Nicorette - instructions for use, dose, side effects, contraindications

Excipients: propylene glycol 150.0 mg / ml, ethanol 97.0 mg / ml, trometamol 40.5 mg / ml, noloxamer 40.0 mg / ml, glenzerol 25.0 mg / ml, sodium hydrogen carbonate 14, 3 mg / ml, levomenthol - 10.0 mg / ml, mint flavor QL24245 - 4.0 mg / ml, flavoring Cooler 2 SN046680 3.0 mg / ml, sucralose 1.5 mg / ml, acesulfame potassium 1.5 mg / ml, hydrochloric acid 10% sufficient to pH 9, water sufficient to 1 ml.

Description:

from colorless to light yellow color, a clear or slightly opalescent solution with the smell of mint.

Pharmacotherapeutic group:a remedy for the treatment of nicotine addiction.

ATX: & nbsp

N.07.B.A Drugs used in nicotine addiction

N.07.B.A.01 Nicotine

Pharmacodynamics:

Nicotine is an agonist of nicotinic receptors in the peripheral and central nervous system (CNS), has a pronounced effect on the central nervous system and the cardiovascular system.

Clinical studies have shown that drugs for nicotine replacement therapy allow smokers to refrain from smoking by facilitating

withdrawal symptoms. Compared with nicotine gum or dissolving tablets, the absorption of nicotine from the spray for topical use is quicker (see the section "Pharmacokinetics") and, based on the accumulated experience with the use of nicotine replacement therapy, this leads to a faster reduction in traction and other symptoms.

Increased appetite is a well-known symptom of the "withdrawal" of nicotine, often after the cessation of smoking, there is an increase in body weight.

Pharmacokinetics:

The pharmacokinetics of nicotine has been extensively studied; it was found that the way the substance is delivered to the body has a significant effect on the speed and degree of absorption.

The pharmacokinetics of the topical spray was studied in four studies, including 141 subjects.

Suction

The medicinal form of the sherd for topical application assumes that the dose of nicotine comes immediately and, as a consequence, its absorption from the oral cavity is rapid: according to studies, the absorption of nicotine from the spray for topical application occurred after 2 minutes (at the first time point).

A maximum concentration of 5.3 ng / ml is achieved within 13 minutes after the administration of 2 mg nicotine. 10 minutes after application of the spray at doses of 1 and 2 mg, the area under the concentration-time curve (AUC) exceeded the similar values obtained in studies of chewing gum and tablets containing 4 mg of nicotine (0.48 and 0.64 chhig / ml vs. 0.33 and 0.33 chihg / ml). Values AUG, indicate that the bioavailability of nicotine with spray application is slightly higher than with nicotine chewing gum or tablets. AUC, For a spray of 2 mg, the dose was 14.0 ccg / ml compared to 23.0 ccg / ml for a chewing reznik with 4 mg dosage and 26.7 ccg / ml for tablets with a dosage of 4 mg.

The average equilibrium concentration of nicotine in the blood plasma, achieved after the administration of the maximum dose (i.e., 2 sprays injected at a dose of 1 mg every 30 minutes), was approximately 28.8 ng / ml compared to 23.3 ng / ml with a chewable gum with a dosage of 4 mg (1 pillow every hour) and 25.5 and g / ml for nicotine tablets with a dosage of 4 mg (1 tablet every hour).

Taking into account the rapid absorption and similar high relative bioavailability, most of the nicotine released from the spray is absorbed, obviously, through the mucous membrane of the cheeks.

Distribution

The volume of distribution after intravenous injection of nicotine is from 2-3 l / kg.

The binding of nicotine to plasma proteins is less than 5%. For this reason, changes in the binding of nicotine with the use of concomitant drugs or changes in the content of plasma proteins in a number of diseases are not supposed to exerta significant effect on the pharmacokinetics of nicotine.

Biotransformation

Metabolism and excretion of nicotine do not depend on the dosage form, therefore the results of the study of nicotine with intravenous administration are suitable for their description.

The main body that eliminates nicotine, is the liver. Nevertheless, nicotine also metabolized in the kidneys and lungs. More than 20 nicotine metabolites are known, all of which are apparently less active than the parent compound.

The plasma half-life of the main metabolite of nicotine - coti pin - is 15-20 hours, and its concentration exceeds that for nicotine by 10 times.

Excretion

The average plasma clearance of nicotine is 70 liters / hour, the period of nil excretion is 2-3 hours.

The main metabolites of nicotine found in urine are cotinne (12% of the administered dose) and trans-3-hydroxycotinin (37% of the administered dose). Approximately 10% of nicotine is excreted in the urine unchanged. At high filtration rates and urine pH below 5 with urine, up to 30% of unchanged nicotine can be excreted.

Linearity / non-linearity

At 1, 2, 3 and 4 pressures of the spray with a dosage of 1 mg / dose, only a slight deviation from linearity AUC, and C_max.

Special patient groups

Impaired renal function

Progression of renal failure is accompanied by a decrease in overall nicotine clearance. The nicotine clearance in patients with severe renal impairment is reduced by an average of 50%. Patients on hemodialysis had an increase in nicotine concentration.

Impaired liver function

The pharmacokinetics of nicotine did not change in patients with mild violations of the liver function (5 on the Child-New scale), but in the presence of a malfunction of the liver of an average degree (7 on the Child-Pyo scale) was reduced by 40-50%. Data on the pharmacokinetics of nicotine for violations of liver function greater than 7 on the Child-Pugh scale are not available.

Elderly patients

In healthy elderly patients there was a slight decrease in total nicotine clearance, which does not require a change in the dose of the drug.

Indications:

Nicorette® Spray facilitates and (or) prevents cravings for smoking and withdrawal symptoms arising from tobacco dependence. It is shown as support for smokers who are willing to quit smoking or reduce the number of cigarettes smoked before full refusal; for the promotion of smokers who do not want to smoke or, in the absence of such a possibility; and as a safer alternative to smoking smokers and their surrounding people.

Spray Nicorette® is indicated for pregnant and lactating women trying to quit smoking.

Contraindications:

- Hypersensitivity to nicotine or other components of the drug.

- Children under 18 years.

Pregnancy and lactation:

Quitting smoking is the single most effective intervention for improving the health of both the pregnant woman and her child. Early quitting is the best option. Ideally, smoking cessation during pregnancy should be carried out without substitution nicotine therapy (31 GG). However, if a woman is not able (or is expected) to give up smoking without pharmacological support, ZIT is used because the risk to the fetus is less than when smoking tobacco. The best option is to completely stop smoking, but if it is unreachable, Nicoretts® spray can be used as a safer alternative to smoking during pregnancy. Due to the presence of potential non-nicotine periods, dosage forms for periodical use are preferred, however, with significant nausea and / or vomiting, patches may be required.

Breast-feeding

The relatively small amounts of nicotine found in breast milk with ZMT are less harmful to a child than passive smoking. Medicinal forms for periodic application minimize the content of nicotine in breast milk and allow breastfeeding with the lowest concentration of nicotine in it.

Dosing and Administration:

Place, for the oral cavity.

The patient should do everything possible to finally quit smoking while treating Nicorette® with spray.

Behavioral therapy, counseling and support, as a rule, increase the success of therapy.

Adults and teenagers over 18 years of age

Spray Nicorette® should be used at a time when there is an irresistible desire to smoke. After filling the container, bring the tip of the spray as close as possible to the open mouth. Click on the dispenser from above, thus releasing one dose of the drug into the oral cavity; avoid getting the spray on the lips. To prevent the ingress of the substance into the respiratory tract, do not inhale when you press the dispenser. For best results, swallow saliva for a few seconds after the injection.

During the use of the spray, the intake of food and liquid is not recommended.

Do 1 or 2 injections in a period of time, when you usually smoke a cigarette, and also in case of a craving for smoking. If, after a single injection, the craving for smoking does not decrease for a few minutes, the second injection should be performed. If two doses are required, the subsequent application of the spray can consist of 2 consecutive injections. Most smokers require the use of spray 1-2 doses every 0.5-1 hours. Every hour, allowed to take no more than 4 dosage injections spray. Do not inject more than 2 doses simultaneously spray fire apply more than 64 doses throughout the day (or 4 doses per hour for 16 hours).

Each bottle contains at least 150 injections.

Spray Nicorette® should be used in all cases of smoking cravings or to avoid draft in situations that can provoke it. Smokers who want to fire able to quit smoking immediately, should immediately replace the smoking of cigarettes spray Nikorette® and as soon as possible, reduce the number of injections to their complete cessation.

Smokers who want to reduce the number of cigarettes smoked,should use a spray for topical use as needed between episodes of smoking in order to increase the time intervals between smoking and with the aim of reducing smoking as much as possible.

As soon as the preparedness is felt, smokers should aim at a complete cessation of smoking.

Behavioral therapy, counseling and support, as a rule, increase the success of therapy. Those who managed to quit smoking, but it is difficult to give up the spray for topical application, it is recommended to consult a doctor for medical help.

Adolescents under the age of 18

It is not recommended to use the drug for people under 18 years of age. The experience of treatment of adolescents under the age of 18 years is absent.

Instructions for use

How to open the spray dispenser / unblock the nozzle

1. With your thumb, slowly lower the dispenser button downward, as shown in figure (a) until you can press the button inwards.

2. While pressing the button, lift the dispenser upwards. Release the button.

When using the spray for the first time you should check the operation of the sprayer. Take the bottle in such a way that the jet was directed at a distance from you, other people, children and pets.Open the spray gun and press 3 times until a small spray appears.

If you do not use the spray for 2 days, you need to repeat this procedure.

1. Hold the bottle with a sprayer to the open mouth and hold it as close as possible.

2. Click on the dispenser to release the dose of the spray into the oral cavity. Spraying, avoid getting a spray on the back of the throat and lips.

Do not inhale the spray during injection to prevent ingestion. For best results, do not swallow for several seconds after spraying.

How to close the spray dispenser / block the nozzle

Slowly lower the dispenser button, as shown up to the possibility of pressing the button inside.

2. Press the dispenser button and lower the dispenser down. Then release the button. Now the spray is closed.

Repeat the above steps for the next application.

Close the spray bottle every time after application to prevent use of the spray by children or accidental spraying.

If the spray accidentally gets into the eyes, rinse the eyes with water.

Side effects:

Some symptoms may be due to the withdrawal of nicotine due to smoking cessation.These include: dysphoria or depressed mood; insomnia; irritability, discontent or anger; anxiety; difficulty concentrating, anxiety or impatience; decreased heart rate; increased appetite or weight gain. They were detected in patients using sherds for topical application.

After cessation of smoking, the incidence of aphthous ulcers, cough and nasopharyngitis may also increase. Causal relationship is established.

In addition, people using the spray for topical use also had other symptoms associated with smoking cessation: dizziness, presyncopal conditions, cough, constipation and bleeding gums.

The craving for nicotine, considered as a clinically significant symptom, is an important manifestation of nicotine withdrawal after smoking cessation.

Spray Nicorette® can cause unwanted reactions associated with nicotine, similar to observed when applying other nicotine-containing drugs, these reactions are predominantly dose-dependent.

Most of the undesirable reactions to Nicorette® spray were observed early in the treatment and similar to those for oral medications.In the first few days of treatment, irritation of the mucous membrane of the oral cavity and pharynx can be observed, and hiccups often occur. Continuation of treatment leads to adaptation.

Daily data collection in the subjects of the study showed that very often unwanted phenomena appear in the first 2-3 weeks of spray application and subsequently disappear.

The adverse events reported in the clinical trials of Nicorette® spray include:

Very frequent (> = 1/10); Frequent (> = 1/100, <1/10); infrequent (> = 1/1000, <1/100); rare (> = 1/10000, <1/1000); very rare (<1/10000); unknown (estimate based on available data is not possible).

Organs and systems .............. Frequency ........................ Undesirable phenomena

Infringements from
nervous system ............... Very frequent ..............Headache, taste change

.............................................. Frequent ... ...................... Dizziness

.............................................. Infrequent ... ..................Parrest

Infringements from
organs of vision ........................ Unknown ...................Blurred vision

Infringements from
hearts .................................. Infrequent .............. ........ Heart palpitations

.............................................. Unknown ... ................ Atrial fibrillation

Infringements from
Vessels ................................. Infrequent ............... ........ Tides

Infringements from
respiratory system
and organs the mediastinum.... Very frequent ...................Hiccups

.............................................. Infrequent ... ...................... Rhinorrhea, shortness of breath, bronchospasm, ........................................ ............................................... sneezing, stuffiness nose

Infringements from
digestive
systems ............................... Very frequent .................Nausea, indigestion

.............................................. Frequent ... .........................Vomiting, swelling, pain in the .......................................................................................stomach, diarrhea

.............................................. Infrequent ... ..................... Gingivitis, glossitis

Infringements from
skin and subcutaneous
cellulose .......................... Infrequent ........................ Dryness of the skin, sweating,

.................................................. .................................... rash, hives, itching

Infringements from
immune system ............ Infrequent ........................ Hypersensitivity

Infringements from
musculoskeletal system
and connective tissue ... infrequent .......................Musculoskeletal pain

Systemic disorders
and complications in place
Introduction .............................. Very frequent ................ Pain in the soft tissues of the cavity ............................................. ......................................... mouth and paresthesia, stomatitis, ... .................................................. ................................. hypersecretion of saliva, .............. .................................................. ...................... Burning lips, dry mouth and ..................... .................................................. .............. (or) pharynx

.............................................. Infrequent ... ..................... The feeling of squeezing into ............................................... ......................................... pharynx, fatigue, pain in ................................................ ........................................ chest, discomfort in ..... .................................................. chest, toothache, ........... .................................................. mucosa exfoliation. .................................................. .......... oral cavity, voice changes

Overdose:

When administered in accordance with the instructions for use, the symptoms of nicotine overdose may occur in patients with low nicotine intake prior to treatment or with the simultaneous use of various sources of nicotine.

Symptoms

The minimum lethal dose for acute overdose for an unaccustomed adult is 40-60 mg of nicotine. In case of an overdose, the same symptoms are noted as with acute nicotine poisoning, namely: nausea, vomiting, excessive salivation, abdominal pain, diarrhea, sweating, headache, dizziness, hearing loss and severe general weakness. At higher doses, arterial hypotension, a weak and irregular pulse, violation of breathing, impairment of consciousness, collapse and generalized convulsions may join them.

Doses of nicotine, which are well tolerated during treatment by adult smokers, can cause symptoms of severe poisoning in young children and even lead to death. Suspicion of nicotine poisoning in children should be regarded as an emergency that requires immediate hospitalization.

Treatment

It should immediately stop using nicotine and begin symptomatic treatment. If necessary, start artificial ventilation. Reception of activated carbon prevents the absorption of nicotine in the gastrointestinal tract.

Interaction:

Clear clinical significance of the interaction between nicotine replacement therapy and other drugs has been established. Hem, however, theoretically, nicotine can enhance the hemodynamic effects of adenosine, t. lead to an increase in blood pressure and heart rate, and also to increase the response to pain (chest pains by the type of angina pectoris), provoked by the introduction of adenosine.

Special instructions:

Any risks that are inherent in SPT significantly outweigh the proven harm caused by smoking.

Concomitant cardiovascular diseases

With a stable course of cardiovascular disease, Nnorrette® spray causes less harm than continued smoking. However, smokers with recent myocardial infarction, unstable angina or worsening of its course, including Prinzmetal angina, with severe arrhythmia,recently suffered cerebrovascular diseases and (or) patients with unstable hemodynamics should be recommended to stop smoking without the help of pharmacological intervention. If such attempts are unsuccessful, you can consider the use of Nnorrette® spray, but since the safety data for this category of patients are limited, such treatment should be started only under strict medical supervision.

Diabetes

Patients with diabetes after smoking cessation and from the beginning of 31 GG are recommended to more closely monitor blood glucose concentration, since a decrease in the content of catecholamines, the release of which is induced by nicotine, can affect the metabolism of carbohydrates.

Diseases of the gastrointestinal tract

Swallowed nicotine can exacerbate the symptoms of esophagitis, gastritis or peptic ulcer, so use drugs for oral PTA in this pathology should be cautious.

Impaired liver and kidney function

In patients with moderate or severe hepatic insufficiency n (or) severe renal insufficiency, the drug should be used with caution,since the clearance of nicotine and its metabolites can be reduced, which can increase the risk of adverse events.

Danger for young children

Doses of nicotine, which are easily tolerated by adult smokers and teenage smokers, can cause severe intoxication in children, which can lead to death. It is important not to leave unattended preparations containing nicotine, as this can lead to incorrect use and swallowing by children (see "Overdose").

Pheochromocytoma and uncontrolled hyperthyroidism

In patients with uncontrolled hyperthyroidism and pheochromocytoma, the drug should be used with caution, since nicotine causes the release of catecholamines.

Formation of dependence

Dependence on the drug may develop, but it is less dangerous to health and more easily surmountable than the dependence on smoking.

To give up smoking

Polycyclic aromatic hydrocarbons contained in tobacco smoke induce metabolism of drugs metabolized by the isoenzyme CYP1A2 (and, perhaps, CYP1A1). Cessation of smoking can cause a slowdown in metabolism and, as a consequence, an increase in the concentration of these drugs in the blood.This has potential clinical relevance for drugs with a narrow therapeutic index, for example, theophylline, clozapine and ropinirole.

Excipients

Spray Nicoretts® contains a small amount of ethanol (alcohol) - less than 10 mg per dose.

If the medicine has become unusable or the expiration date has expired, dispose of it in sewage or on the street! Place the drug in a bag and put it in the trash. These measures will help protect the environment!

The use of Ncoretret® is associated with less risk than smoking!

Effect on the ability to drive transp. cf. and fur:It is necessary to take into account the profile of unwanted reactions of the drug (dizziness, behavior change, etc.), which can worsen the ability to drive vehicles and work with mechanisms.

Form release / dosage:

Spray for topical use dosed with 1 mg / dose.

For 13,2 ml (150 doses), sirsya in a transparent bottle of polyethylene terephthalate, which is placed in an opaque protective case made of polypropylene.

For 1 or 2 bottles (each in a protective case) with a dispenser, together with the instruction, they are laminated to a transparent contour plastic container.

Packaging:(150) - polyethylene terephthalate bottles with dispenser (1) - polypropylene containers-plastic containers
(2) - polyethylene terephthalate bottles with dispenser (1) - polypropylene containers-plastic containers

Storage conditions:

Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-002890

Date of registration:03.03.2015

The owner of the registration certificate:Johnson & Johnson, LLC Johnson & Johnson, LLC Russia

Manufacturer: & nbsp

McNeil AB, Sweden

Representation: & nbspJohnson & Johnson LLC Johnson & Johnson LLC Russia

Information update date: & nbsp09.08.2015

Illustrated instructions

Instructions

Nicorette® (Nicorette®)