NIKVITIN

Active material: Nicotine
When ATH: N07BA01
CCF: Drug for the treatment of nicotine addiction
ICD-10 codes (testimony): F17
When CSF: 02.17
Manufacturer: GlaxoSmithKline Consumer Healthcare (Great Britain)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

◊ Transdermal therapeutic system (TST) with a contact surface 7 cm²; a multilayer adhesive rectangular shape with nominal dimensions 2.5 cm × 2.8 cm; pinkish-bronze base color with markings “NCQ 7”; the downside silver, covered with a transparent removable protective film.

Excipients: EVA, polyethylene / aluminum / polyethylene terephthalate / ethylene vinyl acetate, polyethylene film, polyisobutylene 1 200 000 and 35 000, siliconized polyester film.

1 PC. – bags made of laminate (7) – cardboard boxes.
1 PC. – bags made of laminate (14) – cardboard boxes.

◊ Transdermal therapeutic system (TST) with a contact surface 15 cm²; a multilayer adhesive rectangular shape with nominal dimensions 3.4 cm × 4.4 cm; pinkish-bronze base color with markings “NCQ 14”; the downside silver, covered with a transparent removable protective film.

Excipients: EVA, polyethylene / aluminum / polyethylene terephthalate / ethylene vinyl acetate, polyethylene film, polyisobutylene 1 200 000 and 35 000, siliconized polyester film.

1 PC. – bags made of laminate (7) – cardboard boxes.
1 PC. – bags made of laminate (14) – cardboard boxes.

◊ Transdermal therapeutic system (TST) with a contact surface 22 cm²; a multilayer adhesive rectangular shape with nominal dimensions 4.65 cm × 4.75 cm; pinkish-bronze base color with markings “NCQ 21”; the downside silver, covered with a transparent removable protective film.

Excipients: EVA, polyethylene / aluminum / polyethylene terephthalate / ethylene vinyl acetate, polyethylene film, polyisobutylene 1 200 000 and 35 000, siliconized polyester film.

1 PC. – bags made of laminate (7) – cardboard boxes.
1 PC. – bags made of laminate (14) – cardboard boxes.

Pharmacological action

Drug for the treatment of nicotine addiction (smoking). Nicotine, the principal alkaloid of tobacco, – substance of natural origin. It is a nicotinic receptor agonist peripheral and central nervous system and have marked effects on the CNS and cardiovascular system.

When you stop smoking in dependent smokers may develop withdrawal, which is accompanied by a characteristic cravings, increased irritability, emotional lability, impaired concentration, anxiously, sleepiness, sleep disorders, Light physical disorders (headache, myalgia, constipation, fatigue) and increased appetite and / or weight gain. In some patients, symptoms of withdrawal, such as the craving to smoke, They can be alleviated by maintaining stable lower, than smoking, nicotine levels in plasma.

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

Clinical studies have shown, Nikvitin that relieves the symptoms of smoking cessation. In its application the severity of the urge to smoke decreased by no less than 35% regardless of the time of day for the first two weeks of failure, compared with the placebo group (p<0.05).

Pharmacokinetics

Absorption

After application of the patch to the skin a rapid percutaneous absorption of nicotine, released from the adhesive layer. The concentration of nicotine in the plasma reaches a steady level through 2-4 hours after the first application Nikvitina and remains constant during the 24 h until, until the patch will not be removed. About 68% Nicotine, released from the patch, reaches the systemic circulation, the remainder of the released nicotine evaporates through the plaster edge.

With continuous daily use of the preparation Nikvitin (superimposition on 24 no), stable nicotine dose-dependent plasma concentration achieved and maintained overnight at a second application Nikvitina. These resistant to maximal concentration of about 30% higher, than after the first application of the preparation.

nicotine plasma concentrations are proportional to the dose of the three options Nikvitina dosage.

Average steady plasma concentration was approximately 17 ng / mL for patch 21 mg / day, 12 ng / mL for patch 14 mg / day 6 ng / mL for patch 7 mg / day. For comparison, cigarette smoking provides for half an hour average concentration of nicotine in the plasma of about 44 ng / ml.

Said earlier peak blood levels of nicotine, observed when inhaled in cigarette smoke, It is not observed when using Nikvitina.

Distribution

After removal of the patch Nikvitin nicotine concentrations in plasma are reduced, with a clear half-life 3 no, due to the continued absorption of nicotine in the cutaneous site; for comparison, at / in a half-life of 2 no. Through 10-12 hours after removing the patch at the non-smoking patients the presence of nicotine in the blood has not revealed.

The on / in the introduction of the radioactive isotope is observed nicotine dose distribution in accordance with the blood flow, without selective capture by an authority. V_d is approximately 2.5 l / kg.

Metabolism

metabolized, primarily, liver; plasma clearance averages 1.2 l / min; kidney and lung also metabolise nicotine.

Identified more 20 nicotine metabolites. It is believed, that they are pharmacologically inactive. The main metabolites – cotinine and trans-3-gidroksikotinin. Stable cotinine concentrations exceed those of nicotine 10 time. T_1/2 Nicotine is approximately 1-2 no, and cotinine – 15-20 no.

Deduction

And nicotine, and its metabolites are excreted through the kidneys, about 10% Nicotine in unchanged form excreted in the urine. About 30% It can appear in the urine at the maximum filtration and complete oxidation of urine (pH<5).

Pharmacokinetics in special clinical situations

Differences in nicotine kinetics in men and women in the application of Nikvitina not observed. Obese men when applying Nikvitina marked significantly lower rates of AUC and C_max compared to those of men with normal body weight. Linear regression of AUC against total body weight showed the expected dependence (AUC decreases with increasing mass).

In applying the drug to the upper body and the upper outer part of the arm of nicotine kinetics were similar.

Testimony

- to relieve nicotine withdrawal symptoms, incl. craving for cigarettes for smoking cessation.

Possibly, smoking cessation, in parallel with Nikvitina must be a certain way to change life style.

Dosage regimen

Before initiation of therapy the patient must come to a firm decision to quit.

During the period of failure any attempt to smoking can cause a relapse. Therefore, smoking is not recommended during treatment. It should not be in parallel use other nicotine-containing products. appropriate psychological support is recommended in order to better achieve the desired result.

Adults (including the elderly) it is recommended to impose plaster Nikvitin 1 time / day, at the same time, preferably immediately after lifting. area of ​​skin to overlay patch should be clean, dry and free of hair. After applying the patch must be on 10 s press tightly against the palm. The patch can not be imposed on the affected, reddened or irritated skin. Do not apply to areas of skin folds.

Nikvitin patch should be applied immediately after removal from the bag. Do not shoot for the day. Through 24 h used patch is removed. New impose on another skin. Leave the same patch on the skin more 24 h and apply the patch on the same area of ​​skin, at least, in a week, must not. It can be applied simultaneously, and only wear one patch.

When desired, the patch can be removed before bedtime. However, to reduce the urge to smoke the morning is recommended to wear it for 24 no.

Nikvitinom treatment begins with the application of the patch 21 mg / day and decrease according to the following scheme:

light smokers (who smoke less 10 cigarettes a day) it is recommended to start with 2 Phase (14 mg) on 6 weeks and decrease the dose to 7 mg 2 of the week (Total 8 weeks).

In applying Nikvitina 21 mg / day, in the event of significant side effects, do not pass within a few days, dose should be reduced to 14 mg / day and to continue treatment with this dose until the end of 6 weeks, then go on to use the drug in a dose of 7 mg / day for 2 weeks. If symptoms persist, Talk to your doctor.

To achieve optimum results should fully carry out the 10-week course of treatment (or 8 weeks for light smokers and patients, which reduced dose for the reasons, the above).

The maximum duration of treatment – 10 weeks. Exceeding the course it is not recommended due to the risk of nicotine addiction or toxic reactions.

In the absence of the desired result or return to smoking, later, the course may be repeated.

Side effect

In applying Nikvitina can have side effects, similar to those in the introduction of nicotine into an organism by any means, incl. and by smoking. They are related to the pharmacological effects of nicotine, some of which are dose-dependent. When applied at recommended doses Nikvitina serious side effects were not recorded. When applied in doses Nikvitina, exceeding recommended, smokers, that when smoking is not tightened, there is the risk of nausea, weakness and headache.

Individuals, Quit smoking (different ways), may be such phenomena as asthenia, headache, dizziness, sleep disorders, cough, or flu-like symptoms. Such reactions like depression, irritability, anxiety, mood variability, anxiety, dremota, impaired concentration, insomnia may be related to withdrawal symptoms as a result of smoking cessation.

The most frequent adverse reactions when applying Nikvitina are reactions at the overlay patch.

The following side effects have been reported in clinical trials revealed spontaneously or.

Side effects are classified according to organ system and frequency. The frequency of side effects is defined as follows:: Often (≥ 1/10), often (≥1 / 100 and < 1/10), sometimes (≥ 1/1000 and < 1/100), rarely (≥ 1/10 000 and <1/1000) and very rare ( < 1/10 000).

On the part of the immune system: sometimes – hypersensitivity; rarely – anaphylactic reactions.

CNS: Often – sleep disorders, including abnormal sleep and insomnia, headache, dizziness; often – nervousness, tremor.

Cardio-vascular system: often – palpitation (palpitation); sometimes – tachycardia.

The respiratory system: often – breathlessness, pharyngitis, cough.

From the digestive system: Often – nausea, vomiting; often – dyspepsia, stomach ache, diarrhea, dry mouth, constipation.

Dermatological reactions: often – increased perspiration; rarely – atopic dermatitis, contact dermatitis, photosensitivity.

On the part of the musculoskeletal system: often – arthralgia, myalgia.

From the body as a whole: often – chest pain, pain in the extremities, pain at the site of patch application, asthenia, fatigue; sometimes – malaise, flu-like symptoms.

Local reactions: Often – transient rashes, itch, burning, pricking, numbness, edema, pain and urticaria. Most local reactions are mild severity and pass quickly after removal of the patch. There may be pain or a feeling of heaviness in the limbs, or in place of overlay patch.

Contraindications

- myocardial infarction (shortly before treatment);

- unstable or progressive angina;

- Prinzmetal angina;

- severe cardiac arrhythmia;

- recent cerebrovascular disease;

- Hypersensitivity to the drug.

Nikvitin plaster should not be applied to non-smokers people, irregular smokers and children.

Pregnancy and lactation

Adverse effect of nicotine on the health of the mother and fetus are already installed. A reduction in body weight, increased risk of spontaneous abortion and fetal death in the perinatal period. There have been reports of spontaneous abortion during the application Nikvitina. Nikvitin can not be excluded from the number of impact factors.

Patients should be advised to quit smoking, without applying therapeutic nicotine replacement system, but if this is not possible, it is necessary to evaluate the risk / benefits of using Nikvitina.

Cautions

When smoking or use an additional source of nicotine during use Nikvitina there is a possibility of adverse effects due to the growth level of nicotine, substantially greater than that only by smoking or use of other nicotine preparations.

There are reports of the development of tachycardia during treatment with Nikvitina.

Before applying Nikvitina medical consultation is required in cases where there is:

- cardiovascular diseases (stable angina, heart failure, cerebrovascular diseases, vasospastic diseases, severe peripheral vascular disease);

- uncontrolled hypertension, since nicotine may be a risk factor for the development of malignant hypertension;

- atopic or eczematous dermatitis (the likelihood of local hypersensitivity to the patch);

- severe dysfunction of kidney and liver, active peptic ulcer;

- hyperthyroidism, pheochromocytoma or insulin-dependent diabetes mellitus.

In case of severe or persistent local reactions at the application site (vyrazhennnaya erythema, itch, edema) or generalized skin reaction (hives, rash or generalized skin rash), Nikvitin should be discontinued and consult a doctor.

Patients with contact sensitization should be borne in mind the possibility of the reactions expressed by smoking or parallel application of other nicotine-containing products.

Precautions should be used drug in renal failure and severe moderate, as nicotine or its metabolites clearance may be reduced, potentially increasing the risk of side effects.

Precautions drug should be used in severe to moderate hepatic insufficiency, as nicotine or its metabolites clearance may be reduced, potentially increasing the risk of side effects.

Regardless of the use of nicotine-replacement therapy in smoking cessation blood glucose limits may be more variable, so it's important, to diabetics continued blood glucose monitoring using patch Nikvitin. Patients, hospitalized for myocardial infarction, severe arrhythmias, or stroke, in unstable hemodynamic better use of non-pharmacological methods of smoking cessation.

If no result can be considered the possibility of using the patch Nikvitin, but due to limited data on the safety of the drug in these patients therapy should be initiated only under medical supervision. After discharge, patients can use nicotine replacement therapy alone.

In the event of clinically significant amplification reactions on the part of the cardiovascular system or other symptoms, associated with the use of nicotine, necessary to reduce the dose or stop Nikvitin.

If redness, edema or skin rashes, not passing over 4 days, or generalized skin reactions, you must stop using the product and consult a doctor. The probability of these reactions is higher in those with a history of dermatitis. Avoid contact patch with the mucous membranes of the eyes and nose. After application it is necessary to wash your hands with water only, as soap can enhance the absorption of nicotine.

Use in Pediatrics

Data on safety and efficacy in children and adolescents with no smokers. Application Nikvitina in children is not recommended. Use in Adolescents (aged 12-17 years) It is possible only after consultation with your doctor.

The amount of nicotine, which is well tolerated by adult smokers, can cause poisoning, death or, when used in children, incl. random. Even after using the patches contain enough nicotine, to cause adverse effects on children's health.

Effects on ability to drive vehicles and management mechanisms

Nikvitin not affect the ability to drive and use sophisticated technology.

Overdose

Cases ingestion or simultaneous use of various known dosage forms Nikvitina.

Symptoms overdose Nikvitinom same, as well as in cases of poisoning by nicotine: paleness, cold sweat, nausea, salivation, vomiting, abdominal pain, diarrhea, headache, dizziness, hearing and visual impairment, tremor, weakness, confusion, hypotension; in case of reception of nicotine in too high dose may prostration, convulsions, expressed respiratory disorders and, more rarely, disorders of the cardiovascular activity, hypotension.

Treatment of overdoses when applied topically: in case of overdose or the appearance of symptoms of overdose you should immediately remove the patch. You should immediately seek medical help. skin, on which there was a patch, rinse with water and dry; apply soap is not recommended, tk. it can enhance the absorption of nicotine. It will be appreciated, that the absorption of nicotine in the blood will continue for several hours after removal of patch, It formed as a depot in the skin.

Treatment of overdose by swallowing: when ingested patch patient should be given activated charcoal, since allocation of nicotine in the gastrointestinal tract will continue for a few hours, then seek medical advice.

Treatment of nicotine poisoning: appointment of diazepam or barbiturates – for the relief of cramps, atropyna – for the prevention of bronchial hypersecretion and diarrhea, respiratory analeptics and in / in a sufficient amount of infusion solutions – for the prevention of arterial hypotension and collapse.

Drug Interactions

Smoking cessation, with the use of nicotine replacement therapy or without, can change the effect of the administered drugs. Dosage adjustment may be required for the following drugs:

Conditions of supply of pharmacies

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

Conditions and terms

The drug should be stored only in the reach of children at a temperature not higher than 25 ° C. Shelf life – 3 year.