Назонекс®

General characteristics. Structure:

Active ingredient: 50 mkg of a mometazon of furoate in the form of monohydrate in 1 dose (500 mkg in 1 g of solution).

Excipients: cellulose disperse (cellulose microcrystallic, processed karmellozy sodium), глицерол, citric acid monohydrate, citrate sodium a dihydrate, polysorbate 80, a benzalkoniya chloride (in the form of 50% of solution), the water purified.

Pharmacological properties:

Pharmacodynamics. GKS for topical administration. Has antiinflammatory and antiallergic effect. Local antiinflammatory effect of drug is shown at its use in doses at which there are no system effects.

Slows down release of mediators of an inflammation. Raises products of the lipomodulin which is inhibitor of a phospholipase And that causes decrease in release of arachidonic acid and, respectively, oppression of synthesis of products of metabolism of arachidonic acid - cyclic endoperoxides, prostaglandins. Prevents regional accumulation of neutrophils that reduces inflammatory exudate and products of lymphokines, slows down migration of macrophages, leads to reduction of processes of infiltration and granulation. Reduces an inflammation due to decrease in formation of substance of a chemotaxis (influence on late reactions of an allergy), slows down development of allergic reaction of immediate type (it is caused by braking of products of metabolites of arachidonic acid and decrease in release from mast cells of mediators of an inflammation).

In researches with provocative tests with putting antigens for a mucous membrane of a nasal cavity high antiinflammatory activity of drug, both on early, and on late stages of allergic reaction was shown.

It was confirmed with decrease (in comparison with placebo) the level of a histamine and activity of eosinophils, and also reduction (in comparison with initial level) quantities of eosinophils, neutrophils and proteins of adhesion of epithelial cells.

Pharmacokinetics. Absorption. At intranasal use system bioavailability of a mometazon of furoate makes <1% (at test-sensitivity of determination of 0.25 pg/ml).

Mometazon is very badly soaked up from a GIT.

Metabolism and removal. A small amount of active agent which can get into a GIT after intranasal use is exposed to active metabolism at "the first passing" through a liver. It is removed with urine and bile.

Indications to use:

— treatment of seasonal and year-round allergic rhinitis at adults, teenagers and children since 2 years;

— acute sinusitis or an exacerbation of chronic sinusitis at adults (including advanced age) and teenagers since 12 years - as supportive therapeutic application at treatment by antibiotics;

— acute rinosinusit with lungs and moderately expressed symptoms without symptoms of a heavy bacterial infection at patients at the age of 12 years and is more senior;

— prevention of seasonal allergic rhinitis of a medium-weight and heavy current at adults and teenagers since 12 years (it is recommended to carry out in 2-4 weeks prior to the estimated beginning of a season of dusting);

— nose polyposes, accompanied with disturbance of nasal breath and sense of smell at adults (of 18 years).

Route of administration and doses:

Drug is used intranazalno. Treatment of seasonal or year-round allergic rhinitis. Adults (including patients of advanced age) and teenagers since 12 years. The recommended preventive and therapeutic dose of drug makes 2 inhalations (on 50 mkg everyone) in each nostril of 1 times/days (a total daily dose - 200 mkg). On reaching medical effect for a maintenance therapy reduction of a dose to 1 inhalation in each nostril of 1 times/days is possible (a total daily dose - 100 mkg).

If reduction of symptoms of a disease does not manage to be reached use of drug in the recommended therapeutic dose, the daily dose can be increased to 4 inhalations in each nostril of 1 times/days (a total daily dose - 400 mkg). After reduction of symptoms of a disease the dose decline is recommended.

The beginning of effect of drug is usually noted clinically already in 12 h after the first use of drug.

Children aged from 2 up to 11 years. The recommended therapeutic dose - 1 inhalation (50 mkg) in each nostril of 1 times/days (a total daily dose - 100 mkg).

Use of drug for children of younger age requires the help of adults.

Auxiliary treatment of acute sinusitis or exacerbation of chronic sinusitis. Adults (including patients of advanced age) and teenagers since 12 years. The recommended therapeutic dose makes 2 inhalations (on 50 mkg everyone) in each nostril of 2 times/days (a total daily dose - 400 mkg).

If reduction of symptoms of a disease does not manage to be reached use of drug in the recommended therapeutic dose, the daily dose can be increased to 4 inhalations in each nostril of 2 times/days (a total daily dose - 800 mkg). After reduction of symptoms of a disease the dose decline is recommended.

Treatment of an acute rinosinusit without symptoms of a heavy bacterial infection. The recommended dose for adults and teenagers makes 2 inhalations on 50 mkg in each nasal course of 2 times/days (a total daily dose of 400 mkg). At deterioration in symptoms during treatment consultation of the specialist is necessary.

Treatment nose polypose. For adults (including patients of advanced age) of 18 years the recommended therapeutic dose makes 2 inhalations (on 50 mkg everyone) in each nostril of 2 times/days (a total daily dose - 400 mkg).

After reduction of symptoms of a disease the dose decline to 2 inhalations (on 50 mkg everyone) in each nostril of 1 times/days is recommended (a total daily dose - 200 mkg).

Rules of use of the drug Nazoneks®. Inhalation of the suspension which is contained in a spray bottle is performed by means of the special dosing nozzle on a bottle.

Before the first use of nasal Nazoneks® spray it is necessary to carry out calibration by pressing of the portioning device of 10 times until there are splashes that testifies to readiness of drug for use.

It is necessary to incline the head and to inject medicine into each nostril as the attending physician recommended.

If nasal spray was not used within 14 days or longer, it is necessary to press the dosing nozzle 2 times until splashes appear.

Before each use it is necessary to stir up a bottle vigorously.

Cleaning of the dosing nozzle. It is important to clean regularly dosing nozzle to avoid its misoperation. It is necessary to remove the cap protecting a nozzle from dust then to accurately remove a spray hand piece. It is necessary to wash out carefully a spray hand piece and a cap for protection against dust in warm water and to rinse under the crane.

It is not necessary to try to open the nasal applicator by means of a needle or other sharp object since it will lead to damage of the applicator therefore it is possible to receive the wrong dose of drug.

It is necessary to dry up a cap and a tip in the warm place. After that it is necessary to attach a spray hand piece on a bottle and again to fasten to a bottle a cap for protection against dust. At the first use of nasal spray after cleaning it is necessary to carry out repeated calibration by pressing the dosing nozzle 2 times.

Features of use:

Use at pregnancy and feeding by a breast. Special, well controlled researches of safety of use of the drug Nazoneks® at pregnancy were not conducted.

As well as it is necessary to appoint other GKS for intranasal use, Nazoneks® at pregnancy and during breastfeeding only if the expected advantage of its use justifies potential risk for a fruit or the baby.

Babies whose mothers at pregnancy received GKS need to be inspected carefully for identification of a possible hypoadrenalism.

Use at abnormal liver functions. A small amount of active agent which can get into a GIT at intranasal use is absorbed in insignificant degree and biotransformirutsya actively at "the first passing" through a liver.

Use for children. It is contraindicated at seasonal and year-round allergic rhinitises - at children's age up to 2 years, at acute sinusitis or an exacerbation of chronic sinusitis - up to 12 years, at a polypose - up to 18 years (due to the lack of the relevant data).

When carrying out placebo - controlled clinical trials at children when Nazoneks® was applied in a dose of 100 mkg/days within a year, the growth inhibition was not noted.

Special instructions. At use of nasal Nazoneks® spray for a long time (as well as at any long-term treatment) periodic survey of a mucous membrane of a nose by the ENT specialist is necessary. At development of a local fungal infection of a nose or throat treatment by drug is recommended to stop and begin performing special treatment. The irritation of a mucous membrane of a nasal cavity and a throat remaining for a long time is the basis for drug withdrawal.

At prolonged use of drug of signs of suppression of function гипоталамо - the pituitary and adrenal system was not observed.

Patients who pass to treatment with nasal Nazoneks® spray after long therapy of GKS of systemic action require to themselves special attention. Cancellation of GKS of systemic action at such patients can result in insufficiency of function of adrenal glands which subsequent recovery can take up to several months. In case of symptoms of adrenal insufficiency it is necessary to resume reception of system GKS and to take other necessary measures.

During transition from treatment of GKS of systemic action to treatment by nasal Nazoneks® spray some patients can have symptoms of cancellation of GKS for system use (for example, a joint pain and/or muscles, feeling of fatigue, a depression), despite reduction of expressiveness of the symptoms connected with damage of a mucous membrane of a nose; such patients need to be convinced specially of expediency of continuation of treatment by nasal Nazoneks® spray. Change of therapy can reveal also earlier developed allergic diseases, such as allergic conjunctivitis and eczema which masked before therapy of GKS of systemic action.

Patients to whom therapy of GKS was carried out have potentially reduced immune responsiveness and have to be warned about the increased risk of infection at contact with sick infectious diseases (including chicken pox, measles), and also about need of consultation of the doctor if such contact happened.

At emergence of symptoms of the expressed bacterial infection (for example, fevers, persistent and sharp pain on the one hand of the person or a dentagra, a swelling in orbital or periorbital area) needs immediate consultation of the doctor.

After use of the drug Nazoneks® within 12 months of symptoms of a mucosal atrophy of a nose it was not noted. At a research of bioptat of a mucous membrane of a nose it is revealed that a mometazona furoate showed a tendency to contribute to normalization of a histologic picture.

Use in pediatrics. When carrying out placebo - controlled clinical trials at children when Nazoneks® was applied in a dose of 100 mkg/days within a year, the growth inhibition was not noted.

Side effects:

At adults and teenagers: a headache, nasal bleedings (i.e. explicit bleeding, and also allocations by the painted blood of slime or clots), pharyngitis, a burning sensation in a nose, irritation of a mucous membrane of a nasal cavity, an ulceration of a mucous membrane of a nose. Nasal bleedings, as a rule, stopped independently and were not heavy; they arose with a frequency a little bigger, than when using placebo (5%), but equal or smaller, than at purpose of other studied GKS for intranasal use which were used as active control (at some of them the frequency of nasal bleedings made up to 15%). Frequency of emergence of other side effects was comparable to that at placebo use.

At children: nasal bleedings, a headache, feeling of irritation in a nose, sneezing. Frequency of emergence of the specified undesirable phenomena is comparable to the frequency of emergence of side effects at children at placebo use.

Hypersensitivity reactions of immediate type were seldom noted (for example, a bronchospasm, an asthma).

Very seldom: anaphylaxis, Quincke's disease, disturbances of taste and sense of smell.

Very seldom at intranasal use of GKS cases of perforation of a nasal partition or increase in intraocular pressure were noted.

Interaction with other medicines:

The combination therapy with loratadiny was well transferred by patients. At the same time any influence of drug on concentration of a loratadin or its main metabolite in a blood plasma was not noted. In these researches of a mometazon furoate in a blood plasma was not found (at test-sensitivity of determination of 50 pg/ml).

Contraindications:

— a recent operative measure or an injury of a nose with injury of a mucous membrane of a nasal cavity - to a wound repair (in connection with an inhibiting effect of GKS on healing processes);

— children's and teenage age (at seasonal and year-round allergic rhinitises - up to 2 years, at acute sinusitis or an exacerbation of chronic sinusitis - up to 12 years, at a polypose - up to 18 years) - due to the lack of the relevant data;

— hypersensitivity to drug components.

With care it is necessary to use drug at a tuberculosis infection (active or latent) a respiratory path, not treated fungal, bacterial, system viral infection or an infection caused by Herpes simplex with damage of eyes (purpose of drug at the listed infections according to instructions of the doctor is by way of exception possible), existence of not treated local infection with involvement in process of a mucous membrane of a nasal cavity.

Overdose:

At prolonged use of GKS in high doses or at simultaneous use of several GKS oppression гипоталамо - pituitary and adrenal system is possible.

Drug has low system bioavailability (<1%, at test-sensitivity of determination of 0.25 pg/ml) therefore it is improbable that at accidental or intended overdose acceptance of any special measures, except observation with possible subsequent resuming of administration of drug in the recommended dose will be required.

Storage conditions:

Drug should be stored in the place, unavailable to children, at a temperature from 2 °C to 25 °C; not to freeze. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

60 doses (10 g) - bottles polyethylene (1) complete with the portioning device - packs cardboard.
120 doses (18 g) - bottles polyethylene (1) complete with the portioning device - packs cardboard.
120 doses (18 g) - bottles polyethylene (2) complete with the portioning device - packs cardboard.
120 doses (18 g) - bottles polyethylene (3) complete with the portioning device - packs cardboard.