Mometazon Sandoz, 50 mcg/dose 18 g spray

GCS of intranasal application.

It has anti-inflammatory and anti-allergic effect.

The mechanism of anti-allergic and anti-inflammatory action is due to the ability to inhibit the release of inflammatory mediators. It increases production of lipomodulin, which is an inhibitor of phospholipase A, thus reducing the release of arachidonic acid, and, accordingly, inhibiting the synthesis of products of arachidonic acid metabolism – cyclic endoperoxides, prostaglandins.

It prevents marginal accumulation of neutrophils that reduces inflammatory exudate and lymphokine production, inhibits macrophage migration, results in a decrease of infiltration and granulation processes.

In vitro reduces inflammation due to a decrease in chemotaxis substance formation (effect on late allergic reactions), inhibits the development of immediate allergic reactions (caused by inhibition of arachidonic acid metabolites production and decrease in inflammatory mediators release from mast cells).

In vitro mometasone furoate significantly inhibits the release of leukotrienes from leukocytes. In cell cultures, mometasone furoate has demonstrated a high ability to inhibit the synthesis and release of IL-1,IL-5, IL-6, and TNFα; it is also an inhibitor of leukotriene production and is an extremely potent inhibitor of Th2 cytokines, IL-4 and IL-5, by human CD4+ T-cells.

In studies in preclinical models, mometasone reduced inflammatory cell accumulation (including eosinophils), infiltrated the walls of the upper and lower airways, and improved lung function after a provocation test. Mometazone decreased lymphocyte counts and mRNA concentrations of cytokines IL-4 and IL-5.

In studies with nasal mucosa antigen provocation tests, high anti-inflammatory activity of Mometazone was demonstrated in both the early and late stages of an allergic reaction.

This was confirmed by a decrease (compared with placebo) in histamine levels and eosinophil activity, as well as a decrease (compared with baseline) in eosinophils, neutrophils and epithelial cell adhesion proteins.

Pharmacokinetics.

After intranasal administration, the systemic bioavailability of mometasone is low, particularly because of low absorption and significant presystemic metabolism upon swallowing mometasone.

When used at the recommended doses, the plasma concentration of mometasone is near or below the threshold of determination (50 pg/mL). As a consequence, neither the T1/2 nor the Vd of mometasone after inhalation can be determined. It is excreted in the urine and bile.

Indications

For intranasal application:

Active ingredient

Mometazone

How to take, the dosage

Dosing regimen is set individually, depending on the indications, the age of the patient, the drug form used.
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Special Instructions

Caution should be exercised in case of tuberculosis infection (active or latent) of the respiratory tract, untreated fungal, bacterial, systemic viral infection or infection caused by Herpes simplex with eye involvement (as an exception, the drug may be prescribed for the above infections as directed by a doctor), presence of untreated local infection with involvement of the nasal mucosa.