Nicorette therapeutic system patch 25mg/16h №7

NIKORETTE THERAPE. SIS. PLASTER 25MG / 16CH №7

Registration number: LP-001122

Trade name: Nicorette® (Nicorette®)

Grouping name: nicotine

Dosage Form: transdermal patch

Composition:

Nicotine base:

active substance:

nicotine 15.75 mg (10 mg / 16 h), 23.62 mg (15 mg / 16 h), 39.37 mg (25 mg / 16 h),

Excipients:

triglycerides (average chain length) 18.27 mg / 27.41 mg / 45.68 mg, copolymer

basic butyl methacrylate 14.58 mg / 21.87 mg / 36.45 mg, polyethylene terephthalate

film, 19 μm (on one side can be lacquered) - layer carrier,

containing active ingredient

Acrylate base:

acrylic adhesive solution 123.84 mg / 185.76 mg / 309.60 mg, potassium hydroxide

0.70 mg / 1.05 mg / 1.80 mg, croscarmellose sodium 5.00 mg / 7.49 mg / 12.50 mg, aluminum

acetylacetonate 0.06 mg / 0.09 mg / 0.12 mg, polyethylene terephthalate film 100 μm,

aluminized on one side and siliconized on both sides -

carrier, performs the function of protecting the adhesive layer (removable substrate),

discarded before use.

Description:

Rectangular plaster with rounded corners, translucent,

beige, on rectangular aluminized and siliconized

detachable substrate.

10 mg / 16 h, area 9 cm2

+ 2%, 27.7 x 33.2 mm

15 mg / 16 h with an area of ​​13.5 cm2

+ 2%, 33.2x41.3 mm

25 mg / 16 h with an area of ​​22.5 cm2

+ 2%, 43х53 mm

PHARMACOLOGICAL PROPERTIES

Pharmacotherapeutic group: nicotine treatment

dependencies

ATX code: N07BA01

Pharmacodynamics

After abrupt smoking cessation in patients who used daily

tobacco products for a long time may develop

withdrawal syndrome, which includes: dysphoria, insomnia,

irritability, anxiety, impaired concentration,

decrease in heart rate, increase in appetite or increase

body mass. An important symptom of the syndrome of "cancellation" is also the desire

to smoke

In the treatment of tobacco dependence, nicotine replacement therapy reduces

the need for the number of cigarettes smoked reduces the severity of symptoms

“Cancellations” arising from the complete cessation of smoking by those who decided to quit

to smoke; facilitates temporary abstinence from smoking and also contributes to

reducing the number of cigarettes smoked by those who cannot or do not want

completely stop smoking.

Pharmacokinetics

In the therapeutic range (10-25 mg / 16 hours), the relationship between

The concentration of nicotine in the blood plasma and its dose is linear.

Below are the maximum concentrations of nicotine (Cmax) at

use of various doses.

Nicotine dose (mg / 16 hours) Cmax (ng / ml)

10 10

15 15,5

25 26,5

Calculated on the model of the maximum concentration of nicotine in the blood plasma

fit measured: 11 ng / ml when using transdermal

a patch of 10 mg and 25 ng / ml for 25 mg.Interpolated value

maximum plasma concentration when using transdermal

15 mg patch was 16 ng / ml.

The time to reach the maximum plasma concentration (tmax) is

approximately 9 hours and is created in the afternoon or evening, when

the risk of recurrence is maximum.

The volume of distribution of nicotine is approximately 2-3 l / kg, its period

elimination half-life is approximately 3 hours. Nicotine is predominantly excreted.

the liver; average plasma clearance is about 70 l / h. Nicotine also

metabolized in the kidneys and lungs. More than 20 metabolites identified

nicotine, whose activity is inferior to the activity of the original substance.

Communication of nicotine with plasma proteins is less than 5%. In connection with this violation

nicotine binding with the simultaneous use of other drugs or

changes in plasma protein content in various diseases should not

have a significant effect on nicotine kinetics.

The main metabolite of nicotine - cotinine - has a half-life of 15-20

hours and is detected in blood plasma at a concentration greater than that

nicotine 10 times.

The main metabolites of nicotine excreted in the urine are cotinine.

(12% of the administered dose) and trans-3-hydroxy-cotinin (37% of the administered dose).

Approximately 10% of nicotine is excreted in the urine unchanged.

The progression of renal failure may be accompanied by a decrease in

total clearance of nicotine.In smokers with concomitant chronic

renal failure treated with hemodialysis was observed

increasing the concentration of nicotine in the blood plasma.

Nicotine pharmacokinetics in mild hepatic insufficiency

(class A according to Child-Pugh classification) does not change, with hepatic

moderate failure (class B according to Child-Pugh classification)

reduced clearance of nicotine.

A slight decrease in total clearance of nicotine was observed in healthy

elderly patients, which, however, does not require correction of its dose.

The concentration of nicotine in the blood plasma increases with the use of three types

transdermal patches are dose proportional.

INDICATIONS FOR USE

To treat tobacco dependence by reducing the need for nicotine,

relieving “withdrawal” symptoms that occur when quitting smoking in patients,

having the appropriate motivation.

Contraindications

Hypersensitivity to nicotine or other components of the drug.

Carefully

Patients constituting a cardiovascular risk group (those who have

serious cardiovascular diseases hospitalized for

cardiovascular disorders, for example, stroke, myocardial infarction,

unstable angina, cardiac arrhythmias, shunting or angioplasty

coronary arteries, within 4 previous weeks or with uncontrolled

hypertension) should use Nikorette® only after

consultation with a doctor.

The drug should be used with caution in patients with severe or

moderate liver failure, severe renal failure,

and also a peptic ulcer of a stomach or duodenum in a stage

aggravations. At the same time, the risk of nicotine replacement therapy should

correlated with the risk of continuing to smoke.

Nicotine, both released from substitution treatment, and

absorbed while smoking, stimulates the release of catecholamines from the brain

substances adrenal glands. Therefore, the drug should be used with

caution in patients with uncontrolled hyperthyroidism and

pheochromocytoma.

Patients with diabetes may require a reduction in insulin dose.

after quitting smoking.

PREGNANCY AND LACTATION

Nicotine penetrates the placenta and affects the amount of respiratory movements.

and fetal hemocirculation (the latter effect is dose dependent). Smoking can

have a serious adverse effect on the fetus and newborn, and

therefore should be terminated. The use of the patch Nikorette®

pregnancy or lactation is possible only after consultation with

a doctor. The risk to the fetus with Nikorette® is not fully understood.

However, the benefits of nicotine replacement therapy in pregnant women

who can not quit smoking without such treatment, significantly

exceeds the risk of continuing to smoke.

Nicotine in small amounts penetrates into breast milk and can negatively

to influence the child even when used in therapeutic doses.

METHOD OF ADMINISTRATION AND DOSES

Adults and Elderly

The patch is applied to the intact skin immediately after

wake up in the morning and removed before bedtime. Treatment with this drug

imitates fluctuations in the concentration of nicotine during the day in a smoker; at

this during sleep nicotine intake does not occur. Application

during the day, the nicotine transdermal patch does not cause any disruption,

observed during intake of nicotine during sleep.

Heavy smokers (more than 20 cigarettes per day) are recommended to start with 1

stages of therapy, using 1 patch 25 mg / 16 hours daily for 8

weeks.

Then begin a gradual reduction in the dose of the drug: 1 patch 15 mg / 16

hours, daily, for 2 weeks, and then - 1 patch 10 mg / 16 hours,

daily for 2 weeks.

Smooth smokers (10–20 cigarettes per day) are advised to begin therapy.

from stage 2 (15 mg) for 8 weeks, then dose reduction to stage 3 (10 mg)

during the final 4 weeks.

Heavy smokers Non-smoking smokers

Dosage regimen Duration Dosage regimen Duration

Stage 1 Nikorette®

25 mg patch

First

8 weeks

Stage 2 Nikorette®

15 mg patch

The following

2 weeks

Stage 2 Nikorette®

15 mg patch

First

8 weeks

Stage 3 Nikorette®

10 mg patch

The last

2 weeks

Stage 3 Nikorette®

10 mg patch

The last

4 weeks

In most cases, the use of a transdermal patch for more than

6 months is not recommended. However, some people may need

longer therapy to not resume smoking.

How to apply a transdermal patch

Nikorette® plaster should be applied to a dry, clean, undamaged

skin that does not contain hair, such as the thigh, upper limb, or chest

cells It is necessary to change the location of the overlay every day: do not

use the same area over the next two days.

1. Wash your hands thoroughly before applying the patch.

2. Cut the packaging of the patch with scissors along the edge as indicated on it.

6504887Choose a clean, dry skin that does not contain hair (for example,

thigh, upper limb or chest).

3. Remove one half of the silver aluminized protective film, not

touching the adhesive surface of the patch.

4. Strengthen part of the patch released from the protective film on the skin and

remove the remaining half of the silver aluminized protective

film.

5. Press the patch firmly onto the skin with your palm or fingertips.

6. Slide your finger along the edge of the patch, making sure it is tight.

glued.

Please note that the next day should apply

just a new patch!

SIDE EFFECT

The Nikorette® plaster may cause undesirable reactions similar to

developing with other methods of nicotine administration; Most of them

dose-dependent.

Approximately 20% of patients develop during the first weeks of therapy.

unexpressed local skin reactions.

Some symptoms, including dizziness, headache and insomnia,

may be due to the syndrome of "cancellation" with quitting smoking. Same

circumstance may be caused by an increase in the frequency of aphthous

stomatitis, however true causation is unclear.

Very often (> 1/10); often (> 1/100, but <1/10); infrequently (> 1/1 000, but <1/100);

rarely (> 1/10 000, but <1/1000); very rarely (<1/10 000), including some

messages.

Violations by

nervous system:

Often dizziness, headache

pain

Cardiac Disorders: Infrequently Palpitations

Very rarely reversible fibrillation

atrial

Violations by

digestive system:

Often gastrointestinal

discomfort, nausea, vomiting.

Adverse events with

skin side and subcutaneous

fabrics

Infrequent urticaria

Systemic abnormalities and

complications in place

introductions

Very often itchy skin

Often erythema

Overdose

Excessive intake of nicotine during replacement therapy and / or smoking

may cause symptoms of overdose.

Nicotine overdose may occur with simultaneous use

several transdermal patches, depending on the very

low doses, as well as when combining transdermal patches with other

sources of nicotine, including smoking.

Signs of overdose that develop in acute nicotine poisoning,

include nausea, excessive salivation, abdominal pain, diarrhea,

sweating, headache, dizziness, hearing impairment and severe

weakness.With the use of high doses following these symptoms may

decrease in blood pressure, weak and irregular heartbeats, difficulty

respiration, prostration, collapse and generalized convulsions.

Nicotine in doses tolerated by adult smokers can cause in children

severe symptoms of intoxication, including fatal.

Treatment of overdose: should stop quitting nicotine immediately

and prescribe symptomatic treatment. Activated carbon reduces

absorption of nicotine in the gastrointestinal tract.

INTERACTION WITH OTHER MEDICINES

Smoking (but not nicotine) causes an increase in the activity of the CYP1A2 isoenzyme.

After smoking cessation, a decrease in substrate clearance may be observed.

of this isoenzyme. This may lead to an increase in the concentration of some

plasma drugs that has potential clinical

value when using drugs with a narrow therapeutic range,

such as theophylline, takrin, clozapine and ropinirole.

After cessation of smoking, plasma concentrations may also increase.

other drugs that are partially metabolized by the isoenzyme CYP1A2,

such as imipramine, olanzapine , clomipramine and fluvoxamine, although the data

confirming this hypothesis, are absent, and the possible clinical significance

no such effect is known.

Limited evidence suggests that smoking may induce

Flecainide and pentazocine metabolism.

SPECIAL INSTRUCTIONS

Patients constituting a cardiovascular risk group (those who have

serious cardiovascular diseases hospitalized for

cardiovascular disorders, for example, stroke, myocardial infarction,

unstable angina, cardiac arrhythmias, shunting or angioplasty

coronary arteries, within 4 previous weeks or with uncontrolled

hypertension), should use the Nikorette® patch only

after consulting a doctor.

Nikorette® should be used with caution in patients with severe or

moderate liver failure, severe renal failure,

and also a peptic ulcer of a stomach or duodenum in a stage

aggravations. At the same time, the risk of nicotine replacement therapy should

correlated with the risk of continuing to smoke.

Nicotine, both released from substitution treatment, and

absorbed while smoking, stimulates the release of catecholamines from the brain

substances adrenal glands. Therefore Nikorette® should be applied with

caution in patients with uncontrolled hyperthyroidism and

pheochromocytoma.

Patients with diabetes mellitus may need a lower dose of insulin

after quitting smoking.

Information about the possible effects of the drug for

medical use on the ability to manage transport

means, mechanisms.

The side effect profile of the drug should be taken into account.

(dizziness), which may impair the ability to manage traffic

means and engage others.activities requiring increased

concentration of attention and quickness of psycho-motor reactions.

If the drug has become unusable or has expired - not

throw it in sewage or on the street! Place the medicinal

means in the package and put in the trash. These measures will help protect

environment!

The use of Nikorette® is accompanied by a lower risk than smoking!

FORM ISSUE

Transdermal patch 10 mg / 16 h, 15 mg / 16 h, 25 mg / 16 h.

1 patch 10 mg / 16 h, 15 mg / 16 h or 25 mg / 16 h in a sachet. On 7, 14 or 28 sachets

together with the application instruction in a cardboard pack.

STORAGE CONDITIONS

Store at a temperature not higher than 25 ° С.

Keep out of the reach of children.

SHELF LIFE

3 years.

Do not use after the expiration date printed on the package!

CONDITIONS FOR VACATION FROM DRUGSTORES

It is released without a prescription.

MANUFACTURER

Manufacturer of finished dosage form:

“LTS Lohmann Therapy-Systems AG”, Germany

Legal address: Lohmannstr 2, 56626 Andernach, Germany / Lohmannstrasse

2, 56626 Andernach, Germany.

Issuing quality control:

McNeil AB, Sweden.

Legal address: McNeil AB, Norrbroplatsen 2, SE-251 09, Helsingborg, Sweden / McNeil AB, Sweden, Helsingborg, SE-251 09, Norbroplatzen 2.

Claims handling organization:

LLC Johnson & Johnson, Russia, 121614, Moscow, ul. Krylatskaya, 17,