Nicotine Dosage Guide

Active substance Nicotine Similar preparations Dosage Form: transdermal therapeutic system Composition: Each TTC 7 mg / day (patch 10 cm2, No. 3) contains:

Active ingredient: nicotine 17.5 mg. The average amount of nicotine released into the skin is 7 mg over 24 hours.

Each TTC 14 mg / day (patch 20 cm 2, No. 2) contains:

Active ingredient: nicotine 35 mg. The average amount of nicotine released into the skin is 14 mg over 24 hours.

Each TTC 21 mg / day (patch 30 cm 2, No. 1) contains:

Active ingredient: nicotine 52.5 mg. The average amount of nicotine released into the skin is 21 mg over 24 hours.

 

 

N.07.B.A.01 Nicotine

Pharmacodynamics: H-holostimulyator, reduces the desire to smoke. Allows you to avoid the development of the syndrome of “cancellation” in people who quit smoking, which is expressed in a pronounced desire for smoking, dysphoria, irritability, frustration, anxiety, irritability, increased appetite or weight gain. The nicotine contained in the patches replaces part of the nicotine that entered the body during smoking, and reduces the severity of the “withdrawal” syndrome, as well as reduces the craving for smoking. Pharmacokinetics: Absorption:

Nicotine is rapidly absorbed through the skin and mucous membranes. In healthy smokers who do not use tobacco (using patches to stop smoking), there is a gradual increase in the concentration of nicotine in the blood plasma 1-2 hours after the application of the nicotinell® patch. Then the concentration of nicotine in the blood plasma gradually increases and levels out after 8-10 hours after application.

After removing the patch, the concentration of nicotine in plasma decreases more slowly than expected, taking into account the half-life of nicotine (2 hours after intravenous administration). About 10% of the total amount of nicotine entering the bloodstream is released from the skin depot formed during the application of the patch. The absolute bioavailability of nicotine in the form of a patch against intravenous levels is about 77%. The area under the concentration-time curve (AUC about -24 h) increases in direct proportion to the increase in the dosage of the patch: 7 mg / day, 14 mg / day, 21 mg / day. With repeated application of the patch with a dosage of 14 mg / day and 21 mg / day, the concentration of nicotine in the plasma ranges from 7.1 to 12.0 ng / ml and from 10.3 to 17.7 ng / ml, respectively. The peak concentration of nicotine in the blood plasma after the application of Nicotinell® TTC № 1 reaches 12.3 ng / ml. The steady plasma concentration of C max after repeated application of Nicotinell® TTC is 12 ng / ml (TTC No. 2), 17.7 ng / ml (TTC No. 1); the minimum concentrations are 7.1 ng / ml (TTC No. 2) and 10.3 ng / ml (TTS No. 1).

In the preparation Nicotinell® TTC nicotine is present in a free form. Nicotine is absorbed continuously throughout the entire period of wearing the patch from the moment of its application.

Distribution:

Nicotine is distributed throughout the body, the volume of distribution is from 1 to 3 l / kg. Nicotine penetrates the blood-brain and placental barriers, as well as penetrates into breast milk. Nicotine has a very low level of binding to plasma proteins (less than 5%), plasma clearance is 0.92-2.43 l / min.

The concentration of nicotine in the blood plasma is in the range that is usually observed with moderate smoking, i.e. when smoking 1 cigarette per hour.

 

 

Metabolism:

Nicotine is derived mainly by the liver. The main metabolites are cotinine and nicotine-GN-oxide. Most of cotinine undergoes repeated metabolism, its metabolites are pharmacologically inactive. Excretion:

The half-life of nicotine is about 2 hours, the clearance from blood plasma is 0.92 – 2.43 l / min.

Through the kidneys, only a small amount of nicotine is excreted unchanged.

Excretion by the kidneys of unchanged nicotine (5-10% of the total) is a pH-dependent process. At alkaline pH values, the level of excretion is low. The cumulation of the substance is very small.

There was an increase in the concentration of cotinine and nicotine in the blood plasma of smokers with impaired liver and kidney function.

Renal failure Progressive renal failure is associated with a decrease in the total clearance of nicotine. In patients with severe renal failure, the clearance of nicotine is reduced by an average of 50%.

Liver failure Nicotine is mainly metabolized in the liver by the CYP2A6 isoenzyme, and its systemic clearance depends mainly on the hepatic blood flow. The pharmacokinetics of the drug Nicotinell® in patients with liver failure has not been studied. It is expected that the pharmacokinetics of nicotine will be under the influence of factors that alter the expression of CYP2A6 and hepatic blood flow. Indications: Treatment of nicotine addiction. Relieving symptoms associated with quitting smoking.

Contraindications: Increased sensitivity of the skin to nicotine or one of the components that make up the drug, vasospastic angina pectoris, acute myocardial infarction, arrhythmia, recently suffered a stroke, pregnancy and lactation.

The drug is contraindicated in non-smokers, children and adolescents.

It is allowed to use the nicotinell® patch as recommended by the doctor for the treatment of adolescents in cases where there is marked nicotine dependence.

 

Carefully: Severe cardiovascular diseases or hospitalization in the preceding 4 weeks (stroke, myocardial infarction, unstable stenocardia, arrhythmia, coronary artery bypass surgery or angioplasty), peripheral blood circulation insufficiency, impaired kidney function, diabetes, uncontrollable arteries, unregulated arteries, unregulated arteries, unregulated arteries, unregulated arteries a stomach ulcer. Pregnancy and lactation: Pregnant women are recommended to quit completely without using nicotine replacement therapy. Nicotine entering the body of a pregnant woman in any form (cigarettes, nicotine replacement therapy drugs, etc.) can have a negative effect on the fetus. Tobacco cessation with the help of nicotine-replacement therapy can only be carried out according to strict indications and directly under the supervision of a physician after assessing the risk / benefit ratio. Breast-feeding

Nicotine penetrates into breast milk in quantities that can have an effect on the newborn. Therefore, during lactation, the use of nicotinell® patches is not recommended.

The use of Nicotinell® patches during the breastfeeding period is carried out only according to strict indications and directly under the supervision of a physician after assessing the risk / benefit ratio.

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