Nikorette

Nikorette – the drug used at treatment of nicotine addiction.

Form of release and structure

Nikorette is let out in the following dosage forms:

• The plaster is transdermalny: beige, translucent, squared with the rounded-off corners on the silikonizirovanny and aluminized separated substrate; 10 mg / 16 h – the size 27,7×33,2 of mm, of 9 cm ² ± 2%; 15 mg / 16 h – the size 33,2×41,3 of mm, of 13,5 cm ² ± 2%; 25 mg / 16 h – the size 43×53 of mm, of 22,5 cm ² ± 2% (on 1 piece in a sachet, on 7, 14, 28 sachets in a cardboard pack);
• Transdermal Therapeutic System (TTS): a rectangular plaster with the rounded edges, one party – "nicorette", light brown with a text, the second – silver-white, sticky, with a transparent synthetic protective film; the area of a plaster – 10, 20 or 30 cm ² (on 1 piece in a sachet, on 7 or 14 sachets in a cardboard pack);
• Tablets are hypoglossal: white or almost white, flat, round, with slanted edges, with the squeezed-out texts (on one party - "NIC", on another – "2") (on 10 pieces in blisters, on 2, 3, 9 or 10 blisters in a cardboard pack);
• Tablets are hypoglossal lemon: white or almost white, flat, round, with slanted edges, on one party the text of "N2" is squeezed out (on 10 pieces in blisters, on 2, 3, 9 or 10 blisters in a cardboard pack);
• Chewing gums: white (on 2 mg) or yellow (on 4 mg) square small pillows the mm size 14×14×5, with a characteristic smell (on 15 pieces in blisters, on 1, 2 or 7 blisters in a cardboard pack);
• Chewing gums "Spicy Mint": white or almost white (on 2 mg) or light yellow with a greenish or brownish shade (on 4 mg) square small pillows the size near 15×15×6 mm, are allowed small roughnesses on each side (on 15 pieces in blisters, on 1, 2 or 7 blisters in a cardboard pack);
• Chewing gums "Fresh Mint": white (on 2 mg) or from color, light brown to light yellow with a greenish shade (on 4 mg) square small pillows the mm size 15×15×6, with a mint smell (on 6 pieces in blisters, on 1 blister in a cardboard pack; on 15 pieces in blisters, on 1, 2 or 7 blisters in a cardboard pack);
• Chewing gums "Frosty Mint": almost white or white (on 2 mg) or light yellow with a greenish or brownish shade (on 4 mg) square small pillows the size near 15×15×6 mm, are allowed small roughnesses on each side (on 15 pieces in blisters, on 2 blisters in a cardboard pack);
• Chewing gums "Fresh Fruit": almost white or white (on 2 mg) or light yellow with a greenish or brownish shade (on 4 mg) square small pillows the size near 15×15×6 mm, are allowed small roughnesses on each side (on 6 pieces in blisters, on 1 blister in a cardboard pack; on 15 pieces in blisters, on 1, 2 or 7 blisters in a cardboard pack);
• Chewing gums mint: light-beige (on 2 mg) or light yellow square small pillows the size near 14×14×5 mm with characteristic mint taste (on 15 pieces in blisters, on 1, 2, 7 or 14 blisters in a cardboard pack);
• Solution for inhalations (absorbed): in a cartridge (in the form of the white or slightly painted porous cylinder in the corked transparent plastic cartridge with the specified number of a series and a text of "NICORETTE") (on 10 mg in inhalers, on 6 inhalers in blisters, on 1 or 3 blisters in a cardboard pack);
• Spray for topical administration dosed: color from light yellow to colourless, slightly opalescent or transparent solution with a mint smell (on 150 doses (13,2 ml) in bottles from polyethyleneterephthalate, on 1 or 2 bottles in a protective case from polypropylene complete with the doser in a plastic planimetric container).

Transdermalny is a part of 1 plaster:

• Active agent: nicotine – 15,75 / 23,62/39,37 mg (the dose allocated in 16 hours – 10, 15 or 25 mg respectively);
• Auxiliary components (10/15/25 mg in 16 h respectively): triglycerides (average length of a chain) – 18,27/27,41/45,68 mg, copolymer of the main butylmethacrylate – 14,58/21,87/36,45 mg, a polietilentereftalatny film 19 μм (on the one hand can be varnished) – the carrier of the layer containing active agent;
• Acrylate basis (10/15/25 mg in 16 h respectively): acrylic adhesive solution – 123,84/185,76/309,6 mg, potassium hydroxide – 0,7/1,05/1,8 mg, croscarmellose sodium – 5/7,49/12,5 mg, aluminum acetylacetonate – 0,06/0,09/0,12 mg, a polietilentereftalatny film 100 μм, silikonizirovanny on both sides and aluminized on the one hand – the deleted substrate (the carrier, is protection of adherent layer), is discarded before use.

² TTS is a part of 1 cm:

• Active agent: nicotine – 0,83 mg (the dose allocated to TTS in 16 hours – 5, 10 or 15 mg);
• Auxiliary components: substrate film, nonwoven polyether, middlemolecular polyisobutylene, low-molecular polyisobutylene, polybutene, silikonizirovanny polyether.

Hypoglossal is a part of 1 tablet:

• Active agent: nicotine – 2 mg (in a look никотин-β-циклодекстринового a complex – 17,1 mg);
• Auxiliary components: Бетадекс (β-cyclodextrin) – 69,55 mg, кросповидон – 2 mg, magnesium stearate – 0,9 mg, colloid silicon dioxide – 0,45 mg.

Is a part of 1 tablet of hypoglossal lemon:

• Active agent: nicotine – 2 mg (in the form of a dihydrate of ditartrate of nicotine of-6,14 mg);
• Auxiliary components: Mannitolum, microcrystallic cellulose, K90 povidone, methyl cellulose, ProSolv (microcrystallic cellulose – 98%; colloid silicon dioxide – 2%), magnesium stearate, fragrance 501438 AP1051, fragrance the Lemon 501163 TP0551, aspartame.

Is a part of 1 chewing gum:

• Active agent: nicotine – 2 or 4 mg (in a look nicotine - a polymeric complex – 10 or 20 mg);
• Auxiliary components: a basis of chewing gum, powdery sorbitol, the sorbitol solution (crystallizing) solution of a glitserol of 85%, sodium carbonate, hydrosodium carbonate, Haverstroo ZD49284 fragrance, a fragrance 84.6422.

Is a part of 1 Spicy Mint chewing gum:

• Active agent: nicotine – 2 or 4 mg (in a look nicotine - a polymeric complex – 11 or 22 mg);
• Auxiliary components: basis of chewing gum, ксилитол, sodium carbonate, peppermint oil, to potassium atsesulfa, hydrosodium carbonate, left menthol, magnesium oxide;
• Internal cover: gipromelloza, Burning Spicy Mint fragrance of SN679712, sukraloz, polysorbate 80;
• Outside cover: ксилитол, gum of an acacia (arabic gum), titanium dioxide, SN679712 Burning Spicy Mint fragrance, karnaubsky wax.

Is a part of 1 Fresh Mint chewing gum:

• Active agent: nicotine – 2 or 4 mg (in a look nicotine - a polymeric complex – 11 or 22 mg);
• Auxiliary components: basis of chewing gum, hydrosodium carbonate, ксилитол, sodium carbonate, peppermint oil, to potassium atsesulfa, left menthol, magnesium oxide;
• Cover of chewing gum: Arabian gum, ксилитол, titanium dioxide, peppermint oil, karnaubsky wax.

Is a part of 1 Frosty Mint chewing gum:

• Active agent: nicotine – 2 or 4 mg (in a look nicotine - a polymeric complex – 11 or 22 mg);
• Auxiliary components: basis of chewing gum, sodium carbonate, ксилитол, peppermint oil, left menthol, hydrosodium carbonate, to potassium atsesulfa, magnesium oxide;
• Internal cover: Winterfresh fragrance, sukraloz, gipromelloza, polysorbate 80;
• Outside cover: ксилитол, prezhelatinizirovanny starch, titanium dioxide, Winterfresh fragrance, karnaubsky wax.

Is a part of 1 Fresh Fruit chewing gum:

• Active agent: nicotine – 2 or 4 mg (in a look nicotine - a polymeric complex – 11 or 22 mg);
• Auxiliary components: a basis of chewing gum – 560 mg, ксилитол – 314 mg, peppermint oil – 30 mg, left menthol – 2 mg, hydrosodium carbonate – 10 mg, sodium carbonate – 20 mg, to potassium atsesulfa – 2 mg, magnesium oxide – 1 mg;
• Internal cover: a gipromelloza – 7,5 mg, a sukraloza – 5 mg, tutti-frutt of Kuel84441 – 9 mg, polysorbate of 80 - 0,5 mg;
• Outside cover: tutti-frutt of Kuel84441 – 5 mg, ксилитол – 277,5 mg, titanium dioxide – 6 mg, an acacia – 8,5 mg, karnaubsky wax – 1 mg.

Mint is a part of 1 chewing gum:

• Active agent: nicotine – 2 or 4 mg (in a look nicotine - a polymeric complex);
• Auxiliary components: basis of chewing gum, xylitol, anhydrous sodium carbonate, peppermint oil, hydrosodium carbonate, talc, left menthol, magnesium oxide, dye quinolinic yellow, nitrogen.

Basis of chewing gums of all types: calcium carbonate mix (to 40%) and various types of pitch, wax and other hydrocarbons (about 60%).

Is a part of 1 cartridge (inhaler):

• Active agent: nicotine – 10 mg;
• Auxiliary components: left menthol – 1 mg, nitrogen – in enough, ethanol – 133 mg (evaporates by production).

For topical administration is a part of 1 ml of spray:

• Active agent: nicotine – 13,6 mg;
• Auxiliary components: propylene glycol – 150 mg, ethanol – 97 mg, трометамол – 40,5 mg, half-oxameasures – 40 mg, глицерол – 25 mg, hydrosodium carbonate – 14,3 mg, left menthol – 10 mg, Cooler 2 SN046680 fragrance – 3 mg, mint QL24245 fragrance – 4 mg, to potassium atsesulfa – 1,5 mg, a sukraloza – 1,5 mg, Acidum hydrochloricum of 10% – in enough to pH 9, water – in enough to 1 ml.

Indications to use

Nikorette is appointed for treatment of tobacco addiction by decrease in need for nicotine in the following situations:

• Full refusal of smoking at the patients who decided to leave off smoking (for reduction of symptoms of cancellation);
• Incomplete refusal of smoking (for decrease in quantity of the smoked cigarettes at unwillingness or impossibility to leave off smoking completely);
• Temporary refusal of smoking.

Contraindications

Contraindication to Nikorette's use is hypersensitivity to drug components.

With care and only after medical consultation drug is appointed in the presence of the following diseases / states:

• Disturbances of cardiovascular system, including uncontrollable arterial hypertension, and states after the postponed cardiovascular diseases within 30 days before use (including a myocardial infarction, a stroke, arrhythmia, unstable stenocardia, angioplasty, aortocoronary shunting);
• The moderated or expressed functional disturbances of a liver, heavy renal failure, aggravation of a peptic ulcer of a stomach and duodenum;
• Uncontrollable hyperthyroidism, pheochromocytoma, diabetes mellitus.

Route of administration and dosage

Tablets hypoglossal and tablets hypoglossal lemon
It is necessary to keep Nikorette's tablets under language about 30 minutes (before full dissolution).

For the first days from the moment of the beginning of therapy emergence of unpleasant feelings in an oral cavity, in a throat is possible (pass after a while independently).

Depending on degree of tobacco addiction the initial dose is selected individually – from 1 (at small dependence) to 2 tablets (if the quantity of the smoked cigarettes in day is more than 20 pieces or Fagerstrom's test for nicotine addiction more than 6 points) on reception. At the beginning of a course of treatment drug each 1-2 hours, as a rule, accept enough 8-12 tablets a day (2 mg), but it is no more than 30 tablets in day (2 mg).

For full refusal of smoking it is necessary to accept drug not less than 3 months, gradually reducing quantity of the taken pill. Therapy stop 1-2 tablets at a daily dose.

For reduction of quantity of the smoked cigarettes drug is recommended to be accepted between smoking episodes that will allow to extend intervals between smoking of cigarettes. In the absence of result in 1,5 months of therapy it is necessary to consult with the doctor.

It is possible to apply to temporary refusal of smoking of a tablet during the periods when it is necessary to refuse smoking temporarily.

Transdermal therapeutic system
It is necessary to plaster daily in the morning (directly after awakening) on the unimpaired skin and to delete before going to bed.

Therapy begin with use of 1 plaster 15 mg / 16 h. Duration of an initial stage of therapy is determined individually. As a rule, it makes not less than 3 months then the dose is gradually reduced, applying for 2-3 weeks plasters on 10 mg / 16ч, and then throughout the same period – on 5 mg / 16 h.

The plaster is transdermalny
The plaster transdermalny is applied also as well as TTS.

Heavy smokers (from 20 cigarettes a day) therapy are recommended to begin with daily use of 1 plaster 25 mg / 16 h for 2 months. After that the dose is reduced – 1 plaster on 15 mg / 16 h within 2 weeks, then — on 10 mg / 16 h throughout the same period.

Not heavy smokers (from 10 to 20 cigarettes a day) are recommended to begin therapy with use of a plaster on 15 mg / 16 h for 2 months, then treatment is continued using a plaster on 10 mg / 16 h for 2 months.

In cases when against the background of use of a plaster of people continues to have periodically insuperable desire to smoke or if it was not succeeded to leave off smoking, applying only a plaster or chewing gums, perhaps combined treatment. Chewing gum on 2 mg in a complex with a plaster allows to remove quickly strong desires to smoking.

During initial therapy apply, at least, 4 chewing gums on 2 mg a day (no more than 15 pieces a day). In 2 months of treatment gradually the dose of drug is reduced.

Cancel a combination therapy in two ways:

• Way 1: gradually reduce a plaster dose (2 weeks on 15 mg / 16 h, then 2 weeks on 10 mg / 16 h), without changing amount of the applied chewing gums. Then gradually reduce amount of chewing gums before full cancellation;
• Way 2: full cancellation of use of a plaster upon termination of the initial stage of treatment. Further gradually reduce amount of chewing gums to full cancellation.

The general duration of a course should not exceed 12 months.

Chewing gums of all types
Depending on expressiveness of addiction to smoking apply chewing gums with various concentration of active agent.

If the patient smokes up to 20 cigarettes a day, appoint Nikorette on 2 mg. At insufficiency of effect it is recommended to use drug with the content of nicotine of 4 mg.

Nikoretta needs to apply in all cases when there is insuperable desire to smoke. The elastic band needs to be chewed slowly, before emergence of sharp taste then it is placed between the interior of a cheek and a gum. It is necessary to resume chewing after smack disappearance. For 1 reception it is necessary to use only 1 chewing gum.

The average daily dose for full refusal of smoking makes 8-12 pieces (as much as possible – 15 elastic bands). Continuously drug is used for 3 months then the dose is gradually reduced.

To reduce quantity of the smoked cigarettes, Nikoretta needs to apply between smoking episodes at the expense of what the interval between smoking of cigarettes is extended. In the absence of improvement for 1,5 months of therapy it is necessary to consult at the doctor.

Solution for inhalations
The inhaler is applied at emergence of insuperable desire to light. The number of inhalations in day is appointed individually, considering degree of manifestation of nicotine addiction, but no more than 12 cartridges a day. The chosen dose of inhalations should be applied for 1,5-3 months then the dose should be reduced gradually.

1 cartridge replaces 4 cigarettes. If the patient smoked 20 cigarettes a day, then use can result less than 6 cartridges a day in lack of effect of the carried-out treatment. The recommended therapy duration – is not less than 3 months.

If within 1,5 months it was not succeeded to achieve decrease in daily consumption of cigarettes, it is necessary to see a doctor.

The inhaler can also be applied in a combination with a plaster (transdermal therapeutic system with nicotine).

Spray for topical administration
Nikorette in the form of spray is applied at emergence of insuperable desire to light. To exclude hit of substance in respiratory tracts, it is not necessary to make a breath at the time of pressing the doser. For achievement of optimum effect it is not necessary to swallow saliva within several seconds after injection.

Reception of liquid and food in usage time of spray is not recommended.

In a span when the patient usually smokes a cigarette, and also in cases of emergence of thirst for smoking it is necessary to make 1-2 injections. If within several minutes draft does not decrease, it is necessary to make the second injection.

In most cases there is enough use of 1-2 doses of spray each 30-60 minutes.

Within an hour it is allowed to apply no more than 4 dosed spray injections. It is not necessary to inject more than 2 doses of spray in one step or to apply more than 64 doses during the day.

Nikorette's use in various dosage forms longer is not recommended than 6-12 months. Sometimes more long treatment can be required by the left off smoking patients.

Efficiency of therapy is usually increased by psychological support and medical consultation.

Side effects

The undesirable reactions arising at use of various forms of Nikorette are similar and have dozozavisimy character. The majority of side effects is noted within the first 3-4 weeks of therapy.

Frustration of a dream, a headache and dizziness can be symptoms of the withdrawal connected with refusal of smoking. Also increase in frequency of developing of aphthous stomatitis is noted (communication of these reactions using Nikorette is unevident).

During therapy development of disturbances is possible:

• Central nervous system: often – dizziness, a headache;
• Cardiovascular system: often – a cardiopalmus; seldom – atrial fibrillation;
• Alimentary system: often – a hiccups, gastrointestinal discomfort, nausea;
• Respiratory system: often – rhinitis, cough;
• Others: often – irritation of a mucous membrane of an oral cavity, a pharyngalgia, dryness in a throat.

At external use of Nikorette the local reactions which are shown in the form of moderately expressed reddening and an itch can develop.

Special instructions

At a diabetes mellitus after smoking cessation decrease in a dose of insulin can be required.

Nikorette's use has smaller risk, than smoking.

During therapy it is necessary to be careful at control of motor transport and the performance of work demanding the increased concentration of attention and bystry psychomotor reactions.

Medicinal interaction

After refusal of smoking it can be observed:

• Increase in activity of an isoenzyme of CYP1A2 that can lead to increase in concentration of some medicines in a blood plasma (for example, theophylline, clozapine, a takrin, a ropinirol);
• Increase in concentration of other drugs which are partially metabolized under the influence of CYP1A2 isoenzyme (for example, Imipraminum, a klomipramin, olanzapine, a fluvoksamin).

Smoking can induce metabolism of pentazocine and a flekainid.

Terms and storage conditions

To store in the place, unavailable to children, at a temperature up to 25 °C.

Period of validity – 3 years.