Nasonex, spray 50 mcg/dose 60 doses

Nasonex is an anti-allergic, anti-inflammatory.

Pharmacodynamics

Mometasone furoate is a synthetic glucocorticosteroid for topical use. It has anti-inflammatory and anti-allergic effects when used in doses at which there are no systemic effects. It inhibits release of inflammatory mediators, increases production of lipomodulin, which is an inhibitor of phospholipase A, which causes reduction of release of arachidonic acid and, accordingly, inhibition of synthesis of products of arachidonic acid metabolism – cyclic endoperoxides, PG. Prevents marginal accumulation of neutrophils, reduces inflammatory exudate and lymphokine production, inhibits macrophage migration, leads to a decrease in infiltration and granulation processes. It reduces inflammation due to decrease in formation of chemotaxis substance (effect on “late” allergic reactions) and inhibits development of “immediate” allergic reaction (conditioned by inhibition of production of arachidonic acid metabolites and decrease in release of inflammatory mediators from mast cells).

. In studies with provocation tests with application of antigens to the nasal mucosa high anti-inflammatory activity of Nasonex was demonstrated both in the early and late stages of the allergic reaction, which was confirmed by reduction (compared to placebo) of histamine and eosinophil activity as well as reduction (compared to baseline) of eosinophil, neutrophil and epithelial cell adhesion proteins.

Pharmacokinetics

The bioavailability of mometasone furoate is negligible (≤0.1%) and it is almost not detected in plasma when given by intranasal inhalation (even when using the sensitive 50 pg/ml sensitivity threshold method). 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 may enter the gastrointestinal tract after inhalation into the nasal cavity is still undergoing active primary metabolism before excretion with urine or bile.

Indications

Active ingredient

Composition

Active substance:

mometasone furoate (as monohydrate) 50 mcg;

Ancillary substances:

PB 65 cps dispersed cellulose;

Glycerol;

Sodium citrate dihydrate;

Citric acid monohydrate;

Polysorbate 80;

Benzalkonium chloride;

Phenylethyl alcohol;

Purified water.

How to take, the dosage

Intranasally. Nasonex® is used in the form of intranasal inhalation of the suspension contained in the spray bottle. Inhalations are performed using a special dispensing nozzle on the bottle.

Before using Nasonex® nasal spray for the first time, it is necessary to “calibrate” it by pressing the dosing device 6-7 times. After “calibration”, a stereotypic delivery of the medication is established in which approximately 100 mg of mometasone furoate suspension containing mometasone furoate monohydrate in an amount equivalent to 50 µg of chemically pure mometasone furoate is released with each press of the button. If the nasal spray has not been used for 14 days or longer, a re-calibration is necessary before new use.

Shake the spray bottle vigorously before each use.

Treatment of seasonal or year-round allergic rhinitis

In adults (including seniors) and adolescents from 12 years of age, the normally recommended prophylactic and therapeutic dose of the drug is 2 inhalations (50 mcg each) into each nostril, once (total daily dose of 200 mcg). After achieving the desired therapeutic effect for maintenance therapy it is reasonable to reduce the dose to 1 inhalation per nostril once a day (total daily dose 100 mcg).

If reduction of symptoms of the disease could not be achieved by using the drug in the recommended therapeutic dose, the daily dose may be increased to 4 inhalations in each nostril once a day (total daily dose of 400 mcg). After reduction of symptoms of the disease, reduction of the dose is recommended.

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

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

Auxiliary treatment of exacerbations of sinusitis

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

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

After 12 months of treatment with Nasonex® nasal spray, there was no evidence of nasal mucosal atrophy; in addition, mometasone furoate tended to promote normalization of the histologic picture on nasal mucosal biopsy specimens.

Interaction

Contraindications

Side effects

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

In adults:

Overdose

Symptoms: inhibition of hypothalamic-pituitary-adrenal system function is possible with prolonged use of GCS in high doses, as well as with simultaneous use of several GCS.

Treatment: Due to low (less than 0.1%) systemic bioavailability, it is unlikely that any measures other than observation of the patient followed by continuation of therapy at the recommended dose will be necessary if there is an accidental or intentional overdose.

Pregnancy use

After intranasal administration of the drug at the maximum therapeutic dose, mometazone is not detectable in plasma even at minimal concentrations; therefore, its effect on the fetus can be expected to be negligible and its potential toxicity to reproduction is very low.

However, because no specific, well-controlled studies of the drug in pregnant women have been performed, Nasonex should be administered to pregnant, breastfeeding, or childbearing women only if the expected benefits of its administration justify the potential risk to the fetus and the newborn.

Newborns whose mothers have used GCS during pregnancy should be carefully evaluated for possible adrenal hypofunction.

Similarities