Momenaz

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT MOMEMAZ (MOMENAS)

Composition:

Active substance: mometasone furoate;

One dose contains 50 mcg of mometasone furoate monohydrate, calculated as the anhydrous form;

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

Pharmaceutical form. Nasal spray, metered.

Main physicochemical properties: viscous suspension, white to almost white in color.

Pharmacotherapeutic group. Anti-inflammatory and other locally acting drugs for nasal cavity disorders. Corticosteroids. ATC code R01AD09.

Pharmacological properties.

Pharmacodynamics. Mometasone furoate is a synthetic corticosteroid for topical use that exerts a pronounced anti-inflammatory effect. The local anti-inflammatory action of mometasone furoate occurs at doses that do not produce systemic effects.

The primary mechanism of the anti-inflammatory and antiallergic action of mometasone furoate is related to its ability to inhibit the release of mediators of allergic reactions. Mometasone furoate significantly reduces the synthesis/release of leukotrienes from leukocytes of patients suffering from allergic diseases. In cell culture studies, mometasone furoate demonstrated 10-fold greater activity than other steroids—including beclomethasone dipropionate, betamethasone, hydrocortisone, and dexamethasone—in suppressing the synthesis/release of IL-1, IL-5, IL-6, and TNFα. It is also a potent inhibitor of Th2-cytokine production, including IL-4 and IL-5, from human CD4+ T-cells. Mometasone furoate is also 6 times more active than beclomethasone dipropionate and betamethasone in inhibiting IL-5 production.

In challenge studies involving antigen application to the nasal mucosa, mometasone furoate nasal spray demonstrated high anti-inflammatory activity in both the early and late phases of the allergic response. This was confirmed by a reduction (compared to placebo) in histamine levels and eosinophil activity, as well as a decrease (compared to baseline) in the number of eosinophils, neutrophils, and epithelial cell adhesion proteins.

A pronounced clinical effect within the first 12 hours of treatment with mometasone furoate nasal spray was achieved in 28% of patients with seasonal allergic rhinitis. On average (50%), symptom relief occurred within 35.9 hours. In addition, mometasone furoate nasal spray demonstrated significant efficacy in reducing ocular symptoms (redness, tearing, itching) in patients with seasonal allergic rhinitis.

In clinical studies involving patients with nasal polyps, mometasone furoate nasal spray demonstrated significant clinical efficacy in relieving nasal congestion, reducing polyp size, and restoring the sense of smell compared to placebo.

In clinical studies involving patients aged 12 years and older, mometasone furoate nasal spray at a dose of 200 mcg twice daily demonstrated high efficacy in alleviating symptoms of rhinosinusitis compared to placebo. Over 15 days of treatment, rhinosinusitis symptoms were assessed using the Major Symptom Score (MSS) scale (facial pain, pressure in the nasal sinuses, tenderness upon palpation, pain in the sinus area, rhinorrhea, postnasal drip, and nasal congestion). The efficacy of amoxicillin 500 mg three times daily did not differ significantly from placebo in reducing rhinosinusitis symptoms on the MSS scale. During the follow-up period after treatment completion, the recurrence rate in the group receiving mometasone furoate nasal spray was low and comparable to that in the amoxicillin and placebo groups. Treatment duration for acute rhinosinusitis exceeding 15 days was not evaluated.

Pharmacokinetics. The bioavailability of mometasone furoate following administration as a nasal spray is <1% in plasma (based on data obtained using a sensitive method with a lower limit of quantification of 0.25 mg/mL). Mometasone furoate suspension is very poorly absorbed from the gastrointestinal tract, and any small amount that may be swallowed and absorbed undergoes extensive first-pass metabolism prior to excretion, primarily in the form of metabolites via bile and to a lesser extent via urine.

Clinical characteristics.

Indications.

• For the 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 the antibiotic treatment of acute episodes of sinusitis in adults (including elderly) and children aged 12 years and older.
• For the treatment of symptoms of acute rhinosinusitis without signs of severe bacterial infection in adults and children aged 12 years and older.
• For the 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.

The medicinal product should not be used in the presence of untreated localized infections involving the nasal mucosa, such as herpes simplex.

Due to the ability of corticosteroids to suppress wound healing, nasal corticosteroids should not be administered to patients who have recently undergone nasal surgery or have experienced nasal trauma until healing has occurred.

Interaction with other medicinal products and other forms of interaction. Concomitant therapy with CYP3A inhibitors, including products containing cobicistat, is expected to increase the risk of systemic adverse effects. Concomitant use should be avoided unless the benefit outweighs the increased risk of systemic corticosteroid side effects; in such cases, patients should be monitored for the occurrence of systemic corticosteroid adverse effects.

In a clinical study, mometasone furoate nasal spray was administered concomitantly with a non-sedating oral antihistamine (loratadine). The pharmacokinetic parameters and safety profile of both drugs remained unchanged.

Special precautions for use.

The medicinal product MOMENAZ should be used with caution or not used at all in patients with active or latent respiratory tract tuberculosis, as well as in cases of untreated fungal, bacterial, or systemic viral infections.

Patients receiving corticosteroids may have a potentially suppressed immune system and should be warned about the increased risk of infection upon contact with certain infectious diseases (such as chickenpox, measles), and advised to consult a physician if such contact occurs.

Local effects

After 12 months of treatment with mometasone furoate in patients with perennial allergic rhinitis, no signs of nasal mucosal atrophy were observed; moreover, mometasone furoate contributed to normalization of the histological picture of the nasal mucosa. As with any long-term therapy, patients using the medicinal product for several months or longer should undergo periodic examinations to detect possible changes in the nasal mucosa. If a local fungal infection of the nose or throat develops, therapy with the medicinal product may need to be discontinued or appropriate treatment initiated. Persistent irritation of the nasal or pharyngeal mucosa may also be an indication for discontinuation of the medicinal product.

The use of mometasone furoate is not recommended in the event of nasal septum perforation.

In clinical studies, the incidence of epistaxis (nosebleeds) was higher compared to placebo. Nosebleeds were generally mild in severity and resolved spontaneously.

Systemic effects of corticosteroids

Systemic effects of nasal corticosteroids may occur, particularly when high doses are used for prolonged periods. These effects are significantly less common than with oral corticosteroids and may vary among different patients and with different corticosteroid products. Potential systemic effects may include Cushing's syndrome, Cushingoid features, adrenal suppression, growth retardation in children and adolescents, cataract, glaucoma, and less frequently, a range of psychological or behavioral effects such as psychomotor hyperactivity, sleep disturbances, anxiety, depression, or aggression (particularly in children).

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

Vision disturbances may occur with the use of both systemic and locally acting 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 of visual impairment, which may include cataract, glaucoma, or rare conditions such as central serous chorioretinopathy, which has been reported after the use of both systemic and locally acting corticosteroids.

Patients transitioning to treatment with nasal spray after prolonged systemic corticosteroid therapy require careful monitoring. Discontinuation of systemic corticosteroids in these patients may lead to adrenal insufficiency for several months until recovery of the hypothalamic-pituitary-adrenal axis. If such patients exhibit signs and symptoms of adrenal insufficiency or withdrawal syndrome (e.g., joint and/or muscle pain, fatigue, depression), despite resolution of nasal symptoms, systemic corticosteroid therapy should be reinstated along with other treatment measures. During this transition, pre-existing allergic conditions such as allergic conjunctivitis or eczema, previously suppressed by systemic corticosteroid therapy, may also become apparent.

Use of doses higher than recommended may lead to clinically significant adrenal suppression. If evidence of doses exceeding the recommended amount is present, consideration should be given to the possible need for additional systemic corticosteroid coverage during periods of stress or elective surgical procedures.

Nasal polyps

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

Unilateral polyps, which are atypical and rarely occur, especially if associated with ulceration or bleeding, should be investigated further.

Effect on growth in children

Regular monitoring of growth in children receiving long-term treatment with nasal corticosteroids is recommended. If growth retardation occurs, therapy should be reviewed with the aim of reducing the dose of the nasal corticosteroid, if possible, to the lowest dose at which effective symptom control is maintained. In addition, the patient should be referred for consultation with a pediatrician.

Non-nasal symptoms

Although the medicinal product controls nasal symptoms in most patients, concomitant use of appropriate additional therapy may provide further relief of other symptoms, particularly ocular symptoms.

The medicinal product MOMENAZ contains benzalkonium chloride, which may cause irritation and swelling of the nasal mucosa, especially with prolonged use.

Use during pregnancy or breastfeeding.

Pregnancy

Data on the effects of mometasone furoate when used during pregnancy are limited or absent. Animal studies have shown reproductive toxicity. Like other nasal corticosteroids, MOMENAZ should be used during pregnancy only if the expected benefit justifies the potential risk to the mother, fetus, or infant. Infants born to mothers who used corticosteroids during pregnancy should be carefully monitored for possible adrenal insufficiency.

Breastfeeding

It is unknown whether mometasone furoate passes into breast milk. As with other nasal corticosteroids, breastfeeding should be discontinued or treatment with mometasone furoate nasal spray should be discontinued or avoided, taking into account the benefits of breastfeeding for the child and the therapeutic benefit for the mother.

Fertility

Clinical data on the effect of mometasone furoate on fertility are lacking. Animal studies have shown reproductive toxicity, but no effect on fertility.

Ability to affect reaction speed when driving or operating machinery.

Unknown.

Method of administration and dosage.

Before using a new bottle of the medicinal product, it should be primed. Priming is performed by approximately 10 actuations of the metered-dose pump-sprayer, after which a consistent delivery of the medicinal substance is established, with each actuation delivering approximately 100 mg of suspension containing 50 µg of mometasone (1 dose). If the nasal spray has not been used for 14 days or longer, re-priming is required before the next use by 2 actuations until full delivery is observed. Do not pierce the nozzle before starting use.

The bottle should be shaken vigorously before each administration.

If the nozzle becomes clogged, remove the plastic cap by gently pressing on the white ring, carefully remove the nozzle, rinse it under warm running water, dry it, and replace it in its original position. Do not attempt to clear the nozzle with a needle or other sharp object, as this may damage the dispenser.

Regular cleaning of the nozzle is very important.

The nose should be thoroughly cleared of mucus before each administration.

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

If symptom relief cannot be achieved with the recommended therapeutic dose, the daily dose may be increased to the maximum: 4 sprays in each nostril once daily (total daily dose — 400 µg). After symptom relief, dose reduction is recommended.

The product 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 full therapeutic effect.

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

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

If symptom relief cannot be achieved with the recommended therapeutic dose, the daily dose may be increased to 4 sprays in each nostril twice daily (total daily dose — 800 µg). 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 µg each) in each nostril twice daily (total daily dose — 400 µg).

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

Children. During placebo-controlled clinical studies in children receiving mometasone furoate nasal spray at a daily dose of 100 µg for one year, no growth retardation was observed.

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

Overdose. Overdose is unlikely to require any therapy other than observation.

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

Adverse reactions.

Adverse reactions associated with treatment with mometasone furoate observed in clinical studies in patients with allergic rhinitis are presented in Table 1.

Table 1.

Treatment-related adverse reactions with mometasone furoate in patients with allergic rhinitis

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

In children, the incidence of adverse events was similar to that with placebo, for example: nasal bleeding (6%), headache (3%), nasal irritation (2%), 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.

Adverse reactions related to treatment with mometasone furoate observed in clinical trials in more than 1% of patients are listed in Table 2.

Table 2.

Treatment-related adverse reactions with mometasone furoate in patients with nasal polyps

After intranasal administration of mometasone furoate, hypersensitivity reactions, including bronchospasm and dyspnea, may occasionally occur. Very rarely, anaphylactic reactions, angioedema, 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 are listed in Table 3.

Table 3.

Treatment-related adverse reactions with mometasone furoate in patients with acute rhinosinusitis

The most common adverse reaction — nasal bleeding — occurred at approximately the same frequency in the placebo group (2.6%) and in the mometasone furoate medicinal product group (2.9% and 3.7%, respectively).

Systemic effects of nasal corticosteroids may occur, especially with prolonged use of high doses.

Cases of glaucoma / increased intraocular pressure have been reported with the use of intranasal corticosteroids. Reports of blurred vision have also occurred.

Reporting of adverse reactions after medicinal product registration is of great importance. It enables ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmaceutical professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 2 years.

Shelf life after first opening — 2 months.

Storage conditions. Store at temperatures not exceeding 25 °C.

Store in a light-protected place, away from fire and heating devices.

Do not freeze.

Keep out of reach of children.

Packaging. 10 g (60 doses) or 18 g (140 doses) of suspension in a polyethylene bottle with a metered dose pump-sprayer, closed with a cap; 1 bottle per cardboard box.

Prescription status. Prescription only.

Manufacturer. PHARMEA.

Manufacturer's address. ZAC d'Orgeval, 10 rue Boucher de Touraine, ANGERS, 49000, France.