Mometasone-teva

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT Mometasone-Teva (Mometasone-Teva)

Composition:

Active substance: mometasone furoate;

1 metered dose (0.1 ml) contains mometasone furoate monohydrate (calculated as mometasone furoate) 50 mcg;

Excipients: microcrystalline cellulose and sodium carmellose, glycerin, benzalkonium chloride solution, polysorbate 80, citric acid monohydrate, sodium citrate dihydrate, water for injections.

Pharmaceutical form. Nasal spray, suspension.

Main physicochemical properties: milky-white suspension, free from agglomerates.

Pharmacotherapeutic group. Anti-inflammatory and other drugs for local application in 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 suppress the release of mediators of allergic reactions. Mometasone furoate significantly reduces the synthesis/release of leukotrienes from leukocytes of patients suffering from allergic diseases. Mometasone furoate has demonstrated high efficacy in cell culture studies in suppressing the synthesis/release of IL-1, IL-5, IL-6, and TNFα; it is also a potent inhibitor of leukotriene production. In addition, it is a potent inhibitor of Th2 cytokine production, including IL-4 and IL-5, from human CD4+ T-cells.

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

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

Pharmacokinetics.

The bioavailability of mometasone furoate following administration as a nasal spray is < 1% in plasma (according to data obtained using a sensitive method, the lower limit of quantification of which is 0.25 pg/mL). Mometasone furoate suspension is very poorly absorbed from the nasal mucosa, and the small amount that may be swallowed and absorbed undergoes extensive first-pass metabolism in the liver, with metabolites excreted in bile and urine.

Clinical characteristics.

Indications.

• Treatment of seasonal or perennial allergic rhinitis in adults and children aged 3 years and older.

• Treatment of nasal polyps 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 infections involving the nasal mucosa, such as herpes simplex.

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

Interaction with other medicinal products and other forms of interaction.

In a clinical study, no interaction was observed between the medicinal product and loratadine.

Concomitant therapy with CYP3A inhibitors, particularly agents containing cobicistat, is expected to increase the risk of systemic adverse effects. Such combination should be avoided, except when the expected benefit outweighs the increased risk of systemic corticosteroid adverse effects. In such cases, monitoring of patients for systemic corticosteroid adverse effects is necessary.

Special precautions for use.

Immunosuppression

The medicinal product Mometasone-Teva should be used with caution or not used at all in patients with active or latent tuberculosis infection of the respiratory tract, as well as in those with untreated fungal, bacterial, or systemic viral infections.

Patients receiving corticosteroids may potentially have suppressed immunity and should be warned about the increased risk of contracting certain infectious diseases (such as varicella or measles) upon exposure, and advised to consult a physician if such exposure 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; furthermore, mometasone furoate contributed to the normalization of the histological appearance of the nasal mucosa. As with any long-term therapy, patients using this 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 pharynx develops, discontinuation of treatment or initiation of appropriate antifungal therapy may be necessary. Persistent irritation of the nasal or pharyngeal mucosa may also be an indication for discontinuing the use of the medicinal product.

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

In clinical studies, the incidence of epistaxis was higher compared to placebo. Epistaxis was generally mild in severity and resolved spontaneously.

Systemic effects of corticosteroids

Systemic effects of intranasal corticosteroids may occur, particularly with high doses used over prolonged periods. These effects are much less common than with oral corticosteroids and may vary among different patients and 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 following the use of intranasal corticosteroids.

Patients who switch to intranasal spray treatment after prolonged systemic corticosteroid therapy require careful monitoring. Discontinuation of systemic corticosteroids in these patients may result in 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 appropriate treatment measures. During such transition, pre-existing allergic conditions such as allergic conjunctivitis or eczema, previously suppressed by systemic corticosteroid therapy, may become apparent.

Use of doses higher than recommended may lead to clinically significant adrenal suppression. If there is evidence of doses exceeding the recommended levels, consideration should be given to administering additional systemic corticosteroids 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, particularly those with ulceration or bleeding, which are atypical in presentation, require further investigation.

Visual disturbances

Visual disturbances may occur with the use of systemic and topical corticosteroids. If a patient develops symptoms such as blurred vision or other visual disturbances, the patient should be referred to an ophthalmologist for evaluation of possible causes, including cataract, glaucoma, or rare conditions such as central serous chorioretinopathy, which have been reported after systemic and local corticosteroid use.

Effect on growth in children

It is recommended to regularly monitor the growth of children receiving long-term treatment with intranasal corticosteroids. If growth retardation occurs, therapy should be re-evaluated with the aim of reducing the dose of the intranasal corticosteroid, if possible, to the lowest dose that maintains adequate symptom control. Additionally, the patient should be referred to a pediatrician. No growth retardation was reported in children treated with mometasone furoate at a daily dose of 100 mcg for one year.

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 Mometasone-Teva 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. As with other intranasal corticosteroids, Mometasone-Teva should be used during pregnancy only if the potential 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 is excreted in human breast milk. As with other intranasal corticosteroids, a decision should be made whether to discontinue breastfeeding or to discontinue/abstain from mometasone furoate nasal spray therapy, taking into account the benefits of breastfeeding for the child and the benefits of therapy for the woman.

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

Ability to affect reaction speed when driving or operating machinery.

Unknown.

Method of Administration and Dosage

Before using the first dose, shake the bottle well and press the spray pump ten times (until a uniform spray is obtained). If the spray pump has not been used for 14 days or longer, it must be re-primed by pressing the pump twice until a uniform spray is obtained. Shake the bottle well before each use. After the number of doses indicated on the label has been used, or 2 months after first use, the bottle should be discarded.

After priming the spray pump of the medicinal product Mometasone Teva, each spray delivers approximately 100 mg of mometasone furoate suspension, containing the equivalent of mometasone furoate monohydrate – 50 mcg of mometasone furoate to each nostril.

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

If symptoms are not adequately controlled 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 mcg). After symptom relief is achieved, dose reduction is recommended.

For children aged 3–11 years, the recommended therapeutic dose is 1 spray (50 mcg) in each nostril once daily (total daily dose – 100 mcg).

Treatment with mometasone furoate nasal spray may be initiated several days before the anticipated start of the pollen season in patients with a history of moderate to severe seasonal allergic rhinitis.

The medicinal 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 the full therapeutic effect.

Nasal polyps: Adults (including elderly patients) the recommended dose is 2 sprays (50 mcg each) in each nostril once daily (total daily dose – 200 mcg). If symptoms are not adequately controlled after 5–6 weeks of treatment, the daily dose may be increased to 2 sprays in each nostril twice daily (total daily dose – 400 mcg). After achieving a clinical response, the dose should be reduced to 2 sprays in each nostril once daily (total daily dose – 200 mcg). If symptoms are not adequately controlled after 5–6 weeks of treatment with 2 sprays twice daily, alternative treatment options should be considered.

Clinical studies on the efficacy and safety of mometasone furoate nasal spray in the treatment of nasal polyposis lasted four months.

Children

Seasonal or perennial allergic rhinitis

The safety and efficacy of Mometasone Teva in children under 3 years of age have not been established.

Nasal polyps

The safety and efficacy of Mometasone Teva in children under 18 years of age have not been established.

Overdose

Due to the low systemic bioavailability of the medicinal product (< 1%), it is unlikely that any measures other than patient observation and subsequent use of the medicinal product 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

In clinical trials of allergic rhinitis, nasal bleeding was mainly self-limiting, mild, and occurred slightly more frequently than with placebo (5%), but at a comparable or lower frequency than with other investigational intranasal corticosteroids used as active control (up to 15%). The incidence of other adverse reactions was comparable to that observed with placebo. In patients with nasal polyps, the overall incidence of adverse reactions was similar to that observed in patients with allergic rhinitis.

Systemic effects of intranasal corticosteroids are more likely to occur with high-dose and long-term use.

The adverse reactions listed below (≥ 1%) were observed during clinical trials in patients with allergic rhinitis or nasal polyposis, as well as during post-marketing use.

Adverse reactions are classified by system organ class and frequency of occurrence. Frequency categories are defined as follows: very common (≥ 1/10); common (≥ 1/100, < 1/10); uncommon (≥ 1/1000, < 1/100). The frequency of adverse reactions in post-marketing experience is considered "unknown" (cannot be estimated based on available data).

Infections and infestations.
Common: pharyngitis, upper respiratory tract infections².

Immune system disorders.
Unknown: hypersensitivity, including anaphylactic reactions, angioneurotic edema, bronchospasm, and dyspnea.

Nervous system disorders.
Common: headache.

Eye disorders.
Unknown: glaucoma, increased intraocular pressure, cataract, blurred vision.

Respiratory, thoracic and mediastinal disorders.
Very common: epistaxis¹.
Common: epistaxis, burning sensation of nasal mucosa, nasal mucosa irritation, nasal mucosa ulceration.
Unknown: nasal septum perforation.

Gastrointestinal disorders.
Common: throat irritation¹.
Unknown: disturbances of taste and smell.

¹ Observed with twice-daily administration for the treatment of nasal polyposis.
² Observed uncommonly with twice-daily administration for the treatment of nasal polyposis.

Children

In children, the incidence of reported adverse reactions during clinical trials—such as epistaxis (6%), headache (3%), nasal mucosa irritation (2%), and sneezing (2%)—was comparable to that observed with placebo.

Reporting of suspected adverse reactions

It is important to report suspected adverse reactions after marketing authorization. This enables ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are encouraged to report any suspected adverse reactions.

Shelf life. 2 years.

After first use – 8 weeks.

Storage conditions.

Store at temperatures not exceeding 25 °C. Keep out of the reach of children. Do not freeze.

Packaging.
10 g (60 doses) in a high-density polyethylene bottle with a polypropylene metered spray pump and nozzle, closed with a polypropylene cap. One bottle per cardboard box.

Prescription category. Prescription only.

Manufacturer. Teva Czech Industries s.r.o.

Manufacturer's address and place of business.
Ostravska 305/29, Komarov, 747 70 Opava, Czech Republic.