Nicorette, 25 mg/16 h 7 pcs.

Pharmacodynamics:

After abrupt smoking cessation in patients who have used tobacco-containing products daily for a long time, development of “withdrawal” syndrome is possible, which includes: dysphoria or depressed mood, insomnia, increased irritability, frustration or anger, anxiety, impaired concentration, anxiety or impatience, reduced heart rate, increased appetite or increased body weight. An important symptom of withdrawal syndrome is also a desire to smoke.

In the treatment of tobacco addiction nicotine replacement therapy reduces the number of cigarettes smoked, reduces the severity of withdrawal symptoms arising from complete smoking cessation in those who choose to quit smoking; facilitates temporary abstinence from smoking, and helps to reduce the number of cigarettes smoked by those who can not or do not want to give up smoking completely.

Pharmacokinetics:

Nicotine is slowly released from the Nicorette® patch and is continuously absorbed through the skin. The Nicorette® patch is designed to be used during waking hours, i.e. for approximately 16 hours, which coincides with the period of nicotine intake from smoking. This prevents sleep disturbances 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 plasma nicotine concentration 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 10
15 15 15.5
25 26.5

The maximum plasma nicotine concentrations calculated from the model correspond to those measured: 11 ng/mL for the 10 mg transdermal patch and 25 ng/mL for 25 mg. The maximum plasma concentration value obtained by interpolation when using the 15 mg transdermal patch was 16 ng/ml.

The time of reaching 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 administration of nicotine is approximately 2-3 L/kg and its half-life is approximately 2-3 hours. Nicotine is primarily excreted by the liver, the average plasma clearance is about 70 liters/hour. Nicotine is also metabolized in the kidneys and lungs. More than 20 metabolites of nicotine have been identified, the activity of which is inferior to that of the original substance.

The binding of nicotine to plasma proteins is less than 5%.

The main metabolite of nicotine – cotinine – has a half-life of 15-20 hours and is found in plasma at a concentration 10 times higher than that of nicotine.

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).

About 10% of nicotine is excreted unchanged in the urine. At high filtration rate and urine pH below 5, the amount of nicotine excreted unchanged in the urine may reach 30%.

Progression of renal failure may be accompanied by decreased total nicotine clearance. Smokers with concomitant chronic renal failure treated with hemodialysis have increased plasma nicotine concentration.

Pharmacokinetics of nicotine in mild hepatic failure (5 points on the Child-Pugh scale) does not change, in moderate hepatic failure (7 points on the Child-Pugh scale) nicotine clearance is reduced.

A slight decrease in total nicotine clearance has been noted in healthy elderly patients, which, however, does not require dose adjustment.

Plasma nicotine concentration increases with the three types of transdermal patches in proportion to the dose.

No differences in nicotine pharmacokinetics were observed in men and women.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Synopsis

Contraindications

Side effects

Overdose

Pregnancy use

Smoking during pregnancy is associated with risks such as intrauterine delay, premature birth or stillbirth. Smoking cessation 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 fetal respiratory activity and circulation. The effect on circulation is dose-dependent. Smoking can have serious adverse effects on the fetus and the newborn, and should therefore be stopped. Therefore, ideally, smoking cessation during pregnancy should be done without nicotine replacement therapy.

The risks to the fetus when using Nicorette® have not been fully studied. However, the benefits of nicotine replacement therapy in pregnant women who are unable to quit smoking without such treatment far outweigh the risk of continued smoking. Nicorette® patch should only be used in pregnant women with high dependence after consulting a physician.

Nicotine passes into breast milk in amounts that may affect the baby, even when used in therapeutic doses. Therefore, you should refrain from using Nicorette® patch during breastfeeding. If it is not possible to stop smoking, the drug should be started only after consulting a physician.

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