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

For intranasal application:

• treatment of seasonal and year-round allergic rhinitis in adults, adolescents and children from 2 years of age;
• acute sinusitis or exacerbation of chronic sinusitis in adults (including adults (including elderly) and adolescents from 12 years of age (as adjunctive therapy to antibiotic treatment);
• acute rhinosinusitis with mild to moderately expressed symptoms without signs of severe bacterial infection in patients aged 12 years and older;
• prevention of seasonal allergic rhinitis of moderate to severe course in adults and adolescents from 12 years of age;
• nasal polyposis accompanied by impaired nasal breathing and sense of smell in adults.

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Active ingredient

Mometazone

Composition

1 dose:

mometasone furoate monohydrate 0.0517 mg,

which corresponds to the content of mometasone furoate 0.05 m.

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

Dosing regimen is established individually, depending on the indications, the age of the patient, the dosage form used.

Special Instructions

Mometasone should be used with caution 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.

During prolonged intranasal use of mometasone it is necessary to periodically check the nasal mucosa by ENT physician. If local bacterial or fungal infection of the nose or pharynx develops, it is recommended to stop treatment and start special treatment.

Long lasting irritation of nasal and pharyngeal mucosa is an indication for discontinuation of the drug.

Special caution is required when switching from GCS for systemic use to intranasal use of mometasone due to the possible risk of adrenal insufficiency. After discontinuation of systemic GCS, several months are required to restore hypothalamic-pituitary-adrenal function.

During stressful situations, including trauma, surgery, infectious disease, or severe asthma attacks, patients who previously received systemic GCS require an additional short course of systemic GCS, which is then gradually discontinued as symptoms subside.

If we switch from systemic GCS to intranasal use mometasone may manifest concomitant allergic diseases whose symptoms were previously suppressed by systemic corticosteroids.

During this period, some patients may show signs of withdrawal of systemic GCS, including muscle and/or joint pain, depression, and fatigue, even though pulmonary function is stable or even improving.

If signs of adrenal insufficiency occur, the dose of systemic GCS should be temporarily increased and thereafter withdrawn more gently.

Patients receiving GCS or other immunosuppressants should be advised to avoid contact with patients with certain infections (chicken pox, measles) and be sure to consult a physician if such contact occurs (especially important when used in adolescents over 12 years).

To maintain a low potential for hypothalamic-pituitary-adrenal suppression, the recommended doses should not be exceeded, and in each patient the dose of mometasone should be titrated, achieving a minimum effective.

When using mometasone, note that the effect on cortisol production may vary from patient to patient.

The occurrence of candidiasis may require appropriate antifungal therapy or discontinuation of mometasone.

Use in Pediatrics

Regular growth monitoring of adolescents receiving long-term mometasone therapy is recommended. If growth slows down, therapy should be reconsidered to reduce the dose of mometasone to the lowest effective dose to control symptoms.

In placebo-controlled clinical studies in children, no growth retardation was observed when mometasone was administered intranasally at a dose of 100 mcg/day for one year.

Contraindications

• High sensitivity to mometasone;
• Nasal surgery or recent trauma with nasal mucosa damage – until wound healing (due to the inhibitory effect of GCS on healing processes);
  
• children and adolescents under 18 years of age with nasal polyposis;
• children under 12 years of age with acute sinusitis or exacerbation of chronic sinusitis;
• children under 2 years of age with seasonal and year-round allergic rhinitis.

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Side effects

Respiratory system: with intranasal use nasal bleeding, pharyngitis, burning sensation in the nose, sneezing; irritation of the nasal mucosa; very rare with intranasal use – cases of nasal septum perforation.

Other: headache.

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

Desrinit spray, Momat Rhino, Nosefrin, Rialtris, Momeyd