Назонекс®

General characteristics. Structure:

Active agent: a mometazona the furoate (micronized in the form of monohydrate) in an equivalent to a mometazon to furoate anhydrous - 0,5 mg.
Excipients: cellulose disperse (cellulose microcrystallic, processed karmellozy sodium), глицерол, citric acid monohydrate, sodium of a hitrat a dihydrate, polysorbate 80, a benzalkoniya chloride (in the form of 50% of solution), фенилэтанол, the water purified

Pharmacological properties:

Pharmacodynamics. Mometazon is a synthetic glucocorticosteroid (GKS) for topical administration. Has antiinflammatory and antiallergic effect at 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 o|bolochka of a nasal cavity high antiinflammatory activity of a mometazon both in early, and in a late stage 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) numbers of eosinophils, neutrophils and proteins of adhesion of epithelial cells.

Pharmacokinetics. Negligible bioavailability (≤0,1%) is inherent to Mometazon, and at appointment in the form of inhalation he practically does not decide in a blood plasma, even when using a sensitive method of definition on a threshold of sensitivity, equal 50 pg/ml. In this regard the relevant pharmacokinetic data for this dosage form do not exist; (Suspension of a mometazon is very poorly soaked up in digestive tract. That small amount of suspension of a mometazon which can get into digestive tract after nasal inhalation to excretion with urine or bile is exposed to active primary metabolism.

Indications to use:

- Seasonal and year-round allergic rhinitises at adults, teenagers and children from 2-year age.
- 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.
- Preventive treatment of seasonal allergic rhinitis of a medium-weight and heavy current at adults and teenagers since 12 years (it is recommended for two - four weeks till 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:

Intranazalno. 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 its "calibration" by pressing of the portioning device of 6-7 times. After "calibration" stereotypic supply of medicinal substance at which to each pressing of the portioning device there is an emission about 100 mg of the suspension containing a mometazon furoate (in the form of monohydrate) in the quantity equivalent to 50 mkg of a mometazon of furoate anhydrous is established. If nasal spray was not used within 14 days or longer, then before new use repeated "calibration" is necessary.
Before each use it is necessary to stir up a spray bottle vigorously.

Treatment of seasonal or year-round allergic rhinitis
Adults (including 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 once a day (a total daily dose - 200 mkg). On reaching medical effect for a maintenance therapy reduction of a dose to 1 inhalation in each nostril is possible once a day (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 once a day (a total daily dose of-400 mkg). After reduction of symptoms of a disease the dose decline is recommended. The beginning of effect of drug is usually noted clinically in 12 hours after the first use of drug.
Children of 2-11 years:
The recommended therapeutic dose - 1 inhalation (50 mkg) in each nostril once a day (a total daily dose - 100 mkg).
For use of drug for children of younger age it is required pomoshch.vzrosly.

Auxiliary treatment of acute sinusitis or exacerbation of chronic sinusitis
Adults (including advanced age) and teenagers since 12 years:
The recommended therapeutic dose makes 2 inhalations (on 50 mkg everyone) in a sazhdy nostril 2 times a day (a total daily dose - 400 mkg).
Vsluchaye, if reduction of symptoms of a disease does not manage to be reached use of drug in the recommended therapeutic dose, a daily dose can be increased to 4 inhalations in each nostril 2 times a day (a total daily dose of-800 mkg). After reduction of symptoms of a disease the dose decline is recommended.

Treatment nose polypose
Adults (including advanced age) of 18 years:
The recommended therapeutic dose makes 2 inhalations (on 50 мкгч everyone) in each nostril 2 times a day (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 is recommended once a day (a total daily dose - 200 mkg).

Features of use:

As well as at any long-term treatment, the patients using nasal NAZONEKS® spray within several months and longer have to have periodically examination at the doctor regarding possible changes of a mucous membrane of a nose.
In case of development of a local fungal infection of a nose or a throat the therapy termination by nasal NAZONEKS® spray and performing special treatment can be required. The irritation of a mucous membrane of a nose and throat remaining for a long time can also form the basis to the treatment termination by nasal NAZONEKS® spray.
When carrying out placebo - controlled clinical tests at children when the NAZONEKS nasal spray was applied in a daily dose of 100 mkg within a year, the growth inhibition at children was not noted.
At long treatment by nasal NAZONEKS® spray 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 by glucocorticosteroids of systemic action require to themselves special attention. Cancellation of glucocorticosteroids 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 signs of adrenal insufficiency it is necessary to resume reception of system glucocorticosteroids and to take others необходимыех measures. During transition from treatment by glucocorticosteroids of systemic action to treatment by nasal NAZONEKS® spray some patients can have initial symptoms of cancellation of system glucocorticosteroids (for example, a joint pain and/or muscles, feeling of fatigue and 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. Transition from system to local glucocorticosteroids can reveal, also, already existing, but masking therapy by glucocorticosteroids of systemic action, allergic diseases, such as allergic conjunctivitis and eczema.
Patients to whom treatment is carried out by glucocorticosteroids have potentially reduced immune responsiveness and have to be warned about the risk of infection increased for them in case of contact with sick some infectious diseases (for example, chicken pox, measles), and also about need of medical consultation 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 medical consultation.
At use of nasal NAZONEKS® spray within 12 months there were no symptoms of a mucosal atrophy of a nose; besides, a mometazona furoate showed a tendency to contribute to normalization of a histologic picture at a research of bioptat mucous a nose.

Use during pregnancy and a lactation
After intranasal use of drug in a therapeutic dose of 400 mkg a day мометазон is not defined in a blood plasma even in the minimum concentration, therefore, it is possible to expect that effect of drug on a fruit will be negligible, and potential toxicity concerning reproductive function - very low.
However, because special, well controlled researches of effect of drug at pregnant women were not conducted, НАЗОНЕКС® it is necessary to appoint variable or nursing only if the expected advantage of purpose of drug justifies potential risk for a fruit or the baby.
Babies whose mothers during pregnancy received GKS have to be inspected carefully concerning a possible hypoadrenalism.

Side effects:

At adults and teenagers: a headache, nasal bleedings (i.e. explicit bleeding, and also allocation by the painted blood of slime or clots), pharyngitis, a burning sensation in a nose, irritation of a mucous membrane of a nose, an ulceration of a mucous membrane of a nose. Nasal bleedings, as a rule, were moderate and stopped independently, the frequency of their emergence was a little bigger, than when using placebo (5%), but equal or smaller, than at purpose of other nasal GKS which were used as active control (at some of them the frequency of developing of nasal bleedings (left up to 15%). Frequency of emergence of all other undesirable phenomena was comparable to the frequency of their emergence at purpose of placebo.
At children: nasal bleedings, a headache, feeling of irritation in a nose, sneezing. Frequency of emergence of the specified undesirable phenomena at children was comparable with a frequency of their emergence at placebo use.
Hypersensitivity reactions of immediate type were seldom noted ([for example, a bronchospasm, an asthma).
Very seldom - an anaphylaxis, a Quincke's disease, disturbances of taste and sense of smell. Also very seldom at intranasal use of GKS cases of perforation of a nasal partition and 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 in plasma of a loratadin or its main metabolite was not noted.

Contraindications:

- Hypersensitivity to any of the substances which are a part of drug.
- Presence of not treated local infection with involvement in process of a mucous membrane of a nasal cavity.
- 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 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.

With care
НАЗОНЕКС® it is necessary to apply with care 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).

Overdose:

At prolonged use of GKS in high doses, and also at simultaneous use of several GKS function oppression гипоталамо - pituitary and adrenal system is possible. Owing to small system bioavailability of drug (<0,1%) it is improbable that at accidental or intended overdose acceptance of any measures in addition to observation with possible subsequent resuming of administration of drug in the recommended dose will be required.

Storage conditions:

Period of validity - 3 years. Not to use after a period of validity. In the place, unavailable to children; at a temperature from 2 to 25 °C. Not to freeze.

Issue conditions:

According to the recipe

Packaging:

Spray nasal dosed 50 mkg / a dose.
On 18 g (120 doses) of suspension in the polyethylene bottles of white color supplied with the portioning device and which are closed a cap. On 1 bottle together with the application instruction in a cardboard pack.