Nasonex, nasal spray 50 µg/dose 60 doses

Composition

Active ingredient:

mometasone furoate (as a monohydrate) 50 mcg;

Auxiliary substances:

dispersed cellulose BP 65 cps;

glycerol;

sodium citrate dihydrate;

citric acid monohydrate;

polysorbate 80;

benzalkonium chloride;

phenylethyl alcohol;

purified water.

Pharmacological action

Nasonex is an anti-allergic, anti-inflammatory drug.

Pharmacodynamics

Mometasone furoate is a synthetic glucocorticosteroid for topical use. It has an anti-inflammatory and anti-allergic effect when used in doses that do not cause systemic effects. Inhibits the release of inflammatory mediators, increases the production of lipomodulin, which is an inhibitor of phospholipase A, which leads to a decrease in the release of arachidonic acid and, accordingly, inhibits the synthesis of arachidonic acid metabolism products-cyclic endoperoxides, PG. It prevents the marginal accumulation of neutrophils, reduces inflammatory exudate and lymphokine production, inhibits macrophage migration, and reduces the processes of infiltration and granulation. Reduces inflammation by reducing the formation of the chemotaxis substance (the effect on “late” allergic reactions), inhibits the development of an” immediate ” allergic reaction (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, when applying antigens to the nasal mucosa, high anti-inflammatory activity of Nasonex was demonstrated in both the early and late stages of an allergic reaction, which was confirmed by a decrease (compared to placebo) in the level of histamine and eosinophil activity, as well as a decrease (compared to the initial level) in the number of eosinophils, neutrophils and epithelial cell adhesion proteins.

Pharmacokinetics

Mometasone furoate is characterized by negligible bioavailability (≤0.1%) and when administered as an intranasal inhalation, it is practically not detected in blood plasma (even when using a sensitive determination method with a sensitivity threshold of 50 pg / ml). Therefore, there are no relevant pharmacokinetic data for this dosage form. The suspension is very poorly absorbed from the gastrointestinal tract, so the small amount that can enter the gastrointestinal tract after inhalation into the nasal cavity, even before excretion in the urine or bile, undergoes active primary metabolism.

Indications

• treatment of allergic rhinitis (seasonal and perennial) in adults, adolescents and children 2 years of age;
• exacerbation of sinusitis (combined therapy with antibiotics) in adults (including elderly) and children 12 years of age;
• prevention of seasonal allergic rhinitis moderate and severe (recommended for 2-4 weeks before the anticipated start of the season dusting).

Use during pregnancy and lactation

After intranasal use of the drug at the maximum therapeutic dose, mometasone is not detected in blood plasma even at the minimum concentration; therefore, it can be expected that its effect on the fetus will be negligible, and the potential toxicity to reproductive function is very low.

However, due to the fact that special, well-controlled studies of the drug’s effect in pregnant women have not been conducted, Nasonex should be prescribed to pregnant women, mothers, breast-feeding or women of childbearing age only if the expected benefit of its use justifies the potential risk to the fetus and newborn.

Newborns whose mothers have used corticosteroids during pregnancy should be carefully examined for possible adrenal hypofunction.

Contraindications

• hypersensitivity to any component of the drug;
• the presence of an untreated local infection involving the nasal mucosa;
• recent surgery or trauma to the nose (before the wound heals);
• tuberculosis infection (active or latent) of the respiratory tract, untreated fungal, bacterial, viral systemic infection or infection caused by Herpes simplex with eye damage (as an exception, the appointment of the drug in these cases is possible on the instructions of a doctor with great caution);
• children under 2 years of age (there are no data on the safety of use).

Side effects

In the treatment of seasonal or year-round allergic rhinitis.

For adults:

• nosebleeds (obvious or discharge of blood-stained mucus or blood clots)
• pharyngitis,
• burning sensation in the nose,
• irritation of the nasal mucosa.

Nosebleeds generally stopped on their own and were not severe; they occurred with a frequency slightly higher than when using placebo (5%), but equal to or less than when using other corticosteroids for intranasal use, which were used as active controls (in some of them, the incidence of nosebleeds was up to 15%). The incidence of all other adverse events was comparable to that of placebo.

For children:

• nosebleeds,
• headache,
• irritated nose,
• sneezing.

The incidence of these adverse events in children was comparable to that of placebo.

In the treatment of exacerbations of sinusitis (when using Nasonex spray as an auxiliary agent).

For adults and adolescents:

• headache,
• pharyngitis,
• burning sensation in the nose,
• irritation of the nasal mucosa.

Nosebleeds were moderate, and the incidence of nosebleeds with Nasonex was also comparable to the incidence of nosebleeds with placebo (5% compared to 4%, respectively).

Very rarely, cases of perforation of the nasal septum or increased intraocular pressure have been reported with intranasal use of corticosteroids.

Interaction

Concomitant therapy with loratadine was well tolerated in patients. Interaction studies with other drugs have not been conducted.

How to take, course of use and dosage

Intranasally. Nasonex® is used as an intranasal inhalation of a suspension contained in a spray bottle. Inhalations are carried out using a special dosing nozzle on the bottle.

Before applying the Nasonex® nasal spray for the first time, it is necessary to “calibrate” it by pressing the dosing device 6-7 times. After” calibration”, a stereotypical drug supply is established, in which approximately 100 mg of mometasone furoate suspension containing mometasone furoate monohydrate in an amount equivalent to 50 mcg of chemically pure mometasone furoate is released with each push of a button. If the nasal spray has not been used for 14 days or longer, a second “calibration” is required before applying it again.

Shake the spray bottle vigorously before each use.

Treatment of seasonal or year-round allergic rhinitis

Adults (including senile age) and adolescents from 12 years of age usually recommended preventive and therapeutic dose of the drug is 2 inhalations (50 mcg each) in each nostril, once (a total daily dose of 200 mcg). After achieving the desired therapeutic effect for maintenance therapy, it is advisable to reduce the dose to 1 inhalation in each nostril 1 time a day (total daily dose of 100 mcg).

If the reduction of symptoms of the disease could not be achieved by using the drug at the recommended therapeutic dose, the daily dose can be increased to 4 inhalations in each nostril 1 time a day (a total daily dose of 400 mcg). After reducing the symptoms of the disease, it is recommended to reduce the dose.

The onset of action of the drug is usually noted clinically within the first 12 hours after the first use of the drug.

Children 2-11 years of age: the recommended therapeutic dose is 1 inhalation (50 mcg) in each nostril once a day (the total daily dose is 100 mcg).

Auxiliary treatment of sinusitis exacerbations

Adults (including senile age) and adolescents from 12 years of age: the recommended therapeutic dose is 2 inhalations (50 mcg) in each nostril 2 times a day (a total daily dose of 400 mcg).

If the reduction of symptoms of the disease could not be achieved by using the drug at the recommended therapeutic dose, the daily dose can be increased to 4 inhalations in each nostril 2 times a day (the total daily dose is 800 mcg). After reducing the symptoms of the disease, it is recommended to reduce the dose.

After 12 months of treatment with Nasonex ® nasal spray, there were no signs of atrophy of the nasal mucosa; in addition, mometasone furoate showed a tendency to normalize the histological picture in the study of nasal mucosal biopsies.

Overdose

Symptoms:  with prolonged use of corticosteroids in high doses, as well as with the simultaneous use of several corticosteroids, it is possible to inhibit the function of the hypothalamic-pituitary-adrenal system.

Treatment:  due to the low (less than 0.1%) systemic bioavailability, it is unlikely that accidental or intentional overdose will require any measures other than monitoring the patient and then continuing treatment at the recommended dose.

Form of production

Nasonex nasal spray.

Storage conditions

At a temperature of 2-25 °C. (do not freeze)

Shelf life

3 years

Active ingredient

Mometasone

Conditions of release from pharmacies

By prescription

Dosage form

nasal spray

Purpose

For adults as prescribed by a doctor, Children as prescribed by a doctor, Children over 2 years of age

Indications

Nasal Polyposis, Pollinosis, Sinusitis, Allergic Rhinitis, Allergy