Instructions Flix spray nasal suspension 0.05% bottle with pump dispenser 9 g
Composition
active ingredient: mometasone furoate;
1 dose contains 51.8 mcg of mometasone furoate monohydrate, which is equivalent to 50 mcg of mometasone furoate;
excipients: glycerin, sodium carboxymethylcellulose-microcrystalline cellulose (Avicel RC-591), sodium citrate dihydrate, citric acid monohydrate, benzalkonium chloride solution, polysorbate 80, purified water.
Dosage form
Nasal spray, suspension.
Main physicochemical properties: viscous, homogeneous, whitish, odorless suspension.
Pharmacotherapeutic group
Anti-edematous and other drugs for topical use in diseases of the nasal cavity. Corticosteroids. ATX code R01A D09.
Pharmacological properties
Pharmacodynamics
Mometasone furoate is a synthetic corticosteroid for topical use that has a pronounced anti-inflammatory effect. The local anti-inflammatory effect of mometasone furoate is manifested when using doses that do not cause systemic effects.
The mechanism of anti-inflammatory and antiallergic action of mometasone furoate is mainly 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. Mometasone furoate has demonstrated 10 times greater activity in cell culture than other steroids, including beclomethasone dipropionate, betamethasone, hydrocortisone and dexamethasone, in inhibiting the synthesis/release of IL-1, IL-5, IL-6 and TNFα. It is also a potent inhibitor of the production of Th2 cytokines, 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 the production of IL-5.
In nasal challenge studies, mometasone furoate nasal spray demonstrated high anti-inflammatory activity in both the early and late stages of allergic reactions, as evidenced by reductions in histamine and eosinophil activity compared to placebo, as well as reductions in eosinophil, neutrophil and epithelial cell adhesion protein levels compared to baseline.
A significant clinical effect within the first 12 hours of using mometasone furoate nasal spray was achieved in 28% of patients with seasonal allergic rhinitis. On average (50%) relief occurred within 35.9 hours. In addition, mometasone furoate nasal spray was significantly effective in reducing visual symptoms (redness, tearing, itching) in patients with seasonal allergic rhinitis.
In clinical studies involving patients with nasal polyps, mometasone furoate in the form of a nasal spray demonstrated significant clinical efficacy in relieving nasal congestion, reducing polyp size, and restoring the sense of smell compared to placebo.
In clinical trials in patients 12 years of age and older, mometasone furoate nasal spray 200 mcg twice daily was shown to be more effective than placebo in reducing symptoms of rhinosinusitis. Symptoms of rhinosinusitis were assessed using the Major Symptom Score (MSS) (facial pain, sinus pressure, pressure pain, sinus pain, rhinorrhea, postnasal drip, and nasal congestion) over 15 days of treatment. Amoxicillin 500 mg three times daily was not significantly different from placebo in reducing symptoms of rhinosinusitis on the MSS scale. During the follow-up period after completion of treatment, the number of relapses in the mometasone furoate group was low and comparable to the number of relapses in the amoxicillin and placebo groups. The duration of treatment for acute rhinosinusitis beyond 15 days has not been evaluated.
Pharmacokinetics
The bioavailability of mometasone furoate when administered as a nasal spray is < 1% in plasma (based on data obtained using a sensitive method, the lower limit of quantification is 0.25 pg/mL). Mometasone furoate suspension is very poorly absorbed from the gastrointestinal tract, and the small amount that can be swallowed and absorbed undergoes extensive first-pass metabolism before being excreted primarily as metabolites in the bile and, to some extent, in the urine.
Distribution.
In vitro protein binding of mometasone furoate was reported to be 98-99% over the concentration range of 5-500 ng/mL.
Metabolism.
In the study of the metabolism of mometasone furoate, the absence of its major metabolites in plasma was proven. In vitro, one of the minor metabolites was identified - 6β-hydroxymometasone furoate, which is metabolized with the participation of P-450 3A4 (CYP3A4).
Breeding.
The half-life is 5.8 hours. The main part of the metabolites is excreted in the bile, the rest is excreted in the urine.
Indication
As an adjunctive therapy in the antibiotic treatment of acute episodes of sinusitis in adults (including the elderly) and children aged 12 years and older.
Treatment of symptoms of acute rhinosinusitis without evidence 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.
Contraindication
Hypersensitivity to the active substance or to any inactive component of the medicinal product.
Interaction with other medicinal products and other types of interactions
Concomitant therapy with CYP3A inhibitors, including cobicistat-containing products, is expected to increase the risk of systemic adverse reactions. Concomitant use should be avoided unless the benefit outweighs the increased risk of systemic corticosteroid adverse reactions, in which case patients should be monitored for systemic corticosteroid adverse reactions.
In a clinical study, mometasone furoate was administered concomitantly with a non-sedating oral antihistamine (loratadine). The pharmacokinetic parameters and safety profile were unchanged for both drugs.
Application features
The drug should not be used in the presence of untreated local infection involving the nasal mucosa.
Because corticosteroids have the effect of inhibiting wound healing, patients who have recently had nasal surgery or trauma should not use a nasal corticosteroid until healing has occurred.
Flix should be used with caution or not at all in patients with active or latent tuberculosis infection of the respiratory tract, as well as in untreated fungal, bacterial, systemic viral infections, or herpes simplex infection with eye involvement.
As with any long-term treatment, patients receiving the drug for several months or longer should be periodically examined for possible changes in the nasal mucosa. In clinical studies, after 12 months of treatment with mometasone furoate, there was no evidence of atrophy of the nasal mucosa; in addition, mometasone furoate contributed to the normalization of the histological picture of the nasal mucosa.
In the event of the development of a local fungal infection of the nose or throat, it may be necessary to discontinue therapy with the drug or to conduct appropriate treatment. Irritation of the nasal and pharyngeal mucosa that persists for a long time may also be an indication for discontinuation of treatment with the drug.
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, the patient should be evaluated by an ophthalmologist to evaluate possible causes of visual disturbances, including cataracts, glaucoma, or rare conditions such as central serous chorioretinopathy, which have been reported following the use of systemic and topical corticosteroids.
There is no evidence of suppression of the hypothalamic-pituitary-adrenal axis during long-term treatment with mometasone furoate. However, long-term use of nasal corticosteroids may affect adrenal function and cause hypercorticism, particularly in corticosteroid-sensitive patients. Patients transferred to Flixonase after long-term systemic corticosteroid therapy should be carefully monitored for adrenal insufficiency.
The safety and efficacy of mometasone furoate in the treatment of unilateral polyps, polyps associated with cystic fibrosis, or polyps that obstruct the nasal cavity have not been studied.
Unilateral polyps, which are unusual and rare, should be investigated in more detail, especially if ulceration or bleeding occurs.
Patients taking corticosteroids may have reduced immune reactivity and should be warned of the increased risk of infection from contact with patients with certain infectious diseases (e.g., chickenpox, measles), and of the need to consult a doctor if such contact occurs.
The safety and efficacy of mometasone furoate in the treatment of nasal polyps in children and adolescents (under 18 years of age) have not been studied.
When switching from systemic corticosteroid therapy to mometasone furoate, some patients may experience corticosteroid withdrawal symptoms along with relief of nasal symptoms. Such patients should be specifically advised to continue treatment with mometasone furoate.
High doses or prolonged use of glucocorticosteroids may cause systemic effects such as growth suppression in children. The long-term effects of intranasal/inhaled steroids in children are not fully understood. As a general rule, the physician should closely monitor the growth of a child receiving long-term glucocorticosteroid treatment. In a study of 49 children treated with mometasone furoate 100 mcg/day for one year, no growth retardation was observed.
Cases of increased intraocular pressure have been reported following the use of intranasal corticosteroids.
Acute rhinosinusitis: Patients should be advised to seek immediate medical attention if they develop symptoms of a serious bacterial infection, such as fever, severe unilateral facial or dental pain, orbital or periorbital swelling/edema, or worsening of symptoms after initial improvement.
The safety and efficacy of mometasone furoate in the treatment of symptoms of rhinosinusitis in children under 12 years of age have not been studied.
Benzalkonium chloride: Flix contains benzalkonium chloride. 1 g of Flix contains 0.6 mg of benzalkonium chloride. This amount is not expected to cause bronchospasm.
Use during pregnancy or breastfeeding
Systemic (subcutaneous) corticosteroids have been shown to be teratogenic in animals. Clinical studies in pregnant or lactating women have not been conducted.
Corticosteroid medications should not be used by pregnant or breastfeeding women unless absolutely necessary.
Ability to influence reaction speed when driving vehicles or other mechanisms
Unknown.
Method of administration and doses
Before each use, the nose should be thoroughly cleaned of mucus.
Treatment and prevention of seasonal or perennial allergic rhinitis in adults and children over 12 years of age. The recommended prophylactic and therapeutic dose of the drug for adults (including elderly patients) and children over 12 years of age is 2 injections (50 mcg each) into each nostril once a day (total daily dose - 200 mcg). After achieving a therapeutic effect, for maintenance therapy, it is advisable to reduce the dose to 1 injection into each nostril once a day (total daily dose - 100 mcg).
If relief of symptoms is not achieved by using the drug in the recommended therapeutic dose, the daily dose can be increased to the maximum: 4 sprays in each nostril once a day (total daily dose - 400 mcg). After relief of symptoms, it is recommended to reduce the dose.
Mometasone furoate has demonstrated a clinically significant onset of action within 12 hours of first application in some patients with seasonal allergic rhinitis. However, the full benefit of treatment may not be achieved within the first 48 hours, so the patient must continue regular application to achieve the full therapeutic effect.
The recommended therapeutic dose for children aged 2-11 years is 1 spray (50 mcg) in each nostril once a day (total daily dose – 100 mcg).
Treatment of patients with seasonal allergic rhinitis should begin with prophylactic use of the drug 2 to 4 weeks before the flowering season.
Adjunctive treatment of acute episodes of sinusitis. The recommended therapeutic dose for adults (including elderly patients) and children aged 12 years and over is 2 sprays (50 mcg) in each nostril 2 times a day (total daily dose – 400 mcg).
If relief of symptoms is not achieved by using the drug at the recommended therapeutic dose, the daily dose can be increased to 4 sprays in each nostril 2 times a day (total daily dose - 800 mcg). After relief of symptoms, a dose reduction is recommended.
Acute rhinosinusitis. The recommended therapeutic dose for adults and children aged 12 years and over is 2 sprays (50 mcg) in each nostril 2 times a day (total daily dose – 400 mcg).
Nasal polyps. The recommended dose for patients aged 18 years and over (including elderly patients) is 2 sprays (50 mcg) in each nostril 2 times a day (total daily dose – 400 mcg). After achieving a clinical effect, it is recommended to reduce the dose to 2 sprays in each nostril 1 time a day (total daily dose – 200 mcg).
Children
In studies in children treated with mometasone furoate at a daily dose of 100 mcg for one year, no growth retardation was observed.
The safety and efficacy of mometasone furoate 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, or seasonal or perennial allergic rhinitis in children under 2 years of age have not been studied.
Overdose
It is unlikely that an overdose will require any treatment other than observation.
Inhalation or oral administration of excessive doses of corticosteroids may lead to suppression of the function of the hypothalamic-pituitary-adrenal axis.
Adverse reactions
Adverse reactions associated with mometasone furoate treatment observed in clinical trials in patients with allergic rhinitis are listed in Table 1.
Table 1. Adverse reactions associated with mometasone furoate treatment in patients with allergic rhinitis very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1000, <1/100), rare (≥ 1/10000, <1/1000), very rare (<1/10000) |
| Respiratory, thoracic and mediastinal disorders |
| Often | Nosebleed, pharyngitis, burning sensation in the nose, feeling of irritation in the nose, nasal ulcers |
| General disorders and administration site conditions |
| Often | Headache |
Epistaxis was self-limiting and mild, occurring somewhat more frequently than with placebo (5%), but less frequently than with other intranasal corticosteroids studied and used as active controls (some of which had an incidence of up to 15%). The incidence of other adverse events was comparable to that with placebo.
In children, the incidence of adverse events was comparable to that seen with placebo, such as: nosebleeds (6%), headache (3%), nasal irritation (2%), and sneezing (2%).
In patients with nasal polyps, the overall incidence of adverse events was comparable to that seen with placebo and similar to that seen in patients with allergic rhinitis.
Adverse reactions associated with mometasone furoate treatment that occurred in more than 1% of patients in clinical trials are listed in Table 2.
Table 2. Adverse reactions associated with mometasone furoate treatment in patients with nasal polyps very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1000, <1/100), rare (≥ 1/10000, <1/1000), very rare (<1/10000) |
| 200 mcg once daily | 200 mcg 2 times a day |
| Respiratory, thoracic and mediastinal disorders |
| Upper respiratory tract |
| Infections | often | infrequently |
| Nosebleeds | often | very often |
| Gastrointestinal tract |
| Throat irritation | - | often |
| General disorders and administration site conditions |
| Headache | often | often |
Hypersensitivity reactions, including bronchospasm and dyspnoea, may occasionally occur following intranasal administration of mometasone furoate. Anaphylactic reactions, angioedema or disturbances of smell and taste have been reported very rarely.
In patients with acute rhinosinusitis, the overall incidence of adverse events was comparable to that seen with placebo and similar to that seen in patients with other indications. Treatment-related adverse reactions that occurred in more than 2% of patients in clinical trials are listed in Table 3.
Table 3. Adverse reactions associated with mometasone furoate treatment in patients with acute rhinosinusitis very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1000, <1/100), rare (≥ 1/10000, <1/1000), very rare (<1/10000) |
| 200 mcg once daily | 200 mcg 2 times a day |
| Respiratory, thoracic and mediastinal disorders |
| Upper respiratory tract |
| Nosebleeds | often | often |
| Gastrointestinal tract |
| Abdominal pain | often | often |
| Diarrhea | often | often |
| Nausea | often | often |
| General disorders and administration site conditions |
| Headache | often | often |
The most common adverse reaction, nosebleed, occurred with approximately the same frequency in the placebo group (2.6%) and the mometasone furoate group (2.9% and 3.7%, respectively).
Systemic effects of nasal corticosteroids may occur, especially when used at high doses for long periods.
Cases of glaucoma/increased intraocular pressure have been reported with the use of intranasal corticosteroids.
Blurred vision has been reported during post-marketing use.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C out of the reach of children.
Do not freeze.
Packaging
9 g or 18 g in a polyethylene bottle with a dosing pump; 1 bottle in a cardboard box.
Vacation category
According to the recipe.
Producer
ABDI IBRAHIM Ilach Sanai ve Tijaret A.S.
Location of the manufacturer and address of its place of business
Orhan Gazi Mahallesi, Tunç Caddesi No. 3, Esenyurt, Istanbul, Turkey.
Applicant
Delta Medical Promotions AG.
Applicant's location
Ottenbachgasse 26, Zurich CH – 8001, Switzerland.
