Nasonex, spray 50 mcg/dose 60 doses

Nasonex is an anti-allergic, anti-inflammatory.

Pharmacodynamics

Mometasone furoate is a synthetic glucocorticosteroid for topical use. It has anti-inflammatory and anti-allergic effects when used in doses at which there are no systemic effects. It inhibits release of inflammatory mediators, increases production of lipomodulin, which is an inhibitor of phospholipase A, which causes reduction of release of arachidonic acid and, accordingly, inhibition of synthesis of products of arachidonic acid metabolism – cyclic endoperoxides, PG. Prevents marginal accumulation of neutrophils, reduces inflammatory exudate and lymphokine production, inhibits macrophage migration, leads to a decrease in infiltration and granulation processes. It reduces inflammation due to decrease in formation of chemotaxis substance (effect on “late” allergic reactions) and inhibits development of “immediate” allergic reaction (conditioned by inhibition of production of arachidonic acid metabolites and decrease in release of inflammatory mediators from mast cells).

. In studies with provocation tests with application of antigens to the nasal mucosa high anti-inflammatory activity of Nasonex was demonstrated both in the early and late stages of the allergic reaction, which was confirmed by reduction (compared to placebo) of histamine and eosinophil activity as well as reduction (compared to baseline) of eosinophil, neutrophil and epithelial cell adhesion proteins.

Pharmacokinetics

The bioavailability of mometasone furoate is negligible (≤0.1%) and it is almost not detected in plasma when given by intranasal inhalation (even when using the sensitive 50 pg/ml sensitivity threshold method). Therefore, there are no relevant pharmacokinetic data for this dosage form. The suspension is very poorly absorbed from the gastrointestinal tract, so the small amount that may enter the gastrointestinal tract after inhalation into the nasal cavity is still undergoing active primary metabolism before excretion with urine or bile.

Indications

– Seasonal and year-round allergic rhinitis in adult adolescents and children from 2 years of age.
– Acute sinusitis or exacerbation of chronic sinusitis in adults (including the elderly) and adolescents over 12 years of age – as an auxiliary therapeutic agent in antibiotic treatment.
– Acute rhinosinusitis with mild to moderate symptoms without signs of severe bacterial infection in patients 12 years of age or older.
– Preventive treatment of moderate and severe seasonal allergic rhinitis in adults and adolescents from 12 years of age (recommended two to four weeks before the expected start of the dust season).
– Nasal polyposis accompanied by impaired nasal breathing and sense of smell in adults (over 18 years old).

Pharmacological effect

Pharmacotherapeutic group
Glucocorticosteroid for local use

ATX code
R01AD09

Pharmacodynamics:
Mometasone is a synthetic glucocorticosteroid (GCS) for topical use. It has anti-inflammatory and antiallergic effects when used in doses at which systemic effects do not occur. Inhibits the release of inflammatory mediators. Increases the production of lipomodulin, which is an inhibitor of phospholipase A, which causes a decrease in the release of arachidonic acid and. accordingly, inhibition of the synthesis of arachidonic acid metabolic products – cyclic endoperoxides of prostaglandins. Prevents the marginal accumulation of neutrophils, which reduces inflammatory exudate and the production of lymphokines, inhibits the migration of macrophages, leading to a decrease in the processes of infiltration and granulation. Reduces inflammation by reducing the formation of a chemotaxis substance (impact on “late” allergy reactions) and inhibits the development of an immediate 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 with the application of antigens to the nasal mucosa, the 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:
When administered intranasally, the systemic bioavailability of mometasone furoate is <1% (with a sensitivity of the detection method of 025 pg/ml). The mometasone suspension is very poorly absorbed from the gastrointestinal tract and the small amount of mometasone suspension that can enter the gastrointestinal tract after injection into the nasal passage even before excretion in the urine or bile undergoes active primary metabolism.

Special instructions

As with any long-term treatment, patients using Nasonex® nasal spray for several months or longer should be periodically examined by a doctor for possible changes in the nasal mucosa. It is necessary to monitor patients receiving intranasal corticosteroids for a long time. Possible development of growth retardation in children. If growth retardation is detected in children, it is necessary to reduce the dose of intranasal corticosteroids to the lowest that allows for effective control of symptoms. In addition, the patient should be referred to a pediatrician for consultation.
If a local fungal infection of the nose or throat develops, it may be necessary to discontinue treatment with Nasonex® nasal spray and undergo special treatment. Irritation of the nasal and pharyngeal mucosa that persists over a long period of time may also serve as a reason to discontinue treatment with Nasonex® nasal spray.

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

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

When using intranasal corticosteroids, systemic side effects may develop, especially with long-term use in high doses. The likelihood of developing these effects is much less than with the use of oral corticosteroids. Systemic side effects may vary in individual patients and depending on the glucocorticosteroid drug used. Potential systemic effects include Cushing’s syndrome, characteristic features of Cushingoid, adrenal suppression, growth retardation in children and adolescents, cataracts, glaucoma, and, less commonly, a range of psychological or behavioral effects including psychomotor hyperactivity, sleep disturbance, anxiety, depression, or aggression (especially in children).

During the transition from treatment with systemic glucocorticosteroids to treatment with Nasonex® nasal spray, some patients may experience initial symptoms of systemic glucocorticosteroid withdrawal (for example, joint and/or muscle pain, fatigue and depression) despite a decrease in the severity of symptoms associated with damage to the nasal mucosa. Such patients must be specifically convinced of the advisability of continuing treatment with Nasonex® nasal spray. The transition from systemic to local glucocorticosteroids may also reveal pre-existing allergic diseases such as allergic conjunctivitis and eczema that were masked by systemic glucocorticosteroid therapy.

Patients undergoing treatment with glucocorticosteroids have a 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), as well as the need for medical advice if such contact occurs.

If signs of a severe bacterial infection appear (for example, fever, persistent and sharp pain on one side of the face or toothache, swelling in the orbital or periorbital area), immediate medical consultation is required.

When using Nasonex® nasal spray for 12 months, there were no signs of atrophy of the nasal mucosa. In addition, mometasone furoate tended to contribute to the normalization of the histological picture when examining biopsy samples of the nasal mucosa.

With systemic and local (including intranasal inhalation and intraocular) use of GCS, visual impairment may occur. If the 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 cataracts, glaucoma or rare diseases such as central serous chorioretinopathy (CSC), which have been observed in a number of cases with systemic and local use of GCS.

The effectiveness and safety of mometasone have 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 an unusual or irregular shape, especially ulcerated or bleeding, are identified, additional medical examination should be performed.

Impact on the ability to drive vehicles. Wed and fur.:
There is no data on the effect of the drug Nasonex® on the ability to drive vehicles or moving machinery.

Active ingredient

Mometasone

Composition

1 g of spray contains:

Active ingredient: mometasone furoate (micronized, in the form of monohydrate) equivalent to mometasone furoate anhydrous – 0.5 mg.
Excipients: dispersed cellulose (microcrystalline cellulose treated with sodium carmellose) 20.0 mg, glycerol 21.0 mg, citric acid monohydrate 2.0 mg, sodium citrate dihydrate 2.8 mg, polysorbate-80 0.1 mg, benzalkonium chloride (as a 50% solution) 0.2 mg, purified water 0.95 g

Pregnancy

There have been no properly designed and well-controlled studies of the drug in pregnant women.

As with the use of other intranasal corticosteroids, Nasonex® should be prescribed to pregnant or breastfeeding women only if the expected benefit from the drug justifies the potential risk to the fetus or infant. Infants whose mothers received corticosteroids during pregnancy should be carefully monitored for the possibility of developing adrenal hypofunction.

Contraindications

Hypersensitivity to any of the substances included in the drug.

Recent surgery or trauma to the nose with damage to the mucous membrane of the nasal cavity – before the wound heals (due to the inhibitory effect of GCS on the healing processes).

Children’s age (for seasonal and year-round allergic rhinitis – up to 2 years; for acute sinusitis or exacerbation of chronic sinusitis – up to 12 years; for polyposis – up to 18 years) – due to the lack of relevant data.

With caution:
Nasonex® should be used with caution in case of tuberculosis infection (active or latent) of the respiratory tract, untreated fungal bacterial systemic viral infection or infection caused by Herpessimplex with eye damage (as an exception, the drug can be prescribed for the listed infections as directed by a doctor), the presence of an untreated local infection involving the mucous membrane of the nasal cavity.

Side Effects

Use of the drug in clinical trials

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

Nosebleeds were usually moderate and stopped on their own, the frequency of their occurrence was slightly higher than when using placebo (5%) but equal or less than when prescribing other intranasal corticosteroids that were used as an active control (in some of them the incidence of nosebleeds was up to 15%). The incidence of all other adverse events was comparable to that observed with placebo.

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 placebo.

When using intranasal corticosteroids, the development of systemic side effects is possible, especially with long-term use of intranasal corticosteroids in high doses (see section “Special instructions”).

The frequency of adverse reactions is established as follows: very often (≥1/10); (often (≥1/100<1/10); rarely (≥1/1000<1/100).

For adverse reactions during post-registration surveillance, the frequency has not been established (cannot be determined based on available data).

Infectious and parasitic diseases: Often – Pharyngitis, upper respiratory tract infection*

Immune system disorders: Frequency not established – Hypersensitivity reactions including anaphylactic reactions, angioedema, bronchospasm, shortness of breath.

Nervous system disorders: Often – Headache.

Visual disorders: Frequency not established – Increased intraocular pressure, glaucoma, cataracts.

Disorders of the respiratory system of the chest and mediastinum: Very often – Nosebleeds**, Often – Nosebleeds (i.e. obvious bleeding and the release of blood-stained mucus or blood clots) burning sensation in the nose irritation of the nasal mucosa ulceration of the nasal mucosa, Frequency not established – Perforation of the nasal septum.

* detected with a frequency of “rarely” when using the drug twice a day for nasal polyposis

** detected when using the drug twice a day for nasal polyposis

Children

Disorders of the respiratory system of the chest and mediastinum: nosebleeds (6%) irritation of the nasal mucosa (2%) sneezing (2%).

Nervous system disorders: headache (3%).

The incidence of these adverse events in children was comparable to the incidence when using placebo.

Post-registration use of the drug

During post-registration use of the drug Nasonex®, additional adverse reactions were identified: blurred vision.

Interaction

Combination therapy with loratadine was well tolerated by patients. However, no effect of the drug on the concentration of loratadine or its main metabolite in the blood plasma was noted. In these studies, mometasone furoate was not detected in blood plasma (with a sensitivity of the detection method of 50 pg/ml). Mometasone furoate is metabolized by CYP3A4.

Concomitant use with strong inhibitors of CYP3A4 (for example, ketoconazole, itraconazole, clarithromycin, ritonavir, and drugs containing cobicistat) may lead to an increase in the concentration of glucocorticosteroids in the blood plasma and possibly an increased risk of systemic side effects of glucocorticosteroid therapy. The benefits of co-administration of mometasone furoate with strong CYP3A4 inhibitors and the potential risk of systemic side effects of glucocorticosteroids should be assessed. In the case of combined use of drugs, monitoring of patients’ condition for the development of systemic side effects of glucocorticosteroid therapy is required.

Overdose

With long-term use of GCS in high doses, as well as with the simultaneous use of several GCS, inhibition of the function of the hypothalamic-pituitary-adrenal system is possible. Due to the low systemic bioavailability of the drug (< 1% with a sensitivity of the detection method of 025 pg/ml), it is unlikely that in case of an accidental or intentional overdose, any measures other than observation will be required with the possible subsequent resumption of the drug at the recommended dose.

Storage conditions

At temperatures from 2 to 25 °C. Do not freeze.
Keep out of the reach of children.

Shelf life

2 years. Do not use after expiration date.

Manufacturer

Organon Heist bv, Belgium