NIKORETTE (Transdermal therapeutic system)

Active material: Nicotine
When ATH: N07BA01
CCF: Drug for the treatment of nicotine addiction
ICD-10 codes (testimony): F17
When CSF: 02.17
Manufacturer: JOHNSON & JOHNSON LTD (Russia)

PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING

◊ Transdermal therapeutic system (TST) with a contact surface 10 cm²; It is a rectangular patch with rounded edges, one side is light brown with inscription “Nicorette^®“, the second side of the adhesive, silvery-white, covered with a transparent protective film of synthetic.

Excipients: film substrate, polyester nonwoven, medium weight polyisobutylene, low molecular weight polyisobutylene, polybutene, siliconized polyester.

1 PC. – sachet (7) – packs cardboard.

◊ Transdermal therapeutic system (TST) with a contact surface 20 cm²; It is a rectangular patch with rounded edges, one side is light brown with inscription “Nicorette^®“, the second side of the adhesive, silvery-white, covered with a transparent protective film of synthetic.

Excipients: film substrate, polyester nonwoven, medium weight polyisobutylene, low molecular weight polyisobutylene, polybutene, siliconized polyester.

1 PC. – sachet (7) – packs cardboard.

◊ Transdermal therapeutic system (TST) with a contact surface 30 cm²; It is a rectangular patch with rounded edges, one side is light brown with inscription “Nicorette^®“, the second side of the adhesive, silvery-white, covered with a transparent protective film of synthetic.

Excipients: film substrate, polyester nonwoven, medium weight polyisobutylene, low molecular weight polyisobutylene, polybutene, siliconized polyester.

1 PC. – sachet (7) – packs cardboard.

Pharmacological action

Drug for the treatment of nicotine addiction. After a sharp smoking cessation in patients, daily use nicotine products for a long time, may develop withdrawal, which includes dysphoria, insomnia, increased irritability, alarm, impaired concentration, a decrease in heart rate, increased appetite and weight gain, as well as the desire to smoke.

In the treatment of nicotine addiction with nicotine replacement therapy can reduce the need for smoking (and the number of cigarettes smoked), reduce the severity of withdrawal symptoms, arising from the full smoking cessation in those, who decided to quit smoking. Facilitates temporary abstinence from smoking and reduces the number of cigarettes smoked in those, who can not or does not want to completely give up smoking.

Pharmacokinetics

The pharmacokinetics of nicotine comparable to when applying the patch to the skin of the hand or thigh.

Absorption

After applying the patch to the skin of the hand, or hip about 95% liberated nicotine enters the systemic circulation. The remainder of the edges of the patch evaporated. All patches indicated the average amount of nicotine, is absorbed in the average patient during 16 no.

C_max of nicotine in the blood plasma after application of the patch is achieved by 6-10 hour after applying the patch 15 mg / 16 hours of 9-15 ng / ml. If the patch 15 mg / 16 hours to leave 24 no (rather than 16 no), the concentration of nicotine during the last 8 h is reduced from an average of 7.2 to 5.6 ng / ml. When using smaller patches can expect similar changes in the plasma concentration of nicotine.

If three doses patch nicotine plasma concentrations were somewhat different from a proportional increase in dose: patch size is increased a corresponding increase in the concentration was slightly below the expected.

Distribution

V_d nicotine / introduction is about 2-3 l / kg. Nicotine binding to plasma proteins is less than 5%. Therefore disturbances nicotine binding, while the application of other drugs or modify the amount of protein in the plasma at various diseases should not have a significant effect on the kinetics of nicotine.

Repeated use of the concentration of nicotine patch is not significantly higher than that after a single use.

Metabolism

Nicotine is metabolized in the liver, kidney and lung. Identified more 20 metabolites, are inferior to the activity of nicotine. Metabolite concentration pervichnogo – cotinine – greater than the concentration of nicotine in 10 time.

Deduction

Write mainly by the liver. The average plasma clearance is about 70 l /. T_1/2 – about 2 no.

The urine output is mainly cotinine (15% dose, T_1/2 – 15-20 no) and trans-3-hydroxy-cotinine (45% dose). 10-30% nicotine dose is excreted in the urine in unchanged form.

Pharmacokinetics in special clinical situations

The progressive deterioration of renal function associated with reduced total clearance of nicotine.

The pharmacokinetics of nicotine is not significantly altered in patients with cirrhosis of the liver with slightly severe hepatic impairment (5 points on the Child-Pugh) and reduced in patients with liver cirrhosis with moderately severe hepatic impairment (7 points on the Child-Pugh).

Patients, hemodialysis, marked increase in the concentration of nicotine in the blood plasma.

Elderly patients have a decrease in the total clearance of nicotine, that does not require dose adjustments.

Testimony

- Treatment of tobacco dependence by reducing the need for nicotine;

- The removal of withdrawal symptoms, arising from smoking cessation in patients, having the proper motivation.

Dosage regimen

In Adult (incl. the elderly) treatment begins with the application 1 Patch 15 mg / 16 h (30 cm²), which is applied to intact skin every morning (directly after waking) and removed before bedtime.

The duration of the initial period of treatment is determined individually, thus it is generally, at least, 3 Months. Then gradually phased replacement therapy. Thus for 2-3 weeks of daily impose one patch 10 mg / 16 h (20 cm²), and during subsequent 2-3 weeks - one patch 5 mg / 16 h (10 cm²).

Apply patches for more 6 months is generally not recommended.

In some cases, persons, dropped out smoking, It may require longer therapy.

Side effect

Plasters Nïkorette^® can cause dose-related adverse (primarily) effects, similar to those arising from the application of nicotine, entering the body through the other.

In the description, the following adverse effects frequency of criteria: Often (>1/10), often (>1/100 <1/10), infrequently (>1/1000, <1/100), rarely (>1/10 000, <1/1000), rarely (<1/10 000), including individual cases.

Dizziness, headache, Sleep disorders can be manifestations of the syndrome, caused by quitting smoking. When quitting smoking may increase the incidence of canker sores (cause unknown).

Local reactions: about 20% – moderately expressed redness, itch.

Cardio-vascular system: infrequently - palpitations; very rarely - atrial fibrillation.

From the digestive system: often - nausea, vomiting.

Dermatological reactions: rarely - urticaria.

From the body as a whole: very often - itching; often - erythema.

Contraindications

- Hypersensitivity to the drug.

FROM caution and only after consulting a doctor should be prescribed to patients, suffered a cardio-vascular disease, or hospitalized in this regard during the previous 4 weeks (incl. stroke, myocardial infarction, unstable angina, arrhythmia, coronary artery bypass grafting, Angioplasty), or with uncontrolled hypertension.

FROM caution It should be prescribed to patients with moderate or severe hepatic impairment, severe renal insufficiency, aggravation of gastric ulcer and duodenal ulcer.

FROM caution should be applied to patients with uncontrolled hyperthyroidism, pheochromocytoma (because, that nicotine causes the release of catecholamines from the adrenal medulla).

Pregnancy and lactation

The possibility of the use of the drug during pregnancy is solved individually.

Nicotine crosses the placental barrier and affect the respiratory system and fetal circulation (dose dependent). The risk for the fetus, associated with the use of the drug during pregnancy, is not fully understood. The use of nicotine replacement therapy for pregnant women, who can not give up smoking, far outweighs the risk, associated with continuing smoking.

Nicotine (even when used in therapeutic doses) in small quantities vydelyaetchya breast milk and may affect the newborn. If necessary, use during lactation should stop breastfeeding.

Cautions

Patients with diabetes after stopping smoking may require dose reduction of insulin.

Use in Pediatrics

The question of the appointment of the drug patients in age of 18 years It is decided by the doctor individually. The experience of the patch in this age group is limited.

Overdose

Excessive intake of nicotine replacement therapy and / or smoking might cause symptoms of an overdose.

Symptoms: nausea, salivation, abdominal pain, diarrhea, Sweating, headache, dizziness, hearing disorder, severe weakness (similar to the symptoms of acute nicotine poisoning). When using high doses of nicotine may decrease blood pressure, weak and intermittent pulse, difficulty breathing, vascular collapse, generalized seizures, prostration.

Nicotine in adult smokers tolerated doses can cause severe intoxication in small children (incl. Fatal).

Treatment: should immediately stop using the product (remove patch) and initiate symptomatic treatment. Activated charcoal reduces the absorption of nicotine from the gastrointestinal tract.

Drug Interactions

Smoking (but the use of nicotine) It causes an increase in activity of CYP1A2 isoenzyme. After stopping smoking there may be a decrease in clearance of substrates of this enzyme, which may lead to increased concentrations of certain drugs in plasma, that has potential clinical value while using drugs, characterized by small breadth of therapeutic action (theophylline, tacrine, klozapyn, ropynyrol).

After quitting smoking may increase plasma concentrations of other drugs, which are partly metabolized by CYP1A2 isoenzyme action (such as imipramine, olanzapine, clomipramine, fluvoxamine), although data, prove it, no, and the possible clinical significance of this interaction is not known.

Limited data suggest that, smoking may induce the metabolism of flecainide and pentazocine.

Conditions of supply of pharmacies

The drug is resolved to application as an agent Valium holidays.

Conditions and terms

The drug should be stored out of reach of children at or above 25 ° C. Shelf life - 3 year.