Mometazon Sandoz, spray 50 mcg/dose 10 g

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 of 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 reduced 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 the low absorption and significant presystemic metabolism upon ingestion of 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

Active ingredient

Composition

Auxiliary Substances:

Microcrystalline cellulose and sodium carmellose (Avicel RC-591) – 2 mg,

Glycerin – 2.1 mg,

citric acid monohydrate – 0.2 mg,

sodium citrate dihydrate – 0.28 mg,

polysorbate 80 – 0.01 mg,

benzalkonium chloride – 0.02 mg,

d/i water – up to 100 mg.

How to take, the dosage

Special Instructions

Contraindications

Side effects

Pregnancy use

There are no adequate and well-controlled studies of the use of mometasone in pregnancy. It is not known whether mometasone is excreted with breast milk.

Intranasal use of mometasone in pregnancy and during breastfeeding is possible only if the expected benefit to the mother exceeds the potential risk to the fetus or the infant.

Newborns whose mothers received GCS during pregnancy should be monitored for possible symptoms of adrenal cortical insufficiency.

Similarities