NIKORETTE (Chewing gum)

Active material: Nicotine
When ATH: N07BA01
CCF: Drug for the treatment of nicotine addiction
ICD-10 codes (testimony): F17
When CSF: 02.17
Manufacturer: JOHNSON & JOHNSON LTD (Russia)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

◊ Chewing Gum Fresh Mint square, coated white, with the smell of mint; size 15 × 15 × 7 mm.

* nicotine content 2.2 mg, including 10% excess.

Excipients: gum base **, Xylitol, peppermint oil, sodium carbonate, natriya carbonate, acesulfame potassium, levomenthol, magnesium oxide.

** The gum base: a mixture of different types of wax, resins and other hydrocarbons (about 60%) and calcium carbonate (to 40%).

Sheath gum: Xylitol, peppermint oil, Gum arabic, Titanium dioxide, carnauba wax.

15 PC. – blisters (2) – packs cardboard.

◊ Chewing Gum Fresh Mint square, coated liner from light brown to light yellow with a greenish tint, with the smell of mint; size 15 × 15 × 7 mm.

* nicotine content 4.4 mg, including 10% excess.

Excipients: gum base **, Xylitol, peppermint oil, sodium carbonate, acesulfame potassium, levomenthol, magnesium oxide, quinoline yellow (E104).

** The gum base: a mixture of different types of wax, resins and other hydrocarbons (about 60%) and calcium carbonate (to 40%).

Sheath gum: Xylitol, peppermint oil, Gum arabic, Titanium dioxide, carnauba wax, quinoline yellow (E104).

15 PC. – blisters (2) – packs cardboard.

Pharmacological action

Drug for the treatment of nicotine addiction. After a sharp smoking cessation in patients, daily use nicotine products for a long time, may develop withdrawal, which includes dysphoria, insomnia, increased irritability, alarm, impaired concentration, a decrease in heart rate, increased appetite and weight gain, as well as the desire to smoke.

In the treatment of nicotine addiction with nicotine replacement therapy can reduce the need for smoking (and the number of cigarettes smoked), reduce the severity of withdrawal symptoms, arising from the full smoking cessation in those, who decided to quit smoking. Facilitates temporary abstinence from smoking and reduces the number of cigarettes smoked in those, who can not or does not want to completely give up smoking.

Pharmacokinetics

Absorption

Nicotine, coming from gum, rapidly absorbed through the buccal mucosa and is found in the blood 5-7 m.

C_max nicotine plasma levels achieved after 30 min after the start of chewing gum.

Distribution

V_d nicotine / introduction is about 2-3 l / kg. Nicotine binding to plasma proteins is less than 5%. Therefore disturbances nicotine binding, while the application of other drugs or modify the amount of protein in the plasma at various diseases should not have a significant effect on the kinetics of nicotine.

Metabolism

Nicotine is metabolized in the liver, kidney and lung. Identified more 20 metabolites, are inferior to the activity of nicotine. Metabolite concentration pervichnogo – cotinine – greater than the concentration of nicotine in 10 time.

Deduction

Write mainly by the liver. The average plasma clearance is about 70 l /. T_1/2 – about 2 no.

The urine output is mainly cotinine (15% dose, T_1/2 – 15-20 no) and trans-3-hydroxy-cotinine (45% dose). 10-30% nicotine dose is excreted in the urine in unchanged form.

Pharmacokinetics in special clinical situations

The progressive deterioration of renal function associated with reduced total clearance of nicotine.

The pharmacokinetics of nicotine is not significantly altered in patients with cirrhosis of the liver with slightly severe hepatic impairment (5 points on the Child-Pugh) and reduced in patients with liver cirrhosis with moderately severe hepatic impairment (7 points on the Child-Pugh).

Patients, hemodialysis, marked increase in the concentration of nicotine in the blood plasma.

Elderly patients have a slight decrease in the total clearance of nicotine, that does not require dose adjustments.

Testimony

For the treatment of tobacco dependence:

- Reduction of withdrawal symptoms, arising from the full smoking cessation in patients, who decided to quit smoking;

- In temporary smoking cessation;

- To reduce the number of cigarettes smoked in those, who can not or does not want to completely give up smoking.

Dosage regimen

Depending on the severity of addiction to smoking use Nicorette gum^® with different concentrations of active substance.

If the patient smokes 20 or less cigarettes per day or first cigarette smoked through 30 minutes after awakening, should be used chewing gum containing nicotine 2 mg.

If the patient smokes more 20 cigarettes per day, or he failed to quit using chewing gum containing nicotine 2 mg, it is recommended to use a chewing gum containing nicotine 4 mg.

Nikorette^® It should be used in all cases, when there is an irresistible urge to smoke. Gum should be chewed slowly until a sharp taste, then should stop chewing and place the gum between the gum and the inside of the cheek. After the disappearance of taste should resume chewing. For 1 Reception should be used only 1 gum.

At full smoking cessation the average daily dose is 8-12 gums, maximum – 15 gums. It is necessary to continuously use the drug in the first 3 Months after quitting. Followed by gradually reducing the amount consumed gums. When the daily intake of the drug to fall to 1-2 gums, its application should be discontinued.

At reducing the number of cigarettes smoked chewing gum should be used between episodes of smoking to lengthen the intervals between smoking a cigarette, to minimize the consumption of cigarettes. Patients should be warned, that if through 6 weeks of the drug failed to reduce daily consumption of cigarettes, should consult a specialist doctor.

The patient should try to quit smoking, when it will be ready for it, but no later than 6 months after initiation of treatment. If during the 9 months after initiation of therapy was unable to quit smoking, should consult a specialist.

Not recommended for use Nicorette gum^® more 12 Months. However, some patients may require a longer treatment, to prevent a return to smoke or not to return to the previous level of tobacco consumption.

Chewing gum can be used during periods, when necessary temporarily give up smoking, for example while in the field, where non-smoking, or in other situations, when you need to refrain from smoking.

Professional consultation and psychological support contribute to the effectiveness of therapy.

Side effect

Most adverse reactions observed during the first 3-4 weeks of the drug and are dose-dependent.

Early treatment: sometimes – slight irritation of the throat and increased salivation; by ingestion of excessive amounts of dissolved nicotine – Ikotech.

Excessive use of the drug by persons, not accustomed to smoke inhalation: nausea, weakness, headache.

From the digestive system: when used chewing gum containing nicotine 4 mg in patients, prone to indigestion - dyspepsia, heartburn.

Dizziness, headache, Sleep disorders can be manifestations of the syndrome, caused by quitting smoking. When quitting smoking may increase the incidence of canker sores.

In the description, the following adverse effects frequency of criteria: Often (>1/10), often (>1/100 <1/10), infrequently (>1/1000, <1/100), rarely (>1/10 000, <1/1000), rarely (<1/10 000).

CNS: Often – headache; often – dizziness.

Cardio-vascular system: Infrequent - palpitation; very rarely - atrial fibrillation.

From the digestive system: very often - gastrointestinal discomfort, Ikotech, nausea; often – vomiting.

Dermatological reactions: rarely - erythema, hives.

Other: very often - pain in the throat or mouth, pain in the masticatory muscles; rarely – allergic reactions, including angioedema.

Contraindications

- Hypersensitivity to nicotine and other ingredients.

FROM caution and only after consulting your doctor should be applied to patients with disorders of the cardiovascular system, incl. suffered a cardiovascular disease within 1 months before the application (incl. stroke, myocardial infarction, unstable angina, arrhythmia, coronary artery bypass grafting, Angioplasty), or with uncontrolled hypertension.

FROM caution It should be prescribed to patients with moderate or severe hepatic impairment, severe renal insufficiency, aggravation of gastric ulcer and duodenal ulcer.

FROM caution should be applied to patients with uncontrolled hyperthyroidism, pheochromocytoma (because, that nicotine causes the release of catecholamines from the adrenal medulla), and diabetes.

Pregnancy and lactation

Nicotine crosses the placental barrier and can have a negative effect on the respiratory system and the fetal circulation. Smoking can harm the fetus, therefore, patients should try to convince of the need of quitting without using drugs-nicotine replacement therapy. With the failure of these attempts decision to conduct therapy is made after comparing the possible positive effects and potential harm.

Nicotine (even when used in therapeutic doses) in small amounts excreted in breast milk and may have an adverse effect on the infant while taking the drug nursing mother. In order to reduce the negative impact of nicotine on child drug Nicorette^® It should be applied immediately after feeding.

Cautions

Use of the drug Nicorette^® accompanied by a lower risk, than smoking.

Patients, who wear dentures, there may be difficulties in applying the gum Nicorette^®. Chewing gum can stick to dentures and in rare cases damage it.

Patients with diabetes mellitus after smoking cessation may be necessary to decrease insulin doses.

Slight indigestion, in the application of a chewing gum containing nicotine 4 mg can be eliminated by a slow chewing gum or gum use, contains 2 mg nicotine (optionally with smaller intervals).

The patient should be informed, that he should wear a gum Nicorette^® with myself, to take advantage of it, if he suddenly want to smoke.

Use in Pediatrics

The question of the appointment of the drug patients aged to 18 years It is decided by the doctor individually.

Effects on ability to drive vehicles and management mechanisms

The negative impact on the ability to drive a car and operate machinery is not installed.

Overdose

Excessive intake of nicotine replacement therapy and / or smoking might cause symptoms of an overdose.

Symptoms: nausea, drooling, stomach ache, diarrhea, Sweating, headache, dizziness, hearing loss and severe weakness; high doses of nicotine – hypotension, weak pulse and spasmodic, labored breathing, vascular collapse and generalized seizures, ie. Symptoms of acute nicotine poisoning.

Doses of nicotine, are well tolerated in the treatment of adult smokers, can cause severe poisoning symptoms in young children, and even lead to death.

Treatment: stop taking nicotine and start symptomatic treatment. Activated charcoal reduces the absorption of nicotine in the gut. If necessary, designate the ventilator and oxygen.

Drug Interactions

Smoking (but the use of nicotine) It causes an increase in activity of CYP1A2. After stopping smoking there may be a decrease in clearance of substrates of this enzyme, which may lead to increased concentrations of certain drugs in plasma, that has potential clinical value while using drugs, characterized by small breadth of therapeutic action (theophylline, tacrine, klozapyn, ropynyrol).

Limited data suggest that, smoking may induce the metabolism of flecainide and pentazocine.

Conditions of supply of pharmacies

The drug is resolved to application as an agent Valium holidays.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life - 2 year.