Expiration date: 10/2025
The composition and form of issue:
Transdermal therapeutic system (patch) 7 mg/cm2 7 days
active substance: nicotine 36 mg
(which ensures intake of 7 mg of nicotine over 24 hours)
§Transdermal therapeutic system (patch) 14 mg/day 15 cm2
active substance: nicotine 78 mg
(which ensures intake of 14 mg of nicotine over 24 hours)
§Transdermal therapeutic system (patch) 21 mg/day 22 cm2
active substance: nicotine 114 mg
(which provides that the intake of 21 mg of nicotine over 24 hours)
auxiliary substances: copolymer of ethylene and vinyl acetate, polyethylene/aluminium/polyethylene terephthalate/a copolymer of ethylene and vinyl acetate, PE film, polyisobutylene 1200000 and 35000 siliconised polyester film
bags from laminate 1 PC. in cardboard box for 7 or 14 sachets.
Description pharmaceutical form:
Patch 7 mg/day: layered, rectangular in shape, the base pinkish-bronze color marking NCQ 7, the underside is silver, covered with a transparent protective film remove the nominal dimensions of 2.5 × 2.8 cm
Patch 14 mg/day: layered, rectangular in shape, the base pinkish-bronze color marking NCQ 14, the underside is silver, covered with a transparent protective film remove the nominal dimensions are 3.4 × 4.4 cm.
Patch 21 mg/day: layered, rectangular in shape, the base pinkish-bronze color marking NCQ 21, the underside is silver, covered with a transparent protective film remove the nominal dimensions of 4.65 x 4,75 cm
Pharmacokinetics:
Absorption
After application of the patch to the skin is the rapid percutaneous absorption of nicotine released from the adhesive layer. The concentration of nicotine in plasma reaches a stable level 2-4 hours after first application Niquitin and remains constant for 24 h to until the patch is released. Approximately 68% of the nicotine released from the patch into the blood system, the remaining part of the released nicotine evaporates through the edges of the patch.
With continuous daily use of the drug Niquitin (laying 24 hours), dose-dependent steady concentration of nicotine in plasma achieved and maintained during the day when the second application Niquitin. These sustainable Cmax approximately 30% higher than after the first treatment. Concentration of nicotine in plasma is proportional to dose three dosage options Niquitin. Average steady plasma concentration is approximately 17 ng/ml for the patch 21 mg/day, 12 ng/ml for the patch 14 mg/day and 6 ng/ml for the patch 7 mg/day. For comparison, Smoking cigarettes for half an hour gives the average concentration of nicotine in the plasma of about 44 ng/ml.
The previously reported peak levels of blood nicotine observed in cigarette smoke, is not marked in the application Niquitin.
Distribution
After removing the patch Niquitin concentration of nicotine in plasma are reduced with a clear half-life of 3 hours due to continued absorption of nicotine in the skin area. For comparison, the on/in the introduction of the half-life is 2 h. after 10-12 hours after removing the patch from non-Smoking patients nicotine in the blood is not detected.
The on/in the introduction of a radioactive isotope of nicotine observed the dose distribution in accordance with the blood flow, without the selective capture of any authority. Vd nicotine is about 2.5 l/kg.
Metabolism
The primary organ of elimination — the liver, the plasma clearance is in average 1.2 l/min kidneys and lungs also metaboliziruet nicotine. Identified more 20 metabolites of nicotine. It is believed that all of them are pharmacologically inactive. The main metabolites of cotinine and TRANS-3-hydroxycotinine. Stable concentrations of cotinine higher than those of the nicotine in 10 times. The half-life of nicotine is approximately 1-2 hours, and cotinine 15-20 hrs
Excretion
And nicotine, and its metabolites are excreted through the kidneys approximately 10% of the nicotine in unchanged form excreted in the urine. About 30% may appear in the urine when maximum filtration and a significant acidification of urine (pH<5). p="">
The difference in the kinetics of nicotine in men and women in the application Niquitin was not observed. In obese men, the application Niquitin showed significantly lower AUC and Cmax as compared to those in men of normal weight. Linear regression of AUC as compared to the total body weight showed the expected dependence (AUC decreases with increasing weight). In applying the drug on the upper body and upper outer arm kinetics of nicotine were odinakovoi.
Description pharmacological action:
Nicotine, the main alkaloid of tobacco, is a substance of natural origin. It is an agonist of nicotinic receptors in the peripheral and Central nervous system and has a pronounced effect on CNS and CVS. When quitting in dependent smokers may develop the syndrome, which is accompanied by the typical urge to smoke, increased irritability, emotional lability, impaired concentration, anxiety, sleepiness, sleep disturbance, mild somatic disorders (headache, myalgia, constipation, fatigue) and an increase in appetite and/or weight gain. In some patients, withdrawal symptoms such as craving, can be alleviated by maintaining a stable lower than when Smoking, the nicotine levels in plasma.
In the treatment of tobacco dependence replacement therapy nicotine reduces the number of cigarettes smoked, reduces the severity of withdrawal symptoms that occur when the full stop Smoking those, who have decided to quit Smoking facilitates temporary abstinence from Smoking and also helps to reduce the number of cigarettes smoked among those who can not or do not want to completely give up Smoking.
Clinical studies have shown that Niquitin eases the withdrawal symptoms of Smoking. In its application the severity of the urge to smoke has decreased at least 35%, regardless of time of day, during the first two weeks of failure compared with the placebo group (p<0.05). p="">
Indications:
Niquitin shown to relieve the symptoms of nicotine withdrawal, including cravings for cigarettes when quitting Smoking. With Smoking cessation, in conjunction with the use Niquitin, you need some way to change the style of life.
Contraindications:
- hypersensitivity to the drug
- myocardial infarction in history (shortly before the treatment)
- unstable or progressive angina
- Prinzmetal's angina
- severe cardiac arrhythmia
- recent cerebrovascular disease.
Niquitin the patch should not be applied to people non-smokers, irregular smokers and children.
Application of pregnancy and breast-feeding:
Harmful effects of nicotine on maternal health and the fetus is already installed. Such effects include: weight loss, increased risk of spontaneous abortion and fetal death in the perinatal period. There are reports of spontaneous abortion during the application Niquitin. Niquitin cannot be excluded from a number of factors. Patients should be encouraged to quit Smoking without using therapeutic system, substitution of nicotine, otherwise it is necessary to evaluate the risk/benefits of using Niquitin.
Side effects:
When applying Niquitin can be side effects are similar to those for introduction of nicotine into the body by any means, including by Smoking. They are associated with the pharmacological effects of nicotine, some of which are dose-dependent. When applying Niquitin in recommended doses, serious side effects were not registered. When applying Niquitin in doses, exceeding recommended, in smokers, that when Smoking is not delayed, there is a likelihood of nausea, weakness and headaches.
In individuals quit Smoking (through various means), there may be symptoms such as asthenia, headache, dizziness, sleep disturbances, cough, or flu-like symptoms.
Reactions such as depression, irritability, nervousness, anxiety, mood volatility, anxiety, drowsiness, weakened concentration, insomnia may be associated with a withdrawal syndrome due to the cessation of Smoking.
The most common adverse reactions in the application Niquitin are reactions in the overlap area of the patch.
The following side effects have been reported in clinical trials or spontaneously revealed.
Side effects classified according to organ system and frequency. The frequency of side effects is defined as follows: very common (&ge1/10) frequently (&GE. 1/100 and <1 10="" ge1="" 1000="" 1="" 100="" 000="" p="">
The immune system: sometimes — hypersensitivity very rare — anaphylactic reactions.
Psychiatric disorders: very often — sleep disturbances, including abnormal sleep and insomnia is often anxiety.
From the nervous system: very often — headache, dizziness and often tremor.
From the CCC: often — palpitations (palpitation) and sometimes tachycardia.
The respiratory system: often — shortness of breath, pharyngitis, cough.
From the blood: very often — nausea, vomiting often dyspepsia, abdominal pain, diarrhea, dry mouth, constipation.
The skin and subcutaneous tissue: often — increased sweating very rarely — allergic dermatitis, contact dermatitis, photosensitivity.
From the side of musculoskeletal system: often — artralgia, myalgia.
Common reactions: often — pain in the chest, pain in the extremities, pain at the site of application of the patch, asthenia, fatigue and sometimes malaise, flu-like symptoms.
Local reactions: very often — adverse reactions in the overlap area of the patch, including transient rash, itching, burning, tingling, numbness, swelling, pain and urticaria.
Most local reactions have low severity and quickly pass after the removal of the patch. There may be pain or a feeling of heaviness in the limbs or in the overlap area of the patch (e.g. on the chest).
In case of serious and persistent local reactions at the site of application (e.g. erythema, pruritus or edema) or reactions of an organism in General (for example, urticaria or rash), the patient should stop the use of Niquitin and consult with your doctor.
In the event of clinically significant amplification reactions from the CCC or other reactions related to the administration of nicotine, the dose Niquitin should be reduced or stop taking the drug.
Drug interactions:
Quitting Smoking, using nicotinecontaining therapy or without it, can change the effect of the applied drugs. Dose adjustment may be required to forth in the table drugs.
| The adjustments | Drugs requiring dose adjustment | Possible mechanism of action |
| Dose reduction | Caffeine, theophylline, imipramine, pentazocine, phenacetin, phenylbutazone, tacrine, clomipramine | The decrease in the activity of liver enzymes |
| Insulin | The increased subcutaneous absorption of insulin | |
| Blockers (prazosin, propranolol) | Decrease circulating catecholamines | |
| Higher doses | Adrenergic agonists (isoprenaline, salbutamol) | Decrease circulating catecholamines |
Method of application and dose:
Before therapy the patient is required to come to a firm decision to quit Smoking.
During the period of refusal of any attempt Smoking can cause a relapse. Therefore, during the course of treatment to Smoking is not recommended. You should not in parallel use other nikotinsoderzhaschie products. For more successful achievement of the desired result it is recommended that appropriate psychological support.
Adults (including elderly). Patch Niquitin to apply 1 time a day, at the same time, preferably immediately after waking up. The area of skin for application of plaster shall be clean, dry and free from hair. After applying the patch you need for 10 with tight squeeze with his hand. Niquitin the patch should be applied immediately after removal from the bag.
Not to shoot during the day.
The patch cannot be applied on damaged, reddened or irritated skin. Not to impose on areas of the skin folds.
After 24 hours the used patch is removed. New applied to another area of the skin. Leave the same patch on the skin for more than 24 hours and apply the patch to the same skin area at least during the week, it is impossible. Simultaneously you can apply and wear only one patch.
If desired, the patch can be removed before bedtime. However, to reduce morning cravings for Smoking, it is recommended to wear it for 24 hours
Treatment Nikitina start with 21 mg and reduce according to the following scheme:
| Stage | Niquitin, mg | Duration, weeks |
| 1 | 21 | The first 6 |
| 2 | 14 | The following 2 |
| 3 | 7 | The last 2 |
Light smokers (who smokes <10 2="" 14="" 6="" 7="" 8="" p="">
When using Niquitin 21 mg, in case of occurrence of important side effects (see "Contraindications") that does not pass within a few days, decrease dose to 14 mg/day. It should continue until the end of the 6 weeks, and then go to the dose of 7 mg for 2 weeks. If symptoms persist, consult a doctor.
For optimal result it is recommended to complete the 10-week course of treatment (or 8 weeks for light smokers and patients who reduced dose for the reasons mentioned above).
The maximum duration of treatment — 10 weeks. The excess rate is not recommended due to the risk of developing nicotine addiction or toxic reactions.
In the absence of the desired result or return to Smoking, later the course may be repeated.
Overdose:
Cases of ingestion or simultaneous use of different dosage forms Niquitin unknown.
The symptoms are the same as with nicotine poisoning: pallor, cold sweat, nausea, salivation, vomiting, abdominal pain, diarrhea, headache, dizziness, impaired hearing and vision, tremor, weakness, confusion, hypotension.
In case of overdose small dose of nicotine possible: prostration, convulsions, severe respiratory and, in rare cases, cardiovascular activity, hypotension.
Treatment of overdose in the local application. In case of overdose, or symptoms of overdose you should immediately remove patch. You should immediately seek medical help. The area of the skin, which was a band-aid, rinse with water and wipe. Apply soap should not be, because it can increase the absorption of nicotine. It should be borne in mind that the absorption of nicotine into the bloodstream will continue for several hours after removing the patch, because the skin is the depot.
Treatment of overdosage as a result of ingestion. In case of ingestion of the patch to the patient should be given activated charcoal, because the release of nicotine in the blood will continue for several more hours. To go to the doctor.
Treatment of poisoning by nicotine. Symptomatic therapy includes the appointment of diazepam or barbiturates for relief of seizures, atropine for prevention of bronchial hypersecretion and diarrhea, respiratory analeptics and transfusion of adequate amounts of fluid for prevention of hypotension, and collapse.
Precautions:
If you smoke or use any source of nicotine during the application Niquitin there is a likelihood of side effects as a result of growth of nicotine level, significantly exceeding that only when Smoking or using other nicotine products. In the case of a clinically significant gain reactions from the CCC or other symptoms associated with the use of nicotine, it is necessary to reduce the dose or stop Niquitin. Also, you may need a dose adjustment parallel to the prescribed drugs (see "Interactions").
There are reports of the development of tachycardia on the background of primenena Niquitin.
Before applying Niquitin doctor's consultation is mandatory in case of:
- cardiovascular diseases (stable angina, heart failure, cerebrovascular disease, vasospastic disease, severe pathology of the peripheral vessels)
- uncontrolled hypertension because the nicotine may be a risk factor for development of malignant hypertension
- atopic or eczematous dermatitis (the possibility of local hypersensitivity to the patch)
- severe renal dysfunction and liver, active peptic ulcer
- hyperthyroidism, pheochromocytoma, or insulinnezavisimogo of diabetes.
In the case of severe or persistent local reactions at the application site (vyrazhennaya erythema, itching, oedema) or a generalised skin reaction (hives, rashes or generalized skin rash) Niquitin should cancel and consult with your doctor.
Patients with contact sensitization should be aware of the possibility of the development of pronounced reactions when Smoking or concurrent use of other nikotinsoderzhaschie products.
Children. Data on safety and efficacy in children and adolescents-smokers no. Application Niquitin in children is not recommended. Use in adolescents (aged 12-17 years) is possible only after consultation with your doctor.
The amount of nicotine, which is well tolerated by adult smokers can cause poisoning or even fatal, when used in children, including accidental. Even after use, a patch contains enough nicotine to cause adverse effects on the health of children.
The drug should be stored only in places inaccessible to children.
Renal failure. The drug needs with caution used in patients with severe and moderate renal impairment as the clearance of nicotine or its metabolites may be reduced, which potentially increases the risk of side effects.
Liver failure. The drug needs with caution used in patients with severe and moderate hepatic impairment as the clearance of nicotine or its metabolites may be reduced, which potentially increases the risk of side effects.
Diabetes. Regardless of the application nicotinamidase therapy (NRT) in the period of quitting the borders of the level of glucose in the blood may be more variable, so it is very important that diabetic patients continued to monitor blood sugar level when you use the patch Niquitin.
Patients hospitalized for myocardial infarction, severe arrhythmias or stroke, with an unstable hemodynamic ispolzovanpokoleniya better methods of quitting Smoking.
If no result can be considered the application of the patch Niquitin, but due to the limited data on the safety of the drug in this group of patients, therapy should be initiated only under medical supervision. After discharge, patients may use NRT on their own.
In the case of a clinically significant gain reactions from the CCC or other symptoms associated with the use of nicotine, it is necessary to reduce the dose or stop Niquitin.
With redness, skin edema or rash, do not pass within 4 days, or at generalizovanny skin reactions, you must stop using the product and seek the advice of a physician. The probability of these reactions is higher in people with dermatitis in history.
Avoid contact with the eyes and nose. After application wash hands with water alone, since soap may increase nicotine absorption.
