Nozefrin - instructions for use, dose, side effects, contraindications

Composition:1 dose contains:
active substance: mometasone furoate - 50 mcg;
Excipients: microcrystalline cellulose and sodium carboxymethylcellulose - 2000 μg, glycerol - 2100 μg, citric acid monohydrate - 200 μg, sodium citrate dihydrate 280 μg, polysorbate 80 - 10 μg, benzalkonium chloride (50% solution) - 40 μg, purified water - up to 0 , 1 g.

Description:White or almost white suspension. Has a gel-like structure, which when shaken turns into a liquid.

Pharmacotherapeutic group:Glucocorticosteroid for topical application.

ATX: & nbsp

R.01.A.D.09 Mometasone

Pharmacodynamics:Mometasone is a synthetic glucocorticosteroid (GCS) for topical application. Has anti-inflammatory and antiallergic effect when used in doses, in which no systemic effects occur. It inhibits the release of inflammatory mediators. Increases the production of lipomodulin, which is an inhibitor of phospholipase A, which causes a decrease in the release of arachidonic acid and, accordingly, inhibition of the synthesis of metabolic products of arachidonic acid-cyclic endoperoxides, prostaglandins.It prevents the accumulation of neutrophils, which reduces inflammatory exudate and production of lymphokines, inhibits the migration of macrophages, leads to a decrease in the processes of infiltration and granulation. Reduces inflammation by reducing the formation of the chemotaxis substance (effect on the "late" allergy reaction), inhibits the development of an allergic reaction of immediate type (due to inhibition of the production of arachidonic acid metabolites and a decrease in the release of inflammatory mediators from mast cells).
In studies with provocative tests with application of antigens to the mucosa of the nasal cavity, high anti-inflammatory activity of mometasone was demonstrated both in the early and late stages of the allergic reaction. This was confirmed by a decrease (in comparison with placebo) of the level of histamine and eosinophil activity, as well as a decrease in the number of eosinophils, neutrophils and adhesion proteins of epithelial cells (as compared to the baseline level).

Pharmacokinetics:With intranasal application, the system bioavailability of mometasone is less than 1% (with sensitivity of the 0.25 pg / ml assay method).The suspension of mometasone is very poorly absorbed in the gastrointestinal tract, and then a small amount of mometasone suspension that can enter the gastrointestinal tract after nasal inhalation, even before excretion by the kidneys or with bile, undergoes active primary metabolism.

Indications:- seasonal or all-the-year-round allergic rhinitis in adults, adolescents and children from 2 years;
- Acute sinusitis or exacerbation of chronic sinusitis in adults (including the elderly) and adolescents with 12 years of age as part of complex therapy;
- Acute rhinosinusitis with mild and moderate symptoms without signs of severe bacterial infection in patients 12 years and older;
- prophylactic treatment of seasonal allergic rhinitis of moderate and severe course in adults and adolescents from the age of 12 (recommended 2-4 weeks before the expected beginning of the dusting season);
- Polyposis of the nose, accompanied by violation of nasal breathing and smell, in adults (from 18 years).

Contraindications:- Hypersensitivity to mometasone or to any of the components that make up the drug;
- a recent surgery or injury to the nose with damage to the nasal mucosa - until the wound is healed (due to the inhibitory effect of GCS on healing processes);
- Children's age (with seasonal and allergic rhinitis all year round - up to 2 years, with acute sinusitis or exacerbation of chronic sinusitis - up to 12 years, with polyposis - up to 18 years) due to the lack of relevant data.

Carefully:- tuberculosis infection (active or latent) of the respiratory tract;
- An untreated fungal, bacterial, systemic viral infection or infection caused by Herpes simplex with eye damage (as an exception, it is possible to use the drug in case of the listed infections as directed by the doctor);
- untreated local infection involving the mucous membrane of the nasal cavity;
- long-term therapy with glucocorticosteroids of systemic action;
- Pregnancy;
- the period of breastfeeding.

Pregnancy and lactation:Studies of the effect of the drug in pregnant women and in women breast-feeding were not conducted.
As with the use of other nasal SCS, Nozefrin should be used during pregnancy and during breastfeeding only if,if the expected benefit for the mother exceeds the potential risk to the fetus or newborn. Newborns whose mothers used Nozefrin® during pregnancy should be carefully examined to identify possible hypofunction of the adrenal glands.

Dosing and Administration:Intranasally. Injection of the suspension contained in the vial is carried out by means of a special dispensing nozzle on the vial.
Tilt your head and inject the drug into each nasal passage as recommended by your doctor.
Before the first application of the nasal spray Nosefrin®, it is necessary to "calibrate" it by pressing the dispensing nozzle 6-7 times, after which the stereotype supply of the preparation is established - 0.1 g suspension (50 μg mometasone).
If the spray is not used for 14 or more days, then a "calibration" is necessary.
Before each use, vigorously shake the bottle.
Treated seasonal or year-round allergic rhinitis Adults (including the elderly) and adolescents with 12 years of age:
The recommended preventive and therapeutic dose of the drug is two injections (50 μg each) in each nasal passage once a day (daily dose of -200 μg).When the therapeutic effect for maintenance therapy is achieved, it is possible to reduce the dose to one injection in each nasal passage once a day (daily dose - 100 μg).
If the symptoms can not be reduced by applying the drug at the recommended therapeutic dose, the daily dose can be increased to four injections in each nasal passage once a day (daily dose -400 μg).
After reducing the symptoms of the disease, a dose reduction is recommended.
Children 2-11 years old:
The recommended therapeutic dose is one injection (50 μg) in each nasal passage once a day (daily dose of 100 μg).
For the use of the drug in children, it may be necessary to help adults.
The onset of the drug is usually observed clinically within 12 hours after the first use of the drug.
Auxiliary treatment of acute sinusitis or exacerbation of chronic sinusitis
The recommended therapeutic dose for adults (including the elderly) and adolescents from the age of 12 is two injections (50 μg each) in each nasal passage twice a day (daily dose is 400 μg).
If the symptoms can not be reduced by applying the drug at the recommended therapeutic dose,the daily dose can be increased to four injections in each nasal passage twice a day (daily dose of -800 μg).
After reducing the symptoms of the disease, a dose reduction is recommended.
Treatment of acute rhinosinusitis without signs of severe bacterial infection
The recommended therapeutic dose for adults and adolescents from the age of 12 is two injections (50 μg each) in each nasal passage twice a day (daily dose is 400 μg). If symptoms worsen during treatment, specialist consultation is necessary.
Treatment of polyposis of the nose
The recommended therapeutic dose for adults from 18 years (including the elderly) is two injections (50 μg each) in each nasal passage twice a day (daily dose of 400 μg).
After reducing the symptoms of the disease, it is recommended that the dose be reduced to two injections (50 μg each) in each nasal passage once a day (daily dose of -200 μg).

Side effects:In adults and adolescents: headache, nasal bleeding (ie, obvious bleeding, as well as secretion of blood-colored mucus or blood clots), pharyngitis, burning sensation in the nose, irritation of the nasal mucosa, ulceration of the nasal mucosa, upper respiratory tract infections, sensation of irritation of the pharyngeal mucosa.Nasal bleeding, as a rule, was moderate and stopped on their own, the frequency of their occurrence was slightly higher than when using placebo (5%), but equal to or less than with the appointment of other nasal SCS, which were used as active controls (some of them the incidence of nasal bleeding was up to 15%). The incidence of all other adverse events was comparable to the incidence of their occurrence with a placebo.
Children: nosebleeds, headache, irritation in the nose, sneezing. The incidence of these adverse events in children was comparable to the incidence of their occurrence with placebo.
Rarely there were reactions of hypersensitivity of immediate type (for example, bronchospasm, dyspnea).
Very rarely - anaphylaxis, angioedema, a violation of taste and smell.
Also very rarely with nasal application of GCS there were cases of perforation of the nasal septum and increased intraocular pressure.
With prolonged use of nasal SCS in high doses, it is possible to develop systemic side effects.Potential systemic effects include Cushing's syndrome, characteristic signs of cushingoid, suppression of adrenal function, growth retardation in children and adolescents, cataracts, glaucoma and, more rarely, a number of psychological or behavioral effects, including psychomotor hyperactivity, sleep disturbance, anxiety, depression or aggression (especially in children).

Overdose:Symptoms
Oppression of the hypothalamic-pituitary-adrenal system (can occur in the case of long-term use of GCS in high doses, as well as the simultaneous use of several GCS).
Treatment
Due to the low systemic bioavailability of the drug (less than 1% with the sensitivity of the 0.25 pg / ml assay method), it is unlikely that any accidental or intentional overdose will require taking any measures other than observation with possible subsequent resumption of the drug at the recommended dose. If necessary, treatment is symptomatic.

Interaction:With the simultaneous use of mometasone with loratadine, patients were well tolerated. There was no evidence of any effect of mometasone on the concentration of loratadine or its basicmetabolite in the blood plasma.
Studies of interactions with other drugs have not been conducted.

Special instructions:Do not use in ophthalmology.
When using the drug for a long time (for several months and longer), periodic examination with a doctor is necessary to detect possible changes in the mucous membrane of the nasal cavity in time.
In case of development of a local fungal infection of the nose or throat, it may be necessary to stop the therapy with the drug and conduct special treatment. The long-term irritation of the mucous membrane of the nasal cavity and pharynx is also an indication for the abolition of therapy with the drug.
Patients who switch to nasal spray nasal spray® after long-term therapy with SCS of systemic action require special attention. The abolition of SCS systemic action in such patients may lead to adrenal insufficiency, the restoration of which may take several months. If signs of adrenal insufficiency appear, the systemic GCS should be resumed and other necessary measures taken.
During the transition from the treatment of SCS systemic action to the treatment with nasal spray Nosefrin®, symptoms of cancellation of systemic SCS (for example, joint and / or muscle pain, fatigue and depression) may occur in some patients. Such patients need to be persuaded of the advisability of continuing the treatment with nasal spray Nosefrin®. Transition from systemic to local SCS can also reveal previously developed allergic diseases, such as allergic conjunctivitis and eczema, which were previously masked by GCS therapy of systemic action.
Patients who use SCS have potentially decreased immune reactivity and should be warned of the increased risk of infection if they become infected with certain infectious diseases (for example, chicken pox, measles) and the need for consultation with a doctor if such contact occurs.
It is necessary to regularly monitor the condition of patients receiving the drug for a long time. With prolonged use of nasal SCS in high doses, it is possible to develop systemic side effects. The probability of developing these effects is much less than when using systemic GCS, and may differ in individual patients, as well as between different GCS.Potential systemic effects include Cushing's syndrome, characteristic signs of cushingoid, suppression of adrenal function, growth retardation in children and adolescents, cataracts, glaucoma and, more rarely, a number of psychological or behavioral effects, including psychomotor hyperactivity, sleep disturbance, anxiety, depression or aggression (especially in children).
It is recommended to regularly monitor the growth of children receiving long-term therapy with mometasone. If the growth slows down, the current therapy should be reviewed in order to reduce the dose of mometasone to the minimum effective dose, which allows controlling the symptoms of the disease. In addition, you should refer the patient to a consultation with the pediatrician.
Treatment with SCS with higher doses than recommended, can lead to clinically significant suppression of adrenal function.
If there are signs of severe bacterial infection (eg, fever, persistent and sharp pain on one side of the face or toothache, swelling in the orbital or periorbital area) immediate medical consultation is necessary. With the application of mometasone in a dosage form, nasal spray for 12 months did not cause signs of atrophy of the mucous membrane of the nasal cavity.The efficacy and safety of mometasone has not been studied in the treatment of unilateral polyps, polyps associated with muscovicosis, and polyps that completely cover the nasal cavity. Unilateral polyps of irregular shape or bleeding polyps should be further inspected.

Effect on the ability to drive transp. cf. and fur:Data on the negative effect of the drug at recommended doses on the ability to control vehicles and mechanisms, as well as other activities that require concentration and speed of psychomotor reactions, are not available.

Form release / dosage:Spray nasal dosed with 50 mcg / dose.

Packaging:18 g (120 doses) in a vial of plastic (high-density polyethylene) with a dispenser for nasal use complete with a cap.
One bottle together with the instruction but application in a pack of cardboard.

Storage conditions:Store at a temperature not exceeding 25 ° C.
Keep out of the reach of children.
Do not freeze!

Shelf life:3 years.
Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003402

Date of registration:31.12.2015

Expiration Date:31.12.2020

The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia

Manufacturer: & nbsp

VERTEKS, AO Russia

Information update date: & nbsp2016-10-18

Illustrated instructions

Instructions

Nosephrine® (Nozefrin)