Nicorette, spray 1 mg/dose 150 doses mint 2 pcs

Nicorette® Spray alleviates and/or prevents smoking cravings and withdrawal symptoms that occur with tobacco addiction.

It is indicated as support for smokers who intend to quit smoking or reduce the number of cigarettes smoked before giving up completely; to help smokers who do not want to smoke or in the absence of such an opportunity; and as a safer alternative to smoking.

Indications

Nicorette® spray relieves and/or prevents cravings for smoking and withdrawal symptoms that occur with tobacco addiction.

Indicated as support for smokers who intend to quit smoking or reduce the number of cigarettes smoked before quitting completely; in order to assist smokers who do not want to smoke or do not have such an opportunity; and also as a safer alternative to smoking.

Special instructions

The use of Nicorette® is associated with less risk than smoking.

An assessment of the risk-benefit ratio should be made by a physician of the appropriate specialty in patients with the following conditions:

Concomitant cardiovascular diseases

With a stable course of cardiovascular diseases, Nicorette® spray causes less harm than continued smoking. However, smokers with a recent myocardial infarction, unstable or worsening angina, including Prinzmetal’s angina, severe arrhythmia, recent cerebrovascular disease, and/or patients with uncontrolled hypertension should be advised to stop smoking without pharmacological intervention. If such attempts are unsuccessful, the use of Nicorette® spray may be considered, however, since safety data in this category of patients are limited, such treatment should only be initiated under strict medical supervision.

Diabetes mellitus

Patients with diabetes mellitus are advised to monitor their blood glucose concentrations more closely after stopping smoking and starting nicotine replacement therapy, since a decrease in catecholamines, the release of which is induced by nicotine, may affect carbohydrate metabolism.

Allergic reactions

The drug should be used with caution in patients predisposed to angioedema and urticaria.

Diseases of the gastrointestinal tract

Ingested nicotine can aggravate the symptoms of esophagitis, gastritis or peptic ulcers, so oral nicotine replacement therapy should be used with caution for these pathologies.

Liver and kidney dysfunction

In patients with moderate to severe hepatic impairment and/or severe renal impairment, the drug should be used with caution as the clearance of nicotine and its metabolites may be reduced, which may increase the risk of adverse events.

Danger for small children

Doses of nicotine that are easily tolerated by adult and teenage smokers can cause severe toxicity in children, which can lead to death. It is important not to leave preparations containing nicotine unattended, as this may lead to their misuse and ingestion by children (see section “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 overcome than addiction to smoking.

Quitting smoking

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

Excipients

Nicorette® spray contains a small amount of ethanol (alcohol) – less than 10 mg per dose.

When using Nicorette® Spray, be careful not to get the spray in your eyes.

Warnings and precautions for combination therapy of Nicorette® transdermal patch spray are the same as those for either drug alone.

If the medicine has become unusable or has expired, do not throw it into wastewater or onto the street! Place the medication in a bag and place it in the trash. These measures will help protect the environment!

Active ingredient

Nicotine

Composition

1 ml of the drug contains:

Active ingredient:

nicotine – 13.6 mg;

Excipients: propylene glycol – 150.0 mg, ethanol – 97.0 mg, trometamol – 40.5 mg, poloxamer – 40.0 mg, glycerol – 25.0 mg, sodium bicarbonate – 14.3 mg, levomenthol – 10.0 mg, mint flavor QL24245 – 4.0 mg, Cooler flavor 2 SN046680 – 3.0 mg, sucralose – 1.5 mg, acesulfame potassium – 1.5 mg, hydrochloric acid 10% – sufficient amount up to pH 9, purified water – sufficient amount up to 1 ml.

Pregnancy

Pregnancy

Smoking during pregnancy is associated with risks such as intrauterine growth restriction, premature birth, or stillbirth. Smoking cessation is the single most effective intervention for improving the health of both the pregnant woman and her baby. Quitting smoking early is the best option.

Nicotine penetrates the placental barrier and affects the respiratory activity and blood circulation of the fetus. The effect on blood circulation is dose-dependent.

Therefore, ideally, smoking cessation during pregnancy should be carried out without nicotine replacement therapy. However, if a woman is unable (or expected) to quit smoking without pharmacological support, then nicotine replacement therapy is used, since continued smoking carries a greater risk to the fetus compared to nicotine replacement therapy. Quitting smoking is the best option, but if this is not possible, Nicorette® Spray can be used as a safer alternative to smoking during pregnancy. Due to the potential for nicotine-free periods, intermittent dosage forms are preferred, but patches may be required if nausea and/or vomiting is significant. A pregnant woman should begin using Nicorette® spray only after consulting a doctor.

Breastfeeding

Nicotine passes into breast milk in quantities that can affect the baby even when the drug is used in therapeutic doses. Therefore, you should refrain from using Nicorette® spray during breastfeeding. If you are unable to quit smoking, use of the drug should only be started after consultation with your doctor.

Dosage forms for periodic use minimize the nicotine content in breast milk and allow breastfeeding with the lowest nicotine concentration in it. In order to reduce the negative effects of nicotine on a child, the drug should be used immediately after feeding. The periods between the use of the drug and the next feeding should be as long as possible (at least 2 hours are recommended).

Smoking increases the risk of infertility in men and women. In vitro studies have shown that nicotine negatively affects sperm quality in men.

Contraindications

• Hypersensitivity to nicotine or other components of the drug.

• Children under 18 years of age.

Side Effects

Regardless of the dosage form of the nicotine product used, some symptoms may be due to nicotine withdrawal due to smoking cessation. These include the following: dysphoria or depressed mood; insomnia; irritability, dissatisfaction or anger; anxiety; difficulty concentrating, restlessness, or impatience; decreased heart rate; increased appetite or weight gain; cough; aphthous ulcers; nasopharyngitis. A cause-and-effect relationship has not been established.

In addition, users of the oral spray also reported other symptoms associated with smoking cessation: dizziness, near-syncope, cough, constipation and bleeding gums.

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

Nicorette® Spray may cause nicotine-related adverse reactions similar to those observed with other nicotine-containing medications, these reactions being predominantly dose-dependent.

Allergic reactions (such as angioedema, urticaria and anaphylactic shock) may occur in susceptible individuals.

Most adverse reactions to Nicorette® spray were observed in the early phase of treatment and are similar to those for drugs taken orally. In the first few days of treatment, irritation of the mucous membrane of the oral cavity and pharynx may occur, and hiccups are common. Continuation of treatment leads to adaptation.

Daily data collection from study subjects showed that very common adverse events occurred in the first 2-3 weeks of use of the spray and subsequently disappeared.

Interaction

There are no clear clinically significant interactions between nicotine replacement therapy and other drugs. However, theoretically, nicotine may enhance the hemodynamic effects of adenosine, i.e., lead to an increase in blood pressure and heart rate, and also enhance the pain response (angina-type chest pain) provoked by the administration of adenosine.

Overdose

When used in accordance with the instructions for use, symptoms of nicotine overdose may occur in patients with a low pre-treatment nicotine intake or when using multiple nicotine sources simultaneously.

Symptoms

The minimum lethal dose for an acute overdose for an unaccustomed adult is 40–60 mg of nicotine. In case of an overdose, the same symptoms are observed as in acute nicotine poisoning, namely: nausea, vomiting, increased salivation, abdominal pain, diarrhea, sweating, headache, dizziness, hearing loss and severe general weakness. At higher doses, they may be accompanied by arterial hypotension, weak and irregular pulse, respiratory failure, impaired consciousness, collapse and generalized convulsions.

Doses of nicotine that are well tolerated during treatment in adult smokers can cause symptoms of severe poisoning in young children and can even be fatal. Suspicion of nicotine poisoning in children should be regarded as an emergency condition requiring immediate hospitalization.

Treatment

Nicotine use should be stopped immediately and symptomatic treatment should be initiated. If necessary, artificial ventilation should be started. Taking activated charcoal prevents the absorption of nicotine in the gastrointestinal tract.

Clinical pharmacology

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.

Abrupt cessation of smoking causes the development of a characteristic withdrawal syndrome, including cravings for smoking.

Clinical studies have shown that nicotine replacement therapy drugs help smokers abstain from smoking by easing withdrawal symptoms. A single-dose study in 200 healthy smokers demonstrated that using two doses of a 1 mg spray reduced the desire to smoke from the first minute after using the spray and to a significantly greater extent than using lozenges containing nicotine. Compared with nicotine gum or lozenges, nicotine absorption from an oral spray is faster (see Pharmacokinetics) and, based on experience with nicotine replacement therapy, results in a more rapid reduction in cravings and other symptoms.

Increased appetite is a well-known symptom of nicotine withdrawal, and weight gain often occurs after smoking cessation. An important symptom of withdrawal syndrome is also the desire to smoke.
Pharmacokinetics: 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 oral mucosal spray were studied in four studies involving 141 subjects.

Suction

The dosage form of the spray for the oral mucosa assumes that the dose of nicotine is delivered immediately and, as a result, its absorption from the oral cavity is rapid.

The maximum concentration of 5.3 ng/ml is achieved within 13 minutes after administration of 2 mg of nicotine. At 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 nicotine (0.48 and 0.64 h×ng/ml, compared with 0.33 and 0.33 h×ng/ml).

AUC∞ values ​​indicate that the bioavailability of nicotine when applied as a spray to the oral mucosa is similar to the bioavailability when using tablets and is slightly higher than when using nicotine chewing gum. The AUC∞ for the 2 mg spray was 14.0 h×ng/mL compared with 23.0 h×ng/mL for the 4 mg chewing gum and 26.7 h×ng/mL for the 4 mg tablets.

The mean steady-state plasma nicotine concentration achieved after administration of the maximum dose (i.e., 2 puffs of 1 mg spray every 30 minutes) was approximately 28.8 ng/mL, compared with 23.3 ng/mL for 4 mg gum (1 puff every hour) and 25.5 ng/mL for 4-mg nicotine tablets. 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 due to the use of 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, and therefore 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, cotinine, 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 half-life 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, the amount of nicotine excreted unchanged in urine can reach 30%.

Linearity/nonlinearity

With 1, 2, 3 and 4 sprays of the 1 mg/dose spray, only minor deviations from linearity were detected in AUC∞ and Cmax.

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%. Increased nicotine concentrations were observed in hemodialysis patients.

Liver dysfunction

The pharmacokinetics of nicotine in patients with mild liver dysfunction (5 points on the Child-Pugh scale) did not change, but in the presence of moderate liver dysfunction (7 points on the Child-Pugh 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.

Short product description

Helps reduce cravings for smoking. Activation in 60 seconds 1.

1-When using 2 doses of 1 mg according to the instructions for use.

Storage conditions

Store at a temperature not exceeding 25 °C.

Keep out of the reach of children.

Manufacturer

McNeil AB, Sweden