Nicorette spray for local use 1 mg/dose 150 doses (Johnson)

Nicorette spray for local use 1 mg/dose 150 doses (Johnson)

For application to the oral mucosa. The patient should do everything possible to permanently quit smoking while being treated with Nicorette® spray. Adults over 18 years of age Nicorette® Spray should be used at the moment when an irresistible urge to smoke occurs. After preparing the spray for use (see below for Instructions for Use when using the spray for the first time), place the tip of the spray as close to your open mouth as possible. Press the dispenser from above, thus releasing one dose of the drug into the oral cavity; Avoid getting the spray on your lips. To prevent the substance from entering the respiratory tract, do not inhale when pressing the dispenser. For best results, do not swallow saliva for several seconds after injection. While using the spray, eating and drinking is not recommended. If symptoms of overdose appear (see section “Overdose”), use of the drug must be stopped immediately. Complete smoking cessation Nicorette® Spray should be used in all cases of craving for smoking or to prevent cravings in situations that may provoke it. Smokers who want or are able to quit smoking immediately should immediately replace smoking cigarettes with Nicorette® spray and, as soon as possible, reduce the number of injections until they stop completely. If you completely quit smoking, take 1 or 2 injections during the period of time when you usually smoked a cigarette, as well as if you have a craving for smoking. If after a single injection the craving for smoking does not decrease within a few minutes, a second injection should be made. If two doses are required, subsequent application of the spray may consist of 2 consecutive injections. Every hour you are allowed to take no more than 4 dosed injections of the spray. Do not inject more than 2 doses of spray at a time or use more than 64 doses per day (or 4 doses per hour for 16 hours). Each bottle contains at least 150 doses. The average course of use of the spray at the indicated dose is 6 weeks. Then you should begin to reduce the number of injections so that by the end of the 9th week the number of doses is half the average number of doses per day received in the first 6 weeks, and during the 12th week - no more than 4 doses per day. When the daily dose drops to 2-4 injections, use of the spray should be discontinued. After completion of therapy, to prevent a return to smoking, patients can use Nicorette® spray if they have an irresistible urge to smoke. In such situations, you can make 1 injection, and if after a single injection the craving for smoking does not decrease within a few minutes, you should make a second injection. In this case, you should not exceed 4 dosed injections per day. Regular use of the spray for more than 6 months is usually not recommended, but some patients may require longer therapy to avoid relapse into smoking. Reducing the number of cigarettes smoked Smokers who want to reduce the number of cigarettes they smoke should use the spray as needed between smoking episodes to increase the amount of time between smoking and to reduce smoking as much as possible. Once readiness is felt, smokers should aim to quit completely. After quitting smoking, you should follow the recommendations for therapy and gradual dose reduction indicated above for complete smoking cessation. Behavioral therapy and psychological support usually increase treatment success. Those who have managed to quit smoking but find it difficult to give up the spray are advised to consult a doctor for medical help. Temporary smoking cessation The spray can be used during periods when it is necessary to abstain from smoking, for example, when in places where smoking is prohibited, or in other situations when it is necessary to abstain from smoking. The maximum daily dose for temporary smoking cessation is 64 doses. In combination with a transdermal patch For smokers with a severe nicotine addiction (more than 20 cigarettes per day) or experiencing an irresistible craving for smoking, or smokers who have not been able to quit smoking using only one type of nicotine replacement therapy, it is possible to use a spray for the mucous membrane Nicorette® oral membranes in combination with Nicorette® transdermal patch for rapid relief of smoking cravings. The patch is applied to an intact area of ​​skin immediately after waking up in the morning and removed before going to bed. The patch should be applied to dry, clean, intact, hair-free skin, such as the thighs, upper limbs or chest. It is necessary to change the application site every day: do not use the same area for two consecutive days. After applying the patch, wash your hands thoroughly to avoid eye irritation from possible nicotine contact. Initial therapy: Treatment should begin with a 25 mg/16 hour patch (stage 1) in combination with a 1 mg/dose spray. Usually 13 doses of spray per day are sufficient. The maximum daily dose of the spray is 32 doses. Patients should completely stop smoking during therapy. Usually the general course of treatment lasts for 8 weeks. After this, the dose of nicotine should be gradually reduced. Withdrawal of combination therapy: There are two ways to discontinue combination therapy. Method 1: Over the next 2 weeks, switch from the 25 mg/16 hour patch (Stage 1) to the 15 mg/16 hour patch (Stage 2), and then, over the next 2 weeks, to the 10 mg/16 hour patch ( stage 3), while maintaining, if necessary, the number of doses of Nicorette® spray used, as with Initial therapy. Next, the number of doses of the spray is gradually reduced until complete withdrawal for the time that the patient needs depending on his needs, but no later than 12 months after the start of combination therapy. Method 2: involves completely removing the patch immediately after completing the Initial Therapy phase. Next, gradually reduce the number of doses of Nicorette® spray until complete withdrawal during the time that the patient needs depending on his needs, but no later than 12 months after the start of combination therapy. Children and adolescents under 18 years of age The drug is not recommended for use by persons under 18 years of age. There is no experience in treating adolescents under 18 years of age with the spray.

Nicorette®

The pharmacokinetics of nicotine have been extensively studied; it was found that the method of delivery of the substance to the body has a significant impact on the rate and extent of absorption.

The pharmacokinetics of the topical spray were studied in four studies involving 141 subjects.

Suction

The topical dosage form of Sirey assumes that the dose of nicotine is delivered immediately and, as a result, its absorption from the oral cavity is rapid: according to studies, the absorption of nicotine from a topical spray occurred after 2 minutes (at the first time point).

The maximum concentration of 5.3 ng/ml is achieved within 13 minutes after administration of 2 mg of nicotine. 10 minutes after application of the 1 and 2 mg spray, the area under the concentration-time curve (AUC) exceeded those obtained in studies of chewing gum and tablets containing 4 mg of nicotine (0.48 and 0.64 hig/ml compared to 0.33 and 0.33 hhig/ml). AUG values ​​indicate that the bioavailability of nicotine when using a spray is slightly higher than when using nicotine chewing gum or tablets. The AUC for the 2 mg spray was 14.0 hig/ml compared to 23.0 hig/ml for the 4 mg chewable gummies and 26.7 hig/ml for the 4 mg tablets.

The mean steady-state plasma nicotine concentration achieved after administration of the maximum dose (i.e., 2 sprays of 1 mg spray every 30 minutes) was approximately 28.8 ng/ml compared to 23.3 ng/ml with chewable nicotine. gum with a dosage of 4 mg (1 tablet every hour) and 25.5 g/ml for nicotine tablets with a dosage of 4 mg (1 tablet every hour).

Given the rapid absorption and similar high relative bioavailability, most of the nicotine released from the spray is apparently absorbed through the buccal mucosa.

Distribution

The volume of distribution after intravenous administration of nicotine ranges from 2-3 l/kg.

The binding of nicotine to blood plasma proteins is less than 5%. For this reason, changes in nicotine binding when using concomitant drugs or changes in plasma protein levels in a number of diseases should presumably not have a significant effect on the pharmacokinetics of nicotine.

Biotransformation

The metabolism and elimination of nicotine do not depend on the dosage form, so the results of studies of nicotine administered intravenously are suitable for their description.

The main organ that eliminates nicotine is the liver. However, nicotine is also metabolized in the kidneys and lungs. More than 20 nicotine metabolites are known, all of which appear to be less active than the parent compound.

The plasma half-life of the main metabolite of nicotine, cotipin, is 15-20 hours, and its concentration is 10 times higher than that of nicotine.

Removal

The average plasma clearance of nicotine is 70 l/hour, the elimination period is 2-3 hours.

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

Linearity/non-linearity

With 1, 2, 3 and 4 sprays of the 1 mg/dose spray, only a slight deviation from the linearity of AUC and Cmax was detected.

Special patient groups

Renal dysfunction

The progression of renal failure is accompanied by a decrease in the overall clearance of nicotine. Nicotine clearance in patients with severe renal impairment is reduced by an average of 50%. In hemodialysis patients, an increase in nicotine concentration was observed.

Liver dysfunction

The pharmacokinetics of nicotine in patients with mild liver dysfunction (5 points on the Child-New scale) did not change, but in the presence of moderate liver dysfunction (7 points on the Child-New scale) it decreased by 40-50%. There are no data on the pharmacokinetics of nicotine in liver dysfunction of more than 7 points on the Child-Pugh scale.

Elderly patients

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

pharmachologic effect

A drug for the treatment of nicotine addiction. Nicorette allows you to avoid the development of withdrawal syndrome (irritability, malaise and the desire to smoke), which develops when you quit smoking, reduce the number of cigarettes and temporarily quit in situations where smoking is not allowed. When using the drug, nicotine enters the body; At the same time, ingredients of tobacco smoke such as tar, carcinogens, and carbon monoxide do not enter the body. It must be borne in mind that the patient himself decides to quit smoking, and the drug Nicorette only helps him in this, reducing the physiological dependence on nicotine. In cases where it is not possible to quit smoking immediately, reducing the number of cigarettes smoked is also a positive result. Success associated with reducing the number of cigarettes smoked can encourage complete smoking cessation.

special instructions

• The drug should be prescribed with caution to patients with severe diseases of the cardiovascular system (occlusive diseases of the peripheral arteries, cerebrovascular diseases, stable angina, congestive heart failure in the decompensation phase), with vascular spasms, uncontrolled arterial hypertension, with severe and moderate liver diseases , with severe kidney disease, with peptic ulcer of the stomach and duodenum in the acute phase.
• The inhaler should be used with caution in case of chronic diseases of the pharynx and bronchial asthma.
• Nicotine causes the release of catecholamines in the adrenal medulla, so Nicorette should be used with caution in patients with hyperthyroidism or pheochromocytoma.
• Patients with diabetes may require a reduction in insulin doses as a result of quitting smoking.
• When using the drug, a transition from tobacco addiction to nicotine may occur, but the use of pure nicotine causes less harm to health than tobacco use.
• It is recommended to use the inhaler at temperatures above 15°C, because At low temperatures, the effectiveness of the inhaler decreases.
• After smoking cessation, plasma concentrations of drugs such as theophylline, tacrine and clozapine, as well as imipramine, olanzapine, clomipramine and fluvoxamine, which have a narrow therapeutic range, may increase. In addition, there is some evidence indicating a possible stimulating effect of smoking on the metabolism of flecainide and pentazocine.
• Use in pediatrics. There is no experience with the use of Nicorette in children and adolescents under the age of 18, so the drug should not be used in this category of patients without a doctor’s prescription.

Directions for use and doses

The inhalation solution should be used at the moment when an irresistible desire to smoke arises.

• The dose is selected individually, taking into account the severity of nicotine addiction in the patient. However, you should not use more than 12 cartridges per day. This maximum daily dose can be used for 6-12 weeks, after which it should be reduced. The more often you use your inhaler, the easier it is to quit smoking for a long time.
• The recommended dose for adults (including elderly patients) is 6-12 cartridges per day. 1 cartridge replaces 4 cigarettes. If a patient smoked 20 cigarettes per day, then he should use 6 cartridges per day. Each cartridge can be used in approximately 4 doses, each lasting approximately 20 minutes.
• If you completely quit smoking, the course is carried out for at least 3 months. Then you should begin to gradually reduce the number of cartridges used. It is recommended to have several additional cartridges with you, because... An unexpected urge to smoke may arise. When reducing the number of cigarettes smoked, the inhaler should be used in breaks between smoking to increase their duration and to reduce the number of cigarettes smoked as much as possible. The patient should be warned that if after 6 weeks the number of cigarettes smoked daily has not decreased, a doctor should be consulted.
• As a rule, it is not recommended to use the inhaler for more than 6 months. Some patients who quit smoking require longer use of the inhaler to prevent relapse. The patient should try to quit smoking when he is ready, but no later than 6 months after starting treatment. If you have not been able to quit smoking within 9 months after starting therapy, you should consult a specialist. Specialist consultations and psychological support help improve the effectiveness of therapy.

Nicorette, 2 pcs., 1 mg/dose, dosed topical spray, fruity-mint

For application to the oral mucosa.

The patient should do everything possible to permanently quit smoking while being treated with Nicorette® spray.

Adults over 18 years old

Nicorette® spray should be used at the moment when an irresistible urge to smoke arises. After preparing the spray for use (see below for Instructions for Use when using the spray for the first time), place the tip of the spray as close to your open mouth as possible. Press the dispenser from above, thus releasing one dose of the drug into the oral cavity; Avoid getting the spray on your lips. To prevent the substance from entering the respiratory tract, do not inhale when pressing the dispenser. For best results, do not swallow saliva for several seconds after injection.

While using the spray, eating and drinking is not recommended.

If symptoms of overdose appear (see section “Overdose”), use of the drug must be stopped immediately.

Complete smoking cessation

Nicorette® Spray should be used in all cases of craving for smoking or to prevent cravings in situations that may provoke them.

Smokers who want or are able to quit smoking immediately should immediately replace smoking cigarettes with Nicorette® spray and, as soon as possible, reduce the number of injections until they stop completely.

If you completely quit smoking, take 1 or 2 injections during the period of time when you usually smoked a cigarette, as well as if you have a craving for smoking. If after a single injection the craving for smoking does not decrease within a few minutes, a second injection should be made. If two doses are required, subsequent application of the spray may consist of 2 consecutive injections.

Every hour you are allowed to take no more than 4 dosed injections of the spray. Do not inject more than 2 doses of spray at a time or use more than 64 doses per day (or 4 doses per hour for 16 hours).

Each bottle contains at least 150 doses.

The average course of use of the spray at the indicated dose is 6 weeks. Then you should begin to reduce the number of injections so that by the end of the 9th week the number of doses is half the average number of doses per day received in the first 6 weeks, and during the 12th week - no more than 4 doses per day. When the daily dose drops to 2-4 injections, use of the spray should be discontinued.

After completion of therapy, to prevent a return to smoking, patients can use Nicorette® spray if they have an irresistible urge to smoke. In such situations, you can make 1 injection, and if after a single injection the craving for smoking does not decrease within a few minutes, you should make a second injection. In this case, you should not exceed 4 dosed injections per day.

Regular use of the spray for more than 6 months is usually not recommended, but some patients may require longer therapy to avoid relapse into smoking.

Reducing the number of cigarettes smoked

Smokers wishing to reduce the number of cigarettes they smoke should use the spray as needed between smoking episodes to increase the time between smoking and to reduce smoking as much as possible.

Once readiness is felt, smokers should aim to quit completely.

After quitting smoking, you should follow the recommendations for therapy and gradual dose reduction indicated above for complete smoking cessation.

Behavioral therapy and psychological support usually increase treatment success. Those who have managed to quit smoking but find it difficult to give up the spray are advised to consult a doctor for medical help.

Temporary cessation of smoking

The spray can be used during periods when it is necessary to abstain from smoking, for example, when in places where smoking is prohibited, or in other situations when it is necessary to abstain from smoking. The maximum daily dose for temporary smoking cessation is 64 doses.

In combination with a transdermal patch

For smokers with a severe nicotine addiction (more than 20 cigarettes per day) or who experience an irresistible craving for smoking, or smokers who have not been able to quit smoking using only one type of nicotine replacement therapy, it is possible to use Nicorette® oral mucosal spray in combination with Nicorette® transdermal patch to quickly relieve smoking cravings.

The patch is applied to an intact area of ​​skin immediately after waking up in the morning and removed before going to bed. The patch should be applied to dry, clean, intact, hair-free skin, such as the thighs, upper limbs or chest. It is necessary to change the application site every day: do not use the same area for two consecutive days. After applying the patch, wash your hands thoroughly to avoid eye irritation from possible nicotine contact.

Initial therapy:

Treatment should begin with a 25 mg/16 hour patch (stage 1) in combination with a 1 mg/dose spray. Usually 13 doses of spray per day are sufficient. The maximum daily dose of the spray is 32 doses.

Patients should completely stop smoking during therapy. Usually the general course of treatment lasts for 8 weeks. After this, the dose of nicotine should be gradually reduced.

Cancellation of combination therapy:

Combination therapy can be discontinued in two ways.

Method 1: Over the next 2 weeks, switch from the 25 mg/16 hour patch (Stage 1) to the 15 mg/16 hour patch (Stage 2), and then, over the next 2 weeks, to the 10 mg/16 hour patch ( stage 3), while maintaining, if necessary, the number of doses of Nicorette® spray used, as with Initial therapy

. Next, the number of doses of the spray is gradually reduced until complete withdrawal for the time that the patient needs depending on his needs, but no later than 12 months after the start of combination therapy.

Method 2: involves completely removing the patch immediately after completing the Initial Therapy

. Next, gradually reduce the number of doses of Nicorette® spray until complete withdrawal during the time that the patient needs depending on his needs, but no later than 12 months after the start of combination therapy.

Recommended dose:

Children and teenagers under 18 years of age

The drug is not recommended for use by persons under 18 years of age. There is no experience in treating adolescents under 18 years of age with the spray.

Instructions for use

How to open the spray dispenser/unlock the nozzle

1. Use your thumb to smoothly push down the dispenser button, as shown in figure (a), until the button can be pressed inward (see figure b).

2. While pressing the button, lift up the dispenser as shown in figure (c). Release the button.

First use of Nicorette® spray

When using the spray for the first time, you should check the operation of the sprayer. Take the bottle so that the stream is directed away from you, other people, children and pets. Open the spray nozzle and press 3 times until fine spray appears.

If you do not use the spray within 2 days, you must repeat this procedure.

How to use Nicorette® spray

1. Apply the spray bottle to your open mouth and hold it as close as possible.

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

Do not inhale the spray while spraying to prevent ingestion.

For best results, do not swallow within a few seconds of spraying.

How to close the spray dispenser/lock the nozzle

1. Smoothly lower the dispenser button downwards, as shown in the figure (d), until the button can be pressed inwards (e).

2. Press the dispenser button (e) and lower the dispenser down (f). Then release the button. The spray is now closed.

For next use, repeat the above steps.

Close the spray bottle each time after use to prevent children from using the spray or accidental spraying.

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