Nicorette Fruit, 4 mg 20 pcs.

H-cholinomimetic. An alkaloid found in the leaves of tobacco (Nicotiana tabacum and Nicotiana rustica) and some other plants. It affects peripheral and central n-cholinoreceptors. The most sensitive to nicotine are the n-cholinoreceptors of the autonomic ganglia, on which nicotine has a biphasic effect. The excitation phase is characterized by depolarization of ganglionic neurons membranes, the inhibition phase is due to competitive antagonism with acetylcholine.

Nicotine stimulates chemoreceptors of sinocarotid zone, which is accompanied by reflex excitation of respiratory and vasomotor centers. The phase of inhibition is observed in case of significant amount of nicotine accumulation in blood.

In low doses nicotine excites n-cholinoreceptors of adrenal chromaffin cells and therefore increases adrenaline release into blood. In high doses nicotine causes the opposite effect.
At doses much higher than those required to influence the autonomic ganglia, nicotine first facilitates and then inhibits neuromuscular transmission.

In the action of nicotine on synaptic transmission in the CNS there is also a biphase: in low doses the substance causes an excitatory effect, in high – inhibitory.

HR after nicotine injection first slows down (excitation of vagus nerve center and intramural parasympathetic ganglia), then it increases (stimulation of sympathetic ganglia and increase in adrenaline by chromaffin cells).

Nicotine in low doses increases BP due to excitation of sympathetic ganglia and the vasomotor center, increased adrenaline release by the adrenal medullary layer and direct myotropic vasoconstrictor effect.

The effect of nicotine is often manifested by nausea (central origin), sometimes vomiting. Intestinal motility nicotine increases. Salivary and bronchial gland secretion is initially increased, followed by inhibition.

Pharmacokinetics

It is well absorbed from mucous membranes. Binding of nicotine with plasma proteins is less than 5%. Metabolism of nicotine occurs mainly in liver, also metabolized in kidneys and lungs. Passes through the BBB. It is excreted with breast milk. T1/2 is 2-3 hours. 10-30% of nicotine dose is excreted unchanged by the kidneys.

Indications

Treatment of tobacco addiction and relief of symptoms arising from smoking cessation.

Composition

1 tablet contains:

nicotine resinate – 21 mg, which corresponds to the nicotine content – 4 mg;

Excipients: Mannitol – 536.9 mg, xanthan gum – 12 mg, Tutti Frutti flavoring – 9.6 mg, sodium carbonate – 7 mg, sucralose – 1 mg, acesulfame K – 0.

Tablet shell: Hypromellose – 17 mg, Tutti Frutti liquid flavoring – 1 mg, titanium dioxide – 2.2 mg, sucralose – 0.8 mg, acesulfame potassium – 0.4 mg, polysorbate-80 – 0.1 mg, polishing agent Sepifilm Gloss – 1 mg.

How to take, the dosage

Set individually, depending on the degree of dependence on tobacco and the drug form used.

Interaction

Smoking (but not nicotine) causes increased activity of CYP1A2 enzyme. After smoking cessation, a decrease in clearance of substrates of this enzyme may be observed. This may lead to increased plasma levels of some drugs, which has potential clinical significance in the use of drugs characterized by low therapeutic latency, such as theophylline, tacrine, clozapine and ropinirole.

Plasma concentrations of other active substances metabolized with cytochrome CYT1A2 (such as caffeine, paracetamol, phenazone, phenylbutazone, pentazocine, lidocaine, benzodiazepines, warfarin, estrogens, vitamin B12) may also increase.

Smoking may decrease the analgesic effect of propoxyphene, decrease the diuretic effect of furosemide, weaken the effects of propranololol on BP and HR, and lead to delayed ulcer scarring with H2-antagonists.

Cortisol and catecholamine blood levels may increase under the influence of smoking and nicotine administration, i.e.i.e., this may lead to a reduction in the effect of nifedipine or adrenergic receptor antagonists and an increase in the effect of adrenoreceptor agonists.

As a result of increased subcutaneous insulin absorption that occurs after smoking cessation, patients may need to reduce the insulin dose.

Special Instructions

Patients with diabetes mellitus after stopping smoking and since the start of nicotine replacement therapy are recommended to monitor blood glucose concentration more carefully, since a decrease in catecholamines, the release of which is induced by nicotine, may affect carbohydrate metabolism. Patients with diabetes may need to reduce their insulin doses after stopping smoking.

Polycyclic aromatic hydrocarbons in tobacco smoke induce the metabolism of drugs metabolized by the CYP1A2 isoenzyme (and possibly CYP1A1). Smoking cessation may cause slower metabolism and, consequently, increased blood concentrations of these drugs. This has potential clinical implications for drugs with a narrow therapeutic index – such as theophylline, tacrine, clozapine, and ropinirole.

Nicotine is used in experimental pharmacology to analyze the effects of substances. Because of the widespread use of tobacco smoking, nicotine is of considerable interest in toxicological terms. In medical practice, its use is limited to use to facilitate smoking cessation.

Contraindications

Hypersensitivity to nicotine; severe arrhythmia, arterial hypertension, unstable angina, myocardial infarction and cerebral circulation disorders (recently suffered); pregnancy and breast-feeding – depending on the dosage form; children and adolescents under 18 years – depending on the dosage form.

With caution: patients who have undergone bypass surgery or angioplasty within the last month; patients with moderate or severe liver function abnormalities, severe renal failure; exacerbation of esophagitis, duodenal and gastric ulcers; with inflammatory diseases of the mouth or throat; patients with diseases of cerebral vessels.

Nicotine, entering the body during substitution therapy or smoking, causes release of catecholamines from the cerebral adrenal layer. Therefore, this drug should be used with caution in patients with uncontrolled hyperthyroidism, pheochromocytoma, diabetes mellitus.