Nicotine-polymer complex * 22 mg, which corresponds to the nicotine content ** 4 mg.
A remedy for the treatment of nicotine addiction. After abrupt smoking cessation, patients who use tobacco-containing products for a long time every day may develop withdrawal syndrome, which includes: dysphoria, insomnia, irritability, anxiety, impaired concentration, decreased heart rate, increased appetite or weight gain. An important symptom of withdrawal is also the desire to smoke. When treating tobacco addiction, nicotine replacement therapy can reduce the need for smoking (and the number of cigarettes smoked), reduce the severity of withdrawal symptoms that occur when you quit smoking completely. It facilitates temporary abstinence from smoking and helps to reduce the number of cigarettes smoked by those who are unable or unwilling to completely quit smoking. Promotes removal of pigmented plaque on the teeth, has a bleaching effect.
Absorption: Nicotine, coming from a chewing gum, is quickly absorbed through the buccal mucosa and is found in the blood in 5-7 minutes. Cmax of nicotine in the blood plasma is reached 30 minutes after the start of the use of chewing gum. Distribution: Vd nicotine with a / in the introduction of about 2-3 l / kg. The binding of nicotine to plasma proteins is less than 5%. In this regard, violations of nicotine binding with the simultaneous use of other drugs or changes in the amount of protein in plasma in various diseases should not have a significant impact on the kinetics of nicotine. Metabolism: Nicotine is metabolized in the liver, kidneys and lungs. Identified more than 20 metabolites that are inferior in activity to nicotine. The concentration of the primary metabolite - cotinine - is 10 times higher than the nicotine concentration. Withdrawal Excreted mainly in the liver. The average plasma clearance is about 70 l / h. T1 / 2 - about 2 hours. Cotinine (15% of the dose, T1 / 2 - 15-20 hours) and trans-3-hydroxy-cotinine (45% of the dose) are mainly excreted with urine. 10-30% of the dose of nicotine is excreted in the urine unchanged.Pharmacokinetics in special clinical situations: Progressive deterioration in renal function is accompanied by a decrease in the overall clearance of nicotine. The pharmacokinetics of nicotine does not change significantly in patients with cirrhosis of the liver with mildly impaired liver function (5 points on the Child-Pugh scale) and decreases in patients with cirrhosis of the liver with moderately expressed impaired liver function (7 points on the Child-Pugh scale). In patients on hemodialysis, an increase in plasma nicotine concentration was noted. In elderly patients, there is a slight decrease in total clearance of nicotine, which does not require dose adjustment.
For the treatment of tobacco addiction by reducing the need for nicotine: - reduction of withdrawal symptoms that occur when patients quit smoking completely — when temporarily quitting smoking — to reduce the number of cigarettes smoked by those who are unable or unwilling to completely give up from smoking.
- Hypersensitivity to nicotine and other components of the drug. With caution and only after consulting with a physician, the drug should be used in patients with impaired cardiovascular system, including suffered a cardiovascular disease within 1 month before the start of use (including stroke, myocardial infarction, unstable stenocardia, arrhythmia, coronary artery bypass surgery, angioplasty), or with uncontrolled arterial hypertension. With caution, the drug should be prescribed to patients with died or impaired liver function, severe renal failure, exacerbation of gastric ulcer and duodenal ulcer. With caution, use the drug in patients with uncontrolled tireozom, pheochromocytoma (due to the fact that nicotine induces the release of catecholamines from the adrenal medulla) and also diabetic.
Use during pregnancy and lactation
Nicotine penetrates the placental barrier and can have a negative effect on the fetus. Smoking can harm the fetus, so patients should try to be convinced about the need to quit smoking without using replacement therapy with nicotine-containing drugs.With the failure of such attempts, the decision to conduct therapy is taken after comparing the possible positive effect and potential harm. Nicotine in small quantities is excreted in breast milk, even when taken in therapeutic doses, and may have an adverse effect on an infant when taking the drug by a nursing mother. In order to reduce the negative effects of nicotine on a child, the drug Nicorette should be applied immediately after feeding and no later than 2 hours before the next feeding.
Dosage and administration
Depending on the severity of addiction to smoking, use Nicotette chewing gum with different concentrations of the active substance. If the patient smokes 20 or less cigarettes per day or smokes the first cigarette 30 minutes after waking up, you should use chewing gum with nicotine content of 2 mg. If the patient smokes more than 20 cigarettes per day or he could not quit using chewing gums with nicotine 2 mg, it is recommended to use chewing gum with a nicotine content of 4 mg. Nicorette should be used in all cases where there is an irresistible desire to smoke. The gum should be chewed slowly until a sharp taste appears, then chewing should be stopped and the gum should be placed between the gum and the inside of the cheek. After the disappearance of taste should resume chewing. For 1 reception, you should use only 1 chewing gum. In case of total cessation of smoking, the average daily dose is 8-12 gum, the maximum is 15 gum. It is necessary to continuously use the drug in the first 3 months after quitting. Then you should gradually reduce the number of consumed gum. When daily intake of the drug is reduced to 1-2 gum, its use should be discontinued. When reducing the number of cigarettes smoked, chewing gum should be used between smoking episodes to lengthen the intervals between smoking cigarettes to minimize cigarette consumption. The patient should be warned that if after 6 weeks of use of the drug it was not possible to reduce the daily consumption of cigarettes, you should consult a specialist doctor. The patient should try to quit smoking when he is ready for this, but no later than 6 months after starting treatment .If it was not possible to stop smoking within 9 months after the start of therapy, you should consult a specialist. It is not recommended to use Nicorette chewing gum for more than 12 months. However, some patients may need longer treatment to prevent a return to smoking or a previous level of tobacco consumption. Chewing gum can be used during periods when you need to temporarily stop smoking, for example, when you are in places where it is forbidden to smoke or in other situations when you need to refrain from smoking. Specialist consultations and psychological support contribute to the effectiveness of therapy. Use in combination with TTC (patch) Nicorette: If you can’t get about smoking can only be used when chewing gum is used, or if it is necessary to reduce the daily consumption of chewing gum due to local adverse reactions, Nikorette can be used in the form of a patch (TTC) along with chewing gum 2 mg. Initial therapy. Treatment should begin with a single patch of 15 mg / 16 h, which is placed every day on an intact skin area after waking up in the morning and removed before bedtime, in combination with 2 mg chewing gum. Apply at least 4 chewing gum 2 mg per day; 5-6 chewing gums are usually enough. Do not use more than 15 chewing gum per day. The full dose should be applied within 6-12 weeks, after which it should be gradually weaned off the drug. The withdrawal from the combination of drugs is carried out in two ways. The first method: using a lower dosage patch, i.e. use the patch 10 mg / 16 h for 3-6 weeks and then apply for 3-6 weeks the patch 5 mg / 16 h with the same number of chewing gum in 2 mg as in the initial therapy, and then gradually reducing the number of chewing gum 2 mg for 12 months. The second method is to stop the use of the patch and gradually reduce the number of chewing gum 2 mg for 12 months.
At the recommended dose, Nicorette does not cause serious adverse effects. At the beginning of treatment, the nicotine contained in chewing gum can sometimes cause mild throat irritation and increased salivation, and if an excessive amount of dissolved nicotine is swallowed, a hiccup is possible.With excessive use of the drug by persons who are not accustomed to inhaling tobacco smoke, nausea, weakness, and headache are possible (similar to the symptoms that occur in these patients when tobacco smoke is inhaled). From the side of the central nervous system: very often - headache; often dizziness. Since the cardiovascular system: sometimes - rapid heartbeat; very rarely - atrial rhythm disturbances. On the part of the digestive system: very often - gastrointestinal discomfort, hiccups, nausea; often - vomiting. Dermatological reactions: sometimes - erythema, urticaria. Others: very often - sore throat or mouth, pain in the masticatory muscles; rarely, allergic reactions, including angioedema. Some symptoms, such as dizziness, headache, sleep disturbances, can be manifestations of withdrawal caused by quitting smoking. When you quit smoking, the incidence of aphthous stomatitis may increase. When using chewing gum with a nicotine content of 4 mg in patients prone to indigestion, slight digestive disorders or heartburn are possible. Usually, this problem is eliminated by slower chewing gum or using gum containing 2 mg of nicotine (if necessary with a smaller interval).
Excessive intake of nicotine during replacement therapy and / or smoking can cause symptoms of overdose. Symptoms: nausea, increased salivation, abdominal pain, diarrhea, hyperhidrosis, headache, dizziness, hearing loss, and severe general weakness; when taking high doses of nicotine - hypotension, weak and irregular pulse, difficulty breathing, vascular collapse and generalized seizures, i.e. symptoms of acute nicotine poisoning. Doses of nicotine, which are well tolerated in the course of treatment by adult smokers, can cause symptoms of severe poisoning in young children and even be fatal. Treatment: Immediately stop taking nicotine and start symptomatic treatment. Activated carbon reduces the absorption of nicotine in the digestive tract. If necessary, artificial respiration and oxygen.
Interaction with other drugs
Smoking (but not the use of nicotine) causes an increase in CYP1A2 activity.After smoking cessation, a decrease in the substrate clearance of this enzyme can be observed, which can lead to an increase in the concentration of certain drugs in the blood plasma, which has potential clinical significance with the simultaneous use of drugs characterized by a narrow therapeutic range (theophylline, tacrine, clozapine, ropinirole). Limited evidence suggests that smoking may induce the metabolism of flekainida and pentazocine.
The use of the drug Nicorette is accompanied by a lower risk than smoking. The patient should be informed that he should wear a chewing gum with Nicorette with him in order to use it if he suddenly wants to smoke. Patients with diabetes after smoking cessation may require a decrease in insulin doses. Patients with impaired chewing function are encouraged to use other dosage forms. Use in pediatrics: Experience with Nicorette in adolescents younger than 18 years is absent, so the drug should be used strictly as prescribed by a doctor. Impact on ability to drive motor vehicles and control mechanisms: Negative impact on ability to drive a car and work with mechanisms has not been established.