Nosefrine, spray 50 mcg/dose 18 g 120 doses

Pharmacotherapeutic group
Glucocorticosteroid for topical use.

TAC code
R01AD09

Pharmacological properties

Pharmacodynamics

Mometazon is a synthetic GCS for topical use. It has anti-inflammatory and anti-allergic effects when used in doses at which there are no systemic effects.

Inhibits the release of inflammatory mediators. It increases lipomodulin production, which is an inhibitor of phospholipase A, resulting in decreased release of arachidonic acid and, accordingly, inhibiting the synthesis of products of arachidonic acid metabolism – cyclic endoperoxides, PG. It prevents marginal accumulation of neutrophils, which reduces inflammatory exudate and lymphokine production, inhibits macrophage migration, leads to a decrease in infiltration and granulation processes.

It reduces inflammation due to decrease of chemotaxis substance formation (effect on delayed allergy reactions), inhibits development of immediate allergic reaction (caused by inhibition of arachidonic acid metabolites production and decrease of inflammatory mediators release from mast cells).

In studies with provocation tests with application of antigens on nasal mucosa high anti-inflammatory activity of mometasone was demonstrated both in early and in late stage of allergic reaction. This was confirmed by a decrease (compared to placebo) in the level of histamine and eosinophil activity, as well as a decrease (compared to baseline) in the number of eosinophils, neutrophils and epithelial cell adhesion proteins.

Pharmacokinetics

When administered intranasally, the systemic bioavailability of mometasone is less than 1% (with a sensitivity of 0.25 pg/mL determination method). The mometasone suspension is very poorly absorbed in the gastrointestinal tract, and the small amount of mometasone suspension that may enter the gastrointestinal tract after nasal inhalation is actively metabolized before excretion by the kidneys or with bile.

Indications

Sinusitis, Nasal Polyposis, Allergies, Pollinosis, Allergic Rhinitis

• Seasonal or year-round allergic rhinitis in adults, adolescents and children from 2 years old;
• acute sinusitis or exacerbation of chronic sinusitis in adults (including elderly.
• acute rhinosinusitis with mild to moderate symptoms without signs of severe bacterial infection in adults (including elderly) and teenagers from 12 years of age as part of complex therapy
• acute rhinosinusitis with mild to moderate symptoms without signs of severe bacterial infection in patients aged 12 years and olderprophylactic treatment of moderate to severe seasonal allergic rhinitis in adults and adolescents from 12 years of age (recommended 2-4 weeks before the anticipated start of the dusting season);
• Nasal polyposis accompanied by nasal breathing and olfactory disturbances in adults (from 18 years of age).

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Active ingredient

Mometazone

Composition

1 dose contains:
active ingredient: mometasone furoate – 50 micrograms;
excipients: microcrystalline cellulose and sodium carboxymethylcellulose – 2000 µg, glycerol – 2100 µg, citric acid monohydrate – 200 µg, sodium citrate dihydrate – 280 µg, polysorbate 80 – 10 µg, benzalkonium chloride (50 % solution) – 40 µg, purified water – to 0.1 g.

How to take, the dosage

Intranasally. The suspension in the bottle is injected using a special dispensing nozzle on the bottle.

Tilt your head and inject into each nasal passage as recommended by your doctor.

Before the nasal spray is used for the first time, it needs to be “calibrated” by pressing the dosing tip 6-7 times, after which time the stereo dose is set at 0.1 g of suspension (50 mcg of mometasone).

If the spray has not been used for 14 days or more, a re-calibration is necessary.

Shake the bottle vigorously before each use.

Treatment of seasonal or year-round allergic rhinitis

Adults (including the elderly) and adolescents from 12 years:

The recommended prophylactic and therapeutic dose of the drug is 2 injections (50 µg of mometasone furoate each) into each nasal passage once daily (daily dose is 200 µg). Once the therapeutic effect for maintenance therapy is achieved, it is possible to reduce the dose to 1 injection in each nasal passage once a day (daily dose – 100 mcg).

If reduction of symptoms is not achieved by using the drug in the recommended therapeutic dose, the daily dose can be increased to 4 injections into each nasal passage once daily (daily dose is 400 mcg).

Dose reduction is recommended once symptoms have decreased.

The onset of action of the drug is usually seen clinically as early as 12 hours after the first use of the drug.

Children 2-11 years of age:

The recommended therapeutic dose is 1 injection (50 mcg of mometasone furoate) in each nasal passage once daily (daily dose 100 mcg).

You may need the help of an adult to use in children.

Auxiliary treatment for acute sinusitis or exacerbation of chronic sinusitis

Adults (including the elderly) and adolescents from 12 years of age:

The recommended therapeutic dose is 2 injections (50 µg of mometasone furoate each) into each nasal passage 2 times a day (daily dose is 400 µg).

If reduction of symptoms is not achieved by using the drug in the recommended therapeutic dose, the daily dose may be increased to 4 injections into each nasal passage 2 times daily (the total daily dose is 800 mcg).

Dose reduction is recommended once symptoms have decreased.

Treatment of acute rhinosinusitis without signs of severe bacterial infection

The recommended therapeutic dose of the drug for adults and adolescents from 12 years is 2 injections (50 µg of mometasone furoate) in each nasal passage 2 times daily (daily dose – 400 µg). If symptoms worsen during treatment, specialist consultation is necessary.

Treatment of nasal polyposis

Adults (including the elderly) from 18 years of age:

The recommended therapeutic dose of the drug is 2 injections (50 µg of mometasone furoate each) into each nasal passage 2 times a day (daily dose is 400 µg).

After reduction of symptoms, it is recommended that the dose be reduced to 2 injections (50 mcg of mometasone furoate each) in each nasal passage once daily (daily dose is 200 mcg).

Interaction

Combination therapy with loratadine was well tolerated by patients. No effect of the drug on plasma concentrations of loratadine or its major metabolite was observed. In these studies, mometasone furoate was not detected in plasma (with a sensitivity of 50 pg/ml detection method). Mometasone furoate is metabolized by CYP3A4. Co-administration with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, medicinal products containing cobicistat) may lead to increased glucocorticosteroid plasma concentrations and possibly to an increased risk of systemic side effects of glucocorticosteroid therapy. The benefits of co-administration of mometazone furoate with strong CYP3A4 inhibitors and the potential risk of systemic side effects of glucocorticosteroids should be assessed. Patients should be monitored for systemic side effects of glucocorticosteroid therapy if the drugs are coadministered.

Special Instructions

As with any long-term treatment, patients using mometazone nasal spray for months or longer should be periodically evaluated by a physician for possible nasal mucosal changes. Patients receiving intranasal GCS for long periods of time should be monitored.

The development of growth retardation in children is possible. If growth retardation in children is detected, the dose of intranasal GCS should be reduced to the lowest dose that effectively controls symptoms. In addition, the patient should be referred to a pediatrician for consultation.

If a local fungal infection of the nose or pharynx develops, discontinuation of nasal spray therapy and specific treatment may be necessary. Persistent irritation of the mucous membranes of the nose and pharynx over a long period of time may also be a reason to discontinue treatment with the drug.

In placebo-controlled clinical studies in children when mometasone nasal spray was used in a daily dose of 100 mcg for one year, no growth retardation was observed in children.

There was no evidence of suppression of GGNS function with prolonged treatment with mometasone nasal spray. Patients who switch to treatment with the drug after long-term therapy with systemic GCS require special attention. Withdrawal of systemic GCS in such patients may lead to insufficiency of adrenal function, subsequent recovery of which may take up to several months. If signs of adrenal insufficiency occur, systemic hormones should be restarted and other appropriate measures taken.

The use of intranasal GCS may result in systemic side effects, especially with long-term use at high doses. The likelihood of these effects is significantly less than with oral GCS. Systemic side effects may vary both in individual patients and depending on the GCS drug used. Potential systemic effects include Cushing’s syndrome, characteristic cushingoid signs, suppression of adrenal function, growth retardation in children and adolescents, cataracts, glaucoma, and less commonly, a number of psychological or behavioral effects including psychomotor hyperactivity, sleep disturbance, anxiety, depression or aggression (especially in children).

During the transition from systemic GCS treatment to drug treatment, some patients may experience initial withdrawal symptoms from systemic GCS (e.g., joint and/or muscle pain, fatigue, and depression) despite a reduction in the severity of symptoms associated with nasal mucosal lesions. Such patients should be specifically persuaded to continue treatment with the drug. Switching from systemic to topical GCS may also reveal pre-existing allergic diseases, such as allergic conjunctivitis and eczema, masked by systemic GCS therapy.

Patients treated with GCS have potentially compromised immune reactivity and should be advised of their increased risk of exposure to certain infectious diseases (e.g., chickenpox, measles) and the need for medical consultation if this occurs. If there are signs of a significant bacterial infection (e.g., fever, persistent and severe pain on one side of the face or toothache, swelling of the orbital or periorbital area), immediate medical consultation is needed.

There were no signs of nasal mucosal atrophy when using mometasone intranasal spray for 12 months. In addition, mometasone furoate tended to promote normalization of the histologic picture on examination of nasal mucosal biopsy specimens.

With systemic and topical (including intranasal, inhalation, and intraocular) use of GCS, visual disturbances may occur. If symptoms such as blurred vision or other visual disturbances are present, the patient should be advised to see an ophthalmologist for possible causes of visual disturbances, including cataracts, glaucoma or rare conditions such as central serous chorioretinopathy, which have been seen in some cases with systemic and topical use of GCS.

The efficacy and safety of mometasone has not been studied in the treatment of unilateral polyps, polyps associated with cystic fibrosis, and polyps that completely cover the nasal cavity. If unilateral polyps of unusual or irregular shape, particularly ulcerated or bleeding polyps, are found, further medical evaluation should be performed.

Influence on ability to drive vehicles, machinery

As visual impairment has been reported in patients receiving the drug, patients should exercise caution before driving vehicles and machinery.

Contraindications

• hypersensitivity to mometazon or to any of the ingredients of the drug;
• Nasal surgery or trauma with nasal mucosa damage – until the wound healing (due to the inhibitory effect of GCS on healing processes);
• childhood (in seasonal and year-round allergic rhinitis – under 2 years, in acute sinusitis or exacerbation of chronic sinusitis – under 12 years, in
  polyposis – under 18 years) due to the lack of relevant data.

With caution

• Tuberculosis infection (active or latent) of the respiratory tract;
• untreated local infection with involvement of the nasal mucosa.

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Side effects

The use of the drug in clinical trials

The adverse events associated with the use of mometasone (>1%) identified in clinical trials in patients with allergic rhinitis or nasal polyposis and during post-registration use of the drug, regardless of indication, are presented in Table 1. Adverse reactions are listed according to the MedDRA system-organ classifications. Within each system-organ class, adverse reactions are classified by frequency of occurrence.

Nasal bleeding was generally moderate and stopped on its own. Their incidence was slightly higher than with placebo (5%), but equal to or lower than with other intranasal GCSs used as active controls (some had incidence rates of up to 15%).

The incidence of all other adverse events was comparable to that of placebo administration. The overall incidence of adverse events in patients treated for nasal polyposis was comparable to the incidence in patients with allergic rhinitis.

The overall incidence of adverse events in patients treated for acute rhinosinusitis was comparable to the incidence in patients with allergic rhinitis and when given placebo. When using intranasal GCS, systemic side effects may develop, especially with long-term use of high-dose intranasal GCS (see “Special Precautions”).

Table 1

The frequency of adverse reactions is set as follows: very common (≥1/10); common (≥1/100, < 1/10); rare (≥1/1000, < 1/100). For adverse reactions during post-registration follow-up, the frequency has not been determined (cannot be determined on the basis of available data).

*See with frequency “rare” when using the drug twice daily for nasal polyposis.

**Discovered when using the drug 2 times daily for nasal polyposis.

Children

Injuries to the respiratory system, thoracic and mediastinal organs:

Nasal bleeding (6%), nasal mucous membrane irritation (2%), sneezing (2%).

Nervous system disorders:headache (3%).

The incidence of these adverse events in children was comparable to that of placebo.

Post-registration use of the drug

In post-registration use of mometazone nasal spray, additional adverse reactions were noted: blurred vision.

Overdose

Symptoms
Suppression of hypothalamic-pituitary-adrenal system function (may occur in case of long-term use of high-dose GCS, as well as in case of simultaneous use of several GCS).
Treatment
Due to low systemic bioavailability of the drug (less than 1% at the sensitivity level of 0.25 pg/ml), it is unlikely that in case of accidental or intentional overdose any measures will be required aside from monitoring with possible resumption of therapy in recommended dose. If necessary, treatment is symptomatic.

Pregnancy use

Appropriately designed and well-controlled studies of the drug in pregnant women have not been conducted. As with other nasal GCSs, mometasone should be used during pregnancy and breastfeeding only if the expected benefit to the mother outweighs the potential risk to the fetus or neonate. Newborns whose mothers have used mometasone during pregnancy should be closely monitored for the possibility of developing adrenal hypofunction.

Similarities

Desrinit spray, Momat Rhino, Mometazone, Rialtris, Momeyd