Nasonex^® allergy (Spray) Instructions for Use

Marketing Authorization Holder

Organon, LLC (Russia)

Manufactured By

Organon Heist, BV (Belgium)

Packaging and Quality Control Release

SCHERING-PLOUGH LABO, N.V. (Belgium)

Or

AKRIKHIN Chemical and Pharmaceutical Plant, JSC (Russia)

Contact Information

ORGANON LLC (Russia)

ATC Code

R01AD09 (Mometasone)

Active Substance

Mometasone (Rec.INN registered by WHO)

Dosage Form

Nasonex® allergy

Dosed nasal spray 50 µg/dose: 10 g or 18 g bottle

Dosage Form, Packaging, and Composition

Dosed nasal spray in the form of a white or almost white suspension.

Excipients: dispersed cellulose 65 cps – 20 mg, glycerol – 21 mg, citric acid monohydrate – 2 mg, sodium citrate dihydrate – 2.8 mg, polysorbate 80 – 0.1 mg, benzalkonium chloride – 0.2 mg (as a 50% solution – 0.4 mg), purified water – q.s. to 1 g.

10 g (60 doses) – high-density polyethylene bottles (1) complete with a dosing device – cardboard packs.
18 g (120 doses) – high-density polyethylene bottles (1) complete with a dosing device – cardboard packs.

Clinical-Pharmacological Group

Intranasal corticosteroids

Pharmacotherapeutic Group

Topical glucocorticosteroid

Pharmacological Action

Pharmacodynamics

Mometasone is a synthetic topical glucocorticosteroid. It has anti-inflammatory and anti-allergic effects when used in doses that do not cause systemic effects. Mometasone inhibits the release of inflammatory mediators and increases the production of lipomodulin, which is an inhibitor of phospholipase A, which leads to a decrease in the release of arachidonic acid and, accordingly, inhibition of the synthesis of arachidonic acid metabolites – cyclic endoperoxides, prostaglandins. Mometasone prevents the marginal accumulation of neutrophils, which reduces inflammatory exudate and the production of lymphokines, inhibits macrophage migration, and leads to a reduction in infiltration and granulation processes.

Mometasone reduces inflammation by reducing the formation of chemotaxis substance (effect on the “late” phase of the allergic reaction), inhibits the development of an immediate-type allergic reaction (due to inhibition of the production of arachidonic acid metabolites and a decrease in the release of inflammatory mediators from mast cells).

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

Pharmacokinetics

With intranasal use, mometasone furoate has low systemic bioavailability <1% (with a method sensitivity of 0.25 pg/ml). The mometasone suspension is very poorly absorbed in the gastrointestinal tract, and the small amount of the mometasone suspension that may enter the gastrointestinal tract after spraying into the nasal passage undergoes active primary metabolism before being excreted in urine or bile.

Indications

• Treatment of seasonal and perennial allergic rhinitis in adults aged 18 years and older (relief of symptoms such as nasal congestion, runny nose, sneezing, nasal itching, watery eyes).

ICD codes

Dosage Regimen

The drug is intended for intranasal use.

The drug should be used only according to the indications, method of application, and doses specified in the instructions. If after 14 days of treatment there is no improvement, or the symptoms worsen, or new symptoms appear, the patient should immediately consult a doctor. Without consulting a doctor, the drug Nasonex^® allergy should not be used for more than 3 consecutive months.

The spraying of the suspension contained in the bottle is carried out using a special dosing nozzle on the bottle.

Treatment of seasonal or perennial allergic rhinitis in adults

The recommended dose of the drug for the treatment of seasonal or perennial allergic rhinitis is 2 sprays (50 µg of mometasone furoate each) into each nostril once a day (total daily dose – 200 µg). After achieving the therapeutic effect, for maintenance therapy, it is possible to reduce the dose to 1 spray into each nostril once a day (total daily dose – 100 µg).

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

Recommendations for patients on the use of the drug

Before the first use of the drug Nasonex^® allergy, it is necessary to “calibrate” it. Do not pierce the nasal applicator.

If the drug has not been used for 14 days or longer, it is necessary to press the dosing nozzle twice or until a uniform spray appears.

1. Before using the drug, it is necessary to clear the nasal passages.
2. Gently shake the bottle before each use, then remove the cap from the nasal applicator.
3. Before the first use of the drug Nasonex^® allergy, “calibrate” it. To do this, press the shoulders of the white nasal applicator with your index and middle fingers, while holding the bottom of the bottle with your thumb.
4. The nostril into which the drug will not be administered should be closed with a finger, and the applicator should be inserted into the other nostril. Then tilt your head slightly forward so that the bottle is in a vertical position.
5. Inhale lightly through the nose and simultaneously press the nasal applicator once and spray a dose of the drug.
6. Exhale through the mouth.

When re-administering the drug into the same nostril, repeat the actions described in points 5-6.

To spray the drug into the other nostril, repeat steps 4-6.

After using the drug, wipe the top of the applicator with a clean tissue and put the cap on the dosing nozzle.

Cleaning the dosing nozzle

It is important to clean the dosing nozzle regularly, otherwise it may not work properly. It is necessary to remove the cap that protects the nozzle from dust, then carefully remove the spray tip. Wash the spray tip and the dust protection cap in warm water and rinse under the tap.

Do not attempt to open the nasal applicator with a needle or other sharp object, as this will damage the applicator, resulting in the risk of receiving an incorrect dose of the drug.

Dry the cap and tip in a warm place. After that, attach the spray tip to the bottle and screw the dust protection cap back onto the bottle. When using the drug for the first time after cleaning the dosing nozzle, it is necessary to re-“calibrate” by pressing the dosing nozzle twice.

Adverse Reactions

Use of the drug in clinical studies

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

Nosebleeds were generally moderate and self-limiting, their incidence was somewhat higher than with placebo (5%), but equal to or lower than with other intranasal glucocorticosteroids used as active controls (some of them had an incidence of nosebleeds up to 15%). The incidence of all other adverse reactions was comparable to the incidence with placebo.

When using intranasal glucocorticosteroids, systemic side effects may develop, especially with long-term use of intranasal glucocorticosteroids in high doses (see the “Special Precautions” section).

Table 1

The frequency of adverse reactions is defined as follows: very common (≥1/10); common (≥1/100, <1/10); uncommon (≥1/1000, <1/100).

For adverse reactions from the post-marketing surveillance period, the frequency is not established (cannot be estimated from the available data).

* Identified with “uncommon” frequency when using the drug twice a day for nasal polyposis.

** Identified when using the drug twice a day for nasal polyposis.

Contraindications

• Hypersensitivity to mometasone furoate or to any of the excipients included in the drug;
• The presence of an untreated local infection involving the nasal mucosa, for example, caused by Herpes simplex;
• Recent surgery or nasal trauma with damage to the nasal mucosa – until the wound has healed (due to the inhibitory effect of glucocorticosteroids on healing processes);
• Children under 18 years of age.

With caution

The drug Nasonex^® allergy should be used with caution in tuberculosis infection (active or latent) of the respiratory tract, untreated fungal, bacterial, systemic viral infection (as an exception, the drug may be prescribed for the listed infections as directed by a doctor).

Use in Pregnancy and Lactation

It is necessary to consult a doctor before using the drug Nasonex^® allergy during pregnancy and breastfeeding.

Pregnancy

Information regarding the use of mometasone furoate in pregnant women is absent or limited. Studies in animals have demonstrated reproductive toxicity. Like other intranasal glucocorticosteroids, the drug Nasonex^® allergy should be used during pregnancy only if the expected benefit of its use justifies the potential risk to the mother, fetus, or infant. Infants whose mothers used glucocorticosteroids during pregnancy should be carefully examined for the possibility of developing hypoadrenalism.

Breastfeeding period

It is not known whether mometasone furoate is excreted in breast milk. As with other intranasal glucocorticosteroids, a decision should be made to discontinue breastfeeding or to discontinue/abstain from therapy with Nasonex^® allergy, taking into account the benefit of breastfeeding for the child and the benefit of treatment for the woman.

Fertility

There are no clinical data on the effect of mometasone furoate on fertility. Animal studies have demonstrated reproductive toxicity but have not revealed an effect on fertility.

Pediatric Use

Contraindicated for use in children under 18 years of age.

Special Precautions

The drug is indicated for intranasal use only.

The drug Nasonex^® allergy should not be used for more than 3 consecutive months. If it is necessary to use the drug for more than 3 consecutive months, a doctor’s consultation is required.

As with any long-term treatment, patients using the drug Nasonex^® allergy for several months or longer should be periodically examined by a doctor for possible changes in the nasal mucosa. Patients receiving intranasal glucocorticosteroids for a long time should be monitored.

If a local fungal infection of the nose or pharynx develops, it may be necessary to discontinue therapy with the drug Nasonex^® allergy and carry out appropriate treatment. Persistent irritation of the nasal and pharyngeal mucosa may also be a reason to discontinue treatment with the drug Nasonex^® allergy.

No signs of suppression of the hypothalamic-pituitary-adrenal system function were observed during long-term treatment with mometasone nasal spray. Patients who switch to treatment with the drug Nasonex^® allergy after long-term therapy with systemic glucocorticosteroids require special attention. Withdrawal of systemic glucocorticosteroids in such patients may lead to adrenal insufficiency, the subsequent recovery from which may take up to several months. If signs of adrenal insufficiency appear, systemic glucocorticosteroids should be resumed and other necessary measures taken.

The use of the drug Nasonex^® allergy is not recommended in case of nasal septum perforation (see the “Adverse Reactions” section).

In clinical studies, nosebleeds were observed more frequently compared to placebo. Nosebleeds were self-limiting and moderate (see the “Adverse Reactions” section).

The drug Nasonex^® allergy contains benzalkonium chloride, which may cause irritation of the nasal mucosa.

Systemic side effects may vary between individual patients and depending on the glucocorticoid drug used. Potential systemic effects include Cushing’s syndrome, cushingoid features, adrenal suppression, cataract, glaucoma, and, less commonly, a range of psychological or behavioral effects, including psychomotor hyperactivity, sleep disturbance, anxiety, depression, or aggression.

Cases of increased intraocular pressure have been reported after the use of intranasal glucocorticosteroids (see the “Adverse Reactions” section).

Visual disturbances may occur with systemic and local (including intranasal, inhaled, and intraocular) use of glucocorticosteroids. If a patient has symptoms such as blurred vision or other visual disturbances, it is necessary to recommend that the patient consult an ophthalmologist to identify possible causes of visual disturbances, including cataract, glaucoma, or rare conditions, such as central serous chorioretinopathy, which have been observed in a number of cases with systemic and local use of glucocorticosteroids.

During the transition from treatment with systemic glucocorticosteroids to treatment with the drug Nasonex^® allergy, some patients may experience initial symptoms of withdrawal of systemic glucocorticosteroids (for example, joint and/or muscle pain, feeling of fatigue, and depression), despite a decrease in the severity of symptoms associated with nasal mucosa damage. Such patients need to be specifically convinced of the advisability of continuing treatment with the drug Nasonex^® allergy. The transition from systemic to local glucocorticosteroids may also reveal pre-existing but masked by systemic glucocorticosteroid therapy allergic diseases, such as allergic conjunctivitis and eczema. Treatment with higher doses than recommended may lead to clinically significant suppression of adrenal function. If higher doses than recommended have been used, the patient should consult a doctor.

Patients undergoing treatment with glucocorticosteroids have potentially reduced immune reactivity and should be warned about their increased risk of infection in case of contact with patients with certain infectious diseases (for example, chickenpox, measles), and about the need for medical consultation if such contact occurs.

No signs of nasal mucosal atrophy occurred during the use of mometasone nasal spray for 12 months. Furthermore, mometasone furoate tended to promote normalization of the histological picture when examining nasal mucosal biopsies.

Effect on the ability to drive vehicles and operate machinery

There are no data on the effect of the drug Nasonex^® allergy on the ability to drive vehicles or operate machinery.

Overdose

With long-term use of glucocorticosteroids in high doses, as well as with the simultaneous use of several glucocorticosteroids, suppression of the hypothalamic-pituitary-adrenal system function is possible. Due to the low systemic bioavailability of the drug (<1%, with a method sensitivity of 0.25 pg/ml), it is unlikely that any measures other than observation with possible subsequent resumption of the drug at the recommended dose will be required in case of accidental or intentional overdose. In case of overdose, the patient should consult a doctor.

Drug Interactions

Clinical studies on interaction with loratadine have been conducted. No interaction was observed.

Concomitant use with CYP3A inhibitors, including drugs containing cobicistat, is expected to increase the risk of systemic side effects. The physician should evaluate the benefits of co-administering mometasone furoate with strong CYP3A4 inhibitors and the potential risk of developing systemic corticosteroid side effects. Concomitant use of these drugs should be avoided, except in cases where the potential benefit to the patient outweighs the increased risk of systemic corticosteroid side effects, and in this case, the patient’s condition should be monitored for the development of systemic side effects of glucocorticoid therapy.

If the patient is taking the above-mentioned drugs or other medications (including over-the-counter ones), it is necessary to consult a doctor before using Nasonex^® allergy.

Storage Conditions

The drug should be stored out of the reach of children at a temperature not exceeding 25°C (77°F). Do not freeze.

Shelf Life

Shelf life is 2 years. Do not use after the expiration date.

Dispensing Status

The drug is available without a prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.