MOMIXON

I N S T R U C T I O N for medical use of the medicinal product MОMІXON (MOMIXON)

Composition:

Active substance: mometasone furoate monohydrate;

1 spray dose contains mometasone furoate monohydrate 0.05173 g, equivalent to mometasone furoate 50 μg;

Excipients: benzalkonium chloride solution; glycerin; polysorbate 80; microcrystalline cellulose; sodium croscarmellose; citric acid monohydrate; sodium citrate; purified water.

Pharmaceutical form. Nasal spray, suspension.

Main physicochemical properties: white or almost white, viscous suspension.

Pharmacotherapeutic group. Anti-inflammatory and other drugs for local use in diseases of the nasal cavity. Corticosteroids.

ATC code R01AD09.

Pharmacological Properties

Pharmacodynamics

Mechanism of Action

Mometasone furoate is a glucocorticoid for topical use that exerts a pronounced anti-inflammatory effect. The local anti-inflammatory activity of mometasone furoate is observed at doses that do not produce systemic effects.

The primary mechanism of the anti-inflammatory and anti-allergic action of mometasone furoate is related to its ability to suppress the release of mediators of allergic reactions. Mometasone furoate significantly reduces the synthesis and release of leukotrienes from leukocytes of patients suffering from allergic diseases. In cell cultures, mometasone furoate demonstrated high efficacy in inhibiting the synthesis and release of IL-1, IL-5, IL-6, and TNF-alpha. It is also a potent inhibitor of leukotriene production and a strong inhibitor of Th2 cytokine production, including IL-4 and IL-5, by human CD4+ T cells.

In studies using nasal allergen challenge tests, mometasone furoate demonstrated anti-inflammatory effects during both the early and late phases of the allergic reaction. This was evidenced by reduced activity (compared to placebo) of histamine and eosinophils, as well as a decrease (compared to baseline) in the number of eosinophils, neutrophils, and epithelial cell adhesion proteins.

Pronounced clinical effect within the first 12 hours of mometasone furoate administration was achieved in 28% of patients with seasonal allergic rhinitis. On average, symptom relief occurred within 35.9 hours (in 50% of patients).

Pharmacokinetics

After intranasal administration as an aqueous spray, mometasone furoate has a systemic bioavailability in blood plasma of less than 1%, as determined by a sensitive assay method with a lower limit of quantification of 0.25 mcg/mL.

Mometasone furoate suspension is very poorly absorbed from the gastrointestinal tract. Any small amount that may be swallowed and absorbed undergoes extensive first-pass metabolism, with excretion occurring predominantly in the form of metabolites via bile and to a lesser extent via urine.

Children

It is known that in children treated with mometasone furoate at a daily dose of 100 mcg for one year, no growth suppression was observed.

Clinical characteristics.

Indications.

• Treatment of seasonal or perennial allergic rhinitis in adults and children aged 2 years and older. Prophylactic treatment of moderate to severe allergic rhinitis should be initiated 4 weeks before the anticipated start of the pollen season.
• As an adjunctive therapeutic agent in antibiotic treatment of acute episodes of sinusitis in adults (including elderly) and children aged 12 years and older.
• Treatment of symptoms of acute rhinosinusitis without signs of severe bacterial infection in adults and children aged 12 years and older.

Treatment of nasal polyps and associated symptoms, including nasal congestion and loss of smell, in patients aged 18 years and older.

Contraindications.

Hypersensitivity to the active substance or to any of the excipients of the medicinal product.

The medicinal product should not be used in the presence of untreated localized infection involving the nasal mucosa (e.g., herpes simplex).

Since corticosteroids may impair wound healing, patients who have recently undergone nasal surgery or have nasal trauma should not use nasal corticosteroids until healing has occurred.

Interaction with other medicinal products and other forms of interaction.

Mometasone furoate was administered concomitantly with loratadine, and no effect on plasma concentrations of loratadine or its major metabolite was observed; mometasone furoate was not detectable in plasma even at minimal concentrations. Combination therapy was well tolerated by patients.

Data on interactions with other medicinal products are not available.

Concomitant use with CYP3A inhibitors, including medicinal products containing cobicistat, is expected to increase the risk of systemic adverse effects. Such combinations should be avoided unless the benefit outweighs the increased risk of systemic corticosteroid side effects; in such cases, patients should be monitored for possible systemic corticosteroid adverse effects.

Special precautions for use.

The drug should not be used in the presence of untreated local infection involving the nasal mucosa.

Since corticosteroids may impair wound healing, patients who have recently undergone nasal surgery or have experienced nasal trauma should not use nasal corticosteroids until healing has occurred.

MOMIXON, nasal spray, should be used with caution in patients with active tuberculosis or inactive tuberculosis infections of the respiratory tract, or in patients with untreated fungal, bacterial, systemic viral infections, or herpes simplex infection involving the eyes.

Patients receiving corticosteroids, in whom immunosuppressive effects may occur, should be warned about the risks associated with exposure to certain infectious diseases (e.g., varicella, measles), and advised to seek medical advice if such exposure occurs.

The safety and efficacy of MOMIXON in the treatment of nasal polyps in children and adolescents under 18 years of age have not been established.

After 12 months of treatment with mometasone furoate in a study involving patients with perennial rhinitis, no symptoms of atrophy of the nasal mucosa were observed; furthermore, mometasone furoate demonstrated the ability to restore near-normal histological structure of the nasal mucosa. However, patients treated with the drug for several months or longer should be periodically examined to detect any possible changes in the nasal mucosa. If a local fungal infection of the nose or throat develops, discontinuation of therapy or appropriate antifungal treatment may be required. Persistent irritation of the nasal or pharyngeal mucosa may also be an indication for discontinuation of treatment.

MOMIXON, nasal spray, is not recommended for use in patients with nasal septum perforation.

Systemic effects of corticosteroids.

Systemic effects of nasal corticosteroids may occur, particularly with high doses used over prolonged periods. Such effects are considerably less likely than with oral corticosteroids and may vary between different patients and different corticosteroid-containing products. Potential systemic effects may include Cushing's syndrome, Cushingoid facial features, adrenal cortex suppression, growth retardation in children and adolescents, cataracts, glaucoma, and, less frequently, various psychiatric symptoms or behavioral changes such as excessive psychomotor hyperactivity, sleep disturbances, fear, depression, or aggression (particularly in children).

Cases of increased intraocular pressure have been reported with the use of nasal corticosteroids.

No signs of suppression of the hypothalamic-pituitary-adrenal (HPA) axis have been observed during long-term treatment with MOMIXON. Patients who are switching from systemic corticosteroid therapy to treatment with nasal spray should be closely monitored. Discontinuation of systemic corticosteroids in such patients may lead to adrenal insufficiency, which may require reinstatement of systemic corticosteroid therapy and other appropriate treatment.

When switching from systemic corticosteroid therapy to treatment with MOMIXON nasal spray, some patients may experience corticosteroid withdrawal symptoms (e.g., joint and/or muscle pain, fatigue, depression), despite improvement in nasal symptoms. Such patients should be specifically reassured about the importance of continuing spray therapy. The change in therapy may also unmask previously suppressed allergic conditions (e.g., allergic conjunctivitis, eczema).

The potential risk of Cushing's syndrome may arise with prolonged use of the drug at high doses.

Nasal polyps.

The safety and efficacy of mometasone furoate in the treatment of unilateral nasal polyps, polyps associated with cystic fibrosis, or polyps completely obstructing the nasal cavity have not been studied.

Unilateral polyps with unusual or irregular appearance, especially those ulcerated or bleeding, should be thoroughly investigated.

Effects on growth in children and adolescents.

Regular monitoring of growth is recommended in children undergoing long-term treatment with nasal corticosteroids. If growth retardation occurs, the dose of nasal corticosteroid should be reduced to the lowest effective dose controlling symptoms, if possible. Referral to a specialist pediatrician should also be considered.

Although MOMIXON nasal spray allows control of nasal mucosal inflammation symptoms in most patients, additional concurrent therapy may help relieve other symptoms, particularly ocular ones.

Patients should be advised to seek immediate medical attention if signs or symptoms of severe bacterial infection occur, such as fever, severe unilateral facial pain or toothache, orbital or periorbital swelling/edema, or worsening condition after initial improvement.

Visual disturbances may occur with systemic and topical corticosteroids (including intranasal, inhaled, and intraocular administration). If symptoms such as blurred vision or other visual disturbances occur, patients should undergo ophthalmological examination to evaluate possible causes, including cataract, glaucoma, or rare conditions such as central serous chorioretinopathy, which has been reported after use of systemic and topical corticosteroids.

The safety and efficacy of MOMIXON in the treatment of rhinosinusitis symptoms in children under 12 years of age have not been studied.

Use during pregnancy or breastfeeding.

Specific studies on the effects of the drug in pregnant women have not been conducted.

As with other intranasal corticosteroids, MOMIXON may be used during pregnancy or breastfeeding only if the expected benefit justifies the potential risk to the mother, fetus, or infant. Infants born to mothers who received corticosteroids during pregnancy should be carefully monitored for possible adrenal insufficiency.

Ability to affect reaction speed when driving or operating machinery.

Unknown.

Method of Administration and Dosage

Before starting to use a new bottle of the medication, it should be primed. Priming is performed by approximately 10 actuations of the dosing device, establishing a consistent delivery of the drug so that each actuation releases approximately 100 mg of suspension containing 50 mcg of mometasone (one dose). If the nasal spray has not been used for 14 days or longer, re-priming is required before the next use by two actuations until a full spray is observed.

The bottle should be shaken vigorously before each use.

A used bottle, as well as a bottle opened two months prior, should be discarded.

Treatment of seasonal or perennial allergic rhinitis: The recommended prophylactic and therapeutic dose for adults (including elderly patients) and children aged 12 years and older is 2 sprays (50 mcg each) in each nostril once daily (total daily dose – 200 mcg). After achieving the therapeutic effect, the dose should be reduced to 1 spray in each nostril once daily (total daily dose – 100 mcg) for maintenance therapy.

If symptoms are not adequately controlled with the recommended therapeutic dose, the daily dose may be increased to the maximum of 4 sprays in each nostril once daily (total daily dose – 400 mcg). After symptom relief, dose reduction is recommended.

For children aged 2–11 years, the recommended therapeutic dose is 1 spray (50 mcg) in each nostril once daily (total daily dose – 100 mcg).

The medication has demonstrated a clinically significant onset of action within 12 hours after the first dose in some patients with seasonal allergic rhinitis. However, full benefit from treatment may not be achieved within the first 48 hours; therefore, patients should continue regular use to achieve the full therapeutic effect.

Adjunctive treatment of acute sinusitis episodes: For adults (including elderly patients) and children aged 12 years and older, the recommended therapeutic dose is 2 sprays (50 mcg each) in each nostril twice daily (total daily dose – 400 mcg).

If symptoms are not adequately controlled with the recommended therapeutic dose, the daily dose may be increased to 4 sprays in each nostril twice daily (total daily dose – 800 mcg). After symptom relief, dose reduction is recommended.

Acute rhinosinusitis: For adults and children aged 12 years and older, the recommended therapeutic dose is 2 sprays (50 mcg each) in each nostril twice daily (total daily dose – 400 mcg).

Nasal polyps: For patients aged 18 years and older (including elderly patients), the recommended dose is 2 sprays (50 mcg each) in each nostril twice daily (total daily dose – 400 mcg). After achieving clinical response, the dose should be reduced to 2 sprays in each nostril once daily (total daily dose – 200 mcg).

Children.

In placebo-controlled clinical studies in children who received Mommixon at a daily dose of 100 mcg for one year, no growth suppression was observed.

The safety and efficacy of Mommixon in the treatment of nasal polyps in children and adolescents under 18 years of age, symptoms of rhinosinusitis in children under 12 years of age, and seasonal or perennial allergic rhinitis in children under 2 years of age have not been studied.

Overdose.

Due to the systemic bioavailability of the drug being < 1% (according to results from a sensitive quantitative assay, plasma levels are approximately 0.25 pg/mL), it is unlikely that any measures other than patient observation and subsequent administration of the drug at the recommended dose will be required in case of overdose.

Inhalation or oral ingestion of excessive doses of corticosteroids may lead to suppression of the hypothalamic-pituitary-adrenal (HPA) axis function.

Adverse reactions.

Treatment-related adverse reactions observed in clinical studies with Momyxone in patients with allergic rhinitis are listed in Table 1.

Table 1

Nasal bleeding stopped spontaneously and was mild, occurred somewhat more frequently than with placebo (5%), but less frequently than with other intranasal corticosteroids studied and used as active control (in some of these, the incidence of nasal bleeding was up to 15%). The incidence of other adverse events was comparable to that observed with placebo.

In children, the incidence of adverse events was comparable to that with placebo, for example, epistaxis (6%), headache (3%), nasal irritation (2%), and sneezing (2%).

In patients with nasal polyps, the overall number of adverse events was comparable to that with placebo and similar to the number observed in patients with allergic rhinitis.

Treatment-related adverse reactions observed in clinical trials occurring in more than 1% of patients treated with Mommixon are listed in Table 2.

Table 2

After intranasal administration of mometasone furoate, hypersensitivity reactions, including bronchospasm and dyspnea, may occasionally occur. Very rarely, anaphylactic reactions, angioneurotic edema, or disturbances of smell and taste have been reported.

In patients with acute rhinosinusitis, the overall incidence of adverse events was comparable to that with placebo and similar to the incidence observed in patients with other indications. Treatment-related adverse reactions observed in clinical trials in more than 2% of patients, associated with other indications, are listed in Table 3.

Table 3

The most common adverse reaction, nosebleed, occurred with approximately the same frequency in the placebo group (2.6%) and in the Mometasone group (2.9% and 3.7%, respectively).

Systemic effects of intranasal corticosteroids may occur, particularly with long-term use of high doses.

Cases of glaucoma/increased intraocular pressure have been reported with the use of intranasal corticosteroids.

Cases of blurred vision have been reported.

Reporting of suspected adverse reactions and lack of drug efficacy after marketing authorization is of great importance. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, are encouraged to report all suspected adverse reactions and lack of efficacy via the automated pharmacovigilance information system at: https://aisf.gov.ua.

Shelf life. 2 years.

Shelf life after first opening of the container – 2 months.

Storage conditions. Store at a temperature not exceeding 25 °C.

Packaging. 10 g (60 doses), 16 g (120 doses), 18 g (140 doses) of suspension in a polyethylene bottle with a metering pump and nasal applicator. One bottle per cardboard box.

Prescription status. Prescription only.

Manufacturer.

Farmea, France/Farmea, France.

Adamed Pharma S.A., Poland/Adamed Pharma S.A., Poland.

Manufacturer's address and location of its business operations.

10 rue Bouche Thomas, ZAC d’Orgemont, Angers, 49000, France.

ul. marsz. J. Pilsudskiego 5, Pabianice, 95–200, Poland.