Nicorette Transdermal Therapeutic System 15mg/16 h, 7pcs

Composition

Nicotine base: Active ingredient: nicotine – 23.62 mg; Excipients: triglycerides (average chain length) – 27.41 mg, copolymer of basic butyl methacrylate-21.87 mg, polyethylene terephthalate film 19 µm (on the one hand can be varnished) – carrier layer containing the Active ingredient. Acrylate base: acrylic adhesive solution-185.76 mg, potassium hydroxide-1.05 mg, croscarmellose sodium-7.49 mg, aluminum acetylacetonate-0.09 mg, polyethylene terephthalate film 100 µm, aluminized on one side and siliconized on both sides-carrier, performs the function of protecting the adhesive layer (removable substrate), discarded before use.

Pharmacological action

Pharmacodynamics : After abruptly quitting smoking, patients who have used tobacco-containing products daily for a long time may develop a “withdrawal” syndrome, which includes: dysphoria or depressed mood, insomnia, increased irritability, dissatisfaction or anger, anxiety, impaired concentration, restlessness or impatience, decreased heart rate, increased appetite or weight gain. An important symptom of “withdrawal” syndrome is also the desire to smoke. In the treatment of tobacco dependence, nicotine replacement therapy reduces the need for the number of cigarettes smoked, reduces the severity of withdrawal symptoms that occur when completely quitting smoking in those who have decided to quit smoking; facilitates temporary abstinence from smoking, and also helps to reduce the number of cigarettes smoked in those who cannot or do not want to completely quit smoking. Pharmacokinetics: Nicotine is slowly released from the Nicorette ® patch and is continuously absorbed through the skin. The Nicorette ® patch is intended for use during waking hours, i. e. for approximately 16 hours, which coincides with the period of nicotine intake during smoking. This allows you to avoid sleep disorders caused by nicotine intake during sleep. Absolute bioavailability exceeds 90%, regardless of where the patch is applied. In the therapeutic range (10-25 mg/16 hours), the relationship between the concentration of nicotine in blood plasma and its dose is linear. The values of maximum nicotine concentrations (Cmax ) at different doses are shown below. Nicotine dose (mg/16 hours) Cmax (ng / ml) 10 1015 15.5 25 26.5 The maximum concentrations of nicotine in blood plasma calculated by the model correspond to the measured values: 11 ng / ml for the use of a 10 mg transdermal patch and 25 ng/ml for 25 mg. The value of the maximum concentration in blood plasma obtained by interpolation when using a 15 mg transdermal patch was 16 ng / ml. The time to reach the maximum plasma concentration (tmax) is approximately 9 hours and is created in the afternoon or evening, when the risk of relapse is maximum. The volume of distribution after intravenous use of nicotine is approximately 2-3 l / kg, its half-life is approximately 2-3 hours. Nicotine is mainly excreted by the liver, with an average plasma clearance of about 70 l / h. Nicotine is also metabolized in the kidneys and lungs. More than 20 nicotine metabolites were identified, the activity of which is inferior to that of the parent substance. The binding of nicotine to plasma proteins is less than 5%. In this regard, violations of nicotine binding with the simultaneous use of other drugs or changes in the content of plasma proteins in various diseases should not significantly affect the kinetics of nicotine. The main metabolite of nicotine, cotinine, has a half-life of 15-20 hours and is found in blood plasma at a concentration that exceeds that of nicotine by 10 times. The main metabolites of nicotine excreted in the urine are cotinine (12% of the administered dose) and trans-3-hydroxy-cotinine (37% of the administered dose). Approximately 10% of nicotine is excreted unchanged in the urine. With a high filtration rate and a urine pH below 5, the amount of nicotine excreted unchanged in the urine can reach 30%. The progression of renal failure may be accompanied by a decrease in total nicotine clearance. In smokers with concomitant chronic renal failure treated with hemodialysis, an increase in the concentration of nicotine in blood plasma was observed. The pharmacokinetics of nicotine in mild hepatic insufficiency (5 points on the Child-Pugh scale) does not change, while in moderate hepatic insufficiency (7 points on the Child-Pugh scale), nicotine clearance decreases. A slight decrease in total nicotine clearance was observed in healthy elderly patients, which, however, does not require dose adjustment. The concentration of nicotine in the blood plasma increases with the use of three types of transdermal patches in proportion to the dose. There were no differences in the pharmacokinetics of nicotine in men and women.

Indications

For the treatment of tobacco addiction by reducing the need for nicotine, removing the “withdrawal” symptoms that occur when quitting smoking in patients with appropriate motivation.

Use during pregnancy and lactation

Smoking during pregnancy is associated with risks such as delayed fetal development, premature birth, or stillbirth. Quitting smoking is the single most effective intervention to improve the health of both the pregnant woman and her baby. Early smoking cessation is the best option.

Nicotine penetrates the placental barrier and affects the fetal respiratory activity and blood circulation. The effect on blood circulation is dose-dependent. Smoking can have serious adverse effects on the fetus and newborn, and therefore should be stopped. Therefore, ideally, quitting smoking during pregnancy should be done without nicotine replacement therapy.

The risk to the fetus when using Nicorette® is not fully understood. However, the benefits of nicotine replacement therapy in pregnant women who cannot stop smoking without such treatment significantly outweigh the risk of continuing smoking. Nicorette ® patch should only be used in highly dependent pregnant women after consulting a doctor.

Nicotine passes into breast milk in amounts that can have an effect on the baby, even if the drug is used in therapeutic doses. Therefore, you should refrain from using the Nicorette ® patch during breastfeeding. If you can’t stop smoking, you should start using the drug only after consulting your doctor.

Smoking increases the risk of infertility in both 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.

Side effects

Regardless of the drug used as a treatment for tobacco addiction, some symptoms may be due to nicotine withdrawal due to smoking cessation. These include: dysphoria or depressed mood; insomnia; irritability, dissatisfaction, or anger; anxiety; difficulty concentrating; restlessness or impatience; decreased heart rate; increased appetite or weight gain; dizziness or pre-fromness; cough, constipation, and bleeding gums. After smoking cessation, the incidence of aphthous ulcers, cough, and nasopharyngitis may also increase. No causal relationship has been established. Nicotine craving, considered a clinically significant symptom, is an important manifestation of nicotine withdrawal after smoking cessation. Nicorette ® patch may cause nicotine-related adverse reactions similar to those observed with other nicotine-containing medications. Most of the adverse reactions reported by patients occur in the early phase of therapy and are mainly dose-dependent. Approximately 20% of patients develop mild local skin reactions during the first weeks of therapy. Allergic reactions (including anaphylactic reactions) may rarely occur in predisposed individuals.

Interaction

There is no clear clinically significant interaction between nicotine replacement therapy and other drugs. However, theoretically, nicotine can enhance the hemodynamic effects of adenosine, i. e., lead to an increase in blood pressure and heart rate, as well as increase the response to pain (chest pain like angina pectoris) provoked by the introduction of adenosine.

How to take it, course of use and dosage

Nicorette ® transdermal patch treatment simulates fluctuations in the nicotine concentration during the day in a smoker; however, during sleep, nicotine does not enter the body. The use of a transdermal nicotine patch during the day does not cause the disturbances observed when nicotine enters the body during sleep.Nicorette ® transdermal patch can be used as monotherapy or in combination with Nicorette® chewing gum 2 mg, Nicorette® sublingual tablets 2 mg or Nicorette® topical spray 1 mg / dose. If symptoms of overdose occur (see section “Overdose”), the drug should be discontinued immediately. Children and adolescents There is no experience of using Nicorette® patch in adolescents under 18 years of age, so the drug should be used by persons under 18 years of age strictly as prescribed by a doctor. Adults Nicorette ® transdermal patch can be used for abrupt smoking cessation, as well as to increase the time intervals between smoking in order to reduce smoking as much as possible until complete smoking cessation. The patient should do everything possible to permanently stop smoking during treatment with Nicorette ® patch. Patients with a high degree of addiction (more than 20 cigarettes per day) are recommended to start with stage 1 therapy, using 1 patch of 25 mg/16 hours, daily, for 8 weeks. Then begin a gradual reduction in the dose of the drug: 1 patch of 15 mg/16 hours, daily, for 2 weeks, and then – 1 patch of 10 mg/16 hours, daily, for the next 2 weeks. Patients with a low degree of addiction (10-20 cigarettes per day) are recommended to start therapy from stage 2, using 1 patch of 15 mg/16 hours, daily, for 8 weeks. Then begin a gradual reduction in the dose of the drug to 3 stages: 1 patch of 10 mg/16 hours, daily, for the next 4 weeks. How to apply a transdermal Patchthe patch is applied to an undamaged area of skin immediately after waking up in the morning and removed before going to bed. The patch should be applied to dry, clean, undamaged skin that does not contain hair, such as the thigh, upper limb or chest. You must change the overlay location 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 ingestion. 1. Wash your hands thoroughly before applying the patch. 2. Cut the patch package with scissors along the edge as indicated on it. Choose a clean, dry area of skin that does not contain hair (for example, the thigh, upper limb, or chest).3. Remove one half of the silver aluminized protective film without touching the adhesive surface of the patch. 4. Fix the part of the patch released from the protective film on the skin and remove the remaining half of the silver aluminized protective film. 5. Press the patch firmly against the skin with your palm or fingertips. 6. Run your finger along the edge of the patch, making sure that it is firmly glued. 7. If the patch comes off, apply a new one. The use of skin care oil or talcum powder may prevent the patch from attaching properly. In combination with chewing gum, sublingual tablets, topical spray For smokers with severe nicotine dependence (more than 20 cigarettes per day) or experiencing an irresistible craving for smoking, or smokers who were unable to quit smoking with only one type of nicotine replacement therapy, the use of Nicorette® patch in combination with Nicorette® chewing gum dosage of 2 mg/Nicorette sublingual tablets is possible to quickly relieve cravings for smoking® dosage of 2 mg/spray for topical application Nicorette® dosage of 1 mg/dose. The patch is applied to an undamaged area of skin immediately after waking up in the morning and removed before going to bed. The patch should be applied to dry, clean, undamaged skin that does not contain hair, such as the thigh, upper limb or chest. You must change the overlay location 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 ingestion. Initial therapy:Treatment should begin with a patch of 25 mg/16 hours (stage 1) in combination with chewing gum 2 mg/sublingual tablets 2 mg/topical spray 1 mg/dose. Usually,5-6 chewable gums/sublingual tablets per day or 13 doses of topical spray per day are sufficient. The maximum daily dose for chewing gum is 15 pieces, for sublingual tablets-24 pieces, for topical spray-32 doses. Patients should completely stop smoking during therapy. Usually, the general course of treatment lasts for 8 weeks. After that, the nicotine dose should be gradually reduced. Discontinuation of combination therapy:There are two ways to cancel combination therapy. Method 1: during the next 2 weeks, it is necessary to switch from the 25 mg/16 hours patch (stage 1) to the 15 mg/16 hours patch (stage 2), and then, during the next 2 weeks, to the 10 mg/16 hours patch (Stage 3), while maintaining, if necessary, the number of chewable gums/sublingual tablets/topical spray doses used, as with Initial therapy. Then gradually reduce the number of chewable gums/sublingual tablets/topical spray doses until complete withdrawal during the time that the patient needs, depending on his needs, but not later than 12 months after the start of combination therapy. Method 2: consists in complete cancellation of the patch immediately after the end of the Initial therapy stage. Then gradually reduce the number of chewable gums/sublingual tablets/topical spray doses until complete withdrawal during the time that the patient needs, depending on his needs, but not later than 12 months after the start of combination therapy.

Overdose

Excessive intake of nicotine during substitution therapy and / or smoking can cause symptoms of overdose. Symptoms of nicotine overdose may occur in patients with low nicotine intake before treatment or when using different sources of nicotine at the same time. Overdose causes the same symptoms as acute nicotine poisoning, such as nausea, vomiting, increased salivation, abdominal pain, diarrhea, sweating, headache, dizziness, hearing loss, and severe general weakness. When high doses are used, the following symptoms may follow these symptoms: low blood pressure, weak and irregular pulse, difficulty breathing, loss of strength, collapse, and generalized convulsions. Nicotine in doses tolerated by adult smokers can cause severe poisoning symptoms in children and even lead to death. Suspected nicotine poisoning in children should be considered as an emergency requiring immediate hospitalization. Treatment of overdose: you should immediately stop using nicotine and prescribe symptomatic treatment. Remove the patch and rinse the patch site with water. Activated charcoal reduces the absorption of nicotine in the gastrointestinal tract. The minimum lethal dose for an acute overdose for a non-smoking adult is 40-60 mg of nicotine.

Description

The patch is rectangular in shape with rounded corners, semi-transparent, beige in color, on a rectangular aluminized and siliconized detachable substrate.

• 10 mg / 16 h with an area of 9 cm 2 +2%,27.7 x 33.2 mm
• 15 mg / 16 h with an area of 13.5 cm 2 +2%,33.2 x 41.3 mm
• 25 mg / 16 h with an area of 22.5 cm 2 +2%,43 x 53 mm.

Special instructions

The use of Nicorette ® is associated with a lower risk than smoking. The Nicorette ® transdermal patch should be removed before performing an MRI (magnetic resonance imaging) scan to avoid burns. Nicotine overdoses, which are easily tolerated by adult smokers and adolescent smokers, can cause severe intoxication in children, which can lead to death. It is important not to leave nicotine-containing products unattended, as this may result in their misuse and ingestion by children (see the section “Overdose”). Addiction Developmentmay develop drug addiction, but it is less dangerous to health and more easily overcome than smoking addiction. Smoking cessation: Polycyclic aromatic hydrocarbons found in tobacco smoke induce the metabolism of drugs that are metabolized by the CYP1A2 isoenzyme (and possibly CYP1A1). Stopping smoking can cause your metabolism to slow down and, as a result, increase the concentration of these drugs in your blood. This has potential clinical implications for drugs with a narrow therapeutic index, such as theophylline, tacrin, clozapine, and ropinirole. Plasma concentrations of other drugs that are partially metabolized by the CYP1A2 isoenzyme, such as imipramine, olanzapine, clomipramine, and fluvoxamine, may also increase after smoking cessation, although there is no evidence to support this hypothesis and the possible clinical significance of this effect is not known. Limited evidence suggests that smoking may induce the metabolism of flecainide and pentazocine. After use, the patch should be folded with the adhesive side inside and disposed of out of the reach of children. Warnings and precautions for the combination therapy of Nicorette transdermal patch with chewable gum/sublingual tablets/topical spray are similar to the warnings and precautions for the use of each of the drugs separately. If the medicine has fallen into disrepair or the expiration date has expired, do not throw it into the sewer or on the street! Place the medicine in a plastic bag and put it in the trash can. These measures will help protect the environment!

Form of production

Transdermal patch

Storage conditions

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

Shelf life

3 years

Active ingredient

Nicotine

Dosage form

transdermal system

Purpose

Nursing mothers as prescribed by a doctor, For adults, Pregnant women as prescribed by a doctor

Indications

Smoking Cessation