Pharmacy No. 84. Delivery of medicines to your home and office.

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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.

Compound

1 tab. nicotine-?-cyclodextrin complex 17.1 mg, which corresponds to a nicotine content of 2 mg Excipients: ?-cyclodextrin (Betadex) - 69.55 mg, crospovidone - 2 mg, magnesium stearate - 0.9 mg, colloidal silicon dioxide - 0.45 mg. 1 ml nicotine 13.6 mg Excipients: propylene glycol - 150 mg, ethanol - 97 mg, trometamol - 40.5 mg, poloxamer - 40 mg, glycerol - 25 mg, sodium bicarbonate - 14.3 mg, levomenthol - 10 mg, mint flavor QL24245 - 4 mg , flavor Cooler 2 SN046680 - 3 mg, sucralose - 1.5 mg, acesulfame potassium - 1.5 mg, hydrochloric acid 10% - sufficient amount up to pH 9, water - sufficient amount up to 1 ml. 1 tab. nicotine-?-cyclodextrin complex 17.1 mg, which corresponds to a nicotine content of 2 mg Excipients: ?-cyclodextrin (Betadex) - 69.55 mg, crospovidone - 2 mg, magnesium stearate - 0.9 mg, colloidal silicon dioxide - 0.45 mg. nicotine 830 mcg/cm2 15 mg/dose Excipients: backing film, non-woven polyester, medium molecular weight polyisobutylene, low molecular weight polyisobutylene, polybutene, siliconized polyester. Nicotine 15.75 mg; Auxiliary ingredients: triglycerides, copolymer of basic butyl methacrylate Nicotine 323.62; Auxiliary ingredients: triglycerides, copolymer of basic butyl methacrylate Nicotine 39.37; Excipients: triglycerides, copolymer of basic butyl methacrylate nicotine 5 mg Excipients: support film, non-woven polyester, medium molecular weight polyisobutylene, low molecular weight polyisobutylene, polybutene, siliconized polyester. nicotine 10 mg Excipients: support film, non-woven polyester, medium molecular weight polyisobutylene, low molecular weight polyisobutylene, polybutene, siliconized polyester. nicotine-polymer complex 22 mg, which corresponds to nicotine content* 4 mg * nicotine content 4.4 mg, including 10% excess. Excipients: chewing gum base**, xylitol, peppermint oil, sodium carbonate, acesulfame potassium, levomenthol, magnesium oxide, quinoline yellow (E104). ** Chewing gum base: a mixture of various types of wax, resin and other hydrocarbons (about 60%) and calcium carbonate (up to 40%). Chewing gum shell: xylitol, peppermint oil, acacia gum, titanium dioxide, carnauba wax, quinoline yellow (E104). nicotine-polymer complex 11 mg, which corresponds to the nicotine content** 2 mg * - nicotine resinate containing 20% nicotine. ** — nicotine content 2.2 mg, including 10% excess. Excipients: chewing gum base (a mixture of various types of wax, resin and other hydrocarbons (about 60%) and calcium carbonate (up to 40%)), xylitol, peppermint oil, sodium carbonate, sodium bicarbonate, acesulfame potassium, levomenthol, magnesium oxide . Inner shell composition: Winterfresh flavor, hypromellose, sucralose, polysorbate 80. Outer shell composition: xylitol, pregelatinized starch, titanium dioxide, Winterfresh flavor, carnauba wax. nicotine-polymer complex* 11 mg, which corresponds to the nicotine content** 2 mg Excipients: chewing gum base (a mixture of various types of wax, resin and other hydrocarbons (about 60%) and calcium carbonate (up to 40%)), xylitol, oil peppermint, sodium carbonate, sodium bicarbonate, acesulfame potassium, levomenthol, magnesium oxide. Composition of the inner shell: tutti-frutti KuEl84441, hypromellose, sucralose, polysorbate 80. Composition of the outer shell: xylitol, acacia, titanium dioxide, tutti-frutti KuEl84441, carnauba wax. * - nicotine resinate containing 20% nicotine. ** — nicotine content 2.2 mg, including 10% excess. nicotine-polymer complex* 11 mg, which corresponds to the nicotine content** 4 mg Excipients: chewing gum base (a mixture of various types of wax, resin and other hydrocarbons (about 60%) and calcium carbonate (up to 40%)), xylitol, mint oil pepper, sodium carbonate, sodium bicarbonate, acesulfame potassium, levomenthol, magnesium oxide. Composition of the inner shell: tutti-frutti KuEl84441, hypromellose, sucralose, polysorbate 80. Composition of the outer shell: xylitol, acacia, titanium dioxide, tutti-frutti KuEl84441, carnauba wax. * - nicotine resinate containing 20% nicotine. ** — nicotine content 2.2 mg, including 10% excess. nicotine-polymer complex* 22 mg, which corresponds to the nicotine content** 4 mg * - nicotine resinate containing 20% nicotine. ** — nicotine content 4.4 mg, including 10% excess. Excipients: chewing gum base (a mixture of various types of wax, resin and other hydrocarbons (about 60%) and calcium carbonate (up to 40%)), xylitol, peppermint oil, sodium carbonate, acesulfame potassium, levomenthol, magnesium oxide, quinoline yellow (E104). Inner shell composition: Winterfresh flavor, hypromellose, sucralose, polysorbate 80. Outer shell composition: xylitol, pregelatinized starch, titanium dioxide, Winterfresh flavor, carnauba wax, quinoline yellow (E104). nicotine-polymer complex 11 mg, which corresponds to nicotine content * 2 mg * nicotine content 2.2 mg, including 10% excess. Excipients: chewing gum base**, xylitol, peppermint oil, sodium carbonate, sodium bicarbonate, acesulfame potassium, levomenthol, magnesium oxide. ** Chewing gum base: a mixture of various types of wax, resin and other hydrocarbons (about 60%) and calcium carbonate (up to 40%). Chewing gum shell: xylitol, peppermint oil, acacia gum, titanium dioxide, carnauba wax.

Contraindications

- hypersensitivity to nicotine and other components of the drug. The drug should be used with caution and only after consultation with a doctor in patients with disorders of the cardiovascular system, incl. who have had a cardiovascular disease within 1 month before starting use (including stroke, myocardial infarction, unstable angina, arrhythmia, coronary artery bypass grafting, angioplasty), or with uncontrolled arterial hypertension. The drug should be prescribed with caution to patients with moderate or severe liver dysfunction, severe renal failure, exacerbation of gastric and duodenal ulcers. The drug should be used with caution in patients with uncontrolled hyperthyroidism, pheochromocytoma (due to the fact that nicotine entering the human body during replacement therapy or smoking causes the release of catecholamines from the adrenal medulla), as well as diabetes mellitus.

pharmachologic effect

N-cholinomimetic. Interacts with peripheral and central n-cholinergic receptors. In low concentrations it excites them, in high concentrations it blocks them. In ganglia, the first phase (excitation) is associated with depolarization of the membranes of ganglionic neurons, the second (inhibition) is associated with competitive antagonism with acetylcholine. In the central nervous system, it influences the content and modulates the release of acetylcholine, norepinephrine, serotonin and other mediators in the endings of neurons. Reduces the secretion of growth hormone and gonadotropins, increases the secretion of catecholamines and ADH. Promotes the release of endorphins. The effect on the central nervous system (excitation or depression) depends on the doses, the intervals between them and the psychological state of the person. Small doses excite the central nervous system, incl. vomiting center Nicotine can cause tremors and seizures. Stimulates the respiratory center (reflexively from the chemoreceptors of the sinocarotid zone, and directly). The effect on the cardiovascular system is due to the activation of sympathetic influences: tachycardia (ventricular extrasystole is possible), increased blood pressure, impaired blood supply to organs and tissues (vasoconstriction), hypernoradrenalinemia, increased glycogenolysis, etc. Nicotine increases cardiac output, cardiac function and increases myocardial oxygen consumption . Activation of the parasympathetic ganglia leads to increased secretion (of bronchial glands and acidic gastric juice) and tone of smooth muscles of the bronchi and gastrointestinal tract. Facilitates neuromuscular transmission. Increases the content of fatty acids in the blood and the adhesive ability of platelets. Addiction to nicotine gradually develops. Well absorbed from mucous membranes. The plasma half-life is 2 hours. Metabolic products and a small amount of unchanged alkaloid are excreted in the urine in the first 10-15 hours. Nicotine penetrates into mother's milk and can create high concentrations in it, sufficient for the development of intoxication, incl. respiratory arrest in a child. During pregnancy, the risk of spontaneous abortion (as a result of oxygen deficiency in the blood) and disturbances in the development of the placenta associated with a large amount of abnormal DNA in it increases.

How to use Nicorette patch

This remedy is recommended for heavy smokers who find it difficult to tolerate giving up their usual doses. One patch is intended for 1 day, it must be put on in the morning and removed before bed:

the plate should be carefully cut out of the packaging with scissors;
detach the backing and apply the adhesive side to the skin: on the inner thigh or other area where there is no thick hair or damage, the skin must be dry and clean;
Carefully press the patch over the entire surface, avoiding touching the adhesive side.

Nicotine is released from the drug gradually, absorbed through the pores into the blood in small doses and neutralizes negative withdrawal symptoms. A new patch must be used daily. The course of use of the product is up to 8 weeks.

For moderate or slight cravings for smoking, it is recommended to apply the product every other day or every 2 days, each time extending the nicotine-free break until the need for nicotine doping subsides. For intense cravings, you can supplement the action of the patches with another Nicorette product: spray, tablets or chewing gum.