Forinex nasal spray 50 mcg/dose, 140 doses — Made in Ukraine — Free Delivery

Pharmacological properties

Pharmacodynamics.

Mometasone furoate is a synthetic topical corticosteroid that has a pronounced anti-inflammatory effect. The local anti-inflammatory effect of mometasone furoate is manifested at doses at which no systemic effects occur.

Basically, the mechanism of anti-inflammatory and anti-allergic action of mometasone furoate is associated with its ability to inhibit 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 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 IL-5 production.

In studies with provocative tests with the application of antigens to the nasal mucosa, a high anti-inflammatory activity of the aqueous nasal spray of mometasone furoate was found both in the early and in the late stages of the 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 the initial level) in the number of eosinophils, neutrophils and adhesion proteins of epithelial cells.

A pronounced clinical effect was achieved in 28% of patients with seasonal allergic rhinitis in the first 12 hours of application of an aqueous nasal spray of mometasone furoate. On average (50%) relief occurred within 35.9 hours. In addition, mometasone furoate was significantly effective in reducing the severity of eye symptoms (redness, lacrimation, itching) in patients with seasonal allergic rhinitis.

In clinical studies involving patients with nasal polyps, mometasone furoate spray has shown significant clinical efficacy in restoring nasal breathing, reducing the size of polyps, and renewing the sense of smell compared to placebo.

In clinical studies involving patients over the age of 12 years, mometasone furoate nasal spray 200 μg 2 times a day has been shown to be highly effective in reducing the severity of rhinosinusitis symptoms compared with placebo. During 15 days of treatment, the symptoms of rhinosinusitis were assessed on the scale of the severity of symptoms (Major Symptom Score - MSS) (pain in the face, feeling of pressure in the paranasal sinuses, pain on pressure, pain in the paranasal sinuses, rhinorrhea, runoff of mucus on the back wall throat and nasal congestion). The efficacy of amoxicillin 500 mg 3 times a day did not differ significantly from placebo in terms of reducing the severity of rhinosinusitis symptoms 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 amoxicillin and placebo group. The duration of treatment for acute rhinosinusitis for 15 days has not been evaluated.

Pharmacokinetics.

The bioavailability of mometasone furoate when used in the form of a nasal spray is 1% in blood plasma (according to data obtained using a sensitive method, the lower limit of quantitative determination is 0.25 pg / ml). Suspension of mometasone furoate is very poorly absorbed from the gastrointestinal tract, and the small amount that can be swallowed and absorbed lends itself to active primary metabolism even before excretion, mainly in the form of metabolites with bile and, to some extent, with urine.

Indications

Treatment of seasonal or perennial allergic rhinitis in adults and children 2 years of age. It is recommended to start prophylactic treatment of moderate to severe allergic rhinitis 4 weeks before the expected start of the dusting season. as an auxiliary therapeutic agent in the antibiotic treatment of acute episodes of sinusitis in adults (including the elderly) and children over the age of 12 years.

Treatment of symptoms of acute rhinosinusitis without signs of severe bacterial infection in adults and children over the age of 12.

Treatment of nasal polyps and related symptoms, including nasal congestion and loss of smell, in patients over the age of 18.

Application

Before using a new vial of the preparation, it should be calibrated. the calibration is carried out by approximately 10 pushes of the dosing device, during which a stereotyped delivery of the preparation is established, in which approximately 100 mg of a suspension containing 50 μg of mometasone (one dose) is released with each press. if the nasal spray has not been used for ≥14 days, re-spray 2 times before the next use until a full delivery is observed. do not pierce the tip before using.

Shake the bottle vigorously before each use.

If the nozzle is clogged, it is necessary to remove the plastic cap by gently pressing on the white ring, easily remove the nozzle and rinse it with warm running water, dry it and reinstall it. Do not try to clean the nozzle with a needle or other sharp object, as doing so will damage the dispenser.

Regular cleaning of the brush head is very important.

Before each use, thoroughly cleanse the nose of mucus.

Treatment of seasonal or year-round allergic rhinitis: for adults (including the elderly) and children over the age of 12, the recommended prophylactic and therapeutic dose of the preparation is 2 injections (50 μg each) into each nasal passage 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 in each nasal passage once a 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 nasal passage once a day (total daily dose - 400 mcg). After the symptoms of the disease have subsided, 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 effect of the treatment cannot be obtained in the first 48 hours, therefore, 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 nasal passage once a day (total daily dose - 100 mcg).

Adjunctive treatment of acute episodes of sinusitis. For adults (including the elderly) and children over the age of 12 years, the recommended therapeutic dose is 2 injections (50 mcg each) into each nasal passage 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 nasal passage 2 times a day (total daily dose - 800 mcg). After the symptoms of the disease have subsided, a dose reduction is recommended.

Acute rhinosinusitis. For adults and children 12 years old, the recommended therapeutic dose is 2 injections (50 mcg each) into each nasal passage 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 each) into each nasal passage 2 times a day (total daily dose - 400 mcg). After achieving the clinical effect, it is recommended to reduce the dose to 2 injections into each nasal passage once a day (total daily dose - 200 mcg).

Contraindications

Hypersensitivity to the active substance or to any inactive component of the preparation.

The preparation should not be used in the presence of untreated localized infection involving the nasal mucosa.

Because corticosteroids have the effect of inhibiting wound healing, patients who have recently had nasal surgery or who have been injured should not be given a nasal corticosteroid until healing has taken place.

Side effects

During clinical studies with seasonal and year-round allergic rhinitis, such undesirable phenomena associated with the use of the preparation mometasone furoate in the form of a nasal spray 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. the development of such adverse events is typical with the use of any nasal spray containing corticosteroids. nosebleeds stopped on their own 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 (in some of them the incidence of nosebleeds was up to 15%). the incidence of other adverse reactions was comparable to that with placebo.

In children, the incidence of adverse reactions, including nosebleeds (6%), headache (3%), nasal irritation (2%) and sneezing (2%), was comparable to that with placebo.

After intranasal use of mometasone furoate, an immediate allergic reaction (for example, bronchospasm, dyspnea) can sometimes occur. Very rarely, anaphylactic reaction and angioedema have occurred.

Isolated cases of taste and smell disorders have been reported.

When using mometasone furoate nasal spray as an adjuvant in the treatment of acute episodes of sinusitis, such adverse events were noted, the frequency of which is comparable to that of placebo: headache (2%), pharyngitis (1%), burning sensation in the nose (1%) and irritation of the nasal mucosa (1%). Nosebleeds were moderately pronounced, and their incidence with mometasone furoate spray was also comparable to the incidence of nosebleeds with placebo (5% and 4%, respectively).

In patients with nasal polyps, acute rhinosinusitis, when using a spray of mometasone furoate, 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.

The occurrence of an upper respiratory tract infection was observed in 1% of patients who used mometasone furoate for the treatment of nasal polyps, which was comparable to the placebo group.

Very rarely, with intranasal use of corticosteroids, there have been cases of perforation of the nasal septum or increased intraocular pressure.

Rare cases of glaucoma and / or cataracts have been reported with the use of intranasal corticosteroids.

Special instructions

The use of the preparation in young children should be carried out with the help of adults.

The preparation Forinex 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 in case of Herpes simplex infection with eye damage.

After 12 months of treatment with mometasone furoate, 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 who use the preparation for several months or longer need to be periodically examined to identify possible changes in the nasal mucosa. If a local fungal infection of the nose or pharynx develops, 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 preparation treatment.

Although the preparation controls nasal symptoms in most patients, the concomitant use of appropriate adjunctive therapy may reduce the severity of other symptoms, in particular eye symptoms.

With long-term treatment with mometasone furoatom, signs of suppression of the function of the hypothalamic-pituitary-adrenal system were not observed. Patients who switch to nasal spray treatment after prolonged therapy with systemic corticosteroids should be closely monitored. Discontinuation of systemic corticosteroids in such patients may lead to adrenal insufficiency, which may require resumption of systemic corticosteroid therapy and other appropriate treatment.

During the transition from treatment with systemic corticosteroids to treatment with Forinex, some patients, along with a decrease in the severity of nasal symptoms, may experience corticosteroid withdrawal symptoms (for example, joint and / or muscle pain, fatigue and depression). Such patients need to be convinced of the advisability of continuing the spray treatment. Changes in therapy may also reveal allergic diseases (such as allergic conjunctivitis, eczema) that developed earlier and were masked by systemic corticosteroid therapy.

Patients who use corticosteroids can potentially have a reduced immune reactivity, and they should be warned about the increased risk of infection when they come into contact with patients with certain infectious diseases (for example, chickenpox, measles), as well as the need to consult a doctor if such contact occurs.

The potential risk of developing Cushing's syndrome can arise with long-term use of preparations in high doses.

After the use of intranasal corticosteroids, cases of perforation of the nasal septum or increased intraocular pressure have been reported very rarely.

During placebo-controlled clinical studies in children in whom mometasone furoate was used in a daily dose of 100 μg for 1 year, growth retardation was not observed.

Patients should be warned about the need for immediate medical attention in case of symptoms of a severe bacterial infection, such as fever, severe unilateral facial pain or toothache, orbital or periorbital swelling / edema, worsening after initial improvement.

The preparation contains benzalkonium chloride, which can cause bronchospasm.

Application during pregnancy or lactation.

Special studies of the effect of the preparation in pregnant women have not been conducted.

Like other intranasal corticosteroids, Forinex can be used in pregnant and breastfeeding women only if the expected benefit justifies the potential risk to the mother, fetus or infant. Infants whose mothers have used corticosteroids during pregnancy should be carefully examined for possible adrenal hypofunction.

Children.

During placebo-controlled clinical studies in children who received mometasone furoate in a daily dose of 100 μg for a year, no growth retardation was observed.

The safety and efficacy of mometasone furoate has not been investigated in the treatment of nasal polyps in children and adolescents over the age of 18, symptoms of rhinosinusitis in children over 12 years of age, seasonal or perennial allergic rhinitis in children over 2 years of age.

The ability to influence the reaction rate when driving vehicles or other mechanisms. Unknown.

Interactions

With the simultaneous use of mometasone furoate with loratadine, there was no effect on the plasma concentration of loratadine or its main metabolite, and mometasone furoate was not detected in blood plasma even at a minimum concentration. the combination therapy was well tolerated by the patients.

Data on interactions with other preparations are not presented.

Overdose

Since the systemic bioavailability of the preparation  is 1% (according to the results of the sensitive method, the lower limit of quantitative determination is 0.25 pg / ml), it is unlikely that in case of an overdose, other measures will be necessary, except for monitoring the patient's condition, followed by the use of the preparation at the recommended dose.

Inhalation or oral administration of excessive doses of corticosteroids can lead to suppression of the function of the hypothalamic-pituitary-adrenal system.

Storage conditions

Store in original packaging at a temperature not exceeding 25 ºС. do not freeze.