Pharmacodynamics. Mometasone furoate - synthetic corticosteroids for topical use, has a pronounced anti-inflammatory effect. The local anti-inflammatory effect of mometasone furoate is manifested in doses at which there are no systemic effects.
Basically, the mechanism of anti-inflammatory and anti-allergic action of mometasone furoate is associated with its ability to suppress the release of mediators of allergic reactions. Mometasone furoate significantly reduces the synthesis / release of leukotrienes from leukocytes of patients with allergic diseases. Mometasone furoate has been shown to be 10 times more active in cell culture than other steroids, including beclomethasone dipropionate, betamethasone, hydrocortisone, and dexamethasone, in inhibiting the synthesis / release of interleukin (IL) -1, IL-6, and tumor necrosis factor-α. 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 potent than beclomethasone dipropionate and betamethasone in inhibiting IL-5 production.
In the course of studies with provocative tests with the application of antigens to the nasal mucosa, a high anti-inflammatory activity of the nasal spray mometasone furoate was revealed both in the early and in the late stages of an allergic reaction. This was confirmed by a decrease (compared with placebo) in the level of histamine and eosinophil activity, as well as a decrease (compared to baseline) in the number of eosinophils, neutrophilic granulocytes and epithelial cell adhesion proteins.
A pronounced clinical effect in the first 12 hours of mometasone furoate nasal spray application was achieved in 28% of patients with seasonal allergic rhinitis. On average (50%) improvement occurred within 35.9 hours. In addition, Flix showed significant efficacy in relieving eye symptoms (redness, lacrimation, itching) in patients with seasonal allergic rhinitis.
During clinical studies in patients with nasal polyps, Flix has demonstrated significant clinical efficacy in eliminating nasal congestion, reducing the size of polyps, and restoring the sense of smell compared to placebo.
In clinical trials involving patients aged 12 years and older, the use of a spray of 200 μg 2 times a day has been shown to be highly effective in reducing the symptoms of rhinosinusitis compared with placebo.
Pharmacokinetics. The bioavailability of mometasone furoate when used in the form of a water-based nasal spray is insignificant (≤0.1%), and it is practically not detected in blood plasma even when using a sensitive method of determination with a sensitivity threshold of 50 pg / ml. In this regard, there are no corresponding pharmacokinetic data for this dosage form. A suspension of mometasone furoate is very poorly absorbed in the gastrointestinal tract, and a small amount that can be swallowed and absorbed undergoes active primary metabolism even before excretion, mainly in the form of metabolites in the bile and to some extent in the urine.
Distribution. It was reported that in vitro binding of mometasone furoate to blood proteins was 98–99% in the concentration range of 5–500 ng / ml.
Metabolism. When studying the metabolism of mometasone furoate, the absence of its main metabolites in blood plasma was proved. In vitro, one of the minor metabolites, 6β-hydroxymethasone furoate, was identified, which is metabolized with the participation of P450 3A4 (CYP 3A4).
Excretion. T½ is 5.8 hours. The main part of the metabolites is excreted in the bile, the rest in the urine.
Treatment in the presence of symptoms of seasonal and perennial allergic rhinitis in adults and children aged 2 years and older; preventive treatment of moderate to severe seasonal allergic rhinitis in adults and children over the age of 12 years; as an auxiliary therapeutic agent in the treatment of acute episodes of sinusitis with antibiotics in adults (including elderly patients) and children over the age of 12 years; treatment in the presence of symptoms of acute rhinosinusitis without signs of severe bacterial infection in adults and children over the age of 12 years; treating nasal polyps and related symptoms, including nasal congestion and loss of olfactory sensations in patients over the age of 18.
The duration of the course of treatment is determined by the doctor. Before each use, you should thoroughly cleanse the nose of mucus.
Application for the treatment and prevention of seasonal or perennial allergic rhinitis in adults and children over the age of 12 years. For adults (including elderly patients) and children over the age of 12, the recommended prophylactic and therapeutic dose of the preparation is 2 injections (50 mcg each) in each nostril 1 time per day (total daily dose - 200 mcg). After achieving a therapeutic effect for maintenance therapy, it is advisable to reduce the dose to 1 injection in each nostril 1 time per day (total daily dose - 100 mcg).
If the weakening of the symptoms of the disease cannot be achieved by using the preparation in the recommended therapeutic dose, the daily dose can be increased to the maximum: 4 injections into each nostril 1 time per day (total daily dose - 400 mcg). After a decrease in the severity of symptoms of the disease, a dose reduction is recommended.
The preparation showed a clinically significant onset of action within 12 hours after the first use in some patients with seasonal allergic rhinitis. However, the full benefit of the treatment cannot be obtained in the first 48 hours, so the patient must continue to use it regularly to achieve the full therapeutic effect.
For children aged 2–11 years, the recommended therapeutic dose is 1 injection (50 mcg) into each nostril 1 time per day (total daily dose - 100 mcg).
Treatment of patients with known seasonal allergic rhinitis should begin with prophylactic use of the preparation for 2–4 weeks prior to flowering season.
Adjunctive treatment for acute sinusitis. For adults (including the elderly) and children over the age of 12, the recommended therapeutic dose is 2 injections (50 mcg each) into each nostril 2 times a day (total daily dose - 400 mcg).
If the weakening of the symptoms of the disease cannot be achieved by using the preparation in the recommended therapeutic dose, the daily dose can be increased to 4 injections into each nostril 2 times a day (total daily dose - 800 mcg). After weakening the severity of the symptoms of the disease, a dose reduction is recommended.
Acute rhinosinusitis. For adults and children over the age of 12, the recommended therapeutic dose is 2 injections (50 mcg) into each nostril 2 times a day (total daily dose is 400 mcg).
Nasal polyps. For patients over the age of 18 (including the elderly), the recommended dose is 2 injections (50 mcg) into each nostril 2 times a day (total daily dose is 400 mcg). After achieving the clinical effect, it is recommended to reduce the dose to 2 injections into each nostril once a day (total daily dose - 200 mcg).
Hypersensitivity to one of the ingredients of the preparation. the presence of an untreated localized infection with lesions of the nasal mucosa. recent nose surgery or nasal trauma until the injury is completely healed.
During clinical studies with seasonal and year-round allergic rhinitis, the following side effects associated with the use of the preparation were noted: headache (8%), nosebleeds (that is, obvious bleeding, as well as the release of bloody mucus or blood clots) (8%), pharyngitis (4%), burning sensation in the nose (2%), irritation (2%) and ulcerative changes (1%) of the nasal mucosa, as well as upper respiratory tract infections. noted isolated cases of immediate hypersensitivity. the development of such undesirable phenomena is typical when using any nasal spray containing GCS. nosebleeds stopped spontaneously and were moderate, occurred somewhat more often than with placebo (5%), but less often than with other intranasal corticosteroids, which were studied and used as active control (when using some of them, the incidence of nosebleeds was up to 15%). the incidence of other adverse events was comparable to that with placebo.
In children, the incidence of adverse events, including nosebleeds (6%), headache (3%), nasal irritation (2%) and sneezing (2%), was comparable to that with placebo (4%) ...
After intranasal use of mometasone furoate, an immediate allergic reaction (eg, bronchospasm, shortness of breath) may sometimes occur. Very rarely, anaphylactic reaction and angioedema have occurred.
Isolated cases of disturbances in taste and olfactory sensations have been reported.
When using a nasal spray as an adjuvant for the treatment of acute episodes of sinusitis, adverse events were noted, the incidence of which was comparable to that with placebo: headache (2%), pharyngitis (1%), burning sensation in the nose (1%) and irritation of the nasal mucosa (1%). Nosebleeds were moderately pronounced and the frequency of their occurrence with the preparation was also comparable to the frequency of nosebleeds with placebo (5% and 4%, respectively).
In patients with nasal polyps, acute rhinosinusitis, when using the spray, the total number of the above adverse events was comparable to that when using placebo and similar to the amount that was observed in patients with allergic rhinitis.
Very rarely, with intranasal use of corticosteroids, cases of perforation of the nasal septum or increased intraocular pressure were noted.
The use of the preparation in young children should be carried out under supervision and with the help of adults.
When conducting placebo-controlled clinical studies, there was no growth retardation in children who received mometasone furoate at a dose of 100 μg for a year.
The preparation should not be used in the presence of untreated local infection with involvement of the nasal mucosa in the process.
Due to the fact that corticosteroids slow down wound healing, such preparations should not be prescribed for local intranasal use in patients who have recently undergone surgery or nasal trauma, until the wounds are completely healed.
The spray should be used with caution or not at all in patients with active or latent tuberculosis infection of the respiratory tract, as well as untreated fungal, bacterial, systemic viral infections or herpes simplex infections with eye damage.
After 12 months of treatment with Flix, there were no signs of atrophy of the nasal mucosa; in addition, mometasone furoate contributed to the normalization of the histological picture of the nasal mucosa. As with any long-term treatment, patients using the preparation for several months or longer should be periodically examined to identify possible changes in the nasal mucosa. In case of development of a local fungal infection of the nose or pharynx, it may be necessary to discontinue preparation therapy or conduct appropriate treatment. Irritation of the nasal and pharyngeal mucosa, which persists for a long time, may also be an indication for discontinuation of treatment.
With long-term therapy with Flix, no signs of suppression of the function of the hypothalamic-pituitary-adrenal system were observed. Patients who switch to nasal spray treatment after prolonged therapy with systemic corticosteroids require careful monitoring. Discontinuation of systemic corticosteroids in these patients may lead to insufficiency of adrenal cortex function, which may require the restoration of therapy with systemic corticosteroids and the use of other appropriate treatment.
When switching from therapy with systemic corticosteroids to treatment with a spray, in some patients, along with the relief of nasal symptoms, symptoms of corticosteroids cancellation may occur (for example, pain in joints and / or muscles, a feeling of fatigue and depression). Such patients need to be specially convinced of the advisability of continuing the spray treatment. A change in therapy may also reveal allergic diseases (such as allergic conjunctivitis, eczema, etc.) that developed earlier and were masked by systemic GCS therapy.
Patients using GCS can potentially have a reduced immune reactivity and should be warned about the increased risk of infection in case of contact with patients with certain infectious diseases (for example, chickenpox, measles), as well as the need to consult a doctor if such contact took place.
Patients should be warned to seek immediate medical attention if signs or symptoms of severe bacterial infection occur, such as fever, severe one-sided facial pain or toothache, orbital or periorbital swelling / edema, or worsening after initial improvement.
Controlled clinical studies have shown that intranasal corticosteroids can slow down the growth rate in children. It is necessary to monitor the growth rate of children taking intranasal corticosteroids. The effect of long-term treatment on growth, the clinical benefit obtained, and the safety and efficacy of alternative treatment with non-steroidal preparations should be evaluated. The depressing effect of the preparation on growth should not be ignored when treating sensitive patients and when using the preparation in high doses.
The ability to influence the reaction rate when driving vehicles or other mechanisms. There is no information on the effect on the ability to drive vehicles and work with mechanisms.
Application during pregnancy or lactation. The preparation belongs to category C of the use of preparations during pregnancy. Sufficient or well-controlled studies in pregnant women have not been conducted. Plasma concentrations of mometasone after intranasal administration of the maximum recommended clinical dose are not determined; thus, the impact on fetal development of the fetus is expected to be negligible and the potential for reproductive toxicity is expected to be very low.
As with other nasal corticosteroids, when deciding on the use of mometasone furoate spray in pregnant women, it is necessary to compare the potential risk to the fetus / infant with the expected benefit.
The preparation should not be used during pregnancy, unless absolutely necessary.
Children born to mothers who used GCS during pregnancy should be carefully examined for possible adrenal hypofunction.
It is not known whether mometasone passes into breast milk. Since it is known that other corticosteroids are excreted in breast milk, caution should be exercised when using the nasal spray of mometasone furoate.
When deciding to discontinue breastfeeding or preparation treatment, the benefits of breastfeeding for the baby and treatment with mometasone furoate for the mother should be considered.
Children. Not prescribed for children under 2 years of age. The safety and efficacy of the preparation in the treatment of nasal polyps in children (under the age of 18), symptoms of rhinosinusitis - under the age of 12, seasonal or perennial allergic rhinitis - in children under 2 years of age have not been investigated.
When using mometasone furoate in combination with loratadine, there was no pronounced effect on the concentration of loratadine and its main metabolite in blood plasma. the concentration of mometasone in blood plasma was not determined. the combination treatment was well tolerated by the patients.
Given the low (≤0.1%) systemic bioavailability of the preparation, it is unlikely that in case of an overdose, other measures will be required, besides monitoring the patient's condition, followed by the use of the preparation at the recommended dose.
Inhalation or ingestion of GCS in excessive doses can lead to suppression of the function of the hypothalamic-pituitary-adrenal system.
At a temperature not exceeding 25 ° c. do not freeze.
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