokinetics:

Absorption:

Nicotine is rapidly absorbed through the skin and mucous membranes. In healthy non-tobacco smokers (using patches for smoking cessation), a gradual increase in the concentration of nicotine in the blood plasma is observed 1-2 hours after the application of the Nicotinell® patch.Then the concentration of nicotine in the blood plasma gradually grows and becomes even after 8-10 hours after the application.

After removal of the patch, the concentration of nicotine in the plasma drops more slowly than expected, given the half-life of nicotine (2 hours with intravenous administration). About 10% of the total nicotine, entering the bloodstream, is released from the skin depot formed during the application of the patch.

Absolute bioavailability of nicotine in the form of a patch relative to the indicators with intravenous administration is about 77%. The value of the area under the concentration-time curve (AUC about-24 ь) increases in direct proportion to the increase in the dosage of the patch: 7 mg / day, 14 mg / day, 21 mg / day. At repeated application of the patch with a dosage of 14 mg / day and 21 mg / day the concentration of nicotine in the plasma ranges from 7.1 to 12.0 ng / ml and from 10.3 to 17.7 ng / ml, respectively. Peak concentrations of nicotine in blood plasma after application of Nicotinell® TTC № 1 reaches 12.3 ng / ml. Stable concentration in blood plasma C_max After repeated application of Nicotinell® TTC is 12 ng / ml (TTC № 2), 17.7 ng / ml (TTC № 1); the minimum concentrations are - 7.1 ng / ml (TTC № 2) and 10.3 ng / ml (TTC № 1).

In the preparation Nicotinell® TTC nicotine is present in free form. Nicotine absorbed continuously throughout the entire period of wearing the adhesive from the time of its application.

Distribution:

Nicotine is distributed throughout the body, the volume of distribution is from 1 to 3 liters / kg. Nicotine penetrates through blood-brain and placental barriers, and also penetrates into breast milk. Nicotine has a very low level of binding to plasma proteins (less than 5 %), the plasma clearance is 0.92-2.43 l / min.

The concentration of nicotine in the blood plasma is in the range that is usually observed with moderate smoking, i.e. when smoking 1 cigarette per hour.

Metabolism:

Nicotine is excreted mainly by the liver. The main metabolites are cotinine and nicotine-G-N-oxide. Most of the cotinine undergoes repeated metabolism, its metabolites are pharmacologically inactive.

Excretion:

The half-life of nicotine is about 2 hours, the clearance from the blood plasma is 0.92 - 2.43 l / min.

Through the kidneys, in an unchanged form, only a small amount of nicotine is excreted.

Excretion by the kidneys of unchanged nicotine (5-10% of the total) is pH-dependent process. At alkaline pH values, the excretion level is low.Cumulation of the substance is very insignificant.

There was an increase in the concentration of cotinine and nicotine in the blood plasma in smokers with impaired liver and kidney function.

Renal insufficiency The progressive course of renal failure is associated with a decrease in overall nicotine clearance. In patients with severe renal failure, nicotine clearance is reduced by an average of 50%.

Liver failure Nicotine is mainly metabolized in the liver by isoenzyme CYP2A6, and its systemic clearance depends mainly on the hepatic blood flow. The pharmacokinetics of the drug Nicotinell® in patients with hepatic insufficiency has not been studied. It is expected that the pharmacokinetics of nicotine will be influenced by factors that alter expression CYP2A6 and hepatic blood flow.

Indications:

Treatment of nicotine addiction. Relief of symptoms arising from quitting smoking.

Contraindications:

Increased sensitivity of the skin to nicotine or one of the components that make up the drug, vasospastic angina, acute myocardial infarction, arrhythmia, recently suffered stroke, pregnancy and lactation.

The drug is contraindicated for non-smokers, children and adolescents.

The use of the Nicotinella® patch is recommended on the recommendation of a doctor for the treatment of adolescents in those cases where pronounced nicotine dependence is observed.

Carefully:severe diseases of the cardiovascular system or hospitalization in the previous 4 weeks (stroke, myocardial infarction, unstable angina, arrhythmia, the operation of aorto-coronary bypass surgery or angioplasty), insufficiency of peripheral circulation, renal failure, diabetes, uncontrolled hypertension, pheochromocytoma, hyperthyroidism , stomach ulcer.

Pregnancy and lactation:

Pregnant women are recommended to quit without using nicotine replacement therapy.

Nicotine enters the body of a pregnant, in any form (cigarettes, drugs, nicotine replacement therapy, etc.) can have a negative effect on the fetus. Tobacco cancellation with the help of nicotine replacement therapy can be carried out only under strict indications and directly under the supervision of a doctor after evaluating the ratio

risk / benefit.

Breast-feeding Nicotine penetrates into breast milk in quantities that can have an effect on the newborn. Therefore, during the lactation period, the use of Nicotinella® patches is not recommended.

The use of Nicotinell® patches during breastfeeding is carried out only on strict indications and directly under the supervision of the doctor after assessing the risk / benefit ratio.

Dosing and Administration:

Transdermal (patch application).

Nicotinell ® is intended for use in adults (in exceptional cases - in adolescents, see the section "Contraindications").

Before starting treatment, you must completely stop smoking.

Use only one patch for a day, sticking it on the surface of the skin.

The amount of nicotine liberated from the Nicotinella® patch per cm² skin, constantly, thus, the absorbed dose depends on the size of the area in direct contact with the patch. The plaster should be pasted on various sites of a skin to avoid local irritation. Existing forms of Nicotinell® patch release 21 mg of nicotine per day (No. 1), 14 mg of nicotine per day (No. 2) and 7 mg of nicotine per day (No. 3).Do not reduce the dose by cutting the patch.

Nicotinell® No. 1 is usually used to treat smokers with a pronounced nicotine addiction (ie, smoking more than 20 cigarettes a day). Nicotinell® No. 2 is effective in smokers with moderate nicotine addiction (smokers less than 20 cigarettes a day).

Nicotinell® No. 3 is intended for use at the final stage of treatment (during the last month) for a gradual reduction in the dose of nicotine-replacement therapy.

Duration of treatment

Treatment begins with a maximum or intermediate dose (Nicotinell® No. 1 or No. 2) and then gradually reduced. The initial dosage can be adjusted after a few days depending on the reaction of the body. Treatment of smokers with a pronounced nicotine dependence begins with the use of Nicotinella® No. 1, then transferred to Nicotinell® No. 2 and finishes using Nicotinella® No. 3, using each dosage for about a month.

Treatment of mild smokers begins with the use of Nicotinell® No. 2 for about eight weeks, then goes to Nicotinell® No. 3, which is used for four weeks.It is very important that during the treatment a higher dosage is not used than is required by the patient.

The duration of treatment should not exceed 3 months.

Mode of application

Remove the protective layer and paste the patch on a clean, dry, undamaged skin without hair, on the chest or on the arm. The place on which the adhesive will be applied should not be covered with lotion, shaving cream, perfume, cream, etc. Apply the palm and hold for about 10 seconds. Each day, you should paste a patch on a new area of the skin.

If, after completing the course of nicotine replacement therapy in accordance with the recommended method of application with the help of Nicotinell® patches, you did not quit smoking, then the drug should be discontinued. You can try again to stop smoking with Nicotinella® patches later.

Side effects:

The use of the Nicotinella® TTC can lead to the development of side reactions similar to those that can occur during smoking. In addition, the inhalation of cigarette smoke, in addition to getting nicotine into the body, entails an additional risk associated with the known harmful effects of carbon monoxide.Nicotinell® patches induce significantly lower levels of nicotine in the blood plasma than it does when smoking cigarettes, cigars, and tubes, so side effects appear to be much less pronounced when using Nicotinella® patches. Side effects of nicotine can develop more often and manifest more intensively in those who continue to smoke, despite the use of Nicotinella® patches.

The most common skin reactions at the site of application of the patch. They led to the early cancellation of the transdermal patch of Nicotinell® in approximately 6% of participants in clinical trials. These reactions include burning sensation at the site of application, edema, erythema, irritation, itching, rash, hives and blisters. Most of the skin reactions took place within 48 hours, but in more severe cases of erythema and infiltration persisted for 1-3 weeks. Significant skin reactions began to develop in the period from 3 to 8 weeks from the start of therapy. Registered as an undesirable reaction cough may be is associated with chronic bronchitis, which has arisen because of prolonged smoking in the past.

With the cessation of smoking, aphthous stomatitis may occur, but its relationship with substitution therapy with nicotine has not been clarified.

In clinical trials, the following side effects have been reported following the use of patches with frequency: very frequent (>1/10), frequent (from> 1/100 to <1/10), infrequent (from> 1 / 1,000 to <1/100), rare (from> 1 / 10,000 to <1 / 1,000), very rare (<1 / 10,000), including individual reports and reactions with unknown frequency (can not be calculated based on available data).

Immune system disorders Unknown: Quincke's edema, anaphylactic and anaphylactoid reactions, hives, itching.

Mental disorders *

Often: agitation, anxiety, nervousness, insomnia, unusual dreams. Infrequently: loss of concentration, drowsiness, affective lability, irritability, depressed mood and confusion.

Disturbances from the nervous system * Often: headache, dizziness, motor disorders.

Infrequently: paresthesia, perversion of taste, vague vision.

Rarely: tremor, migraine.

Heart Disease * *

Infrequently: a feeling of palpitations.

Rarely: chest pain, shortness of breath, arrhythmia. Vascular disorders **

Infrequently: arterial hypertension, hot flashes.

Disturbances from respiratory system, chest organs and

the mediastinum

Often: cough.

Infrequently: infections of the upper respiratory tract.

Disorders from the gastro-intestinal tract *

Often: nausea, abdominal pain, indigestion.

Infrequently: vomiting, constipation, diarrhea, flatulence, dry mouth.

Rarely: increased appetite, stomach ulcer, pain when swallowing.

Disturbances from the skin and subcutaneous fabrics

Often: erythema in severe form ***. Infrequently: sweating.

Rarely: rash, discoloration, herpes simplex, vasculitis.

Musculoskeletal disorders system and connective tissue Often: myalgia, arthritis.

Infrequently: arthralgia, muscle cramps, back pain.

General disorders and disorders in place introduction of

Often: reaction in the place of application. Often: influenza-like symptoms. Infrequently: asthenic conditions, pain, discomfort.

Rarely: labored breathing.

* These reactions can also be attributed to withdrawal symptoms due to cessation of smoking, as well as due to insufficient substitution therapy with nicotine.

** Patients with cardiovascular diseases may develop symptomatic progression and / or develop peripheral circulatory disturbances (intermittent claudication).

*** Reversible after removal of the patch, manifests itself with increasing frequency, starting from the third week of therapy. To avoid the appearance of local irritation on the skin, you should choose a new place for the application every day.

Overdose:

The application of several nicotinell® patches can lead to severe overdose. At the same time, the slow absorption of nicotine through the skin provides a duration of toxic effects.

In the event of accidental chewing or ingestion of Nicotinella® TTC, this will not result in a rapid systemic release of nicotine, since nicotine is released slowly and immediately metabolized.

Acute overdose:

Symptoms of overdose are the same as in acute nicotine poisoning: pallor, sweating, nausea, increased salivation, vomiting, intestinal cramps, diarrhea, headache, dizziness, visual and hearing disorders, tremors, confusion, tachycardia, increased blood pressure, dyspnea, mydriasis, muscle weakness, convulsions, prostration, disappearance of reflexes, respiratory failure.Death occurs as a result of respiratory arrest of peripheral or central origin, less often from sudden cardiac arrest.

Chronic overdose:

Regular smokers develop tachyphylaxis, which allows them to tolerate the effects of nicotine, which is highly toxic in acute intoxication. In chronic overdose, symptoms are similar to those observed with acute intoxication with nicotine.

First aid:

Immediately remove the patch from the skin, wash the skin with water (do not use soap), dry it. It should be borne in mind that nicotine will continue to be released into the bloodstream within a few hours after removal of the TTS from the skin.

In acute nicotine intoxication: emergency therapy in conditions hospital with the use of symptomatic therapy, including with the implementation of activities aimed at maintaining the respiratory and cardiovascular systems.

Even in small quantities nicotine It is dangerous for children, because it causes symptoms of poisoning up to a lethal outcome. In case of accidental overdose with nicotine, children need emergency medical care.

Interaction:

In smokers, the induction of enzyme systems is noted, which is due not so much to the effect of nicotine proper, but to resinous compounds present in tobacco smoke. In this regard, those who quit smoking may experience a change (normalization) of metabolism, therefore, the pharmacological efficacy of the drugs may change, even against the background of nicotine-replacement therapy in the form of a nicotinell® patch.

Smoking can reduce the concentration of the drug in the blood, this applies to such drugs as phenazone, estrogens, nordazepam, lidocaine, oxazepam, warfarin, phenacetin, caffeine, theophylline, imipramine and pentazocine.

Other effects caused by smoking include: a decrease in the analgesic effect of propoxyphene, as well as the diuretic effect of furosemide, a change in the pharmacological response to propranolol and a change in the rate of ulcer healing by the action of blockers H₂-gistaminovyh receptors.

Tobacco smoke and nicotine can also increase the levels of cortisol and catecholamines circulating in the body. It may be necessary to adjust the dose of nifedipine, as well as stimulants or adrenergic receptor blockers.

At the cessation of smoking, suppression of the above-described phenomena can be observed even in patients carrying out partial replacement therapy with help with Nicotinell® patches. When prescribing therapy with the use of Nicotinell® patches, doctors should evaluate the need for dose adjustment of the above drugs. The effect of beta-blockers can vary in different ways, because nicotine affects various parts of the sympathetic and parasympathetic nervous system.

Special instructions:Before starting the application of Nicotinella® patches, you should completely stop smoking. If you continue to smoke during the course of treatment with Nicotinella® TTS, the risk of side effects and their severity increases, including side effects from the cardiovascular system. Nicotinell® TTS is recommended in combination with other

programs designed to help those who want to quit. An important role in the treatment is played by personal motivation and psychotherapeutic help. This allows to increase the effectiveness of treatment.

Incompatibility

Local toleranceNicotinella® TTC: With transdermal administration, it is very important to clearly identify the difference between skin tolerance to the active ingredient nicotine and skin tolerance to the adhesive system itself.

Children

Nicotine is a highly toxic substance. Doses normally tolerated by adults undergoing treatment can lead to severe intoxication in children. Therefore, the Nicotinell® patch should be stored out of the reach of children.

The Nicotinell® patches are packed in individually tightly sealed bags that children can not open by themselves. Before use, cut the scissors packet, making sure not to damage the adhesive that is in it.

In the used plasters, too nicotine, so you need to ensure that they also do not fall into the hands of children.

Allergic reactions:

In some patients, nicotinic hypersensitivity was observed during the application of Nicotinella patches. It must be remembered that in such persons the use of other drugs containing nicotine, as well as smoking can lead to the development of allergic reactions.

For persons suffering from chronic sleep disorders, it is allowed to remove the patch 16 hours after the application. The Nicotinell® patch contains aluminum. When conducting magnetic resonance imaging, defibrillation, or diathermocoagulation, the patch should be removed from the skin.

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

The drug does not affect the ability to drive a car or work with mechanisms that require increased concentration. However, it must be remembered that the need for smoking can cause changes in behavior.

Form release / dosage:10cm patch² (7 mg / day), 20 cm² (14 mg / day) or 30 cm² (21 mg / day) in a multilayer bag (paper / aluminum / polyamide / polyacrylonitrile). By 2, 7, 14, 21 and 28 bags together with instructions for use in a pack of cardboard.

Packaging:(1) - sachets (14) - packs of cardboard
(1) - sachets (2) - packs of cardboard
(1) - sachets (21) - packs of cardboard
(1) - sachets (28) - packs of cardboard
(1) - sachets (7) - packs of cardboard

Storage conditions:

Store at a temperature not higher than 30 ° C. Keep out of the reach of children's place.

Shelf life:

3 years. The drug should not be used after expiry date, indicated on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LSR-004223/09

Date of registration:28.05.2009

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

Manufacturer: & nbsp

LTS LOHMANN THERAPIE-SYSTEME, AG Germany

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

Information update date: & nbsp12.08.2015

Illustrated instructions

Instructions

Nicotinell® (Nicotinell®)